Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/156)
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Publication number: 20130281487Abstract: 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: ApplicationFiled: April 20, 2012Publication date: October 24, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Brian Luisi, Sneha Ghanshyam Arekar, Adriana Costache, Kirk Raymond Dinehart, Steven C. Johnston, Bobbianna J. Neubert-Lagille
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Publication number: 20130273581Abstract: The invention relates to haptens, immunogens and secondary immunoreactive agents, to the use thereof for producing wide-spectrum antibodies against quinolone-type antibiotics, to the application thereof to immunochemical analysis techniques, and to a kit enabling the detection of said antibiotics in biological samples from food products of animal origin.Type: ApplicationFiled: November 21, 2011Publication date: October 17, 2013Inventors: Maria Pilar Marco Colas, Francisco José Sánchez Baeza, Daniel González Pinacho
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Patent number: 8552029Abstract: Provided is a quinoline derivative of Chemical Formula (I): wherein, R1 is a substituted or unsubstituted phenyl group, R2 is a halogen, and R3 is a substituted or unsubstituted phenyl group, and one of the carbon atoms in the phenyl ring of the phenyl group is optionally substituted by a nitrogen atom (N). The quinoline derivative can efficiently inhibit cancer cell proliferation and can be used for treating cancer, especially for treating cancers related to the Janus kinase-signal transducers and activators of transcription (JAK-STAT) pathway and/or the mitogen-activated protein kinase (MAPK) pathway.Type: GrantFiled: February 6, 2012Date of Patent: October 8, 2013Assignee: National Taipei University of TechnologyInventors: Kuo-Yuan Hwa, Yu-May Lee, Yeh-Long Chen, Cherng-Chyi Tzeng, Hsin-Yuan Cho
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Publication number: 20130253200Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: ApplicationFiled: April 23, 2013Publication date: September 26, 2013Applicant: Gilead Sciences, Inc.Inventors: Eric Dowdy, Steven Pfeiffer
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Patent number: 8524740Abstract: A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(?O)(OH)2, P(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(?O)(OH)(OM), P(?O)(OM)2, P?O(O2M), S(?O)(OH)2, S(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(?O)(OH)(OM), S(?O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 iType: GrantFiled: July 13, 2011Date of Patent: September 3, 2013Assignee: Tairx, Inc.Inventors: Sheng-Chu Kuo, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Tian-Shung Wu, Tzong-Der Way, Jing-Gung Chung, Jai-Sing Yang, Chi-Hung Huang, Meng-Tung Tsai
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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: 8507684Abstract: There is provided a salt of 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid selected from the group consisting of citrate, hemi-fumarate, maleate, L-tartrate, mesylate, hydrochloride, potassium, and sodium salts.Type: GrantFiled: April 6, 2010Date of Patent: August 13, 2013Assignee: Ferrer Internacional S.A.Inventors: Albert Palomer, Luis Anglada
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Publication number: 20130202536Abstract: The invention relates to novel luminescent compositions of matter containing a fluorophore, synthetic methods for making the compositions, macromolecular conjugates of the compositions, and the use of the compositions in various methods of detection. The invention also provides kits containing the compositions and their conjugates for use in the methods of detection.Type: ApplicationFiled: January 13, 2011Publication date: August 8, 2013Applicants: NEW JERSEY INSTITUTE OF TECHNOLOGY, UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Arkady Mustaev, Maxim Kozlov, Salvatore Marras, Lev Krasnoperov, Laura Wirpsza, Shyamala Pillai
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Patent number: 8501774Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: GrantFiled: February 8, 2012Date of Patent: August 6, 2013Assignee: Morphochem Aktiengesellschaft für Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Muller, Michael W. Cappi
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Publication number: 20130184259Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: November 16, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATED
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Publication number: 20130172345Abstract: Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the general formula (1); [wherein R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, a C1-6 alkyl group, or the like; R4, R5, R6, R7, R8, R9 and R16 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or the like; A represents N—R11 or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.Type: ApplicationFiled: February 19, 2013Publication date: July 4, 2013Applicant: KOWA COMPANY, LTD.Inventor: KOWA COMPANY, LTD.
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Publication number: 20130172344Abstract: An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.Type: ApplicationFiled: June 20, 2012Publication date: July 4, 2013Inventors: Motohide SATOH, Hiroshi Kawakami, Yoshiharu Itoh, Hisashi Shinkai, Takahisa Motomura, Hisateru Aramaki, Yuji Matsuzaki, Wataru Watanabe, Shuichi Wamaki
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Publication number: 20130172346Abstract: The invention is directed to kynurenic acid analogues and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds for treating the symptoms of Huntington's disease and preventing the development of the symptoms.Type: ApplicationFiled: June 29, 2011Publication date: July 4, 2013Inventors: László Vécsei, Dénes Zádori, Péter Klivényi, Ferenc Fülöp, István Szatmári, József Toldi, Tamás Freund, Gábor Nyiri, András Szönyi
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Patent number: 8476442Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.Type: GrantFiled: March 19, 2010Date of Patent: July 2, 2013Assignee: Vertex Pharmaceutical IncorporatedInventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Lao Yap, Brian R. Krueger, Peter D. J. Grootenhuis, Fredrick F. van Goor, Martyn C. Botfield, Gregor Zlokarnik
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Patent number: 8476298Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: GrantFiled: May 24, 2007Date of Patent: July 2, 2013Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrisson B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wie Xu
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Patent number: 8476429Abstract: An intermediate for production of a quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria.Type: GrantFiled: April 25, 2012Date of Patent: July 2, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Hisashi Takahashi, Hiroaki Inagaki, Satoshi Komoriya, Makoto Takemura, Rie Miyauchi
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Publication number: 20130165442Abstract: 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: ApplicationFiled: November 30, 2012Publication date: June 27, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8471029Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: GrantFiled: March 21, 2011Date of Patent: June 25, 2013Assignee: Vertex Pharmaceutical IncorporatedInventors: Sneha G. Arekar, Steven C. Johnston, Mariusz Krawiec, Ales Medek, Praveen Mudunuri, Mark Jeffrey Sullivan
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Patent number: 8471027Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: GrantFiled: April 3, 2012Date of Patent: June 25, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Adrian Wai-Hing Cheung, Kevin Richard Guertin, Nancy-Ellen Haynes, Eric Mertz, Lida Qi, Yimin Qian, Nathan Robert Scott
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Publication number: 20130137723Abstract: It is intended to provide a salt of a compound and crystals thereof useful as a therapeutic and/or preventive agent for infectious diseases which has wide and excellent antibacterial activity and has excellent safety. [Solution] The present invention provides the hydrochloride of 7-[(1R,5S)-1-amino-5-fluoro-3-azabicyclo[3.3.0]octan-3-yl]-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid and crystals thereof, as a novel salt form of the compound and crystals thereof.Type: ApplicationFiled: August 5, 2011Publication date: May 30, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: Makoto Ono
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Patent number: 8450243Abstract: The present invention relates to novel herbicidal oxopyridine and thionopyridine derivatives of Formula (I), or an agronomically acceptable salt of said compound wherein R1, R5, R6, R7, X1, X2 and Q are as defined herein. The invention further relates to processes and intermediates for the preparation of the oxopyridine derivatives, to compositions which comprise the herbicidal compounds, and to their use for controlling weeds, in particular in crops of useful plants.Type: GrantFiled: March 31, 2010Date of Patent: May 28, 2013Assignee: Syngenta LimitedInventors: Roger Salmon, Glynn Mitchell, James Alan Morris
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Publication number: 20130123258Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Inventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
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Patent number: 8440831Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: GrantFiled: March 6, 2012Date of Patent: May 14, 2013Assignee: Gilead Sciences, Inc.Inventors: Eric Dowdy, Steven Pfeiffer
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Publication number: 20130116249Abstract: The invention relates to compounds corresponding to formula (I): in which R3 and R4 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R3 and R4 are attached. Preparation process and therapeutic use.Type: ApplicationFiled: July 4, 2011Publication date: May 9, 2013Applicant: SANOFIInventors: Chantal Alcouffe, Corentin Herbert, Gilbert Lassalle
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Publication number: 20130116437Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.Type: ApplicationFiled: September 14, 2012Publication date: May 9, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
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Patent number: 8436014Abstract: The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith.Type: GrantFiled: October 23, 2009Date of Patent: May 7, 2013Assignee: Vertex Pharmaceutical IncorporatedInventors: Beili Zhang, Mariusz Krawiec, Martyn Botfield, Peter D. J. Grootenhuis, Fredrick Van Goor
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Publication number: 20130096157Abstract: Provided is a quinoline derivative of Chemical Formula (I): wherein, R1 is a substituted or unsubstituted phenyl group, R2 is a halogen, and R3 is a substituted or unsubstituted phenyl group, and one of the carbon atoms in the phenyl ring of the phenyl group is optionally substituted by a nitrogen atom (N). The quinoline derivative can efficiently inhibit cancer cell proliferation and can be used for treating cancer, especially for treating cancers related to the Janus kinase-signal transducers and activators of transcription (JAK-STAT) pathway and/or the mitogen-activated protein kinase (MAPK) pathway.Type: ApplicationFiled: February 6, 2012Publication date: April 18, 2013Applicant: NATIONAL TAIPEI UNIVERSITY OF TECHNOLOGYInventors: Kuo-Yuan HWA, Yu-May LEE, Yeh-Long CHEN, Cherng-Chyi TZENG, Hsin-Yuan CHO
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Publication number: 20130096151Abstract: The present invention relates to the use of an anesthetic agent for killing clinically latent microorganisms associated with microbial infections and to novel combinations comprising an anesthetic agent and an antimicrobial agent for the treatment of microbial infections.Type: ApplicationFiled: March 29, 2011Publication date: April 18, 2013Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Yanmin Hu, Anthony M.R. Coates
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Patent number: 8420821Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, the present invention provides, for example, compounds represented by the formulas (6), (7-1), (7-2) and (8): wherein R is a fluorine atom or a methoxy group, R1 is a C1-C4 alkyl group, R2 is a hydroxyl-protecting group, and X2 is a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.Type: GrantFiled: March 6, 2007Date of Patent: April 16, 2013Assignee: Japan Tobacco Inc.Inventors: Koji Matsuda, Koji Ando, Shigeji Ohki, Takahiro Yamasaki, Jun-ichi Hoshi
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Publication number: 20130085281Abstract: 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: ApplicationFiled: October 30, 2012Publication date: April 4, 2013Applicant: ABBOTT LABORATORIESInventor: ABBOTT LABORATORIES
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Patent number: 8410274Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: GrantFiled: January 26, 2012Date of Patent: April 2, 2013Assignee: Vertex PharmaceuticalsInventors: Patricia Hurter, William Rowe, Christopher Ryan Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
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Patent number: 8404679Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.Type: GrantFiled: April 23, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Andreas Koblet, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Publication number: 20130072687Abstract: The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.Type: ApplicationFiled: November 16, 2012Publication date: March 21, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130072522Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.Type: ApplicationFiled: November 6, 2012Publication date: March 21, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Patent number: 8399673Abstract: The invention relates to substituted 2-mercaptoquinoline-3-carboxamides, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: GrantFiled: June 15, 2012Date of Patent: March 19, 2013Assignee: Gruenenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder
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Publication number: 20130060040Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.Type: ApplicationFiled: August 27, 2012Publication date: March 7, 2013Applicant: ABBOTT LABORATORIESInventors: Geoff G.Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
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Patent number: 8389545Abstract: The present invention is directed to quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders, and to novel M1 receptor positive allosteric modulator compounds of formulae (II) to (VIII). The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases in which the M1 receptor is involved.Type: GrantFiled: December 4, 2006Date of Patent: March 5, 2013Assignee: Merck, Sharp & Dohme, Corp.Inventors: William D. Shipe, Craig Lindsley, David Hallett
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Patent number: 8383819Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2?): wherein R is a fluorine atom or a methoxy group, and R400 is a hydrogen atom or a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.Type: GrantFiled: March 6, 2007Date of Patent: February 26, 2013Assignee: Japan Tobacco Inc.Inventors: Koji Matsuda, Koji Ando, Shigeji Ohki, Jun-ichi Hoshi, Takahiro Yamasaki
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Publication number: 20130040989Abstract: There is provided a salt of 1-cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridinyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid selected from the group consisting of citrate, hemi-fumarate, maleate, L-tartrate, mesylate, hydrochloride, potassium, and sodium salts.Type: ApplicationFiled: April 6, 2010Publication date: February 14, 2013Applicant: FERRER INTERNACIONAL S.A.Inventors: Albert Palomer, Luis Anglada
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Publication number: 20130040986Abstract: 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: ApplicationFiled: October 15, 2012Publication date: February 14, 2013Inventors: Hayley Binch, Lev T.D. Fanning, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20130035327Abstract: 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: ApplicationFiled: October 8, 2012Publication date: February 7, 2013Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20130029977Abstract: A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.Type: ApplicationFiled: July 2, 2009Publication date: January 31, 2013Inventors: Hisashi Takahashi, Satoshi Komoriya, Takahiro Kitamura, Takashi Odagiri, Hiroaki Inagaki, Toshifumi Tsuda, Kiyoshi Nakayama, Makoto Takemura, Kenichi Yoshida, Rie Miyauchi, Masatoshi Nagamochi
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Publication number: 20130018071Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: ApplicationFiled: September 19, 2012Publication date: January 17, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130005760Abstract: A heterocyclic compound of formula (I) or a salt thereof: wherein R1 is an optionally protected amino group or an optionally substituted C1-6 alkyl group; R2 and R3 are each independently a C1-2 alkyl group; X is a hydrogen atom or a halogen atom; Z1 is N or C—R4; Z2 is N or C—R5; Z3 is N or C—R6; Z4 is N or C—R7; R4, R5, R6, and R7 are each independently a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group; Z is CH or N; and A is a methylene group or a bond, which has an excellent anti-HIV activity and is useful as an anti-HIV agent.Type: ApplicationFiled: January 20, 2011Publication date: January 3, 2013Applicant: Toyama Chemical Co., Ltd.Inventors: Yuji Oonishi, Kenichiro Awasaguchi, Nobuhiko Nomura, Keisuke Tohdo, Hyouei Kawai, Tomomi Wakatsuki
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Patent number: 8344147Abstract: The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1, 4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: October 21, 2010Date of Patent: January 1, 2013Assignee: Vertex Pharmaceutical IncorporatedInventors: Narendra Bhalchandra Ambhaikar, Robert Hughes, Dennis James Hurley, Elaine Chungmin Lee, Benjamin Littler, Mehdi Numa, Stefanie Roeper, Urvi Sheth
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Patent number: 8334236Abstract: Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C?O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.Type: GrantFiled: February 2, 2010Date of Patent: December 18, 2012Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Fumiaki Takabe, Yuuki Hirano, Akira Funyu, Masami Kobayashi, Takashi Mitsunari
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Patent number: 8329908Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: GrantFiled: September 10, 2010Date of Patent: December 11, 2012Assignee: Morphochem Aktiengesellschaft fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin
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Publication number: 20120309758Abstract: 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: ApplicationFiled: June 8, 2012Publication date: December 6, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Urvi Sheth, Lev T.D. Fanning, Mehdi Numa, Hayley Binch, Dennis James Hurley, Jinglan Zhou, Sara S. Hadida Ruah, Anna R. Hazlewood, Alina Silina, Rajendran Vairagoundar, Fredrick F. Van Goor, Peter Diederik Jan Grootenhuis, Martyn C. Botfield
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Publication number: 20120302582Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-I) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers.Type: ApplicationFiled: January 26, 2011Publication date: November 29, 2012Inventors: Robert Hromas, Andrei Leitao, Tudor I. Oprea, Larry A. Sklar, Elizabeth A. Williamson, Justin Wray, Wei Wang
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Patent number: 8304434Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: GrantFiled: September 30, 2008Date of Patent: November 6, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Prasun K. Chakravarty, Yanbing Ding, Joseph L. Duffy, Hassan Pajouhesh, Pengcheng Patrick Shao, Sriram Tyagarajan, Feng Ye