Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/210.21)
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Publication number: 20130018036Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: September 12, 2012Publication date: January 17, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea LOMBARDI BORGIA, Maria MENICHINCHERI, Paolo ORSINI, Achille PANZERI, Ettore PERRONE, Ermes VANOTTI, Marcella NESI, Chiara MARCHIONNI
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Publication number: 20130017273Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: June 22, 2012Publication date: January 17, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Simon Everitt, Michael Paul Mortimore, Jean-Damien Charrier, Somhairle MacCormick, Pierre-Henri Storck, Ronald Knegtel, Joanne Pinder, Steven John Durrant
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Publication number: 20130018039Abstract: Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.Type: ApplicationFiled: March 31, 2011Publication date: January 17, 2013Inventors: Vera Q. Bodmer, Linda N. Casillas, Michael P. DeMartino, Philip A. Harris, Bryan W. King, Ami Lakdawala Shah, Lara Kathryn Leister, Joshi M. Ramanjulu, Joseph J. Romano, Gren Z. Wang, Matthew A. Wilson, David Duff Wisnoski
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Publication number: 20130018038Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 23, 2011Publication date: January 17, 2013Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20130018035Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: June 22, 2012Publication date: January 17, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Somhairle MacCormick, Pierre-Henri Storck, Michael Paul Mortimore, Jean-Damien Charrier, Ronald Knegtel, Stephen Clinton Young, Joanne Pinder, Steven John Durrant
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Publication number: 20130018037Abstract: Spirocyclic amide derivatives of formula I wherein ArCH2CH2NH— represents a ?-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Inventors: Lilian Alcaraz, Andrew Bailey, Nicholas Kindon
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Patent number: 8354399Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: GrantFiled: December 15, 2009Date of Patent: January 15, 2013Assignee: Nerviano Medical Sciences S.R.L.Inventors: Maria Menichincheri, Jay Aaron Bertrand, Chiara Marchionni, Marcella Nesi, Paolo Orsini, Achille Panzeri
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Publication number: 20130012492Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 29, 2012Publication date: January 10, 2013Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20130012488Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. 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: August 7, 2012Publication date: January 10, 2013Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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Publication number: 20130012493Abstract: The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: He Zhao, Ping Chen, Peishan Lin, Peng Dai, Jason Louis Davis, Duane E. DeMong, Michael W. Miller, Xing Dai, Michael K. Wong, Brian J. Lavey, Wensheng Yu, Guowei Zhou, Andrew W. Stamford, Joseph A. Kozlowski, William J. Greenlee
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Patent number: 8349825Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: October 26, 2010Date of Patent: January 8, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Dawn M. Mampreian, Joey L. Methot, Thomas Miller, Paul Tempest, Anna A. Zabierek
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Patent number: 8349826Abstract: The invention relates to compounds of Formula (I) wherein U, V, W, R1, R1b, A and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament for the prevention or treatment of a bacterial infection.Type: GrantFiled: February 20, 2009Date of Patent: January 8, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20130005706Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20130005687Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
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Publication number: 20130005705Abstract: The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: June 27, 2012Publication date: January 3, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob
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Publication number: 20130005707Abstract: Provided herein are Heteroaryl Compounds of formula (I): wherein R1 and R2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Inventors: Sogole Bahmanyar, R.J. Bates, Kate Blease, Andrew Antony Calabrese, Thomas Oran Daniel, Mercedes Delgado, Jan Elsner, Paul Erdman, Bruce Fahr, Gregory Ferguson, Branden Lee, Lisa Nadolny, Garrick Packard, Patrick Papa, Veronique Plantevin-Krenitsky, Jennifer Riggs, Patricia Rohane, Sabita Sankar, John Sapienza, Yoshitaka Satoh, Victor Sloan, Randall Stevens, Lida Tehrani, Jayashree Tikhe, Eduardo Torres, Andrew Wallace, Brandon Wade Whitefield, Jingjing Zhao
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Publication number: 20130005675Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
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Patent number: 8343954Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.Type: GrantFiled: July 27, 2011Date of Patent: January 1, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Publication number: 20120329777Abstract: The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.Type: ApplicationFiled: August 31, 2012Publication date: December 27, 2012Inventors: Michelle Marie Claffey, Christopher John Helal, Patrick Robert Verhoest
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Publication number: 20120329776Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: November 4, 2011Publication date: December 27, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson
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Publication number: 20120329778Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.Type: ApplicationFiled: September 5, 2012Publication date: December 27, 2012Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Thomas METZ, Flavio SOLCA, Birgit JUNG, Anke BAUM
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Publication number: 20120329774Abstract: A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: ApplicationFiled: September 5, 2012Publication date: December 27, 2012Applicant: UCB Pharma S.A.Inventors: Clive Martin Hutchings, Sarah Catherine Archibald, Daniel Christopher Brookings, Jeremy Martin Davis, James Andrew Johnson, Barry John Langham, Judi Charlotte Neuss
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Publication number: 20120322788Abstract: The present invention relates to spirocyclic amide derivatives of the formula I, pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: April 2, 2012Publication date: December 20, 2012Inventors: Lilian Alcaraz, Andrew Bailey, Richard James Bull, Timothy Johnson, Nicholas David Kindon, Andrew Stuart Lister, Andrew James Robbins, Michael John Stocks, Barry John Teobald
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Publication number: 20120322785Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.Type: ApplicationFiled: December 14, 2011Publication date: December 20, 2012Applicant: Genentech, Inc.Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel Kintz, Hans Edward Purkey
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Publication number: 20120316152Abstract: A method for the treatment or prevention in a mammal of a disease associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase comprising administering to the mammal in need thereof at least one compound of the formula (I)Type: ApplicationFiled: August 15, 2012Publication date: December 13, 2012Applicant: SANOFIInventors: Oliver Plettenburg, Armin Hofmeister, Joachim Brendel, Matthias Löhn
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Patent number: 8329686Abstract: Novel isatin analogues, including isatin analogues comprising Michael Acceptors (IMAs) are disclosed. Further disclosed are methods of synthesis of the isatin analogues, and uses of the analogues, including inhibition of caspase-3 and caspase-7, and in vivo imaging of apoptosis by Positron emission tomography (PET) or Single Photon Emission Computed Tomography (SPECT).Type: GrantFiled: August 29, 2007Date of Patent: December 11, 2012Assignee: Washington UniversityInventors: Robert H. Mach, Michael Welch, Wenhua Chu, Justin Rothfuss
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Publication number: 20120309741Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.Type: ApplicationFiled: August 16, 2012Publication date: December 6, 2012Inventors: Pascal FURET, Diana GRAUS PORTA, Vito GUAGNANO
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Publication number: 20120309698Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: December 6, 2011Publication date: December 6, 2012Inventors: Yasutsugu Ueda, Timothy P. Connolly, Barry L. Johnson, Chen Li, B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Margaret E. Sorenson, Michael A. Walker, Michael S. Bowsher, Rongti Li
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Publication number: 20120309739Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: November 3, 2010Publication date: December 6, 2012Applicant: ALMAC DISCOVERY LIMITEDInventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
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Publication number: 20120309740Abstract: Pharmaceutical compositions having improved dissolution profiles for drugs therein is disclosed.Type: ApplicationFiled: August 14, 2012Publication date: December 6, 2012Applicant: ABBOTT LABORATORIESInventors: Huailiang WU, Geoff G.Z. ZHANG
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Patent number: 8324200Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: GrantFiled: January 22, 2010Date of Patent: December 4, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Sambaiah Thota, Rose Yen
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Publication number: 20120301464Abstract: Methods, kits, and compositions for treating dry eye disorders and other related eye diseases are provided, wherein the methods, kits, and compositions utilize a JAK inhibitor.Type: ApplicationFiled: August 1, 2012Publication date: November 29, 2012Applicant: INCYTE CORPORATIONInventors: Paul A. Friedman, Jordan S. Fridman, Monica E. Luchi, William V. Williams
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Publication number: 20120302524Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).Type: ApplicationFiled: December 28, 2010Publication date: November 29, 2012Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTUREInventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
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Publication number: 20120302547Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I) wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.Type: ApplicationFiled: August 8, 2012Publication date: November 29, 2012Applicant: ELI LILLY AND COMPANYInventors: Macklin Brian Arnold, Yen Dao, Kevin Matthew Gardinier, David Joseph Garmene, Steven James Green, Erik James Hembre, Jianliang Lu
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Publication number: 20120302545Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.Type: ApplicationFiled: August 7, 2012Publication date: November 29, 2012Applicant: Exelixis, Inc.Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
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Patent number: 8318718Abstract: Pyridine and pyrimidine 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, bipolar disorder, obsessive-compulsive disorder, and the like.Type: GrantFiled: November 16, 2009Date of Patent: November 27, 2012Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
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Patent number: 8318702Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.Type: GrantFiled: July 4, 2008Date of Patent: November 27, 2012Assignee: Astellas Pharma Inc.Inventors: Yutaka Kondoh, Kazuhiko Iikubo, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani, Itsuro Shimada, Takahiro Matsuya, Kazuo Kurosawa, Akio Kamikawa, Hiroyuki Mano
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Publication number: 20120295885Abstract: This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: May 16, 2012Publication date: November 22, 2012Inventors: Roland Joseph Billedeau, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens, Yimin Qian, Sung-Sau So, Kshitij C. Thakkar, Jutta Wanner
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Publication number: 20120294930Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.Type: ApplicationFiled: February 23, 2012Publication date: November 22, 2012Applicant: Intellikine LLCInventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
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Publication number: 20120295883Abstract: The present invention relates to substituted pyrazolopyridine compounds, and pharmaceutically acceptable salts or esters thereof. The present invention further relates to therapeutic uses of pharmaceutical compositions comprising the substituted pyrazolopyridine compounds, for example, in cancer and neurodegenerative diseases.Type: ApplicationFiled: September 21, 2011Publication date: November 22, 2012Applicants: GENENTECH, INC., MEDICAL RESEARCH COUNCIL TECHNOLOGYInventors: Bryan K. CHAN, Huifen CHEN, Anthony ESTRADA, Daniel SHORE, Zachary SWEENEY, Edward Giles MCIVER
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Patent number: 8314098Abstract: The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.Type: GrantFiled: June 27, 2011Date of Patent: November 20, 2012Assignee: Ajinomoto Co., Inc.Inventors: Takashi Yamamoto, Ayatoshi Andou, Nobuhiko Hayakawa, Masatsugu Noguchi, Kanna Kuribayashi, Agung Eviryanti, Ryohei Yokoyama, Shunsuke Fukuda, Toshihiko Sugiura, Shunsuke Kageyama, Yoichiro Shima, Misato Noguchi
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Patent number: 8314121Abstract: The present invention relates to imidazolone derivatives of formula (I) to methods of preparing such derivatives, intermediates thereto, pharmaceutical compositions comprising such derivatives, and methods of inhibiting protein kinase, and methods of treatment comprising administration of such derivatives.Type: GrantFiled: March 31, 2009Date of Patent: November 20, 2012Assignee: SanofiInventors: Vincent Leroy, Eric Bacque, Emmanuel Conseiller, Anke Steinmetz, Baptiste Ronan, Jean-Philippe Letallec
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Publication number: 20120289497Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.Type: ApplicationFiled: January 17, 2011Publication date: November 15, 2012Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
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Publication number: 20120289496Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: May 4, 2012Publication date: November 15, 2012Applicant: Rhizen Pharmaceuticals SAInventors: Dhanapalan NAGARATHNAM, Swaroop Kumar V.S. Vakkalanka, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Prashant K. Bhavar
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Publication number: 20120283241Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: July 19, 2012Publication date: November 8, 2012Inventors: Brian E. Fink, Libing Chen, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Andrew James Nation, Yufen Zhao, Litai H. Zhang
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Publication number: 20120283240Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.Type: ApplicationFiled: June 26, 2012Publication date: November 8, 2012Inventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
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Publication number: 20120283238Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: January 10, 2012Publication date: November 8, 2012Applicant: NIMBUS IRIS, INC.Inventors: Donna L. Romero, Matthew David Wessel, Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse
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Publication number: 20120283239Abstract: The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: ApplicationFiled: January 13, 2011Publication date: November 8, 2012Applicant: MSD OSS B.V.Inventors: Jiaqiang Cai, David Jonathan Bennett, Philip Stephen Jones
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Publication number: 20120277209Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are 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, and the like.Type: ApplicationFiled: June 22, 2012Publication date: November 1, 2012Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Matthew P. Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
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Publication number: 20120277205Abstract: The present invention relates to compounds corresponding to formula (I): in which: A represents a divalent aromatic radical; X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R3 represents a hydroxyl or a group —NR7R8; R4 represents a hydrogen atom, a halogen atom, a cyano, a phenyl, a group Alk, a group OAlk or a group —NR9R10; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.Type: ApplicationFiled: September 13, 2011Publication date: November 1, 2012Applicant: SANOFIInventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon