Abstract: Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors useful as anti-plasmin and antithrombin agents.
Abstract: Compounds of the formula ##STR1## where Het is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors useful as anti-plasmin and anti-thrombin agents.
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;orR.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:
September 29, 1988
Date of Patent:
June 19, 1990
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
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:
November 29, 1988
Date of Patent:
June 19, 1990
Assignee:
Pfizer Inc.
Inventors:
Dennis J. Hoover, Robert L. Rosati, Ronald T. Wester
Abstract: Arylthiazolylimidazoles as 5HT.sub.3 antagonists useful in the treatment of nausea, anxiety, pain, schizoprenia and gastrointestinal disorders.
Type:
Grant
Filed:
May 9, 1989
Date of Patent:
April 3, 1990
Assignee:
Pfizer Inc.
Inventors:
Arthur A. Nagel, James P. Rizzi, Terry J. Rosen
Abstract: An antibiotic has been isolated from fermentation of a new Streptomyces culture. The new ionophore is active as an antibacterial and anticoccidial agent.
Type:
Grant
Filed:
February 29, 1988
Date of Patent:
March 13, 1990
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, John R. Oscarson, Junsuke Tone, Hiroshi Maeda
Abstract: 4-Aryl-2,6-disubstituted-3,5-dicarbamyl-1,4-dihydropyridines and 4-Aryl-2,6-disubstituted-3-alkoxycarbonyl-5-carbamyl-1,4-dihydropyridines as antiallergy and antiinflammatory agents.
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:
February 27, 1989
Date of Patent:
February 27, 1990
Assignee:
Pfizer Inc.
Inventors:
Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
Abstract: 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.
Type:
Grant
Filed:
November 2, 1987
Date of Patent:
January 9, 1990
Assignee:
Pfizer Inc.
Inventors:
David Alker, Simon F. Campbell, Peter E. Cross
Abstract: An antifungal agent of the formula: ##STR1## wherein R is phenyl group which may be substituted by 1 to 3 substituents each independently selected from halo and CF.sub.3 ; R.sup.1 is either (a) a phenyl group substituted by a group of the formula --N.dbd.CH--N(C.sub.1 -C.sub.4 alkyl).sub.2, ##STR2## or (b) a 5- or 6-membered aromatic heterocyclic group which may be benzo-fused and substituted by 1 or 2 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl and halo-(C.sub.1 or C.sub.2 alkyl), said heterocyclic group being attached to the nitrogen atom of the piperazine ring by a carbon atom;andR.sup.2 is H or CH.sub.3 ; or an O-ester or O-ether thereof which is a C.sub.2 -C.sub.4 alkanoyl or benzoyl ester, or a C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or phenyl ether, said phenyl and benzoyl groups of said O-esters and O-ethers may be substituted by one or two substituents each selected from C.sub.1 -C.sub.4 alkyl, halo and halo-(C.sub.1 or C.sub.
Abstract: Improved pharmaceutical salts of amlodipine, particularly the besylate salt, and pharmaceutical compositions thereof. These salts find utility as anti-ischaemic and anti-hypertensive agents.
Abstract: Compounds of the formula ##STR1## where HET is a heterocyclic group, n is an integer of 0 to 2 and R.sup.1 is hydrogen or lower alkyl are protease inhibitors use as anti-plasmin and anti-thrombin agents.
Abstract: Polypeptides and derivatives thereof containing homocyclostatine and cyclostatine are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.
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:
July 11, 1988
Date of Patent:
August 1, 1989
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Peter E. Cross, Michael J. Fray, Kenneth Richardson
Abstract: Compounds of the formula: ##STR1## where R is substituted phenyl, R.sup.1 is alkyl or pyridyl, R.sup.2 is hydrogen, R.sup.3 is alkoxy, alkylamino, hydroxy or benzyloxy, Y is alkylene and X is heterocyclic as antiallergic and antiinflammatory agents.
Type:
Grant
Filed:
May 24, 1988
Date of Patent:
July 25, 1989
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Michael J. Fray, 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:
December 7, 1987
Date of Patent:
May 30, 1989
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:
October 23, 1987
Date of Patent:
March 21, 1989
Assignee:
Pfizer Inc.
Inventors:
Dennis J. Hoover, Robert L. Rosati, Ronald T. Wester