Lin Yan

US Patent:

7659294, Feb 9, 2010

Filed:

Oct 18, 2005

Appl. No.:

11/665046

Inventors:

Jeffrey John Hale - Westfield NJ, US
Lin Yan - East Brunswick NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/4245
C07D 271/10
C07D 413/10

US Classification:

514364, 548125, 548131, 548240, 548251, 548255, 5462681, 5462684, 5462694, 544224, 544242, 544336, 514361, 514378, 514381, 514385

Abstract:

The present invention encompasses compounds of Formula I:.

US Patent:

7999107, Aug 16, 2011

Filed:

Jan 16, 2008

Appl. No.:

12/009114

Inventors:

John S. Debenham - Scotch Plains NJ, US
Jeffrey J. Hale - Westfield NJ, US
Pei Huo - Millburn NJ, US
Thomas F. Walsh - Watchung NJ, US
Lin Yan - East Brunswick NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 491/052
A61K 31/436

US Classification:

546115, 546116, 514302

Abstract:

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

US Patent:

8119806, Feb 21, 2012

Filed:

Jul 27, 2009

Appl. No.:

12/509698

Inventors:

Amjad Ali - Freehold NJ, US
Iyassu K. Sebhat - Jersey City NJ, US
Christopher L. Franklin - Quincy MA, US
Kathleen M. Rupprecht - Cranford NJ, US
Robert K. Baker - Cranford NJ, US
Ravi P. Nargund - East Brunswick NJ, US
Lin Yan - East Brunswick NJ, US
Pei Huo - Millburn NJ, US
Nicoletta Almirante - Milan, IT
Stefano Biondi - Pero, IT
Massimiliano Ferrario - Ceriano Laghetto, IT
Alessia Nicotra - Grandate, IT

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/4355
C07D 491/048

US Classification:

546115, 514302

Abstract:

A compound having the structure.

US Patent:

8354394, Jan 15, 2013

Filed:

Oct 22, 2010

Appl. No.:

13/504581

Inventors:

Amjad Ali - Freehold NJ, US
Christopher Franklin - Quincy MA, US
Ravi Nargund - East Brunswick NJ, US
Michael Man-Chu Lo - Edison NJ, US
Lin Yan - East Brunswick NJ, US
Pei Huo - Millburn NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/655
C07D 491/06
A61P 9/12

US Classification:

514149, 514869, 534551, 534556

Abstract:

A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

US Patent:

8361994, Jan 29, 2013

Filed:

Mar 5, 2012

Appl. No.:

13/412032

Inventors:

Amjad Ali - Freehold NJ, US
Michael Man-Chu Lo - Edison NJ, US
Zhiqiang Guo - Morganville NJ, US
Brent Whitehead - Piscataway NJ, US
Timothy J. Henderson - Edison NJ, US
Lin Yan - East Brunswick NJ, US
Shrenik K. Shah - Metuchen NJ, US

Assignee:

Merck Sharp & Dohme Corp - Rahway NJ

International Classification:

C07D 205/04
C07D 207/12
C07D 211/44
C07D 309/10
C07D 401/02
C07D 401/04
C07D 401/14
C07D 403/02
A61K 31/655
A61P 9/12

US Classification:

514149, 534551, 534556

Abstract:

A compound having the structure.

US Patent:

8377911, Feb 19, 2013

Filed:

Sep 20, 2010

Appl. No.:

13/500509

Inventors:

Amjad Ali - Freehold NJ, US
Michael Man-Chu Lo - Edison NJ, US
Lin Yan - East Brunswick NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/655
C07D 471/06

US Classification:

514149, 514869, 534556

Abstract:

A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

US Patent:

8623846, Jan 7, 2014

Filed:

May 16, 2011

Appl. No.:

13/698444

Inventors:

Amjad Ali - Freehold NJ, US
Lin Yan - East Brunswick NJ, US
Pei Huo - Millburn NJ, US
Ravi Nargund - East Brunswick NJ, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A61K 31/655
C07C 245/02
C09B 44/02

US Classification:

514150, 534556, 534574

Abstract:

A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein Ris hydrogen, deuterium, —OH, —OCalkyl, or halogen; Ris hydrogen, deuterium, or Calkyl; Rand Rare independently hydrogen, —Calkyl, —OH, —OCalkyl, or halogen; Rand Rare independently —Calkyl, —(CH)OH, or —OCalkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or —Calkyl; R15 is —C(O)OH, —C(O)OCHCHNCH)wherein n is 0, 1 or 2, —C(O)NHCH(R)OR, or —C(O)NHCH(R)C(O)NHCH(R)C(O)OR; Ris hydrogen, Calkyl, or (CH)NRRR; R, R, R, R, R, R, R, R, R, R, R, R, and Rare independently hydrogen or —Calkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.

US Patent:

20130289003, Oct 31, 2013

Filed:

Oct 25, 2011

Appl. No.:

13/881929

Inventors:

Amjad Ali - Freehold NJ, US
Michael Man-Chu Lo - Edison NJ, US
Robert K. Baker - Cranford NJ, US
Zhiqiang Guo - Morganville NJ, US
Brent Whitehead - Morristown NJ, US
Timothy J. Henderson - Edison NJ, US
Edward Metzger - Somerset NJ, US
Lin Yan - East Brunswick NJ, US
Shrenik K. Shah - Metuchen NJ, US
James Dellureficio - Millington NJ, US
Jun Wang - Edison NJ, US

International Classification:

C07D 207/12
C07D 205/04
C07D 413/10
C07D 403/10
C07D 307/20
C07D 309/12
C07D 211/44
C07D 401/04

US Classification:

514150, 548531, 546242, 548952, 5462787, 5483641, 548255, 546193, 549475, 549419, 544336, 5482694, 548132, 548144

Abstract:

A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.