公开(公告)号：US20150299167A1

公开(公告)日：2015-10-22

申请号：US14649299

申请日：2013-12-03

申请人： Cheol K. CHUNG ,  Mark E. SCOTT ,  Paul Gerard GER ,  Kevin Michael BELYK ,  John LIMANTO ,  Guy R. HUMPHREY ,  MERCK SHARP & DOHME CORP.

发明人： Cheol K. Chung ,  Mark E. Scott ,  Paul Gerard Bulger ,  Kevin Michael Belyk ,  John Limanto ,  Guy R. Humphrey

IPC分类号： C07D401/10

CPC分类号： C07D401/10

摘要： A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.

摘要翻译： 提供了一种用于有效制备结构式I的不对称化合物的新方法：包括铜催化的碳 - 氮交叉偶联步骤。 作为本发明一部分描述的方法可用于制备可用于治疗癌症的聚（ADP-核糖）聚合酶（PARP）抑制剂。 特别地，本发明描述了制备PARP抑制剂2- {4 - [（3S） - 哌啶-3-基]苯基} -2H-吲唑-7-甲酰胺的方法。

公开(公告)号：US20160280704A1

公开(公告)日：2016-09-29

申请号：US14778019

申请日：2014-03-19

申请人： Matthew Lloyd Childers ,  Christopher Dinsmore ,  Peter Fuller ,  David Guerin ,  Jason David Katz ,  Qinglin Pu ,  Mark E. Scott ,  Christopher F. Thompson ,  Hongjun Zhang ,  Danielle Falcone ,  Luis Torres ,  Jason Brubaker ,  Hongbo Zeng ,  Jiaqiang Cai ,  Xiaoxing Du ,  Chonggang Wang ,  Yunfeng Bai ,  Norman Kong ,  Yumei Liu ,  Zhixiang Zheng ,  Merck Sharp & Dohme Corp.

发明人： Matthew Lloyd Childers ,  Christopher Dinsmore ,  Peter Fuller ,  David Guerin ,  Jason David Katz ,  Qinglin Pu ,  Mark E. Scott ,  Christopher F. Thompson ,  Hongjun Zhang ,  Danielle Falcone ,  Luis Torres ,  Jason Brubaker ,  Hongbo Zeng ,  Jiaqiang Cai ,  Xiaoxing Du ,  Chonggang Wang ,  Yunfeng Bai ,  Norman Kong ,  Yumei Liu ,  Zhixiang Zheng

IPC分类号： C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

公开(公告)号：US20160272634A1

公开(公告)日：2016-09-22

申请号：US14778055

申请日：2014-03-19

申请人： Christopher DINSMORE ,  Peter FULLER ,  David GUERIN ,  Jason David KATZ ,  Christopher F. THOMPSON ,  Danielle FALCONE ,  Wei DENG ,  Luis TORRES ,  Hongbo ZENG ,  Yunfeng BAI ,  Jianmin FU ,  Norman KONG ,  Yumei LIU ,  Zhixiang ZHENG ,  Mark E. SCOTT ,  MERCK SHARP & DOHME CORP.

发明人： Christopher Dinsmore ,  Peter Fuller ,  David Guerin ,  Jason David Katz ,  Christopher F. Thompson ,  Danielle Falcone ,  Wei Deng ,  Luis Torres ,  Hongbo Zeng ,  Yunfeng Bai ,  Jianmin Fu ,  Norman Kong ,  Yumei Liu ,  Zhixiang Zheng ,  Mark E. Scott

IPC分类号： C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

摘要翻译： 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。

公开(公告)号：US20160272633A1

公开(公告)日：2016-09-22

申请号：US14778052

申请日：2014-03-19

申请人： Christopher DINSMORE ,  Peter FULLER ,  David GUERIN ,  Christopher F. THOMPSON ,  Qinglin PU ,  Mark E. SCOTT ,  Jason David KATZ ,  Ravi KURUKLASURIYA ,  Joshua T. CLOSE ,  Danielle FALCONE ,  Jason BRUDAKER ,  Hongbo ZENG ,  Yunfeng BAI ,  Jianmin FU ,  Norman KONG ,  Yumei LIU ,  Zhixiang ZHENG ,  MERCK SHARP & DOHME CORP.

发明人： Christopher Dinsmore ,  Peter Fuller ,  David Guerin ,  Christopher F. Thompson ,  Qinglin Pu ,  Mark E. Scott ,  Jason David Katz ,  Ravi Kuruklasuriya ,  Joshua T. Close ,  Danielle Falcone ,  Jason Brubaker ,  Hongbo Zeng ,  Yunfeng Bai ,  Jianmin Fu ,  Norman Kong ,  Yumei Liu ,  Zhixiang Zheng

IPC分类号： C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.

公开(公告)号：US20160272632A1

公开(公告)日：2016-09-22

申请号：US14778046

申请日：2014-03-19

申请人： Matthew Lloyd CHILDERS ,  Peter FULLER ,  David GUERIN ,  Jason David KATZ ,  Qinglin PU ,  Mark E. SCOTT ,  Christopher E. THOMPSON ,  Michelle MARTINEZ ,  Danielle FALCONE ,  Luis TORRES ,  Yongqi DENG ,  Ravi KURUKULASURIYA ,  Hongbo ZENG ,  Yunfeng BAI ,  Norman KONG ,  Yumei LIU ,  MERCK SHARP & DOHME CORP.

发明人： Matthew Lloyd Childers ,  Peter Fuller ,  David Guerin ,  Jason David Katz ,  Qinglin Pu ,  Mark E. Scott ,  Christopher F. Thompson ,  Michelle Martinez ,  Danielle Falcone ,  Luis Torres ,  Yongqi Deng ,  Ravi Kurukulasuriya ,  Hongbo Zeng ,  Yunfeng Bai ,  Norman Kong ,  Yumei Liu ,  Zhixiang Zheng

IPC分类号： C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

摘要翻译： 本发明提供了作为JAK抑制剂的式（I）化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。

公开(公告)号：US10435386B2

公开(公告)日：2019-10-08

申请号：US15419618

申请日：2017-01-30

申请人： Merck Sharp & Dohme Corp.

发明人： Cheol K. Chung ,  Mark E. Scott ,  Paul Gerard Bulger ,  Kevin Michael Belyk ,  John Limanto ,  Guy R. Humphrey

IPC分类号： C07D401/10

摘要： A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.

公开(公告)号：US10072025B2

公开(公告)日：2018-09-11

申请号：US15519740

申请日：2015-10-21

申请人： Merck Sharp & Dohme Corp.

发明人： Mark E. Scott ,  David Guerin ,  Danielle Molinari ,  Sam Kattar ,  Peter Fuller ,  Christopher Dinsmore ,  Norman Kong ,  Yunfeng Bai ,  Jianmin Fu ,  Yumei Liu ,  Zhixiang Zheng

IPC分类号： C07D519/00 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61K31/541

CPC分类号： C07D519/00 ,  A61K31/00 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P11/06 ,  A61P19/02 ,  A61P35/00 ,  C07D471/04

摘要： The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.

公开(公告)号：US09957265B2

公开(公告)日：2018-05-01

申请号：US14778052

申请日：2014-03-19

申请人： Merck Sharp & Dohme Corp.

发明人： Christopher Dinsmore ,  Peter Fuller ,  David Guerin ,  Christopher F. Thompson ,  Qinglin Pu ,  Mark E. Scott ,  Jason David Katz ,  Ravi Kurukulasuriya ,  Joshua T. Close ,  Danielle Falcone ,  Jason Brubaker ,  Hongbo Zeng ,  Yunfeng Bai ,  Jianmin Fu ,  Norman Kong ,  Yumei Liu ,  Zhixiang Zheng

IPC分类号： C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.

公开(公告)号：US10815214B2

公开(公告)日：2020-10-27

申请号：US16576133

申请日：2019-09-19

申请人： Merck Sharp & Dohme Corp.

发明人： Cheol K. Chung ,  Mark E. Scott ,  Paul G. Bulger ,  Kevin M. Belyk ,  John Limanto ,  Guy R. Humphrey

IPC分类号： C07D401/10

摘要： A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.

公开(公告)号：US10344000B2

公开(公告)日：2019-07-09

申请号：US15770255

申请日：2016-10-27

申请人： Merck Sharp & Dohme Corp.

发明人： Blair T. Lapointe ,  Peter H. Fuller ,  Hakan Gunaydin ,  Kun Liu ,  Danielle F. Molinari ,  Qinglin Pu ,  Mark E. Scott ,  B. Wesley Trotter ,  Hongjun Zhang

IPC分类号： C07D231/56 ,  C07D401/04 ,  C07D491/052 ,  C07D491/107 ,  A61P19/02 ,  A61P17/06 ,  A61P29/00 ,  A61P37/02 ,  A61P11/06 ,  C07D471/04

摘要： The present invention relates to compounds according to Formula I: and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.