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US 2002/0002190 A1Published application
Para-aryl or heterocyclic substituted phenyl glucokinase activators
AssigneeHoffmann-La Roche Inc.
InventorsWendy L. Corbett, Nancy-Ellen Haynes, Ramakanth Sarabu
Life of this patent
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Abstract
Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
Claims95
An amide selected from the group consisting of a compound of the formula
- 70
- wherein R is a heteroaromatic ring, connected by a ring carbon atom, which contains from 5 to 6 ring members with from 1 to 2 heteroatoms selected from the group consisting of oxygen, sulfur or nitrogen, aryl containing 6 or 10 ring carbon atoms, aryl containing from 6 to 10 ring carbon atoms fused with a heteroaromatic ring containing 5 or 6 ring members with 1 or 2 heteroatoms in the ring being selected from the group consisting of nitrogen, oxygen or sulfur, or a saturated 5- or 6-membered cycloheteroalkyl ring, which contains from 1 to 2 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, or a cycloalkyl ring having 5 or 6 carbon atoms;
- R1 is a cycloalkyl ring having 5 or 6 carbon atoms;
- R2 is
- 71
- a five- or six-membered heteroaromatic ring connected by a ring carbon atom to the amide group shown, which heteroaromatic ring contains from 1 to 3 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen with a first heteroatom being nitrogen which is adjacent to the connecting ring carbon atom, said heteroaromatic ring being unsubstituted or 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,
- —(CH2)n—OR6, 72
- n is 0, 1, 2, 3 or 4;
- y and z are independently 0 or 1, * denotes the asymmetric carbon atom center;
- R3 is hydrogen, lower alkyl or
- 73
- R6, R7 and R8 are independently hydrogen or lower alkyl;
- and p is an integer from 0 to 5;
- or a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.