Bicyclo Ring System Having The Oxazine Ring As One Of The Cyclos (e.g., Benzoxazines, Etc.) Patents (Class 544/105)
  • 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES
    Publication number: 20130317216
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: June 4, 2013
    Publication date: November 28, 2013
    Inventors: Rajinder Singh, Ankush Argade, Catherine Sylvain
  • AMINOALCOHOL SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
    Publication number: 20130317004
    Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: November 8, 2011
    Publication date: November 28, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventors: William Johnston Scott, Ningshu Liu, Manfred Möwes, Andrea Hägebarth, Ursula Mönning, Ulf Bömer
  • SUBSTITUTED OXAZOLIDINONES AND THEIR USE IN THE FIELD OF BLOOD COAGULATION
    Publication number: 20130316999
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: August 7, 2013
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
  • COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
    Publication number: 20130310364
    Abstract: 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: Application
    Filed: July 16, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • PYRIMIDINEDIAMINE KINASE INHIBITORS
    Publication number: 20130309228
    Abstract: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
    Type: Application
    Filed: July 23, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Andy Atuegbu, John Ramphal, Hui Li, Marina Gelman, Jeffrey Clough, Carlos Valdez, Somasekhar Bhamidipati, Sambaiah Thota, Darren McMurtrie
  • NOVEL TRIAZINE COMPOUNDS
    Publication number: 20130303516
    Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.
    Type: Application
    Filed: January 25, 2012
    Publication date: November 14, 2013
    Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
  • FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE
    Publication number: 20130303529
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: June 13, 2013
    Publication date: November 14, 2013
    Inventors: Brian K. ALBRECHT, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia W. Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie K. Springer, Markian Stec, Ning Xi, Kevin Yang, Karina Romero, Katrina Woodin Copeland, Emily A. Peterson
  • Mitochondrial inhibitors to treat human disease
    Patent number: 8581005
    Abstract: The present invention relates to inhibitors of mitochondria-associated, granulocyte-macrophage colony stimulating factor signaling molecule (Magmas), and related compositions and uses thereof.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: November 12, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Paul Jubinsky, Bhaskar C. Das, Mary K. Short
  • Gamma secretase modulators
    Patent number: 8580956
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: November 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
  • C-17 BICYCLIC AMINES OF TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY
    Publication number: 20130296554
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: March 13, 2013
    Publication date: November 7, 2013
    Inventors: Ny Sin, Zheng Liu, Jacob Swidorski, Sing-Yuen Sit, Jie Chen, Yan Chen, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • IMIDAZO[1,2-a]PYRIDINE COMPOUNDS
    Publication number: 20130289013
    Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed.
    Type: Application
    Filed: June 24, 2013
    Publication date: October 31, 2013
    Inventors: Qun Kevin FANG, Frank Xinhe Wu, Paul T. Grover, Seth C. Hopkins, Una Campbell, Milan Chytil, Kerry L. Spear
  • Compounds and their administration for treating a neurodegenerative disease as well as a method for identifying a compound capable of inhibiting a kinase, such as LRRK
    Patent number: 8569281
    Abstract: 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: Grant
    Filed: September 21, 2011
    Date of Patent: October 29, 2013
    Assignees: Medical Research Council Technology, Genentech, Inc.
    Inventors: Bryan K. Chan, Huifen Chen, Anthony Estrada, Daniel Shore, Zachary Sweeney, Edward Giles McIver
  • 2-(cyclic amino)-pyrimidone derivatives
    Patent number: 8569294
    Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: October 29, 2013
    Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi
    Inventors: Kenji Fukunaga, Toshiyuki Kohara, Kazutoshi Watanabe, Yoshihiro Usui, Fumiaki Uehara, Satoshi Yokoshima, Daiki Sakai, Shin-ichi Kusaka, Kazuki Nakayama
  • Carboxamide compounds and their use
    Patent number: 8569282
    Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: October 29, 2013
    Assignee: CytoPathfinder, Inc.
    Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
  • NEW CYCLOHEXYLAMINE DERIVATIVES HAVING ß2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES
    Publication number: 20130281415
    Abstract: The present disclosure relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
    Type: Application
    Filed: May 13, 2011
    Publication date: October 24, 2013
    Inventors: Maria Prat Quinones, Silvia Fonquerna Pou, Carlos Puig Duran, Wenceslao Lumeras Amador, Jose Aiguade Bosch, Juan Francisco Caturla Javaloyes
  • THERAPEUTIC COMPOUNDS
    Publication number: 20130281433
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • DNA-PK INHIBITORS
    Publication number: 20130281431
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. 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.
    Type: Application
    Filed: April 23, 2013
    Publication date: October 24, 2013
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE
    Publication number: 20130281445
    Abstract: The present invention relates to compounds useful as inhibitors of choline 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: Application
    Filed: September 21, 2012
    Publication date: October 24, 2013
    Inventors: Simon Everitt, Ronald Knegtel, Michael Mortimore, Alistair Rutherford
  • Methylene furanone derivatives and use of said derivatives as a photoprotecting or antioxidant or depigmentation agent in cosmetic or dermatological compositions
    Patent number: 8563548
    Abstract: The present invention relates to methylene furanone derivatives as well as the use thereof as a protective, antioxidant, or depigmentation agent in cosmetic or dermatological compositions. The invention also relates to a method for preparing said derivatives involving a Suzuki-Miyaura coupling reaction from corresponding dibromofuranone derivatives. The invention also relates to a method of preparation involving a coupling reaction of 2-methoxy-furan derivatives with a ketone followed by dehydration.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: October 22, 2013
    Assignee: Pierre Fabre Dermo-Cosmetique
    Inventors: Estelle Marchal, Philippe Uriac, Yves Brunel, Stëphane Poigny
  • NOVEL PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS
    Publication number: 20130274253
    Abstract: The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 17, 2013
    Applicant: SANOFI
    Inventors: Maurice Brollo, Jean-Christophe Carry, Victor Certal, Eric Didier, Gilles Doerflinger, Youssef EL Ahmad, Bruno Filoche-Romme, Frank Halley, Karl Andreas Karlsson, Laurent Schio, Fabienne Thompson
  • Thienopyranones as kinase inhibitors
    Patent number: 8557807
    Abstract: The invention, relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as P1-3 kinase.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: October 15, 2013
    Assignee: Signal Rx Pharmaceuticals, Inc.
    Inventors: Guillermo A. Morales, Kevin T. Weber, Jessica M. Newblom, Xiaodong Peng, Jingdong Su, Joseph R. Garlich
  • Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
    Patent number: 8557806
    Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: October 15, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
  • IMIDAZOPYRAZINE SYK INHIBITORS
    Publication number: 20130267496
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: May 23, 2013
    Publication date: October 10, 2013
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
  • Furo[3,2-]pyrimidine compounds
    Patent number: 8551981
    Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: October 8, 2013
    Assignee: AbbVie Inc.
    Inventors: David J. Calderwood, Noel S. Wilson, Philip Cox, Michael Z. Hoemann, Bruce Clapham, Anil Vasudevan, Clara I. Villamil, Bin Li, Gagandeep Somal, Kelly D. Mullen
  • HETEROCYCLIC COMPOUNDS FOR TREATING OR PREVENTING DISORDERS CAUSED BY REDUCED NEUROTRANSMISSION OF SEROTONIN, NOREPHNEPHRINE OR DOPAMINE
    Publication number: 20130261081
    Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
    Type: Application
    Filed: September 12, 2011
    Publication date: October 3, 2013
    Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
  • Benzoic pyrrolopyridine derivatives
    Patent number: 8546385
    Abstract: The present invention relates to compounds of formula: in which A, Cy, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the description. The compounds of the invention are modulators of the NURR-1 nuclear receptors.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: October 1, 2013
    Assignee: Laboratoires FOURNIER SA
    Inventors: Jerome Amaudrut, Benaissa Boubia, Fabrice Guillier, Olivia Poupardin-Olivier
  • Substituted sulfonamide compounds
    Patent number: 8541573
    Abstract: Substituted sulfonamide compounds corresponding to the formula I processes for the preparation thereof, pharmaceutical compositions containing these compounds and the use of substituted sulfonamide compounds for the preparation of pharmaceutical compositions for treating pain and other conditions at least partly mediated via the bradykinin 1 receptor.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: September 24, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Ruth Jostock, Klaus Schiene, Jean De Vry, Tieno Germann, Sabine Hees, Stefan Schunk, Melanie Reich
  • IMIDAZOPYRAZINE SYK INHIBITORS
    Publication number: 20130237520
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: April 23, 2013
    Publication date: September 12, 2013
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J.M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
  • IMIDAZOPYRIZINE SYK INHIBITORS
    Publication number: 20130231330
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: April 12, 2013
    Publication date: September 5, 2013
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD
  • Inhibitors of Human Immunodeficiency Virus Replication
    Publication number: 20130231331
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 5, 2013
    Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
  • 1H-Pyrrolo[2,3 b]pyridine derivatives
    Publication number: 20130231519
    Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.
    Type: Application
    Filed: October 12, 2011
    Publication date: September 5, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
  • AMINO PYRIMIDINE ANTICANCER COMPOUNDS
    Publication number: 20130231306
    Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
    Type: Application
    Filed: January 25, 2013
    Publication date: September 5, 2013
    Applicant: OSI Pharmaceuticals, LLC
    Inventors: Andrew P. CREW, Dan Sherman, Rama Devi Appari, Xin Chen, Ramesh Chilukuri, Hanqing Dong, Caterina Ferraro, Kenneth Foreman, Ramesh C. Gupta, An-Hu Li, Kathryn M. Stolz, Brian Volk, Robert Zahler
  • 5-Alkynyl Pyridine
    Publication number: 20130225567
    Abstract: 5-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.
    Type: Application
    Filed: February 19, 2013
    Publication date: August 29, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Ulrich REISER, Gerd BADER, Walter SPEVAK, Andreas STEFFEN, Alastair L. PARKES
  • TRIAZOLOPYRAZINE DERIVATIVES
    Publication number: 20130225568
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis.
    Type: Application
    Filed: July 29, 2011
    Publication date: August 29, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Lars Burgdorf, Melanie Schultz, Carl Deutsch, Horacio Comas, Dominique Swinnen, Vincent Pomel, Pascale Gaillard, Brian Hodous
  • FUROPYRIDINE DERIVATIVES
    Publication number: 20130225569
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: July 29, 2011
    Publication date: August 29, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Lars Burgdorf, Melanie Schultz, Tatjana Ross, Brian Hodous, Justin Potnick, Amanda E. Sutton, Bayard R. Huck
  • PHENYLACETIC ACID COMPOUND
    Publication number: 20130225808
    Abstract: A compound represented by formula (I), wherein R1 represents a hydrogen atom, etc., R2 and R3 each independently represents a hydrogen atom, optionally oxidized C1-4 alkyl group or optionally protected hydroxyl group, or R2 and R3 taken together represent optionally oxidized C2-5 alkylene group, R4 represents an optionally oxidized C1-6 alkyl group, etc., R5 represents an optionally oxidized C1-6 alkyl group, etc., R6 represents an optionally oxidized C1-6 alkyl group, etc., m represents 0 or an integer from 1 to 3, n represents 0 or an integer from 1 to 4, and i represents 0 or an integer from 1 to 7.
    Type: Application
    Filed: April 1, 2013
    Publication date: August 29, 2013
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventor: ONO PHARMACEUTICAL CO., LTD.
  • HETEROBICYCLIC COMPOUNDS
    Publication number: 20130225552
    Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.
    Type: Application
    Filed: February 28, 2013
    Publication date: August 29, 2013
    Applicant: AMGEN INC.
    Inventor: Amgen Inc.
  • Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
    Patent number: 8518972
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: August 27, 2013
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
  • Pyrimidinediamine kinase inhibitors
    Patent number: 8518937
    Abstract: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: August 27, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Andy Atuegbu, John Ramphal, Hui Li, Marina Gelman, Jeffrey Clough, Carlos Valdez, Somasekhar Bhamidipati, Sambaiah Thota, Darren McMurtrie
  • Protein Kinase C Inhibitors and Uses Thereof
    Publication number: 20130210810
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: December 18, 2012
    Publication date: August 15, 2013
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventor: Rigel Pharmaceuticals, Inc.
  • 2-QUINOLINYL-ACETIC ACID DERIVATIVES AS HIV ANTIVIRAL COMPOUNDS
    Publication number: 20130210801
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).
    Type: Application
    Filed: July 1, 2011
    Publication date: August 15, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Kerim Babaoglu, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, John O. Link, Hongtao Liu, Michael L. Mitchell, Jianyu Sun, James Taylor, Randall W. Vivian, Lianhong Xu
  • Novel Heterocyclic Compounds and Uses Thereof
    Publication number: 20130210818
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 15, 2013
    Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • IMIDAZOPYRIDINES SYK INHIBITORS
    Publication number: 20130210802
    Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: March 11, 2011
    Publication date: August 15, 2013
    Applicant: Gilead Connecticut, Inc
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
  • QUINAZOLINE DERIVATIVES
    Publication number: 20130210819
    Abstract: Compounds of the formula I in which R, X, L2 and A1-A6 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.
    Type: Application
    Filed: September 22, 2011
    Publication date: August 15, 2013
    Applicant: MERCK PATENT GMBH
    Inventor: Markus Klein
  • Oxazolidinyl antibiotics
    Patent number: 8507478
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is alkoxy or halogen; U and V each independently are CH or N; is a bond or is absent; W is CH or N or, when is absent, W is CH2 or NH, with the proviso that U, V and W are not all N; A is a bond or CH2; R2 is H or, provided A is CH2, may also be OH; m and n each independently are 0 or 1; D is CH2 or a bond; G represents a phenyl group substituted once or twice in the meta and/or para position(s) by substituents selected from alkyl, (C1-C3)alkoxy and halogen, or G is a group G1 or G2 wherein Z1, Z2 and Z3 may each represent CH or N; X is N or CH and Q is O or S; it being understood that if m and n each are 0, then A is CH2; and salts of such compounds.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: August 13, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Bicyclic pyridinylpyrazoles
    Patent number: 8507472
    Abstract: Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials and for reducing mycotoxins in plants and plant parts, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: April 5, 2011
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Amos Mattes, Hendrik Helmke, Stefan Hillebrand, Gorka Peris, Alexander Sudau, Lars Rodefeld, Stefan Gauger, Jürgen Benting, Peter Dahmen, Ruth Meissner, Ulrike Wachendorff-Neumann, Hiroyuki Hadano
  • Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
    Patent number: 8507482
    Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as conditions such as stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, among others.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: August 13, 2013
    Assignee: Cortex Pharmaceuticals, Inc.
    Inventors: Rudolf Mueller, Leslie J. Street
  • Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy
    Publication number: 20130203749
    Abstract: The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.
    Type: Application
    Filed: March 10, 2013
    Publication date: August 8, 2013
    Applicants: ABBVIE INC., ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles Hutchins
  • Inhibitors of Human Immunodeficiency Virus Replication
    Publication number: 20130203748
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: August 9, 2012
    Publication date: August 8, 2013
    Inventors: B. Narasimhulu Naidu, Manoj Patel
  • INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
    Publication number: 20130203747
    Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 8, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.