Use of aryl-substituted polycyclic amines as medicaments

• US 8,163,741 B2
• Filed: 06/23/2009
• Issued: 04/24/2012
• Est. Priority Date: 08/16/2004
• Status: Expired due to Fees

• Current Assignee: Sanofi-Aventis Deutschland GmbH (Sanofi )
• Original Assignee: Sanofi-Aventis Deutschland GmbH (Sanofi )
• Inventors: Schwink, Lothar, Stengelin, Siegfried, Gossel, Matthias, Hessler, Gerhard, Lennig, Petra
• Primary Examiner(s): Andres, Janet
• Assistant Examiner(s): Rahmani, Niloofar
• Application Number:
  US12/489,648
• Publication Number:
  US 20090258872A1
• Time in Patent Office: 1,036 Days
• Field of Search: 514/233.2, 514/306, 514/299
• US Class Current: 514/233.2
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• 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 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 3/08 for glucose homeostasis pancreatic hormones A61P5/48
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 9/04 Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• 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
• CPC Class Codes: C07D 471/04 Ortho-condensed systems
• CPC Class Codes: C07D 471/08 Bridged systems
• CPC Class Codes: C07D 487/04 Ortho-condensed systems

Abstract

The invention relates to therapeutic use of aryl-substituted polycyclic amines of the formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof;

where the symbols and radicals are explained in the description.

Claims

1. A method for the treatment of obesity which comprises administering to a patient in need of said treatment an effective amount of a compound of formula I:

5. The method as claimed in claim 1, wherein:

A, B, D, and G are, independently of one another, N or C(R3), and the total number of nitrogen atoms in this ring is 0-2.

7. The method as claimed in claim 1, wherein:

A, B, D, and G are, independently of each other, C(R3);

;

R3 is H, F, Cl, Br, CF₃, CN, O—

(C₁-C₆)-alkyl, O—

(C₁-C₄)-alkoxy-(C₁-C₄)-alkyl, S—

(C₁-C₆)-alkyl, (C₁-C₆)-alkyl, (C₀-C₈)-alkylene-aryl, O—

(C₀-C₈)-alkylene-aryl, N(R4)(R5), SO₂—

CH₃, CON(R6)(R7), N(R8)CO(R9), CO(R12), or (CR13R14)_x—

O(R15);

R4, R5, R6, R7, and R8 are, independently of one another, H or (C₁-C₈)-alkyl;

or, alternatively,

R4 and R5, R6 and R7 form, independently of one another, optionally together with the nitrogen atom to which they are bonded, a 5-6 membered ring which, apart from the nitrogen atom, may also include 1 further heteroatom selected from the group consisting of NH, N—

(C₁-C₆)-alkyl, oxygen and sulfur;

R9 and R12 are, independently of one another, H or (C₁-C₈)-alkyl;

R13 and R14 are each H;

R15 is H or (C₁-C₆)-alkyl; and

x is 0, 1 or 2.

8. The method as claimed in claim 1, wherein X is a bond or N(R16), in which R16 is H or (C₁-C₈)-alkyl.

2. A method for the treatment of obesity which comprises administering to a patient in need of said treatment an effective amount of a compound of formula I:

3. The method as claimed in claim 2, wherein Q is:

4. The method as claimed in claim 2, in which the group L-Q has the following meanings:

6. The method as claimed in claim 2, wherein:

K is O, OCH₂, CH₂O, S, SO, SO₂, N(R35), N(R36)CO, CON(R37), (C(R38)(R39))_v, CO, (R31)C═

C(R32), C≡

C, SCH₂, or SO₂.

9. The method as claimed in claim 2, wherein K is OCH₂, CH₂O, N(R36)CO, CON(R37), (C(R38)(R39))₂, (R31)C═

C(R32), C≡

C, SCH₂, or SO₂CH₂.

10. The method as claimed in claim 2, wherein K is OCH₂, CH₂O, CON(R37), C≡

C, or SCH₂.