Abstract: Preparation of 2-oxindole-1-carboxamides by reaction of 2-oxindoles with chlorosulfonyl isocyanate to produce novel N-chlorosulfonyl-2-oxindole-1-carboxamides which are then hydrolyzed to 2-oxindole-1-carboxamides useful as intermediates for analgesic and antiinflammatory agents.
Abstract: Corrosion resistance of stainless steel powder moldings is improved by combining the powder before molding with about 8 to 16% by weight of an additive consisting essentially of about 2 to 30% by weight of tin and 98 to 70% by weight of copper and/or nickel. Stainless steel moldings are prepared by compacting the powder at high pressure and heating to sintering temperature.
Abstract: Racemic endo- and exo-1-methoxybicyclo[2.2.2]oct-5-ene-2-carboxylic acids are starting materials for a novel and efficient synthesis of chiral 3R-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-4R-(3-hydroxypropyl)-1R-cycloh exanol, a compound having valuable central nervous system (CNS) activity, particularly as an analgesic and as an antiemetic.
Abstract: Compounds of the general formula: ##STR1## wherein R is naphthyl, biphenylyl, phenyl or substituted phenyl; n is 0, 1 or 2; and R.sup.1 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkanoyl, or C.sub.1-2 alkyl substituted by C.sub.2-4 alkenyl with the provisos that when R.sup.1 is H or C.sub.2-4 alkanoyl, n is 0; and when n is 2, R.sup.1 is C.sub.1-3 alkyl; and their pharmaceutically acceptable salts are antifungal agents useful in combatting fungal infections in animals, including humans.
Abstract: Topical vaginal forms of tioconazole and related antimicrobic compounds, especially miconazole, econazole, clotrimazole, butaconazole and ketoconazole, are useful for the control (chemotherapeutic and chemoprophylactic) of Herpes virus infections.
Abstract: Dihydropyridine Anti-ischaemic agents of the formula ##STR1## and their salts where R is aryl, R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl, Y is --(CH.sub.2).sub.n -- where n is 2, 3 or 4 and is optionally substituted by 1 or 2 methyl groups and R.sup.3 is pyrimidyl or di- or tetrahydropyrimidyl.
Type:
Grant
Filed:
February 14, 1986
Date of Patent:
April 28, 1987
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs, John E. Arrowsmith
Abstract: Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also on the carboxamide nitrogen atom, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and anti-inflammatory agents in mammalian subjects. Certain 2-oxindole compounds unsubstituted at the 1-position but having an acyl substituent at C-3 of the formula ##STR1## and the base salts thereof, wherein X is hydrogen, 5-fluoro, 5-chloro or 5-trifluoromethyl; Y is hydrogen, 6-fluoro, 6-chloro or 6-trifluoromethyl; and R.sup.1 is benzyl, furyl, thienyl or thienylmethyl; provided that when X and Y are both hydrogen, R.sup.1 is not benzyl are useful as intermediates to the aforementioned analgesic and anti-inflammatory agents.
Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof wherein R is 2-pyridyl, 6-chloro-2-pyridyl, 6-methyl-2-pyridyl or 5-methylisoxazol-3-yl; useful as prodrug forms of the corresponding known oxicam antiinflammatory and analgesic agents, piroxicam, the corresponding 6-chloro-2-pyridyl and 6-methyl-2-pyridylcarboxamides, isoxicam and tenoxicam; methods for their use, pharmaceutical compositions containing them and a process for their preparation.
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)piperazine-1-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: Novel biologically-active tetracyclic spiro-hydantoin derivatives which are potent inhibitors of aldose reductase and useful in treating diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treating chronic diabetic complications are also disclosed. A preferred compound is 9'-chloro-5',6'-dihydro-2'-phenyl-spiro[imidazolidine-5,7'-7'H-pyrido(1,2, 3-de)quinoxaline]2,3',4-trione.
Abstract: 6-.beta.-Substituted penicillanic acids and derivatives thereof as useful enhancers of the effectiveness of several .beta.-lactam antibiotics against many .beta.-lactamase producing bacteria, and 6-.beta.-substituted penicillanic acid derivatives wherein the carboxy group is protected by a conventional penicillin carboxy protecting group as useful intermediates leading to said synergistic agents. A process for converting 6,6-disubstituted penicillanic acid derivatives to the corresponding 6-.beta.-substituted penicillanic acid congeners.
Abstract: Compounds of the formula: ##STR1## where R is an optionally substituted aryl or heteroaryl group;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; and Y is --(CH.sub.2).sub.n -- where n is 2, 3 or 4, --CH.sub.2 CH(CH.sub.3)-- or --Ch.sub.2 C(CH.sub.3).sub.2 --; and their pharmaceutically acceptable salts.The compounds have utility as anti-ischaemic and antihypertensive agents and as synthetic intermediates to other dihydropyridine calcium antagonists.
Type:
Grant
Filed:
April 26, 1985
Date of Patent:
March 31, 1987
Assignee:
Pfizer Inc.
Inventors:
David Alker, Simon F. Campbell, Peter E. Cross
Abstract: Compounds of the formula: ##STR1## and pharmaceutically-acceptable acid addition salts thereof, wherein R.sup.1 is at the 3 or 4 position and is phenyl or phenyl substituted by halo, (C.sub.1 -C.sub.4)alkoxy, or (C.sub.2 -C.sub.5)alkoxycarbonyl; R.sup.2 is at the 2 or 7 position and is a group of the formula X(CH.sub.2).sub.n NR.sup.3 R.sup.4 where X is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; n is 1, 2, 3 or 4; and each of R.sup.3 and R.sup.4 is hydrogen or (C.sub.1 -C.sub.4)alkyl, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a 1-pyrrolidinyl or piperidino group; Y is hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy or (C.sub.2 -C.sub.5)-alkoxycarbonyl at the 4, 5, 6 or 7 position; and wherein R.sup.2 is at the 2-position, R.sup.1 is at the 3- or 4-position, or alternatively when R.sup.2 is at the 7-position, R.sup.1 is at the 3-position; are useful for the treatment of diarrhea in humans and animals.
Abstract: A differential thermal testing system comprising a first thermal conductive sensing plate whose temperature is maintained at a constant first temperature, and a second thermal conductive sensing plate whose temperature can be altered. The temperature differential between the first thermal conductive sensing plate and second thermal conductive sensing plate is detected.
Abstract: This invention relates to an inbred line of corn having the designation 78010, seeds produced by plants of the inbred line 78010, cells which upon growth and differentiation produces the inbred line 78010, hybrid corn seed produced by crossing the inbred line 78010 with another corn line and a process for the production of hybrid corn seed using the inbred line 78010.
Abstract: Preparation of 2-oxindole-1-carboxamides by reaction of 2-oxindoles with chlorosulfonyl isocyanate to produce novel N-chlorosulfonyl-2-oxindole-1-carboxamides which are then hydrolyzed to 2-oxindole-1-carboxamides useful as intermediates for analgesic and antiinflammatory agents.
Abstract: A new polyether antibiotic has been isolated from fermentations of a new microorganism of the genus Streptomyces. This new microorganism is designated as N478-13 and it has been named Streptomyces routienii Huange sp. nov., (ATCC 30446). The new antibiotic exhibits antibacterial activity against a variety of gram-positive bacteria; it can be used to control swine dysentery; and it promotes increased efficiency of feed utilization (i.e. promotes increased growth) in swine and ruminants.
Type:
Grant
Filed:
October 15, 1984
Date of Patent:
March 24, 1987
Assignee:
Pfizer Inc.
Inventors:
Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
Abstract: A socket insert component of an acetabular cup prosthesis is held securely within its support shell by a locking mechanism comprising a circumferential groove in the shell concavity perpendicular to the longitudinal axis of the concavity, a first circumferential rib on the outer surface of the insert congruent with the groove, and a second circumferential rib on the outer surface of the insert parallel to and proximate the first rib, the first rib snapping into the groove and the second rib being deformed and pressed against the concavity when the insert and shell are assembled.
Abstract: A process for the purification of glycolide which comprises dissolving the glycolide to be purified in a suitable organic solvent, adding alumina to the resulting solution to form a slurry wherein the alumina is in intimate contact with the dissolved glycolide, stirring the slurry under controlled conditions for a period of 1 to 60 minutes, and filtering to remove the alumina and, if desired, evaporating to remove the solvent and recovering the purified glycolide; and the production of suture-grade polyglycolic acid by the polymerization of the resulting purified glycolide.
Abstract: There is disclosed an improved absorbable surgical suture. The suture is coated with an absorbable composition consisting essentially of a high molecular weight poly(alkylene oxide).