Thuy T Le

US Patent:

20050043290, Feb 24, 2005

Filed:

Aug 4, 2004

Appl. No.:

10/911030

Inventors:

Jared Cumming - Garwood NJ, US
Ying Huang - East Brunswick NJ, US
Guoqing Li - Belle Mead NJ, US
Ulrich Iserloh - Hoboken NJ, US
Andrew Stamford - Chatham Township NJ, US
Corey Strickland - Martinsville NJ, US
Johannes Voigt - Union NJ, US
Yusheng Wu - New York NY, US
Jianping Pan - Monmouth Junction NJ, US
Tao Guo - Dayton NJ, US
Douglas Hobbs - Yardley PA, US
Thuy Le - Monmouth Junction NJ, US
Jeffrey Lowrie - Pennington NJ, US

International Classification:

A61K031/55
C07D043/02

US Classification:

514210200, 514217050, 514217040, 514217060, 514217090, 540597000, 540601000

Abstract:

Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein

US Patent:

20050119227, Jun 2, 2005

Filed:

Aug 4, 2004

Appl. No.:

10/910987

Inventors:

Jared Cumming - Garwood NJ, US
Ulrich Iserloh - Hoboken NJ, US
Andrew Stamford - Chatham Township NJ, US
Corey Strickland - Martinsville NJ, US
Johannes Voigt - Union NJ, US
Yusheng Wu - New York NY, US
Ying Huang - East Brunswick NJ, US
Yan Xia - Edison NJ, US
Samuel Chackalamannil - Califon NJ, US
Tao Guo - Dayton NJ, US
Douglas Hobbs - Yardley PA, US
Thuy Le - Monmouth Junction NJ, US
Jeffrey Lowrie - Pennington NJ, US
Kurt Saionz - Cranford NJ, US
Suresh Babu - Plainsboro NJ, US

International Classification:

A61K031/675
A61K031/553
A61K031/554
A61K031/55

US Classification:

514079000, 514211150, 514218000, 540542000, 540544000, 540575000, 514217040

Abstract:

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein

US Patent:

20080176868, Jul 24, 2008

Filed:

Jun 12, 2006

Appl. No.:

11/451065

Inventors:

Andrew Stamford - Chatham Township NJ, US
Guoqing Li - Belle Mead NJ, US
William Greenlee - Teaneck NJ, US
Zhaoning Zhu - Plainsboro NJ, US
Brian McKittrick - New Vernon NJ, US
Robert Mazzola - Stewartsville NJ, US
Ying Huang - East Brunswick NJ, US
Tao Guo - Dayton NJ, US
Thuy X.H. Le - Monmouth Junction NJ, US
Gang Qian - Kendall Park NJ, US
Yuefei Shao - Princeton NJ, US

International Classification:

A61K 31/519
C07D 209/44
A61K 31/4035
A61P 25/00
A61P 25/28
A61P 31/18
A61P 9/00
C07D 487/04

US Classification:

5142593, 548471, 514416, 544281

Abstract:

Disclosed are compounds of the formula Ior a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, whereinring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocylcyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected Rmoieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl;and R, R, R, R, R, R, R, R, Rand Rare as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.

US Patent:

20100152138, Jun 17, 2010

Filed:

Dec 18, 2009

Appl. No.:

12/641952

Inventors:

Jared N. Cumming - Garwood NJ, US
Ulrich Iserloh - Hoboken NJ, US
Andrew Stamford - Chatham Township NJ, US
Corey Strickland - Martinsville NJ, US
Johannes H. Voigt - Union NJ, US
Yusheng Wu - New York NY, US
Ying Huang - East Brunswick NJ, US
Yan Xia - Edison NJ, US
Samuel Chackalamannil - Califon NJ, US
Tao Guo - Dayton NJ, US
Douglas W. Hobbs - Yardley PA, US
Thuy X.H. Le - Monmouth Junction NJ, US
Jeffrey F. Lowrie - Pennington NJ, US
Kurt W. Saionz - Cranford NJ, US
Suresh D. Babu - Plainsboro NJ, US

International Classification:

A61K 31/4015
C07D 207/12
C07D 217/24
C07D 413/12
C07D 243/08
A61K 31/47
A61K 31/675
A61K 31/397
A61K 31/5377
A61K 31/551
A61P 25/28

US Classification:

514 82, 548550, 546141, 544130, 540575, 514424, 514309, 51421001, 5142372, 514218

Abstract:

Disclosed are compounds of the formulaor a pharmaceutically acceptable salt or solvate thereof, whereinand the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

US Patent:

20140206715, Jul 24, 2014

Filed:

Mar 26, 2014

Appl. No.:

14/226338

Inventors:

Andrew W. Stamford - Chatham Township NJ, US
Guoqing Li - Belle Mead NJ, US
William Greenlee - Teaneck NJ, US
Zhaoning Zhu - Plainsboro NJ, US
Brian McKittrick - New Vernon NJ, US
Robert Mazzola - Stewartsville NJ, US
Ying Huang - East Brunswick NJ, US
Tao Guo - Daton NJ, US
Thuy X.E. Le - Monmouth Junction NJ, US
Gang Qian - Kendall Park NJ, US
Yuefei Shao - Princeton NJ, US

Assignee:

MERCK SHARP & DOHME CORP. - RAHWAY NJ

International Classification:

C07D 471/04

US Classification:

514300, 546113

Abstract:

Disclosed are compounds of the formula Ior a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein

US Patent:

20140128361, May 8, 2014

Filed:

Jan 6, 2014

Appl. No.:

14/148703

Inventors:

- Princeton NJ, US
- Rahway NJ, US
Andrew Stamford - Chatham NJ, US
Corey Strickland - Martinsville NJ, US
Johannes H. Voight - Cranford NJ, US
Yusheng Wu - New York NY, US
Ying Huang - Berkeley Heights NJ, US
Yan Xia - Edison NJ, US
Samuel Chackalamannil - Califon NJ, US
Tao Guo - Dayton NJ, US
Douglas W. Hobbs - Chesterfield MO, US
Thuy X.H. Le - Monmouth Junction NJ, US
Jeffrey H. Lowrie - Pennington NJ, US
Kurt W. Salonz - Cranford NJ, US
Suresh D. Babu - Pennington NJ, US

Assignee:

Pharmacopeia Drug Discovery, Inc. - Princeton NJ
Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 243/08
C07D 233/32
C07D 205/04

US Classification:

51421001, 548950, 5483241, 514386, 540492, 514218

Abstract:

Disclosed are compounds of the formulaor a pharmaceutically acceptable salt or solvate thereof, whereinRisR is —C(O)—N(R)(R) orand the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.