Abstract: 1-Phenylquinazoline-1H,3H-2,4-diones and 1-phenylpyrido-[2,3d]-pyrimidine-1H,3H-2,4-diones, their esters and acid addition salts, and pharmaceutical compositions containing such compounds have antidepressant, anti-inflammatory and analgesic activity.
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: 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: Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.
Abstract: 1,3,-Dicarboxamidooxindoles as antiinflammatory agents prepared by reaction of the 1-carbamoyloxindole with an isocyanate or by aminolysis of the corresponding alkyl 1-carbamoyloxindole-3-carboxylate.
Abstract: The present invention relates to certain compounds of the formula ##STR1## wherein the broken line is a bond or no bond, and the pharmaceutically acceptable cationic salts thereof having utility as hypoglycemic and anti-atherosclerosis agents, methods for their use and pharmaceutical compositions containing them.
Abstract: A new sulfur-containing polypeptide antibiotic produced by the hydrolysis of thiosporamicin (CP-46,192) is useful for the improving feed utilization efficiency in poultry and swine.
Type:
Grant
Filed:
November 20, 1986
Date of Patent:
November 15, 1988
Assignee:
Pfizer Inc.
Inventors:
Eugene F. Fiese, Charles E. Moppett, Wendell W. Windisch
Abstract: A series of novel heterocyclic-substituted 1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one compounds have been prepared, including their pharmaceutically acceptable salts, wherein the heterocyclic ring moiety is an optionally substituted 5- or 6-membered aromatic heterocyclic group attached to the 6-, 7-, 8- or 9-positions of the aforesaid tetrahydroquinaxolinone ring. These particular compounds are useful in therapy as highly potent inotropic and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 7-(2,4-dimethylimidaxol-1-yl)-9-methyl-1,2,4,5,-tetrahydroimidazo (2,1-b)quinazolin-2-(1H)-one, 3,9-dimethyl-7-(2,4-dimethylimidazol-1-yl) -1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one and 9-methyl-7 -(1,2,4-triazol-4-yl)-1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-on e, respectively. Methods for preparing these compounds from known starting materials are provided.
Abstract: Aqueous gel-forming compositions useful for improving oil recovery from subterranean hydrocarbon-containing reservoirs are prepared by reacting an aminoalkylated polyacrylamide with an aldehyde, dialdehyde or derivative thereof in aqueous medium. These compositions are particularly effective in reducing excessive water encroachment at producer wells.
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: 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 an Y is an alkali metal.
Abstract: An efficient process for converting readily available 4-acetoxy-2-azetidinones to allyl 2-thioxopenam-3-carboxylates, intermediates useful for the synthesis of penem antibiotics.
Abstract: A novel three-step process for preparing 4-(3,4-dichlorophenyl)-4-phenylbutanoic acid is disclosed, which involves (1) reducing 4-(3,4-dichlorophenyl)-4-ketobutanoic acid to 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid; (2) then converting the intermediate hydroxy acid formed in the first step to 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone, and (3) thereafter reacting the resulting gamma-butyrolactone compound with benzene in a Friedel-Crafts type reaction to form the desired final product. The latter compound is known to be useful as an intermediate leading to cis-(1S)(4S)- -N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine (sertraline), which is known to be a preferred anti-depressant agent in the field of medicinal chemistry. The aforementioned 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone and 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid are both novel compounds.
Type:
Grant
Filed:
June 11, 1987
Date of Patent:
October 11, 1988
Assignee:
Pfizer Inc.
Inventors:
George J. Quallich, Michael T. Williams
Abstract: A series of novel, macrocyclic polyether compounds. The macrocycles have a 21-membered ring, containing six oxygen atoms, and they have a carboxy group (or a salt thereof) directed towards the interior of the ring. Administration of the compounds of the invention to ruminant animals (e.g. cattle and sheep) modifies their digestive fermentation processes such that the volatile fatty acids produced in the rumen contain a higher proportion of propionates rather than acetates, thereby increasing the efficiency of feed utilization in said ruminant animals. Additionally, the compounds of the invention show antibacterial activity in vitro against certain gram-positive microorganisms.
Abstract: Antibacterial compounds have the formula ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically aceptable cation, or alkyl; A is CH, CF, CCl or N; Y is alkyl, haloalkyl, cyclopropyl, vinyl, methoxy, N-methylamino, p-fluorophenyl, p-hydroxyphenyl or p-aminophenyl; or A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five to seven membered ring which is optionally substituted; and R.sup.2 is a bridged-diazabicycloalkyl group.
Abstract: Certain 2-azacycloalkylthio-2-penem-3-carboxylic acid compounds are useful as antibacterials for treating mammals and have the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R is ##STR2## A is alkylene having 2-4 carbon atoms, alkylene having 2-4 carbon atoms wherein a carbon atom has an oxo substituent or alkylene having 2-4 carbon atoms wherein a methylene is replaced by oxygen, S(O).sub.m, or N--R.sub.3 ;B is carbonyl, thiocarbonyl, methylene or imine;R.sub.1 is hydrogen or forms an ester group which is hydroyzed in vivo;R.sub.2 is hydrogen, formyl, alkylcarbonyl, N-alkylaminocarbonyl, N-alkylaminosulfonyl, aminosulfonyl, aminocarbonyl, alkoxycarbonyl having 2-5 carbon atoms, alkylsulfonyl, alkyl, or alkyl substituted by aminocarbonyl, alkyl--S(O).sub.m --, hydroxyl, amino, alkylcarbonylamino, formamido or alkylsulfonylamino, wherein each alkyl has 1-4 carbon atoms;R.sub.
Abstract: Aqueous gel-forming compositions are prepared by reacting for 1-10 hours at 50.degree.-95.degree. C., melamine, formaldehyde and a sulfurous acid salt with the optional addition of a gel-modifying agent and/or a gelling agent which is added to the composition immediately prior to use.
Type:
Grant
Filed:
June 20, 1985
Date of Patent:
September 20, 1988
Assignee:
Pfizer Inc.
Inventors:
Clifford N. Meltz, Gordon D. Gruetzmacher, Ping W. Chang