Abstract: There is provided a process for the preparation of a compound according to Formula (II):
which includes the step of cyclising a compound of Formula (III):
wherein R1, R2, R3, R4, X and m have meanings which are given in the description.
Type:
Grant
Filed:
July 30, 2001
Date of Patent:
November 30, 2004
Assignee:
Pfizer Inc.
Inventors:
Desmond John Best, George Burton, Brian Charles Gasson, Neal Frederick Osborne, Graham Walker
Abstract: This invention provides a compound of the following formula:
or the pharmaceutically acceptable salts thereof, wherein
Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl, heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3.
These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.
Type:
Grant
Filed:
August 8, 2001
Date of Patent:
March 30, 2004
Assignee:
Pfizer Inc.
Inventors:
Yoshiyuki Okumura, Yoshinori Murata, Takashi Mano
Abstract: The present invention is directed to compositions and methods for producing avermectins, and is primarily in the field of animal health. The present invention relates to the identification and characterization of two novel genes, herein referred to as the aveR1 and aveR2 genes, that are involved in regulating avermectin polyketide synthase (PKS) expression and avermectin biosynthesis in Streptomyces avermitilis. The present invention is based on the discovery that inactivation of these genes results in an increase in the amount of avermectin produced by S. avermitilis.
Type:
Grant
Filed:
November 16, 2000
Date of Patent:
February 10, 2004
Assignee:
Pfizer Inc.
Inventors:
Kim J. Stutzman-Engwall, Brenda S. Price
Abstract: This invention relates to a compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is (C1-C4)alkyl optionally substituted with halo, amino or an alkyl amino; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
Type:
Grant
Filed:
November 28, 2000
Date of Patent:
November 18, 2003
Assignee:
Pfizer Inc.
Inventors:
Kazuo Ando, Martha L. Minich, Jin Li, Subas M. Sakya, Kristin M. Lundy, Hengmiao Cheng, Brian S. Bronk, Kiyoshi Kawamura, Tomoki Kato
Abstract: This invention relates to a compound of the formula:
or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is NH2; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.