Patents Represented by Attorney Paul D. Thomas
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Patent number: 4680404Abstract: 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: GrantFiled: August 9, 1984Date of Patent: July 14, 1987Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4656265Abstract: 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: GrantFiled: June 21, 1984Date of Patent: April 7, 1987Assignee: Pfizer Inc.Inventors: Joseph G. Lombardino, Anthony Marfat
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Patent number: 4625041Abstract: 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: GrantFiled: August 29, 1985Date of Patent: November 25, 1986Assignee: Pfizer Inc.Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
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Patent number: 4616027Abstract: 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: GrantFiled: July 25, 1983Date of Patent: October 7, 1986Assignee: Pfizer Inc.Inventors: Kenneth Richardson, Peter J. Whittle
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Patent number: 4616026Abstract: 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: GrantFiled: July 25, 1983Date of Patent: October 7, 1986Assignee: Pfizer Inc.Inventors: Kenneth Richardson, Peter J. Whittle
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Patent number: 4601897Abstract: 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: GrantFiled: November 6, 1985Date of Patent: July 22, 1986Assignee: Pfizer Inc.Inventor: Craig A. P. D. Saxton
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Patent number: 4582907Abstract: 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: GrantFiled: April 8, 1985Date of Patent: April 15, 1986Assignee: Pfizer Inc.Inventor: Malcolm M. Campbell
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Patent number: 4576964Abstract: 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: GrantFiled: June 7, 1984Date of Patent: March 18, 1986Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4560690Abstract: 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: GrantFiled: April 30, 1984Date of Patent: December 24, 1985Assignee: Pfizer Inc.Inventor: Lawrence A. Reiter
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Patent number: 4560697Abstract: 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: GrantFiled: January 16, 1984Date of Patent: December 24, 1985Assignee: Pfizer Inc.Inventors: Kenneth Richardson, Peter J. Whittle
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Patent number: 4552843Abstract: 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: GrantFiled: February 17, 1984Date of Patent: November 12, 1985Assignee: Pfizer Inc.Inventors: Walter D. Celmer, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
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Patent number: 4530792Abstract: 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: GrantFiled: November 1, 1982Date of Patent: July 23, 1985Assignee: Pfizer Inc.Inventor: Paul D. Weeks
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Patent number: 4529732Abstract: 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: GrantFiled: March 14, 1983Date of Patent: July 16, 1985Assignee: Pfizer Inc.Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4526579Abstract: 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: GrantFiled: June 17, 1983Date of Patent: July 2, 1985Assignee: Pfizer Inc.Inventor: Parviz R. Ainpour
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Patent number: 4518604Abstract: 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: GrantFiled: October 27, 1983Date of Patent: May 21, 1985Assignee: Pfizer Inc.Inventors: Kenneth Richardson, Peter J. Whittle
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Patent number: 4503063Abstract: 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: GrantFiled: September 26, 1983Date of Patent: March 5, 1985Assignee: Pfizer Inc.Inventors: Kenneth Richardson, Kelvin Cooper
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Patent number: 4486428Abstract: 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: GrantFiled: January 13, 1983Date of Patent: December 4, 1984Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4483862Abstract: 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: GrantFiled: January 16, 1984Date of Patent: November 20, 1984Assignee: Pfizer Inc.Inventors: Kenneth Richardson, Peter J. Whittle
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Patent number: 4482558Abstract: 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: GrantFiled: June 3, 1983Date of Patent: November 13, 1984Assignee: Pfizer Inc.Inventors: Kenneth Richardson, Peter J. Whittle
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Patent number: 4482723Abstract: 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: GrantFiled: April 11, 1983Date of Patent: November 13, 1984Assignee: Pfizer Inc.Inventor: Lawrence A. Reiter