发明名称 AZA spiro alkane derivatives as inhibitors of metalloproteases
摘要 The present invention provides a compound of Formula I or Formula II:; enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
申请公布号 US9403775(B2) 申请公布日期 2016.08.02
申请号 US201314092351 申请日期 2013.11.27
申请人 Incyte Corporation;Incyte Holdings Corporation 发明人 Yao Wenqing;Zhuo Jincong;Xu Meizhong;Zhang Fenglei;Metcalf Brian W.
分类号 A61K31/46;A61K31/497;A61K31/44;A61K31/495;A61K31/55;A61K31/4965;C07D221/10;C07D401/12;C07D401/14;C07D471/04;C07D487/04;C07D221/20;C07D401/06;C07D405/14;C07D409/14;C07D417/14;C07D495/04;C07D405/12 主分类号 A61K31/46
代理机构 Fish & Richardson P.C. 代理人 Fish & Richardson P.C.
主权项 1. A method for treating a cancer selected from prostate cancer, non-small cell lung cancer, colon cancer, pancreatic cancer, and glioma in a mammal, comprising administering to said mammal a therapeutically effective amount of a compound of the following formula:or a pharmaceutically acceptable salt thereof, wherein: X is CH2NRb; Y is (CH2)j; V is piperidin-1-yl, piperazin-1-yl, pyrrolidin-1-yl, pyridin-1-yl or 3,6-dihydropyridin-1-yl each substituted with 0-5 Re; V′ is phenyl substituted with 0-5 Re; Rb is H, C(O)O(CRb′Rc′)r-T, or C(O)(CRb′Rc′)r-T; Rb′ and Rc′ are both H; Re is H, C1-6 alkyl, OH, Cl, F, Br, I, CN, NO2, methoxy, ethoxy, n-propoxy, isopropoxy, phenoxy, benzyloxy, amino, (C1-4 alkyl)amino, (C2-8)dialkylamino, C(O)O(C1-4 alkyl), CONH2, CONH(C1-4 alkyl), CON(C1-4 alkyl)2, C1-6 haloalkyl, phenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, benzyl, or phenethyl; T is H, C1-10 alkyl substituted with 0 to 5 Rb′; C2-10 alkenyl substituted with 0 to 5 Rb′, C2-10 alkynyl substituted with 0 to 5 Rb′, C3-13 carbocyclyl substituted with 0-3 Rb′, or heterocyclyl substituted with 0-5 Rb′; j is 1 or 2; and r is 0, 1 or 2.
地址 Wilmington DE US