Title:
ISOINDOLIN-1-ONE GLUCOKINASE ACTIVATORS
Document Type and Number:
WIPO Patent Application WO2002048106
Kind Code:
A3
Abstract:
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; R<1> is cycloalkyl having from 3 to 9 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R<2> 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-OR<3>, -(CH2)n-C(O)-OR<3>, -(CH2)n-C(O)-NH-R<3>, -C(O)C(O)-or<3>, or -(CH2)n-NHR<3;> where R<3> is hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salts or N-oxides thereof.
Inventors:
GUERTIN KEVIN RICHARD (US)
Application Number:
PCT/EP2001/014404
Publication Date:
November 28, 2002
Filing Date:
December 07, 2001
Export Citation:
Assignee:
HOFFMANN LA ROCHE (CH)
International Classes:
A61K31/4184; A61K31/422; A61K31/427; A61K31/428; A61K31/4439; A61K31/4709; A61K31/497; A61K31/506; A61P3/10; A61P43/00; C07D209/44; C07D277/42; C07D401/12; C07D403/12; C07D413/12; C07D417/12; A61K31/404; A61P3/08; C07D209/46; C07D213/60; C07D241/20; C07D263/58; (IPC1-7): C07D417/12; C07D403/12; C07D401/12; C07D413/12; A61K31/4439; A61K31/427; A61K31/4709; A61K31/506
Domestic Patent References:
| WO2001083478A2 | 2001-11-08 | |||
| WO2001085706A1 | 2001-11-15 | |||
| WO2000058293A2 | 2000-10-05 |
Foreign References:
| US5200408A | 1993-04-06 |
Download PDF: