Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/350)
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Publication number: 20130274468Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: June 12, 2013Publication date: October 17, 2013Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Publication number: 20130267527Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I), in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 13, 2011Publication date: October 10, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
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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: 20130267701Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Publication number: 20130267702Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Patent number: 8552045Abstract: This invention is directed to compounds with the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula 1. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula 1. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula 1. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula 1.Type: GrantFiled: November 18, 2011Date of Patent: October 8, 2013Assignee: H. Lundbeck A/SInventors: Jan Kehler, Jacob Nielsen, Mauro Marigo, John Paul Kilburn, Morten Langgård
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Patent number: 8551996Abstract: Briefly described, embodiments of this disclosure include compounds as described herein, labeled compounds as described herein, pharmaceutical composition including compounds described herein, methods of imaging, method of forming a compound as described herein, and the like. In particular, embodiments of the disclosure include a series of triamino-pyridine derivatives and labeled triamino-pyridine derivatives, methods of synthesizing these compounds, intermediate compounds, methods of treatment using these compounds, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a condition (e.g., corticotropin releasing factor type-1 (CRF1)) and/or related biological events, using triamino-pyridine derivatives, and the like. In addition, the present disclosure includes compositions (e.g., labeled triamino-pyridine derivatives that are ligands for the CRF1 receptor) used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging or SPECT imaging).Type: GrantFiled: March 12, 2010Date of Patent: October 8, 2013Assignee: Emory UniversityInventors: Jeff Stehouwer, Mark Goodman, Clint Kilts, Charles Nemeroff
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Publication number: 20130261081Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).Type: ApplicationFiled: September 12, 2011Publication date: October 3, 2013Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
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Publication number: 20130261115Abstract: The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias.Type: ApplicationFiled: May 30, 2013Publication date: October 3, 2013Inventors: Stephan SIEGEL, Andreas WILMEN, Susanne RÖHRIG, Niels SVENSTRUP, Mark Jean GNOTH, Stefan HEITMEIER, Ulrich RESTER, Adrian TERSTEEGEN, Michael GERISCH
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Publication number: 20130261306Abstract: A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.Type: ApplicationFiled: May 23, 2013Publication date: October 3, 2013Applicant: OSI Pharmaceuticals, LLCInventors: Yunyu Mao, Kristen Michelle Mulvihill, Josef A. Rechka, Paula A. Tavares-Greco
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Patent number: 8546394Abstract: Novel compounds are provided which are 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L are defined herein and Z is selected from the following bicyclic heteroaryl groups: (a), (b), (c), (d).Type: GrantFiled: April 16, 2008Date of Patent: October 1, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Jun Li, James J. Li, Stephen P. O'Connor, Haixia Wang, Lawrence J. Kennedy, Jeffrey A. Robl, Lawrence G. Hamann
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Patent number: 8546568Abstract: There has been a need for coelenterazine analogs that exhibit luminescence properties different from those of known coelenterazine analogs. The present invention provides the compound represented by general formula (1).Type: GrantFiled: February 8, 2010Date of Patent: October 1, 2013Assignees: JNC Corporation, Tokyo Institute of TechnologyInventors: Satoshi Inouye, Yuiko Sahara, Rie Iimori, Takamitsu Hosoya
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Patent number: 8546387Abstract: The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.Type: GrantFiled: April 28, 2012Date of Patent: October 1, 2013Assignees: Cancer Research Technology Limited, Institute of Cancer Research: Royal Cancer HospitalInventors: Caroline Joy Springer, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Richard Marais, Bartholomeus Marinus Josephus Marie Suijkerbuijk, Alfonso Zambon, Arnaud Nourry, Delphine Menard
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Publication number: 20130253186Abstract: Heteroaryloxyheterocyclyl compounds, and 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, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 10, 2013Publication date: September 26, 2013Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
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Patent number: 8541416Abstract: L-malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl) carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.Type: GrantFiled: May 11, 2012Date of Patent: September 24, 2013Assignee: Sunovion Pharmaceuticals Inc.Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
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Publication number: 20130245025Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 3, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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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: 20130245254Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.Type: ApplicationFiled: April 30, 2013Publication date: September 19, 2013Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Gingsee Lee, Garrick Packard, Jingjing Zhao, Patrick Anthony Jokiel, Deborah Mortensen, Jennifer Riggs, Juan Antonio Gamboa, Marie Georges Beauchamps, Matthew Michael Kreilein, Mohit Atul Kothare, Sophie Perrin-Ninkovic, Philip Pye, William Wei-Hwa Leong, Jan Elsner, Anusuya Choudhury
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Publication number: 20130245001Abstract: The present invention relates to salts, hydrates, and polymorphs of bicyclic heteroaryl compounds, and pharmaceutical compositions thereof, which may be useful as inhibitors of H4R for the treatment or prevention of diseases including allergic rhinitis.Type: ApplicationFiled: September 7, 2012Publication date: September 19, 2013Applicant: KALYPSYS, INC.Inventors: Pingyun Chen, Stephen A.R. Carino, Ricky Wayne Couch, Daniel S. Kinder, Beth A. Norton
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Publication number: 20130245264Abstract: The object of the present invention is to provide a compound which is useful as a production intermediate of pyrazine carboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazine carboxamide. The present invention provides a pyrazino[2,3-d]isoxazole derivative represented by the formula (I): wherein X represents a halogen atom, a hydroxyl group or a sulfamoyloxy group, and Y represents —C(?O)R or —CN; wherein R represents a hydrogen atom, an alkoxy group an aryloxy group, an alkyl group, an aryl group or an amino group.Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Applicants: TOYAMA CHEMICAL CO., LTD., FUJIFILM CorporationInventors: Kouki NAKAMURA, Takeshi MURAKAMI, Hiroyuki NAITOU, Naoyuki HANAKI, Katsuyuki WATANABE
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Patent number: 8536332Abstract: Method of modulating ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and/or SAPK signal transduction pathway with a pyrido[2,3-b]pyrazine of formula (Ia).Type: GrantFiled: April 25, 2012Date of Patent: September 17, 2013Assignee: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Tilmann Schuster, Eckhard Claus
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Publication number: 20130237520Abstract: 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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Publication number: 20130231330Abstract: 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 12, 2013Publication date: September 5, 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
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Publication number: 20130231337Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 13, 2013Publication date: September 5, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Publication number: 20130225594Abstract: The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives).Type: ApplicationFiled: November 11, 2011Publication date: August 29, 2013Inventors: Mark Craighead, Ronald Palin, Neil Murray, Derek Lindsay
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Publication number: 20130225568Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis.Type: ApplicationFiled: July 29, 2011Publication date: August 29, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Lars Burgdorf, Melanie Schultz, Carl Deutsch, Horacio Comas, Dominique Swinnen, Vincent Pomel, Pascale Gaillard, Brian Hodous
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Publication number: 20130225552Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and 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, Huntington's Disease, and the like.Type: ApplicationFiled: February 28, 2013Publication date: August 29, 2013Applicant: AMGEN INC.Inventor: Amgen Inc.
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Patent number: 8518945Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X? and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: March 4, 2011Date of Patent: August 27, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
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Patent number: 8518946Abstract: Pharmaceutically acceptable salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed. Of the many acceptable salts, one example is the following.Type: GrantFiled: September 2, 2011Date of Patent: August 27, 2013Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.Inventors: Peng Cho Tang, Piaoyang Sun, Fanglong Yang, Jindong Liang, Guangyuan Shen, Yang Wang, Jiang Fan
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Publication number: 20130217951Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: October 12, 2011Publication date: August 22, 2013Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Margarita Wucherer-Plietker, Thomas J.J. Mueller, Eugen Merkul
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Patent number: 8513248Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis or neurodegenerative disorders.Type: GrantFiled: April 28, 2010Date of Patent: August 20, 2013Assignee: Glaxo Group LimitedInventors: David Kenneth Dean, Jorge Munoz-Muriedas, Mairi Sime, Jon Graham Anthony Steadman, Rachel Elizabeth Anne Thewlis, Giancarlo Trani, Ian David Wall, Daryl Simon Walter
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Patent number: 8513411Abstract: Tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), their preparation methods, pharmaceutical compositions containing the derivatives and uses thereof as medicaments, especially as dipeptidyl peptidase IV inhibitors, wherein the substituents of formula (I) are defined as same as the description.Type: GrantFiled: May 3, 2012Date of Patent: August 20, 2013Assignee: Jiangsu Hengrui Medicine Co., Ltd.Inventors: Peng Cho Tang, Fanglong Yang, Jiang Fan, Hu Feng, Yang Wang, Tao Yang
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Publication number: 20130210818Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: February 14, 2012Publication date: August 15, 2013Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
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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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Publication number: 20130210815Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which A, R1, R3 and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: May 27, 2011Publication date: August 15, 2013Applicant: Bayer Intellectual Property GmbHInventors: Ulrich Klar, Marcus Koppitz, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister, William Scott
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Publication number: 20130210816Abstract: The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined herein. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and methods of using the compound of Formula (I) to treat microbial infections.Type: ApplicationFiled: July 28, 2011Publication date: August 15, 2013Inventors: Tin-Yau Chan, Henry M. Vaccaro
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Publication number: 20130210802Abstract: Certain imidazopyridines (I) 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: March 11, 2011Publication date: August 15, 2013Applicant: Gilead Connecticut, IncInventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
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Publication number: 20130209400Abstract: New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: February 18, 2011Publication date: August 15, 2013Inventors: Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Paul Robert Eastwood, Jacob Gonzalez Rodrigues, Victor Giulio Matassa
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Patent number: 8507478Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is alkoxy or halogen; U and V each independently are CH or N; is a bond or is absent; W is CH or N or, when is absent, W is CH2 or NH, with the proviso that U, V and W are not all N; A is a bond or CH2; R2 is H or, provided A is CH2, may also be OH; m and n each independently are 0 or 1; D is CH2 or a bond; G represents a phenyl group substituted once or twice in the meta and/or para position(s) by substituents selected from alkyl, (C1-C3)alkoxy and halogen, or G is a group G1 or G2 wherein Z1, Z2 and Z3 may each represent CH or N; X is N or CH and Q is O or S; it being understood that if m and n each are 0, then A is CH2; and salts of such compounds.Type: GrantFiled: October 9, 2009Date of Patent: August 13, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8507676Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: GrantFiled: August 6, 2012Date of Patent: August 13, 2013Assignee: Novartis AGInventors: Miao Dai, Xingnian Fu, Feng He, Lei Jiang, Yue Li, Fang Liang, Lei Liu, Yuan Mi, Yao-Chang Xu, Guoliang Xun, Xiaoxia Yan, Zhengtian Yu, Ji Yue Zhang
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Patent number: 8507492Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: GrantFiled: November 14, 2011Date of Patent: August 13, 2013Assignee: Signal Pharmaceuticals, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Fultz, Rama K. Narla, Sabita Sankar, Jan Elsner
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Patent number: 8507486Abstract: 1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2.3-b]pyrazine-6-yl]thiourea which HAS activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases.Type: GrantFiled: April 25, 2012Date of Patent: August 13, 2013Assignee: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Tilmann Schuster, Eckhard Claus
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Patent number: 8507487Abstract: Provided are certain triazolopyridines and triazolopyrazines of Formula 1. wherein X, Y, R1, R2, R3, R4 and R5 have any of the meanings described herein; processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of cell proliferative disorders.Type: GrantFiled: April 10, 2012Date of Patent: August 13, 2013Assignee: Hutchison Medipharma LimitedInventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
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Publication number: 20130203755Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.Type: ApplicationFiled: May 24, 2011Publication date: August 8, 2013Applicant: UNIVERSITY OF ROCHESTERInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
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Publication number: 20130203987Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventor: Rigel Pharmaceuticals, Inc.
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Publication number: 20130203727Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).Type: ApplicationFiled: July 1, 2011Publication date: August 8, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
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Patent number: 8501795Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: December 15, 2010Date of Patent: August 6, 2013Assignee: H. Lundbeck A/SInventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
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Patent number: 8501946Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.Type: GrantFiled: April 28, 2010Date of Patent: August 6, 2013Assignee: Glaxo Group LimitedInventors: David Kenneth Dean, Jorge Munoz-Muriedas, Mairi Sime, Jon Graham Anthony Steadman, Rachel Elizabeth Anne Thewlis, Giancarlo Trani, Daryl Simon Walter
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Patent number: 8501797Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: December 15, 2010Date of Patent: August 6, 2013Assignee: H. Lundbeck A/SInventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
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Publication number: 20130195848Abstract: The present invention relates to imidazopyrazine compounds of general Formula (I): in which X, R1, R2, R3a, R3b, R4a, R4b, R4C, and R4D are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: March 16, 2011Publication date: August 1, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Klar, Marcus Koppitz, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister, Stefan Prechtl, Duy Nguyen, William Scott