Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 546/159)
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Publication number: 20140107094Abstract: 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: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: 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, Joan Pierce, Steven Goldberg, Anne Fourie, Xiaohua Xue
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Publication number: 20140107097Abstract: 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: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: 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, Taraneh Mirzadegan, Kelly Ganamet
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Publication number: 20140107156Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: December 13, 2013Publication date: April 17, 2014Applicant: Merck Patent GmbHInventors: Amanda E. Sutton, Thomas E. Richardson, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Yufang Xiao, Andreas Goutopoulos, Ruoxi Lan, David Perrey, Harold George Vandeveer, Lesley Liu-Bujalski, Frank Steiber, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
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Patent number: 8697875Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.Type: GrantFiled: June 23, 2011Date of Patent: April 15, 2014Assignee: The Trustees of Columbia University in the City of New YorkInventors: Yan Feng, Ottavio Arancio, Shixian Deng, Donald W. Landry
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Patent number: 8697725Abstract: Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.Type: GrantFiled: November 3, 2010Date of Patent: April 15, 2014Assignee: GlaxoSmithKline LLCInventors: Emmanuel Hubert Demont, Neil Stuart Garton, Romain Luc Marie Gosmini, Thomas George Christopher Hayhow, Jonathan Seal, David Matthew Wilson, Michael David Woodrow
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Patent number: 8686002Abstract: The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.Type: GrantFiled: August 21, 2006Date of Patent: April 1, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Francisco Javier Garcia-Ladona, Alfred Hahn
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Patent number: 8680116Abstract: The present invention is directed to quinolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: July 19, 2010Date of Patent: March 25, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Pablo DeLeon, Melissa Egbertson, Ivory D. Hills, Adam Wayne Johnson, Michelle Machacek
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Patent number: 8674108Abstract: The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith.Type: GrantFiled: April 20, 2012Date of Patent: March 18, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Brian Luisi, Sneha Ghanshyam Arekar, Adriana Costache, Kirk Raymond Dinehart, Steven C. Johnston, Bobbianna J. Neubert-Langille
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Publication number: 20140066459Abstract: Tetrahydroquinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: May 2, 2012Publication date: March 6, 2014Applicant: GlaxoSmithkline LLCInventors: Dominique Amans, Emmanuel Hubert Demont, Katherine Louise Jones, Jonathan Thomas Seal, Ann Louise Walker
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Patent number: 8664399Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: December 6, 2012Date of Patent: March 4, 2014Assignee: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Patent number: 8664244Abstract: The present invention relates to compounds, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with the inhibition of the protein tyrosine kinase activity of growth factor receptors such as c-Met, thereby making them useful as anticancer agents, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.Type: GrantFiled: September 8, 2011Date of Patent: March 4, 2014Assignee: Advenchen Pharmaceuticals, LLCInventor: Guoqing Paul Chen
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Patent number: 8653102Abstract: The invention relates to substituted 2-oxo- and 2-thioxo-dihydroquinoline-3-carboxamides to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: GrantFiled: August 26, 2011Date of Patent: February 18, 2014Assignee: Gruenenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder
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Patent number: 8653099Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein A, L, R1, R2, R4 and R5 are defined herein.Type: GrantFiled: August 11, 2009Date of Patent: February 18, 2014Assignee: Janssen PharmaceuticaInventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
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Patent number: 8653263Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: GrantFiled: October 21, 2010Date of Patent: February 18, 2014Assignee: Janssen PharmaceuticaInventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
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Patent number: 8653101Abstract: The invention relates to substituted 2-oxy-quinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: GrantFiled: August 26, 2011Date of Patent: February 18, 2014Assignee: Gruenenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder
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Patent number: 8648195Abstract: An objective of the present invention is to provide a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate having stable physicochemical properties. The objective is attained by a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate that exhibits a diffraction peak pattern shown in FIG. 1 as determined by powder X-ray diffractometry.Type: GrantFiled: February 22, 2011Date of Patent: February 11, 2014Assignees: Nippon Kayaku Co., Ltd., Meiji Seika Pharma Co., Ltd.Inventors: Kouki Tanigakiuchi, Mikio Sekiguchi, Hiroki Hotta, Shizuo Shimano, Akinori Morikawa, Kazumi Yamamoto, Nozomu Nakanishi, Nobuto Minowa, Takashi Watanabe
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Patent number: 8648196Abstract: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.Type: GrantFiled: October 30, 2012Date of Patent: February 11, 2014Assignee: Abbvie Inc.Inventors: Anthony Haight, David M. Barnes, Geoff G. Z. Zhang
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Publication number: 20140039006Abstract: Tetrahydroquinoline derivatives, pharmaceutical compositions containing such compounds and to their use in therapy.Type: ApplicationFiled: April 19, 2012Publication date: February 6, 2014Applicant: GlaxoSmithKline LLCInventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Robert J. Watson
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Patent number: 8642619Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.Type: GrantFiled: August 21, 2012Date of Patent: February 4, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Kenji Otsubo, Yuji Ochi, Masami Nakai, Atsushi Mori
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Patent number: 8633220Abstract: This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.Type: GrantFiled: June 27, 2011Date of Patent: January 21, 2014Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 8629285Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: August 10, 2006Date of Patent: January 14, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
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Patent number: 8623893Abstract: The present invention relates to derivatives of pyridino-pyridinones, and to their preparation and use thereof, having activity as inhibitors of kinase activity of receptors for PDGF (platelet derived growth factors) ligands and optionally of receptors for the FLT3 (fms-like tyrosine kinase receptor) ligand receptors, said derivatives comprising compounds of formula (I): wherein the various substituent groups are more specifically defined herein. The compounds are suitable as therapeutics for the treatment of various proliferative diseases.Type: GrantFiled: May 22, 2012Date of Patent: January 7, 2014Assignee: SANOFIInventors: Gilbert Lassalle, Valérie Martin, Gary McCort, Cécile Volle-Challier
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Publication number: 20140005222Abstract: The present invention provides a compound of the Formula II: wherein A is: R1 is CH3, CF3, or F; R2 is H, CH3, or F; R3 is CH3, OCH3, OH, F; R4 is OH or CH2OH; and X is CH or N; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 20, 2013Publication date: January 2, 2014Inventors: Maria-Jesus BLANCO-PILLADO, Matthew Joseph FISHER, Steven Lee KUKLISH, Tatiana Natali VETMAN
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Publication number: 20130344165Abstract: This disclosure relates to compounds and compositions for forming bone and methods related thereto. In certain embodiments, the disclosure relates to methods of forming bone comprising implanting a bone graft composition comprising a growth factor such as BMP in a subject at a site of desired bone growth or enhancement in combination with a JAB1 blocker.Type: ApplicationFiled: February 23, 2012Publication date: December 26, 2013Applicant: EMORY UNIVERSITYInventors: Scott D. Boden, Sreedhara Sangadala
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Patent number: 8614326Abstract: Disclosed herein is a stable compound having a structure formula (I): therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: August 21, 2008Date of Patent: December 24, 2013Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello, Michael E. Garst
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Patent number: 8614327Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: November 30, 2012Date of Patent: December 24, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Urvi Sheth, Lev T. D. Fanning, Mehdi Michel Djamel Numa, Hayley Binch, Dennis Hurley, Jinglan Zhou, Sara S. Hadida Ruah, Anna Hazlewood, Alina Silina, Rajendran Vairagoundar, Fredrick Van Goor, Peter D. J. Grootenhuis, Martyn Botfield
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Patent number: 8609847Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.Type: GrantFiled: February 5, 2010Date of Patent: December 17, 2013Assignee: Taisho Pharmaceutical Co., LtdInventors: Toshio Nakamura, Seiji Masuda, Aya Futamura
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Patent number: 8604203Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: GrantFiled: October 15, 2012Date of Patent: December 10, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T. D. Fanning, Martyn Botfield, Peter D. J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Patent number: 8604055Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.Type: GrantFiled: June 28, 2006Date of Patent: December 10, 2013Assignee: Dr. Reddy's Laboratories Ltd.Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dagar, Shanavas Alikunju
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Patent number: 8598355Abstract: [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.Type: GrantFiled: May 12, 2009Date of Patent: December 3, 2013Assignee: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo, Susumu Watanuki, Michihito Kageyama
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Patent number: 8598205Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: GrantFiled: April 4, 2012Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T. D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D. J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Patent number: 8592593Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: GrantFiled: September 14, 2012Date of Patent: November 26, 2013Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
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Patent number: 8586570Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: April 27, 2011Date of Patent: November 19, 2013Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
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Patent number: 8580957Abstract: Tetrahydroquinoline compounds of formula (I) or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicted.Type: GrantFiled: November 3, 2010Date of Patent: November 12, 2013Assignee: GlaxoSmithKline LLCInventors: Emmanuel Hubert Demont, Romain Luc Marie Gosmini
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Patent number: 8575348Abstract: The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: July 28, 2010Date of Patent: November 5, 2013Assignee: Auspex Pharmaceuticals, IncInventors: Tadimeti Rao, Chengzhi Zhang
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Patent number: 8569505Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.Type: GrantFiled: January 22, 2010Date of Patent: October 29, 2013Assignee: Janssen Pharmaceutica, NVInventors: Ellen Codd, Scott L. Dax, Michele Jetter, Mark McDonnell, James J. McNally, Mark Youngman
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Patent number: 8563731Abstract: The present disclosure relates to a mesylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 receptor.Type: GrantFiled: December 15, 2009Date of Patent: October 22, 2013Assignee: Almirall, S.A.Inventors: Francesc Carrera Carrera, Carlos Puig Duran, Iolanda Marchueta Hereu, Enrique Moyes Valls
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Patent number: 8563579Abstract: The present application is related to compounds represented by Formula I, which are novel allosteric modulators of ?7nAChR. The application also discloses the treatment of disorders that are responsive to modulation of acetylcholine action on ?7nAChR in a mammal by administering an effective amount of a compound of Formula I.Type: GrantFiled: January 15, 2010Date of Patent: October 22, 2013Assignee: Anvyl LLCInventor: Richard Kanner
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Publication number: 20130261123Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20130253186Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 10, 2013Publication date: September 26, 2013Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
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Patent number: 8536195Abstract: The present invention relates to bicyclic compounds 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: November 16, 2012Date of Patent: September 17, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Andreas Termin, Nicole Hilgraf, Tara Leanne Hampton, Gabriel Martinez-Botella, Esther Martinborough
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Patent number: 8530183Abstract: The present invention provides compounds for use as zinc ligand sensors in cellular imaging. These compounds are sensitive imaging agents that can be used with techniques such a laser scanning microscopy in intact cells in culture or in tissue preparations.Type: GrantFiled: June 10, 2011Date of Patent: September 10, 2013Assignee: The Board of Regents of the University of Texas SystemInventors: Wen-Hong Li, Daliang Li
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Patent number: 8524739Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).Type: GrantFiled: April 25, 2011Date of Patent: September 3, 2013Assignee: State of Oregon acting by and through the State Board of Higher Education on behalf of Portland State UniversityInventors: David H. Peyton, Steven Burgess
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Patent number: 8524907Abstract: Novel methods of preparing a compound of Formula I which is an inhibitor of Factor Xa and its maleate salt, are described herein.Type: GrantFiled: November 1, 2007Date of Patent: September 3, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, James P Kanter, Keiko Sujino, Sharique Sami Zuberi, Carroll Scarborough
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Publication number: 20130225579Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.Type: ApplicationFiled: June 8, 2011Publication date: August 29, 2013Applicant: Tianjin Hemay Bio-Tech Co., Ltd.Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
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Publication number: 20130217671Abstract: The present invention directs a compound represented by formula (I).Type: ApplicationFiled: July 28, 2011Publication date: August 22, 2013Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Raymond Huntley, Joel R. Walker, Helene Decomez
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Patent number: 8513282Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: GrantFiled: October 23, 2009Date of Patent: August 20, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T. D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D. J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Patent number: 8513421Abstract: This invention provides compounds of formula (I): wherein R1a, R1, R2a, and R2b have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: May 18, 2011Date of Patent: August 20, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Alexandra E. Gould, Sean J. Harrison
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Patent number: 8513284Abstract: A series of amino-substituted fused pyridine and pyrazine derivatives, in particular amino-substituted quinoline and quinoxaline derivatives, 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: GrantFiled: February 11, 2010Date of Patent: August 20, 2013Assignee: UCB Pharma, S.A.Inventors: Daniel Rees Allen, Julien Alistair Brown, Roland Burli, Alan Findlay Haughan, Jonathan David MacDonald, Elizabeth Anne Saville-Stones, Andrew Sharpe