| 摘要 |
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 havin g from 2 to 4 carbon atoms; R2 is an unsubstituted or mono-substituted five- o r six-membered heteroaromatic ring connected by a ring carbon atom to the amin e group shown, which five- or six- membered heteroaromatic ring contains from 1 to 3 heteroatoms selected from sulfur, oxygen or nitrogen, with one heteroat om 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 - oxidesthereof. |
