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US 6,441,180 B1Granted
Tetrazolyl-phenyl actamide glucokinase activators
AssigneeHoffmann-La Roche Inc.
InventorAchyutharao Sidduri
Life of this patent
Estimating the term…
Abstract
Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.
Claims17
A tetrazole selected from the group consisting of a compound of the formula:
- wherein
- one of R1 or R2 is
- and the other is hydrogen, halogen, lower alkyl sulfonyl, perfluoro-lower alkyl, cyano, or nitro;
- R3 is cycloalkyl;
- R4 is a 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 adjacent to the connecting ring carbon atom, said heteroaromatic ring being unsubstituted or monosubstituted with halogen at a position on a ring carbon atom other than that adjacent to said connecting carbon atom;
- R5 is lower alkyl, or perfluoro lower alkyl;
- R6 is hydrogen or lower alkyl;
- n is 0 or 1;
- Δ denotes a trans configuration across the double bond;
- and a pharmaceutically acceptable salt thereof.
7 more elements
A tetrazole selected from the group consisting of a compound of the formula:
- wherein
- one of R1 or R2 is
- and the other is hydrogen, halogen, lower alkyl sulfonyl, perfluoro-lower alkyl, cyano, or nitro;
- R3 is cycloalkyl;
- R4 is a 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 adjacent to the connecting ring carbon atom, said heteroaromatic ring being unsubstituted or monosubstituted with halogen at a position on a ring carbon atom other than that adjacent to said connecting carbon atom;
- R5 is lower alkyl, or perfluoro lower alkyl;
- R6 is hydrogen or lower alkyl;
- n is 1 or 1;
- the * represents the asymmetric carbon atom
- and a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.