发明名称 3-phenyl-5-ureidoisothiazole-4-carboximide and 3-amino-5-phenylisothiazole derivatives as kinase inhibitors
摘要 This invention is directed to a compound of Formula I; or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, n, X1, X2, L1, and L2 are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
申请公布号 US8969583(B2) 申请公布日期 2015.03.03
申请号 US201213728502 申请日期 2012.12.27
申请人 Allergan, Inc. 发明人 Malone Thomas C.;Hull C. Eugene;Boral Sougato;Wurster Julie A.;Robinson Michael R.;Edelman Jeffrey L.
分类号 C07D275/03;C07D417/12;A61K31/5377;A61K31/425;A61K31/427;C07D295/13 主分类号 C07D275/03
代理机构 代理人 Kafka Mark D.
主权项 1. A compound of Formula I:or a pharmaceutically acceptable salt thereof, wherein: X1 is N and X2 is S; L1 is selected from the group consisting of —N(R)—, —N(R)—C(═O)—N(R)—, —O—C(═O)—N(R)—, —N(R)—C(═O)— and —C(═O)—N(R)—; L2 is selected from the group consisting of a covalent bond, —N(R)—, —N(R)—C(═O), —C(═O)—N(R)— and —N(R)—C(═O)—N(R)—; each R independently is H or C1-6 alkyl; each R1 independently is selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, halogen, and OR; or wherein two adjacent R1 groups taken together with the carbon atoms to which they are attached form a six-membered aryl or a five- or six-membered heteroaryl; n is 0, 1, or 2; R2 is selected from the group consisting of: a) H; b) C1-6 alkyl that is unsubstituted or substituted with one or two substituents selected from the group consisting of heterocyclyl, —C(═O)OR, hydroxy, and C1-6 alkoxy; andand R3 is selected from the group consisting of H, hydroxy, —NO2, aryl, and heteroaryl, wherein said aryl or heteroaryl is unsubstituted or substituted with one to three substituents selected from the group consisting of halo, C1-6 haloalkyl, and C1-6 alkyl.
地址 Irvine CA US