Additional Hetero Ring Attached Directly Or Indirectly To The Quinoline Ring System By Nonionic Bonding Patents (Class 514/314)
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Publication number: 20140072536Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.Type: ApplicationFiled: March 15, 2013Publication date: March 13, 2014Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of NevadaInventors: Ryan Wuebbles, Dean Burkin
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Patent number: 8669274Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: December 13, 2011Date of Patent: March 11, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
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Patent number: 8669272Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: October 15, 2009Date of Patent: March 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, John D. Schreier, David B. Whitman
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Publication number: 20140066442Abstract: Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y1, Y2, Y3, L1, L2, RG and R1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: ApplicationFiled: November 8, 2013Publication date: March 6, 2014Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Nicola Rahn, Tomaki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
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Publication number: 20140066424Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: March 6, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Christopher L. Carroll, Joe Marszalek, Barbara Czako, Ryan Johnson, Jay Theroff
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Publication number: 20140066412Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: November 6, 2013Publication date: March 6, 2014Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
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Patent number: 8664245Abstract: The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof.Type: GrantFiled: December 8, 2011Date of Patent: March 4, 2014Assignee: SanofiInventors: Beverly C. Langevin, Robert Allan Farr, Dinubhai H. Shah, Daniel Sherer
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Patent number: 8658170Abstract: Provided is a method of treating a proliferative disease, condition, or disorder in a subject by administering a combination of an inhibitor of p53 and MDM2 binding and an EGFR inhibitor. Various embodiments of the disclosed methods provide a synergistic anti-proliferative or anti-apoptotic effect compared to administration of one agent alone.Type: GrantFiled: July 21, 2011Date of Patent: February 25, 2014Inventors: Joseph P. Errico, Benjamin Mugrage, Ignatius Turchi, Matthew Sills, Jane Ong, John Allocco, Pam Wines
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Patent number: 8658636Abstract: The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: GrantFiled: March 23, 2011Date of Patent: February 25, 2014Assignee: GlaxoSmithKline, LLCInventors: Carl A. Brooks, Mui Cheung, Hilary S. Eidam, Ryan M. Fox, Mark A. Hilfiker, Eric S. Manas, Guosen Ye
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Patent number: 8658183Abstract: This invention relates to a parenteral formulation containing an effective amount of the compound of the following formula I: water, and an isotonic agent. Also disclosed is a method of treating an infectious disease by administering this formula to a subject via parenteral injection or infusion.Type: GrantFiled: August 9, 2007Date of Patent: February 25, 2014Assignee: Taigen Biotechnology Company, Ltd.Inventors: Lih-Huei Lee, Po-Yi Wu, Erkuan Sun, Chi-Hsin Richard King
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Publication number: 20140051660Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui, Christopher Flores
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Publication number: 20140051683Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.Type: ApplicationFiled: April 23, 2013Publication date: February 20, 2014Applicant: AbbVie Inc.Inventors: Xilu WANG, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
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Publication number: 20140051682Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: September 24, 2013Publication date: February 20, 2014Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
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Publication number: 20140051688Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui
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Patent number: 8653070Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: December 14, 2010Date of Patent: February 18, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
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Patent number: 8653105Abstract: A series of quinoline derivatives, substituted by an optionally substituted bicyclic heteroaryl moiety consisting of two fused six-membered aromatic rings attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: November 11, 2010Date of Patent: February 18, 2014Assignee: UCB Pharma S.A.Inventors: Daniel Rees Allen, Roland Bürli, Alan Findlay Haughan, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Andrew Sharpe
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Publication number: 20140045855Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: August 2, 2013Publication date: February 13, 2014Applicant: AMGEN INC.Inventors: Kaustav BISWAS, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. HORNE, Matthew R. KALLER, Vu Van MA, Kelvin SHAM, Wenge ZHONG
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Publication number: 20140045890Abstract: Compounds of the general formula (I) wherein the substituents are as defined in claim 1, are useful as fungicides.Type: ApplicationFiled: March 28, 2012Publication date: February 13, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Guillaume Berthon, Fiona Kessabi Murphy, Renaud Beaudegnies, Clemens Lamberth, Laura Quaranta, Stephan Trah
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Publication number: 20140045825Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.Type: ApplicationFiled: September 14, 2011Publication date: February 13, 2014Applicant: Exelixis, Inc.Inventor: James William Leahy
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Publication number: 20140045854Abstract: The present invention relates to methods of treating a disease related to cell hyper-proliferation via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently.Type: ApplicationFiled: October 11, 2013Publication date: February 13, 2014Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Al-Elheiga, Mizuki Watanabe
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Publication number: 20140038965Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comparing cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 17, 2013Publication date: February 6, 2014Applicant: EnVivo Pharmaceuticals, Inc.Inventors: Amy RIPKA, Gideon SHAPIRO, Richard CHESWORTH
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Publication number: 20140038821Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Publication number: 20140038922Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.Type: ApplicationFiled: May 1, 2013Publication date: February 6, 2014Inventors: Lawrence LUM, Michael G. ROTH, Baozhi CHEN, Chuo CHEN, Michael E. DODGE, Wei TANG
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Publication number: 20140038920Abstract: The invention refers to TFEB phosphorylation inhibitors. Such molecules have a therapeutic applicability in all disorders that need induction of the cell authophagic/lysosomal system, such as lysosomal storage disorders, neurodegenerative diseases, hepatic diseases, muscle diseases and metabolic diseases.Type: ApplicationFiled: March 7, 2012Publication date: February 6, 2014Applicant: FONDAZIONE TELETHONInventors: Andrea Ballabio, Carmine Settembre, Diego Luis Medina Sanabria
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Publication number: 20140038942Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.Type: ApplicationFiled: February 10, 2012Publication date: February 6, 2014Applicants: Merck Sharp & Dohme B.V., Merck Sharp & Dohme Corp.Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
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Publication number: 20140038962Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.Type: ApplicationFiled: September 20, 2013Publication date: February 6, 2014Applicant: GEORGETOWN UNIVERSITYInventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
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Patent number: 8642598Abstract: The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound. In particular, compounds of the general formula (I) are useful for inhibiting glycogen synthase kinase 3 (GSK-3).Type: GrantFiled: October 19, 2007Date of Patent: February 4, 2014Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Sean C. Turner, Margaretha Henrica Maria Bakker, Kent D. Stewart
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Publication number: 20140031335Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.Type: ApplicationFiled: April 12, 2012Publication date: January 30, 2014Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: SeoHee Lee, Jung Taek Oh, JaeKwang Lee, JaeWon Lee, Suyeal Bae, Nina Ha, Sera Lee
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Publication number: 20140031391Abstract: The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders.Type: ApplicationFiled: July 18, 2013Publication date: January 30, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Michael HAHN, Markus FOLLMANN, Walter HÜBSCH, Eva-Maria BECKER, Johannes-Peter STASCH, Joerg KELDENICH, Martina DELBECK, Hanna TINEL, Frank WUNDER, Joachim MITTENDORF, Ildiko TEREBESI, Dieter LANG, René MARTIN
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Publication number: 20140031338Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.Type: ApplicationFiled: April 13, 2012Publication date: January 30, 2014Applicant: LABORATOIRE BIODIMInventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
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Patent number: 8637543Abstract: A series of quinoline and quinoxaline derivatives, substituted by a fused bicyclic pyridine or pyrimidine moiety attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: November 11, 2010Date of Patent: January 28, 2014Assignee: UCB Pharma S.A.Inventors: Roland Bürli, Alan Findlay Haughan, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Andrew Sharpe
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Publication number: 20140024671Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: July 9, 2013Publication date: January 23, 2014Inventors: Michael EISSENSTAT, Dehui DUAN
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Publication number: 20140024647Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 18, 2012Publication date: January 23, 2014Inventor: Akira Yukimasa
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Patent number: 8633187Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: GrantFiled: March 5, 2012Date of Patent: January 21, 2014Assignee: GlaxoSmithKline LLCInventors: Steven David Knight, Stanley J. Schmidt
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Publication number: 20140018370Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: July 2, 2013Publication date: January 16, 2014Inventors: Britton Kenneth Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
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Patent number: 8629147Abstract: The present invention provides compounds capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.Type: GrantFiled: November 2, 2006Date of Patent: January 14, 2014Assignee: ChemBridge CorporationInventors: Alexey Vyacheslavovich Anikin, Vidyasagar Reddy Gantla, Vlad Edward Gregor, Luyong Jiang, Yahua Liu, Danny Peter Claude McGee, Charles Chamchoumis Mikel, Jason Conrad Pickens, Thomas Roy Webb, Zheng Yan, Tong Zhu, Aleksander Kadushkin, Sergey Sviridov, Sergey Zozulya, Alexander Chucholowski, Douglas Eric McGrath
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Publication number: 20140011836Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.Type: ApplicationFiled: September 6, 2013Publication date: January 9, 2014Applicant: University of Kentucky Research FoundationInventors: Joseph R. HOLTMAN, Peter Anthony CROOKS, Linda P. DWOSKIN, J. Michael MCINTOSH, Elzbieta Pogonowska WALA
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Publication number: 20140011808Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 17, 2013Publication date: January 9, 2014Inventors: Amy RIPKA, Gideon SHAPIRO, Richard CHESWORTH
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Publication number: 20140011840Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.Type: ApplicationFiled: January 29, 2013Publication date: January 9, 2014Applicant: Hydra Biosciences, Inc.Inventors: Magadalene M. Moran, Jayhong A. Chong, Christopher Fanger, Amy S. Ripka, Glenn R. Larsen, Xiaoguang Zhen, Dennis John Underwood, Manfred Weigele
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Publication number: 20140005221Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.Type: ApplicationFiled: January 30, 2012Publication date: January 2, 2014Applicant: SATO PHARMACEUTICAL CO., LTD.Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
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Publication number: 20140005190Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: ApplicationFiled: June 27, 2013Publication date: January 2, 2014Applicants: Genentech, Inc., The Walter and Eliza Hall Institute of Medical Research, AbbVie Inc.Inventors: JONATHAN BAYLDON BAELL, CHINH THIEN BUI, PETER COLMAN, DANETTE A. DUDLEY, WAYNE J. FAIRBROTHER, JOHN A. FLYGARE, GUILLAUME LAURENT LESSENE, CHUDI NDUBAKU, GEORGE NIKOLAKOPOULOS, CARL STEVEN RYE, BRAD EDMUND SLEEBS, BRIAN JOHN SMITH, KEITH GEOFFREY WATSON, STEVEN W. ELMORE, ANDREW M. PETROS, ANDREW J. SOUERS, PETER CZABOTAR
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Publication number: 20140005195Abstract: The present invention relates to novel bipyridine sulfonamide derivatives of formula (I) and their use for the treatment and/or prophylaxis of a neurodegenerative disease or condition, particularly Alzheimers disease (AD), a cardiovascular disease or a pathology involving ischemia. Additionally, processes for preparing such derivatives5 and pharmaceutical compositions comprising them are provided.Type: ApplicationFiled: November 21, 2011Publication date: January 2, 2014Applicant: Noscira, S.A.Inventors: Francisco Palomo Nicolau, Jorge Sánchez-Quesada, Javier López Ogalla, Félix Hernández Juan, Javier Villasante Prieto, Miguel Medina Padilla, Ana Fuertes Huerta, Juan Manuel Dominguez Correa, Susan Herrero Santos, Mercedes Alonso Cascón
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Publication number: 20140005194Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: MEI Pharma, Inc.Inventors: DiZhong CHEN, Hong Yan SONG, Eric T. SUN, Niefang YU, Yong ZOU
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Publication number: 20140004203Abstract: The present invention provides an oral pharmaceutical formulation comprising coated spheroids of a kinase inhibitor such as neratinib, which formulation is designed to reduce or eliminate side effects associated with existing oral formulations of kinase inhibitors.Type: ApplicationFiled: August 29, 2013Publication date: January 2, 2014Applicant: Wyeth LLCInventors: Sripriya Venkata Ramana Rao, Syed Muzafar Shah, Christopher Richard Diorio, Maja Vencl-Joncic, Eugene Murphy
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Publication number: 20130345199Abstract: The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5 and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.Type: ApplicationFiled: June 21, 2013Publication date: December 26, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Heinz FRETZ, Markus Gude, Philippe Guerry, Thierry Kimmerlin, Francois Lehembre, Thomas Pfeifer, Anja Valdenaire
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Publication number: 20130345196Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.Type: ApplicationFiled: May 24, 2012Publication date: December 26, 2013Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
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Publication number: 20130345241Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, X, Ar, and are defined herein or to a pharmaceutically acceptable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.Type: ApplicationFiled: August 30, 2013Publication date: December 26, 2013Applicant: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Roger Norcross, Alessandra Polara
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Publication number: 20130345154Abstract: The present invention relates to methods of reducing the risk of occurrence of, and/or treating, necrotizing enterocolitis (“NEC”) or inflammatory bowel disease (“IBD”) comprising administering, to a subject in need of such treatment, an effective amount of a gap junction enhancing agent (“GJEA”), for example a peptide (“GJP”) or peptide analog (“GJPA”). It is based, at least in part, on the discovery that greater functionality of gap junctions between enterocytes increases their rate of migration and reduces the severity of intestinal inflammation.Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventor: David J. Hackam
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Publication number: 20130345249Abstract: The invention encompasses pharmaceutical formulations for the prevention and treatment of Wolbachia-related disease wherein the formulations comprise a compound previously unknown and unused for such a purpose, the compound being one or more of: Pararosaniline Pamoate, Pyrvinium Pamoate, Clofoctol, and Isoreserpine, derivatives, metabolites, precursors, pro-drugs and variants thereof.Type: ApplicationFiled: January 13, 2012Publication date: December 26, 2013Applicant: The Regents of the University of CaliforniaInventors: Alain Debec, Laura Serbus, Frederic Landmann, William Sullivan
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Publication number: 20130338155Abstract: The present invention relates to compounds that inhibit the activity of Hsp90 and methods of using these compounds for treating or preventing infection.Type: ApplicationFiled: June 4, 2013Publication date: December 19, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Weiwen Ying