Patents Represented by Attorney Michael P. Straher
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Patent number: 7705168Abstract: Disclosed herein is a manufacturing process for the preparation of tigecycline suitable for intravenous infusion.Type: GrantFiled: June 16, 2006Date of Patent: April 27, 2010Assignee: Wyeth LLCInventors: Gurmukh Chanana, Dominic Ventura, Richard Saunders, Mahdi B. Fawzi
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Patent number: 7368471Abstract: This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.Type: GrantFiled: March 29, 2006Date of Patent: May 6, 2008Assignee: WyethInventors: Hassan Mahmound Elokdah, Geraldine Ruth McFarlane, David Zenan Li, Lee Dalton Jennings, David LeRoy Crandall
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Patent number: 7345032Abstract: The present invention provides methods for the preparation of {2-[(8,9)-dioxo-2,6-diaza-bicyclo[5.2.0]-non-1(7)-en-2-yl]ethyl}phosphonic acid, and esters thereof.Type: GrantFiled: October 20, 2004Date of Patent: March 18, 2008Assignee: WyethInventors: Bogdan K. Wilk, Galina Vid, Weiguo Liu, Xinxu Shi
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Patent number: 7126683Abstract: The present invention provides a simple and direct method for the simultaneous correction of steady-state polarized fluorescence intensities, depolarized (or scrambled) by the effects of applied hydrostatic pressure without having to first determine the scrambling factors from a separate experiment. The method involves direct recalculation of the measured polarized data obtained for the sample of interest at the time of data collection.Type: GrantFiled: September 30, 2005Date of Patent: October 24, 2006Inventors: Lesley Davenport, Piotr Targowski
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Patent number: 7101875Abstract: This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.Type: GrantFiled: November 22, 2002Date of Patent: September 5, 2006Assignee: WyethInventors: John C. McKew, Steve Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
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Patent number: 7097969Abstract: The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is known (“known GPCRs”), and most particularly to mutated (non-endogenous) versions of the known GPCRs for use, most preferably in screening assays for the direct identification of candidate compounds as inverse agonists, agonists and partial agonists.Type: GrantFiled: August 24, 2004Date of Patent: August 29, 2006Assignee: Arena Pharmaceuticals, Inc.Inventors: Karin Lehmann-Bruinsma, Chen W. Liaw, I-Lin Lin
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Patent number: 7053083Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.Type: GrantFiled: April 11, 2002Date of Patent: May 30, 2006Assignee: WyethInventors: Amedeo Arturo Failli, Jay Scott Shumsky, Thomas Joseph Caggiano, John P. Dusza, Kevin A. Memoli
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Patent number: 6989388Abstract: The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula: wherein the constituent variables are as defined herein. The invention further provides methods for the use of the compounds disclosed herein.Type: GrantFiled: October 30, 2001Date of Patent: January 24, 2006Inventors: Roberto Pellicciari, Flavio Moroni
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Patent number: 6960607Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 11, 2002Date of Patent: November 1, 2005Assignee: WyethInventors: Michael S. Malamas, Iwan Gunawan, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
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Patent number: 6956646Abstract: The present invention provides a simple and direct method for the simultaneous correction of steady-state polarized fluorescence intensities, depolarized (or scrambled) by the effects of applied hydrostatic pressure without having to first determine the scrambling factors from a separate experiment. The method involves direct recalculation of the measured polarized data obtained for the sample of interest at the time of data collection.Type: GrantFiled: September 11, 2000Date of Patent: October 18, 2005Inventors: Lesley Davenport, Piotr Targowski
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Patent number: 6903091Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heteType: GrantFiled: April 11, 2002Date of Patent: June 7, 2005Assignee: WyethInventors: Amedeo A. Failli, Thomas J. Caggiano, Jay S. Shumsky, Eugene J. Trybulski, Kevin A. Memoli, John P. Dusza
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Patent number: 6884814Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1, R2, and R3 are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 11, 2002Date of Patent: April 26, 2005Assignee: WyethInventors: Michael S. Malamas, Tam Q. Dinh, Iwan Gunawan, Michael D. Collini, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
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Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze
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Patent number: 6841349Abstract: The invention provides a method for reducing stutter in the amplification of a microsatellite comprising the steps of providing a sample comprising a microsatellite having a G+C content of 50% or less; contacting the sample with at least one enzyme having nucleic acid polymerase activity; and incubating the sample with the enzyme for a sufficient amount of time and under conditions sufficient to amplify the microsatellite; wherein the incubation is performed in the presence of an amount of betaine, sorbitol or mixtures thereof, effective to reduce stutter relative to the amount of stutter observed in the absence of betaine and/or sorbitol. The invention also provides compositions containing betaine and/or sorbitol, kits for amplifying microsatellites having a G+C content of 50% or less, and methods of using all of the foregoing.Type: GrantFiled: May 7, 2001Date of Patent: January 11, 2005Assignee: Applera Corporation Applied Biosystems GroupInventors: Sulekha Rao Coticone, Will Bloch
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Patent number: 6806054Abstract: The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is known (“known GPCRs”), and most particularly to mutated (non-endogenous) versions of the known GPCRs for use, most preferably in screening assays for the direct identification of candidate compounds as inverse agonists, agonists and partial agonists.Type: GrantFiled: April 5, 2001Date of Patent: October 19, 2004Assignee: Arena Pharmaceuticals, Inc.Inventors: Karin Lehmann-Bruinsma, Chen W. Liaw, I-Lin Lin
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Patent number: 6774248Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 16, 2002Date of Patent: August 10, 2004Assignee: WyethInventors: Christopher P. Miller, Michael D. Collini, David H. Kaufman, Robert L. Morris, Robert R. Singhaus, Jr., John W. Ullrich, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Rayomand J. Unwalla
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Patent number: 6753423Abstract: The invention is directed to oligonucleotides and oligonucleosides functionalized to include lipophilic moieties and having improved biostability and altered biodistribution in mammals. In one embodiment, such lipophilic oligonucleotide conjugates are used in a method of targeting antisense oligonucleotides to hepatic tissues and thereby preferentially modulating gene expression in the liver and associated tissues of a mammal.Type: GrantFiled: April 10, 2000Date of Patent: June 22, 2004Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Muthiah Manoharan, Clarence Frank Bennett
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Patent number: 6747014Abstract: The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e.g., neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes.Type: GrantFiled: December 21, 2001Date of Patent: June 8, 2004Assignee: ISIS Pharmaceuticals, Inc.Inventors: Ching-Leou Teng, Phillip Dan Cook, Lloyd Tillman, Gregory E. Hardee, David J. Ecker, Muthiah Manoharan
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Patent number: 6721754Abstract: Disclosed herein are systems and methods for information organization whereby characteristics regarding entities are inferred from the characteristics of similar entities. This is referred to herein as a “fuzzy similarity join” and is exemplified using a chemical similarity join. The disclosed systems and methods are particularly useful for chemical compound analysis in the area of pharmaceutical development.Type: GrantFiled: April 28, 1999Date of Patent: April 13, 2004Assignee: Arena Pharmaceuticals, Inc.Inventors: John R. Hurst, Scott G. Hutton
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Patent number: 6653086Abstract: Disclosed herein are techniques for directly identifying candidate compounds as agonists, partial agonists and/or, most preferably, inverse agonists, to endogenous, constitutively activated orphan G protein-coupled receptors.Type: GrantFiled: July 30, 1999Date of Patent: November 25, 2003Assignee: Arena Pharmaceuticals, Inc.Inventors: Dominic P. Behan, Derek T. Chalmers, Chen W. Liaw, I Lin-Lin, Kevin P. Lowitz, Ruoping Chen