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：US20110195933A1

公开(公告)日：2011-08-11

申请号：US13057510

申请日：2009-07-27

申请人： Jason D. Katz ,  Sandra L. Knowles ,  James P. Jewell ,  David L. Sloman ,  Matthew G. Stanton ,  Njamkou Noucti

发明人： Jason D. Katz ,  Sandra L. Knowles ,  James P. Jewell ,  David L. Sloman ,  Matthew G. Stanton ,  Njamkou Noucti

IPC分类号： A61K31/675 ,  C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  C07D413/14 ,  A61K31/5377 ,  C07D471/10 ,  A61K31/438 ,  A61K31/397 ,  C07F9/576 ,  A61K31/5513 ,  A61P25/28

CPC分类号： A61K31/425 ,  C07D417/04 ,  C07D417/14

摘要： The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明包括选择性抑制微管亲和调节激酶（MARK）的吡唑并[1,5-a]吡啶衍生物，因此可用于治疗或预防阿尔茨海默氏病。 还包括药物组合物和使用方法。

公开(公告)号：US20190315762A1

公开(公告)日：2019-10-17

申请号：US16471675

申请日：2017-12-18

申请人： Xiaolei GAO ,  Sandra L. KNOWLES ,  Chun-sing LI ,  Michael Man-Chu LO ,  Robert D. MAZZOLA, JR. ,  Ling TONG ,  Merck Sharp & Dohme Corp.

发明人： Xiaolei GAO ,  Sandra L. KNOWLES ,  Chunsing LI ,  Michael Man-Chu LO ,  Robert D. MAZZOLA, Jr. ,  Ling TONG

IPC分类号： C07D491/052 ,  C07D471/04 ,  C07D498/04 ,  C07D491/048

摘要： The present invention is directed to 6,6-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：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：US20190315708A1

公开(公告)日：2019-10-17

申请号：US16471679

申请日：2017-12-18

申请人： Jianming BAO ,  Ronald FERGUSON ,  Xiaolei GAO ,  Scott HARRISON ,  Sandra L. KNOWLES ,  Michael Man-chu LO ,  Robert D. MAZZOLA, JR. ,  Jeffrey W. SCHUBERT ,  Merck Sharp & Dohme Corp. ,  MSD R&D (CHINA) CO., LTD.

发明人： Jianming BAO ,  Ronald FERGUSON ,  Xiaolei GAO ,  Scott HARRISON ,  Sandra L. KNOWLES ,  Michael Man-Chu LO ,  Robert D. Mazzola, Jr. ,  Jeffrey W. Shubert

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D417/14 ,  C07D513/04 ,  C07D405/14 ,  C07D413/14 ,  C07D498/08 ,  C07D491/107

摘要： The present invention is directed to 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：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.

公开(公告)号：US08518911B2

公开(公告)日：2013-08-27

申请号：US13057510

申请日：2009-07-27

申请人： Jason D. Katz ,  Sandra L. Knowles ,  James P. Jewell ,  David L. Sloman ,  Matthew G. Stanton ,  Njamkou Noucti

发明人： Jason D. Katz ,  Sandra L. Knowles ,  James P. Jewell ,  David L. Sloman ,  Matthew G. Stanton ,  Njamkou Noucti

IPC分类号： A61K31/675 ,  A61K31/437 ,  A61K31/496 ,  A61K31/397

CPC分类号： A61K31/425 ,  C07D417/04 ,  C07D417/14

摘要： The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.

摘要翻译： 本发明包括选择性抑制微管亲和调节激酶（MARK）的吡唑并[1,5-a]吡啶衍生物，因此可用于治疗或预防阿尔茨海默氏病。 还包括药物组合物和使用方法。