公开(公告)号：US20170015633A1

公开(公告)日：2017-01-19

申请号：US15107233

申请日：2014-12-17

申请人： Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co. Ltd.

发明人： Dong Ming Shen ,  Melissa Egbertson ,  Richard Berger ,  XiaoXia Qian ,  Yimin Qian ,  Bart Harper ,  Meng Yang ,  Zack Zhi Qiang Guo ,  Vanessa L. Rada ,  Deping Wang ,  Timothy A. Cernak ,  Christopher Sinz ,  Ming Wang ,  Jonathan E. Wilson ,  Shimin Xu

IPC分类号： C07D239/36 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D487/04 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D401/06 ,  C07D403/12

CPC分类号： C07D239/36 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D487/04

摘要： Disclosed are pyrimidine carboxamide compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2), pharmaceutical compositions and uses thereof.

摘要翻译： 公开了式（I）的嘧啶羧酰胺化合物，其可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病，药物组合物及其用途的治疗剂。

公开(公告)号：US09815796B2

公开(公告)日：2017-11-14

申请号：US15107233

申请日：2014-12-17

申请人： Merck Sharp & Dohme Corp. ,  MSD R & D (China) Co. Ltd.

发明人： Dong Ming Shen ,  Melissa Egbertson ,  Richard Berger ,  XiaoXia Qian ,  Yimin Qian ,  Bart Harper ,  Meng Yang ,  Zack Zhiqiang Guo ,  Vanessa L. Rada ,  Deping Wang ,  Timothy A. Cernak ,  Christopher Sinz ,  Ming Wang ,  Jonathan E. Wilson ,  Shimin Xu

IPC分类号： C07D239/36 ,  C07D401/12 ,  C07D401/06 ,  C07D403/04 ,  C07D403/14 ,  C07D487/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D403/12 ,  C07D403/06

CPC分类号： C07D239/36 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D487/04

摘要： Disclosed are pyrimidine carboxamide compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2), pharmaceutical compositions and uses thereof.

公开(公告)号：US20200231606A1

公开(公告)日：2020-07-23

申请号：US16326408

申请日：2017-08-24

申请人： Merck Sharp & Dohme Corp.

发明人： Kun Liu ,  Abdelghani Achab ,  Purakkattle Biju ,  Timothy A. Cernak ,  Yongqi Deng ,  Xavier Fradera ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Joseph Kozlowski ,  Derun Li ,  Guoqing Li ,  Qinglin Pu ,  Zhi-Cai Shi ,  Wensheng Yu ,  Hongjun Zhang

IPC分类号： C07F5/02 ,  C07D271/08 ,  C07D413/12

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20160304537A1

公开(公告)日：2016-10-20

申请号：US15103148

申请日：2014-12-05

申请人： Xiaoqing HAN ,  Alan WHITEHEAD ,  Subharekha RAGHAVAN ,  Timothy A. CERNAK ,  Spencer DREHER ,  Jonathan GROEPER ,  Jian GUO ,  Yong ZHANG ,  MERCK SHARP & DOHME CORP.

发明人： Xiaoqing Han ,  Alan Whitehead ,  Subharekha Raghavan ,  Timothy A. Cernak ,  Spencer Dreher ,  Jonathan Groeper ,  Jian Guo ,  Yong Zhang

IPC分类号： C07D519/00 ,  A61K45/06 ,  A61K31/519

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06 ,  C07B2200/05 ,  A61K2300/00

摘要： A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.

公开(公告)号：US09783552B2

公开(公告)日：2017-10-10

申请号：US15103148

申请日：2014-12-05

申请人： MERCK SHARP & DOHME CORP.

发明人： Xiaoqing Han ,  Alan Whitehead ,  Subharekha Raghavan ,  Timothy A. Cernak ,  Spencer Dreher ,  Jonathan Groeper ,  Jian Guo ,  Yong Zhang

IPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06 ,  C07B2200/05 ,  A61K2300/00

摘要： A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.

公开(公告)号：US09511052B2

公开(公告)日：2016-12-06

申请号：US14415210

申请日：2013-07-15

申请人： Merck Sharp & Dohme Corp.

发明人： Timothy A. Cernak ,  Kevin D. Dykstra ,  Dong-Ming Shen ,  Kun Liu ,  Andrew Stamford ,  John Qiang Tan

IPC分类号： C07D231/56 ,  A61K31/416 ,  A61K45/06

CPC分类号： A61K31/416 ,  A61K45/06 ,  C07D231/56 ,  A61K2300/00

摘要： The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.

公开(公告)号：US10988487B2

公开(公告)日：2021-04-27

申请号：US16326408

申请日：2017-08-24

申请人： Merck Sharp & Dohme Corp.

发明人： Kun Liu ,  Abdelghani Achab ,  Purakkattle Biju ,  Timothy A. Cernak ,  Yongqi Deng ,  Xavier Fradera ,  Liangqin Guo ,  Yongxin Han ,  Shuwen He ,  Joseph Kozlowski ,  Derun Li ,  Guoqing Li ,  Qinglin Pu ,  Zhi-Cai Shi ,  Wensheng Yu ,  Hongjun Zhang

IPC分类号： C07F5/02 ,  C07D271/08 ,  C07D413/12

摘要： Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US20150182503A1

公开(公告)日：2015-07-02

申请号：US14415210

申请日：2013-07-15

申请人： Merck Sharp & Dohme Corp.

发明人： Timothy A. Cernak ,  Kevin D. Dykstra ,  Dong-Ming Shen ,  Kun Liu ,  Andrew Stamford ,  John Qiang Tan

IPC分类号： A61K31/416 ,  C07D231/56

CPC分类号： A61K31/416 ,  A61K45/06 ,  C07D231/56 ,  A61K2300/00

摘要： The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.

摘要翻译： 本发明涉及可用于治疗醛固酮介导的疾病的式I化合物及其药学上可接受的盐。 本发明还涉及该化合物的具体非对映异构体和对映异构体，制备式I化合物的方法，以及其用于治疗和预防上述疾病和用于制备用于此目的的药物的潜在用途，以及药物组合物 其包含式I的化合物。