The Second Ring Of The Bicyclo Ring System Is A Five-membered Hetero Ring Including Three Ring Nitrogens (e.g., Triazolo[1,5-a]pyrimidine, Etc.) Patents (Class 514/259.31)
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Patent number: 12004868Abstract: Compositions and methods are provided for preventing one or more cardiac channelopathies or conditions resulting from irregularities or alterations in cardiac patterns, or both, in a human or animal subject comprising: one or more pharmacologically active agents that causes at least one of IKr channel inhibition or QT prolongation by inhibiting the activity of an ether-a-go-go-related gene (hERG); and one or more liposomes, wherein the liposomes are empty liposomes and administered prior to, concomitantly, or after administration of the pharmacologically active agent.Type: GrantFiled: June 5, 2019Date of Patent: June 11, 2024Assignee: Signpath Pharma Inc.Inventors: Lawrence Helson, George M. Shopp, Annie Bouchard
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Patent number: 11987583Abstract: A compound and/or a pharmaceutically acceptable salt thereof has the following formula A: These compounds can be PIKfyve kinase inhibitors.Type: GrantFiled: June 30, 2021Date of Patent: May 21, 2024Assignee: PIKSci INC.Inventors: Sergei Romanov, Robert Greenhouse, Nikolai Sepetov
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Patent number: 11950592Abstract: A method for remarkably enhancing plant disease controlling effects, and a method for controlling plant diseases are provided. A method for enhancing plant disease controlling effects of an aryl phenyl ketone fungicide includes using an aryl phenyl ketone fungicide as a component (a) in combination with at least one component (b) selected from the group consisting of a nonionic surfactant, an anionic surfactant, a cationic surfactant, a vegetable oil, a paraffin, a resin and a terpene.Type: GrantFiled: April 13, 2017Date of Patent: April 9, 2024Assignee: ISHIHARA SANGYO KAISHA, LTD.Inventors: Munekazu Ogawa, Akihiro Nishimura, Shuko Nishimi
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Patent number: 11311538Abstract: In various aspects and embodiments the invention provides a method of treating or preventing a cancer in a mammalian subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of at least one compound selected from the group consisting of a DNA repair inhibitor, a DNA strand break repair inhibitor, and a homologous recombination (HR) repair inhibitor, wherein cells in the cancer comprise a fumarate hydratase (FH) and/or succinate dehydrogenase (SDH) mutation.Type: GrantFiled: July 12, 2019Date of Patent: April 26, 2022Assignee: YALE UNIVERSITYInventors: Ranjit Bindra, Peter Glazer, Parker Sulkowski, Brian Shuch
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Patent number: 11117899Abstract: Provided are a compound represented by formula (I), an isomer or a pharmaceutically acceptable salt thereof, and an application of the same in preparing a drug for treating a disease related to A2A receptor. The R1, R2, R3, ring A, ring B, n, and m are as defined in the specification.Type: GrantFiled: April 8, 2018Date of Patent: September 14, 2021Assignee: MEDSHINE DISCOVERY INC.Inventors: Kevin X Chen, Yanxin Yu, Xinde Chen, Li Zhang, Zhaoguo Chen, Cheng Xie, Xiaofei Wang, Linghui Wu, Guoping Hu, Jian Li, Shuhui Chen
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Patent number: 11066411Abstract: Provided are a compound represented by formula (I), an isomer or a pharmaceutically acceptable salt thereof, and an application of the same in preparing a drug for treating a disease related to A2A receptor. The R1, R2, R3, ring A, ring B, n, and m are as defined in the specification.Type: GrantFiled: April 8, 2018Date of Patent: July 20, 2021Assignee: MEDSHINE DISCOVERY INC.Inventors: Kevin X Chen, Yanxin Yu, Xinde Chen, Li Zhang, Zhaoguo Chen, Cheng Xie, Xiaofei Wang, Linghui Wu, Guoping Hu, Jian Li, Shuhui Chen
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Patent number: 10947242Abstract: The present invention relates to novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivatives as inhibitors of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, such as neurological and psychiatric disorders.Type: GrantFiled: October 31, 2017Date of Patent: March 16, 2021Assignee: Janssen Pharmaceutica, NVInventors: Yves Emiel Maria Van Roosbroeck, Frans Alfons Maria Van den Keybus, Gary John Tresadern, Petrus Jacobus Johannes Antonius Buijnsters, Adriana Ingrid Velter, Edgar Jacoby, Gregor James Macdonald, Henricus Jacobus Maria Gijsen, Abdellah Ahnaou, Wilhelmus Helena Ignatius Maria Drinkenburg
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Patent number: 9695167Abstract: The present invention is directed to [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.Type: GrantFiled: July 9, 2015Date of Patent: July 4, 2017Assignee: Incyte CorporationInventors: Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
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Patent number: 9687488Abstract: A pharmaceutical composition is provided which includes a pharmaceutically acceptable excipient and a pharmaceutically and physically acceptable amount of a compound selected from the group consisting of Chemical Formulas I-IV as described herein, or a pharmaceutically acceptable salt thereof. Also provided are methods of increasing a level of a defined neurotrophic peptide in an organism or tissue comprising the administration of a pharmaceutically and physically acceptable amount of one or more of the compositions described above, and a method for treating a neurodegenerative disease in a subject in need thereof, the method comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 1.Type: GrantFiled: May 3, 2013Date of Patent: June 27, 2017Assignee: ST. LOUIS COLLEGE OF PHARMACYInventor: John M. Beale
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Patent number: 9533990Abstract: Pharmaceutical compositions of the invention comprise triazolopyrimidines useful for the treatment of hepatitis virus in a patient.Type: GrantFiled: November 21, 2014Date of Patent: January 3, 2017Assignees: Drexel University, Baruch S. Blumberg Institute, Arbutus Biopharma, Inc.Inventors: Xiaodong Xu, Andrea Cuconati, Timothy M. Block, Tong Xiao
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Patent number: 9359362Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: GrantFiled: October 7, 2013Date of Patent: June 7, 2016Assignee: Bayer Intellectual Property GmbhInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
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Patent number: 9096589Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: December 15, 2010Date of Patent: August 4, 2015Assignee: H. Lundbeck A/SInventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
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Publication number: 20150148332Abstract: The present invention provides compounds of formula (Ia) and (Ib) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: ApplicationFiled: November 25, 2014Publication date: May 28, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Alexander Flohr, Katrin Groebke Zbinden, Bernd Kuhn, Christian Lerner, Markus Rudolph, Herve Schaffhauser
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Patent number: 9034882Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: March 1, 2013Date of Patent: May 19, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
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Publication number: 20150133429Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: ApplicationFiled: January 14, 2015Publication date: May 14, 2015Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Patent number: 9029377Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.Type: GrantFiled: June 28, 2010Date of Patent: May 12, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
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Patent number: 9012362Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: August 19, 2014Date of Patent: April 21, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Publication number: 20150087659Abstract: Pharmaceutical compositions of the invention comprise triazolopyrimidines useful for the treatment of hepatitis virus in a patient.Type: ApplicationFiled: November 21, 2014Publication date: March 26, 2015Inventors: XIAODONG XU, ANDREA CUCONATI, TIMOTHY M. BLOCK, TONG XIAO
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Patent number: 8980878Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.Type: GrantFiled: April 17, 2013Date of Patent: March 17, 2015Assignee: Gilead Sciences, Inc.Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
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Patent number: 8969360Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables R1, R2, R3, and R4 are as defined herein.Type: GrantFiled: December 6, 2013Date of Patent: March 3, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Chris Davis, Steven Durrant, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Michael O'Donnell, Francoise Pierard, Joanne Pinder, Pierre-Henri Storck, Heather Twin
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Patent number: 8969246Abstract: Pesticidal mixtures comprising, as active components, 1) an anthranilamid compound of the formula I wherein the variables are defined according to the description, and 2) at least one fungicidal compound II selected from the following groups: strobilurins, carboxamides, heterocylic compounds and other active compounds according to the description, in a synergistically effective amount, methods for controlling pests, and harmful fungi, methods of protecting plants from attack or infestation by insects, acarids or nematodes, methods for treating, controlling, preventing or protecting an animal against infestation or infection by parasites, compositions containing these mixtures, and methods for their preparation.Type: GrantFiled: March 13, 2013Date of Patent: March 3, 2015Assignee: BASF SEInventors: Jürgen Langewald, Reinhard Stierl
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Patent number: 8957064Abstract: Compounds of formula (I) or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer, wherein ring B and the pyrimidine to which it is fused, R4, R5, R6, R7, m and n have the meanings as given in the description and the claims, which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: GrantFiled: February 2, 2010Date of Patent: February 17, 2015Assignee: Bayer Intellectual Property GmbHInventors: Matthias Vennemann, Thomas Bär, Thomas Maier, Swen Hölder, Gerrit Beneke, Florian Dehmel, Armin Zülch, Andreas Strub, Stuart Ince, Hartmut Rehwinkel, Ningshu Liu, Ulf Bömer, Barbara Beckers
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Patent number: 8927525Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.Type: GrantFiled: October 24, 2012Date of Patent: January 6, 2015Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
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Publication number: 20150005275Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: May 6, 2014Publication date: January 1, 2015Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
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Patent number: 8921381Abstract: Pharmaceutical compositions of the invention comprise triazolopyrimidines useful for the treatment of hepatitis virus in a patient.Type: GrantFiled: October 4, 2011Date of Patent: December 30, 2014Assignees: Baruch S. Blumberg Institute, Philadelphia Health & Education Corporation, Enantigen Therapeutics, Inc.Inventors: Xiaodong Xu, Andrea Cuconati, Timothy M. Block, Tong Xiao
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Publication number: 20140364415Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.Type: ApplicationFiled: August 26, 2014Publication date: December 11, 2014Applicant: PFIZER LIMITEDInventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
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Publication number: 20140357597Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: ApplicationFiled: August 19, 2014Publication date: December 4, 2014Inventors: Thomas SEITZ, Ulrike Wachendorff-Neumann, Peter Dahmen
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Publication number: 20140357650Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.Type: ApplicationFiled: January 17, 2013Publication date: December 4, 2014Applicant: Fox Chase Cancer CenterInventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
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Publication number: 20140350002Abstract: The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: June 14, 2012Publication date: November 27, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Hannah D. Fiji, Michael J. Kelly, III, Jeffrey C. Kern, Mark E. Layton, Joseph E. Pero, Alexander J. Reif, Michael A. Rossi
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Publication number: 20140322165Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: July 8, 2014Publication date: October 30, 2014Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Publication number: 20140288062Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
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Patent number: 8815875Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: November 10, 2009Date of Patent: August 26, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Abdelghani Abe Achab, Peter Orth, Johannes H. Voigt, Kyle Ann Soucy
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Patent number: 8809330Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.Type: GrantFiled: November 1, 2013Date of Patent: August 19, 2014Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
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Publication number: 20140221298Abstract: The present invention provides an agricultural and horticultural fungicidal composition including a compound A which is at least one selected from a nitrogen-containing heterocyclic compound having a specific structure including a compound represented by the formula (1), and a salt thereof, and a compound B which is at least one selected from the group of specific pesticidally active compounds: in the formula (1), X each independently represents a halogeno group or a C1 to 6 alkyl group; n represents the number of X(s) and is an integer of 0 to 6; and X? represents a halogeno group; and R1, R2 and R3 each independently represent a C1 to 6 alkyl group or a hydroxyl group.Type: ApplicationFiled: September 24, 2012Publication date: August 7, 2014Inventor: Raito Kuwahara
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Patent number: 8796285Abstract: The present invention provides new pyrazol-[1,5-a]-pyrimidone derivates and pharmaceutical compositions comprising said compounds and one or more pharmaceutically acceptable carriers or diluents. The uses of the compounds for the manufacture of potassium channel openers, anti-epilepsy medicaments, anti-anxiety medicaments and analgesic medicaments are also provided in the present invention.Type: GrantFiled: June 3, 2010Date of Patent: August 5, 2014Assignees: Hebei Medical University, Peking UniversityInventors: Hailin Zhang, Jinlong Qi, Diqun Zhang, Kewei Wang, Fan Zhang, Yan Fu, Yi Mi, Wen Xu, Xiaona Du, Yibing Wu, Qingzhong Jia, Shuangge Yang
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Patent number: 8785438Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.Type: GrantFiled: March 13, 2013Date of Patent: July 22, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
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Publication number: 20140200136Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I): wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.Type: ApplicationFiled: August 31, 2012Publication date: July 17, 2014Applicant: BASF SEInventors: Florian Kaiser, Steffen Gross, Egon Haden, Arun Narine
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Publication number: 20140194388Abstract: A pharmaceutical composition comprising a CHK inhibitor, and an Hsp90 inhibitor according to the following formulae or tautomers, or pharmaceutically acceptable salts thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical compositions described herein.Type: ApplicationFiled: May 25, 2012Publication date: July 10, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: David Proia, Suqin He
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Patent number: 8772276Abstract: The present invention is directed to alkyne benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: GrantFiled: April 30, 2012Date of Patent: July 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Jason W. Skudlarek
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Patent number: 8771665Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: GrantFiled: December 16, 2011Date of Patent: July 8, 2014Assignee: Cocrystal Discovery, Inc.Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Patent number: 8765770Abstract: This invention relates to novel substituted [1,2,4]triazolo[1,5-a]pyrimidines and their use as modulators of potassium channels. In other aspects the invention relates to the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: March 30, 2010Date of Patent: July 1, 2014Assignee: Ataxion, Inc.Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dotre Strøbæk, Palle Christophersen
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Patent number: 8759357Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: October 1, 2010Date of Patent: June 24, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Gerald W. Shipps, Jr., Clifford C. Cheng, Xioahua Huang, Abdelghani Achab, Peter Orth, Johannes H. Voigt
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Publication number: 20140171440Abstract: The present invention is directed to methods of enhancing liver repair after injury, resection or transplantation using antagonists of the bone morphogenetic protein (BMP) signaling pathway in the liver.Type: ApplicationFiled: September 3, 2013Publication date: June 19, 2014Applicant: Beth Israel Deaconess Medical Center, Inc.Inventors: Seth J. Karp, Martin Dib, Nhue Do
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Publication number: 20140155263Abstract: Fungicidal mixtures comprising, as active components, 1) azolopyrimidinylamines of the formula I, in which the substituents are as defined in the description and 2) at least one active compound II selected from the following groups: azoles, strobilurins, carboxamides, heterocylic compounds, carbamates and other active compounds selected from the group consisting of guanidines, antibiotics, sulfur-containing heterocyclyl compounds, organophosphorus compounds, organochlorine compounds, inorganic active compounds, growth retardants and cyflufenamid, cymoxanil, dimethirimol, ethirimol, furalaxyl, metrafenone and spiroxamine; in a synergistically effective amount. Methods for controlling harmful fungi using mixtures of the compound I with active compounds II and the use of the compound I with active compounds II for preparing such mixtures, and also compositions comprising these mixtures.Type: ApplicationFiled: February 10, 2014Publication date: June 5, 2014Applicant: BASF SEInventors: Christine Beck, Matthias NIEDENBRÜCK, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Udo HÜNGER
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Publication number: 20140148338Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a thiazolylisoxazoline of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: ApplicationFiled: June 4, 2012Publication date: May 29, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Sebastian Hoffmann, Pierre Wasnaire, Ulrike Wachendorff-Neumann
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Publication number: 20140142122Abstract: Disclosed herein are erythropoietin-mimetic compounds of Formula I, which modulate the survival, function, or differentiation of, for example, kidney cells, neurons, erythroid cells, or other erythropoietin-responsive cells. The present invention also relates to compounds and methods that preferentially modulate cells expressing the tissue-protective erythropoietin receptor. The compounds of the invention are useful in preventing and treating diseases, such as anemia, organ injury, and diseases of the central nervous system, and as an adjunct to cellular treatments, such as stem cell therapies.Type: ApplicationFiled: November 20, 2013Publication date: May 22, 2014Applicant: STATegics, Inc.Inventors: Juha PUNNONEN, Jeffrey R. SPENCER, Timothy J. CHURCH, Connie S. TETTENBORN, Karen LARIOSA-WILLINGHAM, Dimitri LEONOUDAKIS, James L. MILLER
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Patent number: 8722689Abstract: A synergistic antimicrobial composition containing flumetsulam or diclosulam; and diiodomethyl-p-tolylsulfone.Type: GrantFiled: November 4, 2011Date of Patent: May 13, 2014Assignee: Dow Global Technologies LLCInventor: Emerentiana Sianawati
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Publication number: 20140128411Abstract: The present invention provides a fungicidal composition useful as an agricultural and horticultural fungicide having remarkably improved controlling effects against plant diseases, and a method for controlling plant diseases using the composition. A fungicidal composition comprising, as active ingredients, (a) 3-(2,3,4-trimethoxy-6-methylbenzoyl)-5-chloro-2-methoxy-4-methyl-pyridine (pyriofenone) or its salt and (b) at least one fungicide selected from the group consisting of bixafen, fluxapyroxad, penflufen, isopyrazam, fluopyram, ametoctradin, fenpyrazamine and sedaxane, and a method for controlling plant diseases, which comprises applying the fungicidal composition to plants.Type: ApplicationFiled: June 15, 2012Publication date: May 8, 2014Applicant: Ishihara Sangyo Kaisha, Ltd.Inventors: Munekazu Ogawa, Yuzuka Kawai
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Publication number: 20140127322Abstract: Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed. Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: MATTHEW RICHARD OBERHOLZER, ROBERT JAMES PASTERIS
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Publication number: 20140121103Abstract: The present invention relates to synergistic mixtures comprising at least one compound I and at least one active compound II as defined herein and to the use of these mixtures for combating phytopathogenic fungi, and to seeds coated with at least one such mixture. The invention also relates methods for combating harmful fungi using such mixtures.Type: ApplicationFiled: June 15, 2012Publication date: May 1, 2014Applicant: BASF SEInventors: Nadege Boudet, Wassilios Grammenos, Jochen Dietz, Egon Haden, Richard Riggs, Bernd Müller, Jan Klaas Lohmann, Jurith Montag, Ian Robert Craig