Abstract: Certain 7-beta-[2-(2-amino-4-thiazolyl)-(Z)-2-(chloromethylene acetamido]-3-[(substituted)methyl]-ceph-3-em-4-carboxylic acids, pharmaceutically-acceptable salts thereof and conventional in vivo hydrolyzable esters thereof are valuable as broad spectrum antibacterial agents, particularly useful for the treatment of bacterial infections in man and other mammals.
Abstract: A series of bridged bicyclic imides having a 4-[4-(3-benzisothiazolyl)-1-piperazinyl]butyl group attached to the imide nitrogen are useful antipsychotic agents.
Abstract: Improved processes for preparation of racemic, cis- and optically active (3S,4R)-3[1(R)-t-butyl-dimethylsilyloxy)-ethyl]-4-[1-oxo-3-thiolanylthio(t hiocarbonyl)thio]azetidin-2-ones, process improvements for certain intermediates therefor and a novel intermediate for said racemic, cis- and trans-compounds, which compounds are useful as intermediates for antibacterial 5R,6S-6-[1(R)-hydroxyethyl]-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids and the pharmaceutically-acceptable salts and the pivaloyloxymethyl esters thereof.
Type:
Grant
Filed:
January 18, 1991
Date of Patent:
December 24, 1991
Assignee:
Pfizer Inc.
Inventors:
Frank R. Busch, Robert W. Dugger, George J. Quallich
Abstract: An antibiotic compound of the formula: ##STR1## is an antiparasitic agent active against insect pests, acari, free living nematodes and endo- and ectoparasites. It is prepared by fermentation using the microorganism Streptomyces griseochromogenes ATCC 53928.
Type:
Grant
Filed:
July 25, 1990
Date of Patent:
December 17, 1991
Assignee:
Pfizer Inc.
Inventors:
Yasuhiro Kojima, Hiroshi Maeda, Satoshi Nishiyama, David A. Perry
Abstract: This invention relates to the use of certain derivatives of 5-hydroxy and 5-methoxy 2-aminopyrimidines of the formula ##STR1## and the pharmaceutically-acceptable salts thereof, wherein R.sup.1 is H or CH.sub.3 ; R.sup.2 is (C.sub.3 -C.sub.15) straight chain alkyl or (C.sub.7 -C.sub.20)phenylalkyl which may be substituted in the phenyl by one or two fluoro or chloro substituents; and R.sup.3 is H or CH.sub.3 to inhibit interleukin-1 production in a mammal. This invention also relates to the use of such compounds for treating interleukin-1 mediated disorders and dysfunctions such as bone and connective tissue metabolism disorders and immune dysfunction in a mammal. The methods of this invention comprise administering an interleukin-1 production inhibiting amount of the compounds and salts of this invention to such a mammal.
Abstract: The invention provides compounds of the formula: ##STR1## wherein k is 1, 2 or 3;m is 1, 2 or 3;n is 1, 2 or 3;p is 0, 1 or 2;X is O, S or a direct link, with the proviso that when X is O or S, n is 2 or 3;R.sup.1 is H or C.sub.1-C.sub.4 alkyl; andR.sup.2 is an optionally substituted phenyl or heteroaryl group; andpharmaceutically acceptable salts thereof.These compounds are useful for the treatment of motility disorders, particularly those of the gut such as irritable bowel syndrome.
Type:
Grant
Filed:
May 23, 1990
Date of Patent:
December 10, 1991
Assignee:
Pfizer Inc.
Inventors:
David Alker, Robert J. Bass, Peter E. Cross
Abstract: Certain 6-aryl- or 6-heteroaryl- alkylaminobenzoxazolones, and their pharmaceutically-acceptable salts, are dual inhibitors of lipoxygenase and cyclooxygenase enzymes, and so are useful as antiallergy and antiinflammatory agents.
Type:
Grant
Filed:
July 18, 1990
Date of Patent:
December 10, 1991
Assignee:
Pfizer Inc.
Inventors:
Fumitaka Ito, Takashi Mano, Masami Nakane
Abstract: Process for transformation of Yarrowia lipolytica, vectors useful therefor comprising DNA of a microbial vector and chromosomal DNA of Y. lipolytica and transformants comprising said vectors in E. coli and Y. lipolytica, and integrative shuttle vectors for Escherichia-Yarrowia transgeneric cloning. Said vectors or subclones thereof enable creation of Y. lipolytica cloning vectors into which specific or random segments of DNA can be inserted and the resulting vectors used to transform a suitable host microbe, especialy Y. lipolytica, to improve the fermentation characteristics thereof and hence their industrial utilization.The methodology described permits the cloning of genes from a gene library of Y. lipolytica by complementation with an integrating vector.
Abstract: Intermediates useful in the synthesis of dihydropyridine platelet activating factor antagonists of the formula ##STR1## where R is phenyl or substituted phenyl; R.sup.3 is lower alkyl; Y is 1,4-phenylene and X is a benzimidazol-1-yl.
Type:
Grant
Filed:
May 1, 1990
Date of Patent:
December 3, 1991
Assignee:
Pfizer Inc.
Inventors:
Melvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
Abstract: This invention relates to novel 3-(1-substituted-pyrazoyl)-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthease, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-(1-substituted-pyrazoyl-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel compounds useful as intermediates in the preparation of the 3-(1-substituted-pyrazoyl-2-oxindole derivatives of this invention and to a process for the preparation of the 3-(1-substituted-pyrazoyl)-2-oxindole derivatives.
Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces sp. ATCC 53862. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.
Type:
Grant
Filed:
January 28, 1991
Date of Patent:
November 12, 1991
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, James R. Hauske, Gloria J. Kostek, Hiroshi Maeda, Junsuke Tone
Abstract: Platelet activating factor antagonists of formula (I): ##STR1## wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl(C.sub.1 -C.sub.4)alkoxy, fluoro(C.sub.1 -C.sub.4)alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring;R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C.sub.1 -C.sub.4 alkyl)piperazinyl or N-(C.sub.2 -C.sub.4 alkanoyl)-piperazinyl group;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.1 is CN, C.sub.3 -C.sub.7 cycloalkyl, aryl, heteroaryl or a C.sub.1 -C.sub.4 alkyl group substituted by one or more substituents selected from C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, aryl or heteroaryl;Z is selected from C.sub.1 -C.sub.6 alkoxy, aryl(C.sub.1 -C.sub.
Type:
Grant
Filed:
May 1, 1990
Date of Patent:
November 5, 1991
Assignee:
Pfizer Inc.
Inventors:
Kelvin Cooper, Michael J. Fray, Kenneth Richardson, John Steele
Abstract: Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond; A and B are each independently CH or N, with the proviso that when A or B is N, the other is CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro; a pharmaceutically-acceptable cationic salt thereof; or a pharmaceutically-acceptable acid addition salt thereof when A or B is N.
Type:
Grant
Filed:
August 14, 1990
Date of Patent:
October 29, 1991
Assignee:
Pfizer Inc.
Inventors:
David A. Clark, Steven W. Goldstein, Gerald F. Holland, Bernard Hulin, James P. Rizzi
Abstract: Process for making antiinflammatory 3-aroyl-2-oxindole-1-carboxamides by reductive debromination or deiodination of 3-(bromo- or iodoaroyl)-2-oxindole-1-carboxamides.
Abstract: Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.
Type:
Grant
Filed:
August 4, 1989
Date of Patent:
October 22, 1991
Assignee:
Pfizer Inc.
Inventors:
James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
Abstract: Antiparasitic compounds of formula (I): ##STR1## The broken line at the 22-23 position representing an optional double bond and either R.sup.1 is H or OH and the double bond is absent or the double bond is present and R.sup.1 is absent; R.sup.2 is optionally substituted phenyl, or a group of formula (II): ##STR2## wherein X is O, S or --CH.sub.2 13 , abc and d are 0-2 and a+b+c+d.ltoreq.5R.sup.3 is H or MeR.sup.4 is H, OH or 4'-(alpha-L-oleandrosyl)-alpha-L-oleandrosyloxy.The compounds are prepared by fermentation of Streptomyces avermitilis in the presence of an N-alkanoyl cysteamine thioester containing R.sup.2.
Type:
Grant
Filed:
August 29, 1990
Date of Patent:
October 15, 1991
Assignee:
Pfizer Inc.
Inventors:
Christopher J. Dutton, Stephen P. Gibson, Nigel D. A. Walshe
Abstract: An apparatus for mixing and spraying a slurry. The apparatus comprises a housing including a channel. The channel is in fluid communication with an inlet at its upstream end and curves to an outlet at its downstream end. The outlet is in fluid communication with an air atomization nozzle. A mixing surface is capable of rotation with respect to the housing and the channel is open to the mixing surface.
Abstract: Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof, wherein R is 5-chloro-2-pyridyl, or phenyl optionally substituted by one to three substituents, each independently selected from F, Cl, Br, I, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy; R.sup.1 is CN, CSNH.sub.2 or CONR.sup.2 R.sup.3 where either(a) R.sup.2 is H or certain alkyl groups and R.sup.3 is H or certain alkyl, substituted alkyl, aralkyl, phenyl or cycloalkyl groups, or(b) R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached form a nitrogen heterocyclic group, optionally containing an oxygen atom or NR.sup.4 group, as a ring member and R.sup.4 is H, C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.4 alkanoyl or (C.sub.1 -C.sub.4 alkoxy)carbonyl;R.sup.5 and R.sup.6 are each H or CH.sub.