Patents Represented by Attorney, Agent or Law Firm Carl J. Goddard
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Patent number: 6828343Abstract: This invention relates to compounds of Formula I or stereoisomers, pharmaceutically acceptable salts or prod rugs thereof or a pharmaceutically acceptable salts of the prodrugs. This invention also relates to pharmaceutical compositions comprising a compound of Formula I, and to methods of treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, or tissue ischemia.Type: GrantFiled: February 14, 2003Date of Patent: December 7, 2004Assignee: Pfizer, Inc.Inventor: Daisy Joe Du Bois
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Patent number: 6821977Abstract: A compound of the formula whereon R1 is: R5 is: and n, m, Z, R8, R9, R10 and R11 are as defined herein, useful in the treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia, particularly myocardial ischemia.Type: GrantFiled: February 19, 2003Date of Patent: November 23, 2004Assignee: Pfizer, Inc.Inventor: Ronald B. Gammill
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Patent number: 6759534Abstract: The present invention relates to a process for preparing pyridazinone aldose reductase inhibitors which are useful in the prevention and/or treatment of diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. The invention also relates to novel intermediates useful in preparing those aldose reductase inihibitors.Type: GrantFiled: January 7, 2003Date of Patent: July 6, 2004Assignee: Pfizer Inc.Inventor: Norma J. Tom
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Patent number: 6734303Abstract: The invention provides a process for the production of a compound of formula (A) or a pharmaceutically acceptable salt or solvate thereof: which comprises condensing a compound of formula (B) with a compound of formula (C): Compounds of formula (A) are useful in the treatment of benign prostatic hyperplasia.Type: GrantFiled: May 13, 2002Date of Patent: May 11, 2004Assignee: Pfizer Inc.Inventors: Jens Bertil Ahman, Paul Blaise Hodgson, Sarah Jane Lewandowski, Robert Walton
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Patent number: 6696574Abstract: The instant invention provides novel processes and intermediates useful in the preparation of certain N-(indole-2-carbonyl)-&bgr;-alaninamide compounds, which compounds are glycogen phosphorylase inhibitors useful in the treatment of diseases such as hypercholesterolemia, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis, diabetes, diabetic cardiomyopathy, infection, tissue ischemia, myocardial ischemia, and in inhibiting tumor growth.Type: GrantFiled: January 16, 2003Date of Patent: February 24, 2004Assignee: Pfizer Inc.Inventors: Mark T. Barrila, Frank R. Busch, Michel A. Couturier, Susan L. Orrill, Peter R. Rose, Derek L. Tickner, Harry O. Tobiassen, Gregory J. Withbroe
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Patent number: 6683106Abstract: The instant invention provides crystal forms of 5-chloro-N-[(1S,2R)-3-[3R,4S]-3,4-dihydroxy-1-pyrrolidinyl]-2-hydroxy-3-oxo-1-(phenyl) methyl)propyl]-1H-indole-2-carboxamide (I) processes for the production of such crystal forms; pharmaceutical compositions comprising such crystal forms; and methods of treating glycogen phosphorylase dependent diseases, or conditions with such crystal forms, or such pharmaceutical compositions.Type: GrantFiled: April 15, 2003Date of Patent: January 27, 2004Assignee: Pfizer Inc.Inventors: Douglas J. M. Allen, Frank R. Busch, Joseph F. Krzyzaniak, Zheng Jane Li, Susan L. Orrill, Peter R. Rose, Derek L. Tickner, Harry O. Tobiassen
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Patent number: 6683085Abstract: The present invention provides 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)quinazoline mesylate of the formula together with processes for preparing, and compositions containing it. The invention also relates to substantially pure anhydrous crystalline polymorphic forms of the free base. The compounds are particularly useful in the treatment of benign prostatic hyperplasia.Type: GrantFiled: March 1, 2001Date of Patent: January 27, 2004Assignee: Pfizer Inc.Inventors: Patricia Ann Basford, Paul Blaise Hodgson
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Patent number: 6653302Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted; R4 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 ring, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.Type: GrantFiled: December 13, 2002Date of Patent: November 25, 2003Assignee: Pfizer Inc.Inventor: David Nathan Abraham Fox
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Patent number: 6653339Abstract: The present invention is directed to a a method for the treatment of irritable bowel syndrome comprising the multiple daily pulse dosing of an immediate release formulation of the anti-muscarinic darifenacin. Dosing two or three times a day is particularly preferred.Type: GrantFiled: August 13, 2002Date of Patent: November 25, 2003Assignee: Pfizer Inc.Inventors: Peter James Dunn, Michael John Humphrey, Paul Quinn
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Patent number: 6649620Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 alkyl or SO2NH2; R3 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof, are useful in the treatment of a variety of disorders including benign prostatic hyperplasia.Type: GrantFiled: September 23, 2002Date of Patent: November 18, 2003Assignee: Pfizer Inc.Inventors: Alan John Collis, David Nathan Fox
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Patent number: 6649634Abstract: This invention relates to certain indole-2-carboxamides of formula (I) and the pharmaceutically acceptable salts and prodrugs thereof, wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, C(O)NR8R9 or C(O)R12, useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds.Type: GrantFiled: June 14, 2001Date of Patent: November 18, 2003Assignee: Pfizer, Inc.Inventors: Dennis J. Hoover, Bernard Hulin, William H. Martin, Judith L. Treadway
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Patent number: 6642242Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 19, 2001Date of Patent: November 4, 2003Assignee: Pfizer Inc.Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
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Patent number: 6610746Abstract: The present invention provides methods of treating non-insulin dependent diabetes mellitus, insulin resistance, Syndrome X, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, polycystic ovary syndrome, cataracts, hyperglycemia, or impaired glucose tolerance, the methods comprising the step of administering to a patient having or at risk of having non-insulin dependent diabetes mellitus, insulin resistance, Syndrome X, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, polycystic ovary syndrome, cataracts, hyperglycemia, or impaired glucose tolerance a synergistic amount of:1) a sulfonylurea, a non-sulfonylurea K+ ATP channel blocker, or a sulfonylurea and a non-sulfonylurea K+ ATP channel blocker; and 2) a cAMP phosphodiesterase type 3 inhibitor.Type: GrantFiled: April 10, 2001Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: David A. Fryburg, Janice C. Parker
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Patent number: 6576653Abstract: This invention relates to compounds of Formula I or stereoisomers, pharmaceutically acceptable salts or prodrugs thereof or a pharmaceutically acceptable salts of the prodrugs. This invention also relates to pharmaceutical compositions comprising a compound of Formula I, and to methods of treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, or tissue ischemia.Type: GrantFiled: April 5, 2002Date of Patent: June 10, 2003Assignee: Pfizer Inc.Inventor: Daisy Joe Du Bois
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Patent number: 6555578Abstract: The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or R3 is the radical wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R9 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group; R4 is hydrogen, halogen, trifluoromType: GrantFiled: October 16, 2001Date of Patent: April 29, 2003Assignee: Pfizer Inc.Inventors: Peter Cornelius, Diane Hargrove, Bradley P. Morgan, Andrew G. Swick
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Patent number: 6531449Abstract: The invention provides metabolites of the compound 2-amino-N-[2-(3a(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo-[4,3-c]pyridin-5-yl)-1-(R)-benzyl-oxymethyl-2-oxo-ethyl]-isobutyramide, the racemic-diastereomeric mixtures and optical isomers thereof, the prodrugs thereof, and the pharmaceutically acceptable salts of the metabolites, racemic-diastereomeric mixtures, optical isomers, and prodrugs; to pharmaceutical compositions thereof; and to methods of using the metabolites and the compositions in the treatment of diseases associated with reduced levels of growth hormone.Type: GrantFiled: March 8, 2001Date of Patent: March 11, 2003Assignee: Pfizer Inc.Inventors: S. Cyrus Khojasteh, John P. O'Donnell
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Patent number: 6521629Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-4 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted; R4 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 ring, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia, or represents a chain of formula Ib, and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.Type: GrantFiled: November 13, 2001Date of Patent: February 18, 2003Assignee: Pfizer Inc.Inventor: David Nathan Abraham Fox
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Patent number: 6503222Abstract: The present invention provides an apparatus for facilitating the oral delivery of an active agent to a patient in need of treatment therewith, which apparatus comprises an active agent mixing chamber, a mixture delivery tube, and at least one liquid delivery tube. A mixture formed in the mixing chamber which comprises a combination of an active agent, or a pharmaceutical formulation thereof, and a liquid diluent may be delivered into the oral cavity of the patient from the mixing chamber by suction on the mixture delivery tube.Type: GrantFiled: September 21, 2001Date of Patent: January 7, 2003Assignee: Pfizer IncInventor: Julian B. Lo
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Patent number: 6497899Abstract: Described are non-friable, rapidly disintegrating, fast-dissolving solid dosage forms that are produced from pharmaceutically acceptable steam extruded polymers. The solid dosage forms dissolve in the mouth and are particularly useful for subjects that require or desire oral medication but have difficulty swallowing standard oral dosage forms such as tablets or in subjects suffering from emesis. The solid dosage forms are also useful for rapid drug delivery as vaginal or rectal suppositories or for oral delivery of veterinary drugs.Type: GrantFiled: January 18, 2001Date of Patent: December 24, 2002Assignee: Pfizer, Inc.Inventors: Avinash G. Thombre, Larry S. Wigman
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Patent number: 6423351Abstract: The invention provides methods for inhibiting oxidative degradation of pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient which methods comprise adding an oxidation-inhibiting amount of a ferrous ion source, preferably in the form of a pharmaceuticalexcipient, to the formulation. The invention further provides pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient and an oxidation-inhibiting amount of a ferrous iron source, preferably in the form of a pharmaceuticalexcipient. The invention still further provides for the use of a ferrous ion source as an anti-oxidant in pharmaceutical formulations.Type: GrantFiled: March 9, 2001Date of Patent: July 23, 2002Assignee: Pfizer Inc.Inventor: Hai Wang