3-benzazepines (including Hydrogenated) Patents (Class 514/217.01)
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Publication number: 20110269745Abstract: 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: ApplicationFiled: June 9, 2011Publication date: November 3, 2011Applicant: ELI LILLY AND COMPANYInventors: Karin BRINER, Marta ADEVA BARTOLOME, Manuel Javier CASES-THOMAS, 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
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Publication number: 20110269736Abstract: The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases.Type: ApplicationFiled: July 24, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
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Publication number: 20110257130Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.Type: ApplicationFiled: October 16, 2009Publication date: October 20, 2011Inventor: Desikan Rajagopal
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Publication number: 20110251172Abstract: The invention encompasses purine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.Type: ApplicationFiled: July 31, 2009Publication date: October 13, 2011Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti, Christohpher L. Hamblett, Yudith Garcia, Michelle Martinez, Benito Munoz
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Patent number: 8022062Abstract: 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, —O—R12, —S—R14, or —NR24R25; and other substituents are as defined in the specification.Type: GrantFiled: February 18, 2005Date of Patent: September 20, 2011Assignee: Eli Lilly and CompanyInventors: John Gordon Allen, Karin Briner, Michael Philip Cohen, Christopher Stanley Galka, Sarah Lynne Hellman, Maria Angeles Martinez-Grau, Matthew Robert Reinhard, Michael John Rodriguez, Roger Ryan Rothhaar, Michael Wade Tidwell, Frantz Victor, Andrew Caerwyn Williams, Deyi Zhang, Michael Philip Mazanetz
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Substituted prolinamides, the preparation thereof and the use thereof as pharmaceutical compositions
Patent number: 8003639Abstract: The present invention provides new substituted prolinamides of the general formula (I) in which D, L, E, G, J, M, R3, R4, R5, and R13 are defined as in claim 1, their tautomers, their enantiomers, their diastereomers, their mixtures and their salts, more particularly their physiologically tolerated salts with organic or inorganic acids or bases, which exhibit valuable properties.Type: GrantFiled: February 13, 2007Date of Patent: August 23, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Herbert Nar, Roland Pfau, Annette Schuler-Metz, Wolfgang Wienen -
Patent number: 8003638Abstract: Compounds of formula (I) or a salt thereof are disclosed: wherein R1 is pyrazolyl substituted by two or three substituents independently selected from halogen, C1-4alkyl and haloC1-4alkyl; R2 is hydrogen or methyl; and R3 is quinolinyl, oxazolyl or phenyl, each of which is optionally substituted by one or two halogen, C1-4alkyl or haloC1-4alkyl. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.Type: GrantFiled: June 17, 2005Date of Patent: August 23, 2011Assignee: Glaxo Group LimitedInventors: Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco
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Patent number: 7994163Abstract: 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: R6 D R?N—R?R* where R6 is —(CrC3)alkyl-S—(C0-C3)alkyl-R10, —(C1-C3)alkyl-NR11R12, —(CrC3)alkyl-O—R13. and other substituents are as defined in the specification.Type: GrantFiled: September 1, 2006Date of Patent: August 9, 2011Assignee: Eli Lilly and CompanyInventors: John Gordon Allen, Karin Briner, Christopher Stanley Galka, Richard Charles Hoying, Maria Angeles Martinez-Grau, Julie Miyashiro, Natalia Pokrovskaia, Matthew Robert Reinhard
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Patent number: 7989445Abstract: The present invention relates to a compound represented by the formula: wherein Ar is an optionally substituted ring; A is a spacer having a main chain of 1 to 4 atoms; B is a bond, a C1-10 alkylene group or an oxygen atom; R3 and R5 are each independently a hydrogen atom or a substituent; R4 is an optionally substituted cyclic group or an optionally substituted C1-10 alkyl group; and R1 and R2 are each independently a hydrogen atom or a substituent, or R1 and R2 or R1 and B are bonded to form an optionally substituted nitrogen-containing heterocycle, or R1 and Ar are bonded to form an optionally substituted nitrogen-containing fused heterocycle, or a salt thereof. The thienopyrimidone compound of the present invention has a superior melanin-concentrating hormone receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of obesity and the like.Type: GrantFiled: April 27, 2006Date of Patent: August 2, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Toshiki Murata, Shingo Makino
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Patent number: 7981882Abstract: 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: Formula (I) where: R6 is selected from the group consisting of (a, b, c, d, e) and other substituents are as defined in the specification.Type: GrantFiled: September 1, 2006Date of Patent: July 19, 2011Assignee: Eli Lilly and CompanyInventors: Karin Briner, Anne Marie Camp, Alan Cornell, Michael Philip Mazanetz, Roger Ryan Rothhaar, Frantz Victor, Andrew Caerwyn Williams, Deyi Zhang
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Publication number: 20110172204Abstract: A compound of the formula: wherein: R1 represents C1-6 alkyl or H; Y represents —NR2R3 as depicted in formula (B), or a ring of formula (A) wherein a represents the point of attachment to the pyrimidinyl ring; R2 represents C1-4alkyl substituted by C1-3 alkoxy; R3 represents C1-4 alkyl; W represents —(CH2)n—; W1 represents —(CH2)p—; n represents 1 or 2 or 3; p represents 1 or 2; R4 represents C1-4 alkoxy, C1-6 alkyl or halogen; and R5 represents halogen or H, provided that, when R4 represents halogen, R5 is not H, or a pharmaceutically acceptable salt thereof. The compounds of the invention have been found to modulate the histamine H3 receptor.Type: ApplicationFiled: January 7, 2011Publication date: July 14, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Parminder Kaur Pooni, Kevin John Merchant, William John Buffham
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Patent number: 7977329Abstract: 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: GrantFiled: November 14, 2006Date of Patent: July 12, 2011Assignee: Arena Pharmaceuticals, Inc.Inventors: Jeffrey Smith, Brian Smith
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Publication number: 20110166125Abstract: 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: ApplicationFiled: November 14, 2008Publication date: July 7, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
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Publication number: 20110152250Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.Type: ApplicationFiled: September 3, 2010Publication date: June 23, 2011Applicant: ABBOTT LABORATORIESInventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, JR., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
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Publication number: 20110135601Abstract: The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of ?NH or ?O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.Type: ApplicationFiled: June 12, 2008Publication date: June 9, 2011Inventor: Makoto Bamba
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Publication number: 20110130384Abstract: The present invention aims to provide a prophylactic or therapeutic agent for schizophrenia and the like, containing the compound of the present invention having a GPR52 agonist activity. A compound represented by the following formula (I) or a salt thereof: wherein, A is —CONH or the like, B is a hydrogen atom or a substituent, ring Cy1 is a benzene ring or the like, X1, X2 and X3 are each independently —CH? or —N? or the like, ring Cy2 is a carbon ring or the like, Z is a carbon atom or a nitrogen atom, L is a bond or the like, n is 1 or 2, Rb is a hydrogen atom or a substituent, and ring Cy3 is a benzene ring or the like.Type: ApplicationFiled: June 24, 2009Publication date: June 2, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaki Setoh, Yuhei Miyanohana, Mitsunori Kouno
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Publication number: 20110130383Abstract: Use of compounds of general formula (1) and pharmacologically acceptable salts and prodrugs thereof: Formula (1) wherein A and B are CH2 or CH2CH2, R1 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl or heteroaralkyl, R2, R3 and R4 are selected from hydrogen, alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl or cyano; X is R5CO, R5SO2, R5R7NCO, R5R7NSO2, R5SO2NR7CO or CO2R8, Y is R6CO, R6SO2, R6R7NCO, R6R7NSO2, R6SO2NR7CO or CO2R8, R5 and R6 are hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl, R7 is hydrogen, alkyl, aryl or aralkyl, and R8 is alkyl, aryl, aralkyl, alkoxyalkyl, heteroaryl or heteroarylalkyl, provided that when X is R5CO or R5SO2, then Y is not R6CO, R6SO2 or R6R7NCO, in the manufacture of a medicament for the prophylaxis or treatment of inflammatory or immunological disease.Type: ApplicationFiled: September 28, 2007Publication date: June 2, 2011Applicant: LECTUS THERAPEUTICS LIMITEDInventors: Geoff Lawton, Roland Kozlowski, Dayle Hogg
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Publication number: 20110130385Abstract: The present invention relates to novel bicyclic heterocycle derivatives, pharmaceutical compositions comprising the bicyclic heterocycle derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is: I, Ia, Ib ou Ic. R2 is alkyl, alkenyl, aryl, cycloalkyl.Type: ApplicationFiled: July 21, 2009Publication date: June 2, 2011Inventors: Manuel De Lera Ruiz, Michael Y. Berlin, Junying Zheng, Robert G. Aslanian, Kevin D. Mccormick
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Publication number: 20110124626Abstract: A compound having the formula (1) wherein: R1 is a group selected from C3-8 cycloalkyl, C1-6 alkyl, C1-6 alkylene-C3-8 cycloalkyl, each of which groups may optionally be substituted with C1-6 alkyl, halogen, haloC1-6 alkyl or OR15, or R1 is heterocyclyl, optionally substituted with C1-6 alkyl, haloC1-6 alkyl or OR15; n is 0, 1, 2, 3 or 4, the alkylene group —(CH2)m— formed thereby being optionally substituted with a group selected from C1-4 alkyl, C3-8 cycloalkyl and arylsulfonyl; A is a group selected from —N(R2)CO—, —CON(R2)-, —OC(O)—, —C(O)O—, —CO—, —C(R2)(OR3)-, —C(?N—O—R3)-, —C(?CR2R3)-, —C3-8 cycloalkylene-, —C(R2)(haloC1-6alkyl)-, C1-4 alkylene and —C(OR3)(haloC1-6alkyl)-; R2 and R3 are each independently selected from H, C1-6 alkyl, and C3-8 cycloalkyl, or, when A is —N(R2)CO— and X is absent, R2 may form, together with the adjacent nitrogen atom and Z, an N-containing heterocyclyl group, which may optionally be substituted; X is absent or is C14 alkylene or C24 alkenylene, each of which may optionallType: ApplicationFiled: July 17, 2009Publication date: May 26, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Parminder Kaur Pooni, Kevin John Merchant, Catrina Morvern Kerr, Stuart Richard Crosby, Tomohiro Okawa, Mitsuru Sasaki, Mika Gotou, Graham Andrew Showell, Martin Richard Teall
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Publication number: 20110098269Abstract: The present invention provides compounds according to Formulas I, II, III, IV, V, VI, VII or VIII: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: ApplicationFiled: November 17, 2010Publication date: April 28, 2011Applicant: Cephalon, Inc.Inventors: Nadine C. Becknell, Reddeppa reddy Dandu, Derek D. Dunn, Robert L. Hudkins, Kurt A. Josef, Babu G. Sundar, Allison L. Zulli
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Publication number: 20110082130Abstract: Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: August 23, 2010Publication date: April 7, 2011Applicant: LIGAND PHARMACEUTICALS, INC.Inventors: Yang Gao, Bingsong Han, Yuelian Xu, Timothy M Caldwell, Linghong Xie
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Publication number: 20110039827Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: June 21, 2010Publication date: February 17, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
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Publication number: 20110028390Abstract: The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: May 18, 2009Publication date: February 3, 2011Applicant: PFIZER, INC.Inventors: Jeffrey W. Corbett, Richard Elliott, Kevin Freeman-Cook, David A. Griffith, Dennis P. Phillion
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Publication number: 20110021488Abstract: The present invention relates to compounds of general formula I wherein A, B, D, Y, R1, R2, R3, R4 and R5 are defined as in the specification, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: October 5, 2010Publication date: January 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Iris KAUFFMANN-HEFNER, Norbert HAUEL, Rainer WALTER, Heiner EBEL, Henri DOODS, Angelo CECI, Annette SCHULER-METZ, Ingo KONETZKI
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Publication number: 20110020460Abstract: Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.Type: ApplicationFiled: June 4, 2010Publication date: January 27, 2011Inventors: Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
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Publication number: 20110014283Abstract: The present invention relates to a novel dosage form, to a process for preparing the dosage form and to the use of the dosage form in the treatment of neurological and psychiatric disorders.Type: ApplicationFiled: February 28, 2008Publication date: January 20, 2011Inventors: Allan James Clarke, David Geoffrey Cullingford, Yu Li
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Publication number: 20100331312Abstract: Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.Type: ApplicationFiled: February 18, 2009Publication date: December 30, 2010Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Vincent J. Santora, Brian J. Hofilena, Michelle Pulley, Graeme Semple, Yun Shan, Brian M. Smith
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Publication number: 20100317572Abstract: This invention relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a compound of Formula I and an anti-obesity compound. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating obesity or an obesity associated disease.Type: ApplicationFiled: December 18, 2008Publication date: December 16, 2010Applicant: NeuroSearch A/SInventor: Jens Damsgaard Mikkelsen
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Publication number: 20100311693Abstract: This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.Type: ApplicationFiled: June 4, 2010Publication date: December 9, 2010Applicant: CEPHALON, INC.Inventors: Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. Milkiewicz
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Publication number: 20100305099Abstract: 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 characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: December 2, 2008Publication date: December 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Juergen Braunger, Daniel Kuhn
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Publication number: 20100273778Abstract: 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: ApplicationFiled: April 26, 2010Publication date: October 28, 2010Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Gin C. Hsieh, Jorge D. Brioni, James P. Sullivan
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Publication number: 20100273777Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.Type: ApplicationFiled: April 6, 2010Publication date: October 28, 2010Applicant: Hydra Biosciences, Inc.Inventors: Jayhong A. Chong, Christopher Fanger, Glenn R. Larsen, William C. Lumma, JR., Magdalene M. Moran, Amy Ripka, Dennis John Underwood, Manfred Weigele, Xiaoguang Zhen
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Publication number: 20100273771Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: December 19, 2008Publication date: October 28, 2010Inventors: Emmanuel Hubert Demont, Jag Paul Heer, John Skidmore, Ian David Wall, Jason Witherington, Thomas Daniel Heightman, David Nigel Hurst, Christopher Norbert Johnson
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Patent number: 7799773Abstract: The present invention relates to novel benzazepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: December 19, 2008Date of Patent: September 21, 2010Assignee: Glaxo Group LimitedInventors: Mark James Bamford, David Kenneth Dean, Sanjeet Singh Sehmi, David Matthew Wilson, Jason Witherington
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Publication number: 20100222316Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: ApplicationFiled: March 17, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
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Publication number: 20100197664Abstract: 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: ApplicationFiled: July 23, 2008Publication date: August 5, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20100197590Abstract: The invention provides compounds of Formula (Ia) or pharmaceutically acceptable salts thereof, as well as the preparation, compositions and uses thereof, where R1, R2, R3, and m are defined as described above.Type: ApplicationFiled: February 1, 2010Publication date: August 5, 2010Inventors: Robert L. Dow, Michael J. Munchhof
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Publication number: 20100197591Abstract: The invention provides compounds of the general Formula (I) where R1, R2, and A are defined herein, as well as the preparation, compositions and uses thereof.Type: ApplicationFiled: February 1, 2010Publication date: August 5, 2010Inventors: Gary E. Aspnes, Robert L. Dow, Michael J. Munchhof
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Publication number: 20100173894Abstract: 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: ApplicationFiled: March 22, 2010Publication date: July 8, 2010Inventors: Smith Brian, Charles A. Gilson, III, Jeffrey Schultz, Jeffrey Smith
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Publication number: 20100152165Abstract: [Problem] To provide a pharmaceutical, particularly a compound which can be used as an insulin secretion promoter or a preventive or therapeutic agent for diabetes mellitus and the like diseases in which GPR40 is concerned. [Means for resolution] It was found that novel carboxylic acid derivatives or salts thereof, characterized in that carboxylic acid is linked to a 6-membered monocyclic aromatic ring via two atoms and said aromatic ring is linked to a nitrogen-containing bicyclic ring via a linker, have excellent GPR40 receptor agonist action. In addition, since the carboxylic acid derivatives of the invention showed excellent insulin secretion promoting action and blood glucose reducing action, they are useful as an insulin secretion promoter and a preventive or therapeutic agent for diabetes mellitus.Type: ApplicationFiled: November 29, 2007Publication date: June 17, 2010Inventors: Kenji Negoro, Kei Ohnuki, Toshio Kurosaki, Fumiyoshi Iwasaki, Yasuhiro Yonetoku, Kazuyuki Tsuchiya, Norio Asai, Shigeru Yoshida, Takatoshi Soga, Daisuke Suzuki
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Publication number: 20100120748Abstract: 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: ApplicationFiled: January 19, 2010Publication date: May 13, 2010Inventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
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Publication number: 20100120747Abstract: The present invention relates to an active substance combination comprising at least one compound with 5-HT6 receptor affinity, and at least one cholinesterase inhibitor, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament.Type: ApplicationFiled: June 22, 2007Publication date: May 13, 2010Applicant: Laboratorios del Dr. Esteve, S.A.Inventors: Xavier Codony-Soler, Helmut Heinrich Buschmann
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Patent number: 7713966Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: GrantFiled: November 20, 2007Date of Patent: May 11, 2010Assignee: Alantos Pharmaceuticals Holding, Inc.Inventors: Christian Gege, Matthias Schneider, Carine Chevrier, Hongbo Deng, Irving Sucholeiki, Brian M. Gallagher, Jr., Michael Bosies, Christoph Steeneck, Xinyuan Wu, Matthias Hochgürtel, Bert Nolte, Arthur Taveras
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Patent number: 7704994Abstract: The present invention relates to benzazepine derivatives of formula (I) wherein: R1 represents —C3-7 cycloalkyl optionally substituted by C1-3 alkyl; having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: July 31, 2007Date of Patent: April 27, 2010Assignee: Glaxo Group LimitedInventors: Sanjeet Singh Sehmi, David Matthew Wilson, Jason Witherington
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Patent number: 7704993Abstract: 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: GrantFiled: June 16, 2004Date of Patent: April 27, 2010Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Charles A. Gilson, III, Jeffrey Schultz, Jeffrey Smith
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Patent number: 7696193Abstract: The present invention relates to benzazepine derivatives of formula (I) wherein: R1 represents —C3-7 cycloalkyl optionally substituted by C1-3 alkyl; having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: December 18, 2003Date of Patent: April 13, 2010Assignee: Glaxo Group LimitedInventors: Sanjeet Singh Sehmi, David Matthew Wilson, Jason Witherington
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Publication number: 20100069362Abstract: The present invention relates to a compound represented by the formula: wherein Ar is an optionally substituted ring; A is a spacer having a main chain of 1 to 4 atoms; B is a bond, a C1-10 alkylene group or an oxygen atom; R3 and R5 are each independently a hydrogen atom or a substituent; R4 is an optionally substituted cyclic group or an optionally substituted C1-10 alkyl group; and R1 and R2 are each independently a hydrogen atom or a substituent, or R1 and R2 or R1 and B are bonded to form an optionally substituted nitrogen-containing heterocycle, or R1 and Ar are bonded to form an optionally substituted nitrogen-containing fused heterocycle, or a salt thereof. The thienopyrimidone compound of the present invention has a superior melanin-concentrating hormone receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of obesity and the like.Type: ApplicationFiled: April 27, 2006Publication date: March 18, 2010Applicant: Takeda Pharmaceutical Company LimitedInventor: Toshiki Murata
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Patent number: 7678786Abstract: 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: GrantFiled: April 17, 2007Date of Patent: March 16, 2010Assignee: Janssen Pharmaceutica NVInventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Pelton
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Publication number: 20100022514Abstract: The invention relates to the use of compounds in the treatment of deacetylase-associated diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.Type: ApplicationFiled: December 17, 2007Publication date: January 28, 2010Inventors: Young Shin Cho, Lei Jiang, Michael Shultz
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Publication number: 20100004223Abstract: 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, preparations, and uses thereof.Type: ApplicationFiled: December 20, 2005Publication date: January 7, 2010Applicant: Arena Phamaceuticals, Inc.Inventors: Rajesh K. Agarwal, William l. Betts, James A. Henshilwood, Yuan-Hon Kiang, Noah Post