Patents Represented by Attorney, Agent or Law Firm Robert T. Ronau
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Patent number: 6005133Abstract: The enantioselective borane reduction of prochiral ketones to optically pure alcohols is effectively achieved by performing the reduction in the presence of catalytic amounts of the new and valuable oxazaborolidine compounds of formulae (I) and (II). The compounds of formulae (I) and (II) may be isolated and purified prior to use in the reduction reactions or the compounds of formulae (I) and (II) may be generated in situ.Type: GrantFiled: October 10, 1995Date of Patent: December 21, 1999Assignee: Pfizer Inc.Inventor: George Joseph Quallich
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Patent number: 5883080Abstract: Antiparasitic avermectin derivatives of formula (I), where the broken line represents an optional bond, R.sup.1 and R.sup.4 are independently H, OH, halo, oximino, or an organic radical, R.sup.2, R.sup.6 and R.sup.7 are organic radicals and R.sup.3 is alpha-oleandrosyl or 4'-(alpha-oleandrosyl)-alpha-oleandrosyl optionally substituted at the 4'- or 4"-position, and R.sup.12 and R.sup.13 are independently H, CN, CONH.sub.2, C.sub.1 -C.sub.8 alkyl or aryl optionally substituted with at least one halo, OH, C.sub.1 -C.sub.8 alkylthio group.Type: GrantFiled: January 16, 1998Date of Patent: March 16, 1999Assignee: Pfizer Inc.Inventors: Christopher James Dutton, Stephen Paul Gibson, Michael John Witty
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Patent number: 5861393Abstract: This invention relates to compounds of formula (I), ##STR1## pharmaceutically acceptable salt thereof, and pharmaceutically acceptable solvates of either entity, wherein X is CH or N; Y is optionally monousaturated C.sub.3 -C.sub.5 alkylene optionally substituted with C.sub.1 -C.sub.4 allyl or methylene; R.sup.1 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or C.sub.3 -C.sub.6 alkenyl; R.sup.2 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or CONR.sup.5 R.sup.6 ; R.sup.3 and R.sup.4 are each independently selected from H; C.sub.1 -C.sub.4 alkyl optionally substituted with NR.sup.5 R.sup.6 ; C.sub.1 -C.sub.4 alkoxy; halo; CONR.sup.5 R.sup.6 and aryl; and R.sup.5 and R.sup.6 are each independently selected from H and C.sub.1 -C.sub.Type: GrantFiled: July 30, 1997Date of Patent: January 19, 1999Assignee: Pfizer Inc.Inventors: John Christopher Danilewicz, David Ellis, Ryszard Jurek Kobylecki
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Patent number: 5859044Abstract: The present invention relates to certain compounds of the formula (I) the racemic-enantiomeric mixtures and optical isomers of said compounds, prodrugs thereof and the pharmaceutically acceptable salts, depicted below, which are .beta.-adrenergic receptor agonists and accordingly have utility as, inter alia, hypoglycemic and antiobesity agents. The invention also relates to methods of use for the compounds and to compositions containing them. The compounds of the present invention also possess utility for increasing lean meat deposition and/or improving the lean meat to fat ratio in animals, e.g., ungulate animals, companion animals, especially dogs, and poultry. The compounds of formula (I) have the following structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the specification.Type: GrantFiled: July 14, 1997Date of Patent: January 12, 1999Assignee: Pfizer Inc.Inventors: Robert L. Dow, Kristin M. Lundy
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Patent number: 5849730Abstract: A compound of the formula (IV) ##STR1## and a process for preparing the compound of formula (IV). Also disclosed is a process for preparing C-16-demethylrapamycin and C-39-demethylrapamycin. The process of this invention comprises fermenting Actinoplanes sp. ATCC 63771 in the presence of rapamycin and isolating the products produced thereby.Type: GrantFiled: January 16, 1997Date of Patent: December 15, 1998Assignee: Pfizer Inc.Inventors: Mark A. Guadliana, Susan J. Truesdell
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Patent number: 5843972Abstract: The present invention relates to certain compounds of the formula (I) the racemic-enantiomeric mixtures and optical isomers of said compounds and the pharmaceutically acceptable salts or prodrugs thereof, depicted below, which are .beta.-adrenergic receptor agonists and accordingly have utility as, inter alia, hypoglycemic and antiobesity agents. More specifically, the compounds of the instant invention are selective agonists of .beta..sub.3 -adrenergic receptor. The invention also relates to methods of use for the compounds and to pharmaceutical compositions containing them. The compounds of the present invention also possess utility for increasing lean meat deposition and/or improving the lean meat to fat ratio in animals, e.g., ungulate animals, companion animals and poultry. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z are as defined in the specification.Type: GrantFiled: March 28, 1997Date of Patent: December 1, 1998Assignee: Pfizer Inc.Inventors: Robert L. Dow, Stephen W. Wright
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Patent number: 5798352Abstract: This invention is directed to compounds of formula (I), ##STR1## pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates of either entity, wherein Y is optionally monounsaturated C.sub.3 -C.sub.5 alkylene optionally substituted with C.sub.1 -C.sub.4 alkyl or methylene; R.sup.1 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or C.sub.3 -C.sub.6 alkenyl; R.sup.2 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or CONR.sup.5 R.sup.6 ; R.sup.3 and R.sup.4 are each independently selected from H; C.sub.1 -C.sub.4 alkyl optionally substituted with NR.sup.5 R.sup.6 ; C.sub.1 -C.sub.4 alkoxy; halo; CONR.sup.5 R.sup.6 and aryl; aryl is phenyl optionally substituted with one, two or three substituents independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.Type: GrantFiled: October 9, 1997Date of Patent: August 25, 1998Assignee: Pfizer Inc.Inventor: John Christopher Danilewicz
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Patent number: 5789408Abstract: Compounds of formula (I) are active antiviral compounds useful in the treatment of viral infections in mammals. The compounds of the invention are readily prepared by reaction of a suitable 2-thiothiazole derivative with an appropriate Het-(CH.sub.2).sub.n -halide.Type: GrantFiled: January 11, 1996Date of Patent: August 4, 1998Assignee: Pfizer Inc.Inventors: Edward Fox Kleinman, Hiroko Masamune, Vinod Dipak Parikh
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Patent number: 5776735Abstract: The process of this invention is directed to isolating or otherwise obtaining an olefinic macrolide producing microorganism which microorganism does not contain epoxidase enzyme activity. This invention also relates to a process for preparing said olefinic macrolide by fermenting a mutant microorganism lacking epoxidase activity, designated rosX herein, which mutant is obtained from the wild-type microorganism. This invention also relates to a rosX mutant of Micromonospora rosaria, and to any microorganism having the identifying characteristics thereof, said mutant also designated ATCC 55709. This invention also relates to a process for preparing repromicin, the compound of formula (II), ##STR1## by mutating a wild-type microorganism capable of producing rosamicin to produce a mutant microorganism lacking epoxidase activity such that repromicin is produced by said mutant microorganism.Type: GrantFiled: November 6, 1996Date of Patent: July 7, 1998Assignee: Pfizer Inc.Inventors: Claudio D. Denoya, Edmund W. Hafner, Hamish A. I. McArthur
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Patent number: 5767133Abstract: The present invention relates to compounds of the formula ##STR1## having utility as hypoglycemic and antiobesity agents, methods for their use and pharmaceutical compositions containing them. The compounds of the present invention also possess utility for increasing lean meat deposition and/or improving lean meat to fat ratio in edible animals, i.e. ungulate animals and poultry.Type: GrantFiled: December 14, 1995Date of Patent: June 16, 1998Assignee: Pfizer Inc.Inventors: Robert L. Dow, Stephen W. Wright
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Patent number: 5750520Abstract: This invention relates to compounds of formula (I), ##STR1## pharmaceutically acceptable salt thereof, and pharmaceutically acceptable solvates of either entity, wherein X is CH or N; Y is optionally monousaturated C.sub.3 -C.sub.5 alkylene optionally substituted with C.sub.1 -C.sub.4 alkyl or methylene; R.sup.1 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or C.sub.3 -C.sub.6 alkenyl; R.sup.2 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or CONR.sup.5 R.sup.6 ; R.sup.3 and R.sup.4 are each independently selected from H; C.sub.1 -C.sub.4 alkyl optionally substituted with NR.sup.5 R.sup.6 ; C.sub.1 -C.sub.4 alkoxy; halo; CONR.sup.5 R.sup.6 and aryl; R.sup.5 and R.sup.6 are each independently selected from H and C.sub.1 -C.sub.Type: GrantFiled: April 19, 1996Date of Patent: May 12, 1998Assignee: Pfizer Inc.Inventors: John Christopher Danilewicz, David Ellis, Ryszard Jurek Kobylecki
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Patent number: 5723488Abstract: A compound of formula (I): ##STR1## wherein the broken lines represent independently optional bonds, R.sup.1 and R.sup.2 being absent when the C.sub.22 -C.sub.23 double bond is present.Type: GrantFiled: August 12, 1996Date of Patent: March 3, 1998Assignee: Pfizer Inc.Inventor: Nigel Derek Walshe
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Patent number: 5710168Abstract: A method of blocking N-methyl-D-aspartic acid (NMDA) receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of 2-piperidino-1-alkanol derivatives and 2-azabicyclo-1-alkanol derivatives and analogs and pharmaceutically acceptable salts thereof; methods of using these compounds in the treatment of stroke, spinal cord trauma, traumatic brain injury, multiinfarct dementia, CNS degenerative diseases such as Alzheimer's disease, senile dementia of the Alzheimer's type, Huntington's disease, Parkinson's disease, epilepsy, amyotrophic lateral sclerosis, pain, AIDS dementia, psychotic conditions, drug addictions, migraine, hypoglycemia, anxiolytic conditions, urinary incontinence and an ischemic event arising from CNS surgery, open heart surgery or any procedure during which the function of the cardiovascular system is compromised.Type: GrantFiled: November 9, 1994Date of Patent: January 20, 1998Assignee: Pfizer Inc.Inventor: Bertrand L. Chenard
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Patent number: 5696126Abstract: Phenolic prodrug esters of certain 1-(hydroxyphenyl)-2-piperidino-1-alkanol derivatives, which are useful in the treatment of stroke, traumatic head injury and CNS degenerative disease; and intermediates useful in their synthesis.Type: GrantFiled: April 7, 1995Date of Patent: December 9, 1997Assignee: Pfizer Inc.Inventor: Bertrand Leo Chenard
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Patent number: 5677332Abstract: This invention is directed to novel antiparasitic compounds of formula (I), wherein the broken line represents an optional bond, R.sup.1 and R.sup.4 being absent when this bond is present, R.sup.1, R.sup.3, R.sup.4 are independently H, OH, halo mercapto, oxo, oximino, or an organic radical, R.sup.2 and R.sup.7 are organic radicals, R.sup.6 is H or an organic radical and R.sup.12 is OH, halo, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.9 alkanoyloxy, or oximino optionally O-substituted by a C.sub.1 -C.sub.8 alkyl, alkenyl, alkynyl, aryl, trialkylsilyl, aralkyl or C.sub.1 -C.sub.9 alkanoyl group.Type: GrantFiled: December 22, 1995Date of Patent: October 14, 1997Assignee: Pfizer Inc.Inventor: Bernard Joseph Banks
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Patent number: 5665708Abstract: Intermediates and a process for preparing doramectin, the compound of formula (I), semisynthetically from by-product in the fermentation procedure which also yields the compound of formula (I). The intermediates prepared by the process of this invention also have utility as antiparasitic agents. The process of this invention utilizes continuous reaction inert gas sparging during the pyrolysis step, resulting in a significant improvement in the overall yield of this conversion.Type: GrantFiled: March 8, 1996Date of Patent: September 9, 1997Assignee: Pfizer Inc.Inventors: Constantine Sklavounos, Thomas Charles Crawford, Neil Demers, Stephen Paul Gibson, Charles William Murtiashaw, deceased
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Patent number: 5654302Abstract: Phenolic prodrug esters of certain 1-(hydroxyphenyl)-2-piperidino-1-alkanol derivatives, which are useful in the treatment of stroke, traumatic head injury and CNS degenerative disease; and intermediates useful in their synthesis.Type: GrantFiled: April 7, 1995Date of Patent: August 5, 1997Assignee: Pfizer Inc.Inventor: Bertrand Leo Chenard
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Patent number: 5633006Abstract: A pharmaceutical composition having reduced bitterness consisting of a bitter pharmaceutical agent, a taste-masking component and a pharmaceutically acceptable carrier. The taste-masking component is an alkaline earth oxide, an alkaline earth hydroxide or an alkaline hydroxide and does not interfere with the activity of the pharmaceutical agent.Type: GrantFiled: October 24, 1994Date of Patent: May 27, 1997Assignee: Pfizer Inc.Inventors: Joseph S. Catania, Alton D. Johnson
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Patent number: 5631235Abstract: Macrolides of formula (I) and methods of treatment of resistance to transplantation, fungal infections and autoimmune diseases such as rheumatoid arthritis and psoriasis using said macrolides of formula (I), wherein n is 1 or 2; A and B are taken together and form .dbd.O or A and B are taken separately and are each H or A is OH and B is H; R.sup.1 is a 2-aminoglycosyl group; R.sup.2 is OH or a glycosyloxy group; and R.sup.3 is an alkyl or allyl group.Type: GrantFiled: August 6, 1994Date of Patent: May 20, 1997Assignee: Pfizer, Inc.Inventors: Kevin Koch, Gary R. Schulte
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Patent number: 5621084Abstract: This invention relates to a process for the removal of an allyl or allyloxycarbonyl group from an allyl or allyloxycarbonyl group protected compound (such as an allylic ester, carbonate, carbamate, O-allyl derivatives or N-allyl derivatives), which comprises contacting the allyl or allyloxycarbonyl group protected compound with a sulfinic acid compound, in the presence of a palladium catalyst in a reaction-inert solvent. Preferably, the sulfinic acid compound is represented by the formula:X--SO.sub.2 M (I)wherein X is C.sub.1-20 alkyl, substituted C.sub.1-20 alkyl (wherein the substituent(s) are independently halo, nitro, sulfo, oxo, amino, cyano, carboxy, hydroxy or moieties derived therefrom), phenyl, substituted phenyl (wherein the substituent(s) are independently C.sub.1-3 alkyl, halo nitro, sulfo, oxo, amino, cyano, carboxy, hydroxy, acetamido or moieties derived therefrom), furyl or thienyl; and M is hydrogen, an alkali metal or ammonium salt residue.Type: GrantFiled: April 3, 1995Date of Patent: April 15, 1997Assignee: Pfizer Inc.Inventors: Msanori Honda, Hiromasa Morita, Isao Nagakura