Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/117)
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Publication number: 20130116241Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of 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: October 25, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130116213Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.Type: ApplicationFiled: June 20, 2011Publication date: May 9, 2013Applicant: HANMI SCIENCE CO., LTD.Inventors: Mi Young Cha, Seok Jong Kang, Mi Ra Kim, Ju Yeon Lee, Ji Young Jeon, Myoung Gi Jo, Eun Joo Kwak, Kwang Ok Lee, Tae Hee Ha, Kwee Hyun Suh, Maeng Sup Kim
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Publication number: 20130116233Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of 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: October 29, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, AbbVie Inc.
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Patent number: 8435986Abstract: Compounds of the formula (I), in which X1, X2, X3, X4, X5, R1, R2, R3, R3?, R4, R6 and R7 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: July 16, 2009Date of Patent: May 7, 2013Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Patent number: 8435985Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: GrantFiled: November 30, 2011Date of Patent: May 7, 2013Inventors: Keith Menear, Graeme Cameron Murray Smith, Karine Malagu, Heather Mary Ellen Duggan, Niall Morrison Barr Martin, Frederic Georges Marie Leroux
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Publication number: 20130109661Abstract: The present invention relates to the use of novel compounds of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: October 31, 2012Publication date: May 2, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130109852Abstract: The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.Type: ApplicationFiled: December 12, 2012Publication date: May 2, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130102600Abstract: The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBHInventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
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Publication number: 20130102590Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicant: AbbVie IncInventor: AbbVie Inc.
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Publication number: 20130102587Abstract: Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.Type: ApplicationFiled: March 14, 2011Publication date: April 25, 2013Applicant: PROXIMAGEN LIMITEDInventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
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Publication number: 20130102601Abstract: The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicants: F. HOFFMANN-LA ROCHE LTD, EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL), SAVIRA PHARMACEUTICALS GMBHInventors: F. HOFFMANN-LA ROCHE LTD, SAVIRA PHARMACEUTICALS GMBH, EUROPEAN MOLECULAR BIOLOGY LABORAT
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Patent number: 8426405Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof are disclosed. Also disclosed are methods of treating a viral infection in a subject by administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.Type: GrantFiled: July 2, 2009Date of Patent: April 23, 2013Assignee: Avexa LimitedInventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Thienthong, Nicholas Andrew Vandegraaff, Lisa Jane Winfield
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Publication number: 20130096113Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Ambit Biosciences CorporationInventor: Ambit Biosciences Corporation
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Publication number: 20130096302Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Inventors: Hayley Binch, Daniel Robinson, Damien Fraysse, Andrew Miller
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Publication number: 20130090336Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: December 5, 2012Publication date: April 11, 2013Applicant: YM BIOSCIENCES AUSTRALIA PTY LTDInventor: YM Biosciences Australia Pty Ltd
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N3-HETEROARYL SUBSTITUTED TRIAZOLES AND N5-HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20130090330Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: October 4, 2012Publication date: April 11, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: RIGEL PHARMACEUTICALS, INC. -
Publication number: 20130090335Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: ApplicationFiled: March 30, 2012Publication date: April 11, 2013Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian, Rudi Bao
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Patent number: 8410095Abstract: This invention relates to novel compounds of formula (I): and derivatives thereof useful for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?.Type: GrantFiled: May 20, 2010Date of Patent: April 2, 2013Assignee: GlaxoSmithKline LLCInventors: Hong Lin, Juan I. Luengo, Ralph A. Rivero, Mark James Schulz, Ren Xie, Jin Zeng
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Publication number: 20130079324Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Hengmiao Cheng, Theodore Otto Johnson, JR., John Charles Kath, Kevin Kun-Chin Liu, Elizabeth Ann Lunney, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken, Scott Channing Sutton
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Publication number: 20130079341Abstract: The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.Type: ApplicationFiled: May 23, 2011Publication date: March 28, 2013Inventors: Brigitte Johanna Bernita Folmer, de Adrianus Petrus Antonius Man, Elisabeth Sophia Gernette, Rita Corte Real Goncalves Azevedo, Hemen Ibrahim
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Publication number: 20130072482Abstract: The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment.Type: ApplicationFiled: May 26, 2011Publication date: March 21, 2013Inventors: Beom-Seok Yang, Yong-Zu Kim, Tae-Kyo Park, Sung-Ho Woo, Hyang-Sook Lee, Sun-Young Kim, Jong-Un Cho, Hong-Bum Lee
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Publication number: 20130059834Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: August 31, 2012Publication date: March 7, 2013Inventors: Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
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Publication number: 20130053370Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.Type: ApplicationFiled: January 31, 2011Publication date: February 28, 2013Applicants: HANMI SCIENCE CO., LTD., CATHOLIC UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Jung Beom Son, Seung Hyun Jung, Wha ll Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
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Publication number: 20130053371Abstract: There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: January 24, 2011Publication date: February 28, 2013Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLÓGICAS (CNIO)Inventors: Joaquin Pastor Fernández, Sonia Martinez Gonzalez, Rosa Maria Alvarez Escobar, Antonlo Rodriguez Hergueta, José Ignacio Martin Hernando, Francisco Ramos Lima
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Publication number: 20130045963Abstract: The present invention provides cyclohexyl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: August 17, 2012Publication date: February 21, 2013Applicant: INCYTE CORPORATIONInventors: James D. Rodgers, Argyrios G. Arvanitis
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Publication number: 20130040946Abstract: The invention relates to substituted imidazo- and triazolopyrimidines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of haematological disorders, preferably of leucopenias and neutropenias.Type: ApplicationFiled: September 24, 2012Publication date: February 14, 2013Applicant: Bayer Intellectual Property GmbHInventors: Stephan Siegel, Andreas Wilmen, Susanne Röhrig, Niels Svenstrup, Mark Jean Gnoth, Stefan Heitmeier, Ulrich Rester, Dmitry Zubov, Jochen Strayle, Michael Sperzel
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Patent number: 8372970Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.Type: GrantFiled: October 8, 2010Date of Patent: February 12, 2013Assignee: Afraxis, Inc.Inventors: Benedikt Vollrath, David Campbell, Sergio G. Durón, Warren Wade
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Publication number: 20130035324Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 17, 2010Publication date: February 7, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
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Publication number: 20130035335Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.Type: ApplicationFiled: September 18, 2012Publication date: February 7, 2013Applicant: aFRAXis, Inc.Inventor: aFRAXis, Inc.
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Publication number: 20130034616Abstract: 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: February 7, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Pierre-Henri Storck, Jean-Damien Charrier, Alistair Rutherford, Michael Paul Mortimore, Somhairle MacCormick, Ronald Marcellus Alphonsus Knegtel, Steven John Durrant
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Publication number: 20130035325Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.Type: ApplicationFiled: November 16, 2010Publication date: February 7, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
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Publication number: 20130029969Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.Type: ApplicationFiled: February 16, 2011Publication date: January 31, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Misaki Homma, Toru Miyazaki, Yuya Oguro, Osamu Kurasawa
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Publication number: 20130029981Abstract: The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients.Type: ApplicationFiled: June 18, 2012Publication date: January 31, 2013Applicant: Katholieke Universiteit LeuvenInventors: Sigrid De Keersmaecker, Dirk De Vos, Denis Ermolatev, Hans Steenackers, Erik Van Der Eycken, Jozef Vanderleyden, Bharat S. Savaliya
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Publication number: 20130029983Abstract: The present invention is directed to methods of inhibiting a tauopathy in a patient by administration of a compound of formula I: Novel aminothienopyridazine compounds are also described.Type: ApplicationFiled: September 22, 2010Publication date: January 31, 2013Inventors: Carlo Ballatore, Kurt R. Brunden, Alexander L. Crowe, Donna M. Huryn, Virginia M.Y. Lee, John Q. Trojanowski, Amos B. Smith, III, Ruili Huang, Wenwei Huang, Ronald L. Johnson, Francesco Piscitelli
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Publication number: 20130029974Abstract: There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I).Type: ApplicationFiled: January 21, 2011Publication date: January 31, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Danilo Mirizzi, Sten Christian Orrenius, Paolo Trifirò
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Publication number: 20130029944Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: June 20, 2012Publication date: January 31, 2013Applicant: Portola Pharmaceuticals, Inc.Inventors: Yonghong Song, Qing Xu, Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Anjali Pandey
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Publication number: 20130029984Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130023499Abstract: Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. 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 disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: January 4, 2012Publication date: January 24, 2013Applicant: Gilead Connecticut, Inc.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, David M. ARMISTEAD, Joseph RAKER
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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: 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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Patent number: 8354405Abstract: The invention relates to the 6-cycloamino-3-(pyridin-4-yl)imidazo[I,2-b]pyridazine derivatives corresponding to general formula (I): Wherein R2, R3, R7, R8, A, L and B are as defined herein. Also disclosed are the preparative methods and therapeutic use thereof.Type: GrantFiled: December 24, 2009Date of Patent: January 15, 2013Assignee: SanofiInventors: Antonio Almario Garcia, Matthieu Barrague, Philippe Burnier, Cécile Enguehard, Zhongli Gao, Pascal George, Alain Gueiffier, Adrien Tak Li, Frédéric Puech, Roy Vaz, Qiuxia Zhao
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Publication number: 20130012703Abstract: Disclosed are a 2,4,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,4,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.Type: ApplicationFiled: October 22, 2010Publication date: January 10, 2013Inventors: Tae Bo Sim, Jung Mi Hah, Hwan Geun Choi, Young Jin Ham, Jung Hun Lee, Dong Sik Park, Hwan Kim
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Publication number: 20130012389Abstract: Substituted pyridazines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Applicant: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska-Pianowska, Anja Simon, Ruediger Reingruber, Helmut Kraus, Hans Wolfgang Hoeffken, Thomas Mietzner, Thomas Ehrhardt
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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: 20130005576Abstract: Substituted pyridazines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.Type: ApplicationFiled: March 23, 2011Publication date: January 3, 2013Applicant: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschiel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska-Pianowska, Anja Simon, Ruediger Reingruber, Helmut Kraus, Hans Wolfgang Hoeffken, Thomas Mietzner
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Publication number: 20120329792Abstract: The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.Type: ApplicationFiled: March 8, 2011Publication date: December 27, 2012Inventors: José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James MacDonald, Joaquin Pastor-Fernández, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Greta Constantia Peter Vanhoof
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Patent number: 8338412Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: May 13, 2011Date of Patent: December 25, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco G. Salituro, John P. Duffy, John E. Cochran, Edmund M. Harrington, Mark A. Murcko, Keith P. Wilson, Michael Su, Vincent P. Galullo
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Publication number: 20120323002Abstract: By searching various compounds having an inhibiting activity against IL-12/IL-23 production, the present invention provides a pharmaceutical composition or a therapeutic or preventive agent for diseases related to IL-12/IL-23 excessive production each of which comprises the compound(s) of the present invention. More specifically, the present invention provides an imidazopyridazine compound having an inhibiting activity against IL-12/IL-23 production or pharmaceutically acceptable salts thereof; and a useful pharmaceutical composition or a useful therapeutic or preventive agent for diseases related to IL-12/IL-23 excessive production each of which comprises said compound or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: June 25, 2012Publication date: December 20, 2012Applicant: AJINOMOTO CO., INC.Inventors: Takashi YAMAMOTO, Ayatoshi ANDO, Nobuhiko HAYAKAWA, Masatsugu NOGUCHI, Hikaru NISHIO, Agung EVIRYANTI, Ryohei YOKOYAMA, Shunsuke KAGEYAMA, Kanna KURIBAYASHI
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Publication number: 20120322791Abstract: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.Type: ApplicationFiled: January 18, 2011Publication date: December 20, 2012Inventors: M. Arshad Siddiqui, Yang Nan, Mehul F. Patel, Panduranga Adulla P. Reddy, Umar Faruk Mansoor, Zhaoyang Meng, Lalanthi Dilrukshi Vitharana, Lianyun Zhao, Amit K. Mandal, Duan Liu, Shuyi Tang, Andrew McRiner, David B. Belanger, Patrick J. Curran, Chaoyang Dai, Angie R. Angeles, Liping Yang, Matthew Hersh Daniels