发明名称 Novel Inhibitors of System Xc-
摘要 The present invention is directed to novel inhibitors of system Xc−, also known as the cystine/glutamate antiporter. The present invention is further directed to methods of treating and detecting cancer that overexpresses system Xc− which includes but is not limited to gliomas (including glioblastoma), triple negative breast cancer, and bladder cancer. The present invention is further directed to methods of treating seizures including epileptic seizures.
申请公布号 US2015368213(A1) 申请公布日期 2015.12.24
申请号 US201514744707 申请日期 2015.06.19
申请人 The University of Montana, Missoula, MT 发明人 Natale Nicholas R.;Bridges Richard J.;Patel Sarjubhai A.;Duncan Nathan S.;Weaver Matthew J.;Gajewski Mariusz P.
分类号 C07D261/08;C07C311/42;A61K49/00;C07D261/18;A61K51/04 主分类号 C07D261/08
代理机构 代理人
主权项 1. A compound of formula A-B-D wherein: A is selected from —C—OH, —COOH, a compound of formula (I)and formula (II)wherein: n is an integer of 0 or 1; W, R9 and R10 are each independently selected from an H, a halogen, a nitrile, a carbonyl and a nitro group; X is selected from C, N, O, P, and S; R1 and R2 are each independently selected from H, dimethylamine, an optionally substituted alkyl, an optionally substituted aryl and an optionally substituted heteroaryl; and R3 and R4 are each independently selected from, H, O, O—CH3, O—CH2-aryl, and a C1-C6 alkyl, wherein R3 and R4 taken together with the atoms to which they are attached optionally form a 6-membered cycloalkyl or heterocycloalkyl, B is a linker compound selected fromwherein: Y is C or N; Z is C or 0; each R5 is independently selected from H, an optionally substituted C2-C6 alkyl, an optionally substituted aryl, an optionally substituted heteroaryl and R7 is selected from —N—, —NH2—C1-C6 alkyl-NH2—, and piperazine; and R8 is selected from —CO2H, and —CO2—CH2—CH3, and D is a compound of formula (II) wherein R9 and R10 are each independently selected from and H, a halogen, a nitrile, a carbonyl and a nitro group, or a pharmaceutically acceptable salt, ester or prodrug thereof.
地址 Missoula MT US