发明名称 PYRAZOLO PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF
摘要 This invention generally relates to pyrazolo pyrimidine derivatives useful as, inter alia, inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. More specifically, the invention relates to pyrazolo pyrimidine derivatives, including derivatives and analogs of SDR inhibitors, pharmaceutical compositions containing derivatives and analogs of SDR inhibitors, methods of making derivatives and analogs of SDR inhibitors and methods of use thereof.
申请公布号 US2016168151(A1) 申请公布日期 2016.06.16
申请号 US201514864655 申请日期 2015.09.24
申请人 The Regents of the University of California 发明人 Tanaka Masahiro;Zhang Chao;Shokat Kevan M.;Burlingame Alma L.;Hansen Kirk;Bateman Raynard L.;DiMagno Stephen G.
分类号 C07D487/04 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of Formula I: or a pharmaceutically-acceptable salt thereof; wherein: Y is N;Z is NR3R4, halo, H, OH, alkyl, alkyloxy, or haloalkyl;R1a is benzyl or phenyl, wherein said benzyl or phenyl is optionally substituted with one or two OH, —NR3R4, —C(═O)NR6R7, —CN, NO2—C(═O)OH, —C(═O)O-alkyl, (C1-C4)alkyl, haloalkyl or haloaryl;R2 is C1-C6 alkyl or C4-C7 cycloalkyl, wherein said alkyl or said cycloalkyl is optionally substituted with mono- or di-alkoxy, mono- or di-halophenyl, mono- or di-(C1-4)alkoxy phenyl, mono- or di-(C1-4)alkyl phenyl, perhalo(C1-4)alkyl phenyl, carboxyl, tert-butyl carboxyl, phosphoryl, (C1-6)alkyl, (C4-7)cycloalkyl, indolyl, isoindolyl, pyridyl, naphthyl, pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl, thienyl, or alkylmorpholino;R3 and R4 are independently H, C1-C6 alkyl, tert-butyloxycarbonyl, morpholino(C1-C4)alkyl, carboxy(C1-C3)alkyl, (C1-C4)alkoxycarbonyl(C1-C3)alkyl, aryl, heteroaryl, aryloxy, heterocycle, cycloalkyl, alkenyl with the proviso that the double bond of the alkenyl is not present at the carbon atom that is directly linked to N, alkynyl with the proviso that the triple bond of the alkynyl is not present at the carbon atom that is directly linked to N, perfluoroalkyl, —S(O)2alkyl, —S(O)2aryl, —(C═O)heteroaryl, —(C═O)aryl, —(C═O)(C1-C6) alkyl, —(C═O)cycloalkyl, —(C═O)heterocycle, alkyl-heterocycle, aralkyl, arylalkenyl, —CON R6R7, —SO2R6R7, arylalkoxyalkyl, arylalkylalkoxy, heteroarylalkylalkoxy, aryloxyalkyl, heteroaryloxyalkyl, aryloxyaryl, aryloxyheteroaryl, alkylaryloxyaryl, alkylaryloxyheteroaryl, alkylaryloxyalkyamine, alkoxycarbonyl, aryloxycarbonyl, or heteroaryloxycarbonyl;R6 and R7 are independently H, alkyl, aryl, heteroaryl, alkylaryl, arylalkyl, heteroarylalkyl, or alkylheteroaryl;provided the compound is not 1-tert-butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine.
地址 Oakland CA US