Patents Assigned to Pfizer Inc.
  • Patent number: 5185343
    Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH=CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.
    Type: Grant
    Filed: October 23, 1991
    Date of Patent: February 9, 1993
    Assignee: Pfizer Inc.
    Inventor: Bertrand L. Chenard
  • Patent number: 5185369
    Abstract: Compounds having the formula R-(CH.sub.2).sub.m -CO-R' wherein R is ferrocene, a 5 to 7 member azacyclic system or an 8 to 11 member azabicyclic system, having 1 or 2 nitrogen atoms, or any such system substituted with one or more of F, Cl, Br, OH, C1 to C4 alkyl, C1 to C4 alkoxy, CF.sub.3, phenyl, amino, C1 to C4 alkylamino and di(C1 to C4 alkyl)amino; m is 0 or 1; and R' is--[NH(CH.sub.2).sub.n ].sub.x NH.sub.2, with each n being independently 2 to 5 and x being 1 to 6; ##STR1## with each n being independently 2 to 5, x being 0 to 4, y and z being independently 1 to 5 and the sum of x and the greater of y and z being 1 to 5; or ##STR2## with each a being 2 to 5, each b being 2 to 5, each n being independently 2 to 5, x being 0 to 3, each y being 0 or 1, z being 0 to 3 and x+y+z being 0 to 4, and their pharmaceutically acceptable acid addition salts are potent excitatory amino acid neurotransmitter antagonists.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: February 9, 1993
    Assignee: Pfizer Inc.
    Inventors: Nicholas A. Saccomano, Robert A. Volkmann
  • Patent number: 5185449
    Abstract: (C.sub.1 -C.sub.3)Alkyl-4,6,7,8,9,9a-hexahydro-2H,3H-pyrido-[1,2-a]pyrazin-1-one-7- carboxylate esters, important precursors to certain bis-aza-bicyclic anxiolytics, can be prepared from di(C.sub.1 -C.sub.3)alkyl cis-piperidine-2,5-dicarboxylate starting material by a new process via a new class of intermediates, di(C.sub.1 -C.sub.3)alkyl cis-N-(2-(phthalimido)ethyl)piperidine-2,5-dicarboxylates. In the process, the starting material is reacted with either 2-(phthalimido)ethyl triflate or 2-(phthalimido)acetaldehyde to form the new intermediate, which can then be cyclized to the aforementioned precursor.
    Type: Grant
    Filed: February 27, 1991
    Date of Patent: February 9, 1993
    Assignee: Pfizer Inc.
    Inventors: Dennis M. Godek, Charles W. Murtiashaw, Frank J. Urban, Brian C. Vanderplas
  • Patent number: 5185464
    Abstract: A process and intermediates for the manufacture of S-3-methylheptanoic acid from S-citronellol; a novel crystallline form of immunoregulatory N-(S-3-methylheptanoyl)-D-gamma-glutamyl-glycyl-D-alanine, an immunoregulatory agent; and an improved process and intermediates therefor.
    Type: Grant
    Filed: March 17, 1992
    Date of Patent: February 9, 1993
    Assignee: Pfizer Inc.
    Inventor: Charles W. Murtiashaw
  • Patent number: 5182391
    Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thioacetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazoloyridinyl side chains.
    Type: Grant
    Filed: June 30, 1992
    Date of Patent: January 26, 1993
    Assignee: Pfizer Inc.
    Inventors: Banavara L. Mylari, William J. Zembrowski
  • Patent number: 5178796
    Abstract: There is disclosed a method for removing dissolved oxygen from aqueous systems, for example, boiler water systems for oil injection water or brine. The disclosed method uses a salt of a keto-gluconic acid, or a salt of a stereoisomer of a keto-gluconic acid, as the oxygen scavenger a metal containing compound which controls the rate of oxygen removal.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: January 12, 1993
    Assignee: Pfizer Inc.
    Inventors: Herman L. Gewanter, Ralph D. May
  • Patent number: 5175179
    Abstract: A method of using certain thiazolidine-2,4-diones in the treatment of hypertension.
    Type: Grant
    Filed: September 25, 1991
    Date of Patent: December 29, 1992
    Assignee: Pfizer Inc.
    Inventor: Eric R. Larson
  • Patent number: 5171744
    Abstract: Compounds having the formula: ##STR1## wherein X is either (a) a phenyl group optionally substituted by 1 or 2 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and hydroxy, or (b) a thienyl group; and Y is an imidazolyl, pyrazolyl, triazolyl or tetrazolyl group optionally substituted by 1 or 2 substituents each independently selected from halo, CF.sub.3, C.sub.1 -C.sub.4 alkoxy, hydroxy and amino; and pharmaceutically acceptable salts thereof, are antimuscarinic bronchodilators useful in the treatment of chronic obstructive airways disease and asthma.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: December 15, 1992
    Assignee: Pfizer Inc.
    Inventors: Peter E. Cross, Alan Stobie
  • Patent number: 5171862
    Abstract: Oxophthalazinyl acetic acids having benzothiazole side chains are prepared by reacting an oxophthalazinyl thioacetamide acetate with hydrogen sulfide and a nitrophenyl compound having a reactive group such that the benzothiazole side chain may be formed by ring closure involving the thioacetamide group. The oxophthalazinyl thioacetamide may be prepared by reacting the corresponding cyanomethyloxophthalazinyl acetate with hydrogen sulfide in the presence of tertiary amines. Analogous indazole and oxopyridopyridazinone acetic acids may be prepared similarly, as well as oxophthalazinyl, indazole and oxopyridopyridazinone acetic acids having thiazolopyridinyl side chains.
    Type: Grant
    Filed: September 30, 1991
    Date of Patent: December 15, 1992
    Assignee: Pfizer Inc.
    Inventors: Banavara L. Mylari, William J. Zembrowski
  • Patent number: 5169976
    Abstract: Variously substituted 4-(biphen-2-ylmethylcarbamoyl)-3-hydroxybutyric acids and esters, also named as N-(biphen-2-yl)-3-hydroxyglutaramic acid derivatives, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.
    Type: Grant
    Filed: May 3, 1990
    Date of Patent: December 8, 1992
    Assignee: Pfizer Inc.
    Inventor: Peter A. McCarthy
  • Patent number: 5169947
    Abstract: Compounds of the formula ##STR1## wherein one of A, B, D and E is N and the remaining three atoms are C; R.sup.1 and R.sup.2 are independently selected from hydrogen and C.sub.1 to C.sub.6 alkyl; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.8 alkoxy, phenyl-C.sub.1 -C.sub.6 alkoxy, phenoxy, --NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl, and COOR.sup.9 wherein R.sup.9 is hydrogen or C.sub.1 -C.sub.6 alkyl, cyano, COOR.sup.10 wherein R.sup.10 is hydrogen or C.sub.1 -C.sub.6 alkyl, and CONR.sup.11 R.sup.12 where R.sup.11 and R.sup.12 are independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof. The compounds are useful psychotherapeutics and may be used in treating obesity, depression and disorders wherein aggression is a symptom.
    Type: Grant
    Filed: September 20, 1991
    Date of Patent: December 8, 1992
    Assignee: Pfizer Inc.
    Inventor: John E. Macor
  • Patent number: 5166406
    Abstract: The invention provides a process for preparing a compound of the formula: ##STR1## or a base salt thereof, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by up to 3 substituents each independently selected from the group consisting of C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6 alkoxy)-; and R.sup.3 is C.sub.1 -C.sub.6 alkyl or benzyl, said benzyl group being optionally ring-substituted by up to 2 nitro or C.sub.1 -C.sub.4 alkoxy substituents comprising reacting a compound of the formula: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or benzyl or C.sub.1 -C.sub.4 alkoxy; and R.sup.2 and R.sup.3 are as previously defined for a compound of the formula (I), with hydrogen peroxide or a source of peroxide ions: said process being optionally followed by conversion of the compound of the formula (I) to a base salt thereof. The present invention also relates to novel compounds of the formula (II).
    Type: Grant
    Filed: April 4, 1990
    Date of Patent: November 24, 1992
    Assignee: Pfizer Inc.
    Inventor: Stephen Challenger
  • Patent number: 5166400
    Abstract: Process and intermediates for isopropyl 3S-amino-4-cyclohexyl-2R-hydroxybutyrate and 3S-amino-2R-hydroxy-5-methylhexanoate from R-malic acid. These products are of known utility in the synthesis of certain renin inhibitors.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: November 24, 1992
    Assignee: Pfizer Inc.
    Inventor: Robert W. Dugger
  • Patent number: 5166401
    Abstract: Process for the production of 5-fluoro-6-chlorooxindole, (III), which is useful in the synthesis of certain analgesic and antiinflammatory agents, via two different synthetic pathways.Compounds of formula (I) and (II) shown below ##STR1## which are intermediates in the process of this invention.
    Type: Grant
    Filed: June 25, 1991
    Date of Patent: November 24, 1992
    Assignee: Pfizer Inc
    Inventor: Robert W. Dugger
  • Patent number: 5166161
    Abstract: 3-Oxo-4-acyl or carbamyl-bicyclic aromatic and heterocyclic compounds as inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergy and antiinflammatory agents.
    Type: Grant
    Filed: January 22, 1991
    Date of Patent: November 24, 1992
    Assignee: Pfizer Inc.
    Inventors: Toshihide Kokura, Kazunari Nakao, Fumitaka Ito, Masami Nakane
  • Patent number: 5164402
    Abstract: Quinolone carboxylic acids 7-substituted by azabicyclo groups have antibacterial activity.
    Type: Grant
    Filed: February 4, 1991
    Date of Patent: November 17, 1992
    Assignee: Pfizer Inc
    Inventor: Katherine E. Brighty
  • Patent number: 5162339
    Abstract: A series of cis-3-[(cyclic)methylamino]-2-[(.alpha.-substituted)arylmethyl]quinuclidin es, 3-[(cyclic)methylimino]-2-[(.alpha.-substituted)-arylmethyl]quinuclidines and cis-3-[(cyclic)-methyleneamino]-2-[(.alpha.-substituted)arylmethyl]-quinuc lidines, including their pharmaceutically acceptable salts, are disclosed. These particular compounds are found to be useful as substance P antagonists and therefore, are of value in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases and pain or migraine. Preferred member compounds include cis-3-[(2-chlorophenyl)methylamino]-2-benzhydryl-quinuclidine, cis-3-[(2-trifluorophenyl)methylamino]2-benzhydrylquinuclidine and cis-[(2-methoxyphenyl)methylamino]-2-benzhydrylquinuclidine. Methods for preparing these compounds from known starting materials are provided.
    Type: Grant
    Filed: July 20, 1990
    Date of Patent: November 10, 1992
    Assignee: Pfizer Inc.
    Inventor: John A. Lowe, III
  • Patent number: 5158964
    Abstract: A series of novel N-alkyl N-(alkanesulphonamidoheterocyclicmethyl)-4-alkanesulphonamidophenethylamin es have been prepared, including their pharmaceutically acceptable salts and various key novel intermediates therefor. The heterocyclic moiety present in these compounds is a benzo-fused heterocyclic group derived from either benzofuran, benzothiophene, benzoxazole or quinoline, and it is attached to the adjacent methyl group of the molecule by means of the available ring carbon atom which is situated alpha to the hetero atom. These particular compounds are useful in therapy as highly effective anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Preferred member compounds include N-methyl-N-(5 methanesulphonamidobenzofur-2-ylmethyl)-4-methanesulphonamidophenethylamin e and N-methyl-N-(6 methanesulphonamidoquinol-2-ylmethyl)-4-methanesulphonamidophenethylamine. Methods for preparing all these compounds from known starting materials are provided.
    Type: Grant
    Filed: July 8, 1991
    Date of Patent: October 27, 1992
    Assignee: Pfizer Inc.
    Inventors: John E. Arrowsmith, Peter E. Cross, Geoffrey N. Thomas
  • Patent number: 5158798
    Abstract: There is disclosed a low calorie fat substitute comprising an emulsion containing a non-flowable aqueous phase, an oil phase and a fat extender. Also disclosed are low calorie fat substitutes wherein the fat or oil is replaced by a fat mimetic.
    Type: Grant
    Filed: January 11, 1991
    Date of Patent: October 27, 1992
    Assignee: Pfizer Inc.
    Inventors: Fu-Ning Fung, James W. Miller, Michael T. Wuesthoff
  • Patent number: 5158937
    Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 53708. This novel antibiiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, and as a growth promotant in cattle and swine.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: October 27, 1992
    Assignee: Pfizer Inc.
    Inventors: John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone