The Additional Ring Is A Six-membered Hetero Ring Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/318)
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Patent number: 8946236Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.Type: GrantFiled: August 7, 2013Date of Patent: February 3, 2015Assignee: Bayer Cropscience AGInventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
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Publication number: 20150031724Abstract: An aqueous liquid preparation containing (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, which is stabilized with a water-soluble metal chloride, is provided.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventor: Masayo HIGASHIYAMA
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Publication number: 20150031541Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: February 27, 2013Publication date: January 29, 2015Applicant: Syngenta Participations AGInventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cedarbaum, Jayant Umarye, Ravindra Sonawane
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Publication number: 20150031681Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).Type: ApplicationFiled: April 9, 2013Publication date: January 29, 2015Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
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Patent number: 8940774Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.Type: GrantFiled: November 26, 2013Date of Patent: January 27, 2015Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Patent number: 8940768Abstract: Disclosed are novel triazole derivatives. Exhibiting excellent antifungal activity and in vivo safety, they are useful for the treatment or prevention of fungal infections caused by a wide spectrum of fungi.Type: GrantFiled: February 11, 2011Date of Patent: January 27, 2015Assignee: Daewoong Pharmaceutical Co., Ltd.Inventors: Joon Seok Park, Kyung A Yu, Yun Soo Yoon, Mi Ryeong Han, Ji Duck Kim
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Publication number: 20150025056Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Applicant: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
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Publication number: 20150025054Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.Type: ApplicationFiled: October 22, 2012Publication date: January 22, 2015Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
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Publication number: 20150025111Abstract: The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Inventors: Rina Yamin, Dalia Megiddo
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Patent number: 8937181Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: April 13, 2007Date of Patent: January 20, 2015Assignee: Purdue Pharma L.P.Inventors: Akira Matsumura, Hidenori Mikamiyama, Bin Shao, Naoki Tsuno, Jiangchao Yao
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Publication number: 20150018321Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: September 25, 2014Publication date: January 15, 2015Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
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Publication number: 20150018334Abstract: The present invention relates to aryl pyrazoles, and pharmaceutically acceptable salts thereof. The aryl pyrazoles of the present invention are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the aryl pyrazoles of the present invention, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, John BROADWATER, Steven Richard BRUNETTE, Thomas Martin KIRRANE, JR., Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Qiang ZHANG
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Publication number: 20150018344Abstract: Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R7, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: January 15, 2015Inventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
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Publication number: 20150018341Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 15, 2015Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
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Publication number: 20150018366Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: September 26, 2014Publication date: January 15, 2015Inventor: Laykea TAFESSE
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Patent number: 8933098Abstract: The present invention provides a compound of the Formula II: wherein A is: R1 is CH3, CF3, or F; R2 is H, CH3, or F; R3 is CH3, OCH3, OH, F; R4 is OH or CH2OH; and X is CH or N; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 4, 2013Date of Patent: January 13, 2015Assignee: Eli Lilly and CompanyInventors: Maria-Jesus Blanco-Pillado, Tatiana Natali Vetman
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Patent number: 8933099Abstract: The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.Type: GrantFiled: February 19, 2014Date of Patent: January 13, 2015Assignee: Eisai R&D Management Co., Ltd.Inventors: Setsuo Funasaka, Toshimi Okada, Keigo Tanaka, Satoshi Nagao, Isao Ohashi, Yoshinobu Yamane, Yusuke Nakatani, Yuki Karoji
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Publication number: 20150011526Abstract: The present invention relates to 2-oxo-piperidinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: October 10, 2012Publication date: January 8, 2015Inventors: Ali Ates, Florian Montel, Anne Valade, Olivier Lorthioir
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Publication number: 20150011527Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.Type: ApplicationFiled: June 11, 2014Publication date: January 8, 2015Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
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Publication number: 20150011557Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.Type: ApplicationFiled: September 7, 2012Publication date: January 8, 2015Applicant: Merck Patent GmbHInventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
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Publication number: 20150011541Abstract: The present invention relates to compounds having a pipecolate sulfonamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate sulfonamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 8, 2015Inventors: Ranganath Gopalakrishnan, Felix Hausch
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Publication number: 20150011539Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Inventor: Vlad Edward GREGOR
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Publication number: 20150011546Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.Type: ApplicationFiled: February 11, 2013Publication date: January 8, 2015Inventors: Brian K. Albrecht, James Edmund Audia, Andrew S. Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
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Patent number: 8927726Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, (Het)Ar1, (Het)Ar2 and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: July 22, 2013Date of Patent: January 6, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Neil J. Ashweek, Nicole Harriott
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Publication number: 20150005328Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.Type: ApplicationFiled: July 2, 2014Publication date: January 1, 2015Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
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Publication number: 20150005296Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: September 18, 2014Publication date: January 1, 2015Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
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Publication number: 20150005288Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: January 22, 2013Publication date: January 1, 2015Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbHInventors: Frank Süssmeier, Mario Lobell, Sylvia Grünewald, Michael Härter, Bernd Buchmann, Joachim Telser, Hannah Jörissen, Melanie Heroult, Antje Kahnert, Klemens Lustig, Niels Lindner
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Publication number: 20150004181Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.Type: ApplicationFiled: June 27, 2014Publication date: January 1, 2015Inventors: Isabelle BERREBI-BERTRAND, Xavier BILLOT, Thierry CALMELS, Marc CAPET, Denis DANVY, Stéphane KRIEF, Olivier LABEEUW, Jeanne-Marie LECOMTE, Nicolas LEVOIN, Xavier LIGNEAU, Philippe ROBERT, Jean-Charles SCHWARTZ
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Publication number: 20150005277Abstract: The invention is compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.Type: ApplicationFiled: June 21, 2014Publication date: January 1, 2015Inventors: Zhiwei Wang, Yunhang Guo
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Publication number: 20150005303Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: September 18, 2014Publication date: January 1, 2015Inventors: George W. MULLER, Roger Shen-Chu CHEN, Alexander L. RUCHELMAN
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Patent number: 8921563Abstract: Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.Type: GrantFiled: April 8, 2011Date of Patent: December 30, 2014Assignee: Institue of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., ChinaInventors: Yunfeng Li, Rifang Yang, Youzhi Zhang, Yongzhen Li, Zengliang Jin, Peng Li, Li Yuan, Liuhong Yun, Nan Zhao, Cheng Zhang, Xiaodan Xu, Rusheng Zhao, Hongxia Chen, Rui Xue, Juanjuan Qin, Zhenzhen Wang, Jiazhi Yao
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Patent number: 8921559Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: November 30, 2011Date of Patent: December 30, 2014Assignee: Janssen Pharmaceutica NVInventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
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Patent number: 8921373Abstract: The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: June 22, 2011Date of Patent: December 30, 2014Assignee: Shionogi & Co., Ltd.Inventor: Noriyuki Kurose
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Publication number: 20140378429Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) (The chemical formulas should be inserted here) in which the variables are as described herein.Type: ApplicationFiled: January 31, 2013Publication date: December 25, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
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Publication number: 20140378458Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is A1 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.Type: ApplicationFiled: June 2, 2014Publication date: December 25, 2014Applicant: BASF SEInventors: Thomas SCHMIDT, Michael PUHL, Joachim DICKHAUT, Henricus Maria Martinus BASTIAANS, Michael RACK, Deborah L. CULBERTSON, Douglas D. ANSPAUGH, Franz-Josef BRAUN, Toni BUCCI, Henry Van Tuyl COTTER, David G. KUHN, Hassan OLOUMI-SADEGHI
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Publication number: 20140378454Abstract: The present invention relates to the field of methods for providing components of pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to methods for providing stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions.Type: ApplicationFiled: January 11, 2013Publication date: December 25, 2014Applicant: XSPRAY MICROPARTICLES ABInventors: Magnus Brisander, Mustafa Demirbüker, Gérald Jesson, Martin Malmsten, Helene Dérand
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Publication number: 20140371176Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.Type: ApplicationFiled: September 3, 2014Publication date: December 18, 2014Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
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Publication number: 20140371197Abstract: 4-(Azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Inventors: Jean-Guy BOITEAU, Karine BOUQUET, Sandrine Talano, Corinne MILLOIS BARBUIS
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Publication number: 20140371269Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof, where the variables for R1, R2, and R3 are as described herein; methods of treating a condition such as hypertriglyceridemia; and processes for preparing the compounds.Type: ApplicationFiled: January 16, 2013Publication date: December 18, 2014Applicant: Eli Lilly and CompanyInventors: Maria Carmen Fernandez, Maria Rosario Gonzalez-Garcia, Bin Liu, Lance Allen Pfeifer
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Publication number: 20140371195Abstract: The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.Type: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Marc Labelle, Thomas Boesen, Mukund Mehrotra, Qasim Khan, Farman Ullah
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Publication number: 20140371268Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases, gastrointestinal diseases and respiratory diseases.Type: ApplicationFiled: August 31, 2012Publication date: December 18, 2014Applicant: AMAKEM NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
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Publication number: 20140371239Abstract: The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin.Type: ApplicationFiled: June 11, 2014Publication date: December 18, 2014Inventors: Jolanta Grembecka, Tomasz Cierpicki, Sunil Kumar Upadhyay, Shaun R. Stauffer, Rocco D. Gogliotti, Timothy J. Senter
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Publication number: 20140371238Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:Type: ApplicationFiled: March 13, 2014Publication date: December 18, 2014Applicant: FLATLEY DISCOVERY LABInventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
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Patent number: 8912184Abstract: The invention relates to methods of treating diseases, particularly cancers, that respond favorably to the inhibition of Nicotinamide phosphoribosyltransferase (Nampt); it also relates to therapeutic methods that utilize Nampt inhibitors in combination with NAD biosynthesis precursors to intentionally kill cancer cells while limiting or minimizing toxicity to normal host cells; and it relates to methods of identifying cancers that will be most responsive to treatment with Nampt inhibitors, particularly when administered in combination with nicotinic acid.Type: GrantFiled: September 16, 2011Date of Patent: December 16, 2014Assignee: Alzheimer's Institute of America, Inc.Inventors: Tracey C. Fleischer, Daniel M. Cimbora, Jeffrey S. Flick, Andrew D. Gassman, Vijay R. Baichwal, Damon I. Papac
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Patent number: 8912218Abstract: The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.Type: GrantFiled: July 21, 2009Date of Patent: December 16, 2014Assignee: SanofiInventors: Ahmed Abouabdellah, Jochen Görlitzer, Peter Hamley, Antoine Ravet
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Publication number: 20140364419Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Robert Shalwitz, Joseph H. Gardner
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Publication number: 20140364432Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: February 12, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
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Publication number: 20140364433Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: August 14, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
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Patent number: 8906938Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.Type: GrantFiled: May 14, 2013Date of Patent: December 9, 2014Assignee: ChemoCentryx, Inc.Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
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Patent number: RE45364Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.Type: GrantFiled: January 21, 2014Date of Patent: February 3, 2015Assignee: Nippon Soda Co., Ltd.Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa