公开(公告)号：US10329289B2

公开(公告)日：2019-06-25

申请号：US15386009

申请日：2016-12-21

申请人： Jianming Bao ,  Xiaolei Gao ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Debra L. Ondeyka ,  Andrew W. Stamford ,  Fengqi Zhang

发明人： Jianming Bao ,  Xiaolei Gao ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Debra L. Ondeyka ,  Andrew W. Stamford ,  Fengqi Zhang

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

摘要： 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：US11149036B2

公开(公告)日：2021-10-19

申请号：US16621959

申请日：2018-06-22

申请人： John J. Acton, III ,  Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co., Ltd. ,  Jianming Bao ,  Qiaolin Deng ,  Melissa Egbertson ,  Ronald Ferguson, II ,  Xiaolei Gao ,  Scott Timothy Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Meng Na ,  Michael T. Rudd ,  Oleg Selyutin ,  David M. Tellers ,  Ling Tong ,  Fengqi Zhang

发明人： John J. Acton, III ,  Jianming Bao ,  Qiaolin Deng ,  Melissa Egbertson ,  Ronald Ferguson, II ,  Xiaolei Gao ,  Scott Timothy Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Meng Na ,  Michael T. Rudd ,  Oleg Selyutin ,  David M. Tellers ,  Ling Tong ,  Fengqi Zhang

IPC分类号： C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D491/048 ,  C07D498/04

摘要： 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 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：US20160108048A1

公开(公告)日：2016-04-21

申请号：US14895406

申请日：2014-06-02

申请人： Craig A. COBURN ,  Milana MALETIC ,  Yunfu LUO ,  Zhiqi QI ,  Chunsing LI ,  Tingting YU ,  Richard SOLL ,  MERCK SHARP & DOHME CORP.

发明人： Craig A. Coburn ,  Milana Maletic ,  Yunfu Luo ,  Zhiqi Qi ,  Chunsing Li ,  Tingting Yu ,  Richard Soll

IPC分类号： C07D487/04 ,  A61K31/4545 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/4985 ,  A61K45/06 ,  A61K31/496 ,  A61K31/551 ,  C07D405/14 ,  C07D401/06 ,  C07D413/14 ,  C07D401/14 ,  A61K31/454

CPC分类号： C07D487/04 ,  A61K31/4375 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/513 ,  A61K31/5365 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04 ,  A61K2300/00

摘要： The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.

摘要翻译： 本发明涉及式（I）的咪唑衍生物及其药学上可接受的盐，其中A，B，Y，R 1和R 2如本文所定义。 本发明还涉及包含至少一种咪唑衍生物的组合物，以及使用咪唑衍生物抑制CYP450A 3A的方法。 CYP450 3A的抑制可用于改善由CYP450 3A4代谢的药物的药代动力学。

公开(公告)号：US20200207758A1

公开(公告)日：2020-07-02

申请号：US16621959

申请日：2018-06-22

申请人： John J. ACTON, III ,  Jianming BAO ,  Qiaolin DENG ,  Melissa EGBERTSON ,  Ronald FERGUSON, II ,  Xiaolei GAO ,  Scott Timothy HARRISON ,  Sandra L. KNOWLES ,  Chunsing LI ,  Michael Man-Chu LO ,  Robert D. MAZZOLA, Jr. ,  Zhaoyang MENG ,  Meng NA ,  Michael T. RUDD ,  Oleg SELYUTIN ,  David M. TELLERS ,  Ling TONG ,  Fengqi ZHANG

发明人： John J. ACTON, III ,  Jianming BAO ,  Qiaolin DENG ,  Melissa EGBERTSON ,  Ronald FERGUSON, II ,  Xiaolei GAO ,  Scott Timothy HARRISON ,  Sandra L. KNOWLES ,  Chunsing LI ,  Michael Man-Chu LO ,  Robert D. MAZZOLA, Jr. ,  Zhaoyang MENG ,  Meng NA ,  Michael T. RUDD ,  Oleg SELYUTIN ,  David M. TELLERS ,  Ling TONG ,  Fengqi ZHANG

IPC分类号： C07D471/04 ,  C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  C07D405/14 ,  C07D491/048 ,  C07D498/04

摘要： 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 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：US20170183342A1

公开(公告)日：2017-06-29

申请号：US15386009

申请日：2016-12-21

申请人： JIANMING BAO ,  XIAOLEI GAO ,  SANDRA L. KNOWLES ,  CHUNSING LI, I ,  MICHAEL MAN-CHU LO ,  ROBERT D. MAZZOLA, Jr. ,  DEBRA L. ONDEYKA ,  ANDREW W. STAMFORD ,  FENGQI ZHANG

发明人： JIANMING BAO ,  XIAOLEI GAO ,  SANDRA L. KNOWLES ,  CHUNSING LI, I ,  MICHAEL MAN-CHU LO ,  ROBERT D. MAZZOLA, Jr. ,  DEBRA L. ONDEYKA ,  ANDREW W. STAMFORD ,  FENGQI ZHANG

IPC分类号： C07D471/04 ,  C07D491/048 ,  C07D491/052 ,  C07D471/08

CPC分类号： C07D471/04 ,  C07D471/08 ,  C07D491/048 ,  C07D491/052 ,  C07D519/00 ,  C07F9/222 ,  C07F9/6561

摘要： 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.