Abstract: The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a subject in need of increased mucociliary clearance and mucosal hydration.
Type:
Grant
Filed:
September 7, 2007
Date of Patent:
November 15, 2011
Assignee:
Parion Sciences, Inc.
Inventors:
Michael Ross Johnson, Richard C. Boucher, Andrew J. Hirsh
Abstract: The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium channel blocker as defined herein and an osmolyte to a subject to a subject in need of increased mucociliary clearance and mucosal hydration.
Type:
Grant
Filed:
September 7, 2007
Date of Patent:
July 19, 2011
Assignee:
Parion Sciences, Inc.
Inventors:
Michael Ross Johnson, Richard C. Boucher, Andrew J. Hirsh
Abstract: The present invention provides for compounds of Formula I: wherein R2, R3, R4, R5, R6, R7, X, and L have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of central nervous disorders and conditions including attention deficit hyperactivity disorder, neuropathic pain, urinary incontinence, anxiety, depression, and schizophrenia and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
Abstract: The present invention relates to oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. The present invention also relates to crystalline forms of oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
Type:
Grant
Filed:
April 7, 2005
Date of Patent:
August 12, 2008
Assignee:
Warner-Lambert Company
Inventors:
Stephen Douglas Barrett, Cathlin Marie Biwersi, Michael Huai Gu Chen, Michael David Kaufman, Haile Tecle, Joseph Scott Warmus
Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
Type:
Grant
Filed:
January 8, 2007
Date of Patent:
August 5, 2008
Assignee:
Pfizer, Inc.
Inventors:
Mark A. Dombrowski, Allen J. Duplantier
Abstract: The present invention relates to novel to P2X7 inhibitors of formula I and to processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them, and their use in therapy. The active compounds of the present invention are potent inhibitors of P2X7 and as such are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
Type:
Grant
Filed:
October 18, 2005
Date of Patent:
June 26, 2007
Assignee:
Pfizer Inc.
Inventors:
Allen J. Duplantier, Chakrapani Subramanyam
Abstract: The present invention relates to the methods for preparing compounds of the formula I: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R4, R10, and R11 have any of the values defined in the specification. The compounds of the present invention are useful in the treatment of diseases, including inflammatory diseases such as rheumatoid arthritis.
Abstract: A process for preparing (S)-(?)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[-4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide (I) and then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-IId.
Type:
Grant
Filed:
February 28, 2005
Date of Patent:
June 19, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Sonja Suzanne MacKey, Michael E. Matison, Haifeng Wu, Michael Paul Goble, Moses W. McMillan, Vikram Gurudath Kalthod
Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.
Type:
Grant
Filed:
April 29, 2005
Date of Patent:
June 19, 2007
Assignee:
Warner-Lambert Company
Inventors:
Robert Lee Bosch, Richard Joseph McCabe, Thomas Norman Nanninga, Robert Joseph Stahl
Abstract: This invention relates to processes for the preparation of 7-carboxy substituted steroid compounds of Formula I, wherein R1 is selected from H or COR4; R4 is C1–C6 alkyl or C1–C6 alkoxy; R3 is C1–C6 alkyl; Z1 is —CH2— or ?wherein O—COR4 is in the ? configuration; Z2 is —CH—; or Z1 and Z2 may be taken together to form a carbon-carbon double bond; Q is These intermediates are useful in the preparation of 7-carboxy substituted steroid compounds, and particularly, the invention is directed to novel and advantageous methods for the preparation of 9,11-?-epoxy-17-?-hydroxy-3-oxopregn-4-ene-?-7-21-dicarboxylic acid, ?-lactone, methyl ester (eplerenone; epoxymexrenone).
Abstract: Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney.
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
Type:
Grant
Filed:
November 20, 2000
Date of Patent:
October 10, 2006
Assignee:
Warner-Lambert Company
Inventors:
Michael S. South, John J. Parlow, Darin E. Jones, Brenda Case, Tom Dice, Richard Lindmark, Michael J. Hayes, Melvin L. Rueppel, Rick Fenton, Gary W. Franklin, Horng-Chih Huang, Wei Huang, Carrie Kusturin, Scott A. Long, William L. Neumann, David B. Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Matthew W. Mahoney
Abstract: NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.
Type:
Grant
Filed:
December 9, 2002
Date of Patent:
December 13, 2005
Assignee:
Warner-Lambert Company
Inventors:
Ernest S. Hamanaka, Angel Guzman-Perez, Christian J. Mularski, Roger B. Ruggeri, Ronald T. Wester
Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
Type:
Grant
Filed:
June 4, 2002
Date of Patent:
November 23, 2004
Assignee:
Warner-Lambert Company
Inventors:
Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
Abstract: The present invention relates to a method for making 2-N-phenylamino)benzoic acids by coupling a benzoic acid and an aniline using an alkaline metal hexamethyldisilazide as a base.
Abstract: The present invention provide compounds of Formula I
The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.
Type:
Grant
Filed:
July 23, 2001
Date of Patent:
March 4, 2003
Assignee:
Warner-Lambert Company
Inventors:
Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
Abstract: Acetyldinaline in combination with gemcitabine, a pharmaceutically acceptable salt thereof, capecitabine, or cisplatin is synergistic for treating cancer.
Type:
Grant
Filed:
January 19, 2001
Date of Patent:
October 22, 2002
Assignee:
Warner-Lambert Company
Inventors:
William Richard Grove, Wayne Daniel Klohs, Ronald Lynn Merriman
Abstract: This invention provides compounds of Formula I having the structure
wherein,
R1, R2, and X are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.