发明名称 Pyrrolidine derived β3 adrenergic receptor agonists
摘要 The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).;
申请公布号 US8933102(B2) 申请公布日期 2015.01.13
申请号 US201113881548 申请日期 2011.10.24
申请人 Merck Sharp & Dohme Corp. 发明人 Morriello Gregori J.;Chang Lehua;Edmondson Scott D.
分类号 A01N43/40;A61K31/445;A61K31/497;A61K31/4965;A01N43/64;A61K31/41;C07D241/02;C07D405/00;C07D409/00;C07D411/00;C07D413/00;C07D417/00;C07D419/00;C07D421/00;C07D211/06;C07D257/00;C07D207/00;C07D295/00;A61K31/506;A61K31/40;A61K45/06;C07D401/14;C07D403/14;A61K31/454 主分类号 A01N43/40
代理机构 代理人 Shatynski Patricia A.;Ginkel Laura
主权项 1. A compound of Formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof: wherein m is 0 or 1; n is 0, 1, or 2; q is 0 or 1; A is —CH═ or —N═; B1 is —CH2— or —NH—; R6 and R9 are each a hydrogen; or R6 and R9 form a direct bond; each occurrence of R1 and R2 is independently selected from the group consisting of: (1) C1-C4 alkyl optionally substituted with 1 to 3 halogen atoms, and(2) halogen; each occurrence of R3 is independently selected from the group consisting of: (1) C1-C4 alkyl optionally substituted with 1 to 3 groups independently selected from: (a) halogen,(b) —ORa, and(c) a 5- to 6-membered heterocyclic ring with 1 to 4 nitrogen atoms, optionally substituted with 1 to 3 groups independently selected from halogen, C1-C4 alkyl optionally substituted with 1 to 3 halogen atoms,(2) halogen,(3) —ORa,(4) —NRaRb, and(5) a 5- to 6-membered heterocyclic ring with 1 to 4 nitrogen atoms, optionally substituted with 1 to 3 groups independently selected from (a) C1-C4 alkyl optionally substituted with 1 to 3 halogen atoms,(b) halogen,(c) —ORa, and(d) —NRaRb; and each occurrence of Ra and Rb is independently selected from the group consisting of: (1) hydrogen, and(2) C1-C4 alkyl optionally substituted with 1 to 3 halogen atoms.
地址 Rahway NJ US