Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/309)
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Patent number: 8741259Abstract: Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.Type: GrantFiled: October 20, 2008Date of Patent: June 3, 2014Inventors: Marvin C. Gershengorn, Susanne Neumann, Bruce M. Raaka, Craig J. Thomas, James Inglese, Noel T. Southall, Steven Titus, Wei Zheng, Wenwei Huang, Gerd Krause, Gunnar Kleinau
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Publication number: 20140148480Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2— amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.Type: ApplicationFiled: January 15, 2014Publication date: May 29, 2014Applicant: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6)Inventors: Michele REBOUD-RAVAUX, Chahrazade YERROUM-EL AMRI, Xiao TAN, Lixian QIN, Maurice PAGANO, Alain HOVNANIAN, Laetitia FURIO, Bernard PIROTTE
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Patent number: 8735391Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.Type: GrantFiled: September 25, 2009Date of Patent: May 27, 2014Assignee: University of KansasInventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
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Publication number: 20140140956Abstract: The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.Type: ApplicationFiled: November 20, 2013Publication date: May 22, 2014Applicant: RVX Therapeutics Inc.Inventors: David John Fairfax, Gregory Scott Martin, John Frederick Quinn, Bryan Cordell Duffy, Gregory Steven Wagner, Peter Ronald Young
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Publication number: 20140142136Abstract: The present invention relates to methods and compounds for regulating or enhancing erythropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.Type: ApplicationFiled: November 19, 2013Publication date: May 22, 2014Inventors: Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Robert C. Stephenson
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Publication number: 20140135306Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.Type: ApplicationFiled: June 19, 2012Publication date: May 15, 2014Applicant: Novartis AGInventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
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Publication number: 20140135296Abstract: The invention provides methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits. In one embodiment, the invention provides a method of determining whether a subject suffers from, or is at risk of developing, and autophagy mediated disease state and/or condition by evaluating LC3 levels.Type: ApplicationFiled: May 10, 2012Publication date: May 15, 2014Inventors: Vojo Deretic, Eliseo Castillo, Steven Bradfute, Larry A. Sklar
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Publication number: 20140135327Abstract: This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are accordingly expected to be useful for their anti-proliferative activity and in methods of treatment of the human or animal body, for example in preventing or inhibiting tumour growth and metastasis in cancers. The invention also relates to processes for the manufacture of the compounds defined herein, or pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.Type: ApplicationFiled: July 6, 2012Publication date: May 15, 2014Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ronald Ernest Grigg, Martyn Inman, Graham Packham
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COMPOUNDS AND METHODS FOR MODULATING MITOCHONDRIAL METABOLISM AND REACTIVE OXYGEN SPECIES PRODUCTION
Publication number: 20140128352Abstract: Compounds that modulate mitochondrial reactive oxygen species (ROS) production are provided. The compounds may modulate ROS production at defined sites without also altering energy production. Methods of using and identifying such compounds are also provided.Type: ApplicationFiled: September 20, 2013Publication date: May 8, 2014Applicant: Buck Institute for Research on AgingInventors: Martin D. Brand, Adam Orr -
Publication number: 20140128365Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.Type: ApplicationFiled: November 2, 2012Publication date: May 8, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
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Patent number: 8716492Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as 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. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: December 15, 2011Date of Patent: May 6, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
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Patent number: 8710078Abstract: The present invention relates to crystalline solvates of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and the use thereof.Type: GrantFiled: June 27, 2012Date of Patent: April 29, 2014Assignee: SanofiInventors: Norbert Nagel, Bruno Baumgartner, Harald Berchtold, Oliver Plettenburg, Dieter Kadereit, Mandy Mohnicke, Simon Gessler, Joachim Tillner
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Patent number: 8710228Abstract: The invention relates to 6-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: GrantFiled: June 18, 2009Date of Patent: April 29, 2014Assignee: SanofiInventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Stefan Peukert, Sven Ruf, Matthias Löhn, Peter Monecke, Alexander Schiffer, Aimo Kannt, Markus Kohlmann
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Patent number: 8710077Abstract: The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: GrantFiled: June 18, 2009Date of Patent: April 29, 2014Assignee: SanofiInventors: Oliver Plettenburg, Katrin Lorenz, Jochen Goerlitzer, Matthias Löhn, Sandrine Biscarrat, Fréderic Jeannot, Olivier Duclos
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Publication number: 20140107123Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.Type: ApplicationFiled: August 5, 2013Publication date: April 17, 2014Applicant: University of MassachusettsInventors: Roger J. Davis, Anja Jaeschke
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Publication number: 20140094456Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: ApplicationFiled: March 13, 2013Publication date: April 3, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 8685984Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).Type: GrantFiled: July 5, 2013Date of Patent: April 1, 2014Assignee: AbbVie Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
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Patent number: 8680106Abstract: The present invention features interferon-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to the subject effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), an inhibitor of cytochrome P450 (e.g., ritonavir), and ribavirin.Type: GrantFiled: July 5, 2013Date of Patent: March 25, 2014Assignee: AbbVic Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
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Publication number: 20140057941Abstract: The invention relates to methods and compounds useful for treating deficiencies in hemoglobin production. Methods and compounds useful for increasing mean corpuscular volume are provided. Methods and compounds for treating microcytosis and methods and compounds for treating microcytic anemia are also provided.Type: ApplicationFiled: January 13, 2012Publication date: February 27, 2014Inventor: Kin-Hung (Peony) Yu
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Publication number: 20140051681Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: ApplicationFiled: May 3, 2013Publication date: February 20, 2014Inventors: David John AUGERI, Jeffrey Thomas BAGDANOFF, Simon David Peter BAUGH, Marianne CARLSEN, Kenneth Gordon CARSON, John Anthony GILLERAN, Wei HE, Tamas ORAVECZ, Konstantin SALOJIN, Leonard SUNG
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Publication number: 20140045846Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.Type: ApplicationFiled: October 23, 2013Publication date: February 13, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
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Publication number: 20140045872Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.Type: ApplicationFiled: September 14, 2011Publication date: February 13, 2014Applicant: NOVARTIS AGInventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
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Publication number: 20140024676Abstract: The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: July 15, 2013Publication date: January 23, 2014Inventors: Claudia Witschi, Jung Min Park, Michael D. Thompson, Michael John Martinelli, David A. Yeowell, Michael P. Arend
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Publication number: 20140024675Abstract: The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: July 15, 2013Publication date: January 23, 2014Inventors: Claudia Witschi, Jung Min Park, Michael D. Thompson, Michael John Martinelli, David A. Yeowell, Michael P. Arend
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Patent number: 8629161Abstract: There is provided a preventive for glaucoma or a preventive or a remedy for ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. A preventive or a remedy for glaucoma comprising a Rho kinase inhibitor and an ?1 blocker in combination.Type: GrantFiled: June 20, 2006Date of Patent: January 14, 2014Assignee: Kowa Co., Ltd.Inventors: Ken Mizuno, Jiro Matsumoto
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Patent number: 8623877Abstract: The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: January 7, 2014Assignee: SanofiInventors: Zhongli Gao, Ryan Hartung
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Patent number: 8618129Abstract: The invention relates to substituted 1-oxo-dihydroisoquinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: GrantFiled: August 31, 2011Date of Patent: December 31, 2013Assignee: Gruenenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder
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Publication number: 20130344061Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).Type: ApplicationFiled: March 15, 2013Publication date: December 26, 2013Applicant: INFINITY PHARMACEUTICALS, INC.Inventors: Vito J. PALOMBELLA, David G. WINKLER
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Publication number: 20130338187Abstract: The present invention relates to novel 1-(1-Oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: July 16, 2013Publication date: December 19, 2013Inventors: Richard L. Beard, John E. Donello, Tien T. Duong, Michael E. Garst, Veena Viswanath
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Patent number: 8609663Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.Type: GrantFiled: November 17, 2010Date of Patent: December 17, 2013Assignee: University of MassachusettsInventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
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Patent number: 8609691Abstract: The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I?) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: GrantFiled: January 25, 2008Date of Patent: December 17, 2013Assignee: SanofiInventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Joachim Brendel, Matthias Loehn, Jean-Michel Altenburger
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Patent number: 8598201Abstract: The present invention relates to new crystalline polymorphs of 6-(Piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride, processes for their preparation and their use, in particular for the preparation of medicaments.Type: GrantFiled: June 27, 2012Date of Patent: December 3, 2013Assignee: SanofiInventors: Norbert Nagel, Bruno Baumgartner, Harald Berchtold, Oliver Plettenburg, Dieter Kadereit, Mandy Mohnicke, Simon Gessler, Joachim Tillner
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Publication number: 20130317010Abstract: To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HT5A receptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HT5A receptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Applicant: Astellas Pharma IncInventors: Wataru HAMAGUCHI, Isao KINOYAMA, Yohei KOGANEMARU, Takehiro MIYAZAKI, Osamu KANEKO, Ryuichi SEKIOKA, Takuya WASHIO
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Patent number: 8592416Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.Type: GrantFiled: May 19, 2010Date of Patent: November 26, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
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Patent number: 8586570Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: April 27, 2011Date of Patent: November 19, 2013Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
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Patent number: 8580817Abstract: The present invention relates to novel 1-(1-Oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: GrantFiled: February 10, 2012Date of Patent: November 12, 2013Assignee: Allergan, Inc.Inventors: Richard L. Beard, John E. Donello, Tien T. Duong, Michael E. Garst, Veena Viswanath
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Publication number: 20130296333Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: July 9, 2013Publication date: November 7, 2013Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Publication number: 20130296363Abstract: Provided herein are compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 31, 2011Publication date: November 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Raffaella Faraoni, Michael J. Hadd, Mark W. Holladay, Martin W. Rowbottom, Eduardo Setti
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Publication number: 20130289027Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).Type: ApplicationFiled: January 23, 2012Publication date: October 31, 2013Applicant: ViiV Healthcare UK LimitedInventors: Martha Alicia De La Rosa, Simon Haydar, Brian Alvin Johns, Emile Johann Velthuisen
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Patent number: 8569282Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: GrantFiled: December 11, 2008Date of Patent: October 29, 2013Assignee: CytoPathfinder, Inc.Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
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Patent number: 8569298Abstract: The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.Type: GrantFiled: June 15, 2009Date of Patent: October 29, 2013Assignee: Astrazeneca ABInventors: Bernard Christophe Barlaam, Patrick Ple, Kevin Michael Foote, Clifford David Jones
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Publication number: 20130281398Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter R. Young
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Publication number: 20130281397Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter Ronald Young
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Publication number: 20130273004Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.Type: ApplicationFiled: March 14, 2013Publication date: October 17, 2013Inventors: Guoqing CHEN, Jeffrey A. ADAMS, Jean E. BEMIS, Shon BOOKER, Guolin CAI, Lucian V. DIPIETRO, Celia DOMINGUEZ, Daniel ELBAUM, Julie GERMAIN, Stephanie D. GEUNS-MEYER, Michael K. HANDLEY, Qi HUANG, Joseph L. KIM, Tae-Seong KIM, Alexander S. KISELYOV, Xiaohu OUYANG, Vinod F. PATEL, Leon M. SMITH, II, Markian M. STEC, Andrew TASKER, Ning XI, Shimin XU, Chester YUAN, Michael CROGHAN
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Publication number: 20130274286Abstract: The present invention relates to identification of a compound which inhibits the enzyme NMPRTase and glioma cancer cell growth and further used for glioma therapy. Pre-B-cell colony enhancing factor 1 gene (PBEF1) encodes nicotinamide phosphoribosyltransferase (NMPRTase), which catalyses the rate limiting step in the salvage pathway of NAD metabolism in mammalian cells. PBEF1 transcript and protein levels have been shown to be elevated in glioblastoma and a chemical inhibitor of NMPRTase has been shown to specifically inhibit cancer cells. Here a structure based drug discovery approach has been reported with an aim to develop novel inhibitors for glioblastoma therapy. Present invention relates to virtual screening using docking of ligands from a large library of 13,000 compounds against NMPRTase as the macromolecular target resulting in short listing of 34 possible ligands, of which six were tested experimentally, using the NMPRTase enzyme inhibition assay and further with the glioma cell viability assays.Type: ApplicationFiled: March 31, 2011Publication date: October 17, 2013Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Somasundaram Kumaravel, Nagasuma Chandra
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Publication number: 20130267521Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Applicants: Intellikine LLC, Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
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Publication number: 20130253005Abstract: Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.Type: ApplicationFiled: April 29, 2011Publication date: September 26, 2013Applicants: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.Inventors: Alan D. D'Andrea, Gregory D. Cuny, Ross L. Stein, Marcie Glicksman, April Case, Jun Xian, David Wilson, Min Huang
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Patent number: 8541449Abstract: The invention relates to substituted isoquinoline and isoquinolinones of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: GrantFiled: June 19, 2009Date of Patent: September 24, 2013Assignee: SanofiInventors: Oliver Plettenburg, Katrin Lorenz, John Weston, Matthias Loehn, Heinz-Werner Kleemann, Olivier Duclos, Frederic Jeannot
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Publication number: 20130245037Abstract: The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided.Type: ApplicationFiled: May 17, 2013Publication date: September 19, 2013Applicant: FibroGen, Inc.Inventors: Volkmar Guenzler-Pukall, Thomas B. Neff, Qingjian Wang, Michael P. Arend, Lee A. Flippin, Alex Melekhov
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Patent number: 8530469Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.Type: GrantFiled: October 12, 2011Date of Patent: September 10, 2013Assignee: Astex Therapeutics Ltd.Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford, Maria Grazia Carr, Robert Downham, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead