3-benzazepines (including Hydrogenated) Patents (Class 514/217.01)
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Publication number: 20130217676Abstract: 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: ApplicationFiled: September 14, 2012Publication date: August 22, 2013Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20130217677Abstract: 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: ApplicationFiled: September 14, 2012Publication date: August 22, 2013Applicant: Arena Pharmaceuticals, Inc.Inventor: Arena Pharmaceuticals, Inc.
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Publication number: 20130184256Abstract: 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: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Henning PRIEPKE, Georg DAHMANN, Kai GERLACH, Roland PFAU, Wolfgang WIENEN, Annette SCHULER-METZ, Sandra HANDSCHUH, Herbert NAR
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Publication number: 20130172322Abstract: 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: September 14, 2012Publication date: July 4, 2013Inventors: Smith Brian, Charles A. Gilson, III, Jeffrey Schultz, Jeffrey Smith
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Publication number: 20130158013Abstract: 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: ApplicationFiled: June 1, 2011Publication date: June 20, 2013Inventors: Anthony C. Blackburn, Anna Shifrina
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Publication number: 20130150341Abstract: 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: ApplicationFiled: December 3, 2012Publication date: June 13, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Patent number: 8461147Abstract: 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: GrantFiled: December 2, 2008Date of Patent: June 11, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Ioannis Sapountzis, Juergen Braunger, Daniel Kuhn
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Publication number: 20130143870Abstract: 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: ApplicationFiled: November 30, 2012Publication date: June 6, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130123241Abstract: 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: ApplicationFiled: May 10, 2011Publication date: May 16, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Publication number: 20130102590Abstract: 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: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicant: AbbVie IncInventor: AbbVie Inc.
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Patent number: 8420631Abstract: 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: GrantFiled: September 1, 2006Date of Patent: April 16, 2013Assignee: Eli Lilly and CompanyInventors: 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
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Publication number: 20130085134Abstract: Quinoxaline compounds of formula (I) have a PDE9-inhibiting action and are useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: ApplicationFiled: November 27, 2012Publication date: April 4, 2013Applicant: ASTELLAS PHARMA INC.Inventor: ASTELLAS PHARMA INC.
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Patent number: 8404675Abstract: 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: March 22, 2010Date of Patent: March 26, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Charles A. Gilson, III, Jeffrey Schultz, Jeffrey Smith
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Publication number: 20130072427Abstract: 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: July 22, 2010Publication date: March 21, 2013Inventors: Cristiano Guimaraes, Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
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Publication number: 20130059829Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.Type: ApplicationFiled: July 20, 2012Publication date: March 7, 2013Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
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Publication number: 20130059838Abstract: 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: ApplicationFiled: November 6, 2012Publication date: March 7, 2013Applicant: SANOFIInventor: Sanofi
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Patent number: 8367657Abstract: 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: GrantFiled: June 16, 2004Date of Patent: February 5, 2013Assignee: 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
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Publication number: 20130029949Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.Type: ApplicationFiled: July 20, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: 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
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Publication number: 20130018042Abstract: The present invention is directed generally to stable formulations of a TLR agonist preferably a TLR7 or a TLR8 agonist, for use in the treatment of cancer, preferably solid tumors and lymphomas. Specifically, the present invention is directed to stable formulations of up to 50 mg/ml of a TLR agonist which comprise a cyclodextrin.Type: ApplicationFiled: July 16, 2012Publication date: January 17, 2013Inventors: J. Jeffry Howbert, Muralikrishna Duvvuri, Robert Hershberg, Gregory Dietsch
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Publication number: 20130012498Abstract: 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: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20130012495Abstract: 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: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20120316153Abstract: 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: ApplicationFiled: May 10, 2012Publication date: December 13, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co., KGInventors: Wilhelm Amberg, Udo Lange, Michael Ochse, Frauke Pohlki, Berthold Behl, Mario Mezler, Willfried Hornberger, Charles W. Hutchins
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Publication number: 20120295845Abstract: Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is —C(O)—O—R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, —C(O)—NH2, or C1-C6 alkyl substituted with hydroxy or C1-C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, —CH2—(C1-C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or —CH2—(C1—C2)haloalkyl; 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: November 16, 2010Publication date: November 22, 2012Inventors: Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
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Publication number: 20120264743Abstract: 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: ApplicationFiled: March 21, 2012Publication date: October 18, 2012Inventors: Rajesh K. Agarwal, William L. Betts, III, James A. Henshilwood, Yuan-Hon Kiang, Noah Post
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Publication number: 20120258957Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders or diseases influenced by modulation of orexins, such as sleep disorders.Type: ApplicationFiled: November 22, 2010Publication date: October 11, 2012Inventors: Matilda Jane Bingham, Andrew Dunbar, Margaret Jean Laats, Grant Wishart
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Publication number: 20120252788Abstract: 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: ApplicationFiled: June 14, 2012Publication date: October 4, 2012Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20120252786Abstract: 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: ApplicationFiled: March 12, 2012Publication date: October 4, 2012Inventors: Dominic P. Behan, Brian M. Smith, Christina Bienning
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Publication number: 20120252787Abstract: 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: ApplicationFiled: August 31, 2011Publication date: October 4, 2012Inventors: Christen M. Anderson, William R. Shanahan
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Patent number: 8273734Abstract: 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: June 14, 2012Date of Patent: September 25, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20120232061Abstract: 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: ApplicationFiled: March 8, 2012Publication date: September 13, 2012Applicant: GLAXO GROUP LIMITEDInventors: Francis Louis Atkinson, Michael David Barker, John Liddle, David Matthew Wilson
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Publication number: 20120220572Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 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: ApplicationFiled: February 28, 2012Publication date: August 30, 2012Applicant: ABBOTT LABORATORIESInventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
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Patent number: 8252785Abstract: 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: GrantFiled: October 5, 2010Date of Patent: August 28, 2012Assignee: 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: 20120207769Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: April 26, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Publication number: 20120184486Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).Type: ApplicationFiled: October 21, 2010Publication date: July 19, 2012Inventor: Vincent Mascitti
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Publication number: 20120184533Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.Type: ApplicationFiled: July 2, 2010Publication date: July 19, 2012Applicant: ANGION BIOMEDICA CORP.Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
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Patent number: 8217030Abstract: Association of a sinus node If current inhibitor and a ?-blocker and also pharmaceutical compositions containing it. Medicinal products containing the same which are useful in treating angina pectoris, ischaemia, and heart failure.Type: GrantFiled: February 11, 2009Date of Patent: July 10, 2012Assignee: Les Laboratoires ServierInventors: Guy Lerebours-Pegeonniere, Jean-Henri Calvet
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Patent number: 8207160Abstract: The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists.Type: GrantFiled: December 17, 2004Date of Patent: June 26, 2012Assignee: Abbott GmbH & Co. KGInventors: Wilfried Braje, Andreas Haupt, Wilfried Lubisch, Roland Grandel, Karla Drescher, Herve Geneste, Liliane Unger, Daryl R. Sauer
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Patent number: 8207158Abstract: 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: May 27, 2011Date of Patent: June 26, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Publication number: 20120134955Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R1 means a —(C?O)aOb(C1-C6)alkyl group, a —(C?O)aOb(C2-C6)alkenyl group, a —(C?O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C?O)aOb(C1-C6)alkyl group or a group of —(C?O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee 1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.Type: ApplicationFiled: February 18, 2010Publication date: May 31, 2012Inventors: Yasuhiro Goto, Kenji Niyama, Satoshi Sunami, Keiji Takahashi
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Publication number: 20120135982Abstract: 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: ApplicationFiled: May 27, 2011Publication date: May 31, 2012Inventors: Brian Smith, Jeffrey Smith
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Patent number: 8168624Abstract: 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: GrantFiled: December 20, 2005Date of Patent: May 1, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Rajesh K. Agarwal, William L. Betts, III, James A. Henshilwood, Yuan-Hon Kiang, Noah Post
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Publication number: 20120101083Abstract: The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: June 17, 2010Publication date: April 26, 2012Applicant: GLAXO GROUP LIMITEDInventors: James Matthew Bailey, Rino Antonio Bit, Emmanuel Hubert Demont, Lee Andrew Harrison, Katherine Louise Jones, Christian Alan Paul Smethurst, Jason Witherington
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Publication number: 20120094979Abstract: Thiazole or thiadizaloe derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptor are disclosed.Type: ApplicationFiled: June 17, 2010Publication date: April 19, 2012Applicant: Glaxo Wellcome HouseInventors: James Matthew Bailey, Emmanuel Hubert Demont, Xichen Lin, Feng Ren, Christian Alan Paul Smethurst
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Patent number: 8153621Abstract: 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: GrantFiled: December 21, 2005Date of Patent: April 10, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Dominic P. Behan, Brian M. Smith, Christina Bjenning
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Publication number: 20120052130Abstract: Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPFM 19 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: April 12, 2010Publication date: March 1, 2012Inventors: Etzer Darout, Michael Paul DeNinno, Kentaro Futatsugi, Cristiano Ruch Werneck Guimaraes, Bruce Allen Lefker, Vincent Mascitti, Kim Francis McClure, Michael John Munchhof, Ralph Pelton Robinson, JR.
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Publication number: 20120034270Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.Type: ApplicationFiled: October 16, 2009Publication date: February 9, 2012Applicant: Akaal Pharma Pty LtdInventors: Damian W. Grobelny, Gurmit S. Gill
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Publication number: 20120028961Abstract: 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: ApplicationFiled: July 28, 2011Publication date: February 2, 2012Applicant: 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, Steven Armen Boyd, Richard Gerard Conway, Arundhati S. Deo, Wai-Man Lee, Christopher Stephen Siedem, Ajay Singh, Michael Philip MAZANETZ
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Publication number: 20120028919Abstract: The present invention provides a compound of formula I or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula I has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: June 15, 2011Publication date: February 2, 2012Applicant: CEPHALON, INC.Inventors: Henry J. Breslin, Sankar Chatterjee, James L. Diebold, Bruce D. Dorsey, Derek D. Dunn, Diane E. Gingrich, Greg A. Hostetler, Robert L. Hudkins, Rachael Hunter, Kurt A. Josef, Joseph Lisko, Eugen F. Mesaros, Karen L. Milkiewicz, Gregory R. Ott, Babu G. Sundar, Jay P. Theroff, Tho Thieu, Rabindranath Tripathy, Theodore L. Underiner, Linda Weinberg, Gregory J. Wells, Craig A. Zificsak
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Publication number: 20120004206Abstract: 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: August 25, 2011Publication date: January 5, 2012Inventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
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Patent number: 8076325Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group selected from cycloalkyl, benzyl and optionally substituted alkyl, R2, R3, R4 and R5 each represent a hydrogen atom or a hydroxy, methyl, —OSO2R10, —OCOR10 or optionally substituted alkoxy group, or R2 and R3, or R3 and R4, or R4 and R5 together form a group —O—(CH2)q—O—, —O—CH?CH—O— or —O—CH?CH—, R6, R7, R8 and R9 each represent a hydrogen atom or an alkoxy group, or R6 and R7, or R7 and R8, or R8 and R9 together form a group —O—(CH2)q—O—, R10 represents a group selected from linear or branched C1-C6alkoxy, NR11R?11 and optionally substituted alkyl, R11 and R?11 each represent a hydrogen atom or an alkyl group, or R11 and R?11 together with the nitrogen atom carrying them form an optionally substituted, monocyclic or bicyclic, nitrogen-containing heterocycle, X represents O, NH or CH2, m and p each represent 0 or 1, n and q each represent 1 or 2, in racemic form or in the form of optical isomers, and also addition salts thereType: GrantFiled: September 9, 2008Date of Patent: December 13, 2011Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Bertrand Goument, Aimee Dessinges, Pascal Caignard, Jean-Paul Vilaine, Catherine Thollon, Nicole Villeneuve, Stefano Chimenti