Abstract: Intermediates useful in the synthesis of dihydropyridine platelet activating factor antagonists of the formula ##STR1## where R is phenyl or substituted phenyl; R.sup.3 is lower alkyl; Y is 1,4-phenylene and X is 2-alkylimidazopyridyl.
Type:
Grant
Filed:
September 11, 1991
Date of Patent:
September 22, 1992
Assignee:
Pfizer Inc
Inventors:
Kelvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
Abstract: Platelet activating factor antagonists of formula (I): ##STR1## wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl(C.sub.1 -C.sub.4)alkoxy, fluoro(C.sub.1 -C.sub.4)alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring;R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C.sub.1 -C.sub.4 alkyl)piperazinyl or N-(C.sub.2 -C.sub.4 alkanoyl)-piperazinyl group;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.1 is CN, C.sub.3 -C.sub.7 cycloalkyl, aryl, heteroaryl or a C.sub.1 -C.sub.4 alkyl group substituted by one or more substituents selected from C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, aryl or heteroaryl;Z is selected from C.sub.1 -C.sub.6 alkoxy, aryl(C.sub.1 -C.sub.
Type:
Grant
Filed:
May 1, 1990
Date of Patent:
June 9, 1992
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Michael Fray, Kenneth Richardson, John Steele
Abstract: The invention provides antifungal agents of the formula: ##STR1## and their pharmaceutically acceptable salts, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and CF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl; and"Het", which is attached to the adjacent carbon atom by a ring carbon atom, is selected from pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and triazinyl, "Het" being optionally substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, CN, NO.sub.2, NH.sub.2, --NH(C.sub.1 -C.sub.4 alkanoyl) or --NHCO.sub.2 (C.sub.1 -C.sub.4 alkyl).
Abstract: A series of 2-amino-5,6-dimethyl-1,4-benzoquinone derivatives, inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergic and antiinflammatory agents.
Abstract: Intermediates useful in the synthesis of dihydropyridine platelet activating factor antagonists of the formula ##STR1## where R is phenyl or substituted phenyl; R.sup.3 is lower alkyl; Y is 1,4-phenylene and X is a benzimidazol-1-yl.
Type:
Grant
Filed:
May 1, 1990
Date of Patent:
December 3, 1991
Assignee:
Pfizer Inc.
Inventors:
Melvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
Abstract: Platelet activating factor antagonists of formula (I): ##STR1## wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl(C.sub.1 -C.sub.4)alkoxy, fluoro(C.sub.1 -C.sub.4)alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring;R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C.sub.1 -C.sub.4 alkyl)piperazinyl or N-(C.sub.2 -C.sub.4 alkanoyl)-piperazinyl group;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.1 is CN, C.sub.3 -C.sub.7 cycloalkyl, aryl, heteroaryl or a C.sub.1 -C.sub.4 alkyl group substituted by one or more substituents selected from C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, aryl or heteroaryl;Z is selected from C.sub.1 -C.sub.6 alkoxy, aryl(C.sub.1 -C.sub.
Type:
Grant
Filed:
May 1, 1990
Date of Patent:
November 5, 1991
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
Abstract: Process for making antiinflammatory 3-aroyl-2-oxindole-1-carboxamides by reductive debromination or deiodination of 3-(bromo- or iodoaroyl)-2-oxindole-1-carboxamides.
Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.
Type:
Grant
Filed:
December 3, 1990
Date of Patent:
July 30, 1991
Assignee:
Pfizer Inc.
Inventors:
Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
Abstract: Polypeptides and derivatives thereof containing nor-statine and nor-cyclostatine are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.
Type:
Grant
Filed:
March 21, 1990
Date of Patent:
July 23, 1991
Assignee:
Pfizer Inc.
Inventors:
Dennis J. Hoover, Robert L. Rosati, Ronald T. Wester
Abstract: The invention provides triazole antifungal compounds of the formula: ##STR1## wherein R is either (a) a phenyl group optionally substituted with 1 to 3 substituents, each selected independently from halo and CF.sub.3 ; or(b) a 5-chloropyridin-2-yl group; and R.sup.
Type:
Grant
Filed:
June 20, 1989
Date of Patent:
June 11, 1991
Assignee:
Pfizer Inc.
Inventors:
Geoffrey E. Gymer, Subramaniyan Narayanaswami, Kenneth Richardson
Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.
Type:
Grant
Filed:
October 25, 1989
Date of Patent:
April 9, 1991
Assignee:
Pfizer Inc.
Inventors:
Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
Abstract: Compounds of the formula ##STR1## where R.sup.1 is lower alkyl, R.sup.2 is chlorophenyl, Y is alkylene, X is heterocyclic and Z is a fused ring are useful as antiinflammatory and antiallergy agents.
Type:
Grant
Filed:
May 8, 1989
Date of Patent:
February 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Peter E. Cross, Michael J. Fray, Kenneth Richardson
Abstract: Antiparasitic compound of formula (I): ##STR1## The broken line at the 22-23 position representing an optional double bond and eitherR.sup.1 is a H or OH and the double bond is absent or the double bond is present and R.sup.1 is absent;R.sup.2 is optionally substituted phenyl, or a group of formula (II): ##STR2## wherein X is O, S or --CH.sub.2 --, abc and d are 0-2 and a+b+c+d.ltoreq.5 R.sup.3 is H or MeR.sup.4 is H, OH or 4'-(alpha-L-oleandrosyl)-alpha-L-oleandrosyloxy.The compounds are prepared by fermentation of Streptomyces avermitilis in the presence of an N-alkanoyl cysteamine thioester containing R.sup.2.
Type:
Grant
Filed:
June 26, 1989
Date of Patent:
December 25, 1990
Assignee:
Pfizer Inc.
Inventors:
Christopher J. Dutton, Stephen P. Gibson, Nigel D. A. Walshe
Abstract: Heterocyclicguanidines as 5HT.sub.3 antagonists useful in the treatment of nausea, anxiety, pain, schizophrenia and gastrointestinal disorders.
Type:
Grant
Filed:
May 19, 1989
Date of Patent:
October 16, 1990
Assignee:
Pfizer Inc.
Inventors:
Arthur A. Nagel, James P. Rizzi, Terry J. Rosen
Abstract: The invention provides compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by halo;R.sup.1 is C.sub.1 -C.sub.4 alkyl;is hydrogen, C.sub.5 -C.sub.7 cycloalkyl, benzyl or C.sub.1 -C.sub.4 alkyl, said C.sub.1 -C.sub.4 alkyl group being optionally substituted by cyano, trimethylsilyl or C.sub.1 -C.sub.3 alkoxy; and"Het" is ##STR2## wherein R.sup.3 is hydrogen or methyl. The compounds are useful in the treatment of allergic, inflammatory and hypersecretory conditions, and circulatory shock, stroke and thrombosis.
Type:
Grant
Filed:
September 12, 1989
Date of Patent:
October 16, 1990
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
Abstract: Triazoles of the formula ##STR1## where R is phenyl optionally substituted by 1 to 3 substituents each independently selected from F, Cl, Br, I, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, or R is 5-chloro-pyrid-2-yl; and R.sup.1 is H, CH.sub.3 or F; and their pharmaceutically and agriculturally acceptable salts. The compounds are useful as human and agricultural fungicides.