Unsaturated Hetero Ring Attached Directly To The Quinoline Ring System By Nonionic Bonding Patents (Class 546/167)
  • Patent number: 10239844
    Abstract: The present invention relates to disubstituted triazoles, their synthesis, and their use as anti-cancer compounds. In particular, compounds of Formula (I) are provided.
    Type: Grant
    Filed: March 1, 2018
    Date of Patent: March 26, 2019
    Assignee: BioVentures, LLC
    Inventors: Nikhil Reddy Madadi, Narsimha Reddy Penthala, Peter Crooks, Leena Maddukuri, Robert Eoff
  • Patent number: 9796679
    Abstract: Compounds for inhibiting Type 4 Prepilin Peptidases are provided as are methods of using the compounds as anti-bacterial agents.
    Type: Grant
    Filed: February 9, 2015
    Date of Patent: October 24, 2017
    Assignee: TRUSTEES OF DARTMOUTH COLLEGE
    Inventors: Ronald K. Taylor, Gordon W. Gribble
  • Patent number: 9062000
    Abstract: The present disclosure relates to a bis-quinaldine compound of formula I and a process for the same. wherein R2 is a substituent selected from the group consisting of H, C1-C20 straight or branched chain alkyl substituents, aromatic substituents, aliphatic substituents, combinations thereof and the like.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: June 23, 2015
    Inventor: Keki Hormusji Gharda
  • Publication number: 20150148377
    Abstract: The invention relates to quinoline compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, W, U, Q, R1, R5 R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 28, 2015
    Applicant: NOVARTIS AG
    Inventors: Klemens Hogenauer, Konstanze Hurth, Christoph Kalis, Henrik Moebitz, Nicolas Soldermann, Frederic Zecri
  • 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
  • Publication number: 20150133656
    Abstract: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 14, 2015
    Applicants: CARNA BIOSCIENCES INC., NATIONAL CANCER CENTER
    Inventors: Masaaki Sawa, Hideki Moriyama, Tesshi Yamada, Miki Shitashige, Yusuke Kawase, Yuko Uno
  • Patent number: 9029540
    Abstract: Disclosed are novel ruthenium compounds of formula (Ia) and (Ib): wherein R1 and the moiety are defined herein. Also disclosed is a process for using these novel ruthenium compounds as catalysts for asymmetric hydrogenation and transfer hydrogenation of ketones with high reactivities and excellent selectivities.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: May 12, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Nizar Haddad, Heewon Lee, Bo Qu, Sonia Rodriguez, Chris Hugh Senanayake
  • Patent number: 9028728
    Abstract: The present invention relates to photochromic materials that include one or more indeno-fused naphthopyrans that have particular groups at the 7, 11, and 13 positions thereof, and at the position alpha to the oxygen of the pyran ring thereof. With some embodiments, hydrogen or an alkoxy group is bonded to the 7 position, an optionally substituted phenyl is bonded to the 11 position, two alkyl groups are bonded to the 13 position, and two optionally substituted phenyl groups are bonded to the position alpha to the oxygen of the pyran ring of the indeno-fused naphthopyran compound. The 13 position of the indeno-fused naphthopyrans is free of ether groups in which an ether oxygen is bonded to the 13 position, and hydroxyl. The present invention also relates to photochromic articles and compositions that include such indeno-fused naphthopyrans.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Transitions Optical, Inc.
    Inventors: Kevin E. Bancroft, Anu Chopra, Xiao-Man Dai, Beon-Kyu Kim, David B. Knowles, Jason R. Lewis, Victor A. Montes, Stephen D. Straight, Massimiliano Tomasulo, Barry Van Gemert, Robert W. Walters, Wenjing Xiao, Huayun Yu, Elizabeth A. Zezinka
  • Patent number: 9029392
    Abstract: Disclosed are a series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: May 12, 2015
    Assignee: UCB Pharma S.A.
    Inventors: Andrew Harry Parton, Mezher Hussein Ali, Daniel Christopher Brookings, Julien Alistair Brown, Daniel James Ford, Richard Jeremy Franklin, Judi Charlotte Neuss, Joanna Rachel Quincey, Jackalyn Hinkins
  • Publication number: 20150118703
    Abstract: The present invention provides a category of cyano-substituted asymmetric cyanine dyes having the following general structural Formula I and its synthesizing method. The cyano-substituted asymmetric cyanine dyes in present invention are easily synthesized and have long emission wavelength, high molar extinction coefficient, high sensitivity, good light stability, high fluorescence quantum yield after binding with nucleic acid, and low cell toxicity, which is beneficial for application as fluorescent dyes and could also be used in the field of identifying nucleic acid molecules, clinical diagnostics, and immunoassay testing etc.
    Type: Application
    Filed: September 15, 2014
    Publication date: April 30, 2015
    Inventors: Xiaojun PENG, SI ZHANG, JIANGLI FAN, JINGYUN WANG
  • Publication number: 20150105404
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Publication number: 20150094284
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: December 3, 2014
    Publication date: April 2, 2015
    Inventors: Jean-Luc GIRARDET, Yung-Hyo KOH, Martha DE LA ROSA, Esmir GUNIC, Zhi HONG, Stanley LANG, Woo-Hong KIM
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Patent number: 8993595
    Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula Ia or Ib, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Michel Derock, Frederic Leroy, Jean-Christophe Meillon, Thierry Convard, Dominique Surleraux
  • Patent number: 8980918
    Abstract: The invention relates to a stable amorphous form of (5-Fluoro-2-methyl-3-quinolin-2-ylmethyl-indol-1-yl)-acetic acid and its use in the treatment of conditions mediated by the action of PGD2 at the CRTH2 receptor.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 17, 2015
    Assignee: Atopix Therapeutics Limited
    Inventors: Aimesther Betancourt, Marc Lemieux, Roch Thibert
  • Publication number: 20150060787
    Abstract: Provided is a compound represented by Formula 1, Formula 2, or Formula 3:
    Type: Application
    Filed: May 21, 2014
    Publication date: March 5, 2015
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Jun-Ha PARK, Seok-Hwan HWANG, Young-Kook KIM, Hye-Jin JUNG, Eun-Young LEE, Jong-Woo KIM, Jin-O LIM, Sang-Hyun HAN, Eun-Jae JEONG, Soo-Yon KIM
  • Publication number: 20150057218
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 26, 2015
    Inventors: Min ZHONG, Leping LI
  • Publication number: 20150038437
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 5, 2015
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, John David Baird, Guangming Chen, Olya Ginzburg, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
  • Patent number: 8933074
    Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: January 13, 2015
    Assignee: FORUM Pharmaceuticals Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Patent number: 8927551
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: January 6, 2015
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Patent number: 8927709
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20140367657
    Abstract: A heterocyclic compound, an organic light-emitting device, and a flat panel display apparatus, the compound being represented by Formula 1, below:
    Type: Application
    Filed: January 29, 2014
    Publication date: December 18, 2014
    Applicants: PUSAN NATIONAL UNIVERSITY INDUSTRY-UNIVERSITY COOPERATION FOUNDATION, Samsung Display Co., Ltd.
    Inventors: Jae-Hong KIM, Myeong-Suk KIM, Soung-Wook KIM, Hong-Suk SUH, Jin-Soo HWANG
  • Patent number: 8912181
    Abstract: A novel bicyclic compound having an HSP90 inhibitory effect and a carcinostatic effect. A pharmaceutical agent based on the HSP90 inhibitory effect and useful in the prevention and/or treatment of a disease involving HSP90, particularly cancer. The compound has a general formula (I) or is a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are each independently C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are each independently CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: December 16, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
  • Publication number: 20140364432
    Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: December 11, 2014
    Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
  • Publication number: 20140343031
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joesph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140336221
    Abstract: This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicants: Colorado Seminary, Which Owns and Operates The University Of Denver, Regis University
    Inventors: Scott Dusan Pegan, Kateri Ahrendt, Glenn C. Capodagli, Bryan Cowen
  • Publication number: 20140316130
    Abstract: This invention relates to the miniaturisation of radiosyntheses onto microfabricated devices, and in particular to use of microfabricated devices for radiosynthesis, isolation, and analysis of radiotracers for use in Positron Emission Tomography (PET).
    Type: Application
    Filed: April 15, 2014
    Publication date: October 23, 2014
    Applicant: HAMMERSMITH IMANET LIMITED
    Inventors: FRANK BRADY, SAJINDER KAUR LUTHRA, JAMES MILLAR GILLIES, NICHOLAS TOBY JEFFREY
  • Publication number: 20140315881
    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: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Patent number: 8853242
    Abstract: [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided. [Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: October 7, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Takuya Washio, Wataru Hamaguchi
  • Publication number: 20140296066
    Abstract: A compound of formula (I) (I), wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has one or more substituents at least one of which is, for example, a 5 membered heterocycle; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: October 2, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Thomas Pitterna, Olivier Loiseleur, Anthony Cornelius O'Sullivan, Torsten Luksch
  • Publication number: 20140296236
    Abstract: The invention relates to new quinoline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Valerio Berdini, Patrick Rene Angibaud, Steven John Woodhead, Gordon Saxty
  • Publication number: 20140291654
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein R1 to R12 are defined as in the specification.
    Type: Application
    Filed: June 12, 2014
    Publication date: October 2, 2014
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Yoon-Hyun Kwak, Sun-Young Lee, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee
  • Publication number: 20140288311
    Abstract: The present disclosure relates to a bis-quinophthalone pigment of Formula I, and a process for the same. wherein X1, X2, X3 and X4 are independently H or halogen ,preferably Cl or Br; R2 is substituent selected from the group consisting of H, C1-C20 straight or branched chain alkyl substituents, aromatic substituents, aliphatic substituents, and combinations thereof.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 25, 2014
    Inventor: Keki Hormusji Gharda
  • Publication number: 20140275087
    Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
  • Publication number: 20140275549
    Abstract: The present invention is a method for producing a phenyl-substituted heterocyclic derivative represented by general formula (1), which has a step wherein a heteroaromatic compound represented by general formula (2) is reacted with a phenol derivative represented by general formula (3) in the presence of a nickel compound, 1,2-bis(dicyclohexylphosphino)ethane, and a base.
    Type: Application
    Filed: October 10, 2012
    Publication date: September 18, 2014
    Applicant: National University Corporation Nagoya University
    Inventors: Kenichiro Itami, Junichiro Yamaguchi, Kei Muto
  • Publication number: 20140275224
    Abstract: Compounds and methods are provided for enhancing or boosting the transfection rate or efficiency of mammalian cells by foreign DNA, such as bacterial plasmid DNA. Compounds, including natural products and inventive synthetic compounds can increase the effectiveness of uptake and incorporation of foreign DNA by mammalian cells, such as human cells, by suppression of DNA cytosine deamination, which is believed to be a mechanism by which these cells eliminate foreign DNA. Inhibition of the cytosine deaminase enzymes by compounds as described herein serves to provide more effective transfection of eukaryotic cells by plasmids including engineered gene sequences. Transfection can be used to study cellular processes, or to cure genetic diseases in human patients. The inventive materials and methods increase the efficiency and effectiveness of such transfection techniques.
    Type: Application
    Filed: November 3, 2011
    Publication date: September 18, 2014
    Applicant: Regents of the University of Minnesota
    Inventors: Reuben S. Harris, Daniel A. Harki, Angela L. Perkins-Harki, Michael A. Carpenter, Ming Li
  • Publication number: 20140256707
    Abstract: The present invention provides compounds of Formula I or II, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: August 16, 2012
    Publication date: September 11, 2014
    Applicant: AMGEN INC.
    Inventors: Thomas Dineen, Isaac E. Marx, Hanh Nho Nguyen, Matthew Weiss
  • Patent number: 8822690
    Abstract: The present invention relates to high transmission yellow dye for LCD, dye dispersion comprising the dye, coloring composite comprising the dye dispersion, color filter comprising the coloring composite, and synthetic method thereof.
    Type: Grant
    Filed: December 31, 2012
    Date of Patent: September 2, 2014
    Assignee: LG Display Co., Ltd.
    Inventors: YoungHoon Kim, JiChul Lim, ByungGun Ahn, SangHun Han, JaePil Kim, SeHun Kim, Jun Choi, JinWoong Namgoong
  • Patent number: 8822818
    Abstract: Disclosed is a 4,4?-dicarboxy-2,2?-bipyridine derived tridentate ligand represented by formula (I): wherein definitions of Y1, Y2, and R are the same as those defined in the specification. Also disclosed are a metal complex containing the aforesaid tridentate ligand and a dye-sensitized solar cell containing the metal complex.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: September 2, 2014
    Assignee: National Tsing Hua University
    Inventors: Yun Chi, Cheng-Xuan Li, Shen-Han Yang, Hsin-Pei Wu, Kuan-Lin Wu, Chien-Wei Hsu, Shih-Han Chang
  • Patent number: 8815859
    Abstract: Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Gérard Botton, Eric Valeur, Christine Charon, Micheline Kergoat, Samer Elbawab
  • Publication number: 20140235672
    Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W1, W2, W3, Y, Z, R2, R3, R3? and R4, are defined in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Inventor: Douglas G. Batt
  • Publication number: 20140235673
    Abstract: The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Inventors: Zulan Pi, John Llyod, Jennifer X. Qiao, Tammy C. Wang, George O. Tora
  • Patent number: 8809545
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 19, 2014
    Assignee: Novartis AG
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • Publication number: 20140228577
    Abstract: The present invention relates to compounds of formula (I): wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Yves CASSAYRE, Peter RENOLD, Myriem EL QACEMI, Thomas PITTERNA, Julie Clementine TOUEG
  • Publication number: 20140228372
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, G1, G2, G3, Y1, Y2, n, and p are as defined in the claims. The invention also relates to methods of using the compounds of formula (I) to control or prevent infestation of plants, propagation material thereof, harvested crops or non-living materials by phytopathogenic spoilage microorganisms or organisms potentially harmful to man.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 14, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Emil Malcolm Cederbaum
  • Publication number: 20140221387
    Abstract: The present invention relates to a compositions for and methods of cancer treatment in which compounds of Formula I or Formula II. In some aspects, the treatment of B-cell Lymphoma or other hematopoietic cancers is encompassed. In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds of Formula I or Formula II. Combination therapy with, for example, a class of therapeutics known as 26S proteasome inhibitors, for example, Bortezomib, are also included. In another aspect the present invention relates to autoimmune treatment with compounds of Formula I or Formula II. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.
    Type: Application
    Filed: March 8, 2012
    Publication date: August 7, 2014
    Applicant: EUTROPICS PHARMACEUTICALS, INC.
    Inventors: Michael H. Cardone, Andrew F. Kolodziej, David Richard
  • Patent number: 8795848
    Abstract: Disclosed is an organic electroluminescent device (organic EL device) that is improved in the luminous efficiency, fully secured of the driving stability, and of a simple structure and also disclosed is a compound for organic EL device useful for the said device. The compound for organic EL device is, for example, an indolocarbazole derivative represented by the following general formula (3). The organic EL device comprises a light-emitting layer disposed between an anode and a cathode piled one upon another on a substrate and the said light-emitting layer comprises a phosphorescent dopant and the aforementioned indolocarbazole derivative as a host material. In general formula (3), L is an aromatic heterocyclic group of a fused-ring structure with a valence of (n+1), Ar1 to Ar3 each is an alkyl group, an aralkyl group, or a substituted or unsubstituted aromatic hydrocarbon or aromatic heterocyclic group, and n is an integer of 0-5.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: August 5, 2014
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Takahiro Kai, Masaki Komori, Toshihiro Yamamoto
  • Patent number: 8796259
    Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: August 5, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Pingyu Ding, Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Joane Litvak
  • Patent number: 8791263
    Abstract: A compound represented by the general formula (M): (wherein R1 represents a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR3, N(R3)2, C(?O)OR3 or C(?O)N(R3)2, R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, R4 represents a hydrogen atom, an oxygen atom or OR5, and R5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: July 29, 2014
    Assignee: Osaka University
    Inventors: Motomasa Kobayashi, Naoyuki Kotoku, Masayoshi Arai, Satoru Tamura
  • Publication number: 20140206661
    Abstract: The present invention provides a compound of Formula (X) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: January 21, 2014
    Publication date: July 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Jake AXFORD, Natalie DALES, Moo Je SUNG