COMBINATION OF A CHOLINESTERASE INHIBITOR AND A COMPOUND WITH 5-HT6 RECEPTOR AFFINITY

• US 20100120747A1
• Filed: 06/22/2007
• Published: 05/13/2010
• Est. Priority Date: 06/23/2006
• Status: Abandoned Application

• Current Assignee: Laboratories Del Dr Esteve SA (Corporation Quimico Farmaceutica Esteve SA)
• Original Assignee: Laboratories Del Dr Esteve SA (Corporation Quimico Farmaceutica Esteve SA)
• Inventors: Buschmann, Helmut Heinrich, Codony-Soler, Xavier
• Application Number:
  US12/305,516
• Publication Number:
  US 20100120747A1
• Time in Patent Office: Days
• US Class Current: 514/217.10
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 1/14 Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
• CPC Class Codes: A61P 1/16 for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 19/06 Antigout agents, e.g. antihyperuricemic or uricosuric agents
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/22 : Anxiolytics
• CPC Class Codes: A61P 25/24 : Antidepressants
• CPC Class Codes: A61P 25/28 : for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 29/00 : Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/00 : Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 : Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 : Antihyperlipidemics
• CPC Class Codes: A61P 3/10 : for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 35/00 : Antineoplastic agents
• CPC Class Codes: A61P 37/02 : Immunomodulators
• CPC Class Codes: A61P 9/00 : Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/04 : Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• CPC Class Codes: A61P 9/06 : Antiarrhythmics
• CPC Class Codes: A61P 9/10 : for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 : Antihypertensives

Abstract

The present invention relates to an active substance combination comprising at least one compound with 5-HT6 receptor affinity, and at least one cholinesterase inhibitor, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament.

Claims

1. An active substance combination that comprises:

as component (A) at least one compound with 5-HT₆ receptor affinity, and

as component (B) at least one cholinesterase inhibitor,

wherein an active substance combination comprising as component (A) the 5-HT₆ antagonist SB271046 and as component (B) the cholinesterase inhibitor donepezil hydrochloride is excluded.

2. The combination according to claim 1, wherein component (A) has a K_i value for binding to the 5-HT₆-receptor of below or equal to 1 μ

M.

3. The combination according to claim 1, wherein component (A) acts as agonist or inverse agonist of the 5-HT₆ receptor, preferably the compound with 5-HT₆ receptor affinity acts as agonist of the 5-HT₆ receptor.

4. The combination according to claims 1, wherein component (B) has an IC₅₀ for the inhibition of acetylcholinesterase in erythrocytes below or equal to 1 μ

M.

5. The combination according to claim 1, wherein the cholinesterase inhibitor is selected from the group consisting of reversible cholinesterase inhibitors and pseudo-reversible cholinesterase inhibitors.

6. The combination according to claim 1, wherein component (A) is selected from the group consisting of the benzoxazinone-derived sulfonamide compounds of general formula (Ia)

wherein

R^1a, R^2a, R^3a and R^4a, independently of one another, each represent a hydrogen atom;

halogen;

an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl- or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ringsystem;

nitro;

cyano;

—

O—

R^10a;

—

O—

(C═

O)—

R^11a;

—

(C═

O)—

OR^11a;

—

SR^12a;

—

SOR^12a;

—

SO₂R^12a;

—

NH—

SO₂R^12a;

—

SO₂NH₃ or —

NR^13aR^14a;

R^5a represents a hydrogen atom;

an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical or a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical;

R^6a, R^7a, R^8a, R^9a, independetly of one another, each represent a hydrogen atom;

an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical;

a cyano group or a —

C(═

O)—

OR^15a moiety;

W^a represents an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical, which may be bonded via an optionally mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene or alkenylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

a —

NR^16aR^17a moiety, or

a —

C(═

O)—

R^18a moiety;

R^10a represents a hydrogen atom;

an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^11a represents a hydrogen atom;

an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^12a represents an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^13a and R^14a, independently of one another, each represent a hydrogen atom;

an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or R^13a and R^14a together with the bridging nitrogen atom form a saturated, unsaturated or aromatic heterocyclic ring, which is unsubstituted or at least mono-substituted and/or which may contain at least one further heteroatom as a ring member;

R^15a represents a hydrogen atom;

an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as ring member containing cycloaliphatic radical or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^16a represents an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^17a represents an unbranched or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical, and

R^18a represents an unsubstituted or at least mono-substituted aryl radical;

optionally in form of one of its stereoisomers, preferably enantiomers or diastereomers, its racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a solvate, respectively;

indole-derived sulfonamide compounds of general formula (Ib)

wherein

R^1b represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical,

which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

a —

(CH₂)_mb—

NR^13bR^14b moiety with mb=0, 1, 2, 3, 4 or 5;

a —

C(═

O)—

R^8b moiety;

a —

S(═

O)₂—

R^9b moiety;

or a —

S(═

O)₂—

C(H)A^bB^b moiety;

R^2b represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

NH₂;

—

SH;

—

OH;

—

CN;

—

C(═

O)—

OH;

—

O—

R^10b;

—

C(═

O)—

OR^12b;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a chain member containing aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^3b represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R^10b;

—

S—

R^11b;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

a —

CH(OC₂H₅)—

CH₂—

NR^13bR^14b moiety or a —

(CH₂)_nb—

NR^13bR^14b moiety with nb=0, 1, 2, 3, 4 or 5;

a —

S(═

O)₂—

R^9b moiety;

a —

S(═

O)₂—

C(H)A^bB^b moiety;

or a —

C(═

O)—

(CH₂)_pb—

C(═

O)—

N-D^bE^b moiety with pb=0, 1, 2, 3, 4 or 5;

R^4b;

R^5b;

R^6b and R^7b, independently of one another, each represent a hydrogen atom;

—

NO₂;

—

NH₂;

—

SH;

—

OH;

—

CN;

—

C(═

O)—

OH;

—

C(═

O)—

H;

—

S(═

O)₂—

OH;

—

C(═

O)—

NH₂;

—

S(═

O)₂—

NH₂;

—

C(═

O)—

R^8b;

—

S(═

O)₂—

R^9b;

—

O—

R^10b;

—

S—

R^11b;

C(═

O)—

OR^12b;

—

N(R^15b)—

S(═

O)₂R^16b;

—

NH—

R^17b;

—

NR^18bR^19b;

—

C(═

O)—

NHR^20b, —

C(═

O)—

NR^21bR^22b;

—

S(═

O)₂—

NHR^23b;

—

S(═

O)₂—

NR^24bR^25b;

—

O—

C(═

O)—

R^26b;

—

NH—

C(═

O)—

R^27b;

—

NR^28b—

C(═

O)—

R^29b;

NH—

C(═

O)—

O—

R^30b;

NR^31b—

C(═

O)—

O—

R^32b;

—

S(═

O)₂—

O—

R^33b;

a halogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

with the proviso that at least one of the substituents R^4b, R^5b, R^6b and R^7b represents a —

N(R^15b—

S(═

O)₂—

R^16b moiety;

R^8b, R^12b, R^17b, R^18b, R^19b, R^20b, R^21b, R^22b, R^23b, R^24b, R^25b, R^26b, R^27b, R^28b, R^29b, R^30b, R^31b, R^32b and R^33b, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group;

R^9b represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^10b and R^11b, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^13b and R^14b, independently of one another, each represent a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^13b and R^14b together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^15b represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical or a —

S(═

O)₂—

R^16b moiety;

R^16b represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

A^b and B^b together with the bridging carbon form an unsubstituted or at least mono-substituted, saturated or unsaturated cycloaliphatic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

D^b and E^b together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or

D^b and E^b, independently of one another, each represent a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

indazolyl- and (2,3)-dihydro-indolyl-derived sulfonamide compounds of general formula (Ic)

wherein

X^c—

Y^c from left to right represents CR^1c═

N and Z^c is N[(CH₂)_ncR^6c] or

X^c—

Y^c from left to right represents CR^7c═

N, Z^c is NH, R^7c represents the following moiety

A^c represents CH or N and B^c represents NR^8c, O or S;

X^c—

Y^c from left to right represents C[(CH₂)_ncR^9c═

N and Z^c is NR^10c or

X^c—

Y^c represents CH₂—

CH₂ and Z^c is N[(CH₂)_ncR^11c];

nc is 0, 1, 2, 3 or 4;

R^1c represents a hydrogen atom;

NO₂;

—

NH₂;

—

SH;

—

OH;

—

CN;

—

C(═

O)—

R^12c;

—

OR^13c;

—

SR^14c;

—

F;

—

Cl, —

Br;

—

I;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^2c, R^3c, R^4c and R^5c, independently of one another, each represent a hydrogen atom;

—

NO₂;

—

NH₂;

—

SH;

—

OH;

—

CN;

—

C(═

O)—

H;

—

C(═

O)—

R^12c;

—

OR^13c;

—

SR^14c;

—

N(R^15c)—

S(═

O)₂—

R^16c;

—

NH—

R^17c;

—

NR^18cR^19c;

—

F;

—

Cl, —

Br;

—

I;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

with the proviso that at least one of the substituents R^2c, R^3c, R^4c and R^5c represents a —

N(R^15c)—

S(═

O)₂—

R^16c moiety;

R^6c, R^9c and R^11c, independently of one another, each represent a —

NR^20cR^21c radical or

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^8c represents —

C(═

O)—

R^22c;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^10c represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical-;

or a —

S(═

O)₂—

R^23c moiety;

R^12c, R^13c, R^14c, R^17c, R^18c and R^19c, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^15c represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or a —

S(═

O)₂—

R^24c moiety;

R^16c and R^24c, independently of one another, each represent an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^20c and R^21c, independently of one another, each represent a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or R^20c and R^21c together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^22c represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system; and

R^23c represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

phenyl-piperazine-derived compounds of general formula (Id)

wherein

X^d represents a —

NR^1dR^2d moiety t or a —

OR^3d moiety;

R^1d represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

an unsubstituted or at least mono-substituted radical selected from the group consisting of adamantyl, bicyclo[2.2.1]heptyl and bicyclo[3.1.1]heptyl, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group which may contain 1, 2 or 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur as chain member(s);

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group which may contain 1, 2 or 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur as chain member(s);

or a —

C(═

O)—

R^12d moiety;

R^2d represents a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or

R^1d and R^2d together with the bridging nitrogen form an optionally at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^3d represents or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group;

R^4d, R^5d and R^6d, independently of one another, each represent a hydrogen atom or a halogen atom;

or

R^4d and R^5d together with the bridging carbon atoms form an unsubstituted 5- or 6-membered heterocyclic ring which contains 1, 2 or 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur as ring member(s) and which together with the phenyl ring which it is fused with forms a 9- or 10-membered bicyclic aromatic ring system;

R^7d and R^8d, independently of one another, each represent a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^9d and R^10d, independently of one another, each represent a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^11d represents a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical, which may contain 1, 2 or 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur as chain member(s);

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group;

-a-C(═

O)—

R^13d moiety or a —

S(═

O)₂—

R^14d moiety;

R^12d represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group; and

R^13d and R^14d, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group which may contain 1, 2 or 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur as chain member(s);

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

and phenyl-piperazine-derived compounds of general formula (Ie)

wherein

X^e represents —

CN, —

C(═

O)—

OH, —

C(═

O)—

OR^4e, —

O—

R^5e, —

NH₂, —

NR^6e—

C(═

O)—

R^7e, —

NH—

S(═

O)₂—

R^8e or —

NH—

R^9e;

R¹ represents a hydrogen atom;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group which may contain 1, 2 or 3 heteroatom(s) independently selected from the group consisting of nitrogen, oxygen and sulfur as chain member(s);

R^2e represents a hydrogen atom or a —

C(═

O)—

R^10e moiety;

or

R^1e and R^2e together with the bridging nitrogen form a nitro (NO₂)-group or

an unsubstituted or at least mono-substituted 5- or 6-membered heteroaryl radical which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^3e represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^4e represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^5e represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group;

R^6e represents a hydrogen atom or

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group;

R^7e represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^8e represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group;

R^9e represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group; and

R^10e represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

and tetrahydroisoquinoline-derived sulfonamide compounds of general formula (If)

wherein

R^1f represents a hydrogen atom;

a —

C(═

O)—

OR^37f moiety;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^2f, R^3f, R^4f and R^5f, independently of one another, each represent a hydrogen atom;

F, Cl, Br, I, —

NO₂;

—

NH₂;

—

SH;

—

OH;

—

CN;

—

C(═

O)—

OH;

—

C(═

O)—

H;

—

S(═

O)₂—

OH;

—

C(═

O)—

NH₂;

—

S(═

O)₂—

NH₂;

—

C(═

O)—

R^6f;

—

S(═

O)—

R^7f;

—

S(═

O)₂—

R^7f;

—

OR^8f;

—

SR^9f;

—

C(═

O)—

OR^10f;

—

N(R^11f)—

S(═

O)₂—

R^12f;

—

NR^13fR^14f;

—

NH—

R^15f;

—

C(═

O)—

NR^16fR^17f;

C(═

O)—

NHR^18f;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

with the proviso that at least one of the substituents R^2f, R^3f, R^4f and R^5f represents a —

N(R^11f)—

S(═

O)₂—

R^12f moiety;

R^6f, R^7f, R^8f, R^9f, R^10f, R^13f, R^14f, R^15f, R^16f, R^17f and R^18f,

independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

R^11f represents a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^12frepresents a phenyl radical of general formula (Af),

wherein

R^19f, R^20f, R^21f, R^22f and R^38f, independently of one another, each represent a hydrogen atom;

F, Cl, Br, I, —

NO₂;

—

NH₂;

—

SH;

—

OH;

—

CN;

—

C(═

O)—

OH;

—

C(═

O)—

H;

—

S(═

O)₂—

OH;

—

C(═

O)—

NH₂;

—

S(═

O)₂—

NH₂;

—

C(═

O)—

R^23f;

—

S(═

O)—

R^24f;

—

S(═

O)₂—

R^24f;

—

OR^25f;

—

SR^26f;

—

C(═

O)—

OR^27f;

—

N(R^28f)—

S(═

O)₂—

R^29f;

—

NH—

S(═

O)₂—

R^30f;

—

NR^31fR^32f;

—

NH—

R^33f;

—

C(═

O)—

NHR^34f;

—

C(═

O)—

NR^35fR^36f;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system and/or which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group;

or a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

R^23f, R^27f, R^28f, R^29f and R^30f, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

R^24f, R^26f, R^31f, R^32f and R^33f, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

R^25f, R^34f, R^35f and R^36f, represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

and R^37f represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

7. The combination according to claim 6, wherein the indole-derived sulfonamide is selected from the group consisting of compounds of general formula (Ih)

wherein

R^1h represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_mh—

NR^13hR^14h moiety with mh=0, 1, 2, 3, 4 or 5;

R^2h represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R^10h;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^3h represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R^10h;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_nh—

NR^13hR^14h moiety with nh=0, 1, 2, 3, 4 or 5;

R^4h, R^5h and R^7h, independently of one another, each represent a hydrogen atom;

—

NO₂;

—

CN;

—

O—

R^10h;

—

C(═

O)—

OR^12h;

a halogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^10h represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^13h and R^14h, independently of one another, each represent a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or

R^13h and R^14h together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^15h represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical or a —

S(═

O)₂—

R^16h moiety;

and R^16h represents an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

and compounds of general formula (Ik)

wherein

R^1k represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

an unsubstituted or at least mono-substituted phenyl radical or an unsubstituted or at least mono-substituted benzyl radical;

R^3k represents a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_nk—

NR^13kR^14k moiety with nk=0, 1, 2, 3, 4 or 5;

R^13k and R^14k, independently of one another, each represent a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or

R^13k and R^14k together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^15k represents a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

and R^16k represents an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

compounds of general formula (Im)

wherein

R^1m represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_mm—

NR^13mR^14m moiety with mm=0, 1, 2, 3, 4 or 5;

R^2m represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R^10m;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^3m represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R^10m;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_nm—

NR^13mR^14m moiety with nm=0, 1, 2, 3, 4 or 5;

R^4m, R^6m and R^7m, independently of one another, each represent a hydrogen atom;

—

NO₂;

—

CN;

—

O—

R^10m;

a halogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^10m represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^13m and R^14m, independently of one another, each represent a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or

R^13m and R^14m together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^15m represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical or a —

S(═

O)₂—

R^16m moiety;

and R^16m represents an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

and compounds of general formula (In)

wherein

R¹ⁿ represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_mn—

NR¹³ⁿR¹⁴ⁿ moiety with mn=0, 1, 2, 3, 4 or 5;

R²ⁿ represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R¹⁰ⁿ;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R³ⁿ represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R¹⁰ⁿ;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_nn—

NR¹³ⁿR¹⁴ⁿ moiety with nn=0, 1, 2, 3, 4 or 5;

R⁵ⁿ, R⁶ⁿ and R⁷ⁿ, independently of one another, each represent a hydrogen atom;

—

NO₂;

—

CN;

—

O—

R¹⁰ⁿ;

a halogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R¹⁰ⁿ represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R¹³ⁿ and R¹⁴ⁿ, independently of one another, each represent a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or

R¹³ⁿ and R¹⁴ⁿ together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R¹⁵ⁿ represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical or a —

S(═

O)₂—

R¹⁶ⁿ moiety;

R¹⁶ⁿ represents an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

and compounds of general formula (Io)

wherein

R^1o represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_mo—

NR^13oR^14o moiety with mo=0, 1, 2, 3, 4 or 5;

R^2o represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R^10o;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^3o represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

CN;

—

O—

R^10o;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

a —

CH(OC₂H₅)—

CH₂—

NR^13oR^14o moiety or a —

(CH₂)_no—

NR^13oR^14o moiety with no=0, 1, 2, 3, 4 or 5;

R^4o, R^{5o and R6o}, independently of one another, each represent a hydrogen atom;

—

NO₂;

—

CN;

—

O—

R^10o;

a halogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^10o represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^13o and R^14o, independently of one another, each represent a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or

R^13o and R^14o together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^15o represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical or a —

S(═

O)₂—

R^16o moiety;

and R^16o represents an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

compounds of general formula (Ip)

wherein

R^1p represents a —

S(═

O)₂—

R^9p moiety or a —

S(═

O)₂—

C(H)A^pB^p moiety;

R^2p represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

OH;

—

CN;

—

O—

R^10p;

—

S—

R^11p;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^3p represents a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via an unsubstituted or at least mono-substituted alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or a —

(CH₂)_np—

NR^13pR^14p moiety with np=0, 1, 2, 3, 4 or 5;

R^4p, R^5p, R^6pand R^7p, independently of one another, each represent a hydrogen atom;

—

NO₂;

—

NH₂;

—

OH;

—

CN;

—

C(═

O)—

R^8p;

—

O—

R^10p;

—

S—

R^11p;

—

NH—

R^17p;

—

NR^18pR^19p;

a halogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group;

R^8p represents a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^8p, R^17p, R^18pand R^19p, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group;

R^9p represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R^10p and R^11p, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^13p and R^14p, independently of one another, each represent a hydrogen atom;

or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or

R^13p and R^14p together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

A^p and B^p together with the bridging carbon form an unsubstituted or at least mono-substituted, saturated or unsaturated cycloaliphatic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively;

and compounds of general formula (Iq)

wherein

R^1q represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical,

which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

a —

C(═

O)—

R^8q moiety;

a —

S(═

O)₂—

R^9q moiety;

R^2q represents a hydrogen atom;

—

F;

—

Cl;

—

Br;

—

I;

—

NO₂;

—

NH₂;

—

SH;

—

OH;

—

CN;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a chain member containing aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^4q, R^5q, R^6q and R^7q, independently of one another, each represent a hydrogen atom;

—

NO₂;

—

NH₂;

—

SH;

—

OH;

—

CN;

—

C(═

O)—

OH;

—

C(═

O)—

H;

—

S(═

O)₂—

OH;

—

C(═

O)—

NH₂;

—

S(═

O)₂—

NH₂;

—

C(═

O)—

R^8q;

—

S(═

O)₂—

R^9q;

—

O—

R^10q;

—

S—

R¹¹q;

—

C(═

O)—

OR^12q;

—

N(R^15q)—

S(═

O)₂—

R^16q;

—

NH—

R^17q;

—

NR^18qR^19q;

—

C(═

O)—

NHR^20g, —

C(═

O)—

NR^21qR^22q;

—

S(═

O)₂—

NHR^23q;

—

S(═

O)₂—

NR^24qR^25q;

—

O—

C(═

O)—

R^26q;

—

NH—

C(═

O)—

R^27q;

—

NR^28q—

C(═

O)—

R^29q;

NH—

C(═

O)—

O—

R^30q;

NR^31q—

C(═

O)—

O—

R^32q;

—

S(═

O)₂—

O—

R^33q;

a halogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

with the proviso that at least one of the substituents R^4q, R^5q, R^6q and R^7q represents a —

N(R^15q)—

S(═

O)₂—

R^16q moiety;

R^8q, R^12q, R^17q, R^18q, R^19q, R^20q, R^21q, R^22q, R^23q, R^24q, R^25q, R^26q, R^27q, R^28q, R^29q, R^30q, R^31q, R^32q and R^33q, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene, alkenylene or alkinylene group;

R^9q represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

R^10q and R^11q, independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched alkylene group;

R^15q represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical or a —

S(═

O)₂—

R^16q moiety;

R^16q represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

D^q and E^q together with the bridging nitrogen form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain at least one further heteroatom as a ring member and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or

D^q and E^q, independently of one another, each represent a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched alkylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least mono-substituted alkylene, alkenylene or alkinylene group and/or which may be condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, respectively.

8. The combination according to claim 1, wherein component (A) is at least one compound selected from the group consisting of BVT-5182, EMDT, Ro 65-7199, Ro 04-6790, Ro 63-0563, MS-245, SB-271046, LY-483518, ALX-0440, WAY-181189, WAY-466, ALX-1175, ALX-1161, SB-271046, SB-258510, SB-357134, SB-214111, SB-399885, Ro 65-7674, SB-699929, Ro 43-68554, SB-742457, Ro 66-0074, [¹¹C]GSK-215083,

[HT1] N,N-dimethyl-2-(1-(phenylsulfonyl)-1H-indol-3-yl)ethanamine,

[HT2] 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole,

[HT3] 2-(1-(5-(phenylsulfonamido)-1H-indol-3-yl)ethylidene)hydrazinecarboximidamide,

[HT4] 5-fluoro-3-(3-fluorophenylsulfonyl)-1-(piperidin-3-yl)-1H-indole,

[HT5] 2-((1-(4-aminophenylsulfonyl)-1H-indol-3-yl)methylene)hydrazinecarboximidamide,

[HT6] 3-(phenylsulfonyl)-7-(2-(pyrrolidin-1-yl)ethoxy)-1H-indole,

[HT7] N,N-dimethyl-2-(1-(phenylsulfonyl)-1H-indol-4-yloxy)ethanamin,

[HT8] 1-(phenylsulfonyl)-3-(pyrrolidin-2-ylmethyl)-1H-indole,

[HT9] 2-(3-benzyl-1H-indol-1-yl)-N,N-dimethylethanamine,

[HT10] 4-(3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-1-ylsulfonyl)benzenamine,

[HT12] (6S,7S)-7-(dimethylamino)-2-tosyl-2,6,7,8-tetrahydrobenzo[cd]indol-6-ol,

[HT13] 2-(1-(phenylsulfonyl)-6,7-dihydro-1H-indol-4(5H)-ylidene)hydrazinecarboximidamide,

[HT14] 6-(phenylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine,

[HT15] 3-(3-chlorophenylsulfonyl)-1-(pyrrolidin-2-ylmethyl)-1H-pyrrolo[2,3-b]pyridine,

[HT16] 4-(5,6,7,8-tetrahydrocarbazol-9-ylsulfonyl)benzenamine,

[HT17] 3-(2-aminoethyl)-1-(naphthalen-2-ylsulfonyl)-1H-imidazo[4,5-b]pyridin-2(3H)-one,

[HT18] 2-(4-(6-chloroimidazo[2,1-b]thiazol-5-ylsulfonyl)-4H-thieno[3,2-b]pyrrol-6-yl)-N,N-dimethylethanamine,

[HT19] N,N-dimethyl-3-(phenylsulfonyl)-6,7,8,9-tetrahydro-3H-benzo[e]indol-8-amine,

[HT20] N-(4-(piperidin-4-yl)-2H-chromen-6-yl)naphthalene-1-sulfonamide,

[HT21] 2-(3-benzyl-3H-inden-1-yl)-N,N-dimethylethanamine,

[HT22] N-(7-((3S,4S)-3-fluoropiperidin-4-yloxy)benzofuran-5-yl)-2-methoxy-5-methylbenzenesulfonamide,

[HT23] 2-Methoxy-10-(1-methylpyrrolidin-3-yl)-5-thia-4b-aza-indeno[2,1-a]indene 5,5-dioxide,

[HT24] 1-(6-(phenylsulfonyl)pyridin-3-yl)piperazine,

[HT25] 1-(2-methoxy-5-(naphthalen-1-ylsulfonyl)phenyl)piperazine,

[HT26] 1-(2-chloro-5-(phenylsulfonyl)phenyl)piperazine,

[HT27] 8-methoxy-1-(3-methoxy-5-(piperazin-1-yl)benzyl)-3,4-dihydroquinolin-2(1H)-one,

[HT28] 5-chloro-3-(3-chlorophenylsulfonyl)-7-(4-methylpiperazin-1-yl)-1H-indole,

[HT29] 1-(4-(phenylsulfonypnaphthalen-1-yl)piperazine,

[HT30] 3-(phenylsulfonyl)-7-(piperazin-1-yl)-1H-pyrrolo[3,2-b]pyridine,

[HT31] 4-(2-chlorophenylsulfonyl)-6-methyl-8-(piperazin-1-yl)-3,4-dihydro-2H-benzo[b][1,4]oxazine,

[HT32] 5-(4-methylpiperazin-1-yl)-3-(naphthalen-1-ylsulfonyl)-1H-indazole,

[HT33] 4-(4-(4-(4,5-dihydro-1H-imidazol-2-yl)piperazin-1-yl)-1H-indol-1-ylsulfonyl)benzenamine,

[HT34] 5-(4-benzylpiperazin-1-yl)-3-(phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine,

[HT35] 2-(2,3-dichlorophenylsulfonyl)-5-(piperazin-1-yl)-1,2,3,4-tetrahydroisoquinoline,

[HT36] 6-fluoro-4-(2-fluorobenzyl)-8-(piperazin-1-yl)-2H-benzo[b][1,4]oxazin-3(4H)-one,

[HT37] 2-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole,

[HT38] 4-(4-(piperazin-1-yl)naphthalen-1-ylsulfonyl)benzenamine,

[HT39] 8-(4-(4-fluorobenzyl)piperazin-1-yl)-3-(phenylsulfonyl)quinoline,

[HT40] 2,3-dichloro-N-(2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)benzenesulfonamide,

[HT41] 2-(methylthio)-3-(phenylsulfonyl)-4H-pyrido[1,2-a]pyrimidin-4-imine and

[HT42] 8-(4-(3-fluoro-5-(trifluoromethypbenzyl)phenylsulfonyl)-N,N,3-trimethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-amine;

salts thereof, free bases thereof, racemates thereof, enantiomers thereof, and combinations thereof.

9. The combination according to claim 1, wherein component (B) is at least one compound selected from the group consisting of

edrophonium, ganstigmine, demecarium, ambenonium, neostigmine bromide, dehydroevodiamine chloride, eseroline, imperatorin, scopoletin (SCT), huperizine A (Hup A), huperzine A, tacrine hydrochloride (CI-970, THA.HCl), 7-methoxytacrine (7-MEOTA), velnacrine maleate (HP-029, P83-6029A), rivastigmine tartrate (ENA-713, ENA-713D, ONO-2540, SDZ-212-713, SDZ-ENA-713), eptastigmine tartrate (L-693487), heptylstigmine tartrate (MF-201), donepezil hydrochloride (BNAG, E-2020), suronacrine maleate (HP-128), UCB-11056, SM-10888, stacofylline hydrochloride (S-9977, S-9977-2), berberine iodide, zifrosilone (MDL-73745), norpyridostigmine, quilostigmine (HP-290, NXX-066), E-2030, THB-013, F-3796, PD-142012, CI-1002, PD-142676, terestigmine tartrate (CHF-2060), thiacymserine, phenserine tartrate, galantamine hydrobromide (GP-37267), galantamine hydrobromide (R-113675), Ro-46-5934, P11012, MF-8615, MF-268 bitartrate, anseculin hydrochloride (KA-672.HCl), ensaculin hydrochloride, icopezil maleate (CP-118954, CP-118954-11), eserine salicylate, physostigmine salicylate, isovanihuperzine A (IVHA), JWS-USC-751X, FR-152558, UR-1827, P11467, P-10358, bis(7)-tacrine, HMR-2420, T-82, CP-126998, TV-3279, MSF, THA-C8, subergorgic acid, suberogorgin, SPH-1286, huperzine B (Hup B), pyridostigmine bromide (Ro-1-5130), huprine X, ER-127528, tolserine tartrate, huprine Y, coronaridine, RS-1233, kobophenol A, bis(12)-huperine, BGC-20-1259, RS-1259, NP-7557, ZT-1, ITH-4012, TK-19, T-81, TH-171, TH-185, distigmine bromide (BC-51), (−

)-9-dehydrogalanthaminium bromide, memoquin, NP-0361, scopoletin 7-O-beta-D-glucopyranoside (NSC-404560), scopolin (SCN), scopoloside, BW-284c51, SP-004, SP-04, withaferin A (NSC-101088), withaferine (NSC-273757), (+)-corynoline, corynoline, (S)-(−

)-oxypeucedanin, oxypeucedanin, (−

)-voacangine, carbomethoxyibogaine, voacangine, dieckol, phlorofucofuroeckol (PFF), phlorofucofuroeckol A, (−

)-3-O-acetylspectaline hydrochloride and rhaphiasaponin 1, salts thereof, free bases thereof, racemates thereof, enantiomers thereof, and combinations thereof.

10. The combination according to claim 1, which comprises 1-99% by weight of component (A) and 99-1% by weight of component (B), preferably 70 to 95% by weight of component (A) and 30 to 5% by weight of component (B), more preferably 85 to 95% by weight of component (A) and 15 to 5% by weight of component (B), in each case referring to the total weight of both components (A) and (B).

11. An active substance combination as defined in claim 1 which is a pharmaceutical composition.

12. A method of administration of the combination of claim 1 for simultaneous acetylcholinesterase inhibition and 5-HT₆-receptor regulation.

13. A method of administration of the active substance combination of claim 1 for regulation of appetite, for maintenance, increase or reduction of body weight, for prophylaxis and/or treatment of disorders related to food ingestion, preferably for prophylaxis and/or treatment of obesity, anorexia, cachexia, bulimia, diabetes, preferably type II diabetes (non-insulin-dependent diabetes mellitus), or for prophylaxis and/or treatment of gastrointestinal tract disorders, preferably of the irritable bowel syndrome, for prophylaxis and/or treatment of Metabolic Syndrome, Peripheral Nervous System Disorders, Central Nervous System Disorders, arthritis, epilepsy, anxiety, panic, depression, cognitive disorders, memory disorders, cardiovascular diseases, senile dementia processes, such as Alzheimer'"'"'s, Parkinson'"'"'s and/or Huntington'"'"'s Disease, schizophrenia, psychosis, infantile hyperkinesia (ADHD, attention deficit / hyperactivity disorder), pain, hypertensive syndrome, inflammatory diseases, immunologic diseases or for improvement of cognition.

14. A pharmaceutical formulation, characterized in that it comprises an active substance combination according to claim 1 and optionally one or more pharmacologically acceptable adjuvants.

15. The pharmaceutical formulation according to claim 14, which is in solid pharmaceutical forms selected from the group consisting of tablets, tablets, chewing tablets, chewing gums, dragé

es, capsules, suppositories, powder preparations, transdermal therapeutic systems, and transmucosal therapeutic systems.

16. The pharmaceutical formulation according to claim 14, which is in the form of multiple particles, microtablets, microcapsules, microspheroids, granules, crystals or pellets, and is optionally compacted in a tablet, filled in a capsule or suspended in a suitable liquid.

17. The pharmaceutical formulation according to claim 14, which is for oral, intravenous, intramuscular, subcutaneous, intrathecal, epidural, buccal, sublingual, pulmonal, rectal, transdeitual, nasal or intracerebroventricular application.

18. The pharmaceutical formulation according to claim 14, wherein at least one of the components of the active substance combination (A) or (B) is present at least partially in sustained-release form.

19. The pharmaceutical formulation according to claim 18, wherein the medicament has at least one coating or at least one matrix comprising at least one material, which sustains active substance release.

20. The pharmaceutical formulation according to claim 19, wherein the sustained-release material is based on optionally modified, water-insoluble, natural, semisynthetic or synthetic polymer, or a natural wax or fat or fatty alcohol or semisynthetic or synthetic fatty acid, or on a mixture of at least two of these afore mentioned components.

21. The pharmaceutical formulation according to claim 20, wherein the water-insoluble polymer is based on an acrylic resin, which is selected from the group consisting of poly(meth)acrylates, poly(C_1-4)dialkylamino(C_1-4)alkyl(meth)acrylates and/or copolymers thereof, mixtures thereof, and combinations thereof.

22. The pharmaceutical formulation according to claim 20, wherein the water-insoluble polymers are selected from the group consisting of cellulose derivatives, alkyl cellulose ethyl cellulose, and cellulose esters.

23. The pharmaceutical formulation according to claim 20, wherein the wax is selected from the group consiting of carnauba wax, beeswax, glycerol monostearate, glycerol monobehenate, glycerol ditripalmitostearate, microcrystalline wax a, mixtures thereof, and combinations thereof.

24. The pharmaceutical formulation according to claim 20, wherein the polymers are in combination with one or more plasticizers.

25. The pharmaceutical formulation according to claim 24, wherein that besides the sustained-release form, at least one of the active substance components (A) or (B) is present in a non-sustained-release form.

26. The combination according to claim 1, wherein component (A) has a K_i value for binding to the 5-HT₆-receptor below or equal to 500 nM.

27. The combination according to claim 1, wherein component (A) has a K_i value for binding to the 5-HT₆-receptor below or equal to 100 nM.

28. The combination according to claim 1, wherein component (A) has a K_i value for binding to the 5-HT₆-receptor below or equal to 50 nM.

29. The combination according to claim 1, wherein component (A) has a K_i value for binding to the 5-HT₆-receptor below or equal to 25 nM.

30. The combination according to claim 1 wherein component (B) has an IC₅₀ for the inhibition of acetylcholinesterase in erythrocytes below or equal to 500 nM.

31. The combination according to claim 1 wherein component (B) has an IC₅₀ for the inhibition of acetylcholinesterase in erythrocytes below or equal to 300 nM.

32. The combination according to claim 1 wherein component (B) has an IC₅₀ for the inhibition of acetylcholinesterase in erythrocytes below or equal to 200 nM.

33. The combination according to claim 1 wherein component (B) has an IC₅₀ for the inhibition of acetylcholinesterase in erythrocytes below or equal to 100 nM.

34. The pharmaceutical formulation according to claim 14, which is in liquid and semi-liquid pharmaceutical forms selected from the group consisting of drops, juice, sirup, solutions, emulsions, and suspensions.

35. The pharmaceutical formulation according to claim 34, which is in a form selected from the group consisting of tablets, capsules, drops or solution.