Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
Perimidine (including hydrogenated) (Class 514/268)
  • SULFONE SUBSTITUTED 2,3-DIHYDROIMIDAZO [1,2-C] QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES WITH ANGIOGENESIS
    Publication number: 20110190281
    Abstract: This invention relates to novel sulfone 2I3-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 mediated disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: January 13, 2009
    Publication date: August 4, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Martin Hentemann, William Scott, Jill Wood, Jeffrey Johnson, Aniko Redman, Ann-Marie Bullion, Leatte Guernon
  • NOVEL HETEROCYCLIC COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20110190303
    Abstract: The present invention relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the formula (1) and analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxides, pharmaceutically acceptable solvates thereof and the pharmaceutical compositions containing them which are useful in the treatment of allergic and inflammatory diseases including asthma, chronic bronchitis, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, vernal conjuctivitis, eosinophilic granuloma, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and reperfusion injury of the brain, chronic glomerulonephritis, endotoxic shock and adult respiratory distress syndrome.
    Type: Application
    Filed: April 15, 2011
    Publication date: August 4, 2011
    Applicant: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram Gharat, Balasubramanian Gopalan, Neelima Khairatkar Joshi
  • mGluR1 antagonists as therapeutic agents
    Patent number: 7989464
    Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: August 2, 2011
    Assignee: Schering Corporation
    Inventors: Julius J. Matasi, Deen Tulshian, Duane A. Burnett, Wen-Lian Wu, Peter Korakas, Lisa S. Silverman, Thavalakulamgara K. Sasikumar, Li Qiang, Martin S. Domalski
  • Icotinib Hydrochloride, Synthesis, Crystalline Forms, Pharmaceutical Compositions, and Uses Thereof
    Publication number: 20110182882
    Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.
    Type: Application
    Filed: July 7, 2009
    Publication date: July 28, 2011
    Applicant: Beta Pharma, Inc.
    Inventors: Yinxiang Wang, Guojian Xie, Lieming Ding, Fenlai Tan, Yunyan Hu, Wei He, Bin Han, Wei Long, Yong Liu, Haima Ai, Charles Davis, Don Zhang
  • Methods and Compositions for Treating Alzheimer's Disease
    Publication number: 20110183942
    Abstract: A method is disclosed for inhibiting the build-up of amyloid plaques in the brain of a patient with at least one risk factor for, or a diagnosis of, Alzheimer's Disease by administering to the patient an amount of one or more compounds effective to inhibit the phosphorylative activity of eEF2K, thereby inhibiting amyloid plaque deposition.
    Type: Application
    Filed: July 15, 2009
    Publication date: July 28, 2011
    Applicants: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY, JOHNS HOPKINS UNIVERSITY
    Inventors: Paul Worley, Sungjin Park, Alexey G. Ryazanov
  • Method for pain treatment
    Patent number: 7985745
    Abstract: This invention discloses a method of treating pain by administering histamine H4 receptor ligands and compositions comprising the same.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: July 26, 2011
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Robert J. Altenbach, Huaqing Liu, Irene Drizin, Neil Wishart, David J. Babinski, Robert J. Gregg, Arthur A. Hancock, Kathryn J. Hancock, legal representative, Timothy A. Esbenshade, Gin C. Hsieh, Jorge D. Brioni, Marie P. Honore, Lawrence A. Black, Chen Zhao, Brian D. Wakefield
  • HCV PROTEASE INHIBITORS
    Publication number: 20110178107
    Abstract: This invention relates to compounds of Formula (I), (II), or (III) shown in the specification. These compounds can be used to treat hepatitis C virus infection.
    Type: Application
    Filed: January 19, 2011
    Publication date: July 21, 2011
    Applicant: TaiGen Biotechnology Co., Ltd.
    Inventors: Ching-Cheng Wang, Chen-Fu Liu, Kuang-Yuan Lee, Mei-Chun Lin, Shu-Huei Wang, Chi-Feng Yen, Yu-Hsuan Wang, Chi-Hsin Richard King
  • CGRP ANTAGONISTS
    Publication number: 20110172218
    Abstract: The present invention relates to novel CGRP antagonists of the general formula (I) in which U, V, X, Y, R1, R2, R3 are defined as described below, the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts thereof, and the hydrates of the salts, particularly the physiologically compatible salts thereof having inorganic or organic acids or bases, pharmaceuticals comprising said compounds, the use thereof, and the method for the production thereof.
    Type: Application
    Filed: October 16, 2008
    Publication date: July 14, 2011
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Klaus Rudolf, Stephan Georg Mueller, Gerhard Schaenzle, Dirk Stenkamp
  • 3-HETEROCYCLIC SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20110165118
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: November 13, 2008
    Publication date: July 7, 2011
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Fused Ring Azadecalin Glucocorticoid Receptor Modulators
    Publication number: 20110166110
    Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: March 11, 2011
    Publication date: July 7, 2011
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
  • Tricyclic Compounds as Modulators of TNF-alpha Synthesis and as PDE4 Inhibitors
    Publication number: 20110160234
    Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to rheumatoid arthritis.
    Type: Application
    Filed: March 4, 2011
    Publication date: June 30, 2011
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: Adnan M.M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew Kostura, Mustafa Guzel
  • ANTI-VIRAL COMPOUNDS
    Publication number: 20110160233
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
    Type: Application
    Filed: December 19, 2007
    Publication date: June 30, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: David A. Betebenner, Clarence J. Maring, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie VL. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
  • IMIDAZO [2,1-B] QUINAZOLIN-2-ONE DERIVATIVES AND THEIR USE AS PLATELET ANTI-AGGREGATIVE AGENTS
    Publication number: 20110152298
    Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below where the substituents have the meanings defined in claim (I) and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: May 13, 2009
    Publication date: June 23, 2011
    Applicant: SHIRE LLC
    Inventors: Bernard T. Golding, Richard Franklin, Angus Macleod, Peter Cicala
  • NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20110152259
    Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).
    Type: Application
    Filed: February 24, 2011
    Publication date: June 23, 2011
    Inventors: Anandan Palani, Jing Su, Dong Xiao, Xianhai Huang, Ashwin U. Rao, Xiao Chen, Haiqun Tang, Jun Qin, Ying R. Huang, Robert G. Aslanian, Brain A. McKittrick, Syliva J. Degrado
  • Tricyclic compounds as modulators of TNF-? synthesis
    Patent number: 7964608
    Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-alpha or by PDE4, including but not limited to rheumatoid arthritis.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: June 21, 2011
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew Kostura, Mustafa Guzel
  • Fused Pyridine, Pyrimidine and Triazine Compounds as Cell Cycle Inhibitors
    Publication number: 20110142796
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
    Type: Application
    Filed: December 18, 2008
    Publication date: June 16, 2011
    Applicant: Amgen Inc
    Inventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. Mcgee, Rajiv Sharma, Xiaodong Wang, Dustin L. Mcminn, Jeffrey T. Mihalic, Jeffrey Deignan
  • SUBSTITUTED PYRIMIDO ISOQUINOLINE DERIVATIVES
    Publication number: 20110144138
    Abstract: Pyrimido isoquinoline derivatives represented by formula (I): wherein: R1, R2, R3, R4, R7, R8, R9, R10, and are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.
    Type: Application
    Filed: December 15, 2010
    Publication date: June 16, 2011
    Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Alistair LOCHEAD, Mourad SAADY, Philippe YAICHE
  • Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
    Patent number: 7960400
    Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.
    Type: Grant
    Filed: August 27, 2007
    Date of Patent: June 14, 2011
    Assignee: Duquesne University of the Holy Ghost
    Inventor: Aleem Gangjee
  • WNT PROTEIN SIGNALLING INHIBITORS
    Publication number: 20110136813
    Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.
    Type: Application
    Filed: May 27, 2009
    Publication date: June 9, 2011
    Inventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
  • NOVEL FUSED THIAZOLO AND OXAZOLO PYRIMIDINONES
    Publication number: 20110130414
    Abstract: The present invention relates to novel compounds, their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.
    Type: Application
    Filed: September 8, 2010
    Publication date: June 2, 2011
    Applicant: TORRENT PHARMACEUTICALS LIMITED
    Inventors: Sanjay Srivastava, Laxmikant Chhipa, Ramesh Chandra Gupta, Shailesh Deshpande, Anita Chaudhari, Anookh Mohanan, Chaitanya Dutt, Vijay Chauthaiwale, Murali Badanthadka, Prashant G. Jamadarkhana
  • SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS
    Publication number: 20110130405
    Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the meanings of the substituents are defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: May 13, 2009
    Publication date: June 2, 2011
    Applicant: Shire LLC
    Inventors: Bernard Golding, Richard Franklin, Kim Hirst
  • DIAZACARBAZOLES AND METHODS OF USE
    Publication number: 20110124654
    Abstract: The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Application
    Filed: June 10, 2009
    Publication date: May 26, 2011
    Inventors: Huifen Chen, Hazel Joan Dyke, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Joseph Lyssikatos, Calum Macleod, Karen Williams
  • INHIBITORS OF HUMAN METHIONINE AMINOPEPTIDASE 1 AND METHODS OF TREATING DISORDERS
    Publication number: 20110124649
    Abstract: Described herein are novel pyrimidine-pyridine compounds, methods of inhibiting methionine aminopeptidase and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, wherein a compound of the invention is administered to a subject.
    Type: Application
    Filed: November 10, 2008
    Publication date: May 26, 2011
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Jun O. Liu, Xiaoyi Hu, Xiaochun Chen, Dawei Ma, Shridhar Bhat
  • 3,4-DIHYDROPYRIMIDINE TRPA1 ANTAGONISTS
    Publication number: 20110124666
    Abstract: The present invention is related to novel 3,4-dihydropyrimidine compounds of formula (I) having TRPA1 receptor antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.
    Type: Application
    Filed: May 29, 2009
    Publication date: May 26, 2011
    Inventors: Henricus Jacobus Maria Gijsen, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn
  • 8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d] pyrazolo[1,5-a]pyrimidine methanesulfonate as a CRF antagonist
    Patent number: 7947697
    Abstract: 8-(3-pentylamino)-2-methyl-3-(2-chloro-4-methoxyphenyl)-6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidine methanesulfonate of the structural formula (I) has Corticotropin Releasing Factor (CRF) antagonist activity and is useful in treating neuropsychiatric and digestive system diseases.
    Type: Grant
    Filed: June 24, 2004
    Date of Patent: May 24, 2011
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Tomoyuki Hasegawa, Toshiaki Matsui, Hiroshi Araki, Tetsuji Saito, Tetsuo Obitsu, Masaki Okamoto, Yuichi Gemba, Yutaka Mikami
  • RAF KINASE MODULATOR COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20110118245
    Abstract: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
    Type: Application
    Filed: March 17, 2009
    Publication date: May 19, 2011
    Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
  • 2-AMINO-9-[4-(4-METHOXY-PHENOXY)-PIPERIDIN-1-YL]-4-PHENYL-INDENO[1,2-D]PYRIMIDIN-5-ONE AND ITS USE AS A HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONIST
    Publication number: 20110105540
    Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease.
    Type: Application
    Filed: October 19, 2010
    Publication date: May 5, 2011
    Inventors: Paul F. JACKSON, Mark T. Powell, Brian Christopher Shook, Alhua Wang
  • PYRAZOLO--QUINAZOLINES
    Publication number: 20110105542
    Abstract: The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C3-C7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C3-C7 cycloalkyl as substituent of a carboxamide at 3 position of the molecula framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: June 17, 2009
    Publication date: May 5, 2011
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldareli, Mauro Angiolini, Riccardo Colombo, Teresa Disingrini, Stefano Nuvoloni, Helena Posteri, Matteo Salsa, Marco Silvagni
  • HETEROARYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2A RECEPTOR ANTAGONISTS
    Publication number: 20110105494
    Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. wherein X, R2, R3, and R4 are as defined in the specification.
    Type: Application
    Filed: October 19, 2010
    Publication date: May 5, 2011
    Inventors: Paul F. JACKSON, Mark T. Powell, Brian Christopher Shook, Aihua Wang
  • COMPOSITIONS AND METHODS RELATING TO HIV PROTEASE INHIBITION
    Publication number: 20110105477
    Abstract: The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.
    Type: Application
    Filed: September 12, 2008
    Publication date: May 5, 2011
    Applicant: The Regents of the University of Michigan
    Inventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
  • ARYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS
    Publication number: 20110105492
    Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease wherein X, R2, R3, and R4 are as defined in the specification.
    Type: Application
    Filed: October 19, 2010
    Publication date: May 5, 2011
    Inventors: Paul F. Jackson, Mark T. Powell, Brian Christopher Shook, Aihua Wang
  • HETEROCYCLYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS
    Publication number: 20110105493
    Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. wherein X, R2, R3, and R4 are as defined in the specification.
    Type: Application
    Filed: October 19, 2010
    Publication date: May 5, 2011
    Inventors: Paul F. JACKSON, Mark T. Powell, Brian Christopher Shook, Aihua Wang
  • INHIBITOR OF ANALGESIC TOLERANCE
    Publication number: 20110105465
    Abstract: Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.
    Type: Application
    Filed: May 29, 2009
    Publication date: May 5, 2011
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Jun Ouchi, Shunji Kunori, Yozo Kojima, Katsumi Shinoda, Katsutoshi Sasaki, Shiro Shirakura
  • ALKYL SUBSTITUTED ARYLINDENOPYRIMIDINES AND THEIR USE AS HIGHLY SELECTIVE ADENOSINE A2a RECEPTOR ANTAGONISTS
    Publication number: 20110105541
    Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. wherein X, R2, R3, and R4 are as defined in the specification.
    Type: Application
    Filed: October 19, 2010
    Publication date: May 5, 2011
    Inventors: Paul F. Jackson, Mark T. Powell, Brian Christopher Shook, Aihua Wang
  • GABAA RECEPTOR MODULATORS
    Publication number: 20110092525
    Abstract: The resent invention relates to novel compounds of the general formula (I) having anxiolytic, anticonvulsant, sedative-hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals, including humans, as GABAA receptor modulator.
    Type: Application
    Filed: April 2, 2009
    Publication date: April 21, 2011
    Inventors: Mogens Nielsen, Tommy Liljefors, Jakob Nilsson, Olov Sterner
  • USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS
    Publication number: 20110091388
    Abstract: A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.
    Type: Application
    Filed: December 21, 2010
    Publication date: April 21, 2011
    Applicant: OMEROS CORPORATION
    Inventors: John E. Bergmann, Neil S. Cutshall, Gregory A. Demopulos, Vincent A. Florio, George A. Gaitanaris, Patrick Gray, John Hohmann, Rene Onrust, Hongkui Zeng
  • SUBSTITUTED QUINAZOLINES AND THEIR USES FOR MYEOLOPROLIFIC AND THROMBOTIC DISEASES
    Publication number: 20110086851
    Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: May 13, 2009
    Publication date: April 14, 2011
    Inventors: Bernard Golding, Richard Franklin
  • Substituted 2,3-dihydroimidazo[1,2-c]quinazoline Derivatives Useful for Treating Hyper-Proliferative Disorders and Diseases Associated with Angiogenesis
    Publication number: 20110083984
    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: December 5, 2007
    Publication date: April 14, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Martin Hentemann, Jill Wood, William Scott, Martin Michels, Ann-Marie Campbell, Ann-Marie Bullion, Bruce R. Rowley, Aniko Redman
  • COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS
    Publication number: 20110081365
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X3 is N; X4 is N Or CR3; X5 is —CR4?CR5.
    Type: Application
    Filed: February 27, 2009
    Publication date: April 7, 2011
    Applicants: IRM LLC, Novartis 35
    Inventors: Alex Cortez, Yongkai Li, Pranab Mishra, Manmohan Singh, David Skibinski, Nicholas Valiante, Tom Yao-Hsiang Wu, Xiaoyue Zhang, Yefen Zou
  • SUBSTITUTED DIHYDRO, TRIHYDRO AND TETRAHYDRO CYCLOALKYLOXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
    Publication number: 20110077257
    Abstract: The present disclosure relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I): wherein p, n, A, B, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
    Type: Application
    Filed: September 3, 2010
    Publication date: March 31, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Raymond Walter KOSLEY, JR., Rosy SHER
  • TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVES
    Publication number: 20110071170
    Abstract: A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1).
    Type: Application
    Filed: October 29, 2010
    Publication date: March 24, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Hitoshi Ohki, Tooru Okayama, Masahiro Ikeda, Masahiro Ota, Yoshihiro Shibata, Toshiyuki Nakanishi, Yasusi Ueda, Nobuyuki Suzuki, Shinji Matuura
  • IMIDAZOQUINAZOLINE DERIVATIVES AS ANAGRELIDE ANALOGUES FOR THE TREATMENT OF MYELOPROLIFIC DISEASES AND THROMBOTIC DISEASES
    Publication number: 20110071173
    Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: May 13, 2009
    Publication date: March 24, 2011
    Inventors: Bernard Golding, Richard Franklin, Angus Macleod
  • 2H- PYRIMIDO [2, 1-B] QUINAZOLIN-2-ONE DERIVATIVES AND THEIR USE AS PLATELET ANTI-AGGREGATIVE AGENTS
    Publication number: 20110071171
    Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: May 13, 2009
    Publication date: March 24, 2011
    Applicant: Shire LLC
    Inventors: Bernard Golding, Richard Franklin
  • NOVEL TRICYCLIC PROTEIN KINASE MODULATORS
    Publication number: 20110071136
    Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders.
    Type: Application
    Filed: September 16, 2010
    Publication date: March 24, 2011
    Applicant: CYLENE PHARMACEUTICALS, INC
    Inventors: Mustapha HADDACH, Fabrice PIERRE
  • SUBSTITUTED QUINAZOLINES
    Publication number: 20110071174
    Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: May 13, 2009
    Publication date: March 24, 2011
    Inventors: Bernard Golding, Richard Franklin
  • SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS
    Publication number: 20110071172
    Abstract: This invention relates to the discovery of substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim (I): and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Application
    Filed: May 13, 2009
    Publication date: March 24, 2011
    Applicant: Shire LLC
    Inventors: Bernard Golding, Richard Franklin
  • Substituted quinazolines
    Patent number: 7910597
    Abstract: This invention relates to the discovery of 3- and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: March 22, 2011
    Assignee: Shire LLC
    Inventors: Richard Franklin, Bernard T. Golding
  • COMBINATION THERAPIES COMPRISING PAR1 ANTAGONISTS WITH NAR AGONISTS
    Publication number: 20110065676
    Abstract: The present invention is directed to a pharmaceutical composition comprising an effective amount of at least one PAR1 antagonist, at least one NAR agonist, optionally, an effective amount of at least one cardiovascular agent, and, optionally, a pharmaceutically acceptable carrier. The present invention also provides for the use of theses pharmaceutical compositions to treat various diseases associated with thrombosis.
    Type: Application
    Filed: June 22, 2010
    Publication date: March 17, 2011
    Applicant: Schering Corporation
    Inventors: Michael Sidney Perelman, Madhu Chintala
  • HCV PROTEASE INHIBITORS
    Publication number: 20110065737
    Abstract: This invention relates to macrocyclic compounds of formula (I) shown in the specification. These compounds can be used to treat hepatitis C virus infection.
    Type: Application
    Filed: September 15, 2009
    Publication date: March 17, 2011
    Applicant: TaiGen Biotechnology Co., Ltd.
    Inventors: Chen-Fu Liu, Kuang-Yuan Lee, Pei-Chin Cheng, Yo-Chin Liu, Pin Lo, Kuo-Feng Tseng, Chih-Ming Chen, Chi-Hsin Richard King, Chu-Chung Lin
  • NOVEL AGENTS OF CALCIUM ION CHANNEL MODULATORS
    Publication number: 20110065703
    Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.
    Type: Application
    Filed: March 12, 2008
    Publication date: March 17, 2011
    Inventor: Jay Jie-Qiang Wu