3-benzazepines (including Hydrogenated) Patents (Class 514/217.01)
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Publication number: 20090318423Abstract: 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, are of use in the prophylaxis or treatment of diseases and conditions in which Kv1.x channels are involved, such as lower urinary tract disorders, cardiovascular diseases and pain.Type: ApplicationFiled: September 28, 2007Publication date: December 24, 2009Applicant: LECTUS THERAPEUTICS LIMITEDInventors: Geoff Lawton, Roland Kozlowski, Dayle Hogg
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Publication number: 20090258858Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.Type: ApplicationFiled: October 28, 2005Publication date: October 15, 2009Inventors: Jakob Busch-Petersen, Jeffrey Charles Boehm, Huijie Li, John J. Taggart, Hong Xing Yan
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Publication number: 20090239845Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein Z, R1, R2a, R2b, R10, R11 and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: April 24, 2006Publication date: September 24, 2009Inventors: Elizabeth Ann Conway, Gerard Martin Paul Giblin, Mairi Gibson, Adrian Hall, Thomas George Christopher Hayhow, Mark Patrick Healy, David Nigel Hurst, Ian Reginald Kilford, Stephen Carl McKeown, Alan Naylor, Helen Susanne Price, Derek Anthony Rawlings
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Publication number: 20090197868Abstract: 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: December 21, 2005Publication date: August 6, 2009Inventors: Dominic P. Behan, Brian M. Smith, Christina Bjenning
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Patent number: 7560453Abstract: The present invention relates to radiolabelled compounds of formula (I), which are useful for the labelling and diagnostic imaging of histamine H3 receptor functionality.Type: GrantFiled: January 5, 2006Date of Patent: July 14, 2009Assignee: Glaxo Group LimitedInventor: Christophe Plisson
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Publication number: 20090163475Abstract: The present invention relates to a novel polymorphic form of 7-[4-(4-chlorobenzyloxy)benzenesulfonyl]-8-methoxy-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepinium maleate and a pharmaceutically acceptable solvate thereof, pharmaceutical formulation, process for its preparation and its use in medicine, in particular its use as an antipsychotic agent.Type: ApplicationFiled: May 22, 2006Publication date: June 25, 2009Inventors: Celine Bret, Sarah Jane Burgess, Simon John Hollas, Ian James King
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Publication number: 20090143363Abstract: This invention relates to novel compounds that are 3-benzazepine derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 3-benzazepine derivatives that are derivatives of lorcaserin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a 5-HT2C agonist, such as lorcaserin.Type: ApplicationFiled: October 15, 2008Publication date: June 4, 2009Applicant: CoNCERT Pharmaceuticals, Inc.Inventor: Julie F. Liu
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Publication number: 20090118260Abstract: The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.Type: ApplicationFiled: October 16, 2008Publication date: May 7, 2009Applicants: AMR TECHNOLOGY, INC., BRISTOL-MYERS SQUIBB COMPANYInventors: Bruce F. MOLINO, Shuang LIU, Aruna SAMBANDAM, Peter R. GUZZO, Min HU, Congxiang ZHA, Kassoum NACRO, David D. MANNING, Matthew L. ISHERWOOD, Kristen N. FLEMING, Wenge CUI, Richard E. OLSON
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Publication number: 20090105226Abstract: 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: ApplicationFiled: December 19, 2008Publication date: April 23, 2009Inventors: Mark James BAMFORD, David Kenneth Dean, Sanjeet Singh Sehmi, David Matthew Wilson, Jason Witherington
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Publication number: 20090105225Abstract: The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis.Type: ApplicationFiled: April 18, 2007Publication date: April 23, 2009Applicant: GLAXO GROUP LIMITEDInventors: Paul Martin Gore, Ashley Paul Hancock, Simon Teanby Hodgson, Leanda Jane Kindon, Panayiotis Alexandrou Procopiou
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Publication number: 20090105224Abstract: 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: ApplicationFiled: December 17, 2004Publication date: April 23, 2009Inventors: Wilfried Braje, Andreas Haupt, Wilfried Lubisch, Roland Grandel, Karla Drescher, Herve Geneste, Liliane Unger, Daryl R. Sauer
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Publication number: 20090099155Abstract: The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzoazepines 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: ApplicationFiled: September 9, 2005Publication date: April 16, 2009Inventors: 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 Rothaar, 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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Patent number: 7514422Abstract: 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: August 13, 2004Date of Patent: April 7, 2009Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Patent number: 7504392Abstract: The invention provides compounds of the formula or a pharmaceutically acceptable salts thereof. The compounds are useful in therapy, in particular as antipsychotic agents.Type: GrantFiled: May 28, 2003Date of Patent: March 17, 2009Assignee: Glaxo Group LimitedInventors: Ian Thomson Forbes, Vincenzo Garzya, Andrew Derrick Gribble, Andrew Lightfoot, Andrew H. Payne, Graham Walker
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Patent number: 7504393Abstract: A compound of the formula (I): wherein R1 is a C1-C6 alkyl group, an amino group, a (C1-C6 alkyl)amino group, a di(C1-C6 alkyl)amino group or a nitrogen-containing saturated heterocyclic group; R3 is a hydrogen atom or a C1-C6 alkyl group; Arom is an unsubstituted or substituted aryl group or an unsubstituted or substituted heteroaryl group; wherein the substituted aryl group is substituted at 1 to 5 positions and the substituted heteroaryl group is substituted at 1 to 3 positions; and wherein the substituents of the aryl group and of the heteroaryl group are independently selected from the group consisting of halogen atom, C1-C6 alkyl, halogeno C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C3 alkylenedioxy, C1-C7 alkanoyl, C2-C7 alkyloxycarbonyl, amino, C1-C7 alkanoylamino, hydroxyl, mercapto, cyano, nitro and carboxyl; A is a C1-C6 alkylene group; Ra together with R2 is a C2-C3 alkylene group containing a double bond; E is a single bond, an oxygen atom, a sulfur atom or a group of the formula: —NR4—, wType: GrantFiled: October 19, 2006Date of Patent: March 17, 2009Assignee: BTG International LimitedInventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
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Publication number: 20090069296Abstract: 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?1 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 thereoType: ApplicationFiled: September 9, 2008Publication date: March 12, 2009Applicant: LES LABORATOIRES SERVIERInventors: Jean-Louis Peglion, Bertrand Goument, Aimee Dessinges, Pascal Caignard, Jean-Paul Vilaine, Catherine Thollon, Nicole Villeneuve, Stefano Chimenti
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SUBSTITUTED PROLINAMIDES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
Publication number: 20090048231Abstract: 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: ApplicationFiled: February 13, 2007Publication date: February 19, 2009Inventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Herbert Nar, Roland Pfau, Annette Schuler-Metz, Wolfgang Wienen -
Publication number: 20090042862Abstract: The present invention relates to novel bicyclic benzamide 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: ApplicationFiled: September 29, 2008Publication date: February 12, 2009Inventors: Desmond John Best, Barry Sidney Orlek
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Publication number: 20090005361Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising a therapeutic agent acting on the renin-angiotensin system (RAS) or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention of, delay of progression of, treatment of diseases and disorders that may be modulated by action on the renin-angiotensin system (RAS), appetency disorders or substance abuse disorders.Type: ApplicationFiled: February 5, 2007Publication date: January 1, 2009Inventor: Randy Lee Webb
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Publication number: 20080312213Abstract: 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: ApplicationFiled: June 17, 2005Publication date: December 18, 2008Applicant: GLAXO GROUP LIMITEDInventors: Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco
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Patent number: 7446103Abstract: The present invention relates to novel bicyclic benzamide 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: October 20, 2003Date of Patent: November 4, 2008Assignee: Glaxo Group LimitedInventors: Desmond John Best, Barry Sidney Orlek
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Publication number: 20080269197Abstract: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxy C1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR5R6, —SO2NR5R6, —(CH2)pNR5R6, —(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R3 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halogen, —OSO2CF3, —(CH2)pC3-6cycloalkyl, —(CH2)qOC1-6alkyl or —(CH2)pOC3-6cycloalkyl; R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyType: ApplicationFiled: June 24, 2008Publication date: October 30, 2008Inventors: Ian Thomson Forbes, Vincenzo Garzya, Andrew Derrick Gribble, Andrew Lightfoot, Andrew H. Payne, Graham Walker
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Publication number: 20080269196Abstract: 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: September 1, 2006Publication date: October 30, 2008Inventors: Karin Briner, Maria 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: 20080255083Abstract: The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U, V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: ApplicationFiled: August 24, 2007Publication date: October 16, 2008Inventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Joerg Kley, Klaus Rudolf, Armin Heckel, Marcus Schindler, Ralf Lotz, Thorsten Lehmann-Lintz
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Publication number: 20080255092Abstract: 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: ApplicationFiled: September 1, 2006Publication date: October 16, 2008Inventors: 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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Publication number: 20080255093Abstract: The present invention is drawn to combinations of pharmaceutical agents having similar chemical and/or pharmacological properties, wherein the combinations maximize the therapeutic effect of the drug while minimizing their adverse effects. The methods and compositions of the invention are particularly useful in the treatment of obesity and related conditions which involves treating a subject with a sympathomimetic agent (e.g., phentermine or a phentermine-like drug) or bupropion in combination with an anti-epileptic agent (e.g., topiramate, zonisamide), CB1 antagonists (e.g., rimonabant), or a 5HT2C-selective serotonin receptor agonist, (e.g., lorcaserin) for the treatment of obesity and related conditions. The invention also features kits for use in the practice of these novel therapies.Type: ApplicationFiled: April 29, 2008Publication date: October 16, 2008Inventors: Peter Y. Tam, Leland F. Wilson
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Patent number: 7435729Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-? over ER-?. Methods are disclosed for modulating ER-? in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-?. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: December 8, 2003Date of Patent: October 14, 2008Assignee: Signal Pharmaceuticals, LLCInventors: Leah Marie Gayo-Fung, Bernd M. Stein
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Patent number: 7429579Abstract: The invention provides compounds of formula (I): wherein: R2 and R3 independently represent various substituents; R1 and R4 independently represent H, F, Cl, Br, C1-2alkyl, C1alkoxy, OH, CN, or NO2; B represents a sulfur atom or a —CH2-group; t represents 3 or 4; and A represents an optionally substituted 5- or 6-membered aromatic heterocyclic ring, or an optionally substituted bicyclic heterocyclic ring system in which at least the ring bound to the group B in Formula (I) is aromatic; or a salt thereof.Type: GrantFiled: November 12, 2001Date of Patent: September 30, 2008Assignee: SmithKline Beecham, PLCInventors: Michael Stewart Hadley, Andrew Lightfoot, Gregor James MacDonald, Geoffrey Stemp
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Publication number: 20080234252Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, solvate, ester or amide thereof, wherein R1 represents [CH2]n—R2.Type: ApplicationFiled: May 8, 2006Publication date: September 25, 2008Inventors: Justin Stephen Bryans, Patrick Stephen Johnson, Lee Richard Roberts, Thomas Ryckmans
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Publication number: 20080214520Abstract: 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: ApplicationFiled: September 1, 2006Publication date: September 4, 2008Inventors: 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: 20080139532Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. as agents to treat various aspects drug dependency or as antipsychotic agents.Type: ApplicationFiled: March 4, 2005Publication date: June 12, 2008Applicant: Glaxo Group LimitedInventors: Luca Arista, Giorgio Bonanomi, Federica Damiani, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco
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Publication number: 20080095720Abstract: Compositions that benefit skin and that reduce irritation of the skin are described. The compositions have a skin benefit agent like a hydroxy acid and a vanilloid receptor antagonist. The compositions of this invention can reduce wrinkles on the skin when applied, and they can be formulated to contain glycolic acid and capsazepine.Type: ApplicationFiled: October 18, 2006Publication date: April 24, 2008Applicant: CONOPCO, INC., D/B/A UNILEVERInventor: Helen Meldrum
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Publication number: 20080045502Abstract: 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: ApplicationFiled: June 16, 2004Publication date: February 21, 2008Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Beverly L. Wolgast, Charles A. Gilson, Shelley Aytes, Scott A. Estrada, Dipanjan Sengupta, Brian Smith, Max Rey, Ulrich Weigl
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Publication number: 20080009478Abstract: The present invention relates to substituted-2,3,4,5-tetrahydro-3-benzazepine derivatives 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: October 21, 2004Publication date: January 10, 2008Applicant: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Charles A. Gilson III, Jeffrey A. Schultz, Scott A. Estrada
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Publication number: 20070293475Abstract: Aryl tetrahydrobenzazepine derivatives with minimal 5-HT2B activity relative to 5-HT2A and 5-HT2C activity that are useful for treating glaucoma are disclosed.Type: ApplicationFiled: June 12, 2007Publication date: December 20, 2007Applicant: ALCON MANUFACTURING LTD.Inventors: Suchismita Mohapatra, Mark R. Hellberg, Zixia Feng
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Patent number: 7304050Abstract: Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I as disclosed herein can be used in a variety of applications, including using the invention compounds to treat bacterial infections.Type: GrantFiled: September 1, 2004Date of Patent: December 4, 2007Assignee: Pfizer Inc.Inventors: Susan Hagen, Vara Prasad Venkata Nagendra Josyula
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Publication number: 20070244094Abstract: 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: April 17, 2007Publication date: October 18, 2007Inventors: Gee-Hong Kuo, Yan Zhang, Lan Shen, Songfeng Lu, Keith T. Demarest, Patricia Peiton
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Patent number: 7229986Abstract: A melanin-concentrating hormone antagonist comprising a compound of the formula: wherein R is hydrogen atom or a cyclic group which may be substituted; X is a bond or a spacer having a main chain of 1 to 10 atoms; Y is a spacer having a main chain of 1 to 6 atoms; ring A is benzene ring which may be further substituted; ring B is a 5- to 9-membered nitrogen-containing non-aromatic heterocyclic ring which may be further substituted; R1 and R2 are the same or different and are hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; or R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or a salt thereof is useful as a preventive or therapeutic agent for obesity, etc.Type: GrantFiled: May 15, 2001Date of Patent: June 12, 2007Assignee: Takeda Pharmaceutical Company Ltd.Inventors: Yuji Ishihara, Jun Terauchi, Nobuhiro Suzuki, Shiro Takekawa, Kazuyoshi Aso
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Patent number: 7173023Abstract: The present invention relates to novel benzazepine derivatives of the following formula: wherein R1, R2, R3, R4 and R5, X, X?, Y and Y? are as defined in the description and claims, processes for their preparation, pharmaceutical compositions containing said derivatives and their use for the preparation of medicaments useful for the prevention and treatment of diseases in which selective inhibition of monoamine oxidase B activity plays a role or is implicated.Type: GrantFiled: October 18, 2004Date of Patent: February 6, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
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Patent number: 7122538Abstract: The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR5R6, —SO2NR5R6, —(CH2)NR5R6, —(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R3 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8 or —(CH2)pNR7COR8; R4represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, trifluoromethyl, trifluoroType: GrantFiled: October 6, 2003Date of Patent: October 17, 2006Assignee: Glaxo Group LimitedInventors: Ian Thomson Forbes, Andrew Derrick Gribble, Andrew P. Lightfoot, Andrew H. Payne
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Patent number: 7008938Abstract: A benzene-fused heteroring derivative of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of immune diseases (autoimmune diseases, infectious diseases, etc.), inflammatory diseases (inflammatory bowel diseases, multiple cerebrosclerosis, arthritis, etc.), nerve degeneration diseases (Alzheimer's disease, muscular dystrophy, etc.), bone resorption diseases (osteoporosis, etc.), respiratory system diseases, diabetes, shock, etc.Type: GrantFiled: July 29, 2004Date of Patent: March 7, 2006Assignee: Nokia CorporationInventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 7008940Abstract: A compound represented by the formula (I): or a salt thereof exhibits excellent inhibitory activity of lipid peroxidation and is useful as an agent for inhibiting lipoperoxide production, wherein ring A denotes a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, B ring denotes a benzene ring which may be further substituted, C ring denotes a dihydrofuran ring which may be further substituted, and R denotes hydrogen atom or an acyl group.Type: GrantFiled: August 18, 2000Date of Patent: March 7, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigenori Ohkawa, Tadatoshi Hashimoto, Tetsuya Tsukamoto
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Patent number: 6953787Abstract: 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: April 10, 2003Date of Patent: October 11, 2005Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Patent number: 6919329Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.Type: GrantFiled: February 24, 2003Date of Patent: July 19, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Richard Charles Thomas, Toni-Jo Poel, Michael Robert Barbachyn, Mikhail F. Gordeev, Gary W. Luehr, Adam Renslo, Upinder Singh
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Patent number: 6916811Abstract: Disclosed herein are compounds having the structural formula A including pharmaceutically acceptable salts or solvates of said compound, wherein X, Y, Q and R are as defined in the specification; pharmaceutical compositions thereof; methods of treating central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment, and processes for preparing the compound of this invention.Type: GrantFiled: November 26, 2002Date of Patent: July 12, 2005Assignee: Schering CorporationInventors: Craig D. Boyle, Samuel Chackalamannil, William J. Greenlee, Unmesh G. Shah, Yan Xia
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Patent number: 6861420Abstract: The present invention provides compounds of Formula I: wherein X, R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: November 26, 2002Date of Patent: March 1, 2005Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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Patent number: 6855708Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: March 13, 2002Date of Patent: February 15, 2005Assignee: Merck & Co., Inc.Inventors: Linus S. Lin, George Doherty, Shrenik K. Shah, Linda L. Chang, William K. Hagmann, Richard A. Mumford
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Publication number: 20040259765Abstract: Methods for the use of NSAIs in combination with anecortave acetate are disclosed for preventing and treating pathologic ocular angiogenesis and associated edema, retinal edema, PPDR or NPDR.Type: ApplicationFiled: June 14, 2004Publication date: December 23, 2004Inventor: David P. Bingaman
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Publication number: 20040242564Abstract: The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists.Type: ApplicationFiled: July 13, 2004Publication date: December 2, 2004Inventors: Jorg Velker, Hamed Aissaoui, Christoph Binkert, Martine Clozel, Boris Mathys, Claus Mueller, Oliver Nayler, Michael Scherz, Thomas Weller
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Publication number: 20040235821Abstract: The invention relates to thiophene carboxamides of formula (I), wherein R1, R2, R3, A, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: January 22, 2004Publication date: November 25, 2004Inventors: David Griffiths, Carig Johnstone