Thomas J Magee

US Patent:

6649633, Nov 18, 2003

Filed:

Jan 31, 2002

Appl. No.:

10/062813

Inventors:

Robert J. Chambers - Mystic CT
Anthony Marfat - Mystic CT
Thomas V. Magee - Mystic CT

Assignee:

Pfizer Inc - New York NY

International Classification:

A61K 3144

US Classification:

514337, 514357, 514358, 514355, 514338, 546316, 546347, 546329, 5462837, 5462841, 5462834

Abstract:

This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W is âOâ; or âS( O) â, where t is 0, 1, or 2; Y is âC(R ); Q is phenyl or substituted phenyl; Q is biphenyl or substituted biphenyl; and the remaining variables are defined as set forth in the specification. This application is also directed to pharmaceutical compositions comprising those compounds and to methods of treating diseases regulated by the activation and degranulation of eosinophils, in particular asthma, chronic bronchitis and chronic obstructive pulmonary disease.

US Patent:

6740655, May 25, 2004

Filed:

Jul 24, 2002

Appl. No.:

10/181417

Inventors:

Thomas Victor Magee - Mystic CT
Anthony Marfat - Mystic CT
Robert James Chambers - Mystic CT

Assignee:

Pfizer Inc - New York NY

International Classification:

A61K 3138

US Classification:

51425505, 514269, 544319

Abstract:

This invention is directed to compounds of the formula: wherein j is 0 or 1; k is 0 or 1; m is 0 or 1; n is 0 or 1; W is âOâ; âS( O) â, where t is 0, 1, or 2; or âN(R )â; where R is âH, â(C -C ) alkyl, âOR , phenyl, or benzyl; R and R have the same meaning as R and R , except that at least one of R and R must be âH; and the other variables are defined as set forth in the specification. The invention is also directed to pharmaceutical compositions comprising the above compounds and to methods of treating a subject suffering from a disease, disorder or condition mediated by the PDE4 isozyme, the method comprising administering a therapeutically effective amount of a compound as described above. The invention is particularly directed to methods of treating inflammatory, respiratory and allergic diseases and conditions, especially asthma; chronic obstructive pulmonary disease (COPD) including chronic bronchitis, emphysema, and bronchiectasis; chronic rhinitis; and chronic sinusitis.

US Patent:

6756392, Jun 29, 2004

Filed:

Feb 6, 2003

Appl. No.:

10/361083

Inventors:

Thomas V. Magee - Mystic CT

Assignee:

Pfizer Inc - New York NY

International Classification:

A61K 3144

US Classification:

514350, 546298, 546296, 546291, 546290, 546304, 514346, 514348, 514352

Abstract:

The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions as well as for wounds healing.

US Patent:

6828333, Dec 7, 2004

Filed:

Jan 31, 2002

Appl. No.:

10/066503

Inventors:

Anthony Marfat - Mystic CT
Robert J. Chambers - Mystic CT
Thomas V. Magee - Mystic CT

Assignee:

Pfizer Inc. - New York NY

International Classification:

A61K 3144

US Classification:

514338, 5462841, 5462701, 5462811

Abstract:

This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W and W are independently âOâ or âS( O) â, where t is 0, 1, or 2; Y is C(R )â, where R is a member selected from the group consisting of H; F; Cl; CN; NO ; â(C -C ) alkyl; â(C -C ) alkynyl; fluorinated-(C -C ) alkyl; fluorinated-(C -C ) alkoxy; âOR ; and âC( O)NR R ; R and R are defined as set forth in the specification; âR and R are each a member independently selected from the group consisting of H; F; CF ; â(C -C ) alkyl; â(C -C ) cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R , which is defined as set forth in the specification; R and R are defined as set forth in the specification; âR and R have the same meaning as defined above for R and R except that one of them must be âH, and they are selected independently of each other and of R and R ; R and R are each a member independently selected from the group consisting of H; F; Cl; CN; NO ; â(C -C ) alkyl; â(C -C ) alkynyl; fluorinated-(C -C )alkyl; OR ; and âC( O)NR R ; âR is H; â(C -C )alkyl; phenyl; benzyl; or OR ; R , R and R are defined as set forth in the specification; J and J are each independently a moiety comprising a saturated or unsaturated six-membered monocyclic carbon ring; and D is a member independently selected from the group consisting of partial Formulas (1. 1. 1) through (1. 1. 5) as set forth in the specification; a pharmaceutically acceptable salt thereof; which are useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinaphils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease.

US Patent:

6953810, Oct 11, 2005

Filed:

Jul 2, 2003

Appl. No.:

10/613988

Inventors:

Robert J. Chambers - Mystic CT, US
Anthony Marfat - Mystic CT, US
Thomas V. Magee - Mystic CT, US

Assignee:

Pfizer Inc - New York NY

International Classification:

A61K031/44
A61K031/4412
C07D417/12
C07D417/02

US Classification:

514341, 5662687

Abstract:

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; Wis —O—; or —S(═O)—, where t is 0, 1, or 2; or —N(R)—; Wis —O—CRR— or is absent; Y is ═C(R)— or —[N→(O)]— where k is 0 or 1; Rand Rare —H; —F; —CF; —(C-C)alkyl; —(C-C) cycloalkyl; phenyl; or benzyl substituted with 0 to 3 substituents R; or Rand Rare taken together, but only in the case where m is 1, to form a spiro moiety; Rand Rhave the same meaning as Rand Rexcept that one of them must be —H, Rand Rare —H; —F; —Cl; —CN; —NO; —(C-C)alkyl; —(C-C)alkynyl; fluorinated-(C-C)alkyl; —OR; and —C(═O)NRR; Ris —H; —(C-C)alkyl; phenyl; benzyl; or —OR; R, Rand in addition to other meanings may be taken together to form, e. g. , Qis a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that Qis not a discontinuous or restricted biaryl moiety as defined under Q; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; Qis a discontinuous or restricted biaryl moiety consisting of a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; Z is selected from:.

US Patent:

7183293, Feb 27, 2007

Filed:

Aug 13, 2004

Appl. No.:

10/918820

Inventors:

Anthony Marfat - Mystic CT, US
Robert J. Chambers - Msytic CT, US
Thomas V. Magee - Mystic CT, US

Assignee:

Pfizer Inc. - New York NY
Pfizer Products Inc. - Groton CT

International Classification:

C07D 405/12
A61K 31/44

US Classification:

514338, 5462841, 5462701, 5462811

Abstract:

This application is directed to compounds of the formula.

US Patent:

7250518, Jul 31, 2007

Filed:

Feb 17, 2004

Appl. No.:

10/781062

Inventors:

Thomas V. Magee - Mystic CT, US
Anthony Marfat - Mystic CT, US
Robert J. Chambers - Mystic CT, US

Assignee:

Pfizer Inc. - New York NY

International Classification:

C07D 405/12
C07D 213/64

US Classification:

5462841, 546291, 546290, 5462691, 5462684

Abstract:

Compounds of the formula:.

US Patent:

7462600, Dec 9, 2008

Filed:

Dec 21, 2005

Appl. No.:

11/313523

Inventors:

Louis S. Chupak - Old Saybrook CT, US
Mark E. Flanagan - Gales Ferry CT, US
Takushi Kaneko - Guilford CT, US
Thomas V. Magee - Mystic CT, US
Mark C. Noe - Mystic CT, US
Usa Reilly - West Haven CT, US

Assignee:

Pfizer Inc - New York NY

International Classification:

A61K 31/70
C07H 17/08

US Classification:

514 29, 536 74

Abstract:

Macrolide compounds per se, as shown below and defined herein, and their use, e. g. , as antibacterial and antiprotozoal agents in animals, including humans:.