Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
  • Substituted 9H-purin-2-YL compounds, compositions thereof and uses thereof
    Patent number: 8404674
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Grant
    Filed: March 4, 2008
    Date of Patent: March 26, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
  • ANTI-INFLAMMATORY COMPOUND HAVING INHIBITORY ACTIVITY AGAINST MULTIPLE TYROSINE KINASES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
    Publication number: 20130072482
    Abstract: 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: Application
    Filed: May 26, 2011
    Publication date: March 21, 2013
    Inventors: Beom-Seok Yang, Yong-Zu Kim, Tae-Kyo Park, Sung-Ho Woo, Hyang-Sook Lee, Sun-Young Kim, Jong-Un Cho, Hong-Bum Lee
  • MODULATORS OF TOLL-LIKE RECEPTORS
    Publication number: 20130071354
    Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: November 16, 2012
    Publication date: March 21, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • mTOR SELECTIVE KINASE INHIBITORS
    Publication number: 20130072481
    Abstract: The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.
    Type: Application
    Filed: May 18, 2011
    Publication date: March 21, 2013
    Applicant: XCOVERY HOLDING COMPANY, LLC
    Inventor: Congxin Liang
  • Triazolo [4, 5- B] Pyridin Derivatives
    Publication number: 20130065883
    Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 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 PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3, and/or Flt3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
    Type: Application
    Filed: February 18, 2011
    Publication date: March 14, 2013
    Applicant: Centro Nacional de Investigaceiones Oncologicas (CNIO)
    Inventors: Joaquin Pastor Fernández, Julen Oyarzabal Santamarina, Carl-Gustaf Pierre Saluste, Carmen Blanco Aparicio, Rosa Maria Alvarez Escobar, Virginia Rivero Buceta
  • Pyrazolopyridine, Pyrazolopyrazine, Pyrazolopyrimidine, Pyrazolothiophene and Pyrazolothiazole Compounds as MGLUR4 Allosteric Potentiators, Compositions, and Methods of Treating Neurological Dysfunction
    Publication number: 20130065895
    Abstract: Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Application
    Filed: August 13, 2012
    Publication date: March 14, 2013
    Applicant: VANDERBILT UNIVERSITY
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
  • 6-(4-HYDROXY-PHENYL)-3-STYRYL-1H-PYRAZOLO[3,4-b]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20130065894
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4 and R5 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 12, 2011
    Publication date: March 14, 2013
    Applicant: SANOFI
    Inventors: Matthias LOEHN, Maria MENDEZ-PEREZ, Stefania PFEIFFER-MAREK, Aimo KANNT, Guillaume BEGIS, Olivier DUCLOS, Federic JEANNOT
  • Pyrazole [3, 4-B] pyridine Raf inhibitors
    Patent number: 8394795
    Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, 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: Grant
    Filed: February 27, 2009
    Date of Patent: March 12, 2013
    Assignees: Array BioPharma Inc., Genentech, Inc.
    Inventors: Kateri A. Ahrendt, Alexandre J. Buckmelter, Jason De Meese, Jonas Grina, Joshua D. Hansen, Ellen R. Laird, Paul Lunghofer, David Moreno, Brad Newhouse, Li Ren, Jeongbeob Seo, Hongqi Tian, Steven Mark Wenglowsky, Bainian Feng, Janet Gunzner, Kim Malesky, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Wendy B. Young
  • Bicyclic pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use
    Patent number: 8394796
    Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. 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: Grant
    Filed: March 22, 2012
    Date of Patent: March 12, 2013
    Assignee: Genentech, Inc.
    Inventors: Georgette Castanedo, Bryan Chan, David Goldstein, Rama Kondru, Matthew Lucas, Wylie Palmer, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Zachary K. Sweeney
  • AZAINDAZOLES
    Publication number: 20130059849
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: May 5, 2011
    Publication date: March 7, 2013
    Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
  • DIAGNOSTIC AND THERAPEUTIC METHODS FOR CORNEAL ECTASIA FOLLOWING REFRACTIVE SURGERY, KERATOCONUS OR PELLUCID DEGENERATION
    Publication number: 20130058954
    Abstract: The present invention relates to methods of diagnosis and treatment of corneal ectasia following refractive surgery, keratoconus or pellucid marginal degeneration in a subject by determining or modulating the level of expression of molecules associated with the Wnt signalling pathway. Marker molecules of the present invention include SFRP1, PITX2, LEF1, WNT16 and WNT5A.
    Type: Application
    Filed: December 2, 2010
    Publication date: March 7, 2013
    Applicant: THE UNIVERSITY OF SYDNEY
    Inventors: Gerard Sutton, John McAvoy, Michele Madigan
  • SUBSTITUTED N-(3-(PYRIMIDIN-4-YL)PHENYL)ACRYLAMIDE ANALOGS AS TYROSINE RECEPTOR KINASE BTK INHIBITORS
    Publication number: 20130059847
    Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: April 1, 2012
    Publication date: March 7, 2013
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
  • CANNABINOID-2 AGONISTS
    Publication number: 20130059848
    Abstract: The present specification discloses cannabinoid-2 agonists, compositions comprising such cannabinoid-2 agonists, and methods of treating an individual suffering from a disease by administering compositions comprising such cannabinoid-2 agonists.
    Type: Application
    Filed: February 7, 2011
    Publication date: March 7, 2013
    Applicant: ALLERGAN, INC
    Inventors: June Chen, Simon Pettit, Hans Flirl
  • METHODS FOR TREATING MILD COGNITIVE IMPAIRMENT
    Publication number: 20130059824
    Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from Mild Cognitive Impairment.
    Type: Application
    Filed: November 23, 2010
    Publication date: March 7, 2013
    Applicant: AFRAXis, Inc.
    Inventors: Jay Lichter, David Campbell, Benedikt Vollrath, Sergio G. Durón
  • PYRROLOPYRAZINE KINASE INHIBITORS
    Publication number: 20130059834
    Abstract: 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: Application
    Filed: August 31, 2012
    Publication date: March 7, 2013
    Inventors: 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
  • Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
    Patent number: 8389518
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: March 5, 2013
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Laetitia Fioraso-Cartier, Bianca Mottironi
  • PYRIMIDO-PYRIDAZINONE COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20130053346
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Application
    Filed: August 23, 2012
    Publication date: February 28, 2013
    Applicant: Endo Pharmaceuticals Inc
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES
    Publication number: 20130053370
    Abstract: 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: Application
    Filed: January 31, 2011
    Publication date: February 28, 2013
    Applicants: HANMI SCIENCE CO., LTD., CATHOLIC UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: 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
  • PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE
    Publication number: 20130039906
    Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Wendy Lee, Vickie H. Tsui, Xiaojing Wang, Zhaoyang Wen
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    Publication number: 20130034616
    Abstract: 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: Application
    Filed: June 22, 2012
    Publication date: February 7, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Pierre-Henri Storck, Jean-Damien Charrier, Alistair Rutherford, Michael Paul Mortimore, Somhairle MacCormick, Ronald Marcellus Alphonsus Knegtel, Steven John Durrant
  • INHIBITORS OF BRUTON'S TYROSINE KINASE
    Publication number: 20130035334
    Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
    Type: Application
    Filed: September 7, 2012
    Publication date: February 7, 2013
    Applicant: Pharmacyclics, Inc.
    Inventors: Lee HONIGBERG, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen
  • KINASE INHIBITORS
    Publication number: 20130035325
    Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.
    Type: Application
    Filed: November 16, 2010
    Publication date: February 7, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
  • HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20130035324
    Abstract: 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: Application
    Filed: August 17, 2010
    Publication date: February 7, 2013
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
  • COMBINATION COMPRISING A CYCLIN DEPENDENT KINASE 4 OR CYCLIN DEPENDENT KINASE (CDK4/6) INHIBITOR FOR TREATING CANCER
    Publication number: 20130035336
    Abstract: A combination of a CDK4/8 inhibitor and an mTOR inhibitor for the treatment of cancer.
    Type: Application
    Filed: April 12, 2011
    Publication date: February 7, 2013
    Applicant: Novartis AG
    Inventors: Maria Borland, Christopher Thomas Brain, Shivang Doshi, Sunkyu Kim, Jianguo Ma, Josh Murtie, Hong Zhang
  • 8-ETHYL-6-(ARYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS
    Publication number: 20130035335
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.
    Type: Application
    Filed: September 18, 2012
    Publication date: February 7, 2013
    Applicant: aFRAXis, Inc.
    Inventor: aFRAXis, Inc.
  • Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
    Patent number: 8367663
    Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
    Type: Grant
    Filed: January 8, 2010
    Date of Patent: February 5, 2013
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixiao Zhai, Cheng-Jung Lai, Changgeng Qian
  • INDAZOLES
    Publication number: 20130029968
    Abstract: The present invention relates to compounds of formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.
    Type: Application
    Filed: July 5, 2012
    Publication date: January 31, 2013
    Applicant: PFIZER LIMITED
    Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Kortum, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
  • HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20130029984
    Abstract: 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: Application
    Filed: July 18, 2012
    Publication date: January 31, 2013
    Applicants: 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
  • INHIBITORS OF PROTEIN KINASES
    Publication number: 20130029944
    Abstract: 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: Application
    Filed: June 20, 2012
    Publication date: January 31, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Yonghong Song, Qing Xu, Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Anjali Pandey
  • HETEROCYCLIC COMPOUND
    Publication number: 20130029969
    Abstract: 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: Application
    Filed: February 16, 2011
    Publication date: January 31, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Misaki Homma, Toru Miyazaki, Yuya Oguro, Osamu Kurasawa
  • AMINOTHIENOPYRIDAZINE INHIBITORS OF TAU ASSEMBLY
    Publication number: 20130029983
    Abstract: 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: Application
    Filed: September 22, 2010
    Publication date: January 31, 2013
    Inventors: 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
  • PYRIDAZINO[4,5-D]PYRIMIDIN-5(6H)-ONE INHIBITORS OF KINASES
    Publication number: 20130023523
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein B, R1, R2, R4, and m 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: Application
    Filed: July 19, 2012
    Publication date: January 24, 2013
    Applicant: ABBOTT LABORATORIES
    Inventors: Gui-Dong Zhu, Jane Gong, Andrew S. Judd, Virajkumar B. Ghandi, Alexander R. Shoemaker, Thomas D. Penning, Michael R. Michaelides, Chunqiu Lai, Keith W. Woods
  • PYRIMIDO[5,4-D]PYRIMIDYLAMINO PHENYL SULFONAMIDES AS SERINE/THREONINE KINASE INHIBITORS
    Publication number: 20130023531
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Application
    Filed: January 19, 2012
    Publication date: January 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Andreas MANTOULIDIS, Peter ETTMAYER
  • BETA-CELL REPLICATION PROMOTING COMPOUNDS AND METHODS OF THEIR USE
    Publication number: 20130023491
    Abstract: In the invention provides for a method of stimulating or increasing ?-cell replication or growth, by contacting a ?-cell with an inhibitor of adenosine kinase (ADK), an inhibitor of S-Adenosylhomocysteine hydrolase (SAHH) or an activator of AMP activated protein kinase (AMPK).
    Type: Application
    Filed: December 17, 2010
    Publication date: January 24, 2013
    Applicants: President and Fellows of Harvard College, Joslin Diabetes Center, Inc., The Brigham and Women's Hospital, Inc.
    Inventors: Justin P. Annes, Douglas A. Melton, Lee L. Rubin, Gordon Weir
  • INDAZOLYL-PYRIMIDINES AS KINASE INHIBITORS
    Publication number: 20130023532
    Abstract: Disclosed are compounds having the formula: or a salt thereof, wherein A, n, R1, R1A, and R2 are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: March 26, 2011
    Publication date: January 24, 2013
    Inventors: Linda N. Casillas, Subhas J. Chakravorty, Adam Kenneth Charnley, Pamela A. Haile, Terry Vincent Hughes, Jae U. Jeong, Jianxing Kang, Ami Lakdawala Shah, Lara Kathryn Leister, Robert W. Marquis, JR., Nathan Andrew Miller, Daniel J. Price, Clark A. Sehon, Gren Z. Wang, Daohua Zhang, Patrick Eidam
  • Thyazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase
    Patent number: 8357684
    Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: January 22, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Genesis M. Bacani, Eugene Y. Cheung, Christa C. Chrovian, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener
  • SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20130017170
    Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
  • IMIDAZOLYL-IMIDAZOLES AS KINASE INHIBITORS
    Publication number: 20130018039
    Abstract: Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are defined herein, and methods of making and using the same.
    Type: Application
    Filed: March 31, 2011
    Publication date: January 17, 2013
    Inventors: 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
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    Publication number: 20130017273
    Abstract: 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: Application
    Filed: June 22, 2012
    Publication date: January 17, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Simon Everitt, Michael Paul Mortimore, Jean-Damien Charrier, Somhairle MacCormick, Pierre-Henri Storck, Ronald Knegtel, Joanne Pinder, Steven John Durrant
  • SUBSTITUTED PYRROLO-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20130012507
    Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 10, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
  • IMIDAZOLO-, OXAZOLO-, AND THIAZOLOPYRIMIDINE MODULATORS OF TRPV1
    Publication number: 20130005687
    Abstract: 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: Application
    Filed: September 12, 2012
    Publication date: January 3, 2013
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
  • Substituted Imidazopyridinyl-Aminopyridine Compounds
    Publication number: 20120329791
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Applicant: ArQuele, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
  • Novel kinase inhibitors
    Publication number: 20120329780
    Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.
    Type: Application
    Filed: April 23, 2012
    Publication date: December 27, 2012
    Applicant: Origenis GmbH
    Inventors: Michael Thormann, Andreas Treml, Michael Almstetter, Nadine Traube
  • HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20120329776
    Abstract: 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: Application
    Filed: November 4, 2011
    Publication date: December 27, 2012
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson
  • Substituted Imidazopyridinyl Compounds
    Publication number: 20120329793
    Abstract: The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Yuko Yamamoto, Takeshi Isoyama
  • Fused thiazole derivatives as kinase inhibitors
    Patent number: 8338592
    Abstract: A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: December 25, 2012
    Assignee: UCB Pharma, S.A.
    Inventors: Rikki Peter Alexander, Karen Viviane Lucile Crépy, Anne Marie Foley, Richard Jeremy Franklin
  • DEUTERATED COMPOUNDS USEFUL FOR TREATING NEURODEGENERATIVE DISEASES
    Publication number: 20120322799
    Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.
    Type: Application
    Filed: November 30, 2010
    Publication date: December 20, 2012
    Applicant: PHARMATROPHIX, INC.
    Inventor: Gopal Damodara
  • Pyrazolopiperidine Compounds As CCR1 Receptor Antagonists
    Publication number: 20120322790
    Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
    Type: Application
    Filed: December 16, 2011
    Publication date: December 20, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Rajashekhar BETAGERI, Brian Nicholas COOK, Darren DiSALVO, Christian HARCKEN, Daniel KUZMICH, Pingrong LIU, John LORD, Can MAO, Hossein RAZAVI
  • Pyrazolo Piperidine Derivatives as NADPH Oxidase Inhibitors
    Publication number: 20120316163
    Abstract: The present invention is related to pyrazolo piperidine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: GENKYOTEX SA
    Inventors: Patrick Page, Benoît Laleu, Francesca Gaggini, Mike Orchard
  • Methods and Compositions for Treating Cancer
    Publication number: 20120316137
    Abstract: The invention features methods, kits, and pharmaceutical compositions for treating cancer using 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)-methyl)-3-(trifluoromethyl)phenyl)benzamide.
    Type: Application
    Filed: November 1, 2010
    Publication date: December 13, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Wei-Sheng Huang, Victor M. Rivera, Timothy P. Clackson, William C. Shakespeare, Rachel M. Squillace, Joseph M. Gozgit