Hetero Ring Is Seven-membered Consisting Of Two Nitrogens And Five Carbon Atoms Patents (Class 514/218)
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Publication number: 20140286943Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 9, 2014Publication date: September 25, 2014Inventors: Tadimeti Rao, Chengzhi Zhang
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Patent number: 8841287Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: June 11, 2009Date of Patent: September 23, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
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Publication number: 20140275017Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
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Publication number: 20140275041Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: Sareum LimitedInventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
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Publication number: 20140275030Abstract: The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, James D. Rodgers
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Publication number: 20140275040Abstract: The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Proximagen LimitedInventors: Max Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
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Publication number: 20140275025Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
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Publication number: 20140275010Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
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Publication number: 20140256685Abstract: The present invention relates to a method for treating dermal inflammation and dermal diseases by local or systemic delivery, in a subject in need of such treatment, which comprises administering a pharmaceutical composition comprising a therapeutically effective amount of at least one agonist of Formyl peptide receptor 2 (FPR2).Type: ApplicationFiled: March 4, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Richard L. Beard, John E. Donello, Veena Viswanath, Edward Hsia
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Patent number: 8828992Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.Type: GrantFiled: February 25, 2010Date of Patent: September 9, 2014Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
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Patent number: 8828991Abstract: The invention relates to azacyclyl-substituted arylthienopyrimidinones and their derivatives, of the Formula (I); and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted arylthienopyrimidinone according to Formula (I) or its derivative, and the use of the azacyclyl-substituted arylthienopyrimidinones according to Formula (I) and their derivatives as MCH antagonists.Type: GrantFiled: August 14, 2008Date of Patent: September 9, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
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Publication number: 20140249138Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: February 18, 2014Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Publication number: 20140249137Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: October 31, 2013Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis, Harmon J. Zuccola
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Publication number: 20140249139Abstract: The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X1, X2, X3, X4 and R5 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Christina Hebach, Klemens Hogenauer, Gregory Hollingworth, Ian Lewis, Alexander Baxter Smith, Nicolas Solvermann, Frederic Stauffer, Romain Wolf, Frederic Zecri
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Patent number: 8822447Abstract: The present invention is directed to substituted indazole compounds of formula (I) pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.Type: GrantFiled: April 21, 2011Date of Patent: September 2, 2014Assignee: Janssen Pharmaceutica NVInventors: Xuqing Zhang, Marta C. Abad, Alan C. Gibbs, Gee-Hong Kuo, Lawrence C. Kuo, Fengbin Song, Zhihua Sui
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Patent number: 8822495Abstract: The invention relates to azacyclyl-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the azacyclyl-substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.Type: GrantFiled: August 14, 2008Date of Patent: September 2, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
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Publication number: 20140243320Abstract: A compound represented by the following general formula (1) or a salt thereof. R1 represents a halogen atom and so on; R2 and R3 each represent a hydrogen atom and so on; R4 and R5 each represent a hydrogen atom and so on, or R4 and R5 may form an oxo group; Ra and Rb each represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural Rc; Rc represents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2.Type: ApplicationFiled: July 12, 2012Publication date: August 28, 2014Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hiroshi Enomoto, Kenji Kawashima, Shinji Takaoka, Yasutaka Fujioka, Mamoru Matsuda, Koji Ohashi, Yukie Fujita, Shin-ichiro Hirai, Hiroaki Kurashima
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Patent number: 8816079Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: GrantFiled: April 27, 2011Date of Patent: August 26, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Publication number: 20140235616Abstract: The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.Type: ApplicationFiled: September 24, 2012Publication date: August 21, 2014Applicant: SANOFIInventors: Alexandre Benazet, Olivier Duclos, Nathalie Guillo, Gilbert Lassalle, Karim Macary, Valerie Vin
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Publication number: 20140235620Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.Type: ApplicationFiled: September 26, 2012Publication date: August 21, 2014Applicant: NOVARTIS AGInventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
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Publication number: 20140235619Abstract: This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity.Type: ApplicationFiled: November 26, 2013Publication date: August 21, 2014Applicant: NONO INC.Inventors: Xiujun Sun, Michael Tymianski, David Garman
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Publication number: 20140228351Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.Type: ApplicationFiled: March 14, 2014Publication date: August 14, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Publication number: 20140227281Abstract: The present disclosure provides methods for the prevention or treatment of herpes virus infections. The pharmaceutical composition contains a substance inhibiting the binding of glycoprotein B to a non-muscle myosin heavy chain IIA or IIB.Type: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: THE UNIVERSITY OF TOKYOInventors: Yasushi Kawaguchi, Jun Arii, Hisashi Arase
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Publication number: 20140227221Abstract: Erastin analogs are useful in treating various cancers, particularly multiple myeloma. Erastin analogs are also useful in treating cancers that are resistant to other anticancer agents.Type: ApplicationFiled: December 4, 2013Publication date: August 14, 2014Applicant: Prolexys Pharmaceuticals, Inc.Inventors: Paul B. Robbins, Sudhir R. Sahasrabudhe
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Publication number: 20140221315Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.Type: ApplicationFiled: April 3, 2014Publication date: August 7, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
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Publication number: 20140221354Abstract: The present invention provides novel imidazo[1,2-a]pyridine compounds that are useful in therapy of diseases and disorders. The novel compounds inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularization.Type: ApplicationFiled: March 31, 2011Publication date: August 7, 2014Applicant: EMBLEM Technology Transfer GmbHInventors: Marcel Mulbaier, Jorge Alonso, Douglas Thomson, Bernd Janssen, Arantxa Encinas Lopez, Bernd Wendt, Christoph Schultes
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Publication number: 20140221334Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore
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Patent number: 8796256Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: May 24, 2011Date of Patent: August 5, 2014Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Patent number: 8796263Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: GrantFiled: August 12, 2011Date of Patent: August 5, 2014Assignee: Janssen Pharmaceutica NVInventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Patent number: 8796259Abstract: N3-Heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: October 4, 2012Date of Patent: August 5, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Joane Litvak
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Publication number: 20140213580Abstract: Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.Type: ApplicationFiled: June 18, 2012Publication date: July 31, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
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Publication number: 20140213570Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: April 1, 2014Publication date: July 31, 2014Applicant: NOVARTIS AGInventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
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Publication number: 20140212509Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: May 24, 2013Publication date: July 31, 2014Applicant: ABBVIE INC.Inventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
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Patent number: 8791103Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: April 19, 2013Date of Patent: July 29, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
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Publication number: 20140206673Abstract: Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses for treating cancers are also provided.Type: ApplicationFiled: June 18, 2012Publication date: July 24, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
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Patent number: 8785628Abstract: A series of substituted [1,3,5]triazin-2-yl derivatives, 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: March 2, 2010Date of Patent: July 22, 2014Assignee: UCB Pharma, S.A.Inventors: Daniel Rees Allen, Roland Bürli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, David John Nash, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
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Patent number: 8785430Abstract: The invention relates to a compound (I) wherein R is a heterocyclyl radical; R1 and R2 are independently H or alkyl; R3 is H, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl; R4 and R5 are independently H or alkyl; q is a number selected from 0 and 1; and the salts, solvates, prodrugs or stereoisomers thereof having inhibitory activity for UBC13-UEV interactions and which can be used in the production of pharmaceutical compositions intended for antitumor therapy or the treatment and/or prophylaxis of diseases associated to metabolic pathways involving the UBC13 enzyme, metabolic pathways involving transcriptional factor NF-?B, or pathways involving PCNA or RAD6.Type: GrantFiled: July 23, 2012Date of Patent: July 22, 2014Assignee: Consejo Superior de Investigaciones CientificasInventors: Timothy Thomson Okatsu, Johanna Scheper Sigmund, Ángel Messeguer Peypooh, Gloria Sanclimens Pérez de Rozas, Isabel Masip Masip, Alejandra Moure Fernández, Domingo González Ruiz, Antonio Morreale de León, Maria Luz Ortiz Melguizo, Ma Carmen Fabrega Claveria
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20140194402Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: ApplicationFiled: May 3, 2012Publication date: July 10, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventor: Shin-San M. Su
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Publication number: 20140194349Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: AbbVie Inc.Inventors: David A. DeGoey, Charles A. Flentge, William J. Flosi, David J. Grampovnik, Dale J. Kempf, Larry L. Klein, Ming C. Yeung, John T. Randolph, Xiu C. Wang, Su Yu
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Patent number: 8772295Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: GrantFiled: January 22, 2013Date of Patent: July 8, 2014Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Patent number: 8772280Abstract: The present invention relates to substituted pyrrolyl-pyrimidines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: March 23, 2010Date of Patent: July 8, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Marina Caldarelli, Stefano Adele Nuvoloni, Francesca Quartieri
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Publication number: 20140187530Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: ApplicationFiled: November 27, 2013Publication date: July 3, 2014Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
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Publication number: 20140187540Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: ApplicationFiled: February 15, 2012Publication date: July 3, 2014Applicant: The Johns Hopkins UniversityInventors: Donald J. Zack, Cynthia Berlinicke, Laszlo Hackler, Zhiyong Yang, Joseph P. Steiner, Tomas Vojkovsky, Dana Ferraris, Barbara S. Slusher, James Inglese
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Publication number: 20140187539Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.Type: ApplicationFiled: March 4, 2014Publication date: July 3, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger WAGNER, Elke LANGKOPF, Frank HIMMELSBACH, Rolf GOEGGEL, Birgit JUNG
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Patent number: 8765731Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: GrantFiled: November 16, 2012Date of Patent: July 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, Jr., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
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Patent number: 8765739Abstract: Compounds of formula [I]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salts or solvates thereof.Type: GrantFiled: May 14, 2010Date of Patent: July 1, 2014Assignee: Japan Tobacco Inc.Inventors: Kazutaka Ikegashira, Taku Ikenogami, Naoki Ogawa, Tatsuya Matsumoto, Takahiro Oka, Takuya Matsuo, Takayuki Yamasaki
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Patent number: 8765732Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: GrantFiled: December 20, 2012Date of Patent: July 1, 2014Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
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Patent number: 8765939Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: August 16, 2012Date of Patent: July 1, 2014Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Nicholas J. Bennett, Thomas McInally, Tobias Mochel, Stephen Thom, Anna-Karin Tidén
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Publication number: 20140179689Abstract: The subject invention concerns materials and methods for treating diseases and disorders associated with expression of Rho associated kinases (ROCKs). Examples of diseases and disorders contemplated within the scope of the invention include, but are not limited to, oncological disorders, cardiovascular diseases, CNS disorders, and inflammatory disorders. In one embodiment, a method of the invention comprises administering a therapeutically effective amount of one or more compounds of the present invention, or a composition comprising the compounds, to a person or animal in need of treatment. The subject invention also concerns compounds that inhibit ROCKs, and compositions that comprise the inhibitor compounds of the invention. Compounds contemplated within the scope of the invention include, but are not limited to, those compounds shown in Table 5.Type: ApplicationFiled: March 30, 2012Publication date: June 26, 2014Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.Inventors: Nicholas J. Lawrence, Said M. Sebti, ROBERTA PIREDDU