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US 6,486,184 B2Granted
α-acyl- and α-heteroatom-substituted benzene acetamide glucokinase activators
AssigneeHoffmann-La Roche Inc.
InventorsRobert Francis Kester, Ramakanth Sarabu
Life of this patent
Estimating the term…
Abstract
Substituted benzene acetamide compounds which are glucokinase activators and pharmaceutically acceptable salts thereof.
Claims24
An amide selected from the group consisting of a compound of the formula:
- wherein R1 and R2 are independently hydrogen, halo, cyano, nitro, lower alkylthio, perfluoro loweralkylthio, lower alkyl sulfonyl, or perfluoro-lower alkyl sulfonyl;
- R3 a 5 to 7-membered ring which is cycloalkyl, cycloalkenyl, or heterocycloalkyl having one heteroatom selected from oxygen and sulfur;
- R6is an unsubstituted or mono-substituted five- or six-membered heteroaromatic ring connected by a ring carbon atom to the amide group shown, which five- or six-membered heteroaromatic ring contains from 1 to 3 heteroatoms selected from sulfur, oxygen or nitrogen, with one heteroatom being nitrogen which is adjacent to the connecting ring carbon atom;
- with said mono-substituted heteroaromatic ring being monosubstituted at a position on a ring carbon atom other than adjacent to said connecting carbon atom with a substituent selected from the group consisting of lower alkyl, halo, nitro, cyano, —(CH2)n—OR9, —(CH2)n—C(O)—OR10, —(CH2)n—C(O)—NH—R11, —C(O)—C(O)—OR12, —(CH2)n—NHR13;
- n is 0, 1, 2, 3 or 4;
- R7, R8, R9, R10, R11, R12and R13 are independently hydrogen or lower alkyl;
- X is oxygen, sulfur, sulfonyl or carbonyl;
- the * indicates an asymmetric carbon atom;
- and its pharmaceutically acceptable salts.
6 more elements
The amide of claim 19 wherein R1 and R2 are independently chloro or methyl sulfonyl.
Dependencies are inferred from the claim text.