Additional Hetero Ring Containing Patents (Class 546/256)
  • Patent number: 8779154
    Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: July 15, 2014
    Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
  • Patent number: 8779133
    Abstract: Provided are novel ligands for transition metal complexes which exhibit high coordination power with respect to metals by being free of substituents at the positions ortho to phosphorus or arsenic and which have electron-withdrawing power comparable to the highest level known in conventional ligands. One ligand includes a compound represented by General Formula (1): R1R2R3A or General Formula (2): R1R2A-Y-AR3R4 and having a total of 15 to 110 carbon atoms. In the formulae, A is phosphorus or arsenic; R1, R2, R3 and R4 are each independently a substituted pyridyl group having optionally different electron-withdrawing groups bonded to the positions meta to the atom A as well as hydrogen atoms bonded to the positions ortho to the atom A; and Y is a divalent group derived from a C2-20, optionally substituted and optionally heteroatom-containing, aliphatic, alicyclic or aromatic compound or from ferrocene.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: July 15, 2014
    Assignee: National University Corporation Okayama University
    Inventors: Toshinobu Korenaga, Takashi Sakai, Aram Ko
  • Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
  • Patent number: 8778955
    Abstract: The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods for the prophylaxis and therapy of a disease associated with an increased activity of I?B kinase comprising administering such compounds.
    Type: Grant
    Filed: June 6, 2007
    Date of Patent: July 15, 2014
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Olaf Ritzeler, Gerhard Jaehne
  • Patent number: 8778929
    Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.
    Type: Grant
    Filed: September 28, 2009
    Date of Patent: July 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
  • Publication number: 20140194443
    Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: July 10, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
  • Publication number: 20140194469
    Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: December 5, 2013
    Publication date: July 10, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
  • Publication number: 20140194441
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: January 8, 2014
    Publication date: July 10, 2014
    Applicant: Samumed, LLC
    Inventors: Sunil Kumar KC, John Hood
  • Patent number: 8772632
    Abstract: A compound for an organic photoelectric device, an organic photoelectric device including the same, and a display device including the same the compound being represented by the following Chemical Formula 1:
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: July 8, 2014
    Assignee: Cheil Industries, Inc.
    Inventors: Kyu-Yeol In, Myeong-Soon Kang, Ho-Kuk Jung, Nam-Soo Kim, Eui-Su Kang, Mi-Young Chae, Jin-Seong Park
  • Patent number: 8772496
    Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: (I) The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: July 8, 2014
    Assignee: Eli Lilly and Company
    Inventor: Pingyun Chen
  • Patent number: 8772304
    Abstract: The present invention relates to compounds of formula (IA), (IB) and (IC): and pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: October 26, 2011
    Date of Patent: July 8, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephane De Lombaert, Weimin Liu, Ho Yin Lo, Peter Allen Nemoto
  • Patent number: 8772289
    Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is A1 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: July 8, 2014
    Assignee: BASF SE
    Inventors: Thomas Schmidt, Michael Puhl, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Toni Bucci, Henry Van Tuyl Cotter, David G. Kuhn, Hassan Oloumi-Sadeghi
  • Patent number: 8771665
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 8, 2014
    Assignee: Cocrystal Discovery, Inc.
    Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Patent number: 8772320
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: July 8, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
  • Patent number: 8772495
    Abstract: Described herein is the FLAP inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, including solvates, and polymorphs thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: July 8, 2014
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: Kevin Murray Schaab, Nicholas Simon Stock
  • Publication number: 20140187780
    Abstract: The present invention discloses compounds of formula I, II or X, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
    Type: Application
    Filed: December 24, 2013
    Publication date: July 3, 2014
    Applicant: Enanta Pharmaceuticals, Inc.
    Inventors: In Jong Kim, Tongzhu Liu, Jiang Long, Guoqiang Wang, Yao-Ling Qiu, Heejin Kim, Yanchun Wang, Ly Tam Phan, Yat Sun Or
  • Patent number: 8765789
    Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: July 1, 2014
    Assignee: MSD K.K.
    Inventors: Morihiro Mitsuya, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
  • Publication number: 20140179676
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: ABBVIE INC.
    Inventors: Kevin P. Cusack, Thomas D. Gordon, Michael Z. Hoemann, David C. Ihle, Bin Li, Gloria Y. Lo Schiavo, Gagandeep K. Somal, Michael Friedman, Martin E. Hayes, Wouter Iwema Bakker
  • Publication number: 20140179702
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.
    Type: Application
    Filed: October 15, 2013
    Publication date: June 26, 2014
    Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
  • Publication number: 20140179921
    Abstract: A compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Z and Z? are joined by a single or a double bond and are ?C— or —N— provided that both are not N; Ra, R1, R2, R3, R3a, R4 and R8 are specified organic groups; n is 2, 3 or 4 and p is 0-4; or salts or N-oxides thereof.
    Type: Application
    Filed: January 6, 2014
    Publication date: June 26, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Cassayre, Peter Maienfisch, Fredrik Cederbaum, Louis-Pierre Molleyres
  • Patent number: 8759376
    Abstract: Compounds of Formula (I), pharmaceutical compositions comprising compounds of Formulae (I a) or (VII) and a method of treating a subject with an inflammatory cytokine-mediated disorder comprising administering to the subject a compound of Formulae (I a) or (VIIa). The variables of Formulae (I), (I a), (VII) and (VII a) are described herein.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: June 24, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Yousef Al-Abed, Kevin J. Tracey
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Publication number: 20140167007
    Abstract: A pyrene-based compound and an organic light-emitting diode including the pyrene-based compound are provided.
    Type: Application
    Filed: October 8, 2013
    Publication date: June 19, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jun-Ha Park, Eun-Young Lee, Chang-Ho Lee, Jong-Hyuk Lee
  • Publication number: 20140171639
    Abstract: Compounds of Formula I are useful as antagonists 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: February 24, 2014
    Publication date: June 19, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
  • Publication number: 20140171446
    Abstract: The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 3, 2012
    Publication date: June 19, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Gary Bohnert, Jun Jiang, Zhiqiang Xia
  • Patent number: 8754226
    Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: June 17, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Thomas Daniel Aicher, Josef Roland Bencsik, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Scott Alan Pratt, Ajay Singh, Timothy M. Turner, David A. Mareska, Steven Armen Boyd
  • Publication number: 20140163232
    Abstract: A method of producing an aromatic amino compound by using a primary or secondary amine compound having an aromatic ring group and a halogenated aromatic compound as starting materials, reacting the amine compound with the halogenated aromatic compound in the presence of a copper catalyst and a base so as to produce the aromatic amino compound having a structure in which an aromatic ring group derived from the halogenated aromatic compound is coupled to the amino group of the amine compound, wherein the amine compound and the halogenated aromatic compound are reacted together under a condition where an aromatic oxycarboxylic acid having a hydroxyl group and a hydroxycarbonyl group that are bonded to neighboring carbon atoms, is made present together with the copper catalyst and the base.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 12, 2014
    Applicant: HODOGAYA CHEMICAL CO., LTD.
    Inventors: Norimasa YOKOYAMA, Makoto NAGAOKA, Kazunori TOGASHI
  • Publication number: 20140162985
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: September 6, 2013
    Publication date: June 12, 2014
    Applicant: ABBVIE INC.
    Inventors: Andrew Burchat, Thomas D. Gordon, Kelly D. Mullen, David C. Ihle, Michael J. Morytko, Kevin P. Cusack, Gloria Y. Lo Schiavo, Lei Wang, Michael Friedman
  • Publication number: 20140163233
    Abstract: The present invention discloses a novel compound of Formula 1, and an organic electroluminescent device using the same. In Formula 1, X and Y independently represents an aromatic or a hetero aromatic hydrocarbon having a carbon number of from 5 to 10. Ar1 to Ar7 each independently represents an unsubstituted or substituted aromatic hydrocarbon having a carbon number of from 4 to C12, or an unsubstituted or substituted condensed polycyclic aromatic hydrocarbon having a carbon number of from 4 to 12; Ar1 to Ar7 can form an annulated or fused aromatic ring system with the adjacent aromatic hydrocarbons. When the compound of Formula I is used in the device, high luminous efficiency, longer lifetime and low driving voltage can be achieved.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 12, 2014
    Applicant: E-RAY OPTOELECTRONICS TECHONOLOGY CO., LTD.
    Inventors: Banumathy Balaganesan, Heh-Lung Huang, Po-Wei Hsu, Kun-Feng Chiang
  • Patent number: 8748618
    Abstract: This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBF?-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBF? and the CBF?-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBF?-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well selectivity for CBF?-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: June 10, 2014
    Assignee: University of Virginia Patent Foundation
    Inventors: John H. Bushweller, Jolanta Grembecka, Anuradha Illendula, Lauren Dixon
  • Patent number: 8748627
    Abstract: The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: June 10, 2014
    Assignee: AbbVie Inc.
    Inventors: Yu Gui Gu, Moshe Weitzberg, Xiangdong Xu, Richard F. Clark, Tianyuan Zhang, Qun Li, Todd M. Hansen, Hing Sham, Bruce A. Beutel, Heidi S. Camp, Xiaojun Wang
  • Patent number: 8748433
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
  • Publication number: 20140155381
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 5, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140155379
    Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 5, 2014
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
  • Publication number: 20140155401
    Abstract: The present invention relates to novel substituted 2,4?- and 3,4?-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.
    Type: Application
    Filed: February 7, 2014
    Publication date: June 5, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Peter NELL, Walter Hübsch, Barbara ALBRECHT-KÜPPER, Jörg KELDENICH, Andreas KNORR
  • Publication number: 20140155370
    Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
    Type: Application
    Filed: June 28, 2013
    Publication date: June 5, 2014
    Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
  • Publication number: 20140155602
    Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2?, R3, R3?, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: November 20, 2013
    Publication date: June 5, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Patent number: 8742097
    Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Maria-Clemencia Hernandez, Matthew C. Lucas, Andrew Thomas
  • Publication number: 20140148461
    Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: November 22, 2013
    Publication date: May 29, 2014
    Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS
  • Publication number: 20140148471
    Abstract: The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests, which include arthropods and especially insects, and to processes for preparing the novel compounds.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Reiner FISCHER, Martin FÜßLEIN, Peter JESCHKE, Adeline KÖHLER, Joachim KLUTH, Friedrich August MÜHLTHAU, Yoshitaka SATO, Arnd VOERSTE, Eiichi SHIMOJO
  • Patent number: 8735414
    Abstract: The present invention is directed to compounds and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: May 27, 2014
    Assignee: PTC Therapeutics, Inc.
    Inventors: Malcolm MacCoss, F. George Njoroge, Amin Nomeir, Guangming Chen, Song Xiao Huang, Ramesh Kakarla, Gary Mitchell Karp, William Joseph Lennox, Chunshi Li, Ronggang Liu, Yalei Liu, Christie Morrill, Steven D. Paget, Sean W Smith, James Takasugi, Anthony A. Turpoff, Hongyu Ren, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
  • Publication number: 20140141975
    Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. Novel pyridine compounds for use in controlling pests are disclosed.
    Type: Application
    Filed: November 1, 2013
    Publication date: May 22, 2014
    Applicant: Dow AgroSciences, LLC
    Inventors: Noormohamed M. Niyaz, Francis E. Tisdell, Gerald B. Watson, James M. Renga, William C. Lo, Maurice C. H. Yap
  • Publication number: 20140142097
    Abstract: Compounds of the formula (I) in which R, R1 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: April 11, 2012
    Publication date: May 22, 2014
    Applicant: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
  • Publication number: 20140142146
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Application
    Filed: November 21, 2013
    Publication date: May 22, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
  • Publication number: 20140142081
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Application
    Filed: November 21, 2013
    Publication date: May 22, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
  • Publication number: 20140142083
    Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 22, 2014
    Applicant: EPIZYME, INC.
    Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah K. Knutson, Timothy James Nelson Wigle, Masashi Seki
  • Publication number: 20140135322
    Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 15, 2014
    Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
  • Publication number: 20140135331
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 15, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
  • Patent number: 8722208
    Abstract: Disclosed is an organic electroluminescent device (organic EL device) which is improved in luminous efficiency, fully secured of high driving stability, and of a simple structure. The organic EL device is constituted of an anode, organic layers containing a phosphorescent light-emitting layer, and a cathode piled one upon another on a substrate and a phosphine oxide derivative represented by general formula (1) is contained in a phosphorescent light-emitting layer, an electron-transporting layer, a hole-blocking layer, or an exciton-blocking layer. In general formula (1), L1 is a direct bond or an aromatic group with a valence of 1-3 and Ar1 is an aromatic group. The two Ar1 groups linked to the same nitrogen atom may form a nitrogen heterocycle and may further form a fused ring together with the said nitrogen heterocycle.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: May 13, 2014
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Takahiro Kai, Hideki Tanaka, Mitsuru Suda, Toshihiro Yamamoto, Megumi Matsumoto
  • Publication number: 20140124748
    Abstract: Provided is a heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the compound of Formula 1: wherein substituents in Formula 1 above are defined as in the specification.
    Type: Application
    Filed: March 14, 2013
    Publication date: May 8, 2014
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee