发明名称 THERAPEUTIC COMPOUNDS AND COMPOSITIONS
摘要 Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
申请公布号 US2015183760(A1) 申请公布日期 2015.07.02
申请号 US201414505866 申请日期 2014.10.03
申请人 Salituro Francesco G.;Saunders Jeffrey O.;Yan Shunqi 发明人 Salituro Francesco G.;Saunders Jeffrey O.;Yan Shunqi
分类号 C07D401/12;C07D413/14;C07D405/14;C07D417/14;C07D215/06;C07D401/14 主分类号 C07D401/12
代理机构 代理人
主权项 1. A compound of formula (I):or a pharmaceutically acceptable salt thereof wherein: W, X, Y and Z are each independently selected from CH or N; Q and Q1 are independently selected from a bond or NRb; A is optionally substituted bicyclic aryl or optionally substituted bicyclic heteroaryl; L is a bond, —C(O)—, —(CRcRc)m—, —OC(O)—, —(CRcRc)m—OC(O)—, —(CRcRc)m—C(O)—, —NRbC(S)—, or —NRbC(O)— (wherein the point of the attachment to R1 is on the left-hand side); R1 is selected from alkyl, carbocycle, aryl, heteroaryl, and heterocyclyl; each of which is substituted with 0-5 occurrences of Rd; each R3 is independently selected from halo, haloalkyl, alkyl, hydroxyl and —ORa, or two adjacent R3 taken together with the carbon atoms to which they are attached form an optionally substituted heterocyclyl; each R4 is independently selected from halo, haloalkyl, hydroxyl, ═O, and —ORa; each Ra is independently selected from alkyl, acyl, hydroxyalkyl and haloalkyl; each Rb is independently selected from hydrogen and alkyl; each Rc is independently selected from hydrogen, halo, alkyl, alkoxy and halo alkoxy or two Rc taken together with the carbon atoms to which they are attached form an optionally substituted cycloalkyl; each Rd is independently selected from halo, haloalkyl, haloalkoxy, alkyl, alkynyl, nitro, cyano, hydroxyl, —C(O)Ra, —OC(O)Ra, —C(O)ORa, —SRa, —NRaRb and —ORa, or two Rd taken together with the carbon atoms to which they are attached form an optionally substituted heterocyclyl; n is 0, 1, or 2; m is 1, 2 or 3; h is 0, 1, 2; g is 0, 1 or 2; the sum of g+h is equal to or greater than 2; and p is 1 or 2.
地址 Marlborough MA US