Additional Nitrogen Containing Hetero Ring Attached Directly Or Indirectly To The Seven-membered Hetero Ring By Nonionic Bonding Patents (Class 514/211.15)
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Publication number: 20140073621Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 22, 2013Publication date: March 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Siegfried SCHNEIDER, Dirk KESSLER, Lars van der VEEN, Tobias WUNBERG
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Publication number: 20140066428Abstract: The present invention relates to compounds defined by formula I wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.Type: ApplicationFiled: November 5, 2013Publication date: March 6, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan-Georg MUELLER, Christopher John BROWN, Alexander HEIFETZ, Bernd NOSSE, Juergen PRESTLE, Natacha PREVOST, Klaus RUDOLF, Stefan SCHEUERER, Marcus SCHINDLER, Dirk STENKAMP, Leo THOMAS, Heather TYE
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Patent number: 8664214Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I and variables defined herein.Type: GrantFiled: March 25, 2011Date of Patent: March 4, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker, Jayne Froggett
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Publication number: 20140057894Abstract: Disclosed herein is a compound of Formula I: wherein X, R1, R2, and R3 are as defend herein, or a pharmaceutically acceptable salt thereof to allow the drug to penetrate the cell membrane; or a prodrug, or the compound is labeled with a detectable label or an affinity tag thereof. Also disclosed is a pharmaceutical composition, a method of treating a disorder mediated by melanocortin-4 receptors, and a method of treating obesity using the compounds described.Type: ApplicationFiled: January 26, 2012Publication date: February 27, 2014Applicant: Universite De MontrealInventors: Michel Bouvier, Anne Marinier, Rejean Ruel, Patricia René, Yves Chantigny, Philippe Dagneau, Stéphane Gingras
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Publication number: 20140057898Abstract: The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.Type: ApplicationFiled: November 4, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin Friedrich STEFANIC, Frank HILBERG, Gerd MUNZERT, Flavio SOLCA, Anke BAUM, Jacobus C.A. van MEEL
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Patent number: 8658635Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: February 25, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20140045822Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: ApplicationFiled: July 3, 2013Publication date: February 13, 2014Applicant: UNIVERSITY HEALTH NETWORKInventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
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Publication number: 20140045823Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr1, (Het)Ar2 and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: July 31, 2013Publication date: February 13, 2014Applicants: Neurocrine Biosciences, Inc., Boehringer Ingelheim International GmbHInventors: Bernd NOSSE, Matthias ECKHARDT, Frank HIMMELSBACH, Elke LANGKOPF, Neil J. ASHWEEK, Nicole HARRIOTT
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Publication number: 20140045820Abstract: This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.Type: ApplicationFiled: October 22, 2013Publication date: February 13, 2014Applicant: Hoffmann-La Roche Inc.Inventors: David Banner, Wolfgang Guba, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Didier Rombach, Thomas Woltering, Wolfgang Wostl
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Publication number: 20140038938Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Mario JESKE, Ingo FLAMME, Friederike STOLL, Hartmut BECK, Metin AKBABA
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Publication number: 20140031339Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1, A2, L1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 16, 2013Publication date: January 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael Jason BURKE, Thomas Martin KIRRANE, JR., Chuk Chui MAN, Daniel Richard MARSHALL, Anil Kumar PADYANA, Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Roger John SNOW, Ronald John SORCEK, Hidenori TAKAHASHI, Steven John TAYLOR, Michael Robert TURNER, Erick Richard Roush YOUNG, Qiang ZHANG, Yunlong ZHANG, Renee M. ZINDELL
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Publication number: 20140031330Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: July 11, 2013Publication date: January 30, 2014Inventors: Monique Bodil van Niel, Benjamin Fauber, Simon Gaines, Alberto Gobbi, Olivier Rene, David Vesey, Stuart Ward
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Publication number: 20140031340Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I); wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X and Y of Formula (I) are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas (II) and sub-formula embodiments of Formula (I) and (II), intermediates and processes and methods useful for the preparation of compounds of Formulas (I)-(II).Type: ApplicationFiled: February 6, 2012Publication date: January 30, 2014Applicant: AMGEN INC.Inventors: Thomas Dineen, Matthew Weiss, Vinod F. Patel, Xiao Mai Zheng, Ryan White
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Patent number: 8637500Abstract: Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: December 16, 2009Date of Patent: January 28, 2014Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Ning Chen, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Essa Hu Harrington, Matthew R. Kaller, Roxanne K. Kunz, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Aaron C. Siegmund, Guomin Yao
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Patent number: 8633183Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: January 24, 2011Date of Patent: January 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Siegfried Schneider, Dirk Kessler, Lars van der Veen, Tobias Wunberg
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Publication number: 20140018343Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Patent number: 8623861Abstract: The present invention relates to a method of treating demyelination diseases, such as multiple sclerosis, comprising administration of an atypical antipsychotic drug, such as quetiapine or an analog thereof, to a subject in need thereof.Type: GrantFiled: November 5, 2007Date of Patent: January 7, 2014Inventor: Xin-Min Li
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Publication number: 20130345192Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.Type: ApplicationFiled: October 28, 2011Publication date: December 26, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
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Publication number: 20130338139Abstract: Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.Type: ApplicationFiled: June 18, 2013Publication date: December 19, 2013Inventors: Amy Allan, Bryan Branstetter, James Breitenbucher, Brian Dyck, Tawfik Gharbaoui, Laurent Gomez, Andrew Richard Hudson, Tami Jo Marrone, Troy Vickers, Michael I. Weinhouse
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Publication number: 20130338142Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.Type: ApplicationFiled: June 14, 2013Publication date: December 19, 2013Inventors: Peter A. BLOMGREN, Kevin S. CURRIE, Randall HALCOMB, Jeffrey E. KROPF, Seung H. LEE, Jiayao LI, Jennifer R. LO, Scott A. MITCHELL, Aaron SCHMITT, Qiaoyin WU, Jin-Min XIONG, Jianjun XU, Zhongdong ZHAO, Jayaraman CHANDRASEKHAR, Eric LANSDON
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Publication number: 20130324518Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: July 26, 2013Publication date: December 5, 2013Applicant: Celgene CorporationInventors: Hon-Wah MAN, Roger Shen-Chu CHEN, Weihong ZHANG
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Publication number: 20130324517Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: ApplicationFiled: July 24, 2013Publication date: December 5, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Christoph HOENKE, Thomas TRIESELMANN, Patrick TIELMANN, Stefan SCHEUERER, Silke HOBBIE, Frank BUETTNER
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Publication number: 20130324516Abstract: The invention provides novel compounds having the general formula: wherein A, R1, R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Huifen Chen, Terry Crawford, Seth F. Harris, Steven R. Magnuson, Chudi Ndubaku, Lan Wang
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Patent number: 8598157Abstract: 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.Type: GrantFiled: January 24, 2012Date of Patent: December 3, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Tobias Wunberg, Oliver Kraemer, Lars van der Veer
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Patent number: 8591943Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.Type: GrantFiled: April 8, 2010Date of Patent: November 26, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Yongqi Deng, Binyuan Sun, Hongbo Zeng, Matthew Richards, Gerald W. Shipps, Jr., Cliff C. Cheng, Yinyan Zhao, Andrew McRiner, Zhaoyang Meng, Yang Nan, Mehul F. Patel, Iwona E. Wrona, Panduranga Adulla Reddy, Brian M. Eklov, Shuyi Tang, Duan Liu, Amit K. Mandal, Lianyun Zhao, M. Arshad Siddiqui
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Publication number: 20130303516Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.Type: ApplicationFiled: January 25, 2012Publication date: November 14, 2013Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
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Publication number: 20130303507Abstract: The present invention provides a compound of formula (II): where R1 is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancers and other conditions described herein.Type: ApplicationFiled: January 20, 2012Publication date: November 14, 2013Applicant: Novartis AGInventors: William R. Antonios-McCrea, Paul A. Barsanti, Cheng Hu, Xianming Jin, Eric Martin, Yue Pan, Xiaodong Lin, Keith B. Pfister, Paul A. Renhowe, Martin Sendzik, James Sutton, Lifeng Wan
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Patent number: 8580778Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.Type: GrantFiled: October 12, 2011Date of Patent: November 12, 2013Assignee: Bayer Intellectual Property GmbHInventors: Mario Jeske, Ingo Flamme, Friederike Stoll, Hartmut Beck, Metin Akbaba
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Patent number: 8580772Abstract: This invention generally relates to a method for promoting growth and increasing feed utilization efficiency in animals, and, more specifically, to combinations comprising zilpaterol (and salts thereof) and melengestrol acetate. Included within this invention are treatment methods comprising the administration of such combinations to animals, compositions comprising such combinations, uses of such combinations to prepare medicaments, and kits for using such combinations.Type: GrantFiled: December 4, 2008Date of Patent: November 12, 2013Assignee: Intervet Inc.Inventors: Mary Irene Wray, Damon Edward Bradley, Melissa A. Petersen, Auddie Sharp, Celia Shelton, Jayden Lloyd Montgomery
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Publication number: 20130281430Abstract: The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.Type: ApplicationFiled: April 17, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Georg DAHMANN, Horst DOLLINGER, Christian GNAMM, Dennis FIEGEN, Matthias HOFFMANN, Jasna KLICIC, David James LAMB, Andreas SCHNAPP
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Publication number: 20130281359Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: ApplicationFiled: June 14, 2013Publication date: October 24, 2013Inventors: Samarendra N. MAITI, Dai Nguyen, Jehangir Khan, Rong Ling
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Publication number: 20130267496Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: May 23, 2013Publication date: October 10, 2013Applicant: GILEAD CONNECTICUT, INC.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
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Publication number: 20130267494Abstract: Provided is a compound having a monoamine reuptake inhibitory activity, which is represented by the formula (I) wherein ring A is an optionally substituted 6-membered aromatic ring, ring B is the substituents on ring A are optionally bonded to form, together with ring A, an optionally substituted 9- or 10-membered aromatic fused ring, and other symbols are as defined in the specification, or a salt thereof.Type: ApplicationFiled: October 5, 2011Publication date: October 10, 2013Inventors: Yuji Ishichi, Masami Yamada, Taku Kamei, Ikuo Fujimori, Yoshihisa Nakada, Tomoya Yukawa, Nobuki Sakauchi, Yusuke Ohba, Tetsuya Tsukamoto
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Patent number: 8551981Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: October 7, 2011Date of Patent: October 8, 2013Assignee: AbbVie Inc.Inventors: David J. Calderwood, Noel S. Wilson, Philip Cox, Michael Z. Hoemann, Bruce Clapham, Anil Vasudevan, Clara I. Villamil, Bin Li, Gagandeep Somal, Kelly D. Mullen
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Publication number: 20130261104Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.Type: ApplicationFiled: May 9, 2013Publication date: October 3, 2013Applicant: Genentech, Inc.Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum MacLeod, Karen Williams
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Patent number: 8546374Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: GrantFiled: July 9, 2012Date of Patent: October 1, 2013Assignee: Abbvie Inc.Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
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Publication number: 20130252937Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: March 14, 2013Publication date: September 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
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Publication number: 20130245005Abstract: Compounds of Formula (I): able to inhibit kinase activity, in particular Phosphatidylinositol 3-Kinases activity. The disclosure also relates to the use of compounds of Formula (I) for treatment of pathological conditions associated to alterations in Phosphatidylinositol 3-Kinases activity.Type: ApplicationFiled: November 28, 2011Publication date: September 19, 2013Applicants: UNIVERSITA DEGLI STUDI DEL PIEMONTE ORIENTALE "AMEDEO AVOGADRO", UNIVERSITA DEGLI STUDI DI TORINOInventors: Giovanni Sorba, Gian Cesare Tron, Ubaldina Galli, Alberto Massarotti, Emilio Hirsch, Elisa Ciraolo, Tracey Pirali
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Publication number: 20130244996Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael J. BURKE, Suresh R. KAPADIA, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Hossein RAZAVI, Sonia RODRIGUEZ, Anjan SAHA, Robert SIBLEY, Lana Louise SMITH-KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, Jiang-Ping WU, Erick Richard Roush YOUNG, Qiang ZHANG, Qing ZHANG, Renee M. ZINDELL
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Publication number: 20130237521Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: April 23, 2013Publication date: September 12, 2013Applicant: GILEAD CONNECTICUT, INC.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
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Patent number: 8524699Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: GrantFiled: October 26, 2007Date of Patent: September 3, 2013Assignee: Bayer Intellectual Property GmbHInventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
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Publication number: 20130225554Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: ApplicationFiled: November 30, 2012Publication date: August 29, 2013Applicant: NAEJA PHARMACEUTICAL INC.Inventor: Naeja Pharmaceutical Inc.
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Publication number: 20130225555Abstract: The present invention provides compounds of formula (I) wherein Ra, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: March 14, 2013Publication date: August 29, 2013Applicants: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca ABInventors: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
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Patent number: 8518934Abstract: The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: June 11, 2009Date of Patent: August 27, 2013Assignee: Shonogi & Co., Ltd.Inventor: Hidenori Mikamiyama
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Publication number: 20130210768Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.Type: ApplicationFiled: June 6, 2011Publication date: August 15, 2013Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif
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Patent number: 8507471Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: GrantFiled: June 4, 2008Date of Patent: August 13, 2013Assignee: IRM LLCInventors: Christine Dierks, Markus Warmuth, Xu Wu
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Publication number: 20130203732Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicant: GENENTECH, INC.Inventor: GENENTECH, INC.
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Publication number: 20130203730Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
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Publication number: 20130203592Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: January 22, 2013Publication date: August 8, 2013Applicant: Dow AgroSciences LLCInventor: Dow AgroSciences LLC
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Publication number: 20130203593Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: January 23, 2013Publication date: August 8, 2013Applicant: Dow AgroSciences LLCInventor: Dow AgroSciences LLC