公开(公告)号：US10981902B2

公开(公告)日：2021-04-20

申请号：US16621943

申请日：2018-06-22

Applicant: Merck Sharp & Dohme Corp. ,  MERCK R&D (CHINA) CO., LTD.

Inventor： Jianming Bao ,  Timothy J. Henderson ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Meng Na ,  Michael T. Rudd ,  David M. Tellers ,  Ling Tong

IPC: C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention is directed to 5-(pyridine-3-yl)oxaxole compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US10822338B2

公开(公告)日：2020-11-03

申请号：US15738178

申请日：2016-07-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： Amjad Ali ,  Xianhai Huang ,  Yeon-Hee Lim ,  Rongze Kuang ,  Heping Wu ,  Rajan Anand ,  Younong Yu ,  Edward Metzger ,  Michael Man-Chu Lo ,  Pauline C. Ting ,  Andrew W. Stamford ,  Paul Tempest

IPC: C07D487/04 ,  C07D491/153

Abstract: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.

公开(公告)号：US10351564B2

公开(公告)日：2019-07-16

申请号：US16176608

申请日：2018-10-31

Applicant: Merck Sharp & Dohme Corp.

Inventor： Xiaolei Gao ,  Sandra L. Knowles ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr.

IPC: C07D471/04 ,  C07D519/00 ,  C07D491/052 ,  C07D491/048 ,  C07D471/08 ,  C07F9/22 ,  A61K31/437 ,  A61P25/00

Abstract: The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US09745282B2

公开(公告)日：2017-08-29

申请号：US15197957

申请日：2016-06-30

Applicant: Merck Sharp & Dohme Corp. ,  ElexoPharm GmbH

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lina Yin ,  Rolf Hartmann ,  Qingzhong Hu ,  Ralf Heim ,  Christina Zimmer

IPC: C07D401/04 ,  A61K31/4709 ,  A61K31/4439 ,  A61K45/06 ,  C07D409/14 ,  A61K31/4725

CPC classification number: C07D401/04 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D409/14 ,  A61K2300/00

Abstract: This invention relates to indoline compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

公开(公告)号：US20160214997A1

公开(公告)日：2016-07-28

申请号：US14914843

申请日：2014-08-25

Applicant: Amjad ALI ,  Gioconda V. GALLO ,  Timothy J. HENDERSON ,  Rongze KUANG ,  Yeon-Hee LIM ,  Michael Man-Chu LO ,  Edward METZGER ,  Manuel de Lera RUIZ ,  Andrew STAMFORD ,  Paul TEMPEST ,  Brent WHITEHEAD ,  Heping WU ,  MERCK SHARP & DOHME CORP.

Inventor： Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

IPC: C07D519/00 ,  C07D491/147

CPC classification number: C07D519/00 ,  C07D491/147

Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

Abstract translation: 本发明涉及作为A2A受体拮抗剂的2,2-二氟二氧代己基化合物。 本发明还涉及本文所述的2,2-二氟二氧代环戊基化合物在涉及A2A受体的神经障碍和疾病的潜在治疗或预防中的用途。 本发明还涉及包含这些化合物的药物组合物以及这些药物组合物用于预防或治疗其中涉及A2A受体的疾病的用途。

公开(公告)号：US11230556B2

公开(公告)日：2022-01-25

申请号：US16471672

申请日：2017-12-18

Applicant: Merck Sharp & Dohme Corp.

Inventor： Xiaolei Gao ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Debra L. Ondeyka

IPC: C07D498/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D513/04 ,  C07D471/14 ,  C07D498/14 ,  C07D401/14

Abstract: The present invention is directed to 6,5-fused heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US11046714B2

公开(公告)日：2021-06-29

申请号：US14914843

申请日：2014-08-25

Applicant: Merck Sharp & Dohme Corp. ,  Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

Inventor： Ali Amjad ,  Gioconda V. Gallo ,  Timothy J. Henderson ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Edward Metzger ,  Manuel de Lera Ruiz ,  Andrew Stamford ,  Paul Tempest ,  Brent Whitehead ,  Heping Wu

IPC: C07D519/00 ,  C07D491/147

Abstract: The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of A2A receptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which A2A receptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which A2A receptors are involved.

公开(公告)号：US20190000824A1

公开(公告)日：2019-01-03

申请号：US16062500

申请日：2016-12-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： John J. Acton, III ,  Jianming Bao ,  Melissa Egbertson ,  Xiaolei Gao ,  Scott T. Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Michael T. Rudd ,  Oleg B. Selyutin ,  David M. Tellers ,  Ling Tong ,  Jenny Miu-Chun Wai

IPC: A61K31/4439 ,  A61K31/437 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

CPC classification number: A61K31/4439 ,  A61K31/437 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine 5 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US10138212B2

公开(公告)日：2018-11-27

申请号：US15549242

申请日：2016-02-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Amjad Ali ,  Rongze Kuang ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Pauline C. Ting ,  Purakkattle Biju ,  Manuel de Lera Ruiz ,  Sylvia J. Degrado ,  Alexander L. Tung ,  Timothy J. Henderson ,  Liwu Hong ,  Jae-Hun Kim ,  Dong Won-Shik Kim ,  Joe Lee ,  Jie Wu ,  Heping Wu ,  Yushi Xiao ,  Tao Yu ,  Gang Zhou ,  Xiaohong Zhu ,  Kevin D. McCormick ,  Jayaram R. Tagat ,  Dong Xiao ,  Tanweer Khan ,  Jianhua Cao ,  Michael Berlin ,  Yonglian Zhang

IPC: C07D239/84 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61P25/14 ,  A61K31/517

Abstract: The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.

公开(公告)号：US20150225365A1

公开(公告)日：2015-08-13

申请号：US14433441

申请日：2013-10-02

Applicant: Amjad ALI ,  Man-Chu Michael ,  Edward METZGER ,  Lina YIN ,  Rolf HARTMANN ,  Qingzhong HU ,  Ralf HEIM ,  Christina ZIMMER ,  MERCK SHARP & DOHME CORP. ,  ELEXOPHARM GMBH

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Edward Metzger ,  Lina Yin ,  Rolf Hartmann ,  Qingzhong Hu ,  Ralf Heim ,  Christina Zimmer

IPC: C07D401/04 ,  C07D409/14

CPC classification number: C07D401/04 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K45/06 ,  C07D409/14 ,  A61K2300/00

Abstract: This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

Abstract translation: 本发明涉及结构式I的吲哚类化合物或其药学上可接受的盐，其中变量在本文中定义。 本发明化合物选择性地抑制醛固酮合酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗改善或预防可通过抑制醛固酮合酶治疗的病症的方法。