Abstract: Dihydropyridine anti-ischaemic and anti-hypertensive agents of the formula: ##STR1## and their pharmaceutically acceptable salts; wherein R is aryl or heteroaryl; R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 or 2-methoxyethyl; n is 1 or 2; m is 1, 2 or 3; X is a 5 or 6 membered aromatic heterocyclic group which is linked to the adjacent alkoxymethyl group by a ring carbon atoms thereof; and Z is a group--NR.sup.3 R.sup.4 or a 5 to 6 membered nitrogen containing heterocyclic group; where R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; R.sup.4 is H, C.sub.1 -C.sub.4 alkyl, CO(C.sub.1 -C.sub.4 alkyl), COCF.sub.3, CONR.sup.5 R.sup.6, SO.sub.2 (C.sub.1 -C.sub.4 alkyl) or a heterocyclic or SO.sub.2 -heterocyclic group, wherein the heterocyclic group is optionally substituted; R.sup.5 and R.sup.6 and each independently H or C.sub.1 -C.sub.4 alkyl or taken together with the nitrogen atom to which they are attached, they form a pyrrolidinyl, piperidyl, morpholino, piperazinyl or N-(C.sub.1 -C.sub.
Type:
Grant
Filed:
January 16, 1985
Date of Patent:
October 22, 1985
Assignee:
Pfizer Inc.
Inventors:
David Alker, Peter E. Cross, Simon F. Campbell
Abstract: A new polyether antibiotic has been isolated from fermentations of a new microorganism of the genus Streptomyces. This new microorganism is designated as N478-13 and it has ben named Streptomyces routienii Huang sp. nov., (ATCC 39446). The new antibiotic exhibits antibacterial activity against a variety of gram-positive bacteria; it can be used to control swine dysentery; and it promotes increased efficiency of feed utilization (i.e. promotes increased growth) in swine and ruminants.
Type:
Grant
Filed:
November 7, 1983
Date of Patent:
October 15, 1985
Assignee:
Pfizer Inc.
Inventors:
Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
Abstract: 1,4-Dihydropyridine derivatives of the formula ##STR1## and their pharmaceutically acceptable acid addition salts; where:R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or2-methoxyethyl;Y is --(CH.sub.2).sub.2 --, --CH.sub.2).sub.3 --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --;R.sup.3 is ##STR2## , and pharmaceutical compositions containing such compounds, have utility as anti-ischaemic and antihypertensive agents.
Type:
Grant
Filed:
September 1, 1983
Date of Patent:
October 15, 1985
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs
Abstract: Diamidines of the formula ##STR1## wherein X is a propylene, isobutylene, guanidine, pyrrole, tetrazole, imidazole or substituted imidazole group; and 2-[4-(2-imidazolinyl)phenyl]-6-(2-imidazolinyl)indole, are useful in the treatment of certain protozoal infections in mammals, particularly in cattle.
Abstract: An antibiotic complex, consisting of one major and two minor components, has been isolated from fermentation of a new Streptomyces culture. The components from the complex are three new macrolides which are active as antibacterial agents against certain gram-negative and gram-positive microorganisms.
Type:
Grant
Filed:
December 16, 1983
Date of Patent:
September 24, 1985
Assignee:
Pfizer Inc.
Inventors:
Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
Abstract: A series of novel 4-piperidino-6,7-dimethoxyquinazoline compounds, further substituted on the piperidino group, and the pharmaceutically-acceptable salts thereof, possess cardiac stimulating activity in mammals. They are useful in the curative or prophylactic treatment of cardiac conditions, in particular heart failure.
Type:
Grant
Filed:
July 31, 1984
Date of Patent:
September 17, 1985
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Albert A. Jaxa-Chamiec, David A. Roberts
Abstract: 1,4-Dihydropyridine derivatives of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts; where R is aryl or heteroaryl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or2-methoxyethyl;Y is --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --;R.sup.3 is hydrogen or an organic substituentare useful in treating or preventing heart conditions or hypertension.
Type:
Grant
Filed:
September 1, 1983
Date of Patent:
September 3, 1985
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs
Abstract: 6-alpha- and 6-beta-(Aminomethyl)penicillanic acid, 1,1-dioxide esters which are hydrolyzable under physiological conditions, particularly those wherein the ester radical is 1H-isobenzofuran-3-on-1-yl or (5-methyl-1,3-dioxol-2-on-4-yl)methyl, and an improved process and intermediates used in their synthesis.
Abstract: Combination of 6-methyl-1,2,3-oxathiazin-4(3H)-one-2,2-dioxide (acesulfame) with 3-(L-aspartyl-D-alaninamido)-2,2,4,4-tetramethylthietane masks the bitter taste of the oxathiazine and at the same time provides synergistic sweetness over a range of concentrations.
Type:
Grant
Filed:
September 6, 1983
Date of Patent:
August 20, 1985
Assignee:
Pfizer Inc.
Inventors:
Charles R. Stephens, Jr., Anibal Torres
Abstract: A process for the preparation of 1,1-dioxopenicillanoyloxymethyl 6-beta-aminopenicillanate which comprises reacting 1,1-dioxopenicillanoyloxymethyl 6-phenylacetamidopenicillanate or the corresponding phenoxyacetamidopenicillanate under anhydrous conditions with a halogenating agent in the presence of a reaction inert solvent to form an intermediate imino halide, addition of a primary alcohol having from one to four carbon atoms to convert the imino halide to an imino ether and subsequent hydrolysis to give the desired product.
Abstract: Compounds of the formula ##STR1## wherein X is halo and R is an aryl group and their pharmaceutically acceptable salts are useful antifungal agents in animals, including man.
Abstract: 2-[2-Hydroxy-4-(substituted)phenyl]piperidines and derivatives thereof of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is H, benzyl or certain acyl groups, R.sub.2 is H, certain alkyl, alkenyl, alkynyl, hydroxyalkyl, acyl or alkylsulfonyl groups; R.sub.3 is H.sub.2, O, ##STR2## and Z is (C.sub.1 -C.sub.13)alkylene or -(alk.sub.1).sub.m -O-(alk.sub.2).sub.n - where each of (alk.sub.1) and (alk.sub.2) is (C.sub.1 -C.sub.13)alkylene, provided that the number of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 13; each of m and n is 0 or 1; and W is H, pyridyl or optionally substituted phenyl; their use as analgesic agents, intermediates therefor and processes for their preparation.
Type:
Grant
Filed:
March 14, 1983
Date of Patent:
July 16, 1985
Assignee:
Pfizer Inc.
Inventors:
Michael R. Johnson, Lawrence S. Melvin, Jr.
Abstract: Antibacterial 4"-epi-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A, pharmaceutically-acceptable salts thereof, pharmaceutical compositions comprising antibacterially-effective amounts thereof, a method of treatment of bacterial infections with antibacterially effective amounts thereof, and intermediates for the synthesis thereof from erythromycin A.
Abstract: A process for grafting a hydrophilic polymer of a carboxylic acid or a salt thereof onto the surface of a natural rubber article by contacting said article in reaction inert solvent with a vinyl carboxylic acid anhydride and initiator, and subsequent washing and hydrolysis of anhydride groups to carboxylate groups and an article when prepared by the invention process.
Abstract: Salts of readily hydrolyzable esters of 6-alpha-(aminomethyl)penicillanic acid 1,1-dioxide and (a) prodrug forms of ampicillin and amoxicillin or (b) ampicillin and amoxicillin and a dibasic acid are readily absorbed following oral adminstration, and are useful in treating bacterial infections.
Abstract: Certain novel 9-deoxo-4"-deoxy-4"-amino-9a-aza-9a-homoerythromycin A derivatives; a method of treating a bacterial infection in a mammalian subject using the novel erythromycin A derivatives; pharmaceutical compositions containing the novel erythromycin A derivatives; and intermediates and processes for making the novel erythromycin A derivatives.
Abstract: Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is 5-chloro-2-pyridyl, phenyl or phenyl substituted by from 1 to 3 substituents selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)-alkyl and (C.sub.1 -C.sub.4)alkoxy; X is a halogen atom, and n is zero or an integer from 1 to 5, method for their use in combatting fungal infections in plants, seeds and animals, including humans, and pharmaceutical and agricultural compositions containing them.
Abstract: Certain novel 9-deoxo-4"-deoxy-4"-amino-9a-aza-9a-homoerythromycin A derivatives; a method of treating a bacterial infection in a mammalian subject using these novel erythromycin A derivatives; pharmaceutical compositions containing the novel erythromycin A derivatives; and intermediates and processes for making the novel erythromycin A derivatives.
Abstract: A series of 2-guanidino-4-heteroarylthiazoles, wherein the heteroaryl substituent is selected from thiazolyl, triazolyl, imidazolyl, and 2-alkyl, 2-amino and 2-carboxamido derivatives thereof, are disclosed. The novel compounds have activity as antisecretory agents and histamine H.sub.2 antagonists and are useful for the treatment of gastric hyperacidity and peptic ulcers. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention and a method of using the compounds in the treatment of gastric hyperacidity and peptic ulcers. Novel intermediates useful in the preparation of the novel antisecretory compounds are also described.
Type:
Grant
Filed:
March 27, 1984
Date of Patent:
April 9, 1985
Assignee:
Pfizer Inc.
Inventors:
John L. LaMattina, Christopher A. Lipinski
Abstract: Compounds of the formula ##STR1## wherein R is thienyl, mono-, di- and trihalothienyl, furyl, 2-benzothiazolyl, pyridyl or chloropyridyl and their pharmaceutically acceptable salts are useful agents for combating fungal infections in animals, including humans.