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:

20060111370, May 25, 2006

Filed:

Jun 9, 2005

Appl. No.:

11/149027

Inventors:

Zhaoning Zhu - Plainsboro NJ, US
Brian McKittrick - New Vernon NJ, US
Yuanzan Ye - Edison NJ, US
Johannes Voigt - Cranford NJ, US
Corey Strickland - Martinsville NJ, US
Elizabeth Smith - Verona NJ, US
Andrew Stamford - Chatham Township NJ, US
William Greenlee - Teaneck NJ, US
Robert Mazzola - Stewartsville NJ, US
John Caldwell - Ringwood NJ, US
Jared Cumming - Garwood NJ, US
Lingyan Wang - East Brunswick NJ, US
Yusheng Wu - New York NY, US
Ulrich Iserloh - Hoboken NJ, US
Tao Guo - Dayton NJ, US
Thuy Le - Monmouth Junction NJ, US
Kurt Saionz - Cranford NJ, US
Suresh Babu - Plainsboro NJ, US
Rachael Hunter - Princeton NJ, US
Michelle Morris - Lawrenceville NJ, US
Huizhong Gu - Monmouth Junction NJ, US
Gang Qian - Kendall Park NJ, US
Dawit Tadesse - East Windsor NJ, US

International Classification:

A61K 31/519
A61K 31/497
A61K 31/513
A61K 31/4439
A61K 31/454
A61K 31/4245
C07D 413/02
C07D 403/02

US Classification:

514255050, 544314000, 546272700, 544405000, 548311100, 546210000, 548318100, 544231000, 514269000, 514326000, 514257000, 514389000, 514364000

Abstract:

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

US Patent:

20060287294, Dec 21, 2006

Filed:

Jun 12, 2006

Appl. No.:

11/451195

Inventors:

Zhaoning Zhu - Plainsboro NJ, US
Brian McKittrick - New Vernon NJ, US
Andrew Stamford - Chatham Township NJ, US
Tao Guo - Dayton NJ, US
Thuy Le - Monmouth Junction NJ, US

International Classification:

A61K 31/554
A61K 31/553
A61K 31/551
C07D 285/36
C07D 243/10
C07D 223/14

US Classification:

514211080, 514221000, 540543000, 540489000, 540500000

Abstract:

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R, R, Rand R, are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

US Patent:

20070072852, Mar 29, 2007

Filed:

Dec 13, 2004

Appl. No.:

11/010772

Inventors:

Zhaoning Zhu - Plainsboro NJ, US
Brian McKittrick - New Vernon NJ, US
Yuanzan Ye - Edison NJ, US
Johannes Voigt - Cranford NJ, US
Corey Strickland - Martinsville NJ, US
Elizabeth Smith - Verona NJ, US
Andrew Stamford - Chatham Township NJ, US
William Greenlee - Teaneck NJ, US
Robert Mazzola - Stewartsville NJ, US
John Caldwell - Ringwood NJ, US
Jared Cumming - Garwood NJ, US
Lingyan Wang - East Brunswick NJ, US
Yusheng Wu - New York NY, US
Ulrich Iserloh - Hoboken NJ, US
Tao Guo - Dayton NJ, US
Thuy Le - Monmouth Junction NJ, US
Kurt Saionz - Cranford NJ, US
Suresh Babu - Plainsboro NJ, US
Rachael Hunter - Princeton NJ, US

International Classification:

A61K 31/549
A61K 31/5395
A61K 31/513

US Classification:

514229200, 514275000, 514255010, 514389000, 514222500, 544008000, 544066000, 544315000

Abstract:

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)—, —C(═O)—, —O—, —C(R)(R)—, —N(R)— or —C(═N(R))—; X is —O—, —N(R)— or —C(R)(R)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)—, —C(═O)— or —C(═NR)—; U is a bond, —S(O)—, —S(O)—, —C(O)—, —O—, —P(O)(OR)—, —C(═NR)—, —(C(R)(R))— or —N(R)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)—, —O—, or —N(R)—, U is not —S(O)—, —S(O)—, —O—, or —N(R)—; provided that when X is —N(R)— and W is —S(O)—, —S(O)—, —O—, or —N(R)—, then U is not a bond; and R, R, R, R, R, R, and Rare as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

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:

20080200445, Aug 21, 2008

Filed:

Feb 23, 2007

Appl. No.:

11/710582

Inventors:

Zhaoning Zhu - Plainsboro NJ, US
Brian McKittrick - New Vernon NJ, US
Yuanzan Ye - Edison NJ, US
Johannes Voigt - Cranford NJ, US
Corey Strickland - Martinsville NJ, US
Elizabeth Smith - Verona NJ, US
Andrew Stamford - Chatham Township NJ, US
William Greenlee - Teaneck NJ, US
Robert Mazzola - Stewartsville NJ, US
John Caldwell - Ringwood NJ, US
Jared Cumming - Garwood NJ, US
Lingyan Wang - East Brunswick NJ, US
Yusheng Wu - New York NY, US
Ulrich Iserloh - Hoboken NJ, US
Xiaoxiang Liu - River Vale NJ, US
Tao Guo - Dayton NJ, US
Thuy Le - Monmouth Junction NJ, US
Kurt Saionz - Cranford NJ, US
Suresh Babu - Plainsboro NJ, US
Rachael Hunter - Princeton NJ, US
Michelle Morris - Lawrenceville NJ, US
Huizhong Gu - Monmouth Junction NJ, US
Gang Qian - Kendall Park NJ, US
Dawit Tadesse - East Windsor NJ, US
Ying Huang - East Brunswick NJ, US
Guoqing Li - Belle Mead NJ, US
Jianping Pan - Monmouth Junction NJ, US
Jeffrey Misiaszek - Kenilworth NJ, US
Gaifa Lai - Monmouth Junction NJ, US
Jingqi Duo - Monmouth Junction NJ, US
Chuanxing Qu - Scotch Plains NJ, US
Yuefei Shao - Princeton NJ, US

International Classification:

A61K 31/506
A61K 31/4178
A61K 31/4245
A61K 31/4439
A61K 31/454
A61K 31/541
A61P 31/00
C07D 233/02
C07D 271/00
C07D 413/14
C07D 409/14
C07D 409/04
C07D 403/06
C07D 401/14
C07D 401/12
C07D 401/10
C07D 401/06
C07D 239/04
A61P 9/00
A61P 25/00
A61K 31/5377
A61K 31/4545
A61K 31/4709
A61K 31/498

US Classification:

514210020, 514222200, 514229200, 514235800, 514249000, 514272000, 514313000, 514318000, 514326000, 514341000, 514389000, 544295000, 544321000, 544066000, 546162000, 546194000, 546210000, 546274400, 546297000, 548314400, 548550000

Abstract:

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.

US Patent:

20090258868, Oct 15, 2009

Filed:

Dec 10, 2008

Appl. No.:

12/331787

Inventors:

Zhaoning Zhu - Plainsboro NJ, US
Brian A. McKittrick - New Vernon NJ, US
Yuanzan C. Ye - North Brunswick NJ, US
Johannes H. Voigt - Cranford NJ, US
Corey Strickland - Martinsville NJ, US
Elizabeth M. Smith - Verona NJ, US
Andrew Stamford - Chatham Township NJ, US
William J. Greenlee - Teaneck NJ, US
Robert Mazzola - Stewartsville NJ, US
John Caldwell - Ringwood NJ, US
Jared N. Cumming - Garwood NJ, US
Lingyan Wang - East Brunswick NJ, US
Yusheng Wu - New York NY, US
Ulrich Iserloh - Hoboken NJ, US
Tao Guo - Dayton NJ, US
Thuy X.H. Le - Monmouth Junction NJ, US
Kurt W. Saionz - Cranford NJ, US
Suresh D. Babu - Pennington NJ, US
Rachael C. Hunter - Wayne NJ, US
Michelle L. Morris - Lawrenceville NJ, US
Huizhong Gu - Monmouth Junction NJ, US
Gang Qian - Kendall Park NJ, US
Dawit Tadesse - Avenel NJ, US

International Classification:

A61K 31/5355
C07D 401/02
A61K 31/4439
C07D 233/02
A61K 31/4166
C07D 239/24
A61K 31/505
C07D 241/10
A61K 31/497
C07D 261/02
A61K 31/42
A61K 31/454
C07D 277/20
A61K 31/426
C07D 235/04
A61K 31/4184
C07D 211/00
A61K 31/4545
C07D 471/02
A61K 31/4375
C07D 413/14
A61K 31/5377
C07D 487/02
A61K 31/519
C07D 271/06
A61K 31/4245
C07D 273/04
A61P 9/00
A61P 25/00

US Classification:

5142292, 5462744, 514341, 5483215, 514389, 544316, 514274, 544336, 51425505, 548248, 514378, 546210, 514326, 548200, 514365, 5483061, 514395, 546194, 514318, 546122, 514300, 544124, 5142358, 544281, 5142593, 548133, 514364, 544 66

Abstract:

Disclosed are compounds of the formula Ior a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, whereinAlso disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic magonist or mantagonist.