Sandra V Knowles

US Patent:

20210380580, Dec 9, 2021

Filed:

Jun 22, 2018

Appl. No.:

16/621953

Inventors:

- Rahway NJ, US
- SHANGHAI, CN
Qiaolin DENG - Princeton NJ, US
Melissa EGBERTSON - Ambler PA, US
Ronald FERGUSON, II - Scotch Plains NJ, US
Xiaolei GAO - Bridgewater NJ, US
Scott Timothy HARRISON - Elkins Park PA, US
Timothy J. HENDERSON - Natick MA, US
Sandra L. KNOWLES - Princeton NJ, US
Chunsing LI - Shanghai, CN
Michael Man-Chu LO - Bedminster NJ, US
Meng NA - Shanghai, CN
Michael T. RUDD - Collegeville PA, US
Oleg B. Selyutin - West Windsor NJ, US
David M. TELLERS - Lansdale PA, US
Ling TONG - Warren NJ, US
Fengqi ZHANG - Edison NJ, US
Takao SUZUKI - Shanghai, CN

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ
MSD R&D (CHINA) CO., LTD. - SHANGHAI

International Classification:

C07D 471/04
C07D 401/14
C07D 417/14
C07D 413/14
C07D 487/04
C07D 405/14

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 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.

US Patent:

20200095261, Mar 26, 2020

Filed:

Dec 18, 2017

Appl. No.:

16/471672

Inventors:

- Rahway NJ, US
Sandra L. KNOWLES - Princeton NJ, US
Chunsing LI - Shanghai, CN
Michael Man-Chu LO - Bedminster NJ, US
Debra L. ONDEYKA - Fanwood NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 498/14
C07D 487/04
C07D 471/04
C07D 513/04
C07D 401/14
C07D 491/048

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.

US Patent:

20190315708, Oct 17, 2019

Filed:

Dec 18, 2017

Appl. No.:

16/471679

Inventors:

Jianming BAO - Shanghai, CN
Ronald FERGUSON - Rahway NJ, US
Xiaolei GAO - Bridgewater NJ, US
Scott HARRISON - West Point PA, US
Sandra L. KNOWLES - Kenilworth NJ, US
Michael Man-chu LO - Kenilworth NJ, US
Jeffrey W. SCHUBERT - West Point PA, US
- Rahway NJ, US
- Shanghai, CN

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 401/04
C07D 401/14
C07D 417/14
C07D 513/04
C07D 405/14
C07D 413/14
C07D 498/08
C07D 491/107

Abstract:

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.

US Patent:

20190315762, Oct 17, 2019

Filed:

Dec 18, 2017

Appl. No.:

16/471675

Inventors:

Xiaolei GAO - Bridgewater NJ, US
Sandra L. KNOWLES - Rahway NJ, US
Chun-sing LI - Shanghai, CN
Michael Man-Chu LO - Kenilworth NJ, US
Ling TONG - Rahway NJ, US
- Rahway NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 491/052
C07D 471/04
C07D 498/04
C07D 491/048

Abstract:

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.

US Patent:

20190062331, Feb 28, 2019

Filed:

Oct 31, 2018

Appl. No.:

16/176608

Inventors:

- Rahway NJ, US
XIAOLEI GAO - BRIDGEWATER NJ, US
SANDRA L. KNOWLES - PRINCETON NJ, US
CHUNSING LI, I - SHANGHAI, CN
MICHAEL MAN-CHU LO - BEDMINSTER NJ, US
DEBRA L. ONDEYKA - FANWOOD NJ, US
ANDREW W. STAMFORD - CHATHAM NJ, US
FENGQI ZHANG - EDISON NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 471/04
C07F 9/22
C07D 519/00
C07D 491/048
C07D 471/08
C07D 491/052

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.

US Patent:

20170183342, Jun 29, 2017

Filed:

Dec 21, 2016

Appl. No.:

15/386009

Inventors:

JIANMING BAO - SHANGHAI, CN
XIAOLEI GAO - BRIDGEWATER NJ, US
SANDRA L. KNOWLES - PRINCETON NJ, US
CHUNSING LI, I - SHANGHAI, CN
MICHAEL MAN-CHU LO - BEDMINSTER NJ, US
DEBRA L. ONDEYKA - FANWOOD NJ, US
ANDREW W. STAMFORD - CHATHAM NJ, US
FENGQI ZHANG - EDISON NJ, US

International Classification:

C07D 471/04
C07D 491/048
C07D 491/052
C07D 471/08

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.

US Patent:

20160185764, Jun 30, 2016

Filed:

Aug 18, 2014

Appl. No.:

14/912233

Inventors:

- Rahway NJ, US
Fengqi Zhang - Edison NJ, US
Guizhen Dong - Dayton NJ, US
Sandra Lee Knowles - Princeton NJ, US
Milana Maletic - Summit NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 405/14
A61K 31/444
A61K 45/06
C07D 405/06
A61K 31/443

Abstract:

The present invention relates to bicyclic himbacine derivatives of the formulaand the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.