C=o Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/354)
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Publication number: 20140323528Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof.Type: ApplicationFiled: September 21, 2012Publication date: October 30, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Ottmar Franz Hueter, Peter Renold, Peter Maienfisch, Pierre Joseph Marcel Jung, Thomas Pitterna, Christopher Richard Ayles Godfrey, Elke Maria Hillesheim, Andre Stoller
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Publication number: 20140309228Abstract: The present disclosure provides substituted pyridine and pyrimidine compounds of Formula (I): A1-X-A2-Z-R1 (I) and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein A, X, A, Z, and R are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.Type: ApplicationFiled: October 30, 2012Publication date: October 16, 2014Applicant: Purdue Pharma L.P.Inventor: John J. Engel
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Patent number: 8859591Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: GrantFiled: July 3, 2013Date of Patent: October 14, 2014Assignee: Pfizer Inc.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20140288034Abstract: A compound having an ability to bind to an S1P receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.Type: ApplicationFiled: June 4, 2014Publication date: September 25, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Shinji NAKADE, Hirotaka Mizuno, Takeji ONO, Masashi Minami, Hiroshi Saga, Hiroshi Hagiya, Takaki Komiya, Hiromu Habashita, Haruto Kurata, Kazuhiro Ohtsuki, Kensuke Kusumi
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Patent number: 8841457Abstract: The present invention describes a process for preparing a cyclooxygenase-2 selective inhibitor. It provides a synthetic procedure for the said substance namely 5-chloro-3-(4-methylsulphonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine of formula (I). The invention also relates to preparation of a new intermediate of formula (IV) and a process to prepare it. Furthermore, the invention describes a process for preparing another key intermediate of formula (II). Compounds of formula (IV) and formula (II) are useful intermediates in synthesis of the said cyclooxygenase-2 inhibitor.Type: GrantFiled: November 15, 2011Date of Patent: September 23, 2014Assignee: Virdev Intermediates Pvt. Ltd.Inventors: Dharmesh Mahendra Shah, Sanjay Amratlal Solanki, Viral Narendra Jariwala, Ashok Vasantray Vyas, Ashokkumar Bhikhubhai Mistry
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Patent number: 8841331Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: GrantFiled: November 21, 2012Date of Patent: September 23, 2014Assignee: Gilead Sciences, Inc.Inventors: Christiane Yoakim, Murray D. Bailey, Francois Bilodeau, Rebekah Carson, Lee Fader, Stephen Kawai, Sebastien Morin, Carl Thibeault, Bruno Simoneau, Simon Surprenant, Youla S. Tsantrizos, Steven R. Laplante
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Publication number: 20140271931Abstract: Topical formulations containing one or more pharmaceutically acceptable bioadhesive film-forming agent, one or more anti-acne agent, and an aqueous solvent in the form of a solution or suspension are described herein. The formulation may further contain one or more excipients, including evaporation suppressants, humectants, or plasticizers. When the formulation is contacted with the skin of a patient, the solvent evaporates and forms a thin, transparent, and solid bioadhesive film. The bioadhesive film adheres to the skin surface for a prolonged period of time and the anti-acne agent is released into the skin over a prolonged period of time. Typically, the bioadhesive film adheres to the skin for at least 60 minutes following administration of the formulation, preferably for at least 8 hours following administration, more preferably up to 24 hours following administration. The prolonged retention of the anti-acne agent at the site increases the amount of uptake into the skin.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: Perosphere Inc.Inventors: Edith Mathiowitz, Bryan E. Laulicht, Sasha H. Bakhru, Solomon S. Steiner
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Publication number: 20140274692Abstract: A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, a substituted phenol; R6 is, for example, hydrogen; 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 is, for example, A1 is N or C—X, A3 is C—X, and A2, A4 and A5 are C—H, where X, is, for example, halogen; and its use as a pesticidal agent.Type: ApplicationFiled: October 31, 2012Publication date: September 18, 2014Applicant: Syngenta Participations AGInventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch, Anna Kickova
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Publication number: 20140275008Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Qing Xu, Zhe Li
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Patent number: 8835409Abstract: 3-Alkenyl-6-halo-4-aminopicolinic acids and their derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: January 24, 2012Date of Patent: September 16, 2014Assignee: Dow AgroSciences, LLC.Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Paul R. Schmitzer, Thomas L. Siddall
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Patent number: 8835467Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: GrantFiled: January 23, 2013Date of Patent: September 16, 2014Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
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Publication number: 20140256664Abstract: The present application discloses rapid Mycobacterium tuberculosis drug susceptibility utilizing real-time PCR of mycobacteriophage D29 DNA. One protocol involves culturing Tb isolates for 48 hours with and without drugs at critical concentrations, followed by incubation with 103 pfu/ml of D29 mycobacteriophage for 24 hours and then real-time PCR. Many drugs can be incubated instantly with Tb and phage. The change in phage DNA real-time PCR cycle threshold (Ct) between control Tb and Tb treated with drugs was calculated and correlated with conventional agar proportion drug susceptibility results. Specifically, 9 susceptible clinical isolates, 22 MDR, and 1 XDR Tb strains were used and Ct control?Ct drug cutoffs of between +0.3 and ?6.0 yielded 422/429 (98%) accurate results for the drugs tested. The Ct values correlated with isolate minimal inhibitory concentration (MIC) for most agents. This D29 qPCR assay offers a rapid, accurate, 1-3 day phenotypic drug susceptibility test.Type: ApplicationFiled: May 11, 2012Publication date: September 11, 2014Applicant: University of Virginia Patent FoundationInventors: Eric R. Houpt, Kimberly A. Kelly, Suporn Pholwat
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Publication number: 20140249155Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: ApplicationFiled: March 23, 2014Publication date: September 4, 2014Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, VNR Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Publication number: 20140249149Abstract: The present invention relates to the use of known pyridyl carboxamide derivatives and novel pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.Type: ApplicationFiled: October 29, 2012Publication date: September 4, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jörg Nico Greul, Darren Mansfield, Martin Fusslein, Heiko Rieck, Matthias Riedrich, Lars Rodefeld, Kristian Kather, Olga Malsam, Peter Losel, Arnd Voerste, Hans-Georg Schwarz, Kerstin Ilg, Ulrich Gorgens, Lionel Carles, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse
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Publication number: 20140243349Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.Type: ApplicationFiled: February 21, 2014Publication date: August 28, 2014Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Publication number: 20140243378Abstract: Disclosed are methods of treating a muscle disease and improving normal muscle function by administering a therapeutically effective amount of an isoprenoid antibiotic. Also disclosed are methods of upregulating hnRNP L and hnRNP L targets by administering a therapeutically effective amount of an isoprenoid antibiotic. Methods of screening compounds for use in treating muscle disease and improving muscle function are also described.Type: ApplicationFiled: October 19, 2012Publication date: August 28, 2014Applicants: Tufts Medical Center, Inc., Children's Medical Center CorporationInventors: Isabelle Draper, Louis M. Kunkel, Matthew S. Alexander, Alan S. Kopin
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Publication number: 20140242153Abstract: Disclosed are novel methods for making cochleates and cochleate compositions that include introducing a cargo moiety to a liposome in the presence of a solvent. Also disclosed are cochleates and cochleate compositions that include an aggregation inhibitor, and optionally, a cargo moiety. Additionally, anhydrous cochleates that include a protonized cargo moiety, a divalent metal cation and a negatively charge lipid are disclosed. Methods of using the cochleate compositions of the invention, including methods of administration, are also disclosed.Type: ApplicationFiled: January 30, 2014Publication date: August 28, 2014Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Raphael J. Mannino, Susan Gould-Fogerite, Sara L. Krause-Elsmore, David Delmarre, Ruying Lu
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Publication number: 20140243366Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: May 1, 2014Publication date: August 28, 2014Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
Patent number: 8802720Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: April 22, 2013Date of Patent: August 12, 2014Assignee: SanofiInventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek -
Publication number: 20140213611Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.Type: ApplicationFiled: July 6, 2012Publication date: July 31, 2014Applicant: KalVista Pharmaceuticals LimitedInventors: David Michael Evans, Rebecca Louise Davie, Hannah Joy Edwards, David Philip Rooker
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Patent number: 8785490Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).Type: GrantFiled: April 8, 2011Date of Patent: July 22, 2014Assignee: University of Louisville Research Foundation, Inc.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
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Patent number: 8785432Abstract: A single layer pharmaceutical composition comprising active agent(s) amlodipine or a pharmaceutically acceptable salt thereof and valsartan or a pharmaceutically acceptable salt thereof wherein the composition exhibits bioequivalence to the commercially available bilayer tablet dosage form comprising amlodipine besylate and valsartan; when administered to human subject, under the bioequivalence parameters of a 90% Confidence Interval for AUC which is between 80% and 125%, and a 90% Confidence Interval for Cmax, which is between 80% and 125%.Type: GrantFiled: February 21, 2008Date of Patent: July 22, 2014Assignee: Lupin LimitedInventors: Anirudha Bhagirath Kute, Nikhil Prabhakar Malewar, Makarand Krishnakumar Avachat
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Publication number: 20140194445Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: March 10, 2014Publication date: July 10, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Patent number: 8772300Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2? are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2? together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4? are each independently hydrogen or lower alkyl, or R4 and R4? together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: GrantFiled: April 11, 2012Date of Patent: July 8, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20140179746Abstract: The subject matter disclosed herein is directed to amido-pyridyl ether compounds of formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, Ra, a, b and d are as described herein, compositions comprising the compounds of formula I, methods for their preparation and methods for their uses against parasites.Type: ApplicationFiled: June 27, 2012Publication date: June 26, 2014Applicant: MERIAL LIMITEDInventors: Charles Q. Meng, Clare Louise Murray, Itta Bluhn-Chertudi, Mustapha Soukri, Mary George Johnson
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Publication number: 20140171444Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: March 3, 2014Publication date: June 19, 2014Applicant: THE TEXAS A&M UNIVERSITY SYSTEMInventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Publication number: 20140171473Abstract: Disclosed are novel novel polymorphic solvated and desolvated forms of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)phenyl]-benzenesulfonamide. One embodiment of the present invention is directed to a crystalline sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]benzenesulfonamide (hereinafter “Compound A-1,4-dioxane/water solvate”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (° 28), when measured using Cu Ku radiation, at about 4.0,8.1, 10.1, 14.2, 16.2, 18.6,20.3,24.7,25.0, and 26.5.Type: ApplicationFiled: July 20, 2012Publication date: June 19, 2014Applicant: CHEMOCENTRYX, INC.Inventors: Joanna Bis, David H. Igo
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Publication number: 20140171445Abstract: The invention provides a method of enhancing the efficacy of antibiotic treatment of tuberculosis, trypanosomiasis, leprosy, and leishmaniasis involving co-administering to a mammal undergoing antibiotic treatment therapeutically effective amounts of a first compound that is an inhibitor of 5-lipoxygenase and optionally a second compound that is a product of the cyclooxygenase pathways. The invention also provides a pharmaceutical composition comprising an antibiotic, an inhibitor of 5-lipoxygenase, and a product of the cyclooxygenase pathways.Type: ApplicationFiled: August 2, 2012Publication date: June 19, 2014Applicant: The USA, as represented by the Secretary, Department of Health and Human ServicesInventors: Katrin Mayer-Barber, Bruno de Bezerril Andrade, Alan Sher, Daniel Leo Barber
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Patent number: 8754229Abstract: 3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinic acids having a halogen, alkyl or mono-, di- tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: June 29, 2012Date of Patent: June 17, 2014Assignee: Dow AgroSciences, LLC.Inventors: Jeffrey B. Epp, Christian T. Lowe, James M. Renga, Paul R. Schmitzer, Joseph D. Eckelbarger, Katherine A. Guenthenspberger, Thomas L. Siddall, Carla N. Yerkes, Lindsey Gayle Fischer, Natalie Christine Giampietro, Jeremy Kister, Joshua Roth
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Patent number: 8754110Abstract: Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenyl-boronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. The organic phase and the aqueous phase are separated. The 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate, which is deacetylated to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate.Type: GrantFiled: December 28, 2012Date of Patent: June 17, 2014Assignee: Dow AgroSciences, LLC.Inventors: Jossian Oppenheimer, Mark V. M. Emonds, Christopher W. Derstine, Robert C. Clouse
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Patent number: 8754109Abstract: The present invention relates to methods involving avoiding adverse drug interactions with pirfenidone and CYP inducers, such as smoking.Type: GrantFiled: December 3, 2010Date of Patent: June 17, 2014Assignee: Intermune, Inc.Inventors: Williamson Z. Bradford, Javier Szwarcberg
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Patent number: 8748624Abstract: The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.Type: GrantFiled: May 23, 2012Date of Patent: June 10, 2014Assignee: Janssen Pharmaceutica NVInventors: Devraj Chakravarty, Kevin Kreutter, Mark Powell, Brian Shook, Fengbin Song, Guozhang Xu, Shyh-Ming Yang, Rui Zhang, Bao-Ping Zhao
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Publication number: 20140155438Abstract: Disclosed are novel polymorphic trihydrated forms of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl] benzenesulfonamide. One embodiment of the present invention is directed to a crystalline form of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-25 phenyl]-benzenesulfonamide (hereinafter “Compound A _ crystal-line trihydrate form I”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (°28), when measured using Cu Ka radiation, at about 4.5, 9.0, 13.6, 13.9, 15.8, 17.8, 18.2, 18.5, 19.1, 19.9, 20A, 21.2, 22.1, 22.7, 24.3, 25.0, 25.6, 26.2, 26.8, 27.3, 27.6, 28.0, 28.8, and 30.8.Type: ApplicationFiled: July 20, 2012Publication date: June 5, 2014Applicant: CHEMOCENTRYX, INC.Inventors: Joanna Bis, David H. Igo, Bert Ho, Deven Shah
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Publication number: 20140142137Abstract: Provided herein, inter alia, are novel compounds for the inhibition of HIV integrase. The compounds disclosed herein are useful for methods of treating HIV infection in a subject in need thereof.Type: ApplicationFiled: August 2, 2013Publication date: May 22, 2014Applicants: National Institutes of Health, The Regents of the University of CaliforniaInventors: Seth M. Cohen, Arpita Agrawal, Jamie DeSoto, Yves Pommier, Kasthuraiah Maddali
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Publication number: 20140135328Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Patent number: 8722895Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: GrantFiled: April 9, 2013Date of Patent: May 13, 2014Assignee: Akebia Therapeutics, Inc.Inventors: Richard M. Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Publication number: 20140128427Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
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Publication number: 20140127294Abstract: Provided is an oral solid preparation of a compound anti-tubercular drug, wherein the active ingredients are rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride. The compound oral solid preparation is a coated tablet with coated core or a coated three-layer tablet, wherein the two active ingredients rifampicin and isoniazid do not contact directly. The compound oral solid preparation not only improves the stability of the compound preparation, but also improves the bioavailability of rifampicin.Type: ApplicationFiled: April 10, 2012Publication date: May 8, 2014Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.Inventors: Maojian Gu, Qilan Zheng, Chao Xu, Ning Li, Guixian Chen, Lan Zheng, Min Wang, Lintao Jiang
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Patent number: 8710086Abstract: Substituted di-arylhydantoin and di-arylthiohydantoins are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including CRPC and/or hormone-sensitive prostate cancer.Type: GrantFiled: April 9, 2010Date of Patent: April 29, 2014Assignee: Medivation Technologies, Inc.Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
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Patent number: 8710234Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: GrantFiled: September 20, 2013Date of Patent: April 29, 2014Assignee: Mitsui Chemicals, Inc.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Publication number: 20140107160Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: October 9, 2013Publication date: April 17, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
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Publication number: 20140107134Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.Type: ApplicationFiled: September 27, 2013Publication date: April 17, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
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Publication number: 20140107166Abstract: The present invention provides novel compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.Type: ApplicationFiled: February 13, 2012Publication date: April 17, 2014Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Ralph Mazitschek, James E. Bradner, Melissa Grachan Harman
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Patent number: 8697734Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a benzoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.Type: GrantFiled: August 10, 2012Date of Patent: April 15, 2014Assignee: E I du Pont de Nemours and CompanyInventors: George Philip Lahm, Stephen Frederick McCann, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20140094465Abstract: The present invention is directed to compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: June 5, 2012Publication date: April 3, 2014Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Patent number: 8685978Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: GrantFiled: July 26, 2010Date of Patent: April 1, 2014Assignee: University of Tennessee Research FoundationInventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, Vnr Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Publication number: 20140088046Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: September 5, 2013Publication date: March 27, 2014Applicant: ZOETIS LLCInventors: Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
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Patent number: 8680100Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: GrantFiled: December 1, 2009Date of Patent: March 25, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Patent number: 8669370Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: January 24, 2012Date of Patent: March 11, 2014Assignee: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Patent number: 8669209Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.Type: GrantFiled: November 22, 2010Date of Patent: March 11, 2014Assignee: Dow AgroSciences, LLC.Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry