发明名称 Thienopyranones as Kinase and Epigenetic Inhibitors
摘要 The invention relates to methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infection, atheroscleosis, Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-depenent disorder including by modulating biological processes by the inhibition of PI3 kinase and/or bromodomain protein binding to substrates comprising the administration of a compound(s) of Formula I-IX (or pharmaceutically acceptable salts thereof) as defined herein.
申请公布号 US2017101418(A1) 申请公布日期 2017.04.13
申请号 US201615297293 申请日期 2016.10.19
申请人 SignalRx Pharmaceuticals, Inc. 发明人 Durden Donald L.;Morales Guillermo A.;Garlich Joseph R.
分类号 C07D495/04;A61K31/541;A61K31/538;A61K31/5377;A61K45/06 主分类号 C07D495/04
代理机构 代理人
主权项 1. A method for treating a disease in a human selected from cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infaction, atheroscleosis, Type I or 2 diabetes, obesity, inflammatory disease, or Myc-depenent disorder comprising administering a compound of Formula I-IX: wherein M is oxygen (O) or sulfur (S); R1 is selected from H, halogen, alkyl, alkenyl, alkynyl, carbocycle, aryl, heterocycle, heteroaryl, formyl, nitro, cyano, amino, carboxylic acid, carboxylic ester, carboxyl amide, reverse carboxyamide, substituted alkyl, substituted alkenyl, substituted alkynyl, substituted carbocycle, substituted aryl, substituted heterocycle, substituted heteroaryl, phosphonic acid, phosphinic acid, phosphoramidate, phosphonic ester, phosphinic ester, ketone, substituted ketone, hydroxamic acid, N-substituted hydroxamic acid, O-substituted hydroxamate, N- and O-substituted hydroxamate, sulfoxide, substituted sulfoxide, sulfone, substituted sulfone, sulfonic acid, sulfonic ester, sulfonamide, N-substituted sulfonamide, N,N-disubstituted sulfonamide, boronic acid, boronic ester, azo, substituted azo, azido, nitroso, imino, substituted imino, oxime, substituted oxime, alkoxy, substituted alkoxy, aryloxy, substituted aryloxy, thioether, substituted thioether, carbamate, substituted carbamate; R2 is selected from R1 or where X is C, N, P, P(O), SiRb, n is 0, 1, or 2; Y is C—R1, O, S, NRa, —C(O)(NH2), —P(Z)mRa, SiRaRb, BRb; Z is O or S; m=0 or 1; Ra is hydrogen (H) or independently at each instance any group defined in R1; Rb is hydrogen (H) or independently at each instance any group defined in R1; R3 is selected from R1; R4 is selected from R1; and Cyc is an aryl, substituted aryl, heterocyele, substituted heterocycle, carbocycle, and substituted carbocycle.
地址 San Diego CA US