公开(公告)号：US20180105518A1

公开(公告)日：2018-04-19

申请号：US15562617

申请日：2016-04-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Craig A. Stump ,  Yi Heng Chen ,  Ping Liu ,  Dongfang Meng ,  Jane Yang Wu ,  Chun Sing Li ,  Zhiqi Qi

IPC: C07D471/04 ,  C07D417/12 ,  C07D487/04 ,  C07D403/12 ,  A61P25/00 ,  A61P35/00 ,  A61P9/10 ,  A61P17/06 ,  A61P7/02

CPC classification number: C07D471/04 ,  A61P7/02 ,  A61P9/10 ,  A61P17/06 ,  A61P25/00 ,  A61P35/00 ,  C07D403/12 ,  C07D417/12 ,  C07D473/04 ,  C07D487/04

Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

公开(公告)号：US20180009796A1

公开(公告)日：2018-01-11

申请号：US15104537

申请日：2015-01-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： Richard Berger ,  Timothy A. Blizzard ,  Brian T. Campbell ,  Helen Y. Chen ,  John S. Debenham ,  Sunita V. Dewnani ,  Byron Dubois ,  Candido Gude ,  Zack Zhiqiang Guo ,  Bart Harper ,  Zhiyong Hu ,  Songnian Lin ,  Ping Liu ,  Ming Wang ,  Feroze Ujjainwalla ,  Jiayi Xu ,  Libo Xu ,  Rui Zhang

IPC: C07D413/14 ,  C07D417/14 ,  C07D413/12 ,  C07D471/04 ,  C07D401/12

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04

Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

公开(公告)号：US09018224B2

公开(公告)日：2015-04-28

申请号：US14358241

申请日：2012-11-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott Edmondson ,  Zhiyong Hu ,  Ping Liu ,  Gregori J. Morriello ,  Jason W. Szewczyk ,  Bowei Wang ,  Liping Wang ,  Harold B. Wood ,  Cheng Zhu ,  Yuping Zhu ,  Zhiqiang Guo

IPC: A01N43/54 ,  A61K31/505 ,  C07D513/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D239/42 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12

CPC classification number: C07D513/04 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 披露式（I）的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。

公开(公告)号：US11312719B2

公开(公告)日：2022-04-26

申请号：US16695367

申请日：2019-11-26

Applicant: Merck Sharp & Dohme Corp.

Inventor： Matthew A. Larsen ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Elisabeth Hennessy ,  Andrew J. Hoover ,  Ping Liu ,  Kun Liu ,  Umar Faruk Mansoor ,  Jianping Pan ,  Christopher W. Plummer ,  Aaron Sather ,  Uma Swaminathan ,  Huijun Wang ,  Yonglian Zhang

IPC: C07D487/04 ,  C07K16/28

Abstract: In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US20180353507A1

公开(公告)日：2018-12-13

申请号：US15780462

申请日：2016-12-13

Applicant: Merck Sharp & Dohme Corp.

Inventor： David E. Kelley ,  Ping Liu ,  Harold B. Wood ,  Scott D. Edmondson ,  Hideo Makimura ,  Xiaoyan Li ,  Timothy Joseph Kowalski

IPC: A61K31/506 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61P1/18

CPC classification number: A61K31/506 ,  A61K31/00 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61P1/18 ,  C12Q1/02 ,  G01N33/74 ,  G01N2333/726 ,  G01N2800/042

Abstract: Use of a GPR119 agonist in the prevention or treatment of hypoglycemia is disclosed, addition, pharmaceutical compositions and combinations of a GPR1 19 agonist with insulin, insulin analog, insulin secretagogue or or other drug(s) that reduces plasma glucose levels to below 70 mg/dL described herein.

公开(公告)号：US10000501B2

公开(公告)日：2018-06-19

申请号：US15513852

申请日：2015-09-23

Applicant: MERCK SHARP & DOHME CORP. ,  MSD R&D (CHINA) CO., LTD.

Inventor： Jiaqiang Cai ,  Vincent Colandrea ,  Alejandro Crespo ,  John Debenham ,  Xiaoxing Du ,  Deodialsingh Guiadeen ,  Ping Liu ,  Rongqiang Liu ,  Christina B. Madsen-Duggan ,  Joshua G. McCoy ,  Weiguo Quan ,  Christopher Sinz ,  Liping Wang

IPC: C07D491/052 ,  C07D221/22 ,  C07D417/06 ,  C07D471/04 ,  C07D215/56

CPC classification number: C07D491/052 ,  C07D215/56 ,  C07D221/22 ,  C07D417/06 ,  C07D471/04

Abstract: The present invention concerns a compound of formula I or a pharmaceutically acceptable salt thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

公开(公告)号：US09969752B2

公开(公告)日：2018-05-15

申请号：US15514536

申请日：2015-09-23

Applicant: MERCK SHARP & DOHME CORP. ,  MSD R&D (CHINA) CO., LTD.

Inventor： Jiaqiang Cai ,  Alejandro Crespo ,  Xiaoxing Du ,  Byron Gabriel Dubois ,  Deodialsingh Guiadeen ,  Shankaran Kothandaraman ,  Ping Liu ,  Rongqiang Liu ,  Weiguo Quan ,  Christopher Sinz ,  Liping Wang

IPC: C07D471/06 ,  C07D498/06 ,  C07D513/06 ,  C07D498/16

CPC classification number: C07D513/06 ,  C07D471/04 ,  C07D471/06 ,  C07D498/04 ,  C07D498/06 ,  C07D498/16 ,  C07D513/04

Abstract: The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

公开(公告)号：US09862716B2

公开(公告)日：2018-01-09

申请号：US15129206

申请日：2015-03-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Yi-Heng Chen ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Swati P. Mercer ,  Keith P. Moore ,  Ping Liu ,  Harold B. Wood ,  Chun Sing Li ,  Qinghua Mao ,  Douglas C. Beshore

IPC: C07D471/04 ,  C07D513/04

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

公开(公告)号：US20170158698A1

公开(公告)日：2017-06-08

申请号：US15128782

申请日：2015-03-23

Applicant: Helen MITCHELL ,  Mark E. FRALEY ,  Andrew J. COOKE ,  Craig A. STUMP ,  Xu-Fang ZHANG ,  Casey C. MCCOMAS ,  Kathy SCHIRRIPA ,  Melody MCWHERTER ,  Ping LIU ,  Dann PARKER ,  Chun Sing LI ,  Qinghua MAO ,  Merck Sharp & Dohme Corp.

Inventor： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Ping Liu ,  Dann Parker ,  Chun Sing Li ,  Qinghua Mao

IPC: C07D487/04 ,  C07D231/40 ,  C07D417/12 ,  C07D401/04 ,  C07D417/14 ,  C07D471/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D277/46 ,  C07D403/14

CPC classification number: C07D487/04 ,  C07D231/40 ,  C07D277/46 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

公开(公告)号：US20170114071A1

公开(公告)日：2017-04-27

申请号：US15128689

申请日：2015-03-23

Applicant: Merck Sharp & Dohme Corp. ,  MSD R & D (China) Co., LTD.

Inventor： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Yi- Heng Chen ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Swati P. Mercer ,  Kerim Babaoglu ,  Dongfang Meng ,  Jane Wu ,  Ping Liu ,  Harold B. Wood ,  Jianming Bao ,  Chun Sing Li ,  Qinghua Mao ,  Zhiqi Qi

IPC: C07D491/107 ,  C07D403/12 ,  C07D401/12 ,  C07C233/66 ,  C07D417/12 ,  C07D239/42 ,  C07D401/04 ,  C07D413/12 ,  C07D417/14 ,  C07D401/14 ,  C07D405/12 ,  C07D413/14 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D401/06 ,  C07D413/06 ,  C07D403/06 ,  C07D213/75

CPC classification number: C07D491/107 ,  C07C233/66 ,  C07D213/75 ,  C07D231/12 ,  C07D239/42 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.