Patents Examined by Zinna N. Davis
  • Caspase inhibitors and uses thereof
    Patent number: 7612091
    Abstract: The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 is: C1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF3, Cl, F, OMe, OEt, OCF3, CN, or NMe2; C1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with —O— or —NR5—; R2 is C1-6 straight chained or branched alkyl; R3 is hydrogen, halo, OCF3, CN, or CF3; R4 is hydrogen, halo, OCF3, CN, or CF3; and each R5 is independently H, C1-6 straight chained or branched alkyl, aryl, —O—C1-6 straight chained or branched alkyl, or —O-aryl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated disease, particularly in the central nervous system.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: November 3, 2009
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Michael Mortimore, John R. Studley
  • Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof
    Patent number: 7612090
    Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.
    Type: Grant
    Filed: April 29, 2003
    Date of Patent: November 3, 2009
    Assignee: Albany Molecular Research, Inc.
    Inventors: James P. Beck, Matt A. Curry, Mark A. Smith
  • Method for producing bactericidal pyridine compound and bactericidal pyridine compound
    Patent number: 7612097
    Abstract: Provided are novel pyridine compounds represented by the following formula (7): wherein R1 and R4 may be the same or different and are each a linear or branched alkyl group having 1 to 4 carbon atoms; R2 and R5 are hydrogen atoms, or may be the same or different and are each a halogen atom, lower alkyl group or lower alkoxy group; R3 is a linear or branched alkyl group having 2 to 12 carbon atoms; R6 is a linear or branched alkyl group having 1 to 18 carbon atoms; and Z is a chlorine atom, bromine atom or iodine atom or an OSO2R7 group in which R7 is a lower alkyl group or a substituted or unsubstituted phenyl group. Also provided is their production process, which can easily provide them at low cost from readily-available pyridine compounds as starting raw materials.
    Type: Grant
    Filed: November 8, 2004
    Date of Patent: November 3, 2009
    Assignees: Tama Kagaku Kogyo Co., Ltd.
    Inventors: Hiroki Kourai, Yoshio Igarashi, Hirobumi Nobeshima, Satoshi Metoki
  • Phenoxyether derivatives as PPAR modulators
    Patent number: 7608639
    Abstract: The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR), such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
    Type: Grant
    Filed: October 8, 2004
    Date of Patent: October 27, 2009
    Assignee: Eli Lilly and Company
    Inventors: Leonard Larry Winneroski, Jr., Yanping Xu, Jeremy Schulenburg York
  • PDE4B inhibitors
    Patent number: 7605168
    Abstract: Compounds are described that are active on PDE4. Also described are crystal structures of PDE4B determined using X-ray crystallography, the use of PDE4B crystals and structural information for identifying molecular scaffolds, for developing ligands that bind to and modulate PDE4B, and for identifying improved ligands based on known ligands.
    Type: Grant
    Filed: September 2, 2005
    Date of Patent: October 20, 2009
    Assignee: Plexxikon, Inc.
    Inventors: Prabha N. Ibrahim, Ryan Bremer, Sam Gillette, Hanna Cho, Marika Nespi, Shumeye Mamo, Chao Zhang, Dean R. Artis, Byunghun Lee, Rebecca Zuckerman
  • Excitatory amino acid receptor antagonists
    Patent number: 7601738
    Abstract: The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and processes for preparing compounds of Formula (I) or Formula (I(a)).
    Type: Grant
    Filed: December 14, 2005
    Date of Patent: October 13, 2009
    Assignee: Eli Lilly and Company
    Inventors: Thomas John Bleisch, Jose Antonio Martinez-Perez, Paul Leslie Ornstein
  • Compounds having antiestrogenic and tissue selective estrogenic properties, and compounds with anti-androgenic properties for treatment of prostate cancer and androgen receptor dependent diseases
    Patent number: 7601739
    Abstract: Compounds for the treatment of estrogen-receptor related maladies are provided. Compounds with anti-androgenic properties also are provided. In particular, the invention provides compounds that are tetrahydroquinoline phenylamide derivatives and are useful for the treatment of breast and prostate cancer, and osteoporosis.
    Type: Grant
    Filed: February 8, 2006
    Date of Patent: October 13, 2009
    Assignee: Virgina Commonwealth University
    Inventors: Richmond Danso-Danquah, Donald J. Abraham, Hsiang-Ru Lin, Jim Christian Burnett
  • Preparation of 6-hydroxyequilenins
    Patent number: 7601857
    Abstract: This invention relates to a process for the preparation of 6-hydroxyequilenins, which are useful as estrogenic agents.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: October 13, 2009
    Assignee: Wyeth
    Inventors: Sreenivasulu Megati, Galina Vid, Arthur G. Mohan, Panolil Raveendranath, John Potoski
  • Amides that inhibit vanilloid receptor subtype 1 (VR1)
    Patent number: 7595332
    Abstract: The present invention relates to compounds of formula (I) that are novel VR1 antagonists useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.
    Type: Grant
    Filed: January 19, 2006
    Date of Patent: September 29, 2009
    Assignee: Abbott Laboratories
    Inventors: Chih-Hung Lee, John R. Koenig, Brian S. Brown
  • Tyrosine derivatives
    Patent number: 7595399
    Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: September 29, 2009
    Assignee: Genentech, Inc.
    Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
  • Heterocyclic aromatic compounds useful as growth hormone secretagogues
    Patent number: 7592354
    Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
    Type: Grant
    Filed: November 14, 2005
    Date of Patent: September 22, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
  • Tetrahydropyran heterocyclic cyclopentyl heteroaryl modulators of chemokine receptor activity
    Patent number: 7589085
    Abstract: The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
    Type: Grant
    Filed: August 6, 2004
    Date of Patent: September 15, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Lihu Yang, Stephen D. Goble
  • Heterocyclic aromatic compounds useful as growth hormone secretagogues
    Patent number: 7589102
    Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1, R1?, R2, R3, R4, Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.
    Type: Grant
    Filed: November 14, 2005
    Date of Patent: September 15, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guixue Yu, Jun Li, William R. Ewing, Richard B. Sulsky, James J. Li, Joseph Anthony Tino
  • Photoactive metal nitrosyls for blood pressure regulation and cancer therapy
    Patent number: 7582623
    Abstract: Disclosed are nitric oxide delivery agents and methods of their use, more specifically to photoactive compounds, which are able to perform targeted delivery of nitric oxide in vitro and in vivo and are useful for medicinal applications including, but not limited, to blood pressure regulation and cancer treatment.
    Type: Grant
    Filed: May 20, 2005
    Date of Patent: September 1, 2009
    Assignee: The Regents of the University of California
    Inventor: Pradip K. Mascharak
  • Pyridinone derivatives against malaria
    Patent number: 7579353
    Abstract: 4-pyridone derivatives of Formula (I) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
    Type: Grant
    Filed: March 2, 2006
    Date of Patent: August 25, 2009
    Assignee: Glaxo Group Limited
    Inventors: Jose Maria Fiandor Roman, Jose Maria Bueno Calderon, Araceli Mallo Rubio
  • Heterocyclic compounds as inhibitors of factor VIIa
    Patent number: 7576098
    Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: August 18, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter W. Glunz, Nicolas Wurtz, Xuhong Cheng
  • Preparation of pyridonecarboxylic acid antibacterials
    Patent number: 7576216
    Abstract: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.
    Type: Grant
    Filed: July 28, 2005
    Date of Patent: August 18, 2009
    Assignee: Abbott Laboratories
    Inventors: Anthony Haight, David M. Barnes, Geoff G. Z. Zhang
  • Substituted benzofused heterocycles
    Patent number: 7572783
    Abstract: The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for example, for the treatment and prevention of obesity, obesity-related disorders and eating disorders.
    Type: Grant
    Filed: August 12, 2005
    Date of Patent: August 11, 2009
    Assignee: Amgen Inc.
    Inventors: Xi Chen, Xiaoqi Chen, Richard Victor Connors, Kang Dai, Ying Fu, Juan C. Jaen, Yong-Jae Kim, Leping Li, Mike E. Lizarzaburu, Jeffrey T. Mihalic, Stephen J. Shuttleworth
  • Isoquinoline aminopyrazole derivatives
    Patent number: 7572809
    Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: December 12, 2006
    Date of Patent: August 11, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Guy Georges, Alfred Mertens, Xihan Wu
  • Heteroaryl-containing isoflavones as aromatase inhibitors
    Patent number: 7572919
    Abstract: Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO2, and S(CH2)n, wherein n=1-10; R1 and R2 may be the same or different and are selected from H, OH, OCH3, OCH2CH3, OCH2C6H5, NH2, NHCH3, N(CH3)2, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, C(CH3)3, NO2, F, Cl, Br, CF3, SH, SCH3, SCH2CH3, OCOCH3, OCOC(CH3)3, OCOCH2COOH, and CN; and R3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment.
    Type: Grant
    Filed: August 26, 2005
    Date of Patent: August 11, 2009
    Assignee: The Ohio State University Research Foundation
    Inventors: Robert W. Brueggemeier, Young-Woo Kim, John C. Hackett