Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 514/294)
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Patent number: 7994214Abstract: A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability.Type: GrantFiled: August 30, 2004Date of Patent: August 9, 2011Assignee: Lifecycle Pharma A/SInventor: Per Holm
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Publication number: 20110190333Abstract: The invention provides a 3,11b-cis-dihydrotetrabenazine of the formula (Ib): or a pharmaceutically acceptable salt thereof for use in the prophylaxis or treatment of anxiety.Type: ApplicationFiled: June 12, 2009Publication date: August 4, 2011Applicant: Biovail Laboratories International (Barbados) S.R.L.Inventors: Ben Grayson, Roger Anthony Oakes, Andrew John Duffield
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Publication number: 20110172263Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: ApplicationFiled: September 17, 2009Publication date: July 14, 2011Applicant: MERCK FROSST CANADA LTDInventors: John Colucci, Michael Boyd, Mohamed Helmi Zaghdane, Michel Gallant
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Publication number: 20110160243Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.Type: ApplicationFiled: August 26, 2009Publication date: June 30, 2011Applicant: Arena Pharmaceuticals ,Inc.Inventors: Robert M. Jones, Daniel J. Buzard, Andrew M. Kawasaki, Sun Hee Kim, Lars Thoresen, Juerg Lehmann, Xiuwen Zhu
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Publication number: 20110160242Abstract: The present invention relates to a form 1 and form 2 polymorph of (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds.Type: ApplicationFiled: December 22, 2010Publication date: June 30, 2011Applicant: ArQule, Inc.Inventors: David P. Reed, Neil R. Barnes, John C. Kane, Christopher A. Lee, Jian-Xie Chen, Martin P. Redmon
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Publication number: 20110160237Abstract: The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 29, 2010Publication date: June 30, 2011Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Yanbin Liu, Magdi Moussa, Jianqiang Wang, Hui Wu
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Patent number: 7968564Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: April 15, 2010Date of Patent: June 28, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph P. Vacca, Linda S. Payne, Richard C. A. Isaacs
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Patent number: 7968716Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: GrantFiled: September 16, 2010Date of Patent: June 28, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 7956065Abstract: This application describes method of treating dementia and cognitive deficits associated with dementia that involve administration of dihydrotetrabenazine, and isomers and/or pharmaceutically acceptable salts thereof.Type: GrantFiled: September 8, 2009Date of Patent: June 7, 2011Assignee: Biovail Laboratories International (Barbados) S.R.L.Inventor: Philip Paul Nichols
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Patent number: 7947704Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.Type: GrantFiled: March 11, 2005Date of Patent: May 24, 2011Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Klaus Kunz, Stefan Lehr, Dieter Feucht, Peter Lösel, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20110118301Abstract: The invention relates to amine-substituted aza-adamantane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. Radiolabelled compounds useful for evaluating the binding affinity to ?7 nicotinic acetylcholine receptors also are described.Type: ApplicationFiled: January 24, 2011Publication date: May 19, 2011Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson, William H. Bunnelle, Diana L. Nersesian
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Publication number: 20110118300Abstract: The present invention provides, inter alia, dihydropyridone compounds and compositions, including analogs of a vesicular monoamine transporter type 2 (VMAT2) antagonist. The present invention also provides methods of using such compounds/analogs for modulating glucose levels, and/or preventing, treating, or ameliorating the effects of diabetes and hyper-glycemia.Type: ApplicationFiled: April 10, 2009Publication date: May 19, 2011Inventors: Paul Harris, Antonella Maffei, Yuli Xie, Donald Landry
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Publication number: 20110118241Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).Type: ApplicationFiled: May 5, 2009Publication date: May 19, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110112067Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110092535Abstract: The present invention resides in the use of a 5-HT3 receptor antagonist as medicament for the treatment of temporal lobe epilepsy associated with hippocampal sclerosis (TLE-HS) in a human patient. Tropisetron or Dolasetro are the preferred compounds.Type: ApplicationFiled: July 21, 2006Publication date: April 21, 2011Inventor: Nicholas Mark Barnes
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Patent number: 7915282Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: March 21, 2001Date of Patent: March 29, 2011Assignee: Bayer AktiengesellschaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Publication number: 20110053866Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.Type: ApplicationFiled: August 12, 2010Publication date: March 3, 2011Applicant: Biovail Laboratories International (Barbados) S.R.L.Inventors: Andrew John Duffield, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
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Patent number: 7897610Abstract: The invention relates to the use of benzo[c]quinolizinium derivatives for treating diseases that are linked to smooth muscle cell constriction, such as hypertension and asthma.Type: GrantFiled: June 5, 2003Date of Patent: March 1, 2011Assignees: Centre National de la Recherche Scientifique, Universite de PoitiersInventors: Frédéric Becq, Renaud Robert, Laurence Pignoux, Christian Rogier, Yvette Mettey, Jean Michel Vierfond, Michel Joffre, Cécile Marivingt-Mounir
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Publication number: 20110039832Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-a]isoquinoline and pyrrolo[2,1-a]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: February 6, 2009Publication date: February 17, 2011Applicant: N.V. OrganonInventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lar Anders van der Veen, Willem Frederik Johan Karstens
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Publication number: 20110039877Abstract: The invention provides a compound for use in treating multiple sclerosis wherein the compound is a 3, 11b-cis-dihydrotetrabenazine of the formula (Ia): or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 29, 2008Publication date: February 17, 2011Applicant: Biovail Laboratories International (Barbados) S.R.L.Inventor: Andrew John Duffield
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Publication number: 20110003824Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2-X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: ApplicationFiled: September 16, 2010Publication date: January 6, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORDTEDInventors: Jean-Damien Charrier, Guy Brenchley
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Publication number: 20110003844Abstract: The methods and compositions of the present invention find use in altering expression of PKC? in transgenic animals. The compositions of the invention include isolated transgenic animal cells, transgenic tissue, transgenic animals, and transgenic mice. The transgenic animals of the invention exhibit altered PKC? activity. The methods allow generation of transgenic animals with altered expression of PKC?. The invention allows modulation of cardiac contractility. In particular, the invention provides a method for altering the susceptibility of a transgenic animal to cardiomyopathy. A transgenic animal of the invention finds use in identifying anti-cardiomyopathic compounds.Type: ApplicationFiled: April 30, 2010Publication date: January 6, 2011Applicants: Children's Hospital Medical Center, University of CincinnatiInventors: Jeffery Daniel MOLKENTIN, Evangelia Galani Kranias
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Publication number: 20100323019Abstract: Microparticle-bioactive agent based treatments for local treatment of diseased tissues/organs are disclosed.Type: ApplicationFiled: August 19, 2010Publication date: December 23, 2010Applicant: Abbott Cardiovascular Systems Inc.Inventors: Florencia Lim, Mikael Trollsas, Michael Ngo, Thierry Glauser, Jinping Wan
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Publication number: 20100322997Abstract: A method of separating biologically ingestible microparticles is used to obtain biologically ingestible microparticles in a thin film fluid formed between two processing surfaces provided with a solution containing a first solvent in which an objective substance to be pulverized is dissolved and a solvent capable of serving as a second solvent in which the solubility of the microparticles is lower than in the first solvent, the two processing surfaces being arranged so as to be able to approach to and separate from each other, at least one of which rotates relative to the other.Type: ApplicationFiled: July 4, 2008Publication date: December 23, 2010Applicant: M. Technique Co., Ltd.Inventor: Masakazu Enomura
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Publication number: 20100297075Abstract: The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound in combination with a therapeutically effective amount of a second anti-proliferative agent.Type: ApplicationFiled: February 11, 2010Publication date: November 25, 2010Applicants: ArQule, Inc., Kyowa Hakko Kirin Co., Ltd.Inventors: Thomas C.K. Chan, Dennis S. France, Kenichi Ishii, Paolo Pucci
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Publication number: 20100298278Abstract: The invention relates to the substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 to R13, A, B, L and i are defined as in the description and the claims. The invention also relates to the use thereof in the treatment of Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: November 25, 2010Inventors: Christian Eickmeier, Klaus Fuchs, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Patent number: 7838532Abstract: Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.Type: GrantFiled: May 18, 2006Date of Patent: November 23, 2010Assignee: Mpex Pharmaceuticals, Inc.Inventors: Mark W. Surber, Keith A. Bostian, Michael N. Dudley, Olga Lomovskaya, David C. Griffith
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Publication number: 20100273824Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: January 18, 2008Publication date: October 28, 2010Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Publication number: 20100261710Abstract: The present invention provides hydroxamic acid compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the hydroxamic acid compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.Type: ApplicationFiled: August 21, 2008Publication date: October 14, 2010Applicant: ARQULE, INC.Inventors: Mark A. Ashwell, Manish Tandon, Nivedita D. Namdev, Jean-Marc Lapierre, Yanbin Liu, Hui Wu
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Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Publication number: 20100256698Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: ApplicationFiled: April 2, 2010Publication date: October 7, 2010Applicant: MERCK & CO., INC.Inventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
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Publication number: 20100240648Abstract: Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.Type: ApplicationFiled: June 2, 2010Publication date: September 23, 2010Inventors: Richard Apodaca, Ann J. Barbier, Nicholas I. Carruthers, Leslie A. Gomez, John M. Keith, Timothy W. Lovenberg, Ronald L. Wolin
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Publication number: 20100234415Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: ApplicationFiled: February 19, 2010Publication date: September 16, 2010Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey Methot
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Publication number: 20100234411Abstract: The present invention relates to novel pharmaceutical compositions based on telmisartan 1 and anticholinergics 2 processes for preparing them and their use for the treatment of respiratory diseases.Type: ApplicationFiled: July 14, 2008Publication date: September 16, 2010Applicant: BOEHRINGER INGELHEIM INTERMATIONAL GMBHInventors: Yunhai Cui, Wolfgang Wienen, Michael P. Pieper
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Patent number: 7790712Abstract: The application relates to compounds of formula Ia and analogues thereof wherein R1 to R13 and X are as defined herein. The invention also relates to the use of the compounds of formula Ia as inhibitors of Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2), and also to a method for preventing or treating a disease or disorder that can be treated or prevented by modulating the activity of MAPKAP-K2 in a subject and to pharmaceutical compositions and kits that include these MAPKAP-K2 inhibitors.Type: GrantFiled: March 17, 2006Date of Patent: September 7, 2010Assignee: Boehringer Ingelheim Pharmaceutical, Inc.Inventors: Derek Cogan, Donghong A. Gao, Daniel R. Goldberg, Craig Andrew Miller, Neil Moss, Matthew Russell Netherton, Philip Dean Ramsden, Zhaoming Xiong
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Publication number: 20100222340Abstract: The present invention relates to compounds of formula (I) 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 DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Markus Boehringer, Daniel Hunziker, Bernd Kuhn, Bernd Michael Loeffler, Fabienne Ricklin, Hans Peter Wessel
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Publication number: 20100222337Abstract: Conventional fungicidal compositions have had practical problems such that either a preventive effect or a curative effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired. The present invention provides a fungicidal composition containing a carboxylic acid amide derivative of the formula (I) or a salt thereof, as an active ingredient: wherein A is phenyl which may be substituted, benzodioxolanyl which may be substituted, or benzodioxanyl which may be substituted; B is 2- or 3-pyridyl which may be substituted; each of R1 and R2 is alkyl, or R1 and R2 may together form a 3- to 6-membered saturated carbon ring, provided that when B is 3-pyridyl which may be substituted, A is phenyl substituted by at least two substituents.Type: ApplicationFiled: December 13, 2006Publication date: September 2, 2010Applicant: Ishihara Sangyo Kaisha, Ltd.Inventors: Yuji Nakamura, Shigeru Mitani, Shintaro Tsukuda
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Publication number: 20100221351Abstract: In accordance with certain embodiments of the present disclosure, A method for intracellular delivery of cytotoxin in combination with cyoablation is provided. The method includes encapsulation of one or more cytotoxins in a thermally responsive nanocapsule by decreasing the temperature of the nanocapsule to increase the permeability of the nanocapsule whereby the one or more cytotoxins are sucked into or diffuse into the nanocapsule. The temperature of the nanocapsule is increased and the nanocapsule is delivered into a cell. Cryoablation is performed in proximity to the cell resulting in the release of the one or more cytotoxins from the nanocapsule into the cell.Type: ApplicationFiled: March 1, 2010Publication date: September 2, 2010Applicant: UNIVERSITY OF SOUTH CAROLINAInventor: Xiaoming He
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Publication number: 20100215774Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin and/or other active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: February 8, 2008Publication date: August 26, 2010Inventor: Todd Maibach
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Publication number: 20100216763Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. 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: ApplicationFiled: November 27, 2007Publication date: August 26, 2010Applicant: H. LUNDBECK A/SInventors: Alan J. Hutchison, Hongbin Li, Jianmin Mao, David J. Wustrow, Jun Yuan, He Zhao
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Publication number: 20100210622Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: ApplicationFiled: December 17, 2009Publication date: August 19, 2010Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Peter Czabotar, Danette A. Dudley, Wayne J. Fairbrother, John A, Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Lisa A. Hasvold, Andrew M. Petros, Andrew J. Souers, Zhi-Fu Tao, Le Wang, Xilu Wang, Kurt Deshayes
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Publication number: 20100204258Abstract: The present invention relates to methods and compositions for treating or ameliorating the effects of diabetes. In addition, the present invention relates to methods and compositions for treating or preventing hyperglycemia, as well as modulating monoamine levels, islet ?-cell insulin secretion, insulin and/or glucagon levels in a patient. In certain preferred embodiments, such methods include administering to a patient an effective amount of a vesicular monoamine transporter type 2 (VMAT2) antagonist, such as tetrabenazine (TBZ), dihydrotetrabenazine (DTBZ), tetrahydroberberine (THB), reserpine, emetine, Compound 6, or enantiomers, optical isomers, diastereomers, N-oxides, crystalline forms, hydrates, metabolites or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: March 12, 2008Publication date: August 12, 2010Applicant: The Trustees of Columbia University in the City of New YorkInventors: Paul Harris, Yuli Xie, Donald Landry, Shi-Xian Deng, Antonella Maffei
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Publication number: 20100203153Abstract: The present invention is a composition composed of a therapeutic agent encapsulated in a copolymer of an N-alkylacrylamide, a vinyl monomer, and a polyethylene glycol (PEG) conjugate and a method for using the same in the treatment or prevention of a disease or condition.Type: ApplicationFiled: April 19, 2010Publication date: August 12, 2010Inventors: Vinod D. Labhasetwar, Sanjeeb K. Sahoo, Maram K. Reddy
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Publication number: 20100189698Abstract: A method for the treatment and/or prophylaxis of a neurological and/or neuropsychiatric disorder associated with altered dopamine function comprising administering to the eye of a patient in need thereof an effective amount of an agent that modulates neurotransmitter production or function.Type: ApplicationFiled: June 30, 2008Publication date: July 29, 2010Applicant: CLARENCEW PTY LTDInventor: Gregory Lynn Willis
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Publication number: 20100189818Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.Type: ApplicationFiled: January 19, 2010Publication date: July 29, 2010Applicant: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical CenterInventor: GUOCHUAN EMIL TSAI
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Publication number: 20100184650Abstract: Patients are subject to a post-seizure treatment regime to separately inhibitor consecutive targets of an epileptogenic cascade comprising neurotransmitter receptor signaling, kinase/phosphatase activity, protein translation, and apoptosis or inflammation.Type: ApplicationFiled: January 17, 2010Publication date: July 22, 2010Inventors: Frances E. Jensen, Sanjay N. Rakhade
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Publication number: 20100183603Abstract: The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention.Type: ApplicationFiled: June 19, 2008Publication date: July 22, 2010Applicant: ARQULE, INC.Inventors: Neil Westlund, Jason Hill, Mark A. Ashwell, Nivedita Namdev, Jianqiang Wang, Syed Ali
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Publication number: 20100178291Abstract: The present invention relates to pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosucciniroide compounds of formulae (I)-(IV), and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compound of the present invention.Type: ApplicationFiled: June 19, 2008Publication date: July 15, 2010Applicant: ARQULE, INC.Inventors: Jianqiang Wang, Syed M. Ali, Eugene Kelleher, Yanbin Liu, Jason Hill, Mark A. Ashwell
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Patent number: 7754882Abstract: Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.Type: GrantFiled: June 16, 2006Date of Patent: July 13, 2010Assignee: Janssen Pharmaceutica NVInventors: Richard Apodaca, Ann J. Barbier, Nicholas I. Carruthers, Leslie A. Gomez, John M. Keith, Timothy W. Lovenberg, Ronald L. Wolin
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Patent number: 7750160Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein derivatives of urea compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.Type: GrantFiled: November 15, 2004Date of Patent: July 6, 2010Assignee: Ambit Biosciences CorporationInventors: Zdravko V. Milanov, Hitesh K. Patel, Robert M. Grotzfeld, Shamal A. Mehta, Andiliy G. Lai, David J. Lockhart