Patents Represented by Attorney Paul D. Thomas
  • Patent number: 4680404
    Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 and Q.sub.
    Type: Grant
    Filed: August 9, 1984
    Date of Patent: July 14, 1987
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4656265
    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.
    Type: Grant
    Filed: June 21, 1984
    Date of Patent: April 7, 1987
    Assignee: Pfizer Inc.
    Inventors: Joseph G. Lombardino, Anthony Marfat
  • Patent number: 4625041
    Abstract: A new acidic polycyclic ether antibiotic, CP-63,517, having the formula: ##STR1## and cationic salts thereof produced by submerged aerobic propagation of Streptomyces endus subsp. aureus, ATCC-39574, a new strain of microorganism isolated from a soil sample in Japan, a process for producing this antibiotic and methods for its use to improve feed utilization, promote growth of cattle and swine and to control coccidiosis.
    Type: Grant
    Filed: August 29, 1985
    Date of Patent: November 25, 1986
    Assignee: Pfizer Inc.
    Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
  • Patent number: 4616027
    Abstract: Compounds of the general 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 one to three substituents, each independently selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy; 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.
    Type: Grant
    Filed: July 25, 1983
    Date of Patent: October 7, 1986
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Peter J. Whittle
  • Patent number: 4616026
    Abstract: Compounds of the formula ##STR1## 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, each independently selected from F, Cl, Br, I, CF.sub.3, (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy; and R.sup.1 is H, Cl, phenyl, phenyl substituted by from 1 to 3 substituents each independently selected from F, Cl, Br, I and CF.sub.3 or a heterocyclic group linked to the adjacent CF.sub.2 group by a ring carbon atom; method for their use in combatting fungal infections in plants, seeds and animals, including humans, and pharmaceutical and agricultural compositions containing them.
    Type: Grant
    Filed: July 25, 1983
    Date of Patent: October 7, 1986
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Peter J. Whittle
  • Patent number: 4601897
    Abstract: A method for relaxing bronchial tissue in mammals, including humans, by use of a combination of prazosin and pirbuterol or their pharmaceutically acceptable acid addition salts.
    Type: Grant
    Filed: November 6, 1985
    Date of Patent: July 22, 1986
    Assignee: Pfizer Inc.
    Inventor: Craig A. P. D. Saxton
  • Patent number: 4582907
    Abstract: 2-(2-Amino-2-thiazolin-4-yl)acetic acid or a pharmaceutically acceptable acid addition or cationic salt thereof useful in removal of excessive levels of certain metal ions from animals, including humans, and in protection of said animals from exposure to radioactivity.
    Type: Grant
    Filed: April 8, 1985
    Date of Patent: April 15, 1986
    Assignee: Pfizer Inc.
    Inventor: Malcolm M. Campbell
  • Patent number: 4576964
    Abstract: Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.
    Type: Grant
    Filed: June 7, 1984
    Date of Patent: March 18, 1986
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4560690
    Abstract: 2,4-Disubstituted thiazole compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof wherein X is NH and Y is CH or N, orX is S and Y is CH;R.sup.1 is certain straight or branched chain alkyl groups, (R.sup.3).sub.2 C.sub.6 H.sub.3, or (R.sup.3).sub.2 Ar(CH.sub.2).sub.n where n is an integer from 1 to 4, R.sup.3 is H or certain substituent groups and Ar is phenylene, naphthalene or the residue of certain heteroaromatic groups;R.sup.2 is H or (C.sub.1 -C.sub.4)alkyl; orR.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached form certain heterocyclic groups; andR.sup.4 is H, (C.sub.1 -C.sub.5)alkyl, NH.sub.2 or CH.sub.2 OH; a method for their use in treatment of gastric ulcers in mammals and pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: April 30, 1984
    Date of Patent: December 24, 1985
    Assignee: Pfizer Inc.
    Inventor: Lawrence A. Reiter
  • Patent number: 4560697
    Abstract: Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein R is (C.sub.1 -C.sub.5) perfluoroalkyl and R.sup.1 is H or CH.sub.3, method for their use in combatting fungal infections in plants, seeds and animals, including humans; and as antileishmanial agents, and pharmaceutical and agricultural compositions containing them.
    Type: Grant
    Filed: January 16, 1984
    Date of Patent: December 24, 1985
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Peter J. Whittle
  • Patent number: 4552843
    Abstract: A new acidic polycyclic ether antibiotic, CP-63,517, having the formula: ##STR1## and cationic salts thereof produced by submerged aerobic propagation of Streptomyces endus subsp. aureus, ATCC-39574, a new strain of microorganism isolated from a soil sample in Japan, a process for producing this antibiotic and methods for its use to improve feed utilization, promote growth of cattle and swine and to control coccidiosis.
    Type: Grant
    Filed: February 17, 1984
    Date of Patent: November 12, 1985
    Assignee: Pfizer Inc.
    Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
  • Patent number: 4530792
    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.
    Type: Grant
    Filed: November 1, 1982
    Date of Patent: July 23, 1985
    Assignee: Pfizer Inc.
    Inventor: Paul D. Weeks
  • Patent number: 4529732
    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.
  • Patent number: 4526579
    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.
    Type: Grant
    Filed: June 17, 1983
    Date of Patent: July 2, 1985
    Assignee: Pfizer Inc.
    Inventor: Parviz R. Ainpour
  • Patent number: 4518604
    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.
    Type: Grant
    Filed: October 27, 1983
    Date of Patent: May 21, 1985
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Peter J. Whittle
  • Patent number: 4503063
    Abstract: Compounds of the formula ##STR1## a pharmaceutically or agriculturally acceptable salt thereof, wherein R is 5-chloro-2-pyridyl or phenyl optionally substituted by one to three substituents, each independently selected from F, Cl, Br, I, CF.sub.3, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy; R.sup.1 is CONR.sup.2 R.sup.3 where either(a) R.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.3 is C.sub.2 -C.sub.4 alkanoyl or optionally substituted benzoyl; or(b) R.sup.2 and R.sup.3 are each (C.sub.1 -C.sub.4 alkoxy)carbonyl; and R.sup.4 and R.sup.5 are each H or CH.sub.3 ; methods for their use in combating fungal infections in plants, seeds and animals, including humans, and pharmaceutical and agricultural compositions containing them.
    Type: Grant
    Filed: September 26, 1983
    Date of Patent: March 5, 1985
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Kelvin Cooper
  • Patent number: 4486428
    Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.
    Type: Grant
    Filed: January 13, 1983
    Date of Patent: December 4, 1984
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4483862
    Abstract: Compounds of the formula ##STR1## or a pharmaceutically or agriculturally acceptable acid addition salt thereof wherein m and n are independently 0, 1, 2, 3 or 4; method for their use in combatting fungal infections in plants, seeds and animals, including humans; and pharmaceutical and agricultural compositions containing said compounds or salts.
    Type: Grant
    Filed: January 16, 1984
    Date of Patent: November 20, 1984
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Peter J. Whittle
  • Patent number: 4482558
    Abstract: Compounds of the general formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R is naphthyl, biphenylyl, phenyl or substituted phenyl; and R.sup.1 is ##STR2## where X is O or S, R.sup.2 is H, or C.sub.1 -C.sub.4 alkyl and R.sup.3 is H, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, optionally mono- or disubstituted phenyl, benzyl or Het and Het is pyridyl, pyrimidinyl or pyrazinyl; said substituents being halo, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or hydroxy, or R.sup.2 and R.sup.3 taken together complete a 1-pyrrolidinyl or piperidino ring; methods for their use in combatting fungal infections in plants and animals, including humans; pharmaceutical and agricultural compositions containing them and intermediates useful in their preparation.
    Type: Grant
    Filed: June 3, 1983
    Date of Patent: November 13, 1984
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Peter J. Whittle
  • Patent number: 4482723
    Abstract: Novel intermediates of the formula ##STR1## where R.sup.1 and R.sup.2 are each (C.sub.1 -C.sub.4)alkyl or taken together are (C.sub.2 -C.sub.4)alkylene, and their use in a process for preparation of compounds of the formula ##STR2## where R is (C.sub.1 -C.sub.6)alkyl or (CH.sub.2).sub.n Ar, Ar is phenyl or phenyl monosubstituted by Cl, Br, F, CH.sub.3 or OCH.sub.3 and n is 2 to 4; which comprises contacting one of said intermediates with an amidine of formula ##STR3## in the presence of reaction inert solvent and base; and a process for preparing a further intermediate, 1,2-dichloro-1-buten-3-one.
    Type: Grant
    Filed: April 11, 1983
    Date of Patent: November 13, 1984
    Assignee: Pfizer Inc.
    Inventor: Lawrence A. Reiter