Isoindolin-1-one glucokinase activators

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 417/12 (2006.01) A61K 31/427 (2006.01) A61K 31/4439 (2006.01) A61K 31/4709 (2006.01) A61K 31/506 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2430579

Isoindolin-1-one-substituted propionamide glucokinase activators which increase insulin secretion in the treatment of type II diabetes of formula (I) wherein A is unsubstituted phenyl or phenyl which is mono- or di-substituted with halo or mono-substituted with lower alkyl sulfonyl, lower alkyl thio or nitro; R1 is cycloalkyl having from 3 to 9 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R2 is an unsubstituted or mono-substituted five- or six-membered heteroaromatic ring connected by a ring carbon atom to the amine 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, which ring may be monocyclic or fused with phenyl at two of its ring carbons, said monosubstituted 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 halo, lower alkyl, nitro, cyano, perfluoro-lower alkyl; hydroxy -(CH2)n-OR3, -(CH2)n-C(O)-OR3, -(CH2)n- C(O)-NH-R3, -C(O)C(O)-or3, or -(CH2)n-NHR3; where R3 is hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salts or N- oxides thereof.

L'invention concerne des activateurs de la propionamide glucokinase à substitution isoindoline-1-one qui augmentent la sécrétion d'insuline dans le traitement du diabète de type II.

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