The Additional Ring Is A Hetero Ring Patents (Class 514/326)
  • Patent number: 10590122
    Abstract: This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.
    Type: Grant
    Filed: September 11, 2018
    Date of Patent: March 17, 2020
    Assignee: Cyteir Therapeutics, Inc.
    Inventors: Alfredo C. Castro, Casey Cameron McComas, Joseph Vacca, Tyler Maclay
  • Patent number: 10590119
    Abstract: Furoxan compounds, compositions comprising the same, and methods of making and using the same, are described.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: March 17, 2020
    Assignee: The University of Toledo
    Inventors: Isaac Schiefer, Zahoor Shah
  • Patent number: 10570117
    Abstract: Phenylimidazole compounds of formula (1) shown below and pharmaceutically acceptable salts thereof: Also disclosed are a pharmaceutical composition and a lipoprotein lipase activator, each containing one of the phenylimidazole compounds.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: February 25, 2020
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Koushi Iwata, Tadao Shibutani, Satoshi Kido, Daisuke Mori, Hidenori Yoshioka, Hikaru Nakata, Akiko Ishimaru
  • Patent number: 10555935
    Abstract: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: February 11, 2020
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Mary-Margaret Zablocki
  • Patent number: 10550100
    Abstract: The present invention discloses compounds according to Formula I: Wherein R1, R2, R3a, R3b, R6, Cy, and the subscript n are as defined herein. The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering the compound of the invention.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: February 4, 2020
    Assignee: GALAPAGOS NV
    Inventors: Frédéric Gilbert Labéguère, Rama Heng, Frédéric André De Ceuninck, Luke Jonathan Alvey, David Amantini, Franck Laurent Brebion, Pierre Marc Marie Joseph Deprez, Romain Luc Marie Gosmini, Hélène Marie Jary, Christophe Peixoto, Iuliana Ecaterina Pop-Botez, Marie Laurence Claire Varin
  • Patent number: 10472351
    Abstract: The present technology is directed to modulators of nuclear receptor activity, specifically to the modulation of NR2F6 activity and NR2F6 utilizing compounds, and the immune modulation and modulation of cancer stem cell activity through administration of compounds described herein to animals.
    Type: Grant
    Filed: June 14, 2018
    Date of Patent: November 12, 2019
    Assignee: Zander Therapeutics, Inc.
    Inventors: Harry M. Lander, David R. Koos
  • Patent number: 10441580
    Abstract: Aspects of the invention relate generally to the treatment of schizophrenia in an individual and, more specifically, to the treatment of an individual with iloperidone, an iloperidone metabolite, or a pharmaceutically-acceptable salt thereof. In one embodiment, the invention provides a method of preventing schizophrenic relapse in an individual diagnosed with schizophrenia, the method comprising: administering to the individual iloperidone, an iloperidone metabolite, or a pharmaceutically-acceptable salt thereof at a daily dose between about 12 mg and about 16 mg following a period in which the individual's schizophrenia was stabilized.
    Type: Grant
    Filed: February 17, 2016
    Date of Patent: October 15, 2019
    Assignee: Vanda Pharmaceuticals, Inc.
    Inventors: Mihael H. Polymeropoulos, Curt D. Wolfgang
  • Patent number: 10428055
    Abstract: The present invention relates to a substituted piperidines represented by following Chemical Formula 1, which have a GPR119 agonistic activity, a method for preparing the same, and a pharmaceutical composition including the same: wherein A, B, and X are defined therein.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: October 1, 2019
    Assignee: DONG-A ST CO., LTD.
    Inventors: Jae Sung Yang, Gye Rim Baek, Yoon Jung Kim, Chi Young Ahn, Jae Young Lee, Il Hoon Jung, Mi Kyung Kim, So Mi Kang, Hyo Ju Lee, Yu Na Chae, Ye Hwang Cheong, Tae Hyoung Kim, Eun Kyoung Yang, Moon Ho Son, Chang Yell Shin
  • Patent number: 10426169
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols RA1, RA2, X, Y, L1, L2, RB1, RB2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: October 30, 2017
    Date of Patent: October 1, 2019
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Thomas Seitz, Stefan Hillebrand, Juergen Benting, Jan Peter Schmidt, Pierre Cristau
  • Patent number: 10421716
    Abstract: The invention relates to a novel process for preparing ?-carboxamide pyrrolidine derivatives, in particular (2S, 5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide, and to novel intermediates for use in said process along with processes for preparing said intermediates.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: September 24, 2019
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: David MacPherson, David Witty, Gerard Giblin, Michael Williams, Donald Walker, William Kiesman, Tamera Mack
  • Patent number: 10377750
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treatment of neurodegenerative diseases and disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: May 18, 2018
    Date of Patent: August 13, 2019
    Assignee: Eli Lilly and Company
    Inventors: Nicolas Jacques Francois Dreyfus, Peter James Lindsay-Scott, Richard Edmund Rathmell
  • Patent number: 10370405
    Abstract: The invention relates to C-3 novel triterpenone with C-28 amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases (formula 1).
    Type: Grant
    Filed: March 12, 2016
    Date of Patent: August 6, 2019
    Assignee: HETERO LABS LIMITED
    Inventors: Parthasaradhi Reddy Bandi, Rathnakar Reddy Kura, David Krupadanam Gazula Levi, Panduranga Reddy Adulla, Eswara Rao Bammidi, Bhaskar Reddy Kasireddy, Sudhakar Neela, Carl Thomas Wild, David Eugene Martin, Theodore John Nitz
  • Patent number: 10363248
    Abstract: The present disclosure relates to salts of heterocyclic compounds and methods that inhibit HIF pathway activity. The compounds are designed to treat or prevent cancer and other hypoxia-mediated diseases.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: July 30, 2019
    Assignee: Board of Regents, The University of Texas System
    Inventors: Philip Jones, Maria Emilia Di Francesco, Timothy McAfoos
  • Patent number: 10336742
    Abstract: The present invention relates to a novel process for preparing thiazole derivatives.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: July 2, 2019
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Günter Hömberger, Mark James Ford
  • Patent number: 10300110
    Abstract: The application provides data from a clinical trial of a PSD-95 inhibitor in subjects undergoing endovascular repair of an aneurysm in or otherwise affecting the CNS. The subjects were stratified by whether the aneurysm ruptured before performing the endovascular surgery. Rupture is associated with higher mortality or increased debilitation if a subject survives. The trial provided evidence of significant benefit in subjects with and without aneurysm rupture before endovascular was surgery performed. Surprisingly, the subjects benefiting most from treatment as judged both by pathology and neurocognitive outcome were those in which the aneurysm had ruptured causing a subarachnoid hemorrhage. These data constitute evidence that a PSD-95 inhibitor is beneficial not only in ischemic and hemorrhagic stroke but in forms of hemorrhage in or affecting the CNS, particularly, subarachnoid hemorrhage.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: May 28, 2019
    Assignee: NoNO, Inc.
    Inventors: Michael Tymianski, Jonathan David Garman
  • Patent number: 10231950
    Abstract: The present invention is directed to the treatment of erythromelalgia comprising administering to a subject in need thereof, a therapeutically effective amount of 5-(4-{[(2-fluorophenyl)methyl]oxy}phenyl)-prolinamide or a pharmaceutically acceptable salt, solvate or prodrug thereof.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: March 19, 2019
    Assignee: Convergence Pharmaceuticals Limited
    Inventor: Valerie Morisset
  • Patent number: 10226470
    Abstract: Methods are provided for treating autoimmune disease in a subject by inhibiting the activity of DGAT1.
    Type: Grant
    Filed: June 2, 2015
    Date of Patent: March 12, 2019
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Kareem Graham, Eugene C. Butcher
  • Patent number: 10213415
    Abstract: The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: February 26, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Henry J. Breslin, Chaozhong Cai, Wei He, Robert W. Kavash
  • Patent number: 10117857
    Abstract: An external medicine for diffuse plexiform neurofibromas is provided. The external medicine for diffuse plexiform neurofibromas in accordance with an embodiment of the present invention contains, as an active ingredient, at least one selected from the group consisting of sirolimus and sirolimus derivatives.
    Type: Grant
    Filed: March 9, 2016
    Date of Patent: November 6, 2018
    Assignee: Osaka University
    Inventors: Mari Kaneda, Ichiro Katayama
  • Patent number: 10081625
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treatment of neurodegenerative diseases and disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: September 25, 2018
    Assignee: Eli Lilly and Company
    Inventors: Nicolas Jacques Francois Dreyfus, Peter James Lindsay-Scott
  • Patent number: 10040780
    Abstract: Provided herein are Mcl-1 antagonist compositions and methods of treating g the compositions described herein.
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: August 7, 2018
    Assignees: The Regents of the University of California, The Royal Institute for the Advancement of Learning/McGill University
    Inventors: Patrick Harran, James H. Frederich, Gordon Shore, Mai Nguyen
  • Patent number: 10039748
    Abstract: Described herein are compounds of Formula (I-a) and (I-b), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: August 7, 2018
    Assignee: Epizyme, Inc.
    Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei, Kevin Wayne Kuntz
  • Patent number: 9975889
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: May 22, 2018
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stefan Hillebrand, Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Pierre Wasnaire, Tomoki Tsuchiya, Juergen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
  • Patent number: 9937145
    Abstract: The present invention relates to a pharmaceutical composition for treating or preventing epilepsy containing a sulfamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention epilepsy comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of epilepsy.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: April 10, 2018
    Assignee: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Patent number: 9924721
    Abstract: Malonic ester derivatives of the formula (I) in which the symbols A1, A2, Y, R10, p, X, R2, G, Q, L2 and R1 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: August 26, 2014
    Date of Patent: March 27, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Stefan Hillebrand, Matthias Riedrich, Sebastian Hoffmann, Mark James Ford, Joachim Telser, Mazen Es-Sayed, Guenter Hoemberger, Pierre Wasnaire, Ulrike Wachendorff-Neumann, Tomoki Tsuchiya, Valerie Toquin
  • Patent number: 9862701
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein R1, R2, R3a, R3b, R4a, R4b, G1, G2, L, m1, m2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: January 9, 2018
    Assignee: Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Pingda Ren, Yi Liu
  • Patent number: 9783534
    Abstract: The present invention relates to a novel crystalline form of 2-{3-[2-(1-{[3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2-oxazol-5-yl}-3-chlorophenylmethansulphonate, to processes for its preparation and to its use in agrochemical preparations.
    Type: Grant
    Filed: October 13, 2014
    Date of Patent: October 10, 2017
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Britta Olenik, Stefan Hillebrand, Pierre Wasnaire, Martin Weiss, Ulrike Wachendorff-Neumann
  • Patent number: 9757358
    Abstract: The invention refers to a combination comprising a sigma ligand of formula (I) and an opioid or opiate for use in the prevention and/or treatment of pain developed as a consequence of surgery, especially peripheral neuropathic pain, allodynia, causalgia, hyperalgesia, hyperesthesia, hyperpathia, neuralgia, neuritis or neuropathy. The invention also refers to the sigma ligands of formula (I) for use in potentiating the analgesic effect of an opioid or opiate and/or for decreasing the dependency induced thereby when said opioid or opiate is used in the prevention and/or treatment of pain developed as a consequence of surgery.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: September 12, 2017
    Assignee: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: José Miguel Vela Hernández, Daniel Zamanillo-Castanedo
  • Patent number: 9745341
    Abstract: Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations.
    Type: Grant
    Filed: October 23, 2015
    Date of Patent: August 29, 2017
    Assignee: Endocyte, Inc.
    Inventors: Iontcho Radoslavov Vlahov, Christopher Paul Leamon, Kevin Yu Wang
  • Patent number: 9725414
    Abstract: The present invention relates to fungicidal N-bicycloalkyl and N-tricycloalkyl pyrazole-4-(thio)carboxamide derivatives of formula (I), wherein T represents O or S; n represents 0 or 1; and B represents where the bond marked by * is attached to the (CZ2Z3)n-N amide moiety, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: August 8, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jurgen Benting, Stephane Brunet, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Helene Lachaise, Jan-Peter Schmidt, Philippe Rinolfi, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 9669013
    Abstract: This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R1-R5, X1, X2 and p are as defined herein.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: June 6, 2017
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Mark Pickworth, Benjamin Gerald Tehan
  • Patent number: 9662347
    Abstract: The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: May 30, 2017
    Assignee: Gachon University of Industry-Academic Cooperation Foundation
    Inventors: Bong Hee Lee, Kyung Hee Byun
  • Patent number: 9650370
    Abstract: This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand-[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.
    Type: Grant
    Filed: May 16, 2014
    Date of Patent: May 16, 2017
    Assignee: Centrexion Therapeutics Corporation
    Inventors: Doris Riether, Florian Paul Christian Binder, Henri Doobs, Stephan Georg Mueller, Janet Rachel Nicholson, Achim Sauer
  • Patent number: 9617241
    Abstract: The present invention relates to a process for the preparation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (Efinaconazole) and intermediates used in such process.
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: April 11, 2017
    Assignee: MAPI PHARMA LTD.
    Inventors: Anna Gopin, Shai Rubnov, Galina Zats, Ehud Marom
  • Patent number: 9616130
    Abstract: Pharmaceutically acceptable solubilizing compositions comprising (i) at least one tocopheryl compound having a polyalkylene glycol moiety and (ii) at least one alkylene glycol fatty acid monoester or mixture of alkylene glycol fatty acid mono-and diester are disclosed. The solubilizing compositions are useful in the manufacture of pharmaceutical dosage forms comprising a melt-processed mixture of at least one active ingredient and at least one pharmaceutically acceptable polymer. The solubilizing compositions enhance the bioavailability of the active ingredient following oral intake.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: April 11, 2017
    Assignee: ABBVIE DEUTSCHLAND GMBH & CO KG
    Inventors: Jörg Rosenberg, Jörg Breitenbach, Kennan Marsh, Bernd Liepold, Christoph Schmidt, Ute Lander
  • Patent number: 9572343
    Abstract: The invention relates to active compound combinations, in particular within a composition, which comprises (A) an amidine compound of formula (I) and a further fungicidally (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants, 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: Grant
    Filed: September 2, 2013
    Date of Patent: February 21, 2017
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Ulrike Wachendorff-Neumann, Thomas Seitz
  • Patent number: 9550732
    Abstract: An organic carboxylic acid salt of 2-[(3S,4R)-1-{[2-chloro-6-(trifluoromethyl)phenyl]methyl}-3-{[1-(cyclohex-1-en-1-ylmethyl) piperidin-4-yl]carbamoyl}-4-methylpyrrolidin-3-yl]acetic acid and a crystal thereof.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: January 24, 2017
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Kenshi Yoshida, Ikuo Kushida
  • Patent number: 9545105
    Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl) piperidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: January 17, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 9546146
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: March 9, 2016
    Date of Patent: January 17, 2017
    Assignee: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Samuel J. Danishefsky, Joan Massague, Manuel Valiente Cortes, Thordur Oskarsson, Malcolm Moore, Nicolas Lecomte, Ouathek Ouerfelli, Guangli Yang
  • Patent number: 9512117
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: December 6, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stefan Hillebrand, Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Pierre Wasnaire, Tomoki Tsuchiya, Juergen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
  • Patent number: 9476887
    Abstract: Successful application of an engineered protein as therapeutics or in other industries would require the protein to have good expression level, good biophysical properties and often desired affinity to its target. The present invention provides a method of screening large numbers of protein candidates (PCs) in all three aspects simultaneously. PCs are fused to a protein anchor, which is captured by the target/antigen. The captured PCs are evaluated for their expression levels, biophysical properties and affinities using conventional methods.
    Type: Grant
    Filed: August 18, 2010
    Date of Patent: October 25, 2016
    Assignee: National Research Council of Canada
    Inventors: Jianbing Zhang, Tomoko Hirama
  • Patent number: 9434760
    Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: September 6, 2016
    Assignee: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
    Inventors: Min Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
  • Patent number: 9375009
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols RA1, RA2, X, Y, L1, L2, RB1, RB2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: June 28, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Thomas Seitz, Stefan Hillebrand, Juergen Benting, Jan Peter Schmidt, Pierre Cristau
  • Patent number: 9303009
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: April 5, 2016
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Joan Massague, Manuel Valiente Cortes, Thordur Oskarsson, Malcom Moore, Nicolas Lecomte, Ouathek Ouerfelli, Guangli Yang
  • Patent number: 9260406
    Abstract: Specifically useful stereoisomers of 1,3-dioxane derivatives are described and their use in the treatment of a disease or condition dependent on PPAR modulation, such as diabetes, cancer, inflammation, neurodegenerative disorders and infections as well as their use in the treatment of a disease related to TP, such as cardiovascular diseases.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: February 16, 2016
    Assignee: Evolva SA
    Inventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Prathama S. Mainkar, Melya Hughes Crameri
  • Patent number: 9216971
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: December 22, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Patent number: 9204649
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols are each as defined in the description, and agrochemically active salts thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: May 29, 2014
    Date of Patent: December 8, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Sebastian Hoffmann, Pierre Wasnaire, Tomoki Tsuchiya, Pierre Cristau, Thomas Seitz, Joachim Kluth, Jurgen Benting, Ulrike Wachendorff-Neumann
  • Patent number: 9187521
    Abstract: Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: November 17, 2015
    Assignee: Endocyte, Inc.
    Inventors: Iontcho Radoslavov Vlahov, Christopher Paul Leamon, Yu Wang
  • Patent number: 9169248
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: October 27, 2015
    Assignee: ChemoCentryx, Inc.
    Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
  • Patent number: 9150565
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: October 6, 2015
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Pierre Cristau, Thomas Seitz, Joachim Kluth, Stefan Hillebrand, Juergen Benting, Daniela Portz, Ulrike Wachendorff-Neumann