Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 514/294)
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Patent number: 8357697Abstract: Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds are disclosed that are inhibitors of the vesicular monoamine transporter 2 (VMAT2). The compounds of this invention have the structure: wherein R1 is as defined herein, including stereoisomers and pharmaceutically acceptable salts and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use in a subject in need thereof.Type: GrantFiled: September 20, 2011Date of Patent: January 22, 2013Assignee: Neurocrine Biosciences, Inc.Inventor: Kyle W. Gano
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Patent number: 8357696Abstract: 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: January 28, 2010Date of Patent: January 22, 2013Assignee: Mpex Pharmaceuticals, Inc.Inventors: Mark W. Surber, Keith A. Bostian, Michael N. Dudley, Olga Rodny, David C. Griffith
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Publication number: 20130011481Abstract: The present invention provides pyrroloquinolinyl-pyrrole-2,5-dione formulations and methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of the formulations containing pyrroloquinolinyl-pyrrole-2,5-dione compounds.Type: ApplicationFiled: July 6, 2012Publication date: January 10, 2013Applicant: ArQule, Inc.Inventors: Hiroshi Yamakose, Takafumi Kato
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Patent number: 8337817Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.Type: GrantFiled: December 25, 2007Date of Patent: December 25, 2012Assignee: Shin Nippon Biomedical Laboratories, Ltd.Inventors: Ryoichi Nagata, Shunji Haruta
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Publication number: 20120321559Abstract: 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: August 24, 2012Publication date: December 20, 2012Inventors: 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: 8334300Abstract: 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 24, 2011Date of Patent: December 18, 2012Assignee: Bayer AktiengesellshaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Publication number: 20120316193Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.Type: ApplicationFiled: May 10, 2012Publication date: December 13, 2012Inventors: Megan Foley, Bradley Tait, Matthew Cullen
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Publication number: 20120316111Abstract: The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of one or more of the following compounds prazosin, quinacrine, emetine, apomorphine, and debrisoquine, whereby endogenous BMP-2 up-regulation is stimulated in said subject. The endogenous BMP-2 up-regulation may enhance bone formation and/or cartilage formation.Type: ApplicationFiled: June 8, 2011Publication date: December 13, 2012Applicant: SOUTHWEST RESEARCH INSTITUTEInventor: Jorge G. ROSSINI
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Publication number: 20120316157Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more heterocyclic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.Type: ApplicationFiled: March 2, 2011Publication date: December 13, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
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Publication number: 20120309782Abstract: Disclosed herein are compounds represented by the structural formula: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: August 8, 2012Publication date: December 6, 2012Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Richard L. Beard, John E. Donello, Michael E. Garst
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Patent number: 8314119Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.Type: GrantFiled: November 5, 2007Date of Patent: November 20, 2012Assignee: AbbVie Inc.Inventors: Michael R. Schrimpf, Diana L. Nersesian, Kevin B. Sippy, Jianguo Ji, Tao Li, Marc Scanio, Lei Shi, Chih-Hung Lee, William H. Bunnelle, Geoff G. Z. Zhang, Paul J. Brackemeyer, Shuang Chen, Rodger F. Henry
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Publication number: 20120289539Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 21, 2012Publication date: November 15, 2012Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Kenneth L. DUCHIN, Wendy Jade Limayo HERNANDEZ, Roger S. FLUGEL
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Patent number: 8309729Abstract: Disclosed herein are compounds represented by the structural formula: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 1, 2012Date of Patent: November 13, 2012Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita Bhat, Ken Chow, Richard L. Beard, John E. Donello, Michael Garst
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Publication number: 20120282242Abstract: Methods for treating ocular and periocular disorders by administration to a human patient of a therapeutically effective amount of a compound that modulates muscle action.Type: ApplicationFiled: July 20, 2012Publication date: November 8, 2012Inventor: Marcio Marc ABREU
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Patent number: 8304425Abstract: 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: GrantFiled: June 19, 2008Date of Patent: November 6, 2012Assignee: ArQule, Inc.Inventors: Jianqiang Wang, Syed M. Ali, Eugene Kelleher, Yanbin Liu, Jason Hill, Mark A. Ashwell
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Patent number: 8299116Abstract: This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.Type: GrantFiled: August 10, 2011Date of Patent: October 30, 2012Assignee: Wyeth LLCInventors: Joseph T Rubino, Victoria Siskavich, Maureen M Harrison, Pooja Gandhi
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Publication number: 20120252836Abstract: 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: June 18, 2012Publication date: October 4, 2012Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Phillippe Meyer, Peteris Alberts, Mainkar Prathama
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Publication number: 20120245195Abstract: The invention relates to a crystalline monohydrate of (4s)-4-(5-phenyl-1,3,4-thiadiazol-2-yloxy)-1-azatricyclo[3.3.1.13,7]decane dihydrogen citrate, compositions comprising such compound, and a process for preparing such compound.Type: ApplicationFiled: September 21, 2011Publication date: September 27, 2012Applicant: ABBOTT LABORATORIESInventors: Shuang Chen, James J. Napier, Geoff G.Z. Zhang, Paul J. Brackemeyer
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Patent number: 8273761Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa to Xe are each a carbon atom or a nitrogen atom, m is 0 to 2, and ring A to ring C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.Type: GrantFiled: December 7, 2007Date of Patent: September 25, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
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Patent number: 8273762Abstract: 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 2, 2010Date of Patent: September 25, 2012Assignee: 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: 8258300Abstract: The azo dyes relate to thiophene azo dyes of the general formula: where R1 is Cyano or C1-C5 alkoxy carbonyl; R2 is hydrogen, halogene, C1-C2 alkyl, phenyl, or substituted phenyl; and R3 is C1-C5 alkoxy carbonyl, C1-C4 alkanoyl, benzoyl, phenyl, alkyl substituted phenyl, or alkoxy phenyl; or R2 and R3 are fused cycloalkane with C3-C5.Type: GrantFiled: September 29, 2008Date of Patent: September 4, 2012Assignee: King Abdulaziz UniversityInventor: Abdullah Mohamed Asiri
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Patent number: 8252809Abstract: The present invention provides compositions for treating middle-of-the-night insomnia without residual sedative effects upon awakening by administering low doses (about 5 mg or less) of zolpidem or a salt thereof.Type: GrantFiled: June 8, 2010Date of Patent: August 28, 2012Assignee: Transcept Pharmaceuticals, Inc.Inventor: Nikhilesh N. Singh
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Publication number: 20120214838Abstract: Disclosed herein are compounds represented by the structural formula: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 1, 2012Publication date: August 23, 2012Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Richard L. Beard, John E. Donello, Michael E. Garst
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Patent number: 8247429Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa, Xb, Xc and Xd are each a carbon atom or a nitrogen atom, provided that any one or two of Xa, Xb, Xc and Xd is/are nitrogen atom(s), m is 0 to 2, and rings A to C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.Type: GrantFiled: December 27, 2007Date of Patent: August 21, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
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Publication number: 20120208773Abstract: 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: August 16, 2012Applicant: Valeant International (Barbados) SRLInventors: Andrew John Duffield, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
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Patent number: 8242131Abstract: The present invention provides compositions and methods for treating middle-of-the-night insomnia without residual sedative effects upon awakening by administering low doses (about 5 mg or less) of zolpidem or a salt thereof.Type: GrantFiled: May 23, 2006Date of Patent: August 14, 2012Assignee: Transcept Pharmaceuticals, Inc.Inventors: Nikhilesh Singh, Sathasivan Indiran Pather
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Publication number: 20120196890Abstract: The invention relates to compounds that are 4-substituted azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: March 23, 2012Publication date: August 2, 2012Inventor: William H. Bunnelle
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Publication number: 20120190706Abstract: The invention relates to compounds that are acetamide and carboxamide derivatives of azaadamantane, compositions comprising such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: March 23, 2012Publication date: July 26, 2012Inventors: Marc J.C. Scanio, Lei Shi, William H. Bunnelle, Michael R. Schrimpf
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Patent number: 8222272Abstract: The present invention relates to a pharmaceutical formulation and process for preparing the same comprising an oral dosage formulation, such as a capsule formulation, of a macrolide compound, such as tacrolimus, wherein the capsule formulation contains both a solid dispersion of the macrolide along with a non-dispersed form of the macrolide. The pharmaceutical formulation according to the invention is bioequivalent to the FDA approved product according to a bioavailability study conducted in humans.Type: GrantFiled: April 11, 2008Date of Patent: July 17, 2012Assignee: Roxane Laboratories, Inc.Inventors: Greg A. Brubaker, Thomas D. Mahon
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Publication number: 20120178750Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: March 19, 2012Publication date: July 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Subharekha Raghavan, Steven L. Colletti, Fa-Xiang Ding, Hong Shen, James R. Tata, Ashley Rouse Lins, Abigail Lee Smenton, Weichun Chen, Darby Rye Schmidt, George Scott Tria
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Publication number: 20120172346Abstract: The invention concerns the use of a nicotinic acetylcholine receptor alpha 7 activators for the treatment, prevention or delay of progression of dyskinesia associated with dopamine agonist therapy in Parkinson's Disease.Type: ApplicationFiled: September 22, 2010Publication date: July 5, 2012Inventors: Thérèse Di Paolo, Dominik Feuerbach, Baltazar Gomez-Mancilla, Donald Johns
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Publication number: 20120165278Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 23, 2011Publication date: June 28, 2012Applicant: ArQule, Inc.Inventors: Mark A. Ashwell, Darin Kizer, Takahiro Murai, Daisuke Nakai, Takanori Yasukochi
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Patent number: 8188279Abstract: Disclosed herein are compounds represented by the structural formula: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: June 1, 2011Date of Patent: May 29, 2012Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita Bhat, Ken Chow, Richard L. Beard, John E. Donello, Michael Garst
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Publication number: 20120108570Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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Publication number: 20120095022Abstract: The present invention relates to compounds having the following general formula (I): wherein: A represents a SO2 or CX group, X representing O or S; R1, R2, R?, R4 represent in particular H, R represents in particular an alkyl group or an aryl group, as well as to the pharmaceutically acceptable salts thereof, the compound of formula (I) taking the form of a pure stereoisomer or an enantiomer and/or diastereoisomer mixture, including racemic mixtures.Type: ApplicationFiled: March 11, 2010Publication date: April 19, 2012Applicants: UNIVERSITE D'ORLEANS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S.)Inventors: Sylvain Cesar Leonce Routier, Gerald Guillaumet, Rajaa Boulahjar, Laurent Meijer, Matteo Chiurato
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Publication number: 20120077839Abstract: Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds are disclosed that are inhibitors of the vesicular monoamine transporter 2 (VMAT2). The compounds of this invention have the structure: wherein R1 is as defined herein, including stereoisomers and pharmaceutically acceptable salts and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use in a subject in need thereof.Type: ApplicationFiled: September 20, 2011Publication date: March 29, 2012Applicant: NEUROCRINE BIOSCIENCES, INC.Inventor: Kyle W. Gano
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Publication number: 20120045509Abstract: The present invention refers to pharmaceutical composition comprising a DPP-IV inhibitor.Type: ApplicationFiled: October 27, 2011Publication date: February 23, 2012Inventors: Bernd Michael Loeffler, Alexander MacDonald, Cynthia Rocha, Eric Worth
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Patent number: 8105608Abstract: A method and pharmaceutical composition are provided for enhancing the endogenous immune response-mediated elimination of a population of pathogenic cells in a host animal wherein the pathogenic cells preferentially express, uniquely express, or overexpress a binding site for a particular ligand. The invention comprises administering the ligand conjugated to an immunogen to a host animal harboring the population of pathogenic cells. Antibodies, preexisting or administered to the host animal to establish a passive immunity, directed against the immunogen bind to the ligand-immunogen conjugate resulting in elimination of the pathogenic cells by the host's immune response.Type: GrantFiled: November 16, 2005Date of Patent: January 31, 2012Assignee: Purdue Research FoundationInventors: Philip Stewart Low, Yingjuan Lu
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Publication number: 20120015972Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R1 represents halogen, a hydroxy group or the like; R2 represents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and R3 represents hydrogen, fluorine or the like.Type: ApplicationFiled: March 30, 2010Publication date: January 19, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Masato Iizuka, Yasushi Takigawa
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Publication number: 20120003330Abstract: The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: May 31, 2011Publication date: January 5, 2012Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Chengzhi Zhang, Manoucherhr Shahbaz
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Publication number: 20120004191Abstract: 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: July 1, 2011Publication date: January 5, 2012Applicant: ArQule, Inc.Inventors: Giovanni Abbadessa, Dennis S. France, Chang-Rung Chen, Thomas C.K. Chan
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Publication number: 20120004233Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 26, 2010Publication date: January 5, 2012Applicant: AMIRA PHARMACEUTICALS, INCInventors: Brian Andrew Stearns, Ryan Clark
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Publication number: 20110294800Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.Type: ApplicationFiled: August 7, 2009Publication date: December 1, 2011Applicant: The Trustees Of Columbia University in the City of New YorkInventors: Yuli Xie, Shixian Deng, Donald W. Landry, Paul Harris, Antonella Maffei
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Publication number: 20110268654Abstract: The present application provides compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reaction for rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.Type: ApplicationFiled: November 2, 2009Publication date: November 3, 2011Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Scott A. Hilderbrand, Neal K. Devaraj, Ralph Weissleder
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Publication number: 20110257220Abstract: The invention provides the use of 3,11b-cis-dihydrotetrabenazine or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the prophylaxis or treatment of schizophrenia and other psychoses.Type: ApplicationFiled: August 4, 2006Publication date: October 20, 2011Applicant: CAMBRIDGE LABORATORIES (IRELAND) LIMITEDInventors: Andrew John Duffield, Jean Elisabeth Yarrow
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Patent number: 8039627Abstract: Substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds are disclosed that are inhibitors of the vesicular monoamine transporter 2 (VMAT2). The compounds of this invention have the structure: wherein R1 is as defined herein, including stereoisomers and pharmaceutically acceptable salts and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use in a subject in need thereof.Type: GrantFiled: November 8, 2007Date of Patent: October 18, 2011Assignee: Neurocrine Biosciences, Inc.Inventor: Kyle W. Gano
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Patent number: 8026276Abstract: Parenteral formulations of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl) -2-methylpropionic acid (CCI-779) are provided. One parenteral formulation contains CCI-779, an alcoholic co-solvent, and an antioxidant. Another parenteral formulation contains CCI-779, an alcoholic solvent, an antioxidant, a diluent solvent, and a surfactant. Processes for preparing parenteral CCI-779 formulations using a co-solvent concentrate are also provided.Type: GrantFiled: July 25, 2003Date of Patent: September 27, 2011Assignee: Wyeth LLCInventors: Joseph T. Rubino, Victoria Siskavich, Maureen M. Harrison, Pooja Gandhi
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Publication number: 20110212989Abstract: Therapeutic method of treatment, compositions and foodstuffs are described which contain isoflavone compounds described by general formula (I), in which Z is H, R1 is H or RACO wherein Ra is C1-10alkyl or an amino acid, R2 is H, OH or ORB where RB is an amino acid, or CORA where RA is as previously defined, W is H, A is H or OH, and B is selected from (a), (b), (c) or W is H, and A and B taken together form a six-membered ring selected from (d), or W, A and B taken with the groups with which they are associated comprise (f) and B is (g) where R3 is H, CORA where RA is as previously defined, CO2RC where RC is C1-10alkyl, or CORB where RB is as previously defined, R4 is H, CORD where RD is H, OH, C1-10alkyl or an amino acid, CO2RC where RC is as previously defined, CORE where RE is H, C1-10alkyl or an amino acid, COOH, CORC where RC is as previously defined, or CONHRE where RE is as previously defined, R5 is H, CO2RC where RC is as previously defined, or CORCORE where RC and RE are as previously defined, anType: ApplicationFiled: May 6, 2011Publication date: September 1, 2011Applicant: NOVOGEN RESEARCH PTY LTDInventors: Graham Edmund KELLY, George Eustace Joannou
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Publication number: 20110201641Abstract: The compound (+) {7R-[[(4-fluorophenyl)sulfonyl] (methyl)ammo]-6,7,8,9-tetrahydropyrido[1,2-a]mdol-10-yl}acetic acid and pharmaceutically acceptable salts thereof are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-meidated diseases such as asthma.Type: ApplicationFiled: September 17, 2009Publication date: August 18, 2011Applicant: MERCK FROSST CANADA LTDInventor: Zhaoyin Wang
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Publication number: 20110195961Abstract: The invention relates to antibacterial compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is notably H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 orType: ApplicationFiled: October 6, 2009Publication date: August 11, 2011Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Daniel Ritz, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin