发明名称 Therapeutic methods and compositions involving allosteric kinase inhibition
摘要 The present invention is directed to methods and compositions for suppressing lymphangiogenesis, angiogenesis and/or tumor growth. The methods comprise contacting the tumor with a compound that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state.
申请公布号 US9260417(B2) 申请公布日期 2016.02.16
申请号 US201113577431 申请日期 2011.02.07
申请人 AMITECH THERAPEUTIC SOLUTIONS, INC. 发明人 Murphy Eric A.;Cheresh David A.;Arnold Lee Daniel
分类号 A61K31/505;C07D403/12 主分类号 A61K31/505
代理机构 Wilson Sonsini Goodrich & Rosati 代理人 Wilson Sonsini Goodrich & Rosati
主权项 1. A method for treating cancer in a human subject comprising administering to a patient in need a compound having the structure:or an N-oxide, N,N′-dioxide, N,N′,N″-trioxide, or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 are independently hydrogen, optional substituted alkyl, halogen, optional substituted amine, NH2, optional substituted alkyoxy, optional substituted thioalkyl, CF3S optional substituted alkylsulfinyl or optional substituted alkylsulfonyl; Z′ is N or C; Rm is C1-6 alkyl, or halogen substituted C1-6 alkyl; and R3 is independently a C1-6 alkyl, halogen substituted C1-6 alkyl, halogen substituted C1-6 alkoxy, or C3-10cycloalkyl; or, Rm and R3 are joined to form a five to seven membered carbocycle; and n is 1-4; that (i) stabilizes a protein kinase in the inactive state and (ii) is not an ATP competitive inhibitor of the protein kinase in the active state; and wherein the cancer is selected from melanoma, breast cancer, pancreatic cancer, lung cancer, kidney cancer, and colon cancer.
地址 La Jolla CA US
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