The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
  • METHODS FOR INCREASING THE STABILIZATION OF HYPOXIA INDUCIBLE FACTOR-1 ALPHA
    Publication number: 20110111058
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Application
    Filed: November 5, 2010
    Publication date: May 12, 2011
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • COMPOSITIONS AND METHODS FOR TREATING COLITIS
    Publication number: 20110112055
    Abstract: Disclosed herein are compositions and methods for treating colitis and other inflammatory bowel diseases, inter alia, indeterminate colitis, Crohn's disease, irritable bowel syndrome and ischemic colitis.
    Type: Application
    Filed: November 5, 2010
    Publication date: May 12, 2011
    Inventors: Joseph H. Gardner, Robert Shalwitz
  • PYRIDAZINONES, THE PREPARATION AND THE USE THEREOF
    Publication number: 20110112061
    Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.
    Type: Application
    Filed: March 18, 2009
    Publication date: May 12, 2011
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
  • PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20110112063
    Abstract: The invention provides novel pyrimidine derivatives of formula I and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).
    Type: Application
    Filed: June 24, 2009
    Publication date: May 12, 2011
    Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
  • SUBSTITUTED 6-(1-PIPERAZINYL)-PYRIDAZINES AS 5-HT6 RECEPTOR ANTAGONISTS
    Publication number: 20110112107
    Abstract: The present invention is concerned with novel substituted 6-(1-piperazinyl)-pyridazines of Formula (I) wherein R1, R2, R3 and X have the meaning defined in the claims, having 5-HT6-antagonistic properties. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicine.
    Type: Application
    Filed: July 1, 2009
    Publication date: May 12, 2011
    Inventors: José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Michiel Luc Maria Van Gool, Susana Conde-Ceide, Francisca Delgado-Jiménez
  • Substituted Pyridazinone Derivatives as Histamine-3 (H3) Receptor Ligands
    Publication number: 20110098269
    Abstract: The present invention provides compounds according to Formulas I, II, III, IV, V, VI, VII or VIII: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
    Type: Application
    Filed: November 17, 2010
    Publication date: April 28, 2011
    Applicant: Cephalon, Inc.
    Inventors: Nadine C. Becknell, Reddeppa reddy Dandu, Derek D. Dunn, Robert L. Hudkins, Kurt A. Josef, Babu G. Sundar, Allison L. Zulli
  • Gem-Disubstituted and Spirocyclic Amino Pyridines/Pyrimidines as Cell Cycle Inhibitors
    Publication number: 20110097305
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-me-dialed disorders, such as cancer. The subject compounds arc gem-disubstituted or spimcyclic pyridine, pyrimidine and triazine derivatives.
    Type: Application
    Filed: April 6, 2009
    Publication date: April 28, 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
  • Novel Compounds As Casein Kinase Inhibitors
    Publication number: 20110098272
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: October 25, 2010
    Publication date: April 28, 2011
    Inventors: Chakrapani Subramanyam, Travis T. Wager
  • ORGANIC COMPOUNDS
    Publication number: 20110092505
    Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
    Type: Application
    Filed: June 12, 2009
    Publication date: April 21, 2011
    Inventors: Robin Burgis, Michael Paul Capparelli, Lucian Dipietro, Gabriel G. Gamber, Charles Francis Jewell, JR., Erik Meredith, Karl Miranda, Lauren G. Monovich, Chang Rao, Nicolas Soldermann, Taeyoung Yoon, Qingming Zhu
  • Diamino-pyridine, pyrimidine, and pyrazine modulators of the histamine H4 receptor
    Publication number: 20110092474
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: June 11, 2009
    Publication date: April 21, 2011
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
  • Aza-pyridopyrimidinone derivatives
    Patent number: 7928106
    Abstract: The invention is concerned with novel aza-pyridopyrimidinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, X1, X2, X3, Y, Z, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used in treating or preventing diseases which are modulated by HM74A agonists.
    Type: Grant
    Filed: March 17, 2008
    Date of Patent: April 19, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Aurelia Conte, Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Holger Kuehne, Robert Narquizian, Constantinos G. Panousis, Jens-Uwe Peters, Fabienne Ricklin
  • PIPERAZINYL OXOALKYL TETRAHYDROISOQUINOLINES AND RELATED ANALOGUES
    Publication number: 20110082130
    Abstract: Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
    Type: Application
    Filed: August 23, 2010
    Publication date: April 7, 2011
    Applicant: LIGAND PHARMACEUTICALS, INC.
    Inventors: Yang Gao, Bingsong Han, Yuelian Xu, Timothy M Caldwell, Linghong Xie
  • THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN
    Publication number: 20110082152
    Abstract: A compound of formula: wherein Ar, Ar1, Ar2, R3, R4, R5, R6, R13, m, t, and x are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Hydroxyiminopiperazine Compound”); compositions comprising an effective amount of a Hydroxyiminopiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Hydroxyiminopiperazine Compound are disclosed.
    Type: Application
    Filed: November 10, 2010
    Publication date: April 7, 2011
    Applicant: Purdue Pharma L.P.
    Inventors: Qun Sun, Xiaoming Zhou
  • NEW COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS
    Publication number: 20110082137
    Abstract: The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V—W?*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.
    Type: Application
    Filed: March 30, 2010
    Publication date: April 7, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Riccardo GIOVANNINI, Cornelia DORNER-CIOSSEK, Christian EICKMEIER, Dennis FIEGEN, Thomas FOX, Klaus FUCHS, Niklas HEINE, Holger ROSENBROCK, Gerhard SCHAENZLE
  • Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes
    Patent number: 7919496
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, G, J, K, L, M, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: April 5, 2011
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Vishnumurthy Kodumuru, Shifeng Liu, Shaoyi Sun, Nagasree Chakka
  • IMIDAZOPYRIDINE AND RELATED ANALOGS AS SIRTUIN MODULATORS
    Publication number: 20110077248
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: May 28, 2009
    Publication date: March 31, 2011
    Inventors: Chi B. Vu, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • PYRIDYL DERIVATIVES, THEIR PREPARATION AND USE
    Publication number: 20110077252
    Abstract: The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1? (HIF-1?) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1? pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-?.
    Type: Application
    Filed: August 6, 2008
    Publication date: March 31, 2011
    Inventors: Sanjay Kumar, Kalpana Sanjay Joshi, Vijaykumar Deore, Mandar Ramesh Bhonde, Nilambari Nilkanth Yewalkar, Amol Arun Padgaonkar, Asha Adrian Kulkarni-Almeida, Maggie Joyce Rathos, Sapna Parikh, Nilesh Madhukar Dagia
  • Urotensin II receptor antagonists
    Patent number: 7915260
    Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: March 29, 2011
    Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
  • PYRIDAZINYL AMINE DERIVATIVES, THE USE THEREOF IN THE PREPARATION OF PICORNA VIRUS INHIBITORS
    Publication number: 20110059978
    Abstract: The present invention relates to substituted pyridazinylamine derivatives of the formula I or pharmaceutically acceptable salts or hydrates thereof, wherein the substituents are defined as in the description, their preparation process, pharmaceutical compositions comprising them, and uses of the said compounds as picorna virus inhibitors for prevention and/or treatment of diseases caused by picorna viruses.
    Type: Application
    Filed: November 15, 2010
    Publication date: March 10, 2011
    Inventors: Song LI, Chunlai MI, Zhibing ZHENG, Guoming ZHAO, Xinbo ZHOU, Zehui GONG
  • QUINOLINE COMPOUNDS AND METHODS OF USE
    Publication number: 20110053931
    Abstract: Compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof, are useful for inhibiting receptor tyrosine kinases and for treating hyperproliferative disorders mediated thereby. Methods of using compounds of Formula (I), and stereoisomers, geometric isomers, tautomers, solvates 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: Application
    Filed: June 8, 2007
    Publication date: March 3, 2011
    Inventors: John Gaudino, Steven Armen Boyd, Allison L. Marlow, Tomas Kaplan, Kin Chiu Fong, Jeongbeob Seo, Hongqi Tian, James Blake, Kevin Koch
  • NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
    Publication number: 20110046134
    Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
    Type: Application
    Filed: October 29, 2010
    Publication date: February 24, 2011
    Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
  • Pyrimidylmethyl Sulfonamide Compounds
    Publication number: 20110039693
    Abstract: The present invention relates to pyrimidin-4-ylmethyl-sulfonamides of formula (I) wherein Ra, n, R, A, Y and Het are as defined in the claims and to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to a process for preparing these compounds.
    Type: Application
    Filed: February 10, 2009
    Publication date: February 17, 2011
    Applicant: BASF SE
    Inventors: Jan Klaas Lohmann, Alice Glaettu, Wassilios Grammenos, Jurith Montag, Bernd Mueller, Marianna Vrettou-Schultes, Jens Renner, Sarah Ulmschneider, Michael Rack, Jochen Dietz
  • Leukemia Treatment
    Publication number: 20110039850
    Abstract: A combination of a BCR-ABL inhibitor and a hedgehog pathway inhibitor for the treatment of leukemia.
    Type: Application
    Filed: August 12, 2009
    Publication date: February 17, 2011
    Inventors: Mhairi Copland, Marion Dorsch, David Irvine, Paul W. Manley, Stefan Peukert
  • Organic compounds
    Patent number: 7888351
    Abstract: The present invention relates to compounds of the formula; and their use in therapy.
    Type: Grant
    Filed: April 10, 2007
    Date of Patent: February 15, 2011
    Assignee: Novartis AG
    Inventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
  • PYRIDAZINONE DERIVATIVES
    Publication number: 20110034474
    Abstract: Compounds of the formula (I), in which R1, R2, R3, W and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: March 24, 2009
    Publication date: February 10, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • N-SUBSTITUTED HYDROXYPYRIMIDINONE CARBOXAMIDE INHIBITORS OF HIV INTEGRASE
    Publication number: 20110034449
    Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Application
    Filed: September 17, 2010
    Publication date: February 10, 2011
    Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
  • PYRIDAZINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS IN THE TREATMENT OF SKIN DISORDERS
    Publication number: 20110021530
    Abstract: Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human, including administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein, and compositions including a compound of formula (I).
    Type: Application
    Filed: February 19, 2009
    Publication date: January 27, 2011
    Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AG
    Inventors: Andreas Billich, Michael D. Winther, Yigal Paul Goldberg, Gesine Winzenburg, Karin Rapp, Andreas Fritze
  • PYRIDAZINE DERIVATIVES AS FACTOR XIA INHIBITORS
    Publication number: 20110021492
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein the variables A, L1, L2, R2, R11, and M are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: March 12, 2009
    Publication date: January 27, 2011
    Inventors: James R. Corte, Zilun HU, Mimi L. Quan
  • SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS
    Publication number: 20110003825
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Application
    Filed: August 23, 2010
    Publication date: January 6, 2011
    Applicant: Schering Corporation
    Inventors: Ying Huang, Guoqing Li, Andrew W. Stamford
  • Anti-Inflammatory And Protein Kinase Inhibitor Compositions And Related Methods For Downregulation Of Detrimental Cellular Responses And Inhibition Of Cell Death
    Publication number: 20100317665
    Abstract: A novel class of pyridazine compositions and related methods of use.
    Type: Application
    Filed: July 7, 2010
    Publication date: December 16, 2010
    Inventors: D.M. Watterson, Anastasia Velentza, Magdalena Zasadzki, Jacques Halech, Jean-Jacques Bourguignon, Anu R. Sawkar, Thomas J. Lukas, Salida Mirzoeva, Linda J. Van Eldik, Marcel Hibert
  • Amide compound
    Patent number: 7851473
    Abstract: There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I0): wherein Z is oxygen or sulfur; R1 is aryl which may be substituted, or a heterocyclic group which may be substituted; R1a is a hydrogen atom, a hydrocarbon group which may be substituted, hydroxyl, etc.; R2 is piperidin-1,4-diyl which may be substituted, or piperazin-1,4-diyl which may be substituted; R3 is a group formed by eliminating two hydrogen atoms from a 5-membered aromatic heterocyclic group having 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, which may be further substituted, —CO—, etc.; and R4 is a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; or a salt thereof.
    Type: Grant
    Filed: November 17, 2005
    Date of Patent: December 14, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Matsumoto, Masakuni Kori, Junichi Miyazaki, Yoshihiro Kiyota
  • Methods of using 4-Phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-Based Compounds
    Publication number: 20100311764
    Abstract: Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:
    Type: Application
    Filed: April 5, 2010
    Publication date: December 9, 2010
    Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
  • Methods for the use of pyrimidine derivatives which are antagonists of vitronectin receptor
    Patent number: 7846932
    Abstract: A subject of the invention is the compounds of formula (I); in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: December 7, 2010
    Assignee: Galapagos SAS
    Inventors: Jean-Michel Lefrancois, Bertrand Heckmann
  • N-BENZYL-4-METHYLENEAMINO-3-HYDROXY-2-PYRIDONES
    Publication number: 20100305097
    Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.
    Type: Application
    Filed: July 28, 2010
    Publication date: December 2, 2010
    Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
  • HETEROCYCLE-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES
    Publication number: 20100305102
    Abstract: The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO2, but preferably SO, and wherein R3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl and wherein R1 and R2 have the meanings stated in claim 1, as well as pharmaceutical compositions which contain these compounds. These new dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.
    Type: Application
    Filed: October 16, 2008
    Publication date: December 2, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
  • Pharmaceutical Compositions for the Treatment of Pain
    Publication number: 20100305086
    Abstract: This invention discloses a method of treatment of osteoarthritis pain by administration of a composition containing a nicotinic acetylcholine receptor ligand and a nicotinic acetylcholine receptor subtype ?4?2 allosteric modulator. The present application also relates to compositions comprising such compounds for use in treating pain and related disorders mediated by controlling neurotransmitter release in a subject.
    Type: Application
    Filed: May 26, 2010
    Publication date: December 2, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Murali Gopalakrishnan, Chih-Hung Lee, Jianguo Ji, Tao Li, Kevin B. Sippy
  • N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
    Publication number: 20100298334
    Abstract: The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I: which are JAK inhibitors, such as selective JAK1 inhibitors, useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Application
    Filed: May 21, 2010
    Publication date: November 25, 2010
    Inventors: James D. Rodgers, Stacey Shepard, Argyrios G. Arvanitis, Haisheng Wang, Louis Storace, Beverly Folmer, Lixin Shao, Wenyu Zhu, Joseph Glenn
  • TRICYCLIC COMPOUNDS HAVING CORTICOTROPIN-RELEASING FACTOR ANTAGONISTIC ACTIVITY AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20100298287
    Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.
    Type: Application
    Filed: January 21, 2009
    Publication date: November 25, 2010
    Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
  • 4- [3- (4-CYCLOPROPANECARBONYL-PIPERAZINE-I-CARBONYL) -4 -FLUORO-BENZYL] -2H-PHTHALAZ IN-1-ONE
    Publication number: 20100286157
    Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form L, methods of obtaining form L, pharmaceutical compositions comprising Form L and methods of using Form L and compositions comprising Form L.
    Type: Application
    Filed: October 17, 2008
    Publication date: November 11, 2010
    Applicant: KUDOS PHARMACEUTICALS LIMITED
    Inventors: Kathryn Anne Quigley, Ezra John Still, Leonard Jesse Chyall
  • DIHYDROPYRIMIDINONES
    Publication number: 20100286158
    Abstract: This invention relates to dihydropyrimidinones of the formula wherein X and R1 to R7 are as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
    Type: Application
    Filed: April 30, 2010
    Publication date: November 11, 2010
    Inventors: David Banner, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Fabienne Ricklin, Mark Rogers-Evans
  • Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase
    Patent number: 7829712
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: November 9, 2010
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Serguei Sviridov, Sultan Chowdhury, Vishnumurthy Kodumuru
  • 2-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS
    Publication number: 20100280030
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: May 8, 2008
    Publication date: November 4, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
  • Pyrimidine derivatives which are antagonists of vitronectin receptor
    Patent number: 7825119
    Abstract: A subject of the invention is the compounds of formula (I): in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparation process, their use as medicaments having an antagonist activity on the vitronectin receptor and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: May 13, 2005
    Date of Patent: November 2, 2010
    Assignee: Galapagos SAS
    Inventors: Jean-Michel Lefrancois, Bertrand Heckmann
  • 2-BENZYLPYRIDAZINONE DERIVATIVES AS MET KINASE INHIBITORS
    Publication number: 20100273796
    Abstract: Compounds of the formula I in which R1, R2, R3, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: November 25, 2008
    Publication date: October 28, 2010
    Applicant: Merck Patent Gesellschaft MIT Beschrankter Haftung
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat
  • PYRIDAZINE DERIVATIVES USEFUL AS FUNGICIDES AND FOR THE TREATMENT OF CANCER
    Publication number: 20100273804
    Abstract: The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: formula (I) wherein R1 is C1-C6alkyl, C1-C6haloalkyl or C3-C6cycloalkyl; R2 is hydrogen or an optionally substituted alkyl, aryl or heteroaryl; R3 is hydrogen, C1-C6alkyl or C1-C6haloalkyl; R4 is hydrogen, C1-C6alkyl or C1-C6haloalkyl; or R3 and R4 together can be part of a carbocyclic or heterocyclic 3- to 8-membered ring; R5 is optionally substituted aryl or heteroaryl; and R6 is hydroxy, halogen, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylthio or C1-C6haloalkylthio; or an agrochemically usable salt form thereof.
    Type: Application
    Filed: December 19, 2008
    Publication date: October 28, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Clemens Lamberth, Stephan Trah, Raphael Dumeunier, Sebastian Volker Wendeborn
  • 2-substituted pyrimidines and their use as pesticides
    Patent number: 7820647
    Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents L and R1 to R3 are as defined in the description and X is a group —CH—Ra, —N—Rb—, —O— or —S—; Ra may be hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, cyano or C1-C6-alkoxycarbonyl; Rb is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; T is a group —CH—Ra—; p is an integer from 1 to 4; Y is a group —CH—Ra— or —N—Rb—, o is 0 or 1; Z is O, S or a group N(Rc) Rc is hydrogen, C1-C6-alkyl or C1-C6-alkoxy, and to processes for their preparation, to pesticidal compositions comprising them and to their use as pesticides.
    Type: Grant
    Filed: May 17, 2005
    Date of Patent: October 26, 2010
    Assignee: BASF Aktiengesellschaft
    Inventors: Anja Schwögler, Frank Schieweck, Joachim Rheinheimer, Markus Gewehr, Bernd Müller, Thomas Grote, Wassilios Grammenos, Udo Hünger, Carsten Blettner, Peter Schäfer, Oliver Wagner, Reinhard Stierl, Ulrich Schöfl, Siegfried Strathmann, Maria Scherer
  • Heterocyclic H3 Antagonists
    Publication number: 20100267721
    Abstract: Compound of formula (I) wherein W, X, Y, Z is —C(R?)? or N; R1 is hydrogen or alkyl, V is N or C (i.e.
    Type: Application
    Filed: May 19, 2008
    Publication date: October 21, 2010
    Applicant: HIGH POINT PHARMACEUTICALS LLC
    Inventors: Rolf Hohlweg, Jane Marie Lundbeck, Johannes Cornelis de Jong
  • Compounds, Compositions and Methods Comprising Pyridazine Derivatives
    Publication number: 20100267706
    Abstract: The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1 or 2 or encompassed by formulas I, Ia, II, III, and IV) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Application
    Filed: April 20, 2010
    Publication date: October 21, 2010
    Inventors: Michael Geoffrey Neil Russell, Stephen David Penrose, Kevin James Doyle
  • PYRIDAZINONE DERIVATIVES AS PARP INHIBITORS
    Publication number: 20100261709
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinaldamage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.
    Type: Application
    Filed: November 14, 2008
    Publication date: October 14, 2010
    Inventors: Danila Branca, Gabriella Dessole, Federica Ferrigno, Philip Jones, Olaf Kinzel, Samuele Lillini, Ester Muraglia, Giovanna Pescatore, Carsten Schultz-Fademrecht
  • 2-(HETEROCYCLYLBENZYL)PYRIDAZINONE DERIVATIVES
    Publication number: 20100261697
    Abstract: Compounds of the formula (I) in which R1, R2, R3, R4 and R5 have the meanings indicated in claim 1 are inhibitors of tyrosine kinases, in particular of met kinase and can be employed inter alia for the treatment of tumours.
    Type: Application
    Filed: July 12, 2007
    Publication date: October 14, 2010
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber