Abstract: A novel process is described for preparation of biotin comprising preparation of substituted 3H, 5H-imidazo[1,5c]tetrahydro thiazoles by contacting the boron trifluoride adduct of an appropriate thiazoline with the metallic derivative of an ester enolate, reducing the ester, hydrolyzing the thiazolidine moiety and hydrolyzing or oxidizing the resultant compound. Intermediates obtained in the preparation of biotin by the above process and alternate procedures for preparing said intermediates are also presented. A novel process for preparation of d-biotin is also given.
Abstract: Solutions of indolmycin in a pharmaceutically-acceptable solvent are of special value in the treatment of susceptible bacterial infections in mammals, particularly swine.
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: 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: An improved antiinflammatory composition and method of treating inflammation which employs a combination of antiinflammatory piroxicam, or a pharmaceutically acceptable salt thereof, with analgesic acetaminophen, antidepressant doxepin, bronchodilator pirbuterol, minor tranquilizer diazepam, or antihypertensive trimazosin.
Type:
Grant
Filed:
December 12, 1986
Date of Patent:
August 23, 1988
Assignee:
Pfizer Inc.
Inventors:
Thomas C. Crawford, Stanley L. Keely, David L. Larson, Joseph G. Lombardino, James J. Maciejko
Abstract: Spiro-succinimides are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro- compounds and a method of treating diabetic complications are also disclosed.
Abstract: Variously substituted trans-3-[3-(3-hydroxypiperid-2-yl)-2-oxopropyl]quinazolin-4-(3H)-ones, a method of controlling or preventing coccidiosis in poultry therewith, intermediates therefor, and a process for the preparation of certain intermediates therefor.
Abstract: A process for the preparation of penicillanic acid 1,1-dioxide and esters thereof readily hydrolyzable in vivo, which comprises oxidation of a 6,6-dihalopenicillanic acid, or an ester thereof readily hydrolyzable in vivo, to the corresponding 6,6-dihalopenicillanic acid 1,1-dioxide or ester thereof, followed by dehalogenation (e.g. by hydrogenolysis). The 6,6-dihalopenicillanic acid 1,1-dioxides and esters thereof readily hydrolyzable in vivo are novel intermediates. Penicillanic acid 1,1-dioxide, and esters thereof readily hydrolyzable in vivo, are known compounds which are useful as beta-lactamase inhibitors and for enhancing the effectiveness of certain beta-lactam antibiotics (e.g. the penicillins) in the treatement of bacterial infections in mammals, particularly humans.
Abstract: A two-step process for the synthesis of certain indol-2(3H)-ones from indoles, and the 3,3-dibromoindol-2(3H)-ones which are intermediates in that process.
Abstract: A series of novel 2-substituted 4-amino-6,7-dimethoxyquinoline derivatives have been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as highly potent antihypertensive agents. Preferred member compounds include 4-amino-2-[4-(2-furoyl)piperazin-l-yl]-6,7-dimethoxyquinoline, 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquin oline and 4-amino-6,7-dimethoxy-2-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl)qu inoline, respectively. Methods for preparing these compounds from known starting materials are provided.
Abstract: This invention relates to the use of doxazosin or a pharmaceutically acceptable acid addition salt thereof as an agent for retarding the development of atherosclerosis in a mammal, especially for reducing atherosclerotic plaque involvement and for retarding and reducing both the fibrosis and lipid deposition of developing atherosclerotic plaques associated with atherosclerosis.
Abstract: A method for improving the mobility and pipeline transport of a viscous crude oil by forming an oil-in-water emulsion with said oil and from 10 to 80% by weight of water in the presence of 100 to 1500 parts by weight of a surfactant blend per million parts by weight of said emulsion, said blend comprising from 15 to 85 parts by weight of an anionic or amphoteric surfactant (A) selected from those of the formulae Ar(OCH.sub.2 CH.sub.2).sub.n OSO.sub.3 H, ##STR1## a sodium and ammonium salt thereof, and from 85 to 15 parts by weight of a nonionic surfactant selected from (B) of the formula Ar(OCH.sub.2 CH.sub.2).sub.p OH or (C) of the formula ##STR2## the latter having an HLB value of from 10 to 20; where Ar is octylphenyl or nonylphenyl,n is 2 to 10,p is 10 to 100,a is 10 to 40, b is 15 to 55, c is 10 to 40,R.sup.1 is C.sub.8 to C.sub.18 alkyl andR.sup.2 is C.sub.12 to C.sub.18 alkyl;and said emulsion.
Abstract: Hypoglycemic 5-chromanyl, 2,3-dihydro-5-benzo[b]-furanyl, 5-pyridyl, 5-quinolyl, 5-pyrrolyl, 5-indolyl, 5-thiazolyl, 5-oxazolyl, 5-isothiazolyl and 5-isoxazolyl oxazolidine-2,4-diones and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.
Abstract: Particulate calcium carbonate or iron oxide pretreated with a fatty acid such as stearic acid or oleic acid is added to a cementitious product to improve its strength and resistance to water absorption and penetration. Dry, aqueous and nonaqueous methods of addition are employed.
Abstract: Certain novel 2-oxindole compounds, having an acyl substituent at both the 1-position and the 3-position, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and antiinflammatory agents in mammalian subjects. These 1,3-diacyl-2-oxindole compounds are of particular value for acute administration for ameliorating pain in human patients recovering from surgery or trauma, and also for chronic administration to human subjects for alleviating the symptoms of chronic diseases such as rheumatoid arthritis and osteoarthritis.
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: The present invention concerns a novel water-insoluble, hydrophilic, pressure-sensitive adhesive that has a number of unique characteristics including being elastomeric and ultraconformable. This adhesive includes an irradiation cross-linked synthetic organic polymer having a three-dimensional matrix, and an adhesive plasticizer. The plasticizer includes a substantially non-volatile elasticizer. The adhesive is useful either as a coating on a supporting web-like substrate or as a self-supporting layer. Also provided are various articles made using the adhesive such as a bandage or ostomy device, a method of making the adhesive, and methods of using the adhesive.In one embodiment, the adhesive is electroconductive, and is useful for attaching an electrically conductive member of an electrode to a selected surface such as mammalian tissue. Also provided is an electrode having a layer of this adhesive, and a method of adhering this electrode to mammalian tissue.
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: A series of novel peptide and polypeptide derivatives containing statine or derivatives thereof (e.g., aminostatine, cyclostatine) are disclosed that are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Of particular interest are compounds possessing the N-terminal sequence -Pro-Phe-His-Sta-Lys with the terminal proline nitrogen bonded to an amino-protecting acyl moiety or compounds possessing the N-terminal sequence -R-Phe-His-Sta-Lys- wherein R represents an amino protecting acyl group.
Type:
Grant
Filed:
March 10, 1986
Date of Patent:
June 7, 1988
Assignee:
Pfizer Inc.
Inventors:
Jasit S. Bindra, Edward F. Kleinman, Robert L. Rosati