发明名称 Use of peptide epoxyketones for metastasis suppression
摘要 The invention provides a method of repressing metastasis of a cancer compromising the administration of a peptide epoxyketone proteasome inhibitor. Furthermore, the method can be performed in combination with the administration of one or more additional therapeutics.
申请公布号 US8853147(B2) 申请公布日期 2014.10.07
申请号 US201013509226 申请日期 2010.11.11
申请人 Onyx Therapeutics, Inc. 发明人 Kirk Christopher J.;Jiang Jing
分类号 A61K38/00;A61K38/05;A61K31/336;A61K38/06 主分类号 A61K38/00
代理机构 Marshall, Gerstein & Borun LLP 代理人 Marshall, Gerstein & Borun LLP
主权项 1. A method for repressing metastasis of a cancer, comprising administering to a subject in need thereof a therapeutically effective amount of a peptide epoxyketone proteasome inhibitor or a pharmaceutically acceptable salt thereof, wherein the proteasome inhibitor has a structure of formula (I) or a pharmaceutically acceptable salt thereofwherein R1, R2, and R3 are each independently selected from C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxyalkyl, aryl, and C1-6aralkyl, any of which is optionally substituted; R4 is N(R5)L-Z—R6; R5 is selected from hydrogen, OH, C1-6aralkyl-Y—, and C1-6alkyl-Y—; R6 is selected from hydrogen, OR7, C1-6alkenyl, Ar—Y—, carbocyclyl, and heterocyclyl; R7 and R8 are independently selected from hydrogen, C1-6alkyl, and C1-6aralkyl; each Ar is independently an aromatic or heteroaromatic group optionally substituted with 1-4 substituents; L is selected from C═O, C═S, and SO2; X is selected from O, S, NH, and N—C1-6alkyl; Y is absent or is selected from C═O and SO2; and Z is absent or is C1-6alkyl.
地址 South San Francisco CA US