Patents Represented by Attorney D. Stuart McFarlin
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Patent number: 5364938Abstract: The invention provides antifungal agents of the formula: ##STR1## and their pharmaceutically acceptable salts, whereinR is phenyl optionally substituted by 1 to 3substituents each independently selected from halo and CF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl; and"Het", which is attached to the adjacent carbon atom by a ring carbon atom, is selected from pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and triazinyl, "Het" being optionally substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, CN, NO.sub.2, NH.sub.2, --NH(C.sub.1 -C.sub.4 alkanoyl) or --NHCO.sub.2 (C.sub.1 -C.sub.4 alkyl).Type: GrantFiled: March 4, 1993Date of Patent: November 15, 1994Assignee: Pfizer Inc.Inventors: Roger P. Dickinson, Kenneth Richardson
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Patent number: 5334604Abstract: There are disclosed preparative processes and hypoglycemic compounds of the formula ##STR1## wherein R is hydrogen or C1 to C3 alkyl;R.sup.1 and R.sup.2 are taken together and are carbonyl; or R.sup.1 and R.sup.2 are taken separately, wherein R.sup.1 is hydrogen or R.sup.4 and R.sup.2 is--COR.sup.5 and COOR.sup.5 ;R.sup.3, R.sup.4 and R.sup.5 are each independently C1 to C9 alkyl, C3 to C7 cycloalkyl, phenyl, naphthyl, furyl, benzofuryl or thienyl or one of said groups mono- or disubstituted with C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 alkoxy-carbonyl, trifluoromethyl, fluoro or chloro; and n is 0 or 1; or pharmaceutically acceptable cationic salts thereof.Type: GrantFiled: February 22, 1993Date of Patent: August 2, 1994Assignee: Pfizer Inc.Inventors: Steven W. Goldstein, Ruth E. McDermott
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Patent number: 5332857Abstract: Variously substituted 3,5-dihydroxy-6,8-nonadienoic acids and esters, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.Type: GrantFiled: July 6, 1992Date of Patent: July 26, 1994Assignee: Pfizer Inc.Inventors: Peter A. McCarthy, Frederick J. Walker
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Patent number: 5319103Abstract: Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-penem-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, useful as systemic antibacterial agents; and intermediates and processes which are useful in the said synthesis of said diastereoisomers.Type: GrantFiled: February 11, 1993Date of Patent: June 7, 1994Assignee: Pfizer Inc.Inventor: Robert A. Volkmann
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Patent number: 5300668Abstract: 1-[4'-(2"-Ethyl-5",7"-dimethylimidazo[4,5-b]pyridin-3-yl)methylphenyl]cyclo pent-3-ene-1-carboxylic acid and its pharmaceutically acceptable salts inhibit angiotensin II in mammals and are useful in treating conditions such as hypertension, congestive heart failure and glaucoma and as the active ingredient in pharmaceutical compositions for treating such conditions.Type: GrantFiled: March 10, 1993Date of Patent: April 5, 1994Assignee: Pfizer Inc.Inventor: Paul A. Dasilva Jardine
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Patent number: 5278175Abstract: The invention provide antifungal compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;X is CH or N; andY is F or Cl.Type: GrantFiled: October 5, 1992Date of Patent: January 11, 1994Assignee: Pfizer Inc.Inventors: Stephen J. Ray, Kenneth Richardson
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Patent number: 5256789Abstract: Compounds having the structure ##STR1## wherein X is nitrogen, oxygen, sulfur or a bond and Z is oxygen or sulfur have been synthesized. These compounds are lipoxygenase inhibitors and are useful as the active agent in pharmaceutical compositions for treating inflammatory conditions in humans and other mammals for which lipoxygenase activity has been implicated.Type: GrantFiled: February 18, 1992Date of Patent: October 26, 1993Assignee: Pfizer Inc.Inventors: Rodney W. Stevens, Takafumi Ikeda, Hiroaki Wakabayashi, Masami Nakane
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Patent number: 5227397Abstract: This invention relates to certain polyamines and polypeptides found to be present in the venom of the Agelenopsis aperta spider. The polyamines of this invention and the salts thereof antagonize excitatory amino acid neurotransmitters, which neurotransmitters affect cells of various organisms and are useful in antagonizing said neurotransmitters, per se, in the treatment of excitatory amino acid neurotransmitter mediated diseases and conditions and in the control of invertebrate pests. The polypeptides of this invention and one of said polyamines and the salts thereof block calcium channels in cells of various organisms and are useful in blocking said calcium channels in cells, per se, in the treatment of calcium channel mediated diseases and conditions and in the control of invertebrate pests. This invention also relates to compositions comprising said polyamines, polypeptides and salts thereof.Type: GrantFiled: July 17, 1990Date of Patent: July 13, 1993Assignee: Pfizer Inc.Inventors: Nicholas A. Saccomano, Robert A. Volkmann
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Patent number: 5206364Abstract: The invention provides antifungal agents of the formula: ##STR1## and their pharmaceutically acceptable salts, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and CF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl; and"Het", which is attached to the adjacent carbon atom by a ring carbon atom, is selected from pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl and triazinyl, "Het" being optionally substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3, CN, NO.sub.2, NH.sub.2, --NH(C.sub.1 -C.sub.4 alkanoyl) or --NHCO.sub.2 (C.sub.1 -C.sub.4 alkyl).Type: GrantFiled: March 4, 1992Date of Patent: April 27, 1993Assignee: Pfizer Inc.Inventors: Roger P. Dickinson, Kenneth Richardson
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Patent number: 5191077Abstract: Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-penem-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, useful as systemic antibacterial agents; and intermediates and processes which are useful in the said synthesis of said diastereoisomers.Type: GrantFiled: January 28, 1991Date of Patent: March 2, 1993Assignee: Pfizer Inc.Inventor: Robert A. Volkmann
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Patent number: 5185449Abstract: (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: GrantFiled: February 27, 1991Date of Patent: February 9, 1993Assignee: Pfizer Inc.Inventors: Dennis M. Godek, Charles W. Murtiashaw, Frank J. Urban, Brian C. Vanderplas
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Patent number: 5185369Abstract: 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: GrantFiled: August 23, 1991Date of Patent: February 9, 1993Assignee: Pfizer Inc.Inventors: Nicholas A. Saccomano, Robert A. Volkmann
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Patent number: 5169976Abstract: 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: GrantFiled: May 3, 1990Date of Patent: December 8, 1992Assignee: Pfizer Inc.Inventor: Peter A. McCarthy
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Patent number: 5158937Abstract: 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: GrantFiled: June 15, 1990Date of Patent: October 27, 1992Assignee: Pfizer Inc.Inventors: John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
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Patent number: 5157034Abstract: Antipsychotic compounds having the formula ##STR1## wherein Z is H or Cl; Y is O or S; n is 1-4; separately, X is H or (C.sub.1 -C.sub.2)alkyl and L is R(CH.sub.2).sub.m CO, m is 0 or 1-3, R is (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, phenyl, naphthyl, furyl, benzofuranyl, thienyl, benzothienyl, pyrrolyl, indolyl, isoindolyl or one of said groups substituted on aromatic or heteroaromatic ring with fluoro, chloro, (C.sub.1 -C.sub.2)alkyl or (C.sub.1 -C.sub.2)alkoxy; or together L and X, in combination with the nitrogen to which they are attached, form certain cyclic imides, 4-substituted piperidines or a cyclic sulfonamide.Type: GrantFiled: February 27, 1991Date of Patent: October 20, 1992Assignee: Pfizer Inc.Inventors: Gene M. Bright, Kishor A. Desai, Thomas F. Seeger
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Patent number: 5155097Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Streptomyces sp. ATCC 55028. This novel antibiotic is useful as an anticoccidial in chickens, in the prevention or treatment of swine dysentery, as a growth promotant in cattle and swine, and as an anthelmintic in mammals, particularly in dogs, cats, sheep, cattle and swine.Type: GrantFiled: May 23, 1990Date of Patent: October 13, 1992Assignee: Pfizer IncInventors: Walter P. Cullen, John P. Dirlam, Hiroshi Maeda, Junsuke Tone
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Patent number: 5151545Abstract: Variously substituted 3,5-dihydroxy-6,8-nonadienoic acids and esters, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.Type: GrantFiled: March 27, 1990Date of Patent: September 29, 1992Assignee: Pfizer Inc.Inventors: Peter A. McCarthy, Frederick J. Walker
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Patent number: 5147858Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 53676. This novel antibiotic is useful as an anticoccidial in chickens and as a growth promotant in cattle and swine.Type: GrantFiled: April 16, 1990Date of Patent: September 15, 1992Assignee: Pfizer IncInventors: John P. Dirlam, Walter P. Cullen, Hiroshi Maeda, Junsuke Tone
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Patent number: 5122596Abstract: This invention relates to a polypeptide found to be present in the venom of the Agelenopsis aperta spider and to polypeptides having substantially the same amino acid sequence and substantially the same activity as said polypeptide. The polypeptides of this invention and the salts thereof block calcium channels in cells of various organisms and are useful in blocking said calcium channels in cells, per se; in the treatment of calcium channel mediated diseases and conditions; and in the control of invertebrate pests. This invention also relates to compositions comprising said polypeptides and salts thereof.Type: GrantFiled: September 29, 1989Date of Patent: June 16, 1992Assignee: Pfizer Inc.Inventors: Douglas Phillips, Nicholas A. Saccomano, Robert A. Volkmann
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Patent number: 5122525Abstract: Anxiolytic agents which are racemic or optically active pyrido[1,2-a]pyrazine derivatives of the formula ##STR1## wherein x is N or CH and Y represents one of certain pyrazolo, triazolo, tetrazolo or cyclic imido radicals; and intermediates therefor.Type: GrantFiled: July 9, 1991Date of Patent: June 16, 1992Assignee: Pfizer Inc.Inventors: Gene M. Bright, Kishor A. Desai