Abstract: The 2-chloro-1,1,1-tri(C.sub.1 -C.sub.6)alkoxyethanes are prepared from the corresponding tri(C.sub.1 -C.sub.6)alkoxyethanes by chlorination with N-chlorosuccinimide or with chlorine in pyridine and a chlorohydrocarbon cosolvent.
Type:
Grant
Filed:
July 31, 1987
Date of Patent:
May 31, 1988
Assignee:
Pfizer Inc.
Inventors:
Banavara L. Mylari, William J. Zembrowski
Abstract: A new acidic polycyclic ether antibiotic UK-58,852 has the formula: ##STR1## wherein R and R.sup.1 are both hydrogen, and can be prepared by the submerged aerobic propagation in aqueous nutrient media of Actinomadura sp. ATCC 39697. The antibiotic and its cationic salts are active against a variety of microorganisms and are effective in controlling coccidiosis, enteritis, swine dysentery and theileriosis as well as being effective in promotion of growth and/or improving efficiency of feed utilization in swine and ruminants. Two minor components, wherein R is H and R.sup.1 is CH.sub.3 and wherein R and R.sup.1 are both CH.sub.3, have also been isolated from the fermentation.
Type:
Grant
Filed:
June 21, 1985
Date of Patent:
May 24, 1988
Assignee:
Pfizer Inc.
Inventors:
Walter P. Cullen, Hiroshi Maeda, John C. Ruddock, Junsuke Tone
Abstract: Purified diisocyanate polyetherurethane prepolymers and process therefor. Polyetherurethane urea polymers prepared by mixing said prepolymers with an aqueous solution of an amino, ureido or hydroxy substituted amine or a like-substituted alpha-amino acid, and a method of using same as a space filling adhesive sealant in surgery.
Abstract: Aconitic acid, an unsaturated tricarboxylic acid, is obtained by fermentation of an aconitic acid-accumulating strain of Aspergillus terreus or Aspergillus itaconicus, under aerobic conditions, in a carbohydrate-containing medium, followed by isolation of the aconitic acid or a salt thereof. A preferred aconitic acid-accumulating microorganism is the strain of Aspergillus terreus which is on deposit in the Culture Collection of the Commonewealth Mycological Institute at Kew, Surrey, United Kingdom, under Accession No. CMI CC 281924.
Abstract: A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared wherein the heterocyclic ring moiety is a substituted pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent cardiac stimulants and therefore, are of value in the treatment of various cardiac conditions. Typical member compounds include those 6-(heterocyclic-substituted)-8-methyl-2-(1H)-quinolones wherein the heterocyclic ring moiety is a ring-substituted imidazol-1-yl group and preferably, an imidazol-1-yl group substituted with one or two methyl groups and a monoacetyl group. 6-(4-Acetyl-2-methylimidazol-1-yl)-8-methyl--2-(1H)-quinolone represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided.
Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.
Type:
Grant
Filed:
March 27, 1986
Date of Patent:
April 19, 1988
Assignee:
Pfizer Inc.
Inventors:
Michael R. Johnson, Lawrence S. Melvin, Jr.
Abstract: Process and intermediates for the conversion of 3R,4R-4-acetoxy-3-[1R-1-(silyloxy)ethyl]-2-azetidinones to antibacterial 5R,6S-6-(1R-1-hydroxyethyl)-2-(1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids, and the pharmaceutically-acceptable salts and pivaloyloxymethyl esters thereof.
Abstract: Hypoglycemic 5-[1-(5,6,7,8-tetrahydro-2-napthyl-; 1,2,3,4-tetrahydro-6-quinolyl-; 2-indanyl-; and 2-indolyl)alkyl]thiazolidine-2,4-dione derivatives, pharmaceutically acceptable salts thereof, and a method for their use in the treatment of hyperglycemic mammals.
Type:
Grant
Filed:
June 26, 1987
Date of Patent:
April 19, 1988
Assignee:
Pfizer Inc.
Inventors:
James F. Eggler, Gerald F. Holland, Michael R. Johnson, Robert A. Volkmann
Abstract: The present process produces the meso dialkyl 2,5-dihaloadipate from a mixture of the racemic dialkyl 2,5-dihaloadipate and meso 2,5-dihaloadipate. In the disclosed process, a 2,5-dihaloadipoyl halide is formed under conditions which result in the formation of an acidic compound. The 2,5-dihaloadipoyl halide is then esterified under conditions wherein the ester of the dihaloadipoyl halide is allowed to remain in contact with the acidic compound, thus allowing the racemic diester to epimerize in the presence of the acidic compound to the meso form and then the meso diester spontaneously crystallizes. In the last stage, the meso diester produced is removed.
Abstract: 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.
Type:
Grant
Filed:
November 5, 1986
Date of Patent:
March 22, 1988
Assignee:
Pfizer Inc.
Inventors:
David Alker, Simon F. Campbell, Peter E. Cross
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: An age hardened spinodally decomposed alloy prepared by powder metallurgy consisting essentially of from about 5 to about 30 percent by weight nickel, from about 4 to about 13 percent by weight tin, from about 0.5 to about 3.5 percent by weight cobalt and the balance copper exhibits an excellent combination of strength, ductility, formability and electrical conductivity characteristics.
Abstract: A novel process is described for preparation of biotin comprising preparation of substituted 3H, 5H-imidazo[1, 5c]tetrahydro thiazoles by contacting the boron trifluoride adduct of an appropriate thiazoline with the metallic derivative of an ester enolate, reducing the ester, hydrolyzing the thiazolidine moiety and hydrolyzing or oxidizing the resultant compound. Intermediates obtained in the preparation of biotin by the above process and alternate procedures for preparing said intermediates are also presented. A novel process for preparation of d-biotin is also given.
Abstract: A sternum closure device for closing the sternum of a patient comprising a head portion, tail portion and flexible spine portion. The head portion includes a locking tang to prevent backward movement of the spine portion once it is received and engaged in the head portion. The spine is made of a biocompatible metal coated with a biocompatible polymer along part of its length. One end of the spine is sharpened to serve as a needle. The tang pierces the polymer and locks against a serration of the spine. A method of using the sternum closure device is also disclosed.
Type:
Grant
Filed:
March 3, 1986
Date of Patent:
March 15, 1988
Assignee:
Pfizer Hospital Products Group, Inc.
Inventors:
Lloyd A. Sutherland, Alfred V. Vasconcellos
Abstract: A process for preparing [1H]-isoindolin-1-one-3-carboxylic acid comprising the steps of (1) reacting phthalaldehydic acid in an alkanol with ammonia, (2) contacting the resulting solution with an alkali metal cyanide, (3) removing the alkanol, (4) adjusting the pH to 1.0, (5) heating the resulting reaction mixture until product formation is substantially complete and isolating the product.
Abstract: A series of novel polypeptide derivatives, containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, which are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Particularly valuable precursors for many of these compounds are certain other 5-amino-2,5-disubstituted-4-hydroxypentanoic acid derivatives.
Type:
Grant
Filed:
April 30, 1986
Date of Patent:
March 8, 1988
Assignee:
Pfizer Inc.
Inventors:
Edward F. Kleinman, Robert L. Rosati, Jasjit S. Bindra
Abstract: Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.
Abstract: A series of novel heterocyclic-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the heterocyclic ring moiety is a pyrrolyl, imidazolyl, pyrazolyl, triazolyl or tetrazolyl group attached by a nitrogen atom of said group to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 6-(2,4-dimethylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, 6-(2,4-dimethyl-5-nitroimadazol-1-yl)-8-methyl-2-(1H)-quinolone, 8-methyl-6-(tetrazol-1-yl)-2-(1H)-quinolone, 8-methyl-6-(1,2,4-triazol-4-yl)-2-(1H)-quinolone, and 6-(4-cyano-2-methylimidazol-1-yl)-8-methyl-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting materials are provided.
Abstract: A series of novel phenyl-substituted 2-(1H)-quinolone compounds have been prepared, including the 3,4-dihydro derivatives thereof, wherein the phenyl ring moiety is a mono-or di-substituted phenyl group attached to the 5-, 6-, 7- or 8-positions of the quinolone ring. These particular compounds are useful in therapy as highly potent inotropic agents and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 8-methyl-6-[4-methylsulphinylphenyl]-2-(1H)-quinolone, 8-methyl-6-[4-hydroxyphenyl]-2-(1H)-quinolone and 8-methyl-6-[4-carbamoylphenyl]-2-(1H)-quinolone, respectively. Methods for preparing these compounds from known starting materials are provided.
Abstract: A cosmetic case and applicator are disclosed in which the handle of the applicator extends partially outside the case and serves to open the case when turned.