Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
Type:
Grant
Filed:
October 16, 2002
Date of Patent:
July 8, 2008
Assignee:
Glaxo Group Limited
Inventors:
Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, Mark James Bamford, George Stuart Cockerill, Suzanne Joy Merrick, Ann Louise Walker
Abstract: The invention relates to the use of structural analogues of distamycin having the general formula (I), (II), (III), (IV) or (V) or their pharmaceutically acceptable salts, for the preparation of a medicament for the therapeutic treatment of ?-thalassaemia.
Type:
Grant
Filed:
July 1, 2002
Date of Patent:
July 8, 2008
Assignees:
Universita' Degli Studi Di Ferrara, Associazione Veneta per La Lotta Alla Talassemia, Associazione per La Lotta Alla Talassemia Di Ferrara
Inventors:
Pier Giovanni Baraldi, Nicoletta Bianchi, Giordana Feriotto, Roberto Gambari, Carlo Mischiati, Romeo Romagnoli
Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in (I) wherein C is for example wherein A and B are independently selected from R2a to R3b are independently selected from hydrogen and fluorine; R1a and R1b are independently selected from, for example, hydroxy, —NHC(?W)R4, wherein W is O or S; R4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
Type:
Grant
Filed:
September 9, 2002
Date of Patent:
July 8, 2008
Assignee:
AstraZeneca AB
Inventors:
Michael Barry Gravestock, Neil James Hales, Michael Lingard Swain, Sheila Irene Hauck, Stuart Dennett Mills
Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Type:
Grant
Filed:
August 28, 2003
Date of Patent:
July 1, 2008
Assignee:
Merck & Co., Inc.
Inventors:
John J. Acton, III, Peter T. Meinke, Harold B. Wood, Regina M. Black
Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.
Abstract: Pyrrole compounds of Formula (I): and pharmaceutically acceptable salts thereof (where A, B, R11, R12, R13, W, X, Y and Z are as defined herein), which are substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases
Type:
Grant
Filed:
March 31, 2004
Date of Patent:
July 1, 2008
Assignee:
Merck & Co. Inc.
Inventors:
Nicholas D. P. Cosford, Dehua Huang, Jeffrey R. Roppe, Nicholas D. Smith, Lida R. Tehrani
Abstract: The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Type:
Grant
Filed:
November 27, 2006
Date of Patent:
June 17, 2008
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
Abstract: An object of the present invention is to provide an organic semiconductor device comprising a semiconductor layer containing a compound with improved cohesive force, controllable molecular orientation, high packing property, high overall electrical conduction, high durability and high time-dependent stability. The present invention provides; a tertiary amine compound represented by formula (1); an organic semiconductor device comprising a substrate; a gate electrode; source and drain electrodes; and a semiconductor layer, wherein the semiconductor layer contains the tertiary amine comuound represented by formula (1).
Abstract: The present invention relates to derivatives of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide with covalently bonded acids, and to the salts, solvates and prodrugs thereof, to the derivatives as medicaments, to the use of these derivatives for the preparation of a medicament, to the use of these derivatives for the preparation of a pharmaceutical composition, to a process for the preparation of the pharmaceutical compositions, to pharmaceutical compositions obtainable by this process, and to a process for the treatment of diseases which comprises the administration of the pharmaceutical composition.
Abstract: Optically active maleimide derivatives of the formula: (where the various substituents are as defined in the description) are used as separating media for separating optical isomers and geometrical isomers such as by high performance liquid chromatography.
Abstract: The present invention discloses a novel process and novel intermediates for the Preparation of 4-[2-(di-n-propyl amino) ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole (I) and pharmaceutical composition comprising the same. Further the present invention also discloses a method of treatment for cardiovascular disorders and Parkinson's disease.
Abstract: There is provided a process for producing an aromatic hydroxycarboxylic acid which is capable of suppressing the formation of by-products and enhancing the selectivity of the intended product and is free from any purifying step. The process is characterized in that it is obtained by reacting an alkali metal salt of an aromatic hydroxy compound and carbon dioxide in a non-proton polar solvent in the presence of a solid basic catalyst.
Type:
Grant
Filed:
November 9, 2005
Date of Patent:
September 18, 2007
Assignees:
Chiba Institute of Technology, Nippon Oil Corporation
Abstract: The invention relates to a process for preparing substituted imidazole derivatives of formula (I) and acid addition salts thereof in which formula Y is —CH2— or —CO—, R1 is H, halo or hydroxy, R2 is H or halo and R3 is H or lower alkyl, starting from a compound of formula (II) wherein Y, R1, R2 and R3 are as defined above. The invention also relates to intermediates and their preparation.
Type:
Grant
Filed:
January 8, 2004
Date of Patent:
May 29, 2007
Assignee:
Oy Juvantia Pharma Ltd.
Inventors:
Päivi Juujärvi, Seppo Parhi, Jaana Karjalainen
Abstract: Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n+m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. Further provided are methods of using such compounds for the treatment of diabetes and related diseases, and to pharmaceutical compositions containing such compounds.
Type:
Grant
Filed:
July 27, 2004
Date of Patent:
February 7, 2006
Assignee:
Bristol Myers Squibb Company
Inventors:
Lawrence G. Hamann, Ashish Khanna, Mark S. Kirby, David R. Magnin, Ligaya M. Simpkins, James C. Sutton, Jeffrey Robl
Abstract: This invention provides novel arylindenopyridines of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing Adensine A2a receptors or reducing PDE activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.
Type:
Grant
Filed:
September 27, 2002
Date of Patent:
June 7, 2005
Assignee:
Ortho-Muniel Pharmaceutical, Inc.
Inventors:
Geoffrey R. Heintzelman, Kristin M. Averill, John H. Dodd, Keith T. Demarest, Yuting Tang, Paul F. Jackson
Abstract: Tetrahydroquinoline compounds of general formula (I) or pharmacologically acceptable salts thereof, which have a specific and strong binding affinity for AR, exhibit AR agonism or antagonism, have therapeutic effects on AR-mediated diseases, particularly by not acting excessively on the prostate as AR agonists, but by showing potent action on skeletal muscle tissue and bone tissue; and pharmaceutical compositions comprising the compounds or the salts as active ingredients:
Abstract: The invention relates to compounds of formula:
as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin.
The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
Type:
Grant
Filed:
July 24, 2002
Date of Patent:
May 4, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
Abstract: A process for the production of 3-hydroxypropionitrile is provided. This process includes (a) reacting acrylonitrile with water at a defined molar ratio in the presence of a weak base under specific temperature and pressure conditions until a conversion in the range of about 40% to about 80% has been achieved; (b) after cooling the mixture obtained in (a), separating off its aqueous phase; (c) distilling off the acrylonitrile from the organic phase remaining after (b); (d) subjecting the mixture obtained in (c) to pyrolysis at specific temperature and pressure conditions in the presence of a basic catalyst to obtain a mixture consisting mainly of 3-hydroxypropionitrile and acrylonitrile; and (e) isolating the desired 3-hydroxypropionitrile by fractional distillation from the mixture obtained in (d). Such a process in which the basic aqueous phase and the acrylonitrile that has been distilled off are recycled represents a preferred embodiment.
Type:
Grant
Filed:
January 17, 2001
Date of Patent:
October 8, 2002
Assignee:
Roche Vitamins, Inc.
Inventors:
Bruno Burdet, August Ruettimann, Johann Riegl
Abstract: The novel specific immunophilin ligands of the general formula I have an antiasthmatic and immunosuppressive action and are suitable for the preparation of drugs.
Type:
Grant
Filed:
April 25, 1997
Date of Patent:
July 10, 2001
Assignee:
ASTA Medica Aktiengesellschaft
Inventors:
Dietmar Reichert, Bernhard Kutscher, Holger Bang, Kay Brune, Gerhard Quinkert, Hans-Günter Schaible