Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 544/250)
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Patent number: 8927561Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: GrantFiled: April 20, 2011Date of Patent: January 6, 2015Assignee: Kineta, Inc.Inventors: Shawn P. Iadonato, Kristin Bedard
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Patent number: 8921549Abstract: Provided are a light-emitting element including a novel organometallic complex as an emission center, the organometallic complex, a light-emitting device, an electronic device, and a lighting device each using the light-emitting element. One embodiment of the present invention is a light-emitting element including, as an emission center, an organometallic complex in which a benzofuropyrimidine derivative is coordinated to a metal. In particular, another embodiment is a light-emitting element including, as an emission center, an organometallic complex in which a benzofuropyrimidine derivative having an aryl group at the 4-position is coordinated to a metal. Another embodiment is a light-emitting element including, as an emission center, an organometallic complex in which nitrogen at the 3-position of a benzofuropyrimidine derivative having an aryl group at the 4-position is coordinated to a metal and the aryl group is bonded to the metal.Type: GrantFiled: May 30, 2013Date of Patent: December 30, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hideko Inoue, Tomoya Yamaguchi, Hiromi Seo, Satoshi Seo
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Patent number: 8920944Abstract: Use of a precursor of an n-dopant for doping an organic semiconductive material, as a blocking layer, as a charge injection layer, as an electrode material, as a storage material or as a semiconductor material itself in electronic or optoelectronic components, the precursor being selected from the following formulae 1-3c:Type: GrantFiled: June 20, 2008Date of Patent: December 30, 2014Assignee: Novaled AGInventors: Michael Limmert, Andrea Lux, Horst Hartmann
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Publication number: 20140378486Abstract: Disclosed herein are acylated derivatives of 7H-pyrrolo[3,2-f]quinazoline-1,3-diamine and pharmaceutical compositions comprising said derivatives.Type: ApplicationFiled: June 19, 2014Publication date: December 25, 2014Applicant: OREGON HEALTH & SCIENCE UNIVERSITYInventors: Xiangshu Xiao, Jingjin Chen, Bingbing Li
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Patent number: 8916577Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.Type: GrantFiled: January 19, 2012Date of Patent: December 23, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
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Publication number: 20140371230Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: June 25, 2014Publication date: December 18, 2014Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Patent number: 8901141Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: GrantFiled: January 21, 2009Date of Patent: December 2, 2014Assignee: Takeda Pharmaceutical Company, LimitedInventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki
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Publication number: 20140350244Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: ApplicationFiled: August 7, 2014Publication date: November 27, 2014Inventors: Richard V. Connors, Kang DAI, John EKSTEROWICZ, Pingchen FAN, Benjamin FISHER, Jiasheng FU, Kexue LI, Zhihong LI, Lawrence R. MCGEE, Rajiv SHARMA, Xiaodong WANG, Dustin L. MCMINN, Jeffrey T. MIHALIC, Jeffrey DEIGNAN
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Publication number: 20140349992Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: Sunovion Pharmaceuticals Inc.Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Patent number: 8895549Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: GrantFiled: November 8, 2011Date of Patent: November 25, 2014Assignee: Bayer Intellectual Property GmbHInventors: William Johnston Scott, Ningshu Liu, Manfred Möwes, Andrea Hägebarth, Ursula Mönning, Ulf Bömer
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Publication number: 20140343283Abstract: The present invention relates to the technical field of medicine, and specifically provides methods for preparing Icotinib, Icotinib hydrochloride, and intermediates thereof. These methods avoid the use of phosphorus oxychloride, thereby greatly reducing the emission of pollutants, which is of major benefits to the economy and environment.Type: ApplicationFiled: December 28, 2012Publication date: November 20, 2014Applicant: BETTA PHARMACEUTICALS CO., LTD.Inventors: Shaojing Hu, Wei Long, Fei Wang, Zongquan Li
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Publication number: 20140343082Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Inventors: Yinxiang Wang, Guojian Xie, Lieming Ding, Fenlai Tan, Yunyan Hu, Wei He, Bin Han, Wei Long, Yong Liu, Haima Ai, Charles Davis, Don Zhang
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Publication number: 20140343045Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: May 23, 2014Publication date: November 20, 2014Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Patent number: 8889666Abstract: The present invention provides a new compound that has an inhibitory action against EGFR and that has cell growth inhibitory effects. The present invention further provides a pharmaceutical preparation useful for preventing and/or treating cancer, based on the EGFR inhibitory effect of the compound. A compound represented by the following Formula (I) or a salt thereof.Type: GrantFiled: February 22, 2013Date of Patent: November 18, 2014Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Takeshi Sagara, Satoru Ito, Sachie Otsuki, Katsumasa Nonoshita
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Patent number: 8883781Abstract: The present invention relates to compounds of formula IA-i useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: June 12, 2007Date of Patent: November 11, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lev T. D. Fanning, Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson, Yulian Zhang
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Patent number: 8877765Abstract: The present invention features pyrimido-dione-quinoline compounds having improved solubility, pharmaceutical compositions of substituted pyrimido-dione-quinoline compounds and methods of treating a patient suffering from cancer, the method comprising administering to a patient one or more pyrimido-dione-quinoline compounds of the invention.Type: GrantFiled: June 13, 2007Date of Patent: November 4, 2014Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Allan M. Weissman, Yili Yang
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Publication number: 20140323435Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: May 22, 2014Publication date: October 30, 2014Applicants: Cancer Research Technology Limited, Cephalon, Inc.Inventors: Bruce D. Dorsey, Keith S. Learn, Emma L. Morris, Gregory R. Ott, Jonathan R.A. Roffey, Christelle N. Soudy, Jason C. Wagner
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Patent number: 8871776Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: GrantFiled: October 10, 2012Date of Patent: October 28, 2014Assignee: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Publication number: 20140315889Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.Type: ApplicationFiled: October 26, 2012Publication date: October 23, 2014Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
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Patent number: 8859572Abstract: This invention relates to novel sulfone 2I3-dihydroimidazo[1 l2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis mediated disorders, as a sole agent or in combination with other active ingredients.Type: GrantFiled: January 13, 2009Date of Patent: October 14, 2014Assignee: Bayer Intellectual Property GmbHInventors: Martin F. Hentemann, William Scott, Jill Wood, Jeffrey Johnson, Aniko Redman, Ann-Marie Bullion, Leatte Guernon
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Publication number: 20140291645Abstract: A light-emitting element having high emission efficiency is provided. A light-emitting element having a low driving voltage is provided. A novel compound which can be used for a transport layer or as a host material or a light-emitting material of a light-emitting element is provided. A novel compound with a benzofuropyrimidine skeleton is provided. Also provided is a light-emitting element which includes the compound with the benzofuropyrimidine skeleton between a pair of electrodes.Type: ApplicationFiled: March 25, 2014Publication date: October 2, 2014Applicant: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hideko Inoue, Miki Kanamoto, Hiromi Seo, Satoshi Seo, Tatsuyoshi Takahashi, Tomoka Nakagawa
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Patent number: 8841312Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: GrantFiled: December 18, 2008Date of Patent: September 23, 2014Assignee: Amgen Inc.Inventors: Richard V. Connors, Dai Kang, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. McGee, Rajiv Sharma, Xiaodong Wang, Dustin L. McMinn, Jeffrey T. Mihalic, Jeffrey Deignan
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Publication number: 20140275064Abstract: The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.Type: ApplicationFiled: August 17, 2012Publication date: September 18, 2014Applicant: DIAXONHITInventors: Bertrand Leblond, Anne-Sophie Casagrande, Laurent Desire, Alicia Foucourt, Thierry Besson
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Publication number: 20140275092Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Constellation Pharmaceuticals, Inc.Inventors: Brian K. Albrecht, Steven F. Bellon, Victor S. Gehling, Jean-Christophe Harmange
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Publication number: 20140256706Abstract: Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Xu Ran, Yujun Zhao, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachern, Jeanne Stuckey, Jennifer Lynn Meagher, Duxin Sun, Xiaoqin Li, Bing Zhou, Hacer Karatas, Ruijuan Luo, Arul Chinnaiyan, Irfan A. Asangani
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Publication number: 20140249145Abstract: Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) in which variables R1-R7 and X are described in the application.Type: ApplicationFiled: December 8, 2011Publication date: September 4, 2014Applicant: THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human ServInventors: Juan Jose Marugan, Noel Southall, Ehud Goldin, Wei Zheng, Samarjit Patnaik, Ellen Sidransky, Omid Motabar, Wendy Westbroek
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Patent number: 8822482Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.Type: GrantFiled: July 7, 2009Date of Patent: September 2, 2014Assignee: Beta Pharma, Inc.Inventors: Yinxiang Wang, Guojian Xie, Lieming Ding, Fenlai Tan, Yunyan Hu, Wei He, Bin Han, Wei Long, Yong Liu, Haima Ai, Charles Davis, Don Zhang
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Patent number: 8822683Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: GrantFiled: January 23, 2014Date of Patent: September 2, 2014Assignee: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Patent number: 8822483Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.Type: GrantFiled: May 22, 2012Date of Patent: September 2, 2014Assignee: Florida State University Research FoundationInventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
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Publication number: 20140243320Abstract: A compound represented by the following general formula (1) or a salt thereof. R1 represents a halogen atom and so on; R2 and R3 each represent a hydrogen atom and so on; R4 and R5 each represent a hydrogen atom and so on, or R4 and R5 may form an oxo group; Ra and Rb each represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural Rc; Rc represents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2.Type: ApplicationFiled: July 12, 2012Publication date: August 28, 2014Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hiroshi Enomoto, Kenji Kawashima, Shinji Takaoka, Yasutaka Fujioka, Mamoru Matsuda, Koji Ohashi, Yukie Fujita, Shin-ichiro Hirai, Hiroaki Kurashima
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Publication number: 20140228320Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: April 15, 2014Publication date: August 14, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
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Patent number: 8802849Abstract: The invention relates to novel tricyclic benzo[4,5]thieno-[2,3-d]pyrimidine-4-yl-amin derivatives, as well as their pharmaceutically acceptable salts. The subject of the invention too the process for producing the compounds and their use as a pharmaceutically active agent and as pharmaceutical compositions for prophylaxis and/or treatment of proliferative diseases such as cancer.Type: GrantFiled: February 19, 2008Date of Patent: August 12, 2014Assignee: Vichem Chemie Kutató Kft.Inventors: Péter Bánhegyi, György Kéri, Lászlö Örfi, Zsolt Szekélyhidi, Frigyes Wáczek
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Publication number: 20140221405Abstract: Novel compounds of formulae (I) to (VII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylfulfonamide derivatives which are effective platelet ADF receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 31, 2013Publication date: August 7, 2014Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-MaGuire
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Patent number: 8785460Abstract: There is provided a compound of the formula (I?): wherein x is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to 8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: GrantFiled: January 21, 2009Date of Patent: July 22, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20140200209Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: March 14, 2014Publication date: July 17, 2014Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
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Publication number: 20140194417Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: January 8, 2014Publication date: July 10, 2014Applicant: Nimbus Iris, Inc.Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Rosana Kapeller-Libermann, Craig E. Masse, Shaughnessy Robinson, Donna L. Romero, Mee Shelley, Ronald T. Wester
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Patent number: 8772301Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: GrantFiled: December 17, 2010Date of Patent: July 8, 2014Assignee: Sunovion Pharmaceuticals, Inc.Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
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Publication number: 20140187550Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: ApplicationFiled: December 16, 2013Publication date: July 3, 2014Applicant: Novartis AGInventor: Roger John Taylor
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Patent number: 8765757Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: November 13, 2008Date of Patent: July 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
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Publication number: 20140179682Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: ApplicationFiled: June 8, 2012Publication date: June 26, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Publication number: 20140171417Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: Mahbub AHMED, Alexander ASHALL-KELLY, Louisa GUERITZ, Jeffrey MCKENNA, Joseph MCKENNA, Simon MUTTON, Rakesh PARMAR, Jon SHEPHERD, Paul WRIGHT
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Publication number: 20140148436Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Applicant: Array BioPharma, Inc.Inventors: Ian S. Mitchell, Keith L. Spencer, Peter Stengel, Yongxin Han, Nicolas C. Kallan, Mark Munson, Guy P.A. Vigers, James Blake, Anthony Piscopio, John Josey, Scott Miller, Dengming Xiao, Rui Xu, Chang Rao, Bing Wang, April L. Bernacki
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Publication number: 20140142301Abstract: The organic EL material is represented by Formula (1): where X1 to X4 are each independently a nitrogen (N) atom or a carbon atom that is monovalently bonded to R1(C—R1), R1 is a hydrogen atom, a halogen atom, an aryl group having 6 to 18 carbon atoms, a hetero aryl group having 6 to 18 carbon atoms, or an alkyl group having 1-12 carbon atoms, R2 to R10 are each independently hydrogen, an aryl group having 6 to 30 carbon atoms, or hetero aryl group having 6 to 30 carbon atoms, and at least one of X1 to X4 is a nitrogen atom.Type: ApplicationFiled: November 20, 2013Publication date: May 22, 2014Applicant: SAMSUNG DISPLAY CO., LTD.Inventor: Hiroaki ITOI
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Patent number: 8729090Abstract: Embodiments of the invention include compositions effective for inhibiting collagen production and related methods. A preferred method comprises contacting at least one cell capable of producing collagen with a composition effective for inhibiting collagen production thereby. The composition comprises one or more of the compounds effective for inhibiting collagen production disclosed herein.Type: GrantFiled: October 5, 2012Date of Patent: May 20, 2014Assignee: The Florida State University Research Foundation, Inc.Inventor: Branko Stefanovic
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Publication number: 20140128390Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.Type: ApplicationFiled: September 5, 2013Publication date: May 8, 2014Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
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Publication number: 20140121198Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: October 31, 2013Publication date: May 1, 2014Applicant: Incyte CorporationInventors: Yun-Long Li, Wenyu Zhu, Song Mei, Joseph Glenn
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Publication number: 20140113896Abstract: The present invention relates to substituted phenoxypyridine compounds of general formula (I); in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: November 8, 2011Publication date: April 24, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: William Johnston Scott, Orlin Pertov, Manfred Möwes, Ningshu Liu, Ulf Bömer
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Patent number: 8703941Abstract: The present invention provides thienopyrimidine and thienopyridine compounds, compositions thereof, and methods of using the same for the treatment of diseases mediated by IRAK enzymes. Such diseases include inflammatory and proliferative diseases.Type: GrantFiled: January 10, 2012Date of Patent: April 22, 2014Assignee: Nimbus Iris, Inc.Inventors: Donna L. Romero, Matthew David Wessel, Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse, Mee Shelley
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Publication number: 20140093490Abstract: The present invention investigate the two modes of glutamate release and the releasing rate of glutamate, and thus can provide a useful technique for neuron protection and acceleration of neurotransmission by controlling the glutamate release in astroctye. Thus, the present invention provides an inhibitor of the fast-mode release and/or the slow-mode release of astrocytic glutamate, a screening method of the inhibitor and a pharmaceutical composition or method of ameliorating, preventing and/or treating the disease associated with the over-release of glutamate via the Ca2+-activated anion channel, with the inhibition of fast-mode glutamate release.Type: ApplicationFiled: July 23, 2013Publication date: April 3, 2014Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Changjoon Justin LEE, Soo Jin OH, Eun Mi HWANG, Dong Ho WOO
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Publication number: 20140077191Abstract: A compound is represented by a formula (1) below. In the formula (1), X1 to X8 each independently represent a carbon atom to be bonded to a group represented by the following formula (20), CRX or a nitrogen atom. At least one of X1 to X8 is a carbon atom to be bonded to the group represented by the following formula (2). RX is each independently a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 30 carbon atoms, or the like.Type: ApplicationFiled: September 12, 2013Publication date: March 20, 2014Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Sayaka Mizutani, Takayasu Sado