3-benzazepines (including Hydrogenated) Patents (Class 514/217.01)
  • Patent number: 10238653
    Abstract: This invention relates to methods and formulations for treating metabolic disorders and depression. In some embodiments, the methods comprise administering a dopamine receptor agonist and an anti-depressant.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: March 26, 2019
    Assignee: VeroScience LLC
    Inventor: Anthony H. Cincotta
  • Patent number: 9981912
    Abstract: The present invention relates to a new type of eutectic crystal of lorcaserin hydrochloride and benzoic acid, when compared with the prior art, the eutectic crystal has the improved properties of good stability, low solubility, and being suitable for the application of controlled-release preparation; the present invention also relates to a method for preparing the eutectic crystal, a pharmaceutical composition thereof and the use thereof in the manufacture of drugs for treating and/or preventing diseases associated with 5HT2C.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: May 29, 2018
    Assignee: HANGZHOU PUSHAI PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Chenyang Hu, Xiaoxia Sheng, Xiaohong Sheng, Qiang Jia
  • Patent number: 9714225
    Abstract: The present invention relates to stable crystalline Form I of lorcaserin hydrochloride of Formula (IA) and processes for its preparation. The invention also relates to processes for the preparation of lorcaserin and pharmaceutically acceptable salts, solvates and hydrates thereof.
    Type: Grant
    Filed: November 13, 2014
    Date of Patent: July 25, 2017
    Assignee: Cadila Healthcare Limited
    Inventors: Shriprakash Dhar Dwivedi, Jayprakash Ajitsingh Parihar, Alpeshkumar Pravinchandra Shah, Samir Rameshbhai Gajjar, Brij Khera
  • Patent number: 9540361
    Abstract: The present invention relates to novel N-substituted azetidine derivatives < of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N—R5; R1 is H, (C1-8)alkyl, (C3-8)cycloalkyl, (C3-6)heterocycloalkyl, (C2-6)alkenyl, (C2-6)alkynyl, (C1-4)alkylcarbonyl, (C1-4)alkoxy(C2-4)alkyl, (C3-6)cycloalkyl(C1-3)-alkyl, (C3-6)heterocycloalkyl(C1-3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (C1-2)alkyl; R5 is H, (C1-3)alkyl, optionally substituted with one or more fluorine; R17, R18 and R19 are independently of each other H, fluorine, nitrile or (C1-3)-alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, > to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium can
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: January 10, 2017
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Fredericus Antonius Dijcks, Scott James Lusher, Herman Thijs Stock, Arthur Oubrie, Gerrit Herman Veeneman
  • Patent number: 9447074
    Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: September 20, 2016
    Assignee: Glaxo Group Limited
    Inventors: Francis Louis Atkinson, Michael David Barker, John Liddle, David Matthew Wilson
  • Patent number: 9248133
    Abstract: Salts of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine with optically active acids, and pharmaceutical compositions comprising them that are useful for, inter alia, weight management.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: February 2, 2016
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, William Lucas Betts, III, Jaimie Karyn Rueter, Yun Shan, Anna Shifrina, Scott Stirn
  • Patent number: 9186353
    Abstract: This invention discloses a method of treatment of osteoarthritis pain by administration of a histamine H3 receptor antagonist, described herein, a salt thereof, or a composition comprising such compound or salt.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: November 17, 2015
    Assignee: AbbVie Inc.
    Inventors: Marlon D. Cowart, Gin C. Hsieh, Jorge D. Brioni, James P. Sullivan
  • Patent number: 9169213
    Abstract: Provided are methods of determining if an individual is a responder to treatment with (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof. Also provided are methods for selecting an individual for treatment with (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof from a plurality of individuals in need of weight management. Also provided are methods for weight management in an individual in need thereof. Also provided are compounds, compositions, and kits for use in a method of weight management in an individual.
    Type: Grant
    Filed: April 1, 2014
    Date of Patent: October 27, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Matilde Sanchez, William R. Shanahan
  • Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • Patent number: 8999970
    Abstract: The present disclosure relates to methods for weight management in an individual in need thereof by determining the level of renal sufficiency of the individual and prescribing or administering a therapeutically effective amount of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof to the individual, provided that the individual has a level of renal sufficiency selected from the group consisting of: no renal impairment, mild renal impairment, and moderate renal impairment.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: April 7, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Christen M. Anderson, William R. Shanahan
  • Patent number: 8993560
    Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: March 31, 2015
    Assignee: Glaxo Group Limited
    Inventors: Francis Louis Atkinson, Michael David Barker, John Liddle, David Matthew Wilson
  • Publication number: 20150087634
    Abstract: The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Application
    Filed: April 23, 2014
    Publication date: March 26, 2015
    Inventors: Dominic P. Behan, Brian M. Smith, Christina Bjenning
  • Publication number: 20150080380
    Abstract: This invention relates to novel therapeutic uses for compounds which are inverse agonists of the H3 receptor. In particular this invention relates to therapeutic use of these compounds in the treatment of Multiple Sclerosis.
    Type: Application
    Filed: January 15, 2013
    Publication date: March 19, 2015
    Inventors: Hongtao Lu, Rong Wang
  • Publication number: 20150080296
    Abstract: Nutritive proteins are provided. In some embodiments the nutritive proteins comprise a protein digestibility corrected amino acid score (PDCAAS) that exceeds a benchmark protein. Also provided are nucleic acids encoding the proteins, recombinant microorganisms that make the proteins, methods of making the proteins using recombinant microorganisms, compositions that comprise the proteins, and methods of using the proteins, among other things.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 19, 2015
    Inventors: Nathaniel W. Silver, Geoffrey von Maltzahn, Michael J. Hamill, David Arthur Berry
  • Patent number: 8980881
    Abstract: The present invention is directed to crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, compositions containing the same and uses thereof.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: March 17, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Rajesh K. Agarwal, William L. Betts, III, James A. Henshilwood, Yuan-Hon Kiang, Noah Post
  • Publication number: 20150064223
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: July 11, 2012
    Publication date: March 5, 2015
    Applicant: Elcelyx Therapeutics, Inc.
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • Patent number: 8946207
    Abstract: The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 3, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Beverly L. Wolgast, Charles A. Gilson, III, Shelley Aytes, Scott A. Estrada, Dipanjan Sengupta, Brian Smith, Ulrich Weigl, Heidedore Jlsabeth Rey-Papina
  • Publication number: 20150025063
    Abstract: A method of treating a subject for Parkinson's disease comprises administering said subject a phenylisopropylamine in an amount effective to treat said Parkinson's disease. In some embodiments the method is used to treat at least a motor symptom of Parkinson's disease; in some embodiments the method is used to treat at least a non-motor symptom of Parkinson's disease.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 22, 2015
    Inventors: Marc G. Caron, Tatyana D. Sotnikova, Raul R. Gainetdinov
  • Patent number: 8906904
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: December 9, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jehrod Burnett Brenneman, John Ginn, Michael D. Lowe, Christopher Ronald Sarko, Edward S. Tasber, Zhonghua Zhang
  • Publication number: 20140315893
    Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
    Type: Application
    Filed: November 22, 2012
    Publication date: October 23, 2014
    Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
  • Patent number: 8865702
    Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • Publication number: 20140296212
    Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
    Type: Application
    Filed: February 10, 2014
    Publication date: October 2, 2014
    Applicant: CEPHALON, INC.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Allison L. Zulli, Brigitte Lesur, Babu G. Sundar, Christophe Yue
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang
  • Publication number: 20140213579
    Abstract: Provided are methods of determining if an individual is a responder to treatment with (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof. Also provided are methods for selecting an individual for treatment with (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof from a plurality of individuals in need of weight management. Also provided are methods for weight management in an individual in need thereof. Also provided are compounds, compositions, and kits for use in a method of weight management in an individual.
    Type: Application
    Filed: April 1, 2014
    Publication date: July 31, 2014
    Inventors: Matilde Sanchez, William R. Shanahan
  • Publication number: 20140187538
    Abstract: The present invention relates to amorphous lorcaserin hydrochloride; amorphous solid dispersion comprising lorcaserin hydrochloride and one or more pharmaceutically acceptable carries; processes for preparation thereof; pharmaceutical compositions comprising amorphous lorcaserin hydrochloride and one or more pharmaceutically acceptable carries.
    Type: Application
    Filed: December 26, 2013
    Publication date: July 3, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Rajesham Boge, Arjun Kumar Tummala, Vishweshwar Peddy, Srinivasulu Rangineni, Vilas Hareshwar Dahanukar, Bandichhor Rakeshwar, Areveli Srinivas, Macharla Prabhakar, Varanasi Ganesh
  • Publication number: 20140171418
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 19, 2014
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans
  • Patent number: 8741890
    Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
  • Patent number: 8741892
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: June 3, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • Publication number: 20140148383
    Abstract: Obesity is inhibited by administering to a person in need thereof an effective amount of entacapone ((2E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylprop-2-enamide), or a pharmaceutically-acceptable salt thereof, particularly in conjunction with a second, different anti-obesity medicament. Pharmaceutical compositions comprise entacapone copackaged or coformulated with a second, different anti-obesity medicament.
    Type: Application
    Filed: January 4, 2014
    Publication date: May 29, 2014
    Applicant: NATIONAL INSTITUTE OF BIOLOGICAL SCIENCES, BEIJING
    Inventors: Niu Huang, Gang Zhi, Jijie Chai, Shiming Peng, Nannan Hou
  • Publication number: 20140148442
    Abstract: Salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and dosage forms comprising them that are useful for, inter alia, weight management.
    Type: Application
    Filed: August 31, 2011
    Publication date: May 29, 2014
    Inventors: Anthony C. Blackburn, Scott Stirn, Yun Shan, Anna Shifrina
  • Publication number: 20140121201
    Abstract: Screening assays and methods of using same for screening to identify modulator agents or compounds that affect Th17 cell specification are described herein. Pharmaceutical compositions comprising agents or compounds that modulate Th17 cell specification are also encompassed. Methods for modulating Th17 cell specification using agents identified using assays described herein in pharmaceutical compositions are also envisioned. Such pharmaceutical compositions are useful for treating inflammatory conditions and autoimmune diseases associated with Th17 cell mediated pathology.
    Type: Application
    Filed: September 24, 2013
    Publication date: May 1, 2014
    Inventors: Dan Littman, Maria Ciofani, Richard A. Bonneau, JR.
  • Patent number: 8697686
    Abstract: The present invention is directed to crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, compositions containing the same and uses thereof.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 15, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Rajesh K. Agarwal, William L. Betts, III, James A. Henshilwood, Yuan-Hon Kiang, Noah Post
  • Patent number: 8680091
    Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula (I) as selective 5-HT2c receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety, where, R6 is —NR10R11, where R10 is substituted phenylalkyl or substituted pyridylalkyl and other substituents are as defined in the specification.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: March 25, 2014
    Assignee: Eli Lilly and Company
    Inventors: Karen Briner, Manuel Javier Cases-Thomas, Marta Adeva Bartolome, Christopher Stanley Galka, Alicia Marcos Llorente, Maria Angeles Martinez-Grau, Michael Philip Mazanetz, John Cunningham O'Toole, Richard Edmund Rathmell, Matthew Robert Reinhard, Selma Sapmaz, Andrew Caerwyn Williams
  • Publication number: 20140073629
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Jehrod Burnett BRENNEMAN, John GINN, Michael D. LOWE, Christopher Ronald SARKO, Edward S. TASBER, Zhonghua ZHANG
  • Publication number: 20140051684
    Abstract: The present invention is directed to crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, compositions containing the same and uses thereof.
    Type: Application
    Filed: September 14, 2012
    Publication date: February 20, 2014
    Inventors: Rajesh K. Agarwal, William L. Betts, III, James A. Henshilwood, Yuan-Hon Kiang, Noah Post
  • Publication number: 20140030332
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a chemosensory receptor ligand, such as a bitter receptor ligand. Also provided herein are chemosensory receptor ligand compositions, including bitter receptor ligand compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: January 6, 2012
    Publication date: January 30, 2014
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley, Mark S. Fineman
  • Patent number: 8633173
    Abstract: This application relates, in part, to compounds of the general Formula I and/or salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of inhibiting at least JAK2 in subjects in recognized need thereof for the treatment of diseases or disorders for which inhibition of at least JAK2 is indicated.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: January 21, 2014
    Assignee: Cephalon, Inc
    Inventors: Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. Milkiewicz
  • Patent number: 8633184
    Abstract: The invention is directed to compounds of Formula (I) useful as PPAR agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, diabetes, nephropathy, neuropathy, retinopathy, polycystic ovary syndrome, hypertension, ischemia, stroke, irritable bowel disorder, inflammation, cataract, cardiovascular diseases, Metabolic X Syndrome, hyper-LDL-cholesterolemia, dyslipidemia (including hypertriglyceridemia, hypercholesterolemia, mixed hyperlipidemia, and hypo-HDL-cholesterolemia), atherosclerosis, obesity, and other disorders related to lipid metabolism and energy homeostasis complications thereof, using compounds of the invention are also described.
    Type: Grant
    Filed: January 19, 2010
    Date of Patent: January 21, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
  • Publication number: 20140005177
    Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
    Type: Application
    Filed: March 8, 2012
    Publication date: January 2, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventors: Francis Louis Atkinson, Michael David Barker, John Liddle, David Matthew Wilson
  • Publication number: 20130317010
    Abstract: To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HT5A receptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HT5A receptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed.
    Type: Application
    Filed: August 1, 2013
    Publication date: November 28, 2013
    Applicant: Astellas Pharma Inc
    Inventors: Wataru HAMAGUCHI, Isao KINOYAMA, Yohei KOGANEMARU, Takehiro MIYAZAKI, Osamu KANEKO, Ryuichi SEKIOKA, Takuya WASHIO
  • Publication number: 20130315994
    Abstract: The present invention relates to methods for weight management that utilize modified-release dosage forms comprising (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts and crystalline forms thereof. The present invention further relates to (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts, crystalline forms thereof and modified-release dosage forms comprising them.
    Type: Application
    Filed: August 31, 2011
    Publication date: November 28, 2013
    Inventors: Zezhi Jesse Shao, Anthony C. Blackburn, Andrew J. Grottick, Michael Morgan, Jaimie Karyn Rueter, Anna Shifrina, Scott Stirn, Libo Yang, Woo Hyun Yoon
  • Publication number: 20130310369
    Abstract: Salts of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine with optically active acids, and pharmaceutical compositions comprising them that are useful for, inter alia, weight management.
    Type: Application
    Filed: August 31, 2011
    Publication date: November 21, 2013
    Inventors: Anthony C. Blackburn, William Lucas Betts, III, Jaimie Karyn Rueter, Yun Shan, Anna Shifrina, Scott Stim
  • Publication number: 20130303508
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: ABBVIE INC.
    Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
  • Patent number: 8580780
    Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R6 is —S—R14; and other substituents are as defined in the specification.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: November 12, 2013
    Assignee: Eli Lilly and Company
    Inventors: John Gordon Allen, Karin Briner, Christopher Stanley Galka, Maria Angeles Martinez-Grau, Matthew Robert Reinhard, Michael John Rodriguez, Roger Ryan Rothhaar, Michael Wade Tidwell, Frantz Victor, Deyi Zhang, Steven Armen Boyd, Arundhati S. Deo, Wai-Man Lee, Christopher Stephen Siedem, Ajay Singh
  • Patent number: 8575149
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 5, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Jeffrey Smith, Brian Smith
  • Publication number: 20130267500
    Abstract: Uses of 5-HT2C receptor agonists in the treatment of disorders ameliorated by reduction of an individual's norepinephrine level, wherein said disorders include but are not limited to hypernorepinephrinemia, cardiomyopathy, cardiac hypertrophy, cardiomyocyte hypertrophy in post-myocardial infarction remodeling, elevated heart rate, vasoconstriction, acute pulmonary vasoconstriction, hypertension, heart failure, cardiac dysfunction after stroke, cardiac arrhythmia, metabolic syndrome, abnormal lipid metabolism, hyperthermia, Cushing syndrome, pheochromocytoma, epilepsy, obstructive sleep apnea, insomnia, glaucoma, osteoarthritis, rheumatoid arthritis, and asthma.
    Type: Application
    Filed: August 31, 2011
    Publication date: October 10, 2013
    Inventors: Christen M. Anderson, William R. Shanahan
  • Patent number: 8546379
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: October 1, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Brian Smith, Jeffrey Smith
  • Publication number: 20130217677
    Abstract: The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 22, 2013
    Applicant: Arena Pharmaceuticals, Inc.
    Inventor: Arena Pharmaceuticals, Inc.
  • Publication number: 20130217676
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 22, 2013
    Inventors: Brian Smith, Jeffrey Smith
  • Publication number: 20130184256
    Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 18, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Henning PRIEPKE, Georg DAHMANN, Kai GERLACH, Roland PFAU, Wolfgang WIENEN, Annette SCHULER-METZ, Sandra HANDSCHUH, Herbert NAR