Abstract: Growth of cattle and swine is promoted and feed utilization efficiency increased by an improved nutrient feed containing the antibiotic of the formula ##STR1##
Type:
Grant
Filed:
November 9, 1983
Date of Patent:
August 6, 1985
Assignee:
Pfizer Inc.
Inventors:
Walter D. Celmer, Walter P. Cullen, Riichiro Shibakawa, Junsuke Tone
Abstract: A series of substituted phenylacetic acid compounds and their derivatives, including the pharmacologically acceptable base salts of said acids, have been found to be active as oral hypoglycemic agents. Preferred member compounds include 6-ethoxy-1,2,3,4-tetrahydronaphthalene-1-carboxylic acid, 6-benzyloxy-1,2,3,4-tetrahydronaphthalene-1-carboxylic acid, chroman-4-carboxylic acid, p-chlorophenylacetic acid, o-methylphenylacetic acid, o-methoxyphenylacetic acid, p-methoxyphenylacetic acid and .alpha., .alpha.-di(4-methoxyphenyl)acetic acid. Synthetic routes leading to those member compounds which are novel per se are described in some detail.
Abstract: A process for the preparation of 1,1-dioxopenicillanoyloxymethyl 6-beta-aminopenicillanate which comprises reacting 1,1-dioxopenicillanoyloxymethyl 6-phenylacetamidopenicillanate or the corresponding phenoxyacetamidopenicillanate under anhydrous conditions with a halogenating agent in the presence of a reaction inert solvent to form an intermediate imino halide, addition of a primary alcohol having from one to four carbon atoms to convert the imino halide to an imino ether and subsequent hydrolysis to give the desired product.
Abstract: Compounds of the formula ##STR1## wherein X is halo and R is an aryl group and their pharmaceutically acceptable salts are useful antifungal agents in animals, including man.
Abstract: 2-[2-Hydroxy-4-(substituted)phenyl]piperidines and derivatives thereof of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is H, benzyl or certain acyl groups, R.sub.2 is H, certain alkyl, alkenyl, alkynyl, hydroxyalkyl, acyl or alkylsulfonyl groups; R.sub.3 is H.sub.2, O, ##STR2## and Z is (C.sub.1 -C.sub.13)alkylene or -(alk.sub.1).sub.m -O-(alk.sub.2).sub.n - where each of (alk.sub.1) and (alk.sub.2) is (C.sub.1 -C.sub.13)alkylene, provided that the number of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 13; each of m and n is 0 or 1; and W is H, pyridyl or optionally substituted phenyl; their use as analgesic agents, intermediates therefor and processes for their preparation.
Type:
Grant
Filed:
March 14, 1983
Date of Patent:
July 16, 1985
Assignee:
Pfizer Inc.
Inventors:
Michael R. Johnson, Lawrence S. Melvin, Jr.
Abstract: Sorbinil is obtained by cyclization of S-6-fluoro-4-ureidochromane-4-carboxylic acid, which is in turn obtained by resolution of racemic 6-fluoro-4-ureidochroman-4-carboxylic acid via diasteromeric salts with either D-(+)-(1-phenethyl)amine or L-(-)-ephedrine.
Abstract: Antibacterial 4"-epi-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A, pharmaceutically-acceptable salts thereof, pharmaceutical compositions comprising antibacterially-effective amounts thereof, a method of treatment of bacterial infections with antibacterially effective amounts thereof, and intermediates for the synthesis thereof from erythromycin A.
Abstract: A process for grafting a hydrophilic polymer of a carboxylic acid or a salt thereof onto the surface of a natural rubber article by contacting said article in reaction inert solvent with a vinyl carboxylic acid anhydride and initiator, and subsequent washing and hydrolysis of anhydride groups to carboxylate groups and an article when prepared by the invention process.
Abstract: The ductility and electrical conductivity of an age hardened spinodally decomposed copper-nickel-tin alloy can be improved, without detracting from the alloy's strength properties, by reducing the nickel content of the alloy and adding from about 3.5 to about 7 weight percent, based upon the weight of the alloy, of cobalt.
Abstract: Salts of readily hydrolyzable esters of 6-alpha-(aminomethyl)penicillanic acid 1,1-dioxide and (a) prodrug forms of ampicillin and amoxicillin or (b) ampicillin and amoxicillin and a dibasic acid are readily absorbed following oral adminstration, and are useful in treating bacterial infections.
Abstract: Compounds of the 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 1 to 3 substituents selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)-alkyl and (C.sub.1 -C.sub.4)alkoxy; X is a halogen atom, 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 novel 9-deoxo-4"-deoxy-4"-amino-9a-aza-9a-homoerythromycin A derivatives; a method of treating a bacterial infection in a mammalian subject using the novel erythromycin A derivatives; pharmaceutical compositions containing the novel erythromycin A derivatives; and intermediates and processes for making the novel erythromycin A derivatives.
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: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is CH.sub.2 OH or CH.sub.2 OCH.sub.3 ; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, F.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2, C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.
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: 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 13 ; 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:
July 19, 1983
Date of Patent:
May 7, 1985
Assignee:
Pfizer Inc.
Inventors:
Simon F. Campbell, Peter E. Cross, John K. Stubbs
Abstract: An apparatus for adding wire-form processing elements directly into a molten material, comprising: a heat resistant nozzle positionable relative to the surface of the molten material such that an inlet is disposed above the surface and an outlet is disposed beneath the surface; a mechanism for feeding the wire through the nozzle directly into the molten material; and a system for injecting a substantially inert gaseous medium into the molten material together with the wire, whereby the inert gas substantially prevents closure of the nozzle by solidified molten material and promotes mixture of the processing elements with the molten material through gas bubble agitation. The apparatus further comprises a substantially gas-tight conduit connected to the nozzle inlet, through which the wire and the inert gaseous medium are delivered to the nozzle. A pressure-driven seal prevents atmospheric contamination and prevents loss of inert gas.
Abstract: Certain novel 9-deoxo-4"-deoxy-4"-amino-9a-aza-9a-homoerythromycin A derivatives; a method of treating a bacterial infection in a mammalian subject using these novel erythromycin A derivatives; pharmaceutical compositions containing the novel erythromycin A derivatives; and intermediates and processes for making the novel erythromycin A derivatives.
Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.
Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.