Abstract: A process for production of a 2-azetidinone-1-oxoacetate of the formula ##STR1## useful as an intermediate for preparation of 2-SR.sup.2 -substituted-2-penem-3-carboxylate andtibacterial agents;R is a conventional hydroxy protecting group, R.sup.1 is certain carboxy protecting groups and ##STR2## and m and n are each 0, 1 or 2; which comprises contacting a corresponding (2-oxo-1-axetidinyl)-N-2-hydroxyacetate ester of the formula ##STR3## with manganese dioxide.
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: Purified diisocyanate polyetherurethane prepolymers and process therefor. Polyetherurethane urea polymers prepared by mixing said prepolymers with an aqueous solution of an amino, ureido or hydroxy substituted amine or a like-substituted alpha-amino acid, and a method of using same as a space filling adhesive sealant in surgery.
Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.
Type:
Grant
Filed:
March 27, 1986
Date of Patent:
April 19, 1988
Assignee:
Pfizer Inc.
Inventors:
Michael R. Johnson, Lawrence S. Melvin, Jr.
Abstract: Process and intermediates for the conversion of 3R,4R-4-acetoxy-3-[1R-1-(silyloxy)ethyl]-2-azetidinones to antibacterial 5R,6S-6-(1R-1-hydroxyethyl)-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids, and the pharmaceutically-acceptable salts and pivaloyloxymethyl esters thereof.
Abstract: Hypoglycemic 5-[1-(5,6,7,8-tetrahydro-2-napthyl-; 1,2,3,4-tetrahydro-6-quinolyl-; 2-indanyl-; and 2-indolyl)alkyl]thiazolidine-2,4-dione derivatives, pharmaceutically acceptable salts thereof, and a method for their use in the treatment of hyperglycemic mammals.
Type:
Grant
Filed:
June 26, 1987
Date of Patent:
April 19, 1988
Assignee:
Pfizer Inc.
Inventors:
James F. Eggler, Gerald F. Holland, Michael R. Johnson, Robert A. Volkmann
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: 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 series of novel polypeptide derivatives, containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, which are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Particularly valuable precursors for many of these compounds are certain other 5-amino-2,5-disubstituted-4-hydroxypentanoic acid derivatives.
Type:
Grant
Filed:
April 30, 1986
Date of Patent:
March 8, 1988
Assignee:
Pfizer Inc.
Inventors:
Edward F. Kleinman, Robert L. Rosati, Jasjit S. Bindra
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: Certain trans-3-[3-(3-hydroxy-2-piperidyl)-2-oxopropyl]thieno[3,2-d]pyrimidin-4(3H )-one and furo[3,2-d]pyrimidin-4(3H)-one derivatives, a method of using same as anticoccidial agents, intermediates therefor, and a process for certain intermediates therefor.
Abstract: Certain 2-substituted-2-penem-3-carboxylic acid compounds and pharmaceutically-acceptable salts thereof can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization and addition of an electrophilic sulfur compound followed by halogenation and ring closure. The corresponding desulfurized and halogenated olefinic intermediates are disclosed.
Abstract: In the synthesis of biotin and decarboxybiotin, a more direct method for the conversion of 1,3-diacyl-4-(bromomethyl)-5-[(5-alkoxycarbonylpentanoyl) or hexanoyl]-4-imidazolin-2-ones to 1,3-diacyl-4-[(4-alkoxybutanoyl) or pentanoyl]-1H,3H-thieno(3,4-b)imidazol-2-one via the Bunte salt of the formula ##STR1## wherein R is (C.sub.1 -C.sub.5)alkanoyl or (C.sub.2 -C.sub.5)alkoxycarbonyl, X is methyl or (C.sub.2 -C.sub.5)alkoxycarbonyl and Y is an alkali metal.
Abstract: Antibiotic 19-epi-dianemycin, process for its preparation by fermenting a new strain of Streptomyces hygroscopicus, and isolation from the fermentation broth; and its use as an anticoccidial agent and antibacterial agent against gram-positive bacteria.
Type:
Grant
Filed:
November 17, 1986
Date of Patent:
November 17, 1987
Assignee:
Pfizer Inc.
Inventors:
Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, John C. Ruddock, Junsuke Tone
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: An improved process for the preparation of the chloromethyl ester of sulbactam (chloromethyl penicillanate 1,1-dioxide), an intermediate in the synthesis of sultamicillin (the mixed methanediol ester of sulbactam and ampicillin).
Abstract: Chiral sorbinil intermediates of the formula ##STR1## wherein R is hydrogen or benzyloxycarbonyl and Y is hydroxy or amino, processes therefor, and processes for the conversion thereof to sorbinil.
Abstract: Hypoglycemic 2,3-dihydro-5-benzo[b]furanyl-2,3-dihydro-5-benzo[b]thienyl-, 3,4-dihydro(2H)-6-benzopyranyl- and 6-thiochromanyl-thiazolidine-2,4-diones and pharmaceutically acceptable salts thereof, method for their use in treatment of hyperglycemic animals and pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 29, 1986
Date of Patent:
October 27, 1987
Assignee:
Pfizer Inc.
Inventors:
James F. Eggler, Gerald F. Holland, Mickael R. Johnson, Robert A. Volkmann
Abstract: 1,1-Di(p-fluorophenyl)urea, 2-carbobenzoxy-8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4, 3-b]indole, an efficient process for converting the former to the latter, further comprising conversion of the latter to 8-fluoro-5-(p-fluorophenyl)-2-[4-(p-fluorophenyl)-4-hydroxybutyl)]-2,3,4,5 -tetrahydro-1H-pyrido[4,3-b]indole (flutroline) or to 8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (an alternative flutroline intermediate).