Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/155)
  • Patent number: 10370337
    Abstract: The present invention is directed to oxycyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). 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: Grant
    Filed: July 27, 2016
    Date of Patent: August 6, 2019
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Antonella Converso, Mildred L. Kaufman, Kevin Rodzinak
  • Publication number: 20150141458
    Abstract: The subject invention provides a method of treating a subject afflicted with glaucoma, suffering from retinal ganglion cell (RGC) loss or damage, or elevated intraocular pressure (IOP), or of reducing RGC loss or damage, or reducing IOP in a subject, comprising administering to the subject an amount of laquinimod effective to treat the subject, to reduce RGC loss or damage, or to reduce IOP in the subject. Provide also is a pharmaceutical composition, a package and a therapeutic package for treating a subject afflicted with glaucoma.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 21, 2015
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Ron Neumann, Revital Etzyoni
  • Publication number: 20150133493
    Abstract: Compounds including those of the Formula I where X, R1, R2 and subscript t are as defined herein, useful as ?-secretase inhibitors, are provided, as are compositions comprising the compounds, as well as methods for use of the compounds for treating or preventing neurodegenerative diseases, such as, for instance, Alzheimer's disease.
    Type: Application
    Filed: July 3, 2014
    Publication date: May 14, 2015
    Inventors: Lei Zhu, Hakim Djaballah, Yueming Li, Christopher Chad Shelton
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150105376
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 9006443
    Abstract: Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of quinoline-3-carboxamide derivatives such as laquinimod, or a pharmaceutically acceptable salt thereof, in high yield and purity.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: April 14, 2015
    Assignee: Actavis Group PTC ehf
    Inventors: Girish Dixit, Krishnadatt Sharma, Kundan Singh Shekhawat, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • Publication number: 20150086549
    Abstract: This invention provides a method of treating a subject afflicted with active lupus arthritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus arthritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with lupus arthritis.
    Type: Application
    Filed: December 1, 2014
    Publication date: March 26, 2015
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Asi Haviv, Nora Tarcic
  • Patent number: 8980895
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: March 17, 2015
    Assignee: Mercury Therapeutics, Inc.
    Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
  • Publication number: 20150065487
    Abstract: 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: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Publication number: 20150057311
    Abstract: The present invention relates to heterocyclic substituted quinoline derivatives as allosteric inhibitors of the glycogen synthase kinase-3 (GSK-3) enzyme. Therefore, these compounds are useful for the manufacturing of a medicament designed for the treatment and/or prevention of diseases wherein GSK-3 is involved, such as neurodegenerative diseases, inflammatory diseases, cancer, diabetes, and to promote various regenerative processes.
    Type: Application
    Filed: September 28, 2012
    Publication date: February 26, 2015
    Applicant: Consejo Superior de Investigaciones Cientificas (CSIC)
    Inventors: Ana Martinez Gil, Carmen Gil Ayuso-Gontan, Valle Palomo Ruiz, Concepcion Perez Martin, Daniel I. Perez Fernandez, Julio Alberto Reyes Rodriguez
  • Patent number: 8962598
    Abstract: The present invention relates to compounds which are 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: February 24, 2015
    Assignee: Immunahr AB
    Inventor: Lars Pettersson
  • Publication number: 20150038508
    Abstract: This invention provides a method of treating a subject afflicted with active lupus nephritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis.
    Type: Application
    Filed: October 21, 2014
    Publication date: February 5, 2015
    Applicant: Teva Pharmaceutical Industries, Ltd.
    Inventors: Asi Haviv, Nora Tarcic
  • Patent number: 8946430
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: September 24, 2012
    Date of Patent: February 3, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150005287
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: January 1, 2015
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140343096
    Abstract: The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses.
    Type: Application
    Filed: March 14, 2014
    Publication date: November 20, 2014
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Victor Piryatinsky, Avital Laxer
  • Publication number: 20140323725
    Abstract: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.
    Type: Application
    Filed: June 2, 2014
    Publication date: October 30, 2014
    Applicant: BioMarin Pharmaceutical Inc.
    Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Quan Jiang, Lei Lu
  • Patent number: 8871936
    Abstract: A method for preparing a compound of formula (I) by reacting the appropriate alkyl ester and an aniline derivative, in a refluxing mixture containing an aliphatic solvent or a mixture of aliphatic solvents having a boiling point in the range of 68-191° C.; condensing vapors of the refluxing mixture; treating the condensed vapors with an alcohol scavenging agent or a mixture of alcohol scavenging agents; and returning the condensed vapors back to the reaction mixture.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: October 28, 2014
    Assignee: Active Biotech AB
    Inventors: Lillemor Maria Bock, Par Henning Holmberg, Karl-Erik Jansson
  • Publication number: 20140303127
    Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
    Type: Application
    Filed: November 9, 2012
    Publication date: October 9, 2014
    Inventors: Jose Aiguade Bosch, Silvia Gual Roig, Maria Prat Quinones, Carlos Puig Duran
  • Publication number: 20140271878
    Abstract: The subject invention provides a mixture of crystalline laquinimod sodium particles, wherein (i) 90% or more of the total amount by volume of the laquinimod sodium particles have a size of 40 microns or less or (ii) 50% or more of the total amount by volume of the laquinimod sodium particles have a size of 15 microns or less, and wherein: a) the mixture has a bulk density of 0.2 g/mL to 0.4 g/mL; b) the mixture has a tapped density of 0.40 g/mL to 0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 0.002% of heavy metal relative to the amount by weight of laquinimod sodium; d) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline (MCQ) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroqunoline-3-carboxylic acid (MCQCA) in the mixture is no more than 0.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Anton Frenkel, Avital Laxer
  • Publication number: 20140243314
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 28, 2014
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20140235670
    Abstract: This invention provides a method for treating a human subject afflicted with a progressive form of multiple sclerosis, comprising periodically administering to the human subject an amount of laquinimod effective to treat the human subject. This invention also provides laquinimod for use in treating a human subject afflicted with a progressive form of multiple sclerosis. This invention further provides pharmaceutical compositions and packages comprising an effective amount of laquinimod for treating a progressive form of multiple sclerosis.
    Type: Application
    Filed: February 13, 2014
    Publication date: August 21, 2014
    Applicant: Teva Pharmaceutical Industries, Ltd.
    Inventors: Nora Tarcic, Dan Bar-Zohar, Liat Hayardeny, Yossi Gilgun Sherki, Tali Gorfine, Volker Knappertz, Ella Sorani
  • Patent number: 8809537
    Abstract: The subject invention provides pharmaceutical compositions containing laquinimod or a pharmaceutically acceptable salt thereof, an isolated compound of N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide or a salt thereof, compositions containing N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide and methods of preparing the same.
    Type: Grant
    Filed: May 7, 2013
    Date of Patent: August 19, 2014
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Avital Laxer, Konstantin Ulanenko
  • Publication number: 20140213613
    Abstract: A novel crystalline form of a compound is disclosed.
    Type: Application
    Filed: August 31, 2012
    Publication date: July 31, 2014
    Inventor: Mei-yin Lee
  • Publication number: 20140206676
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 24, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20140200243
    Abstract: This application provides for a method of treating a subject suffering from Crohn's disease, the method comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This application provides for use of laquinimod in the manufacture of a medicament for treating a subject suffering from Crohn's disease. This application also provides for a pharmaceutical composition comprising laquinimod for use in treating a subject suffering from Crohn's disease.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Nora Tarcic, Asi Haviv, Eran Blaugrund, Joel Kaye
  • Patent number: 8772493
    Abstract: The present invention relates to a compound represented by formula 1 in the present specification or a pharmaceutically acceptable thereof, which inhibits an apoptosis mechanism of auditory hair cells for various ototoxicities leading to deafness, and protects the auditory organ and hearing, a method for preparation thereof, and a composition containing the same.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: July 8, 2014
    Assignees: Ajou University Industry-Academic Cooperation Foundation, Korea Research Institute of Chemical Technology
    Inventors: Chul Ho Kim, Young Sik Jung
  • Publication number: 20140187550
    Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.
    Type: Application
    Filed: December 16, 2013
    Publication date: July 3, 2014
    Applicant: Novartis AG
    Inventor: Roger John Taylor
  • Publication number: 20140179675
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140171431
    Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.
    Type: Application
    Filed: May 15, 2012
    Publication date: June 19, 2014
    Inventors: Jianhua Shen, Yiping Wang, Kai Wang
  • Publication number: 20140171647
    Abstract: Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.
    Type: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Anton Frenkel, Eduard Gurevich, Avital Laxer
  • Publication number: 20140155431
    Abstract: 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: Application
    Filed: December 19, 2013
    Publication date: June 5, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Publication number: 20140128430
    Abstract: The subject invention provides a Laquinimod amine salt, which is laquinimod meglumine, laquinimod choline hydroxide, laquinimod L-lysine or laquinimod monoethanolamine.
    Type: Application
    Filed: October 31, 2013
    Publication date: May 8, 2014
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Anton Frenkel, Avital Laxer, Judith Aronheim
  • Publication number: 20140112946
    Abstract: Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl)-phenyl]-1,2-dihydroquinoline-3-carboxamide, having a deuterium enrichment in the amide-N methyl group of at least 70%; or a salt thereof with a pharmaceutically acceptable organic or inorganic cation; and a method of preparing said compounds. The compounds are useful in therapy, e.g. for the treatment of a malignant hyperproliferative disorder or an autoimmune disease.
    Type: Application
    Filed: June 22, 2012
    Publication date: April 24, 2014
    Applicant: ACTIVE BIOTECH AB
    Inventor: Leif Svensson
  • Publication number: 20140107094
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Joan Pierce, Steven Goldberg, Anne Fourie, Xiaohua Xue
  • Publication number: 20140107097
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Taraneh Mirzadegan, Kelly Ganamet
  • Publication number: 20140105850
    Abstract: The subject invention provides for methods of reducing the relapse rate and/or reducing the accumulation of physical disability in a relapsing-remitting multiple sclerosis human patient, the method comprising orally administering to the patient a daily dose of 0.6 mg laquinimod. The subject invention also provides for pharmaceutical oral unit dosage forms of 0.6 mg laquinimod for use in reducing the relapse rate and/or for use in reducing the accumulation of physical disability in a relapsing-remitting multiple sclerosis human patient.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 17, 2014
    Applicant: Teva Pharmaceutical Industries, Ltd.
    Inventors: Nora Tarcic, Dan Bar-Zohar, Dina Kofler
  • Publication number: 20140080867
    Abstract: 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: Application
    Filed: November 26, 2013
    Publication date: March 20, 2014
    Applicant: Grünenthal GmbH
    Inventors: Sven KÜHNERT, Gregor BAHRENBERG, Achim KLESS, Wolfgang SCHRÖDER
  • Publication number: 20140051723
    Abstract: The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses.
    Type: Application
    Filed: October 24, 2013
    Publication date: February 20, 2014
    Applicant: Teva Pharmaceutical Industries, Ltd.
    Inventors: Victor Piryatinsky, Avital Laxer
  • Publication number: 20140005401
    Abstract: Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of quinoline-3-carboxamide derivatives such as laquinimod, or a pharmaceutically acceptable salt thereof, in high yield and purity.
    Type: Application
    Filed: September 9, 2013
    Publication date: January 2, 2014
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Girish Dixit, Krishnadatt Sharma, Kundan Singh Shekhawat, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • Publication number: 20130345257
    Abstract: Provided herein are compositions and methods associated with the prevention and treatment of lupus nephritis. In particular, provided herein is a method for delaying onset of active lupus nephritis in a subject at risk for developing active lupus nephritis, comprising periodically administering to the subject an amount of laquinimod effective to delay onset of active lupus nephritis in the subject. Also provided herein are laquinimod (LAQ) and a pharmaceutical composition comprising an amount of LAQ for use in delaying onset of active lupus nephritis in a subject at risk for developing active lupus nephritis.
    Type: Application
    Filed: June 26, 2013
    Publication date: December 26, 2013
    Applicant: The Regents of the University of California
    Inventors: Bevra H. HAHN, Maida Wong, Brian Skaggs, Elaine Lourenco
  • Publication number: 20130345212
    Abstract: The present invention relates to compounds of the formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds as activators of AMPK.
    Type: Application
    Filed: March 5, 2012
    Publication date: December 26, 2013
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Alain Claude-Marie Daugan, Olivier Mirguet, Yann Lamotte
  • Publication number: 20130345256
    Abstract: The subject invention provides pharmaceutical compositions containing laquinimod or a pharmaceutically acceptable salt thereof, an isolated compound of N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide or a salt thereof, compositions containing N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide and methods of preparing the same.
    Type: Application
    Filed: May 7, 2013
    Publication date: December 26, 2013
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Avital Laxer, Konstantin Ulanenko
  • Patent number: 8604056
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: December 10, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Donald J. P. Pinto, Joanne M. Smallheer, James R. Corte, Zilun Hu, Cullen L. Cavallaro, Paul J. Gilligan, Mimi L. Quan, Leon M. Smith, II
  • Patent number: 8592587
    Abstract: The disclosure relates to a method for the synthesis of a compound of the following formula (I) in which: R1 and R2 are independently an N-protective group; R3 is a hydrogen atom, a C1-C6 alkyl group, a C1-C6 arylalkyl group, a C2-C6 alkenyl group, or a alkoxycarbonylalkyl group; Y is a —C(HR4)- group in which R4 is a hydrogen atom, a C1-C6 alkyl group, an aryl group, a C1-C6 arylalkyl group, or a C2-C6 alkenyl group; or an orthophenylene group.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: November 26, 2013
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite de Montpellier I
    Inventors: Jean Martinez, Georges Dewynter, Daniel Farran
  • Patent number: 8580819
    Abstract: The subject invention provides deuterated N-ethyl-N-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: November 12, 2013
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Victor Piryatinsky, Avital Laxer
  • Publication number: 20130267559
    Abstract: The present invention relates to compounds which are quinolinone derivatives of general formula (I) capable of modulating the activity, in particular of inducing the differentiation, of stem and progenitor cells; these compounds are of use in the treatment of disorders related to a stem differentiation defect; the invention also relates to novel compounds among these quinolinone derivatives and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: November 15, 2011
    Publication date: October 10, 2013
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Martial Ruat, Helene Faure, Tatiana Gorojankina, Andre Mann, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Patent number: 8552194
    Abstract: Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of quinoline-3-carboxamide derivatives such as laquinimod, or a pharmaceutically acceptable salt thereof, in high yield and purity.
    Type: Grant
    Filed: April 27, 2009
    Date of Patent: October 8, 2013
    Assignee: Actavis Group PTC EHF
    Inventors: Girish Dixit, Krishnadatt Sharma, Kundan Singh Shekhawat, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • Publication number: 20130245065
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Application
    Filed: November 28, 2011
    Publication date: September 19, 2013
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Patent number: 8524907
    Abstract: Novel methods of preparing a compound of Formula I which is an inhibitor of Factor Xa and its maleate salt, are described herein.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: September 3, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, James P Kanter, Keiko Sujino, Sharique Sami Zuberi, Carroll Scarborough
  • Publication number: 20130217724
    Abstract: The subject invention provides a pharmaceutical composition containing laquinimod or a pharmaceutically acceptable salt thereof, and a compound of N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide or a salt thereof.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 22, 2013
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Vladimir Ioffe, Konstantin Ulanenko, Avital Laxer, Muhammad Safadi, Danit Licht, Ioana Lovinger, Ulf Tomas Fristedt