Abstract: The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.
Abstract: The invention relates to a CB modulator compound of Formula (I) or a pharmaceutically acceptable form thereof and a method for use in treating, ameliorating or preventing a CB receptor mediated syndrome, disorder or disease.
Type:
Application
Filed:
December 7, 2007
Publication date:
April 10, 2008
Inventors:
Fina Liotta, Huajun Lu, Mingde Xia, Michael Wachter
Abstract: Sulfonylguanidine compounds corresponding to the tautomeric formulas I and Ia, a method for producing them, pharmaceutical compositions containing them, and methods of using them to prepare medicaments and for treating various medical conditions. The sulfonylguanidine compounds have an affinity for the gabapentin binding site and can be used to treat conditions such as pain, epilepsy, migraine and others.
Type:
Application
Filed:
May 1, 2007
Publication date:
April 10, 2008
Applicant:
GRUENENTHAL GmbH
Inventors:
MATTHIAS GERLACH, Heinz Uragg, Michael Haurand, Claudia Puetz, Corinna Sundermann, Boris Chizh
Abstract: Heteroaryl substituted quinolin-4-ylamine analogues of Formula I are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
Type:
Application
Filed:
January 13, 2006
Publication date:
April 10, 2008
Applicant:
Neurogen Corporation
Inventors:
Timothy Caldwell, Bertrand Chenard, Kevin Hodgetts
Abstract: The present invention relates to a combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis. The patient is treated with a VEGF inhibitor compound; and one or more chemotherapeutic agents.
Type:
Application
Filed:
September 23, 2004
Publication date:
April 10, 2008
Inventors:
Guido Bold, Josef Bernhard Brueggen, Jerry Min-Jian Huang, Frederick Ray Kinder, Heidi Lane, Elisabeth Jeanne Latour, Paul W. Manley, Jeanette Marjorie Wood
Abstract: The present invention provides novel crystalline forms of aripiprazole and aripiprazole hydrochloride, processes for their preparation and pharmaceutical compositions containing them.
Abstract: Novel 1,5 diphenylpyrazole derivatives of the formula (I), in which R1-R6 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB2 receptors.
Type:
Application
Filed:
September 24, 2007
Publication date:
April 10, 2008
Inventors:
Michel Dietz, Sabine Gruener, Paul Hebeisen, Sylvie Meyer Reigner, Matthias Nettekoven, Bernd Puellmann, Stephan Roever, Christoph Ullmer
Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.
Type:
Application
Filed:
September 27, 2007
Publication date:
April 10, 2008
Inventors:
Mirjana Andjelkovic, Agnes Benardeau, Evelyne Chaput, Paul Hebeisen, Matthias Nettekoven, Ulrike Sander, Constantinos Panousis, Stephan Roever
Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
Abstract: A glycine derivative which is, e.g., the following compound (Chemical formula (1)). It is highly effective in the treatment and prevention of inflammatory bowel diseases. Compared to conventional compounds, the compound is excellent in absorbability in oral administration and in vivo stability. The compound can be orally administered and can retain an excellent therapeutic or preventive effect over a longer period.
Abstract: Methods of utilizing a combined administration or a unit dosage of a combination of an HMG-CoA inhibitor and omega-3 fatty acids for the reduction of apolipoprotein-B levels. The methods are especially useful in the treatment of patients with hypertriglyceridemia or hypercholesterolemia or mixed dyslipidemia, coronary heart disease (CHD), vascular disease, atherosclerotic disease and related conditions, and for the prevention or reduction of cardiovascular, cardiac, and vascular events.
Type:
Application
Filed:
September 7, 2007
Publication date:
April 10, 2008
Applicant:
Reliant Pharmaceuticals, Inc.
Inventors:
Roelof M.L. Rongen, Robert A. Shalwitz, Douglas Kling, Ralph T. Doyle
Abstract: The present invention is directed to novel polymorphic forms of the compound 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol hydrate (gaboxadol monohydrate). The invention is further concerned with pharmaceutical compositions containing the polymorphic forms as an active ingredient, methods for treatment of disorders susceptible to amelioration by GABAA receptor agonism with the polymorphic forms, and processes for the preparation of the polymorphic forms.
Type:
Application
Filed:
January 26, 2006
Publication date:
April 10, 2008
Applicant:
H. LUNDBECK A/S
Inventors:
Daniel Kumke, Jerry Murry, Bryon Simmons, Feng Xu
Abstract: The present invention provides methods for the prevention of, delay progression to overt to, or the treatment of diastolic dysfunction or diastolic heart failure which method comprises administering to a warm-blooded animal a therapeutically effective amount of a renin inhibitor, or a pharmaceutically acceptable salt thereof, alone or in combination with (i) an ACE inhibitor or a pharmaceutically acceptable salt thereof; or (II) an angiotensin II receptor blocker or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
October 6, 2005
Publication date:
April 10, 2008
Inventors:
David Louis Feldman, Friedrich Cameron Luft, Dominik Nicolas Mueller, Randy Lee Webb
Abstract: The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.
Abstract: A method is provided for using ?2? subunit calcium channel modulators or other compounds that interact with the ?2? calcium channel subunit in combination with one or more compounds with smooth muscle modulatory effects to treat and/or alleviate the symptoms associated with painful and non-painful lower urinary tract disorders in normal and spinal cord injured patients. According to the present invention, ?2? subunit calcium channel modulators include GABA analogs (e.g. gabapentin and pregabalin), fused bicyclic or tricyclic amino acid analogs of gabapentin, and amino acid compounds. Compounds with smooth muscle modulatory effects include antimuscarinics, ?3 adrenergic agonists, spasmolytics, neurokinin receptor antagonists, bradykinin receptor antagonists, and nitric oxide donors.
Type:
Application
Filed:
December 7, 2007
Publication date:
April 10, 2008
Applicant:
Dynogen Pharmaceuticals, Inc.
Inventors:
Matthew Fraser, Karl Thor, Edward Burgard, Lee Brettman, Steven Landau, Daniel Ricca
Abstract: The present invention relates to the besylate salt of 7-(2-(4-(3-(trifluoromethyl)phenyl)-1,2,3,6-tetrahydropyrid-1-yl)ethyl)isoquinoline, to its preparation and to its use in therapeutics.
Abstract: The present invention provides an assay for determining the biochemical fitness of a biochemical species in a mutant replicating biological entity relative to its predecessor. The present invention further provides a continuous fluorogenic assay for measuring the anti-HIV protease activity of protease inhibitor. The present invention also provides a method of administering a therapeutic compound that reduces the chances of the emergence of drug resistance in therapy.
Type:
Application
Filed:
October 11, 2007
Publication date:
April 10, 2008
Applicants:
Government of the United States of America, represented by Secretary, Departmemt of Health and, Board of Trustees of the University of Illinois
Inventors:
John ERICKSON, Sergei GULNIK, Hiroaki MITSUYA, Arun GHOSH
Abstract: Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
Type:
Application
Filed:
October 11, 2007
Publication date:
April 10, 2008
Inventors:
Paul Bradley, Kevin Dack, Patrick Johnson, Sarah Skerratt
Abstract: Methods and compositions for the treatment of conditions including stress-associated, chronic pain, and neurodegenerative conditions in a mammal using a composition comprising NB-DNJ or a compound structurally similar thereto.
Type:
Application
Filed:
September 27, 2005
Publication date:
April 10, 2008
Inventors:
John E. Donello, Fabien J. Schweighoffer
Abstract: The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.
Abstract: Multiple stereoisomers of the heterocyclic-substituted tricyclics of the formula: or a pharmaceutically acceptable salt, solvate, or ester of said compound wherein R and the stereochemistry are illustrated in the structural formulas herein are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
Type:
Application
Filed:
October 2, 2007
Publication date:
April 10, 2008
Inventors:
Samuel Chackalamannil, Yuguang Wang, Tiruvettipuram Thiruvengadam, Ilia Zavialov, Tao Li
Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.
Type:
Application
Filed:
December 1, 2003
Publication date:
April 10, 2008
Applicant:
BAYER CROPSCINCE AG
Inventors:
Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Losel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jorg Nico Greul
Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a CNS disorder related to or affected by the 5-HT6 receptor.
Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
Type:
Application
Filed:
October 2, 2007
Publication date:
April 10, 2008
Inventors:
John Stelmach, Emma Parmee, James Tata, Keith Rosauer, Ronald Kim, Amy Bittner, Jiang Chang, Christopher Sinz
Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
Type:
Application
Filed:
October 15, 2007
Publication date:
April 10, 2008
Inventors:
Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan DeAngelis
Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein L, R1, R2, m and n have the meaning given in claim 1 and which can be used in the form of pharmaceutical compositions.
Type:
Application
Filed:
September 24, 2007
Publication date:
April 10, 2008
Inventors:
Wolfgang Haap, Paul Hebeisen, Eric Kitas, Philipp Kohler, Holger Kuehne, Armin Ruf
Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.
Type:
Application
Filed:
July 25, 2007
Publication date:
April 10, 2008
Inventors:
Jae Hyun KIM, Su Kyung LEE, Won Kyu CHOI, Jong Lae LIM, Soon Kil AHN, Hee Jong SHIN, Chung HONG
Abstract: The present invention relates to a novel crystal of (S)-(+)-2-(2-chlorophenyl)-2-hydroxy-ethyl carbamate, pharmaceutical compositions comprising this crystal and, and methods of making and using this crystal.
Abstract: The invention provides a method for treating cancers that are dependent on cyclin D1 for proliferation, survival, metastasis and differentiation, involving administering a composition containing an effective amount of arsenic trioxide to an affected patient. The arsenic trioxide can be administered orally, for example, as a solution, suspension, syrup, emulsion, tablet, or capsule. The composition can also contain one or more pharmaceutically acceptable carriers and/or excipients.
Abstract: The invention provides methods for treating beta-Amyloid protein-induced disease, pharmaceutical compositions and compounds useful for the same, and the use of these compounds for the manufacture of a medicament for treating the same. More particularly, the invention relates to the use of natural product compounds isolated from turmeric, gingko biloba, and ginger, and synthetic chemical analogues thereof, for the treatment of a beta-Amyloid protein-induced disease.
Abstract: Clear aqueous compositions comprising water, a hydrophobic organic compound, and from about 2 to about 50 wt. % of a solubilizer are disclosed. The solubilizer is an alkali metal or alkaline earth metal salt of a monoester of a saturated C6-C20 alcohol and a saturated dicarboxylic acid. The monoester salts are remarkably effective for solubilizing a wide variety of hydrophobic organic compounds in water to provide aqueous compositions that have excellent stability and outstanding clarity. The compositions are valuable for the cosmetic, agrochemical, coatings, pharmaceutical, and flavor & fragrance industries.
Abstract: A composition comprising at least one bisdithiocarbamate fungicide and at least one zinc additive is provided. Processes related thereto are also provided.
Type:
Application
Filed:
October 4, 2007
Publication date:
April 10, 2008
Applicant:
Dow AgroSciences LLC
Inventors:
Norman R. Pearson, Daniel L. Dermody, Melissa A. Mushrush, Christopher J. Tucker
Abstract: A composition comprising at least one bisdithiocarbamate fungicide and at least one zinc additive is provided. Processes related thereto are also provided.
Type:
Application
Filed:
October 4, 2007
Publication date:
April 10, 2008
Applicant:
Dow AgroSciences LLC
Inventors:
Norman R. Pearson, Daniel L. Dermody, Melissa A. Mushrush, Christopher J. Tucker
Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.
Type:
Application
Filed:
June 16, 2005
Publication date:
April 10, 2008
Inventors:
Pier Giovanni BARALDI, Pier Andrea BOREA, Pierangelo GEPPETTI
Abstract: N-(2-hydroxyalkanoyl)-N,N?-dialkylureas of general formula (1) are described A-X-(A)m??(1) where A: m=0 or m=1; when m=0, X=R??, where R?? is an aliphatic, cycloaliphatic, arylaliphatic radical, C1-C18; when m=1, X=—(CH2)n—, where n is an integer from 1 and 20, preferably from 2 to 6; R is chosen among H, and alkyl radicals C1-C8, possibly substituted with halogen atoms; R? is an aliphatic, cycloaliphatic, arylaliphatic radical, C1-C18; R? is chosen among H, aliphatic, cycloaliphatic, arylaliphatic radical, C1-C18. The preparation of said compounds is described, as well as the preparation of corresponding polymers.
Type:
Application
Filed:
November 19, 2007
Publication date:
April 10, 2008
Inventors:
Guido Galliani, Marco Orlandi, Bruno Rindone, Alberto Terraneo
Abstract: The present invention is directed to arylamino-arylpropanolamine 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:
Application
Filed:
October 2, 2007
Publication date:
April 10, 2008
Applicant:
Wyeth
Inventors:
An Thien Vu, Stephen Todd Cohn, Eugene Anthony Terefenko, William Jay Moore, Puwen Zhang, Paige Erin Mahaney, Eugene John Trybulski
Abstract: The present invention is in the field of prevention and treatment of atherosclerosis and atherosclerosis-related clinical conditions. In particular, the present invention relates to the use of sphingolipids, more preferably phytosphingosine, sphingosine, sphinganine, ceramide, cerebroside lyso-sphingomyelin and/or sphingomyelin for prevention and treatment of inflammatory processes associated with atherosclerosis, psoriasis, colitis or auto-immune diseases in a subject.
Type:
Application
Filed:
July 18, 2005
Publication date:
April 10, 2008
Inventors:
Willem Ferdinand Nieuwenhuizen, Aloysius Maria Havekes, Josephus Jan Emeis
Abstract: Method for fabricating and inspecting small holes in a material are disclosed. The method includes directing light onto the material and through the holes formed in the material, and then collecting the light passing through the holes in the material onto a detector. The methods further include analyzing the light for properties of the holes, and modifying the process based these detected properties.
Abstract: A method of dispersing solid which is soluble to not more than 1 part by weight in 100 parts by weight of water at 20° C. and 1020 hPa, which method comprises incorporating at least one self-emulsifying organopolysiloxane (A) and then incorporating solid (B) into an aqueous composition.
Abstract: Airbag fabric is coated with a primer followed by a coating composition to form airbags which retain gas for exceptionally long periods after rapid deployment with low coatweights, resulting in improved airbags, especially side curtain airbags of the one piece woven type. The primer is formed from an ethylenically unsaturated monomer/functionalized polyorganosiloxane mixture in a water/emulsifying agent mixture; and the coating is a reinforcing mineral filler-free composition comprising a mixture of (1) at least one polyorganosiloxane with alkenyl groups bound to the silicon; (2) at least one polyorganosiloxane with hydrogen atoms bound to the silicon; (3) a cross-linking catalyst; (4) an adhesion promoter comprising (4.1) at least one alkoxylated organosilane, (4.2) at least one epoxy-functional organosilicon compound, and (4.
Abstract: A method for manufacturing a polishing pad made from a polyurethane resin foam having very uniform, fine cells therein and a polishing pad obtained by that method provides a polishing pad having better polishing characteristics (especially, in planarization) while providing improved dressability while maintaining the planarization characteristics and polishing speed of a conventional polishing pad. The polyurethane resin foam is a cured product obtained by reacting an isocyanate-terminated prepolymer with an aromatic polyamine chain extender having a melting point of 70° C. or lower, for example.
Abstract: The invention relates to a support part (1) on the basis of foam material, for use in the medical sector, such as, for example, in operating rooms, particularly a head support, whereby the support part (1) has a hard foam material core (2), which is covered with a soft foam material layer (4), as well as furthermore to the production of such a support part. In order to further improve a support part of the type in question with regard to functionality and use, it is provided that furthermore, the soft foam material layer (4) is surrounded by an outer sheath (6). In terms of the method, it is provided that at least one support part outer sheath (6) is laminated onto a soft foam material layer (4) and preformed in a deep-drawing mold, and this laminate is afterwards drawn over the hard foam material core (2).
Abstract: It is to provide a flexible polyurethane foam having favorable vibration characteristics and further having excellent sound absorption characteristics, a process for its production and a seat for an automobile. A process for producing a flexible polyurethane foam, which comprises reacting a polyol compound with a polyisocyanate compound in the presence of a foam stabilizers a blowing agent and a urethane-forming catalyst, wherein as the polyol compound, a polyol compound containing a polyoxyalkylene polyol (A) having an oxyalkylene group obtained by ring opening addition polymerization of an alkylene oxide by using a composite metal cyanide complex catalyst and having an unsaturation value less than 0.04 meq/g, a polyoxyalkylene polyol (B) obtained by random ring opening addition polymerization of ethylene oxide and an alkylene oxide having at least 3 carbon atoms to an initiator, and a polymer-dispersed polyol (C), is used.
Abstract: A method of forming a photo-tailored shape memory article is described. The method includes forming an article that includes a photochemically crosslinkable polymer composition, illuminating at least two different regions of the article with different light exposures to form first and second crosslinked polymer compositions with different shape memory critical temperatures. Also described are photochemically crosslinkable polymer compositions that include a di(meth)acrylate macromer, a multifunctional thiol, and a photoinitiator.
Abstract: Radiation curable compositions suitable for use a optical fiber ribbon matrix materials are provided which have at least two non-silicone urethane(meth)acrylate oligomers, one or more multifunctional diluents and one or more photoinitiators, wherein each of the non-silicone urethane(meth)acrylate oligomers has a number average molecular weight of about 200 or more, but less than about 6000, and the polydispersity index (PDI) of the urethane(meth)acrylate oligomers is from 2:1 to 30:1. The matrix material may be coated and cured on a plurality of optical fibers so as to form an optical fiber ribbon assembly.
Type:
Application
Filed:
October 10, 2006
Publication date:
April 10, 2008
Inventors:
Jeanette L. Ward, Edward J. Murphy, Kelly A. Hawkinson, James J. Schouten