IP Library Granted Patent US 8,138,207
Granted Patent B2
US 8,138,207 · App. 11/855,227 · Granted Mar 20, 2012

Aminocarbonyl-substituted 8-N-benzimidazoles, methods for their preparation and their use in pharmaceutical compositions

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Quick Facts
Patent No.
US 8,138,207
App. No.
11/855,227
Granted
Mar 20, 2012
Kind
B2
Abstract

The present invention comprises the use of amino-carbonyl-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically utilizable blood sugar-lowering action. These compounds are intended to be particularly suitable in the treatment of diabetes, carbohydrate and lipid metabolic disorders and other blood sugar complications.

Claims (10)

1. The compound of formula I

wherein

R20 is H;

R21 is selected from the group consisting of (C 6 -C 10 )-aryl and (C 1 -C 6 )-alkylene-(C 6 -C 10 )-aryl, where the aryl radicals may be mono- or polysubstituted by F, Cl, Br, I, CN, NO 2 , SH, OH, CF 3 , (C 1 -C 6 )-alkyl, O—(C 1 -C 6 )-alkyl, or S—(C 1 -C 6 )-alkyl;

R3 is (C 2 -C 10 )-alkenyl;

R4, R5 are each H;

R11 is selected from the group consisting of F, Cl, Br, I, (C 1 -C 6 )-alkyl, (C 3 -C 8 )-cycloalkyl, NH 2 , NH(C 1 -C 6 )-alkyl, NH(C 3 -C 7 )-cycloalkyl, N((C 1 -C 6 )-alkyl) 2 and O—(C 1 -C 6 )-alkyl, where the alkyl groups may be mono- or polysubstituted by F, Cl, Br or I; and

n is 0;

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising the compound of formula I as recited in claim 1 further combined with one or more additional solvents, bulking agents, binders, lubricants, inert diluents and/or one (or more) surfactants/dispersants, excipients, thickening agents, buffers, polymers, stabilizers, binders, flavorants, sweeteners formulated as a pharmaceutical composition for administration as a tablet, capsule, intravenous solution, transdermal gel, powder, oral solution, syrup, intranasal spray, or lozenge to a patient in need thereof.

Assignments (2)
CHANGE OF NAME Recorded Jun 20, 2012
From: SANOFI-AVENTIS
To: SANOFI
Reel/Frame 028413/0927 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2008
From: DEFOSSA, ELISABETH; SCHOENAFINGER, KARL; JAEHNE, GERHARD; BUNING, CHRISTIAN; TSCHANK, GEORG; WERNER, ULRICH
To: SANOFI-AVENTIS
Reel/Frame 020483/0263 →