发明名称 GLS1 INHIBITORS FOR TREATING DISEASE
摘要 Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I:;;Methods of inhibition GLS1 activity in a human or animal subject are also provided.
申请公布号 US2016002204(A1) 申请公布日期 2016.01.07
申请号 US201514791284 申请日期 2015.07.03
申请人 Board of Regents, The University of Texas System 发明人 Di Francesco Maria Emilia;Jones Philip;Heffernan Timothy;Hamilton Matthew M.;Kang Zhijun;Soth Michael J.;Burke Jason P.;Carroll Christopher Lawrence;McAfoos Timothy;Palmer Wylie;Herrera Zachary
分类号 C07D401/06;A61K31/444;A61K45/06;A61K31/4439;C07D401/14;A61K31/501;C07D403/06;A61K31/513;C07D417/06;C07D487/04;A61K31/519;A61K31/4545;C07D405/14;C07D403/14;C07D409/14;A61K31/5377;A61K31/541;A61N5/10;A61N7/00;C07D417/14 主分类号 C07D401/06
代理机构 代理人
主权项 1. A compound of structural Formula I or a salt thereof, wherein: n is chosen from 3, 4, and 5; each Rx and Ry is independently chosen from alkyl, cyano, H, and halo, wherein two Rx groups together with the atoms to which they are attached optionally form a cycloalkyl ring; A1 and A2 are independently chosen from C—H, C—F, and N; R1 and R4 are independently chosen from alkenyl, alkoxy, alkyl, aryl, arylalkyl, cyano, cycloalkyl, cycloalkylalkyl, H, halo, haloalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, hydroxyl, C(R3)2C(O)R3, C(R3)2C(O)N(R3)2, C(R3)2N(R3)2, C(R3)2NR3C(O)R3, C(R3)2NR3C(O)OR3, C(R3)2NR3C(O)N(R3)2, C(R3)2NR3S(O)R3, C(R3)2NR3S(O)2R3, N(R3)2, NR3C(O)R3, NR3C(O)OR3, NR3C(O)N(R3)2, NR3S(O)R3, NR3S(O)2R3, C(O)N(R3)2, S(O)N(R3)2, S(O)2N(R3)2, C(O)R3, SR3, S(O)R3, and S(O)2R3, wherein each R1 and R4 may be optionally substituted with between 0 and 3 Rz groups; R2 is chosen from alkyl, heterocycloalkyl, cyano, cycloalkyl, H, halo, and haloalkyl, wherein R1 and R2 together with the atoms to which they are attached optionally form an form an aryl, cycloalkyl, heteroaryl, or heterocycloalkyl ring, which may be optionally substituted with between 0 and 3 Rz groups; each R3 is independently chosen from alkenyl, alkoxy, alkyl, aryl, arylalkyl, cyano, cycloalkyl, cycloalkylalkyl, H, halo, haloalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, and hydroxyl, wherein each R3 may be optionally substituted with between 0 and 3 Rz groups, wherein two R3 groups together with the atoms to which they are attached optionally form an aryl, cycloalkyl, heteroaryl, or heterocycloalkyl ring, which may be optionally substituted with between 0 and 3 Rz groups; each RZ group is independently chosen from alkenyl, alkoxy, alkoxyalkyl, alkoxyaryl, alkoxyarylalkyl, alkoxycycloalkyl, alkoxycycloalkylalkyl, alkoxyhaloalkyl, alkoxyheteroaryl, alkoxyheteroarylalkyl, alkoxyheterocycloalkyl, alkoxyheterocycloalkylalkyl, alkyl, alkylaryl, alkylarylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, alkylheteroaryl, alkylheteroarylalkyl, alkylheterocycloalkyl, alkylheterocycloalkylalkyl, aryl, arylalkyl, arylalkyloxy, arylhaloalkyl, aryloxy, cyano, cycloalkyl, cycloalkylalkyl, cycloalkylalkyloxy, cycloalkylhaloalkyl, cycloalkyloxy, H, halo, haloalkoxy, haloalkoxyalkyl, haloalkoxyaryl, haloalkoxyarylalkyl, haloalkoxycycloalkyl, haloalkoxycycloalkylalkyl, haloalkoxyheteroaryl, haloalkoxyheteroarylalkyl, haloalkoxyheterocycloalkyl, haloalkoxyheterocycloalkylalkyl, haloalkyl, haloalkylaryl, haloalkylarylalkyl, haloalkylcycloalkyl, haloalkylcycloalkylalkyl, haloalkylheteroaryl, haloalkylheteroarylalkyl, haloalkylheterocycloalkyl, haloalkylheterocycloalkylalkyl, haloaryl, haloarylalkyl, haloarylalkyloxy, haloaryloxy, halocycloalkyl, halocycloalkylalkyl, halocycloalkylalkyloxy, halocycloalkyloxy, haloheteroaryl, haloheteroarylalkyl, haloheteroarylalkyloxy, haloheteroaryloxy, haloheterocycloalkyl, haloheterocycloalkylalkyl, haloheterocycloalkylalkyloxy, haloheterocycloalkyloxy, heteroaryl, heteroarylalkyl, heteroarylalkyloxy, heteroarylhaloalkyl, heteroaryloxy, heterocycloalkyl, heterocycloalkylalkyl, heterocycloalkylalkyloxy, heterocycloalkylhaloalkyl, heterocycloalkyloxy, hydroxyl, oxo, N(R6)2, NR6C(O)C(R6)3, NR6C(O)OC(R6)3, NR6C(O)N(R6)2, NR6S(O)C(R6)3, NR6S(O)2C(R6)3, C(O)N(R6)2, S(O)N(R6)2, S(O)2N(R6)2, C(O)C(R6)3, SC(R6)3, S(O)C(R6)3, and S(O)2C(R6)3; each R6 is independently chosen from alkenyl, alkoxy, alkyl, aryl, arylalkyl, cyano, cycloalkyl, cycloalkylalkyl, H, halo, haloalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, and hydroxyl, wherein two R6 groups together with the atoms to which they are attached optionally form an aryl, cycloalkyl, heteroaryl, or heterocycloalkyl ring, which may be optionally substituted with between 0 and 3 Rx groups; and Z is heteroaryl, which may be optionally substituted.
地址 Austin TX US