3-benzazepines (including Hydrogenated) Patents (Class 540/594)
  • Patent number: 10526440
    Abstract: A method of making a polymer network. The method includes providing a composition including a polythiol having more than one thiol group and a polyepoxide having more than one epoxide group, applying a solution including a photolatent base catalyst to a surface of the composition, and subsequently exposing the composition to light. Upon exposure to light, the photolatent base catalyst photochemically generates a first amine and at least partially cures at least the surface of the composition to form the polymer network.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: January 7, 2020
    Assignee: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Jonathan D. Zook, Susan E. DeMoss, Sheng Ye, Andrew R. Davis, Tao Gong
  • Patent number: 9102627
    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: August 11, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Beverly L. Wolgast, Charles A. Gilson, III, Shelley Aytes, Scott A. Estrada, Dipanjan Sengupta, Brian Smith, Max Rey, Ulrich Weigl, Heidedore Jlsabeth Rey-Papina
  • 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: 8993750
    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: July 9, 2014
    Date of Patent: March 31, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Brian Smith, Jeffrey Smith
  • 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
  • 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: 20150045552
    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: July 9, 2014
    Publication date: February 12, 2015
    Inventors: Brian Smith, Jeffery Smith
  • Publication number: 20150038701
    Abstract: The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2, 3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
    Type: Application
    Filed: July 1, 2014
    Publication date: February 5, 2015
    Inventors: Ulrich Weigl, Frank Porstmann, Christoph Straessler, Lars Ulmer, Ulf Koetz
  • 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: 20140336375
    Abstract: The disclosure is directed to compounds identified as allosteric modulators of 5-HT 2CR, as well as pharmaceutical compositions and methods using the same. Certain embodiments also include methods of identifying and methods of synthesizing the compounds. Optimization and development of allosteric 5-HT 2CR modulators that bind sites other than the primary ligand binding site generate novel, highly selective, and potent ligands of 5-HT2CR. Such molecules can be used as small molecule probes for the nervous system and as effective therapeutics for a variety of diseases.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 13, 2014
    Applicant: The Board of Regents of the University of Texas system
    Inventors: Jia Zhou, Chunyong Ding, Kathryn A. Cunningham
  • 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
  • Patent number: 8802845
    Abstract: The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are 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: August 12, 2014
    Assignee: Arena Phamaceuticals, Inc.
    Inventors: Ulrich Weigl, Frank Porstmann, Christoph Straessler, Lars Ulmer, Ulf Koetz
  • 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: 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
  • 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
  • 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
  • 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
  • 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: 20140005382
    Abstract: There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula —CR11R12—, —CO—, —CO—O—, or —CO—NH—, W represents a single bond or a C1-3 alkylene group, and Ring B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group, Y represents a nitrogen atom or the formula N+(RF), RF represents a C1-4 alkyl group, and m and n, which may be the same or different, each represent an integer of 0 or 1.
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Tsuyoshi Busujima, Takahiro Oi, Hiroaki Tanaka, Yoshihisa Shirasaki, Kanako Iwakiri, Nagaaki Sato, Shigeru Tokita
  • 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: 20130317005
    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: November 28, 2013
    Inventors: Anthony C. Blackburn, Yun Shan, Anna Shifrina, Scott Stirn
  • 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: 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
  • 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
  • Patent number: 8501935
    Abstract: The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: August 6, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Ulrich Weigl, Frank Porstmann, Christoph Straessler, Lars Ulmer, Ulf Koetz
  • 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
  • Publication number: 20130178620
    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: Application
    Filed: September 14, 2012
    Publication date: July 11, 2013
    Inventors: Beverly L. Wolgast, CHARLES A. GILSON, III, SHELLEY AYTES, SCOTT A. ESTRADA, DIPANJAN SENGUPTA, BRIAN SMITH, MAX REY, ULRICH WEIGL, HEIDEDORE JLSABETH REY-PAPINA
  • Publication number: 20130178619
    Abstract: The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
    Type: Application
    Filed: September 14, 2012
    Publication date: July 11, 2013
    Inventors: Ulrich Weigl, Frank Porstmann, Christoph Straessler, Lars Ulmer, Ulf Koetz
  • Publication number: 20130165648
    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: Application
    Filed: September 14, 2012
    Publication date: June 27, 2013
    Inventors: Beverly L. Wolgast, Charles A. Gilson, III, Shelley Aytes, Scott A. Estrada, Dipanjan Sengupta, Brian Smith, Max Rey, Ulrich Weigl, Heidedore Jlsabeth Rey-Papina
  • Publication number: 20130158013
    Abstract: Processes and intermediates for preparing salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and pharmaceutically acceptable solvates and hydrates thereof, that are useful for, inter alia, weight management.
    Type: Application
    Filed: June 1, 2011
    Publication date: June 20, 2013
    Inventors: Anthony C. Blackburn, Anna Shifrina
  • Publication number: 20130150341
    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: Application
    Filed: December 3, 2012
    Publication date: June 13, 2013
    Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
  • Patent number: 8461147
    Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, R1-R3, Rx and n are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: June 11, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ioannis Sapountzis, Juergen Braunger, Daniel Kuhn
  • Publication number: 20130143870
    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: Application
    Filed: November 30, 2012
    Publication date: June 6, 2013
    Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
  • Publication number: 20130123241
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.
    Type: Application
    Filed: May 10, 2011
    Publication date: May 16, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
  • Publication number: 20130102590
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
    Type: Application
    Filed: October 18, 2012
    Publication date: April 25, 2013
    Applicant: AbbVie Inc
    Inventor: AbbVie Inc.
  • Patent number: 8420631
    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 —C?C—R10, —CH?CR11R11?, or —(C0-C8)alkyl-Ar2 optionally substituted on the alkyl moiety with 1 to 6 fluoro substituents and other substituents are as defined in the specification.
    Type: Grant
    Filed: September 1, 2006
    Date of Patent: April 16, 2013
    Assignee: Eli Lilly and Company
    Inventors: John Gordon Allen, Karin Briner, Anne Marie Camp, Manuel Javier Cases-Thomas, Richard Charles Hoying, Maria Angeles Martinez-Grau, Michael Philip Mazanetz, Natalia Pokrovskaia, Richard Edmund Rathmell, Roger Ryan Rothhaar, Selma Sapmaz, Andrew Caerwyn Williams
  • Patent number: 8404675
    Abstract: The present invention relates to certain 1-substituted-2,3,4,5-tetrahydro-3-benzazepine derivatives of Formula (I), that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the prophylaxis or treatment of 5HT2C receptor associated diseases, conditions or disorders, such as, obesity and related disorders.
    Type: Grant
    Filed: March 22, 2010
    Date of Patent: March 26, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Brian Smith, Charles A. Gilson, III, Jeffrey Schultz, Jeffrey Smith
  • Publication number: 20130059838
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.
    Type: Application
    Filed: November 6, 2012
    Publication date: March 7, 2013
    Applicant: SANOFI
    Inventor: Sanofi
  • Patent number: 8367657
    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: June 16, 2004
    Date of Patent: February 5, 2013
    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: 20130029949
    Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.
    Type: Application
    Filed: July 20, 2012
    Publication date: January 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
  • Publication number: 20130012495
    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: January 10, 2013
    Inventors: Brian Smith, Jeffrey Smith
  • Publication number: 20130005962
    Abstract: The present invention relates to a process for the manufacturing of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-5-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Zhengxu HAN, Kai GERLACH, Dhileepkumar KRISHNAMURTHY, Burkhard MATTHES, Herbert NAR, Roland PFAU, Henning PRIEPKE, Annette SCHULER-METZ, Chris H. SENANAYAKE, Peter SIEGER, Wenjun TANG, Wolfgang WIENEN, Yibo XU, Nathan K. YEE
  • Publication number: 20120316153
    Abstract: The present invention relates to benzazepine derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such benzazepine derivatives, and the use of such benzazepine derivatives for therapeutic purposes.
    Type: Application
    Filed: May 10, 2012
    Publication date: December 13, 2012
    Applicants: Abbott Laboratories, Abbott GmbH & Co., KG
    Inventors: Wilhelm Amberg, Udo Lange, Michael Ochse, Frauke Pohlki, Berthold Behl, Mario Mezler, Willfried Hornberger, Charles W. Hutchins