Abstract: Ketone containing 1-substituted oxindole-3-carboxamides as antiinflammatory agents prepared by reaction of the 1-substituted oxindole with an isocyanate or by aminolysis of the corresponding alkyl oxindole-3-carboxylate.
Abstract: N-(mono or disubstituted Phenoxyalkyl)imidazoles and the pharmaceutically acceptable acid addition salts thereof are able to selectively inhibit the action of the thromboxane synthetase enzyme without significantly inhibiting the action of the prostacycline synthetase or cyclooxygenase enzymes and are thus useful in the treatment of ischaemic heart disease, stroke, transient ischaemic attack, thrombosis migraine and the vascular complications of diabetes.
Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of an antiinflammatory agent (e.g. indomethacin or an oxicam) with a histamine-H.sub.2 antagonist selected from the group consisting of 2-guanidino-4-(4-imidazolyl)thiazole, 2-guanidino-4-(2-methyl-4-imidazolyl )thiazole, 2-(N-benzyl-N'-guanidino)-4-(2-methyl-4-imidazolyl)thiazole, 2-(N-pentyl-N'-guanidino)-4-(2-methyl-4-imidazolyl)thiazole and 2-guanidino-4-[2-(hexylamino)-4-imidazolyl]thiazole.
Abstract: 2-Guanidino-4-(2-methyl-4-imidazolyl)thiazole dihydrobromide and a one-pot, high yield process for its preparation from 2-methyl-4(or 5)-acetylimidazole.
Abstract: Processes and intermediates useful in the preparation of bronchodilator compounds of the formula ##STR1## wherein R is hydrogen, methyl or hydroxymethyl are described. Those compounds wherein R is H or CH.sub.3 have been found to have further utility as intermediates for pirbuterol (wherein R is hydroxymethyl).
Abstract: A Yarrowia lipolytia strain (PC-30827) ATCC 20688 which is utilized as a suitable host for cloning. The strain is a double auxotroph and requires medium supplemented with leucine and uracil for growth.
Abstract: A new acidic polycyclic ether antibiotic, CP-63,517, having the formula: ##STR1## and cationic salts thereof produced by submerged aerobic propagation of Streptomyces endus subsp. aureus, ATCC-39574, a new strain of microorganism isolated from a soil sample in Japan, a process for producing this antibiotic and methods for its use to improve feed utilization, promote growth of cattle and swine and to control coccidiosis.
Type:
Grant
Filed:
August 29, 1985
Date of Patent:
November 25, 1986
Assignee:
Pfizer Inc.
Inventors:
Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
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: Methods for preparing purified, decolorized polydextrose having a lower caloric value, higher pH and less color than presently available commercial material, and the use of said improved product in edible foodstuffs and beverages.
Abstract: Hypoglycemic 5-furyl and 5-thienyl derivatives of oxazolidine-2,4-dione and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; and intermediates useful in the preparation of said compounds.
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: Certain substituted-2-penem-3-carboxylic acid compounds, and pharmaceutically-acceptable salts thereof, can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization, followed by halogenation and ring closure. The corresponding desulfurized and halogenated intermediates are disclosed.
Abstract: Peptide-substituted heterocyclic compounds having the formula below, pharmaceutically acceptable salts thereof and intermediates therefor; processes for their preparation and use as immunostimulant and antiinfective agents. ##STR1## wherein R is a 5- or 6-membered N-containing heterocyclyl moiety which can have an additional hetero atom selected from N, S or O; R.sup.1 is hydrogen or (C.sub.1-4)alkyl; x is 0 or an integer from 1 to 5; and y is 0 or 1; provided that when y is 0, said N-containing heterocyclyl moiety is linked to the ##STR2## group at its N atom.
Abstract: Dihydropyridine derivatives of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts; wherein R is a substituted aryl group;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.3 alkyl;Y is --(CH.sub.2).sub.n -- where n is 2, or --CH.sub.2 CH(CH.sub.3)--; and Het is a 6-membered aromatic heterocyclic group attached to the adjacent oxygen atom by a carbon atom.The compounds have utility as anti-ischaemic and anti-hypertensive agents.
Type:
Grant
Filed:
June 5, 1985
Date of Patent:
October 21, 1986
Assignee:
Pfizer Inc.
Inventors:
David Alker, Simon F. Campbell, Peter E. Cross
Abstract: 1-substituted-1-haloaryl-1-('-[1H-1,2,4-triazol-1-yl]-cyclopropyl)-2-(1H-1, 2,4-triazol-1-yl)ethane compounds and pharmaceutical compositions thereof are useful in treating fungal infections in mammals and plants.
Type:
Grant
Filed:
May 24, 1985
Date of Patent:
October 21, 1986
Assignee:
Pfizer Inc.
Inventors:
Kenneth Richardson, Robert J. Bass, Kelvin Cooper
Abstract: 1,4-Dihydropyridine derivatives of the formula: ##STR1## wherein R is aryl or heteroaryl: R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; Y is --(CH.sub.2).sub.n --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --; n is 1 to 3; and X is a 5 or 6 membered nitrogen containing aromatic heterocyclic ring which may optionally be substituted by one or more C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, CN, --N(R.sup.3).sub.2, (CH.sub.2).sub.m CO.sub.2 H, (CH.sub.2).sub.m CO.sub.2 (C.sub.1 -C.sub.4 alkyl) or (CH.sub.2).sub.m CON(R.sup.3).sub.2 group wherein each R.sup.3 is independently H or C.sub.1 -C.sub.4 alkyl and m is 0 or 1; and their pharmaceutically acceptable acid addition salts, and pharmaceutical preparation containing such compounds, have utility as anti-ischaemic and antihypertensive agents.
Type:
Grant
Filed:
February 21, 1985
Date of Patent:
October 7, 1986
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs
Abstract: Compounds of the formula ##STR1## 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, 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; and R.sup.1 is H, Cl, phenyl, phenyl substituted by from 1 to 3 substituents each independently selected from F, Cl, Br, I and CF.sub.3 or a heterocyclic group linked to the adjacent CF.sub.2 group by a ring carbon atom; method for their use in combatting fungal infections in plants, seeds and animals, including humans, and pharmaceutical and agricultural compositions containing them.
Abstract: Compounds of the general 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 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; 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 2-dioxacycloalkylthio-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 carbonyl, methylene or thiocarbonyl; B is alkylene having 2-5 carbon atoms;alk is alkylene having 1-6 carbon atoms;R.sub.1 is hydrogen or a group which results in an ester which is hydrolyzable in vivo; andn is zero or one.