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1. 发明申请

US20120065154A1 Pyrazolo Pyrimidine Derivatives and Methods of Use Thereof 审中-公开
标题翻译：吡唑并嘧啶衍生物及其使用方法
公开(公告)号：US20120065154A1
公开(公告)日：2012-03-15
申请号：US13016957
申请日：2011-01-28
申请人： Masahiro Tanaka , Chao Zhang , Kevan M. Shokat , Alma L. Burlingame , Kirk Hansen , Raynard L. Bateman , Stephen G. DiMagno
发明人： Masahiro Tanaka , Chao Zhang , Kevan M. Shokat , Alma L. Burlingame , Kirk Hansen , Raynard L. Bateman , Stephen G. DiMagno
IPC分类号： A61K31/704 , A61K31/519 , A61K31/52 , A61P35/00 , C12Q1/18 , A61P29/00 , A61P3/00 , A61P3/10 , A61P3/04 , C07D487/04 , A61P35/02
CPC分类号： C07D487/04
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.
摘要翻译：本发明一般涉及用作特别是NAD（P）（H）依赖性氧化还原酶的短链脱氢酶/还原酶（SDR）家族的抑制剂的吡唑并嘧啶衍生物。更具体地，本发明涉及吡唑并嘧啶衍生物，包括SDR抑制剂的衍生物和类似物，含有SDR抑制剂的衍生物和类似物的药物组合物，制备SDR抑制剂的衍生物和类似物的方法及其使用方法。

2. 发明申请

US20090181988A1 Pyrazolo Pyrimidine Derivatives and Methods of Use Thereof 审中-公开
标题翻译：吡唑并嘧啶衍生物及其使用方法
公开(公告)号：US20090181988A1
公开(公告)日：2009-07-16
申请号：US12194469
申请日：2008-08-19
申请人： Masahiro Tanaka , Chao Zhang , Kevan M. Shokat , Alma L. Burlingame , Kirk Hansen , Raynard L. Bateman , Stephen G. DiMagno
发明人： Masahiro Tanaka , Chao Zhang , Kevan M. Shokat , Alma L. Burlingame , Kirk Hansen , Raynard L. Bateman , Stephen G. DiMagno
IPC分类号： A61K31/522 , C12Q1/02 , C07D473/34 , A61K31/519 , C07D473/30 , A61K31/52 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04
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.
摘要翻译：本发明一般涉及用作特别是NAD（P）（H）依赖性氧化还原酶的短链脱氢酶/还原酶（SDR）家族的抑制剂的吡唑并嘧啶衍生物。更具体地，本发明涉及吡唑并嘧啶衍生物，包括SDR抑制剂的衍生物和类似物，含有SDR抑制剂的衍生物和类似物的药物组合物，制备SDR抑制剂的衍生物和类似物的方法及其使用方法。

3. 发明授权

US07429596B2 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof 有权
标题翻译： 1H-吡咯并[2,3-D]嘧啶衍生物及其使用方法
公开(公告)号：US07429596B2
公开(公告)日：2008-09-30
申请号：US10871732
申请日：2004-06-18
申请人： Masahiro Tanaka , Chao Zhang , Kevan M. Shokat , Alma L. Burlingame , Kirk Hansen , Raynard L. Bateman , Stephen G. DiMagno
发明人： Masahiro Tanaka , Chao Zhang , Kevan M. Shokat , Alma L. Burlingame , Kirk Hansen , Raynard L. Bateman , Stephen G. DiMagno
IPC分类号： C07D487/04 , C07D413/06 , A61K31/519 , A61K31/675 , A61K31/662 , A61K31/497 , A61K31/5355 , C07F9/38 , A61P35/04 , A61P35/02
CPC分类号： C07D487/04
摘要： This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention further relates to pharmaceutical compositions and methods of preventing or treating disease with 1H-Pyrrolo[2.3-d]pyrimidine derivatives. More specifically, the invention relates to a 1H-Pyrrolo[2.3-d]pyrimidine which is a compound of Formula I or II: or a pharmaceutically-acceptable salt or prodrug thereof; wherein: Y is N or CR5; Z is NR3R4, halo, H, OH, alkyl, alkyloxy, or haloalkyl; and R1a is indolyl, thiazolyl, benzyl, biphenylyl, thiophenyl, pyrrolyl, or phenyl, wherein said phenyl is substituted with at least one of OH, —NR3R4, —C(═O)NR6R7, —CN, NO2—C(═O)OH, —C(═O)O-alkyl, (C1-C4)alkyl, halo, haloalkyl or haloaryl; and wherein said indolyl, thiazolyl, benzyl, biphenylyl, thiophenyl, or pyrrolyl is optionally substituted with OH, —NR3R4, —C(═O)NR6R7, —CN, NO2, —C(═O)O—R3, (C1-C4)alkyl, halo, haloalkyl or haloaryl.
摘要翻译：本发明一般涉及可用作NAD（P）（H）依赖性氧化还原酶的短链脱氢酶/还原酶（SDR）家族的抑制剂的吡唑并嘧啶衍生物。本发明还涉及用1H-吡咯并[2,3-d]嘧啶衍生物预防或治疗疾病的药物组合物和方法。更具体地，本发明涉及作为式I或II化合物的1H-吡咯并[2,3-d]嘧啶或其药学上可接受的盐或前药; 其中：Y是N或CR 5; Z是NR 3 R 4，卤素，H，OH，烷基，烷氧基或卤代烷基; 并且R 1a是吲哚基，噻唑基，苄基，联苯基，噻吩基，吡咯基或苯基，其中所述苯基被OH，-NR 3 R 3中的至少一个取代， -C（-O）NR 6 R 7，-CN，NO 2 -C（-O（O））OH，-C（-O）O-烷基，（C 1 -C 4 -C 4）烷基，卤素，卤代烷基或卤代芳基; 并且其中所述吲哚基，噻唑基，苄基，联苯基，噻吩基或吡咯基任选被OH，-NR 3 R 4，-C（ - ）NR -C（O）OR 3，-C（-O）OR 3，（C 1 -C 6） C 1 -C 4烷基，卤素，卤代烷基或卤代芳基。

4. 发明申请

US20050085472A1 Pyrazolo pyrimidine derivatives and methods of use thereof 有权
标题翻译：吡唑并嘧啶衍生物及其使用方法
公开(公告)号：US20050085472A1
公开(公告)日：2005-04-21
申请号：US10871732
申请日：2004-06-18
申请人： Masahiro Tanaka , Chao Zhang , Kevan Shokat , Alma Burlingame , Kirk Hansen , Raynard Bateman , Stephen DiMagno
发明人： Masahiro Tanaka , Chao Zhang , Kevan Shokat , Alma Burlingame , Kirk Hansen , Raynard Bateman , Stephen DiMagno
IPC分类号： A61K20060101 , A61K31/519 , A61K31/5377 , A61P35/00 , C07D487/02 , C07D487/04
CPC分类号： C07D487/04
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.
摘要翻译：本发明一般涉及用作特别是NAD（P）（H）依赖性氧化还原酶的短链脱氢酶/还原酶（SDR）家族的抑制剂的吡唑并嘧啶衍生物。更具体地，本发明涉及吡唑并嘧啶衍生物，包括SDR抑制剂的衍生物和类似物，含有SDR抑制剂的衍生物和类似物的药物组合物，制备SDR抑制剂的衍生物和类似物的方法及其使用方法。

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