Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
Type:
Grant
Filed:
December 16, 2005
Date of Patent:
December 22, 2009
Assignee:
Boehringer-Ingelheim Pharmaceuticals, Inc.
Inventors:
Daniel Kuzmich, Darren DiSalvo, John Robinson Regan, David S. Thomson, Rajashekhar Betageri, Jennifer A. Kowalski
Abstract: Indole compounds of the formula: wherein L1, L2, R1, R2, Ra, Rb, Rc, Rd, and Re are defined herein. Also disclosed are methods of using of the indole compounds in inhibiting tubulin polymerization and treating cancer and other angiogenesis-related disorders.
Abstract: The invention relates to compounds having formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to a method of preparing said compounds and to the application thereof in therapeutics.
Type:
Grant
Filed:
August 8, 2007
Date of Patent:
December 15, 2009
Assignee:
Sanofi-aventis
Inventors:
Francis Barth, Christian Congy, Patrick Gueule, Murielle Rinaldi-Carmona, Didier Van Broeck
Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.
Type:
Grant
Filed:
April 6, 2005
Date of Patent:
December 15, 2009
Assignee:
Merck Patent Gesellschaft mit beschrankter
Inventors:
Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gèrard Ferrand, Yves Bonhomme
Abstract: The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.
Abstract: Method of preparation of maleimides by thermal cyclization of maleamic acids in the presence of a catalyst consists in that reaction of a substituted maleic anhydride with a primary amine is performed in an organic solvent in the presence of betaine at a temperature of 100 to 180° C., at a ratio of the primary amine to the substituted maleic anhydride of 0.6:1.6. Maleimides, obtained in this way, are further purified by extraction, and finally, they are crystallized. As a catalyst, there may be also used betaine in a mixture with inorganic and organic acids, or betaine may be deposited on a solid carrier, or possibly, betaine may be deposited on a carrier in combination with inorganic acids.
Abstract: The invention provides novel indane compounds which are useful in the treatment of affective disorders, pain disorders, attention deficit hyperactivity disorder (ADHD), cognitive disorders, substance abuse, smoking cessation and stress urinary incontinence.
Abstract: The present invention provides a composition containing a benzamidine derivative that does not decompose even when placed under humidification conditions and a method for stabilizing a benzamidine derivative. According to the present invention, decomposition reaction of a benzamidine derivative can be suppressed by adding to a benzamidine derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, at least one type of electrolyte selected from the group consisting of halide salts of alkaline metal or alkaline earth metal and alkaline metal salts or alkaline earth metal salts of perchloric acid.
Abstract: The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Grant
Filed:
September 27, 2006
Date of Patent:
October 13, 2009
Assignee:
Wyeth
Inventors:
Casey Cameron McComas, Puwen Zhang, Eugene John Trybulski, An Thien Vu, Eugene Anthony Terefenko
Abstract: The disclosure concerns substituted pyrroles of formula (I): wherein A, L, Ar, R1, R2, R5, and Ra are as defined in the disclosure, compositions containing the same, methods for making the same and uses thereof, in particular as anti-cancer agents.
Type:
Grant
Filed:
August 1, 2007
Date of Patent:
September 22, 2009
Assignee:
Aventis Pharma S.A.
Inventors:
Baptiste Ronan, Michel Tabart, Catherine Souaille, Fabrice Viviani, Eric Bacque, Jean-Philippe Letallec, Pascal Desmazeau
Abstract: Selective PDE4 inhibition is achieved by novel compounds, e.g., 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds of the present invention are of formula I: wherein R1, R2, and R3 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Type:
Grant
Filed:
October 20, 2005
Date of Patent:
September 8, 2009
Assignee:
Memory Pharmaceuticals Corporation
Inventors:
Allen Hopper, Robert Francis Dunn, Erik Mikal Kuester, Richard Dennis Conticello, Ruiping Liu, Ashok Tehim
Abstract: Disclosed herein are a cosmetic composition comprising at least one diazirine active-agent compound comprising a diazirine covalently bonded to a cosmetic active agent, said at least one diazirine-active agent compound and the uses of the composition or of the compound, as well as cosmetic treatment processes using the composition or the compound.
Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
Type:
Grant
Filed:
September 17, 2007
Date of Patent:
September 1, 2009
Assignee:
Galderma Research & Development
Inventors:
Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
Type:
Grant
Filed:
November 17, 2006
Date of Patent:
August 11, 2009
Assignee:
Synta Pharmaceuticals Corp.
Inventors:
Lijun Sun, Jun Jiang, Christopher Borella, Shoujun Chen, Keizo Koya
Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions of 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, methods of using prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.
Abstract: Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R5 and Q have the meanings indicated in Claim 1, are suitable as ligands of 5 HT receptors; as well as intermediate compounds of the formula (IA).
Type:
Grant
Filed:
March 8, 2004
Date of Patent:
July 28, 2009
Assignee:
Merck Patent GmbH
Inventors:
Kai Schiemann, Oliver Schadt, Christoph Van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
Abstract: Kinetic stabilization of the native state of transthyretin is an effective mechanism for preventing protein misfolding. Because transthyretin misfolding plays an important role in transthyretin amyloid diseases, inhibiting such misfolding can be used as an effective treatment or prophylaxis for such diseases. Treatment methods are disclosed.
Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
Abstract: The present invention relates to modulators of metalloproteinase activity.
Type:
Grant
Filed:
July 11, 2006
Date of Patent:
June 30, 2009
Assignee:
Wyeth
Inventors:
Phaik-Eng Sum, Jerauld Stanley Skotnicki, Steve Yik-Kai Tam, Tarek Suhayl Mansour, David Brian How, Joshua James Sabatini, Jason Shaoyun Xiang, Eric Feyfant
Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.