Patents Assigned to Pfizer
  • Patent number: 6066735
    Abstract: A process for the preparation of a compound of formula (I): ##STR1## which comprises cyclization of a compound of formula (II): ##STR2##
    Type: Grant
    Filed: July 23, 1999
    Date of Patent: May 23, 2000
    Assignee: Pfizer Inc.
    Inventors: Peter James Dunn, Albert Shaw Wood
  • Patent number: 6063928
    Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: May 16, 2000
    Assignee: Pfizer Inc
    Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
  • Patent number: 6060479
    Abstract: The present invention relates to novel quinazolin-4-one derivatives of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.
    Type: Grant
    Filed: May 14, 1998
    Date of Patent: May 9, 2000
    Assignee: Pfizer Inc
    Inventors: Bertrand L. Chenard, Willard M. Welch
  • Patent number: 6057436
    Abstract: The present invention provides the amino acid and nucleotide sequences of a CCV spike gene, and compositions containing one or more fragments of the spike gene for prophylaxis, diagnostic, and treatment of CCV infections.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: May 2, 2000
    Assignee: Pfizer Inc.
    Inventors: Timothy J. Miller, Sharon Klepfer, Albert Paul Reed
  • Patent number: 6057309
    Abstract: The present invention provides novel methods of inhibiting bone loss comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different provided that, when R.sup.1 and R.sup.2 are the same, each is a methyl or ethyl group, and, when R.sup.1 and R.sup.2 are different, one of them is a methyl or ethyl group and the other is hydrogen or a benzyl group; or a pharmaceutically acceptable salt thereof; together with a progestin.
    Type: Grant
    Filed: November 16, 1998
    Date of Patent: May 2, 2000
    Assignee: Pfizer Inc.
    Inventors: David B. MacLean, David D. Thompson
  • Patent number: 6057455
    Abstract: A process for preparing a compound of the formula ##STR1## wherein R.sup.1, m, o and p are described below, which comprises adding a base of the formula ##STR2## wherein R.sup.2, R.sup.3 and R.sup.4 are as described below, to a solution comprising a compound of the formula ##STR3## wherein R.sup.1, m, o and p are as described below, and a halonitromethane of the formula O.sub.2 NCH.sub.2 X, wherein X is a halogen atom dissolved in a non-aqueous inert solvent. The compounds of formula III are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids, and their pharmaceutically acceptable salts and prodrugs, having antibacterial activity. This invention also relates to the base of formula IV wherein each R.sup.2 is butyl, R.sup.3 is hydrogen and each R.sup.4 is t-butyl.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: May 2, 2000
    Assignee: Pfizer, Inc.
    Inventor: Joel M. Hawkins
  • Patent number: 6057364
    Abstract: The invention relates to fluoro-substituted adamantane derivatives of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein. The invention also relates to methods of treating neurological disorders, such as memory loss and Parkinson's disease, and bacterial and viral infections, through administration of a therapeutically effective amount of a compound of formula I.
    Type: Grant
    Filed: April 9, 1998
    Date of Patent: May 2, 2000
    Assignee: Pfizer Inc
    Inventors: Vytautas John Jasys, Robert A. Volkmann
  • Patent number: 6051601
    Abstract: This invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds or a pharmaceutically acceptable salt thereof, and to methods of using such compounds as LTB.sub.4 antagonists. The compounds and the pharmaceutically acceptable salts of this invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfuslon injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: April 18, 2000
    Assignee: Pfizer Inc.
    Inventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
  • Patent number: 6051578
    Abstract: This invention relates to the use of pyrazolopyrimidines and pyrrolopyrimidine of, respectively, the general formula ##STR1## wherein A, X, R.sup.3, R.sup.4 and R.sup.5 are as defined below, and the pharmaceutically acceptable salts of such compounds, to treat, prevent or inhibit certain neuronal and other disorders.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: April 18, 2000
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 6048864
    Abstract: Compounds of formula I, ##STR1## wherein R.sup.1 represents C.sub.1-4 alkoxy optionally substituted by one or more fluorine atoms;R.sup.2 and R.sup.3 independently represent H or C.sub.1-6 alkoxy (which is optionally substituted);R.sup.4 represents a 4-, 5-, 6- or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic, the ring system as a whole being optionally substituted;X represents CH or N; andL is absent,or represents a cyclic group of formula Ia, ##STR2## or represents a chain of formula Ib, ##STR3## and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.
    Type: Grant
    Filed: April 28, 1998
    Date of Patent: April 11, 2000
    Assignee: Pfizer Inc
    Inventors: David Nathan Abraham Fox, Alan John Collis, Simon John Mantell
  • Patent number: 6048880
    Abstract: A compound of the formula: ##STR1## and its pharmaceutically effective salts, wherein R.sup.1 and R.sup.2 are independently selected from the following:(a) hydrogen, halo, R.sup.5 --, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, hydroxy-R.sup.5 --, R.sup.5 --O--R.sup.5 --, or the like; (b) Ar--, Ar--R.sup.5 --, Ar--C.sub.2-6 alkenyl, Ar--C.sub.2-6 alkynyl, Ar--O--, Ar--O--R.sup.5 -- or the like; (c) R.sup.5 --C(O)--, --NO.sub.2, cyano, NH.sub.2 --C(O)--, R.sup.5 --NH--C(O)--, (R.sup.5).sub.2 --N--C(O)--, Ar--C(O)-- or the like; and (d) R.sup.5 --C(O)--NH--, Ar--C(O)--NH-- or the like; wherein Ar is optionally substituted aryl or heteroaryl such as phenyl and pyridyl; and wherein R.sup.5 is optionally halo-substituted C.sub.1-6 alkyl; R.sup.3 is selected from the following: (e) cyano, formyl, tetrazolyl, triazolyl, imidazolyl, oxazolyl, thiazolyl, R.sup.5 --C(O)--, C.sub.2-6 alkenyl-C(O)--, C.sub.2-6 alkynyl-C(O)--, R.sup.5 --C(O)--R.sup.5 --, or the like; (f) R.sup.5 --C(O)--NH--, Ar--C(O)--NH--, or the like; (g) R.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: April 11, 2000
    Assignee: Pfizer Pharamaceuticals Inc.
    Inventors: Akiyoshi Kawai, Makoto Kawai
  • Patent number: 6046213
    Abstract: This invention relates to compounds of formula (I), or pharmaceutically acceptable acid addition salts thereof, wherein: (a) R.sup.2 and R.sup.5 are taken separately and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, (C.sub.1 -C.sub.6) alkyl, halo, CF.sub.3, OH or OR.sup.7 and R.sup.5 is methyl or ethyl; or (b) R.sup.2 and R.sup.5 are taken together, forming a chroman-4-ol ring, and R.sup.1, R.sup.3 and R.sup.4 are each independently hydrogen, (C.sub.1 -C.sub.6) alkyl, halo, CF.sub.3, OH or OR.sup.7 ; and R.sup.6 is a substituted piperidinyl, pyrrolidinyl or 8-azabicyclo(3.2.1)octanyl derivative; provided that (a) when R.sup.2 and R.sup.5 are taken separately, at least one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is not hydrogen; and (b) when R.sup.2 and R.sup.5 are taken together, at least one of R.sup.1, R.sup.3 and R.sup.
    Type: Grant
    Filed: February 13, 1997
    Date of Patent: April 4, 2000
    Assignee: Pfizer Inc.
    Inventors: Bertrand L. Chenard, Todd W. Butler
  • Patent number: 6046338
    Abstract: A method for the separation of R-(+)- and S-(-)-isomers of amlodipine (I) from mixtures thereof, which comprises the reaction of the mixture of isomers with either L- or D-tartaric acid in an organic solvent containing sufficient dimethyl sulphoxide (DMSO) for the precipitation of, respectively, a DMSO, solvate of an L-tartate salt of R-(+)-amlodipine, or a DMSO solvate of a D-tartrate salt of S-(-)-amlodipine.
    Type: Grant
    Filed: May 5, 1998
    Date of Patent: April 4, 2000
    Assignee: Pfizer Inc.
    Inventor: Peter Lionel Spargo
  • Patent number: 6043238
    Abstract: A compound of the formula ##STR1## wherein a, V, X, Y, Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, useful in (a) the treatment of myelosuppression including suppression associated with cancer chemotherapy as well as activation of the immune system for the treatment of cancer or (b) prevention and treatment of viral, fungal, bacterial and parasitic infectious diseases.
    Type: Grant
    Filed: August 15, 1997
    Date of Patent: March 28, 2000
    Assignee: Pfizer Inc.
    Inventors: Christopher B. Cooper, Joseph P. Lyssikatos, Donald W. Mann, Scott J. Hecker
  • Patent number: 6043227
    Abstract: This invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial agents that may be used to treat various bacterial infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.
    Type: Grant
    Filed: May 26, 1999
    Date of Patent: March 28, 2000
    Assignee: Pfizer Inc.
    Inventors: Hengmiao Cheng, Michael Letavic, Carl B. Ziegler, Jr., Jason K. Dutra, Peter Bertinato, Brian S. Bronk
  • Patent number: 6043260
    Abstract: This invention relates to method for treating a mammal which presents with heart failure comprising administering to a mammal a therapeutically effective amount of wherein 4-(1-ethyl-propoxy)-3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-pyridine and (3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-pyridin-4-yl)-(1-ethyl-propyl)-a mine or a pharmaceutically acceptable salt thereof. This invention is also directed to methods of using combinations of those two agents with other congestive heart failure treating compounds to treat congestive heart failure.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: March 28, 2000
    Assignee: Pfizer Inc
    Inventors: Yuhpyng L. Chen, Anthony A. Fossa
  • Patent number: 6043226
    Abstract: This invention relates to compounds of formulas 1 and 2 ##STR1## and to pharmaceutically acceptable salts and solvates thereof, wherein X, X.sup.1, R.sup.1, R.sup.2, R.sup.7, R.sup.17 and R.sup.19 are as defined herein. The compounds of formulas 1 and 2 may be useful in the treatment of bacterial, parasitic and protozoal infections, as well as disorders related to bacterial, parasitic and protozoal infections, in mammals, fish and birds. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and 2 and to methods of treating bacterial, parasitic and protozoal infections by administering the compounds of formula 1 and 2.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: March 28, 2000
    Assignee: Pfizer Inc.
    Inventors: Kristin Marie Lundy, Hengmiao Cheng, Martha L. Minich, Subas Man Sakya, Peter Bertinato
  • Patent number: 6043379
    Abstract: A process for the preparation of the compound of the formula ##STR1## wherein R.sup.1 is OH, which comprises the steps of a) treating the compound of the formula ##STR2## with an inorganic fluoride, of the formula M.sup.2 F wherein M.sup.2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R.sup.4 P.sup.+ Z.sup.- and a compound of the formula R.sup.5 vic (COW).sub.2 wherein R.sup.4 and R.sup.5 are each selected from optionally substituted (C.sub.6 -C.sub.10)aryl and optionally substituted (C.sub.1 -C.sub.6)alkyl, and W is halo; to form the compound of the formula; ##STR3## and b) i) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, andii) treating the product of step i) with a mineral acid. A compound of the formula ##STR4## wherein R.sup.1 is selected from the group consisting of, halo, R.sup.7 O, R.sup.7 COO and N(R.sup.8).sub.2 wherein R.sup.7 is (C.sub.1 -C.sub.6)alkyl or (C.
    Type: Grant
    Filed: July 26, 1999
    Date of Patent: March 28, 2000
    Assignee: Pfizer Inc.
    Inventors: Anthony Marfat, Robert James Chambers
  • Patent number: 6040309
    Abstract: Compounds of formula I, ##STR1## wherein X represents O or S(O).sub.m ;R.sup.1 and R.sup.2 independently represent phenyl, naphthyl or heteroaryl; each of which is optionally fused and optionally substituted;Y represents a bond, O, (CH.sub.2).sub.n, O(CH.sub.2).sub.n, (CH.sub.2).sub.n O, or CH(C.sub.1-6 alkyl)O;R.sup.3 represents H or C.sub.1-6 alkyl;m represents 0, 1, or 2; andn represents 1, or 2;and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of restenosis, renal failure and pulmonary hypertension.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: March 21, 2000
    Assignee: Pfizer, Inc.
    Inventors: Kevin Neil Dack, Roger Peter Dickinson
  • Patent number: 6040329
    Abstract: The invention relates to compounds of the formula I ##STR1## and pharmaceutically acceptable salts thereof, wherein R, R.sub.1, and R.sub.2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula I, or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal.
    Type: Grant
    Filed: June 5, 1997
    Date of Patent: March 21, 2000
    Assignee: Pfizer Inc
    Inventor: Anthony Marfat