Brian Andrew Stearns

US Patent:

7087601, Aug 8, 2006

Filed:

Nov 26, 2002

Appl. No.:

10/497452

Inventors:

Jeannie Arruda - San Diego CA, US
Celine Bonnefous - San Diego CA, US
Brian T. Campbell - San Diego CA, US
Rowena V. Cube - San Diego CA, US
Benito Munoz - San Diego CA, US
Brian Stearns - San Diego CA, US
Jean-Michel Vernier - San Diego CA, US
Bowei Wang - San Diego CA, US
Xiumin Zhao - San Diego CA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/5383
A61K 31/437
C07D 413/14
C07D 491/048

US Classification:

5142342, 514302, 544127, 546115

Abstract:

Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

US Patent:

7105533, Sep 12, 2006

Filed:

Sep 9, 2003

Appl. No.:

10/527044

Inventors:

Brian Thomas Campbell - San Diego CA, US
Janet Lorraine Gunzer - Berkeley CA, US
Benito Munoz - San Diego CA, US
Brian Andrew Stearns - San Diego CA, US
Jean-Michel Andre Vernier - San Diego CA, US
Bowei Wang - San Diego CA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/4375
A61K 31/4439
C07D 471/02
C07D 487/02
C07D 513/02

US Classification:

514299, 514300, 514338, 546112, 546119, 546121, 5462687, 5462701

Abstract:

Phenyl compounds substituted with a fused-heterobicyclo moiety, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

US Patent:

7365074, Apr 29, 2008

Filed:

Jun 23, 2004

Appl. No.:

10/874835

Inventors:

Nicholas D. Cosford - San Diego CA, US
Jeffrey R. Roppe - Temecula CA, US
Lida R. Tehrani - San Diego NJ, US
Nicholas D. Smith - San Diego CA, US
Brian Stearns - San Diego CA, US
Dehua Huang - San Diego CA, US
Bowei Wang - San Diego CA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D 401/06
A61K 31/444

US Classification:

51425203, 51425505, 514256, 544238, 544295, 544333, 544256

Abstract:

In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system.

US Patent:

7462619, Dec 9, 2008

Filed:

Apr 1, 2005

Appl. No.:

11/097047

Inventors:

Nicholas D. Cosford - San Diego CA, US
Jeffrey R. Roppe - Temecula CA, US
Lida R. Tehrani - San Diego CA, US
Nicholas D. Smith - San Diego CA, US
Brian Stearns - San Diego CA, US
Dehua Huang - San Diego CA, US
Bowei Wang - San Diego CA, US
Thomas J. Seiders - San Diego CA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D 401/12
C07D 239/30
A61K 31/444

US Classification:

514256, 514269, 514275, 544315, 544330, 544331, 544333, 544334

Abstract:

In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.

US Patent:

7465730, Dec 16, 2008

Filed:

Jul 8, 2003

Appl. No.:

10/520962

Inventors:

Naomi Burke Anker - Boston MA, US
Jeannie M. Arruda - San Diego CA, US
Brian Thomas Campbell - San Diego CA, US
Benito Munoz - San Diego CA, US
Petpiboon Prasit - San Diego CA, US
Brian A. Stearns - San Diego CA, US
Tao Hu - San Diego CA, US

Assignee:

Merck & Co. Inc. - Rahway NJ

International Classification:

A01N 43/58
A61K 31/5025
C07D 487/06

US Classification:

514252, 544236

Abstract:

6H-pyrrolo[3,4-d]pyridazine compounds and methods of their use of as ligands of voltage gated calcium channels (VGCC), useful in the treatment of neuropathic pain, and 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 and other.

US Patent:

7687541, Mar 30, 2010

Filed:

Oct 18, 2004

Appl. No.:

10/574655

Inventors:

Jeannie M. Arruda - San Diego CA, US
Benito Munoz - San Diego CA, US
Brian A. Stearns - San Diego CA, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 31/215
A61K 31/235
A61K 31/19
A61K 31/195
C07C 315/00

US Classification:

514529, 514533, 514557, 514562, 560 11, 562427, 562429

Abstract:

The invention encompasses the novel compounds of Formula (I) and Formula (II), which are prodrugs that convert in vivo to diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. These prodrugs are far more soluble in aqueous media than the active agents into which they convert, in vivo. As such compounds of Formula (I) and (II) are advantageous for, among other things intravenous administration. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula (I) and Formula (II).

US Patent:

7910561, Mar 22, 2011

Filed:

Dec 9, 2005

Appl. No.:

11/792121

Inventors:

Jeannie M. Arruda - San Diego CA, US
Brian T. Campbell - San Diego CA, US
Nicholas D. P. Cosford - San Diego CA, US
Jacob M. Hoffman - Lansdale PA, US
Essa H. Hu - Camarillo CA, US
Mark E. Layton - Harleysville PA, US
Yiwei Li - Ambler PA, US
Jun Liang - Palo Alto CA, US
Kevin J. Rodzinak - Schwenksville PA, US
Tony Siu - Brookline MA, US
Brian A. Stearns - San Diego CA, US
Lida R. Tehrani - San Diego CA, US
Mark T. Bilodeau - Lansdale PA, US
Peter J. Manley - Harleysville PA, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

A01N 43/04
A01N 43/58
A01N 43/42
A61K 31/541
A61K 31/70
A61K 31/50
A61K 31/495
A61K 31/52
C09B 25/00
C07D 487/00
C07D 491/00
C07H 15/00

US Classification:

514 43, 51421021, 514249, 51426322, 514314, 536 292, 544277, 544350, 546173

Abstract:

The present invention is directed to compounds which contain substituted naphthyridines 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. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.

US Patent:

7919621, Apr 5, 2011

Filed:

Jan 23, 2007

Appl. No.:

11/626222

Inventors:

John Howard Hutchinson - La Jolla CA, US
Thomas Jonathan Seiders - San Diego CA, US
Brian Andrew Stearns - San Diego CA, US
Bowei Wang - San Diego CA, US

Assignee:

Amira Pharmaceuticals, Inc. - San Diego CA

International Classification:

C07D 487/06
A61K 31/4745
A61K 31/4738

US Classification:

546 80, 514290

Abstract:

Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.