SUBSTITUTED 3-AMINO-4 -HYDROXY PYRROLIDINES COMPOUNDS, THEIR PREPARATION AND USE AS MEDICAMENTS
First Claim
Patent Images
1. Substituted pyrrolidine compounds of general formula (I), wherein R1 represents a hydrogen atom, an unbranched or branched, saturated, optionally at least mono-substituted C1-6-aliphatic radical;
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted;
an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system;
a branched or unbranched, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system;
an optionally at least mono-substituted benzhydryl group;
a (C═
O)—
R5 group;
a group;
a (SO2)—
R6 group;
or a (C═
O)—
NR7R7a group;
R2 represents a hydrogen atom;
a substituted or unsubstituted aliphatic group;
a (C═
O)—
R8 group;
a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;
R3 and R4, equal or different, represent a hydrogen atom;
an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted;
an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system;
with the condition (proviso) that R3 and R4 may not at the same time represent a hydrogen atom;
or R3 and R4 together with their bridging nitrogen atom form1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;
2) an A-X—
B group,whereinA represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;
X represents a bond, a —
NH—
group, a —
(C═
O)—
group, a branched or linear, optionally substituted C1-6-aliphatic chain, —
O—
, or a —
SO2—
group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;
3) an A-X—
B—
Y—
C group,whereinA represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;
X represents a bond, a —
NH—
group, a —
(C═
O)—
group, a branched or linear, optionally substituted C1-6-aliphatic chain, —
O—
, or a —
SO2—
group;
B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;
Y represents a bond, a —
NH—
group, a —
(C═
O)—
group, a branched or linear, optionally substituted C1-6-aliphatic chain, —
O—
, or a —
SO2—
group;
C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N1 S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;
R5 and R6 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group;
an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R7 and R7a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group;
an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R8 represents a hydrogen atom;
a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;
R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;
with the provisos that if R2 represents a hydrogen atom;
and R1 represents a hydrogen atom or a condensed aryl group;
R3 and R4 may not form together with their bridging nitrogen atom a triazole group;
if R2 represents a hydrogen atom;
and R1 represents a hydrogen atom;
a substituted C1-2 alkyl group;
a condensed aryl group;
a benzyl group;
R3 and R4 may not form together with their bridging nitrogen atom a substituted, unsaturated, condensed ring system containing at least 4 nitrogen atoms as ring members;
an unsaturated, (C═
O)-substituted, uncondensed, 6-membered ring system in which one additional carbon atom is replaced by nitrogen. if R2 represents a hydrogen atom;
and R3 and R4 form together with their bridging nitrogen atom a pyrrolidine ring, a piperidine ring, a piperazine ring or a morpholine ring;
R1 may not represent a hydrogen atom;
a methyl group;
an unsaturated tert-butyl group;
a (C═
O)-substituted alkyl-heteroaryl group;
if R2 represents a hydrogen atom;
and R1 does not represent a benzyl group;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a substituted alkyl-heteroaryl group;
an alkyl-aryl group;
a substituted heteroaryl group;
an unsubstituted methyl group;
a substituted alkyl group;
an aryl group;
a cyclohexyl group;
an alkyl-cycloalkyl group wherein the cycloalkyl group contains at least one heteroatom;
if R2 represents a hydrogen atom;
and R1 represents an alkyl group;
and either R3 or R4 represents a hydrogen atom;
the other of R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group;
a branched C1-4 alkyl group;
a substituted or unsubstituted C3-6 cycloalkyl group in which optionally at least one carbon atom is optionally replaced by N, S or O;
a cycloheptyl group;
if R2 represents a hydrogen atom;
and R1 represents an alkyl group;
either R3 or R4 may not represent a cyclohexyl group while the other represents at the same time an alkyl-aryl group;
or either R3 or R4 may not represent an alkyl group while the other represents at the same time an alkyl-aryl group;
if R2 represents a hydrogen atom;
and R1 represents a benzhydryl group;
and either R3 or R4 represents a hydrogen atom;
either R3 or R4 may not represent a (C═
O)-substituted alkyl-aryl group;
a (C═
O)-substituted aryl group;
if R2 represents a hydrogen atom;
and R1 represents benzyl;
and either R3 or R4 represents a hydrogen atom;
the other of R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group;
an unsubstituted benzyl group;
a C3-8 substituted alkyl group;
a substituted alkyl-aryl group;
or R3 or R4, together with their bridging nitrogen atom may not form a tetrahydropyrimidine ring;
a triazolo pyrimidine ring;
if R2 represents a benzyl group;
and either R3 or R4 represents a hydrogen atom either R3 or R4 may not represent a (C═
O)-substituted alkyl-aryl group;
if R2 represents a C1-3 alkyl group;
and either R3 or R4 represents a hydrogen atom either R3 or R4 may not represent an unsubstituted C1-2 alkyl group;
a substituted alkyl group;
a substituted or unsubstituted aryl group;
a substituted heteroaryl group;
a (C═
O)-substituted alkyl-aryl group;
optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
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Abstract
The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.
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Citations
59 Claims
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1. Substituted pyrrolidine compounds of general formula (I),
wherein R1 represents a hydrogen atom, an unbranched or branched, saturated, optionally at least mono-substituted C1-6-aliphatic radical; - a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted;
an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system;
a branched or unbranched, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system;
an optionally at least mono-substituted benzhydryl group;
a (C═
O)—
R5 group;
a group;
a (SO2)—
R6 group;
or a (C═
O)—
NR7R7a group;
R2 represents a hydrogen atom;
a substituted or unsubstituted aliphatic group;
a (C═
O)—
R8 group;
a benzyl group which is optionally substituted by one or more substituents independently selected from the group consisting of F, Cl, Br, I, NH2, SH, OH;R3 and R4, equal or different, represent a hydrogen atom;
an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group in which the cycloalkyl group may be optionally at least mono-substituted;
an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be optionally at least mono-substituted and/or condensed with a mono- or polycyclic ring system;
with the condition (proviso) that R3 and R4 may not at the same time represent a hydrogen atom;or R3 and R4 together with their bridging nitrogen atom form 1) a saturated or unsaturated ring system A, comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;2) an A-X—
B group,wherein A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;X represents a bond, a —
NH—
group, a —
(C═
O)—
group, a branched or linear, optionally substituted C1-6-aliphatic chain, —
O—
, or a —
SO2—
group;B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;3) an A-X—
B—
Y—
C group,wherein A represents a saturated or unsaturated ring system comprising 1 to 3 optionally condensed rings, in which additionally at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;X represents a bond, a —
NH—
group, a —
(C═
O)—
group, a branched or linear, optionally substituted C1-6-aliphatic chain, —
O—
, or a —
SO2—
group;B represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N, S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;Y represents a bond, a —
NH—
group, a —
(C═
O)—
group, a branched or linear, optionally substituted C1-6-aliphatic chain, —
O—
, or a —
SO2—
group;C represents a saturated or unsaturated ring system comprising 1 to 2 optionally condensed rings, in which at least 1 carbon atom is optionally replaced by N1 S or O and which is optionally at least mono-substituted by F, Cl, Br, I, NH2, SH, OH, oxo, CF3, a C1-6-aliphatic group;
a C1-6-alkyl-aryl group;
a C1-6-alkyl-heteroaryl group;
a C1-6-alkoxy group;
a (C═
O)—
R9 group;
a (C═
O)—
OR10 group;
a CH2-(C═
O)—
O—
R11 group;
a (SO2)—
R11 group;
a NH—
R11 group;
or a (C═
O)—
NR12R12a group;R5 and R6 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group;
an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;R7 and R7a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group;
an optionally at least mono-substituted aryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
an optionally at least mono-substituted heteroaryl group which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;R8 represents a hydrogen atom;
a branched or unbranched, saturated or unsaturated, unsubstituted aliphatic group;R9, R10 and R11 represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;R12 and R12a, identical or different, represent a hydrogen atom, an unbranched or branched, saturated or unsaturated, optionally at least mono-substituted aliphatic radical;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing alkyl-cycloalkyl group;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with a mono- or polycyclic ring system;
a branched or unbranched, saturated or unsaturated, optionally at least mono-substituted alkyl-heteroaryl group in which the heteroaryl group may be condensed with a mono- or polycyclic ring system;with the provisos that if R2 represents a hydrogen atom; and R1 represents a hydrogen atom or a condensed aryl group; R3 and R4 may not form together with their bridging nitrogen atom a triazole group; if R2 represents a hydrogen atom; and R1 represents a hydrogen atom;
a substituted C1-2 alkyl group;
a condensed aryl group;
a benzyl group;R3 and R4 may not form together with their bridging nitrogen atom a substituted, unsaturated, condensed ring system containing at least 4 nitrogen atoms as ring members;
an unsaturated, (C═
O)-substituted, uncondensed, 6-membered ring system in which one additional carbon atom is replaced by nitrogen.if R2 represents a hydrogen atom; and R3 and R4 form together with their bridging nitrogen atom a pyrrolidine ring, a piperidine ring, a piperazine ring or a morpholine ring; R1 may not represent a hydrogen atom;
a methyl group;
an unsaturated tert-butyl group;
a (C═
O)-substituted alkyl-heteroaryl group;if R2 represents a hydrogen atom; and R1 does not represent a benzyl group; and either R3 or R4 represents a hydrogen atom; either R3 or R4 may not represent a substituted alkyl-heteroaryl group;
an alkyl-aryl group;
a substituted heteroaryl group;
an unsubstituted methyl group;
a substituted alkyl group;
an aryl group;
a cyclohexyl group;
an alkyl-cycloalkyl group wherein the cycloalkyl group contains at least one heteroatom;if R2 represents a hydrogen atom; and R1 represents an alkyl group; and either R3 or R4 represents a hydrogen atom;
the other of R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group;
a branched C1-4 alkyl group;
a substituted or unsubstituted C3-6 cycloalkyl group in which optionally at least one carbon atom is optionally replaced by N, S or O;
a cycloheptyl group;if R2 represents a hydrogen atom; and R1 represents an alkyl group; either R3 or R4 may not represent a cyclohexyl group while the other represents at the same time an alkyl-aryl group;
or either R3 or R4 may not represent an alkyl group while the other represents at the same time an alkyl-aryl group;if R2 represents a hydrogen atom; and R1 represents a benzhydryl group; and either R3 or R4 represents a hydrogen atom; either R3 or R4 may not represent a (C═
O)-substituted alkyl-aryl group;
a (C═
O)-substituted aryl group;if R2 represents a hydrogen atom; and R1 represents benzyl; and either R3 or R4 represents a hydrogen atom; the other of R3 or R4 may not represent a substituted or unsubstituted C1-2 alkyl group;
an unsubstituted benzyl group;
a C3-8 substituted alkyl group;
a substituted alkyl-aryl group;or R3 or R4, together with their bridging nitrogen atom may not form a tetrahydropyrimidine ring;
a triazolo pyrimidine ring;if R2 represents a benzyl group; and either R3 or R4 represents a hydrogen atom either R3 or R4 may not represent a (C═
O)-substituted alkyl-aryl group;if R2 represents a C1-3 alkyl group; and either R3 or R4 represents a hydrogen atom either R3 or R4 may not represent an unsubstituted C1-2 alkyl group; a substituted alkyl group;
a substituted or unsubstituted aryl group;
a substituted heteroaryl group;
a (C═
O)-substituted alkyl-aryl group;optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 58)
- a saturated or unsaturated, optionally at least mono-substituted, optionally at least one heteroatom as ring member containing cycloalkyl group, which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system;
-
34-57. -57. (canceled)
-
59-63. -63. (canceled)
Specification