IP Library Granted Patent US 7,781,459
Granted Patent B2
US 7,781,459 · App. 11/613,433 · Granted Aug 24, 2010

Carboxyalkoxy-substituted acyl-carboxyphenylurea derivatives and their use as medicaments

Assignee: Sanofi-Aventis Deutschland GmbH
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Quick Facts
Patent No.
US 7,781,459
App. No.
11/613,433
Granted
Aug 24, 2010
Kind
B2
Abstract

The invention relates to acyl-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I, in which the radicals have the stated meanings, and the physiological tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example for the treatment of type II diabetes.

Claims (23)

1. A compound of the formula I,

in which

R1 is H, (C 1 -C 6 )-alkyl or (C 0 -C 6 )-alkyl-phenyl wherein the phenyl ring is optionally mono- or disubstituted with F, Cl, Br, CN, OH, (C 1 -C 6 )-alkyl, O—(C 1 -C 6 )-alkyl, CF 3 , OCF 3 , COOH, COO(C 1 -C 6 )-alkyl or CONH 2 ;

R2 is H, (C 1 -C 6 )-alkyl, O—(C 1 -C 6 )-alkyl, CO—(C 1 -C 6 )-alkyl, COO—(C1-C 6 )-alkyl or (C 0- C 6 )-alkylene-COOH;

R3 is H, F, Cl, Br, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl or (C1-C 6 )-alkyl; and

n is 1, 2, 3, 4, 5, 6, 7 or 8;

and pharmaceutically acceptable salts thereof.

2. The compound of claim 1 wherein

R1 is H or (C 1 -C 6 -alkyl;

R2 is H, (C 1 -C 6 )-alkyl, O—(C 1 -C 6 )-alkyl, CO—(C 1 -C 6 )-alkyl, COO—(C 1 -C 6 ) -alkyl or (C 0 -C 6 )-alkylene-COOH;

R3 is H, F, Cl, Br, OH, CF 3 , NO 2 , CN, OCF 3 , O—(C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkyl; and

n is 1, 2, 3, 4, 5, 6, 7or 8;

and pharmaceutically acceptable salts thereof.

3. The compound of claim 2 , wherein R1 is H or (C 1 -C 6 )-alkyl;

R2 is H, COO—(C 1 -C 6 )-alkyl or —COOH;

R3 is H or F; and

n is 1, 2, 3 or 4;

and pharmaceutically acceptable salts thereof.

4. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and one or more compounds of claim 1 .

5. A pharmaceutical composition comprising a pharmaceutically acceptable carrier, one or more compounds of claim 1 , and at least one other active ingredient.

6. The pharmaceutical composition of claim 5 , wherein the other active ingredient comprises one or more antidiabetics, hypoglycemic active ingredients, antiobesics, anorexia, HMG-CoA reductase inhibitors, cholesterol absorption inhibitors, PPAR gamma agonists, PPAR alpha agonists, PPAR alpha/gamma agonists, PPAR delta agonists, fibrates, MTP inhibitors, bile acid absorption inhibitors, CETP inhibitors, polymeric bile acid adsorbents, LDL receptor inducers, cholesterol absorption inhibitors (ezetimibe), ACAT inhibitors, antioxidants, lipoprotein lipase inhibitors, ATP-citrate lyase inhibitors, ACC inhibitors, squalene synthetase inhibitors, lipoprotein(a) antagonists, lipase inhibitors, insulins, sulfonylureas, biguanides, glitinides, thiazolidinediones, α-glucosidase inhibitors, glucagon-receptor antagonists, active ingredients which act on the ATP-dependent potassium channel of the beta cells, CART agonists, NPY agonists, GLP1 agonists, GIP agonists, MC4 agonists, MCH antagonists, orexin agonists, H3 agonists, TNF agonists, CRF agonists, CRF BP antagonists, urocortin agonists, β3 agonists, MSH (melanocyte-stimulating hormone) agonists, CCK agonists, serotonin reuptake inhibitors, mixed serotoninergic and noradrenergic compounds, 5HT agonists, bombesin agonists, galanin antagonists, growth hormones, growth hormone-releasing compounds, TRH agonists, LXR modulators, FXR modulators, uncoupling protein 2 or 3 modulators, leptin agonists, DA agonists (bromocriptine, Doprexin), lipase/amylase inhibitors, PPAR modulators, RXR modulators, TR-β agonists or amphetamines.

7. A method of reducing blood glucose comprising administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 .

8. A process for producing a pharmaceutical composition comprising one or more of the compounds of claim 1 comprising mixing said compound of claim 1 with a pharmaceutically suitable carrier and converting this mixture into a form suitable for administration.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 21, 2010
From: DEFOSSA, ELISABETH; KADEREIT, DIETER; KLABUNDE, THOMAS; BURGER, HANS-JOERG; HERLING, ANDREAS; WENDT, KARL-ULRICH; VON ROEDERN, ERICH; SCHOENAFINGER, KARL; ENHSEN, ALFONS
To: AVENTIS PHARMA DEUTSCHLAND GMBH
Reel/Frame 024265/0346 →
CHANGE OF NAME Recorded Apr 21, 2010
From: AVENTIS PHARMA DEUTSCHLAND GMBH
To: SANOFI-AVENTIS DEUTSCHLAND GMBH
Reel/Frame 024266/0001 →
Priority Claims (1)
DE 102 46 434 · Oct 4, 2002 · national
Continuity (3)
Continuation 1067955000 · Oct 6, 2003
Provisional Application 6044489000 · Feb 4, 2003
Related Publication 20070088083A1 · Apr 19, 2007