发明名称 NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT
摘要 Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment.;
申请公布号 US2015336946(A1) 申请公布日期 2015.11.26
申请号 US201314652944 申请日期 2013.12.12
申请人 MERCK SHARP & DOHME CORP. 发明人 Lin Songnian;Parmee Emma R.;Xu Jiayi
分类号 C07D417/14;C07D417/12;C07F9/6558;A61K31/675;A61K31/4439;A61K31/444 主分类号 C07D417/14
代理机构 代理人
主权项 1. A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 individually represent 6- to 10-membered aryl group, 5- to 10-membered heteroaryl group, a 5- to 7-membered cycloalkyl group, or a 5- to 7-membered aliphatic heterocyclic group, optionally substituted with 1-4 substituents independently selected from: halogen, hydroxy, oxo, C1-6alkyl, C1-6alkylOC1-6alkyl, C1-6alkoxy, CN, NR3R4, C(O)1-2C1-6alkyl, C1-6alkylC(O)1-2C1-6alkyl, C1-6alkylS(O)0-2, S(O)0-2 or arylC1-6alkyl, wherein the alkyl and alkoxy substituents are further optionally substituted by 1-4 substituents independently selected from: halogen or C1-6alkyl where said C1-6alkyl is optionally substituted by 1-6 halogens; ring A represents a 5- to 7-membered monocyclic or 9- to 10-membered bicyclic heteroaryl group in which the carbon atom attached to the amide nitrogen atom contained in formula (I) forms C═N together with the nitrogen atom in the ring, wherein ring A, in addition to the -L-T substituent, is further optionally substituted with 1-4 substituents independently selected from: halogen, hydroxy, C1-6alkyl, C1-6alkylOC1-6alkyl, C1-6alkoxy, C1-6alkylS(O)0-2, CN, NR3R4, C(O)1-2C1-6alkyl, C1-6alkylC(O)1-2C1-6alkyl or S(O)0-2, wherein the alkyl and alkoxy substituents are further optionally substituted by 1-4 substituents independently selected from: halogen, C1-6alkyl or C1-6alkoxy where the alkyl and alkoxy substituents are optionally substituted by 1-6 halogens, L represents C1-6alkyl, C1-6alkylOC1-6alkyl, C1-6alkoxy, NR3R4, C1-6 alkylNR3R4, S(O)0-2C1-6alkyl or S(O)0-2, wherein the alkyl and alkoxy groups are further optionally substituted by 1-4 substituents independently selected from: halogen or C1-6alkyl where said C1-6alkyl is optionally substituted by 1-6 halogens, T represents CO2R, CONR3R4, or P(O)(OR5)2, and R, R3, R4, and R5 are individually selected from hydrogen or C1-6alkyl.
地址 Rahway NJ US