Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
August 30, 2004
Date of Patent:
June 12, 2007
Assignee:
Array BioPharma, Inc.
Inventors:
Eli Wallace, Brian Hurley, Hong Woon Yang, Joseph Lyssikatos, Jim Blake, Alison Marlow
Abstract: The present invention relates to novel dipeptidyl peptidase IV (DPP-IV) inhibitors their analogs, isomers, pharmaceutical compositions, therapeutic uses and methods of making the same.
Type:
Grant
Filed:
February 2, 2005
Date of Patent:
June 12, 2007
Assignee:
Glenmark Pharmaceuticals Ltd.
Inventors:
Abraham Thomas, Balasubramanian Gopalan, V. S. Prasada Rao Lingam, Daisy Manish Shah
Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
August 6, 2004
Date of Patent:
June 5, 2007
Assignee:
Vertex Pharmaceuticals Inc.
Inventors:
Michael J. Arnost, Guy W. Bemis, Robert J. Davies, Cornelia J. Forster, Ronald Grey, Jr., Mark W. Ledeboer, Brian Ledford, Craig Marhefka, David Messersmith, Albert C. Pierce, Francesco G. Salituro, Jian Wang
Abstract: This invention relates to a compound of Formula I, a method for its preparation and its use in the preparation of a compound of Formula II wherein R1, R2, R3, X and n are as defined in the disclosure. This invention also discloses preparation of compounds of Formula III wherein R1, R2, R6, R7, R8 and n are as defined in the disclosure. Also disclosed are certain intermediates of Formula 4 for the preparation of compounds of Formula I wherein X is N and R2, R3 and n are as defined in the disclosure.
Type:
Grant
Filed:
July 6, 2005
Date of Patent:
June 5, 2007
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
John Herbert Freudenberger, George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
Abstract: The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
Type:
Grant
Filed:
June 24, 2005
Date of Patent:
June 5, 2007
Assignees:
Aventis Pharmaceuticals Inc., Axys Pharmaceuticals, Inc.
Inventors:
Jiayo Li, David J. Aldous, Sukanthini Thurairatnam
Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
Type:
Grant
Filed:
March 17, 2006
Date of Patent:
June 5, 2007
Assignee:
SmithKline Beecham Corporation
Inventors:
Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
Type:
Grant
Filed:
April 4, 2005
Date of Patent:
May 29, 2007
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.
Type:
Grant
Filed:
November 30, 2005
Date of Patent:
May 29, 2007
Assignee:
Bristol-Myers Squibb Company
Inventors:
Mark D. Wittman, Neelakantan Balasubramanian, Upender Velaparthi, Kurt Zimmermann, Mark G. Saulnier, Peiying Liu, Xiaopeng Sang, David B. Frennesson, Karen M. Stoffan, James G. Tarrant, Anne Marinier, Stephan Roy
Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a CNS disorder relating to or affected by the 5-HT6 receptor
Abstract: The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the General Formula (I) [where R1 and R2 independently represent a C1-6 alkyl group and the like that may have a hydrogen atom or a substituent; R3 represents a C1-6 alkyl group and the like that may have a substituent; R4 and R5 independent represents a hydrogen atom or a C1-6 alkyl group and the like that may have a substituent; R6 represents a hydrogen atom and the like; W represents —SO2—and the like; and X represents a sulphur atom and the like.] or a salt thereof, or a hydrate thereof.
Abstract: The compound of the formula (I): wherein W is a group of the following formula (VIII) binding to any possible position on the Q: Q is, together with W, a group of the formula: —C(W)?C(R3A)—N(R3)—, etc.; R3A is H or optionally substituted lower alkyl; R4, R5, R6, and R7 are independently H or optionally substituted lower alkyl; R1 is optionally substituted lower alkyl, etc.; R2 is H, etc.; R3 is H, etc.; Ar is phenyl, etc., or a pharmaceutically acceptable salt thereof, where these compounds exhibiting ?3-adrenoceptor-stimulating activity and being useful as a medicament for treatment of obesity, etc.
Abstract: The present invention is related to pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea.
Type:
Grant
Filed:
March 20, 2001
Date of Patent:
May 1, 2007
Assignee:
Applied Research Systems Ars Holding N.V.
Inventors:
Serge Halazy, Anna Quattropani, Alexander Scheer, Matthias Schwarz, Russell J Thomas, Anthony Baxter
Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g.
Type:
Grant
Filed:
August 6, 2002
Date of Patent:
April 24, 2007
Assignee:
Eli Lilly and Company
Inventors:
Daniel Jon Sall, Jolie Anne Bastian, Rushad Eruch Karanjawala, Cynthia Darshini Jesudason, Theo Schotten, Britta Evers, Gerd Reuhter, Don Richard Finley, Freddie Craig Stevens, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, John Xiaoqiang He, John Arnold Werner, William George Trankle, Andrew Michael Ratz
Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.
Type:
Grant
Filed:
October 12, 2005
Date of Patent:
April 17, 2007
Assignee:
Glenmark Pharmaceuticals S.A.
Inventors:
Abraham Thomas, Gopalan Balasubramanian, V. S. Prasada Rao Lingam, Daisy Manish Shah
Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3 and R4 are as defined herein.
Type:
Grant
Filed:
January 12, 2004
Date of Patent:
April 17, 2007
Assignee:
Memory Pharmaceuticals Corp.
Inventors:
Richard A. Schumacher, William F. Brubaker, Michael De Vivo, Hans-Jürgen Ernst Hess, Allen Hopper, Ashok Tehim, Ruiping Liu, Axel Unterbeck
Abstract: The present invention is directed to a compound of formula (I), or a stereoisomer or a mixture of stereoisomer thereof in any ratio, or its physiologically tolerable salt, which is useful as an inhibitor of matrix metalloproteinase. The present invention is also directed to a pharmaceutical preparation comprising a pharmaceutically effective amount of at least one compound of formula (I); processes for their preparation; the use of a compound of formula (I) having activity as an matrix metalloproteinase inhibitor; and for the prophylaxis and therapy of disease states that involve an increase in the activity of matrix metalloproteinase.
Type:
Grant
Filed:
September 27, 2004
Date of Patent:
April 17, 2007
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Manfred Schudok, Hans Matter, Armin Hofmeister
Abstract: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
November 24, 2004
Date of Patent:
April 10, 2007
Assignees:
Bristol-Myers Squibb Company, Icagen, Inc.
Inventors:
John Lloyd, Yoon T. Jeon, Heather Finlay, Lin Yan, Michael F. Gross, Serge Beaudoin
Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein —N-HET is, for example, (Ic) or (If) wherein R1 is, for example, halogen or a (1–4C)alkyl group which is substituted by one substituent selected from, for example, hydroxy, (1–4C)alkoxy, amino, cyano or azido; Q is selected from, for example, Q1 wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
Type:
Grant
Filed:
February 25, 2003
Date of Patent:
April 3, 2007
Assignee:
AstraZeneca AB
Inventors:
Michael Barry Gravestock, Neil James Hales, Folkert Reck, Fei Zhou, Paul Robert Fleming, Daniel Robert Carcanague
Abstract: The present application describes monocyclic and bicyclic lactams and derivatives thereof of Formulae Ia–e: wherein one of one of T1 and T2 is carbonyl, thiocarbonyl, or sulfonyl or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
Type:
Grant
Filed:
June 16, 2003
Date of Patent:
April 3, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Weirong Chen, Jeffrey J. Hale, Zhen Li, Christopher L. Lynch, Sander G. Mills, William E. Neway, III