Brian Scott Eastman

US Patent:

6632825, Oct 14, 2003

Filed:

Jun 13, 2001

Appl. No.:

09/882345

Inventors:

Shao Song Chu - Encinitas CA
Brian Walter Eastman - San Diego CA
Ye Hua - La Jolla CA
Hiep The Luu - San Diego CA
Siegfried Heinz Reich - Solana Beach CA
Donald James Skalitzky - San Diego CA
Yi Yang - San Diego CA
Thomas F. Hendrickson - Encinitas CA
Fora P. Chan - San Diego CA

Assignee:

Agouron Pharmaceuticals, Inc. - San Diego CA

International Classification:

A61K 3144

US Classification:

514306, 514343, 514367, 514387, 514414, 514422, 5462784, 546138, 548162, 5483061, 548525, 548535, 548492

Abstract:

Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

US Patent:

6989384, Jan 24, 2006

Filed:

Jul 23, 2003

Appl. No.:

10/626827

Inventors:

Ye Hua - La Jolla CA, US
Hiep The Luu - San Diego CA, US
Fora P. Chan - San Diego CA, US
Siegfried Heinz Reich - San Diego CA, US
Donald James Skalitzky - San Diego CA, US
Yi Yang - San Diego CA, US
Thomas F. Hendrickson - Encinitas CA, US
Shao Song Chu - Encinitas CA, US
Brian Walter Eastman - San Diego CA, US

Assignee:

Agouron Pharmaceuticals, Inc. - San Diego CA

International Classification:

A61K 31/40
A61K 31/4439
C07D 207/12
C07D 401/02
C07D 403/02

US Classification:

51425505, 514311, 514312, 514343, 514365, 514392, 514422, 514424, 514542, 544354, 546169, 5462784, 548200, 5483061, 5483741, 548467, 548517, 548525, 548550, 560 41, 560 43

Abstract:

Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

US Patent:

7569592, Aug 4, 2009

Filed:

Dec 13, 2002

Appl. No.:

10/497122

Inventors:

Nicholas D. P. Cosford - San Diego CA, US
Chixu Chen - San Diego CA, US
Brian W. Eastman - San Diego CA, US
Dehua Huang - San Diego CA, US
Benito Munoz - San Diego CA, US
Petpiboon Prasit - San Diego CA, US
Nicholas D. Smith - San Diego CA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/4439
A61K 31/4155
C07D 401/04

US Classification:

514341, 514406, 5462754, 5483641

Abstract:

Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.

US Patent:

7592337, Sep 22, 2009

Filed:

Mar 7, 2003

Appl. No.:

10/506479

Inventors:

Chixu Chen - San Diego CA, US
Nicholas D. P. Cosford - San Diego CA, US
Brian W. Eastman - San Diego CA, US
Dehua Huang - San Diego CA, US
Steve F. Poon - San Diego CA, US
Thomas S. Reger - San Diego CA, US
Jeffrey R. Roppe - Temecula CA, US
Nicholas D. Smith - San Diego CA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/535
A61K 31/4965
A61K 31/44
A61K 31/47
A61K 31/425
A61K 31/41
A61K 31/415
A61K 31/385
A61K 31/38
A61K 31/335
A61K 31/34
C07D 413/00
C07D 239/00
C07D 241/00
C07D 221/02
C07D 421/00
C07D 277/04

US Classification:

5142362, 51425505, 514256, 514299, 514314, 514336, 514365, 514381, 514406, 514436, 514444, 514463, 514468, 544111, 544242, 544336, 546112, 5462681, 548146, 548250, 548255, 5483561, 549 17, 549 59, 549472

Abstract:

Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.

US Patent:

7626021, Dec 1, 2009

Filed:

Apr 10, 2007

Appl. No.:

11/733753

Inventors:

William D. Arnold - San Diego CA, US
Pierre Bounaud - San Diego CA, US
Chixu Chen - San Diego CA, US
Brian Eastman - San Diego CA, US
Andreas Gosberg - San Marcos CA, US
Stefan N. Gradl - San Diego CA, US
Stephanie Hopkins - Poway CA, US
Zhe Li - San Diego CA, US
Ian McDonald - Killarney Heights, AU
Paul A. Sprengeler - San Diego CA, US
Ruo W. Steensma - La Jolla CA, US
Mark E. Wilson - Ramona CA, US

Assignee:

SGX Pharmaceuticals, Inc. - San Diego CA

International Classification:

C07D 471/00
C07D 487/00

US Classification:

544350

Abstract:

The present invention provides novel fused ring heterocycle kinase modulators and methods of using the novel fused ring heterocycle kinase modulators to treat diseases mediated by kinase activity.

US Patent:

7705014, Apr 27, 2010

Filed:

Apr 10, 2006

Appl. No.:

11/918386

Inventors:

Chixu Chen - San Diego CA, US
Brian W. Eastman - San Diego CA, US
Essa H. Hu - San Diego CA, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 513/02
C07D 515/02
A01N 43/42
A61K 31/44

US Classification:

514300, 546122

Abstract:

The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

US Patent:

7709645, May 4, 2010

Filed:

Apr 10, 2007

Appl. No.:

11/733758

Inventors:

William D Arnold - San Diego CA, US
Pierre Bounaud - San Diego CA, US
Chixu Chen - San Diego CA, US
Brian Eastman - San Diego CA, US
Andreas Gosberg - San Marcos CA, US
Stefan N. Gradl - San Diego CA, US
Stephanie Hopkins - Poway CA, US
Zhe Li - San Diego CA, US
Ian McDonald - Killarney Heights, AU
Paul A. Sprengeler - San Diego CA, US
Ruo W. Steensma - La Jolla CA, US
Mark E. Wilson - Ramona CA, US

Assignee:

SGX Pharmaceuticals, Inc. - San Diego CA

International Classification:

C07D 471/02

US Classification:

546113

Abstract:

The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity.

US Patent:

7750151, Jul 6, 2010

Filed:

Apr 5, 2005

Appl. No.:

11/547113

Inventors:

Mark T. Bilodeau - Lansdale PA, US
Chixu Chen - San Diego CA, US
Nicholas D. P. Cosford - San Diego CA, US
Brian W. Eastman - San Diego CA, US
John C. Hartnett - Conshohocken PA, US
Essa H. Hu - San Diego CA, US
Peter J. Manley - Harleysville PA, US
Lou Anne Neilson - Sellersville PA, US
Lida R. Tehrani - San Diego CA, US
Zhicai Wu - Quakertown PA, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 471/04
C07D 413/12
C07D 521/00
C07D 401/14
C07D 487/08
A61P 35/00

US Classification:

544127, 544405, 544349, 544331, 544279, 546123, 546121, 546116

Abstract:

The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.