Abstract: A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is amino, hydroxy, alkoxy, phenoxy or benzyloxy, useful in the treatment of hypertension, angina, renal impairment or acute renal failure.
Type:
Grant
Filed:
April 28, 1988
Date of Patent:
February 21, 1989
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Michael J. Humphrey, Alan Stobie
Abstract: Compounds of the formula: ##STR1## where R is 2-substituted phenyl said substituent being chloro, bromo, cyano, methyl, methylthio, methylsulfonyl, trifluoromethyl, hydroxy, methoxy or benzyloxy; R.sup.1 is hydrogen, lower alkyl, pyridyl, thiazolyl, isoxazolyl, thiadiazdyl or thiazdylmethyl; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydroxy, lower alkoxy, benzyloxy, amino, lower alkylamino or morpholino; Y is alkylene having two to six carbon atoms; and X is benzimidazolyl optionally substituted by lower alkyl, chloro or trifluoromethyl.
Type:
Grant
Filed:
October 30, 1987
Date of Patent:
January 31, 1989
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Michael J. Fray, Kenneth Richardson
Abstract: A device for zero order releasing of biologically active substances into a fluid medium comprising a cylindrical tablet or bolus covered with an impermeable wall or coating from which strips of said wall or coating have been removed.
Abstract: Antibacterial penicillins of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is a heterocyclic group and R is hydrogen, the residue of certian carboxy protecting groups or the residue of an ester group readily hydrolyzable in vivo having activity against resistant organisms.
Abstract: A triazole of the formula ##STR1## wherein R is phenyl substituted by difluoro, fluoro, dichloro or chloro and R' is phenyl substituted by chloro or fluoro are useful antifungal agents.
Type:
Grant
Filed:
November 14, 1985
Date of Patent:
August 30, 1988
Assignee:
Pfizer Inc.
Inventors:
Robert J. Bass, Kelvin Cooper, Kenneth Richardson
Abstract: Peptide components of formula 1, pharmaceutically acceptable base salts thereof, pharmaceutical compositions and their use as antiinfective agents ##STR1## where R.sub.1 is alkyl, cycloalkyl or cycloalkylmethyl; R.sub.2 is hydrogen or alkyl and R.sub.3 is hydroxy or an amino acid residu of the formula ##STR2## where X is hydrogen, alkyl or hydroxymethyl and n is an integer of 0 to 4 and R.sub.4 and R.sub.5 are alkyl, hydrogen, benzyl or cyclohexylmethyl.
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:
August 29, 1986
Date of Patent:
June 14, 1988
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, John R. Oscarson, Junsuke Tone, Hiroshi Maeda
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 5, 1986
Date of Patent:
March 22, 1988
Assignee:
Pfizer Inc.
Inventors:
David Alker, Simon F. Campbell, Peter E. Cross
Abstract: A process for preparing [1H]-isoindolin-1-one-3-carboxylic acid comprising the steps of (1) reacting phthalaldehydic acid in an alkanol with ammonia, (2) contacting the resulting solution with an alkali metal cyanide, (3) removing the alkanol, (4) adjusting the pH to 1.0, (5) heating the resulting reaction mixture until product formation is substantially complete and isolating the product.
Abstract: A pharmaceutical tablet which releases an initial burst of therapeutic agent and thereafter releases the agent at an essentially constant rate comprising an acid soluble therapeutic agent in an insoluble matrix, the tablet containing an acid insoluble, base soluble pharmaceutically acceptable component selected from polymers and fatty acids, a pharmaceutically acceptable organic acid and at least one pharmaceutically acceptable excipient, the component and the acid each being present in an amount of from about 1-25 percent by weight of the total composition.
Abstract: Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.
Abstract: Ketone containing 1-substituted oxindole-3-carboxamides as antiinflammatory agents prepared by reaction of the 1-substituted oxindole with an isocyanate or by aminolysis of the corresponding alkyl oxindole-3-carboxylate.
Abstract: Dihydropyridine anti-ischaemic agents of the formula: ##STR1## and their salts where R is aryl or heteroaryl, R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl, Y is --(CH.sub.2).sub.n -- where n is 2, 3, or 4 and is optionally substituted by 1 or 2 CH.sub.3 groups, and R.sup.3 is an optionally substituted 5- or 6-membered heterocyclic group attached to the adjacent N atom by a C atom, said group R.sup.3 being optionally fused to a further heterocyclic group or to a benzene ring.
Type:
Grant
Filed:
February 14, 1986
Date of Patent:
June 2, 1987
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs, John E. Arrowsmith
Abstract: Dihydropyridine Anti-ischaemic agents of the formula ##STR1## and their salts where R is aryl, R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl, Y is --(CH.sub.2).sub.n -- where n is 2, 3 or 4 and is optionally substituted by 1 or 2 methyl groups and R.sup.3 is pyrimidyl or di- or tetrahydropyrimidyl.
Type:
Grant
Filed:
February 14, 1986
Date of Patent:
April 28, 1987
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs, John E. Arrowsmith
Abstract: Compounds of the formula: ##STR1## where R is an optionally substituted aryl or heteroaryl group;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; and Y is --(CH.sub.2).sub.n -- where n is 2, 3 or 4, --CH.sub.2 CH(CH.sub.3)-- or --Ch.sub.2 C(CH.sub.3).sub.2 --; and their pharmaceutically acceptable salts.The compounds have utility as anti-ischaemic and antihypertensive agents and as synthetic intermediates to other dihydropyridine calcium antagonists.
Type:
Grant
Filed:
April 26, 1985
Date of Patent:
March 31, 1987
Assignee:
Pfizer Inc.
Inventors:
David Alker, Simon F. Campbell, Peter E. Cross
Abstract: Dihydropyridines of the formulae ##STR1## wherein R is chlorothienyl or mono- or disubstituted phenyl where said substituent is fluoro, chloro, bromo or trifluoromethyl; R.sup.1 and R.sup.2 are each alykl; R.sup.3 and R.sup.4 when taken separately are each hydrogen or alkyl; R.sup.3 and R.sup.4 when taken together with the nitrogen to which they are attached are piperidine or pyrrolidine; R.sup.5 is alkyl or 2-hydroxyethyl; R.sup.6 is hydrogen or methoxy; X and Z are each hydrogen or methoxy; Y is alkylene; R.sup.7 is chlorophenyl or trifluoromethyl-chlorophenyl; p is 0 or 1; and Q is CH or N are useful in the treatment of hypertension, heart failure and angina.
Type:
Grant
Filed:
June 5, 1985
Date of Patent:
March 3, 1987
Assignee:
Pfizer Inc.
Inventors:
John E. Arrowsmith, Simon F. Campbell, Peter E. Cross, Roger P. Dickinson
Abstract: Ketone containing 1-substituted oxindole-3-carboxamides as antiinflammatory agents prepared by reaction of the 1-substituted oxindole with an isocyanate or by aminolysis of the corresponding alkyl oxindole-3-carboxylate.
Abstract: Methods for preparing purified, decolorized polydextrose having a lower caloric value, higher pH and less color than presently available commercial material, and the use of said improved product in edible foodstuffs and beverages.