Abstract: Certain enol ethers and esters of the formula ##STR1## where X and Y are each hydrogen, fluoro or chloro; R.sup.1 is 2-thienyl or benzyl and R is alkanoyl, cycloalkylcarbonyl, phenylalkanoyl, chlorobenzoyl, methoxybenzyl, phenyl, thenoyl, omega-alkoxycarbonylalkanoyl, alkoxycarbonyl, phenoxycarbonyl, 1-alkoxyalkyl, 1-alkoxycarbonyloxyalkyl, alkyl, alkylsulfonyl, methylphenylsulfonyl or dialkylphosphonate are useful as prodrug forms the known 3-acyl-2-oxindole-1-carboxamide antiinflammatory and analgesic agents.
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 --, abc and d are 0-2 and a+b+c+d.ltoreq.5 R.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:
June 21, 1991
Date of Patent:
May 12, 1992
Assignee:
Pfizer Inc.
Inventors:
Christopher J. Dutton, Stephen P. Gibson, Nigel D. A. Walshe
Abstract: This invention relates to devices useful for the controlled delivery of one or more beneficial agents to an environment of use. More specifically, this invention concerns such devices which are powered by lyotropic liquid crystals. This invention also relates to the controlled delivery of one or more beneficial agents to an aqueous environment of use through the use of such lyotropic liquid crystal powered dispensing devices. Also disclosed are methods for the controlled delivery of one or more beneficial agents to an aqueous environment of use which comprise administering to or otherwise placing the devices of this invention in the environment of use.
Abstract: The invention provides the substantially optically pure 2(S)-stereoisomeric form of compounds of the formulae: ##STR1## and the salts thereof, together with processes for their preparation. The compounds are intermediates for the preparation of antihypertensive agents.
Abstract: Preparation of 2-oxindole-1-carboxamides by reaction of 2-oxindoles with trichloracetyl isocyanate to produce novel N-trichloroacetyl-2-oxindole-1-carboxamides which are then hydrolyzed to 2-oxindole-1-carboxamides useful as analgesic and antiinflammatory agents and/or intermediates for such agents.
Abstract: A visual inspection system for inspecting pharmaceutical tablets. The system comprises a photoelectric detection means for detecting the light intensity within an inspection area on a tablet and for generating a detection signal which varies with that light intensity. The system also comprises a signal processing means for comparing the detection signal to a predetermined standard in order to generate a selection signal and a transducer means which is responsive to the selection signal. A separation means separates the tablets into at least two groups in accordance with the selection signal. Yet another aspect of this invention is a method for inspecting the surface of pharmaceutical tablets using the above-described vision inspection system.
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: 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: 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: 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: Certain spirocyclic heterocyclic compounds, and their pharmaceutically-acceptable salts, are inhibitors of the aldose reductase enzyme, and so are useful for the control of diabetic complications. Exemplary compounds include compounds of the formula ##STR1## wherein Y is ##STR2## X is --O-- or ##STR3## R.sub.1 and R.sub.2 are each independently H, alkyl C.sub.1 -C.sub.6,aryl or arylalkyl (C.sub.1 -C.sub.6);W.sub.1 and W.sub.2 are each independently hydrogen, halogen or nitro; andthe pharmaceutically acceptable base addition salts thereof.
Abstract: This invention relates to devices useful for the controlled delivery of one or more beneficial agents to an environment of use. More specifically, this invention concerns such devices which are powered by lyotropic liquid crystals. This inventioin also relates to the controlled delivery of one or more beneficial agents to an aqueous environment of use through the use of such lyotropic liquid crystal powered dispensing devices. Also disclosed are methods for the controlled delivery of one or more beneficial agents to an aqueous environment of use which comprise administering to or otherwise placing the devices of this invention in the environment of use.
Abstract: A method of removing objectionable impurities from a hop flavor so that the impurities will not cause a fruity aroma of the beer. The method comprises steam stripping the odor forming impurities from the hop flavor at a pH such that the steam stripping is effective in removing the impurities to produce the purified hop flavor.
Abstract: A method of converting alpha acids to hop flavors by exposing the alpha acids to an environment capable of substantially simultaneously isomerizing and reducing the alpha acids to form either THIAA or HHIAA. Another aspect of this invention is directed to a method of reducing hop flavors by exposing an isoalpha acid, a dihydroisoalpha acid or a mixture thereof to conditions suitable to reduce said acids to produce THIAA, HHIAA or a mixture thereof at a pH of about 5 to about 12 in a reaction inert, protic solvent. Yet another aspect of this invention is directed to a method of reducing hop flavors comprising exposing an isoalpha acid, a dihydroisoalpha acid or a mixture thereof to conditions suitable to reduce said acids to produce THIAA, HHIAA or a mixture thereof in a reaction inert, aprotic solvent.
Abstract: An apparatus for mixing and spraying a slurry. The apparatus comprises a mixing chamber and a screw means, disposed within the chamber, for mixing and transporting material downstream to an air atomization nozzle. Another aspect of this invention is a method for mixing and spraying a slurry. The method comprises introducing and propelling a particulate solid along a mixing chamber. A liquid is introduced downstream from the introduction of the solid, a sufficient distance such that no substantial liquid backs up to the introduction of the solid. The solid and liquid are mixed to form a slurry, substantially in the absence of air. The slurry is propelled downstream, substantially in the absence of air, and atomized.
Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.