Ring Oxygen In The Bicyclo Ring System Patents (Class 546/115)
  • Patent number: 9988396
    Abstract: Provided are an oxaziridine compound showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, and a production method thereof. A compound represented by the formula 1: wherein X is a single bond, —C(H)(R6)— or —C(H)(R7)—C(H)(R8)—; and R1-R8 are each independently a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, or a salt thereof.
    Type: Grant
    Filed: January 26, 2017
    Date of Patent: June 5, 2018
    Assignee: SEED RESEARCH INSTITUTE CO., LTD.
    Inventors: Teruhiko Ishikawa, Morita Iwami
  • Patent number: 9938284
    Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: April 10, 2018
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
  • Patent number: 9609870
    Abstract: The invention relates to isoxazolo[5,4-b]pyridine compounds of formula I, to the agriculturally useful salts of isoxazolo[5,4-b]pyridine compounds of formula I, and to their use as herbicides.
    Type: Grant
    Filed: August 17, 2015
    Date of Patent: April 4, 2017
    Assignee: BASF SE
    Inventors: Anna Aleksandra Michrowska-Pianowska, Julia Major, Johannes Hutzler, Trevor William Newton, Richard Roger Evans, Klaus Kreuz, Klaus Grossmann, Dschun Song, Anja Simon, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Helmut Kraus, Thomas Seitz, Andree van der Kloet, Ruediger Reingruber
  • Patent number: 9545416
    Abstract: The present invention relates to pharmaceutical compositions and combination therapies for treating patients having a neoplasm or a proliferative disorder, the combination comprises an inhibitor of the e1F4E gene product, such as ribavirin, and a chemotherapeutic agent, such as cytarabine, wherein said combination therapy overcomes resistance developed in patients during anti-neoplastic treatment. The present invention also provides for the use of a combination therapy for treating patients having a neoplasm, a proliferative disorder, pre-neoplasm or a precancerous lesion, comprising an inhibitor of the e1F4E gene product, a chemotherapeutic agent, and a therapeutically effective amount of a hedgehog pathway inhibitor, such as GDC-0449; and the method of using said combination therapy.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: January 17, 2017
    Assignee: Universite de Montreal
    Inventors: Katherine Borden, Hiba Zahreddine, Biljana Culjkovic Kraljacic
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Patent number: 9034896
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene) Heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 21, 2014
    Date of Patent: May 19, 2015
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
  • Publication number: 20150133446
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, Rx, R1, R2, R3, X1, X2 and s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 14, 2015
    Inventors: R. Michael Lawrence, Michael M. Miller, Dietmar Alfred Seiffert, Shoshana L. Posy, Pancras C. Wong, Jacques Banville, Edward H. Ruediger, Daniel H. Deon, Alain Martel, François Tremblay, Julia Guy, Jean-François Lavallée, Marc Gagnon
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Patent number: 9018134
    Abstract: There is provided a compound having an excellent controlling effect on pests represented by the formula (1): wherein, A1 represents —NR7—, etc., A2 represents a nitrogen atom, etc., A3 represents a nitrogen atom, etc., R1 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R2, R3 and R4 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more halogen atoms, etc., R5 and R6 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R7 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group W, etc., n represents 0, 1 or 2, or an N-oxide thereof.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: April 28, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masaki Takahashi, Takamasa Tanabe, Mai Ito, Yoshihiko Nokura, Atsushi Iwata
  • Patent number: 9018209
    Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: April 28, 2015
    Assignee: Yale University
    Inventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
  • Patent number: 9012456
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, and A are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: April 21, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Bernd Nosse
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Patent number: 9006440
    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: Grant
    Filed: July 29, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Patent GmbH
    Inventors: Lars Burgdorf, Melanie Schultz, Tatjana Ross, Brian Hodous, Justin Potnick, Amanda E. Sutton, Bayard R. Huck
  • Patent number: 9006442
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: April 14, 2015
    Assignee: Lupin Limited
    Inventors: Sanjeev Anant Kulkarni, Sachin Madan, Nirmal Kumar Jana, Prashant Vitthalrao Tale, Narasimha Murthy Cheemala, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Chaitanya Prabhakar Kulkarni, Sapana Suresh Patel, Amolsing Dattu Patil, Seema Prabhakar Zade, Rohan Mahadev Shinde, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 8975407
    Abstract: The present application is related to compounds represented by Formula I, which are novel allosteric modulators of ?7nAChR.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 10, 2015
    Assignee: Anvyl LLC
    Inventor: Richard Kanner
  • Patent number: 8975277
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LQ and Ar are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: March 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf
  • Patent number: 8975235
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 10, 2015
    Assignee: InterMune, Inc.
    Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Publication number: 20150065497
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: March 5, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Publication number: 20150057265
    Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Yun-Long Li, David M. Burns, Hao Feng, Taisheng Huang, Song Mei, Jun Pan, Oleg Vechorkin, Hai-Fen Ye, Wenyu Zhu, Maria Rafalski, Anlai Wang, Chu-Biao Xue
  • Publication number: 20150057268
    Abstract: Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor.
    Type: Application
    Filed: December 6, 2012
    Publication date: February 26, 2015
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Scott Runyon, Yanan Zhang, Carla Hassler, Brian Gilmour
  • Patent number: 8962651
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: February 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kyle J. Eastman, Kyle E. Parcella, John F. Kadow
  • Patent number: 8957062
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: February 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
  • Patent number: 8952873
    Abstract: Provided are a fused polycyclic compound suitable for use mainly as a component for a blue-light-emitting device, and an organic light-emitting device using the compound. The fused polycyclic compound is represented by the general formulae (1), (2), (8) and (9).
    Type: Grant
    Filed: May 1, 2012
    Date of Patent: February 10, 2015
    Assignee: Canon Kabushiki Kaisha
    Inventors: Hiroki Ohrui, Hironobu Iwawaki, Kei Tagami, Masanori Muratsubaki, Ryuji Ishii
  • Publication number: 20150038502
    Abstract: The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: October 19, 2012
    Publication date: February 5, 2015
    Inventors: Dansu Li, Anthony J. Roecker
  • Publication number: 20150038332
    Abstract: The invention relates to isoxazolo[5,4-b]pyridine compounds of formula I, to the agriculturally useful salts of isoxazolo[5,4-b]pyridine compounds of formula I, and to their use as herbicides.
    Type: Application
    Filed: January 4, 2013
    Publication date: February 5, 2015
    Applicant: BASF SE
    Inventors: Anna Aleksandra Michrowska-Pian, Markus Kordes, Johannes Hutzler, Trevor William Newton, Richard Roger Evans, Klaus Kreuz, Klaus Grossmann, Thomas Seitz, Andree van der Kloet, Matthias Witschel, Liliana Parra Rapado, Jens Lerchl
  • Publication number: 20150038527
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: February 5, 2015
    Applicant: Merck Patent GmbH
    Inventors: Lars Burgdorf, Tatjana Ross, Carl Deutsch
  • Publication number: 20150031668
    Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 29, 2015
    Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, James Brown, Wenge Zhong, Thomas T. Nguyen
  • Publication number: 20150025075
    Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, X and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: January 18, 2013
    Publication date: January 22, 2015
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Kurt Hilpert, Francis Hubler, Thierry Kimmerlin, Dorte Renneberg, Simon Stamm
  • Patent number: 8927557
    Abstract: The compounds of Formula (I), wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: January 6, 2015
    Assignee: Takeda GmbH
    Inventors: Josef Stadlwieser, Beate Schmidt, Heiko Bernsmann, Torsten Dunkern, Ewald Benediktus, Andreas Pahl, Ragna Hussong, Olaf Nimz, Matthias Mueller, Martin Viertelhaus
  • Publication number: 20150005284
    Abstract: Compounds of the formula I in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: January 3, 2013
    Publication date: January 1, 2015
    Applicant: Merck Patent GmbH
    Inventors: Hans Michael Eggenweiler, Guenter Hoelzemann, Dieter Dorsch
  • Patent number: 8916584
    Abstract: Benzisoxazole and azabenzisoxazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: December 23, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Darren W. Engers
  • Publication number: 20140364455
    Abstract: The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.
    Type: Application
    Filed: June 10, 2014
    Publication date: December 11, 2014
    Inventors: Matthew BIO, Sebastien CAILLE, Brian COCHRAN, Yuanqing FANG, Brian M. FOX, Brian S. LUCAS, Lawrence R. McGEE, Filisaty VOUNATSOS, Sean WIEDEMANN, Sarah WORTMAN
  • Publication number: 20140364444
    Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Hayato TAKYO, Masaki TAKAHASHI, Takamasa TANABE, Yoshihiko NOKURA, Mai ITO, Atsushi IWATA
  • Patent number: 8889868
    Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: November 18, 2014
    Assignee: Syntarga BV
    Inventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgersma, Wiro Michaël Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus de Groot
  • Publication number: 20140323721
    Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
    Type: Application
    Filed: November 21, 2012
    Publication date: October 30, 2014
    Inventors: Pingda Ren, Liansheng Li, Katrina Chan
  • Publication number: 20140309237
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Patent number: 8859529
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Patent number: 8853238
    Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: October 7, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
  • Patent number: 8853239
    Abstract: The present invention relates to compounds of formula I, wherein R1, LP, LQ, X, A, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: October 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf
  • Publication number: 20140294805
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: September 2, 2011
    Publication date: October 2, 2014
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
  • Publication number: 20140275154
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Kyle J. Eastman, Kyle E. Parcella, John F. Kadow
  • Publication number: 20140275155
    Abstract: This invention relates to bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias GRAUERT, Ralf ANDERSKEWITZ, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
  • Publication number: 20140274926
    Abstract: The present invention provides compounds of Formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: IRM LLC
    Inventors: Arnab Kumar CHATTERJEE, Fang LIANG, Casey Jacob Nelson MATHISON, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh NAGLE, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL
  • Publication number: 20140242135
    Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: April 25, 2012
    Publication date: August 28, 2014
    Applicant: Vanderbilt University
    Inventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
  • Publication number: 20140243302
    Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 28, 2014
    Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
  • Patent number: 8809535
    Abstract: Substituted pyridines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: August 19, 2014
    Assignee: BASF SE
    Inventors: Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska-Pianowska, Anja Simon, Ruediger Reingruber, Helmut Kraus, Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Hans Wolfgang Hoeffken, Thomas Mietzner
  • Publication number: 20140228377
    Abstract: A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which acts relying on an orexin (OX) receptor antagonistic activity and is useful for the treatment or prevention of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, head ache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases and hypertension.
    Type: Application
    Filed: July 4, 2012
    Publication date: August 14, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Masahito Abe, Aya Futamura, Ryo Suzuki, Dai Nozawa, Hiroshi Ohta, Yuko Araki
  • Publication number: 20140228395
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 21, 2014
    Publication date: August 14, 2014
    Applicant: Allergan, Inc.
    Inventors: SANTOSH C. SINHA, LIMING WANG, KEN CHOW, MOHAMMED I. DIBAS, MICHAEL E. GARST