3-benzazepines (including Hydrogenated) Patents (Class 540/594)
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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: 20120283431Abstract: The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.Type: ApplicationFiled: March 22, 2012Publication date: November 8, 2012Inventors: Ulrich Weigl, Frank Porstmann, Christoph Straessler, Lars Ulmer, Ulf Koetz
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Patent number: 8299241Abstract: The present invention provides processes and intermediates for the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and salts thereof which are useful as serotonin-2C (5-HT2C) receptor agonists for the treatment of, for example, obesity.Type: GrantFiled: December 4, 2007Date of Patent: October 30, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Tawfik Gharbaoui, Sagun K. Tandel, You-An Ma, Marlon Carlos, John Robert Fritch
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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: 20120253036Abstract: An agent for treating fibromyalgia containing a 5-HT2C receptor agonist as an active ingredientType: ApplicationFiled: December 10, 2010Publication date: October 4, 2012Inventors: Yukinori Nagakura, Mina Tsukamoto, Tomonari Watabiki
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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: 20120184732Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof, which is useful as an active ingredient of a fungicide for agricultural and horticultural use, having an assured effect and being safely usable.Type: ApplicationFiled: September 22, 2010Publication date: July 19, 2012Inventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Motoaki Sato
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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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Publication number: 20120165519Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: March 6, 2012Publication date: June 28, 2012Applicant: Cephalon, Inc.Inventors: Gulzar Ahmed, Henry Joseph Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Keith S. Learn, Joseph G. Lisko, Rong-qiang Liu, Eugen Mesaros, Karen Milkiewicz, Gregory R. Ott, Jay P. Theroff, Tho V. Thieu, Rabindranath Tripathy, Theodore L. Underiner, Gregory J. Wells, Craig A. Zificsak
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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: 8207331Abstract: 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: February 17, 2010Date of Patent: June 26, 2012Assignee: Glaxo Group LimitedInventors: Mark James Bamford, David Kenneth Dean, Sanjeet Singh Sehmi, David Matthew Wilson, Jason Witherington
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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: 20120135968Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.Type: ApplicationFiled: May 7, 2010Publication date: May 31, 2012Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
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Patent number: 8168782Abstract: The present invention provides processes, methods and intermediates for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, salts, hydrates and crystal forms thereof which are useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.Type: GrantFiled: April 2, 2007Date of Patent: May 1, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Ulrich Weigl, Frank Porstmann, Christoph Straessler, Lars Ulmer, Ulf Koetz
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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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Publication number: 20120053168Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).Type: ApplicationFiled: February 16, 2010Publication date: March 1, 2012Applicant: Targacept, Inc.Inventors: Balwinder Singh Bhatti, Timothy J. Cuthbertson, Anatoly Mazurov, Joseph Pike Mitchener, Julio A. Munoz, Srinivasa V. Murthy, Yunde Xiao, Daniel Yohannes
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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: 20120010185Abstract: 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: September 22, 2011Publication date: January 12, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: 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: 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
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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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Publication number: 20110201805Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.Type: ApplicationFiled: February 15, 2011Publication date: August 18, 2011Applicant: LES LABORATOIRES SERVIERInventors: Jean-Louis Peglion, Pascal Caignard
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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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Publication number: 20110182828Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.Type: ApplicationFiled: December 18, 2008Publication date: July 28, 2011Applicant: Schering CorporationInventors: John C. Anthes, Kevin D. Mccormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Daniel M. Solomon, Phillippa H. Solomon, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar
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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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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: 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