发明名称 Acetamide derivatives as glucokinase activators, their process and medicinal applications
摘要 Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed.;;The disclosure also provides process of preparation of these acetamide derivatives.
申请公布号 US9340506(B2) 申请公布日期 2016.05.17
申请号 US201213399721 申请日期 2012.02.17
申请人 ADVINUS THERAPEUTICS LIMITED 发明人 Bhuniya Debnath;Deshpande Anil;Kandalkar Sachin;Kobal Balasaheb;Kurhade Santosh;Vyavahare Vinod;Kaduskar Rahul
分类号 C07D277/34;C07D277/38;C07D513/04;A61K31/397;A61K31/44;A61K31/437;A61K31/427;C07D213/80;C07D241/26;C07D277/46;C07D277/54;C07D401/04;C07D405/12;C07D405/14;C07D413/12;C07D417/04;C07D417/12;C07D417/14;A61K38/26 主分类号 C07D277/34
代理机构 Perkins Coie LLP 代理人 Perkins Coie LLP
主权项 1. A compound of formula (I) or its stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, solvates and formulations wherein, ring A and ring C are monocyclic ring independently selected from aryl, heteroaryl or heterocyclyl; wherein rings A and C are optionally substituted with 1 to 4 substituents independently selected from halogen, monohaloalkyl, dihaloalkyl or perhaloalkyl, monohaloalkoxy, dihaloalkoxy or perhaloalkoxy, cyano, nitro, alkyl, alkenyl, alkynyl, methylenedioxy, amidino —NR6R7, —OR6, —NR6C(O)R7, —(CR8R9)nC(O)OR6, —(CR8R9)nC(O)NR6R7, —(CR8R9)nC(O)R6, cycloalkyl, heterocyclyl, aryl or heteroaryl groups; n=0-4; R6 and R7 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl and heterocyclylalkyl; wherein R6 and R7 is each optionally substituted with one or more substituents selected from halo, straight chain or branched chain alkyl, cycloalkyl, aryl, heteroaryl, heterocycle, alkylsulfonyl, oxo, nitro, cyano, —(CR8R9)nCOOR6, —(CR8R9)nC(O)NR6R7, —OR6, —SR6 or —NR6R7; or R6 and R7 taken together form a monocyclic or a bicyclic ring system which is saturated or partially unsaturated and optionally have additional heteroatoms selected from O, N or S, said ring system is further optionally substituted with 1 to 4 substituents independently selected from halo, alkyl, nitro, cyano, —OR6, —SR6, —NR6R7, oxo, alkylsulfonyl, —COOR6, —C(O)NR6R7, cycloalkyl, aryl, heterocyclyl or heteroaryl; wherein R6 and R7 are as described above; R8 and R9 are independently selected from the group consisting of hydrogen, fluorine, OR6, alkyl and perfluoroalkyl; or R8 and R9 taken together form a monocyclic or a bicyclic ring system which is saturated or partially unsaturated and optionally have additional heteroatoms selected from O, N or S, said ring system is further optionally substituted with 1 to 4 substituents independently selected from halo, alkyl, nitro, cyano, oxo, —OR6, —SR6, —NR6R7, alkylsulfonyl, —COOR6, —C(O)NR6R7, cycloalkyl, aryl, heterocyclyl or heteroaryl; wherein R6 and R7 are as described above; ring-B is an optionally substituted 4-12 membered mono or bicyclic ring containing 1-4 hetero atoms selected from N, O, S with at least one nitrogen in the ring; X represents O or NR6; wherein R6 is as described above; R1 is selected from cycloalkyl or heterocyclyl; R2 is hydrogen; R3 is selected from the group consisting of hydrogen, alkyl and perfluoroalkyl; R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, mono, di or tri substituted haloalkyl, nitrile, nitro, oxo, —NR6R7, —OR6, —S(O)pR6, —S(O)pNR6R7, —NR6S(O)pR7, —NR6C(O)R7, —OS(O)pR7, —NR6C(O)OR7, —(CR8R9)nC(O)OR6, —(CR8R9)n(CO)NR6R7, —(CR8R9)nS(O)pNR6R7, —(CR8R9)nN(R6)C(O)R6, —(CR8R9)nOR6, —C(R8R9)nNR6R7, —C(R8R9)nCO(R6) and —S(O)pC(R8R9)nC(O)OR6; wherein R4 and R5 is each optionally substituted with one or more substituents selected from halo, straight chain or branched chain alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocycle, alkylsulfonyl, oxo, nitro, cyano, —(CR8R9)nCOOR6, —(CR8R9)nC(O)NR6R7, —OR6, —SR6 or —NR6R7; wherein n=0-4; R6, R7, R8 and R9 are as described above; and in addition to R4 and R5, ring-B is further optionally substituted with one or more substituents selected from halo, straight chain or branched chain alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkylsulfonyl, oxo, nitro, cyano, —COOR6, —C(O)NR6R7, —OR6, —SR6 or —NR6R7.
地址 Bangalore IN