| 摘要 |
The present invention is related to substituted methylene amide derivatives of formula (I)and also its geometrical isomers, its optically active forms as enantiomers, diastereomers and its racemate forms, as well as pharmaceutically acceptable salts and pharmaceutically active derivatives thereof, wherein Ris selected from the group consisting of (C-C) alkyl, CHA or CHCHA moieties (where A is optionally substituted (C-C)aryl or optionally substituted (C-C)heteroaryl), optionally substituted C-Caryl, (3-8-membered)cycloalkyl, (C-C)alkylaryl, mono, bi- or tricyclic heteroaryl with condensed rings, or 3-8-membered) heterocycloalkyl or (C-C)alkylheterocyclyl and which comprise 1-3 heteroatoms selected from oxygen, nitrogen or sulphur; Rand Rare each independently from each other selected from the group comprising or consisting of H or (C-C)alkyl; Cy is optionally substituted (C-C)alkyl, 5-6 membered heteroaryl group with one or several heteroatoms selected from N, O or S; thienyl or phenyl substituted optionally substituted by (C-C)aryl group or optionally substituted by 5-6 membered heteroaryl group with one or several heteroatoms selected from N, O or S; wherein that substituents may be selected from halo, C-Calkoxy, C-Caryloxy, ciano, nitro, C-Calkyl, haloalkyl, hydroxy, C-Calkenyl, C-Calkynyl, B-R, where B is ethynyl group, and Ris (C-C)alkylphenyl; -COR, -COOR, -CO-NRR, -NHCOR, where Ris (C-C)alkyl or (C-C)alkenyl, -SOR, -SOR, -SONRR, wherein R,Rare each independently from each other selected from the group comprising H, linear or branched (C-C)alkyl, (C-C)alkenyl, (C-C)alkynyl, (C-C)aryl, 5-6 membered heteroaryl group with one or several heteroatoms selected from N, O or S, (3-8-membered)cycloalkyl or heterocycloalkyl, (C-C)alkyl-aryl or heteroaryl. With the proviso that the following compounds are excluded:and use thereof for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or pyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of substituted methylene amide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs. Also the present invention relates to a method of treating diabetes type II, obesity and to regulate the appetite of mammals. The present invention is furthermore related to novel substituted methylene amide derivatives and method of preparation thereof. |
