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)
  • Patent number: 11311538
    Abstract: 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: Grant
    Filed: July 12, 2019
    Date of Patent: April 26, 2022
    Assignee: YALE UNIVERSITY
    Inventors: Ranjit Bindra, Peter Glazer, Parker Sulkowski, Brian Shuch
  • Patent number: 11117899
    Abstract: 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: Grant
    Filed: April 8, 2018
    Date of Patent: September 14, 2021
    Assignee: 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
  • Patent number: 11066411
    Abstract: 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: Grant
    Filed: April 8, 2018
    Date of Patent: July 20, 2021
    Assignee: 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
  • Patent number: 10947242
    Abstract: 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: Grant
    Filed: October 31, 2017
    Date of Patent: March 16, 2021
    Assignee: Janssen Pharmaceutica, NV
    Inventors: 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
  • Patent number: 9695167
    Abstract: 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: Grant
    Filed: July 9, 2015
    Date of Patent: July 4, 2017
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
  • Patent number: 9687488
    Abstract: 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: Grant
    Filed: May 3, 2013
    Date of Patent: June 27, 2017
    Assignee: ST. LOUIS COLLEGE OF PHARMACY
    Inventor: John M. Beale
  • Patent number: 9533990
    Abstract: Pharmaceutical compositions of the invention comprise triazolopyrimidines useful for the treatment of hepatitis virus in a patient.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: January 3, 2017
    Assignees: Drexel University, Baruch S. Blumberg Institute, Arbutus Biopharma, Inc.
    Inventors: Xiaodong Xu, Andrea Cuconati, Timothy M. Block, Tong Xiao
  • Patent number: 9359362
    Abstract: 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: Grant
    Filed: October 7, 2013
    Date of Patent: June 7, 2016
    Assignee: Bayer Intellectual Property Gmbh
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
  • Patent number: 9096589
    Abstract: 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: Grant
    Filed: December 15, 2010
    Date of Patent: August 4, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
  • Publication number: 20150148332
    Abstract: 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: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Bernd Kuhn, Christian Lerner, Markus Rudolph, Herve Schaffhauser
  • Patent number: 9034882
    Abstract: 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: Grant
    Filed: March 1, 2013
    Date of Patent: May 19, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
  • Publication number: 20150133429
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 14, 2015
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Patent number: 9029377
    Abstract: 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: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Patent number: 9012362
    Abstract: 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: Grant
    Filed: August 19, 2014
    Date of Patent: April 21, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
  • Publication number: 20150087659
    Abstract: Pharmaceutical compositions of the invention comprise triazolopyrimidines useful for the treatment of hepatitis virus in a patient.
    Type: Application
    Filed: November 21, 2014
    Publication date: March 26, 2015
    Inventors: XIAODONG XU, ANDREA CUCONATI, TIMOTHY M. BLOCK, TONG XIAO
  • Patent number: 8980878
    Abstract: 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: Grant
    Filed: April 17, 2013
    Date of Patent: March 17, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
  • Patent number: 8969360
    Abstract: 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: Grant
    Filed: December 6, 2013
    Date of Patent: March 3, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Patent number: 8969246
    Abstract: 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: Grant
    Filed: March 13, 2013
    Date of Patent: March 3, 2015
    Assignee: BASF SE
    Inventors: Jürgen Langewald, Reinhard Stierl
  • Patent number: 8957064
    Abstract: 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: Grant
    Filed: February 2, 2010
    Date of Patent: February 17, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: 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
  • Patent number: 8927525
    Abstract: 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: Grant
    Filed: October 24, 2012
    Date of Patent: January 6, 2015
    Assignee: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
  • Publication number: 20150005275
    Abstract: 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: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: 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
  • Patent number: 8921381
    Abstract: Pharmaceutical compositions of the invention comprise triazolopyrimidines useful for the treatment of hepatitis virus in a patient.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: December 30, 2014
    Assignees: Baruch S. Blumberg Institute, Philadelphia Health & Education Corporation, Enantigen Therapeutics, Inc.
    Inventors: Xiaodong Xu, Andrea Cuconati, Timothy M. Block, Tong Xiao
  • Publication number: 20140364415
    Abstract: 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: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER LIMITED
    Inventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
  • Publication number: 20140357650
    Abstract: 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: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: Fox Chase Cancer Center
    Inventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
  • Publication number: 20140357597
    Abstract: 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: Application
    Filed: August 19, 2014
    Publication date: December 4, 2014
    Inventors: Thomas SEITZ, Ulrike Wachendorff-Neumann, Peter Dahmen
  • Publication number: 20140350002
    Abstract: 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: Application
    Filed: June 14, 2012
    Publication date: November 27, 2014
    Applicant: 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
  • Publication number: 20140322165
    Abstract: 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: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Publication number: 20140288062
    Abstract: 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: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
  • Patent number: 8815875
    Abstract: 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: Grant
    Filed: November 10, 2009
    Date of Patent: August 26, 2014
    Assignee: 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
  • Patent number: 8809330
    Abstract: 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: Grant
    Filed: November 1, 2013
    Date of Patent: August 19, 2014
    Assignee: 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
  • Publication number: 20140221298
    Abstract: 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: Application
    Filed: September 24, 2012
    Publication date: August 7, 2014
    Inventor: Raito Kuwahara
  • Patent number: 8796285
    Abstract: 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: Grant
    Filed: June 3, 2010
    Date of Patent: August 5, 2014
    Assignees: Hebei Medical University, Peking University
    Inventors: Hailin Zhang, Jinlong Qi, Diqun Zhang, Kewei Wang, Fan Zhang, Yan Fu, Yi Mi, Wen Xu, Xiaona Du, Yibing Wu, Qingzhong Jia, Shuangge Yang
  • Patent number: 8785438
    Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: July 22, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
  • Publication number: 20140200136
    Abstract: 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: Application
    Filed: August 31, 2012
    Publication date: July 17, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Steffen Gross, Egon Haden, Arun Narine
  • Publication number: 20140194388
    Abstract: 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: Application
    Filed: May 25, 2012
    Publication date: July 10, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: David Proia, Suqin He
  • Patent number: 8771665
    Abstract: 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: Grant
    Filed: December 16, 2011
    Date of Patent: July 8, 2014
    Assignee: Cocrystal Discovery, Inc.
    Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Patent number: 8772276
    Abstract: 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: Grant
    Filed: April 30, 2012
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 8765770
    Abstract: 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: Grant
    Filed: March 30, 2010
    Date of Patent: July 1, 2014
    Assignee: Ataxion, Inc.
    Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dotre Strøbæk, Palle Christophersen
  • Patent number: 8759357
    Abstract: 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: Grant
    Filed: October 1, 2010
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gerald W. Shipps, Jr., Clifford C. Cheng, Xioahua Huang, Abdelghani Achab, Peter Orth, Johannes H. Voigt
  • Publication number: 20140171440
    Abstract: 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: Application
    Filed: September 3, 2013
    Publication date: June 19, 2014
    Applicant: Beth Israel Deaconess Medical Center, Inc.
    Inventors: Seth J. Karp, Martin Dib, Nhue Do
  • Publication number: 20140155263
    Abstract: 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: Application
    Filed: February 10, 2014
    Publication date: June 5, 2014
    Applicant: BASF SE
    Inventors: Christine Beck, Matthias NIEDENBRÜCK, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Udo HÜNGER
  • Publication number: 20140148338
    Abstract: 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: Application
    Filed: June 4, 2012
    Publication date: May 29, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Sebastian Hoffmann, Pierre Wasnaire, Ulrike Wachendorff-Neumann
  • Publication number: 20140142122
    Abstract: 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: Application
    Filed: November 20, 2013
    Publication date: May 22, 2014
    Applicant: STATegics, Inc.
    Inventors: Juha PUNNONEN, Jeffrey R. SPENCER, Timothy J. CHURCH, Connie S. TETTENBORN, Karen LARIOSA-WILLINGHAM, Dimitri LEONOUDAKIS, James L. MILLER
  • Patent number: 8722689
    Abstract: A synergistic antimicrobial composition containing flumetsulam or diclosulam; and diiodomethyl-p-tolylsulfone.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: May 13, 2014
    Assignee: Dow Global Technologies LLC
    Inventor: Emerentiana Sianawati
  • Publication number: 20140127322
    Abstract: 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: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: MATTHEW RICHARD OBERHOLZER, ROBERT JAMES PASTERIS
  • Publication number: 20140128411
    Abstract: 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: Application
    Filed: June 15, 2012
    Publication date: May 8, 2014
    Applicant: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Munekazu Ogawa, Yuzuka Kawai
  • Publication number: 20140121103
    Abstract: 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: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: BASF SE
    Inventors: Nadege Boudet, Wassilios Grammenos, Jochen Dietz, Egon Haden, Richard Riggs, Bernd Müller, Jan Klaas Lohmann, Jurith Montag, Ian Robert Craig
  • Publication number: 20140107099
    Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: Genentech, Inc.
    Inventors: Jeffrey Blaney, Paul A. Gibbons, Emily Hanan, Joseph P. Lyssikatos, Steven R. Magnuson, Richard Pastor, Thomas E. Rawson, Aihe Zhou, Bing-Yan Zhu
  • Publication number: 20140099279
    Abstract: A medical device that is at least partially formed of a novel metal alloy, which novel metal alloy improves the physical properties of the medical device.
    Type: Application
    Filed: October 5, 2012
    Publication date: April 10, 2014
    Applicant: ICON MEDICAL CORP.
    Inventors: JOSEPH G. FURST, UDAYAN PATEL, RAYMOND BUCKMAN
  • Publication number: 20140100107
    Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I), (B) an inhibitor of the respiratory chain at complex I or II and (C1) an inhibitor of the ergosterol biosynthesis, in particular an azole compound, or (C2) an inhibitor of the respiratory chain at complex III, in particular a strobilurin compound. 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: Application
    Filed: March 28, 2012
    Publication date: April 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrike Wachendorff-Neumann, Ingo Wetcholowsky, Anton Kraus, Thomas Seitz, Jose Augusto Geraldes