The Ring Nitrogens Are Bonded Directly To Each Other (e.g., Pyridazine, Etc.) Patents (Class 514/236.5)
  • Patent number: 10329259
    Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X and Y are each independently selected from optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted cycloalkyl, optionally-substituted heterocycloalkyl, or optionally-substituted alkyl; Q is H, hydroxyl, or optionally-substituted alkoxy; R1, R2, and R3 are each independently selected from H, optionally-substituted alkyl, optionally-substituted cycloalkyl, halogen, cyano, nitro, hydroxy, optionally-substituted alkoxy, amino, aminocarbonyl, optionally-substituted sulfonyl, optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted carboxyl, acyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted phosphonyl, optionally-substituted phosphinyl, aralkyl, optionally-substituted thiol, or R2 and R3 together with Z form an optionally-substituted cycloalkyl ring or an optionally-substituted heterocycloalkyl ring; Z is B
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: June 25, 2019
    Assignee: The United States of America, as represented by the Secretary, Department of Health & Human Services
    Inventors: George Kunos, Malliga Iyer, Resat Cinar, Kenner C. Rice
  • Patent number: 10323022
    Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(?X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: December 12, 2017
    Date of Patent: June 18, 2019
    Assignee: Array BioPharma Inc.
    Inventors: Shelley Allen, Steven W. Andrews, James F. Blake, Kevin R. Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Gabrielle R. Kolakowski, Jeongbeob Seo
  • Patent number: 10272072
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Grant
    Filed: November 15, 2016
    Date of Patent: April 30, 2019
    Assignees: Forma TM, LLC, Genentech, Inc.
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre Joseph Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
  • Patent number: 10189810
    Abstract: There are provided inter alia pyrazolyl-substituted pyridone compounds, which exhibit biological activity, e.g., inhibitory action, against serine proteases, including thrombin and various kallikreins. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of serine proteases, including thrombin and various kallikreins.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: January 29, 2019
    Assignee: VERSEON CORPORATION
    Inventors: Kevin Michael Short, David Ben Kita, Maria de los Angeles Estiarte-Martinez, Son Minh Pham
  • Patent number: 10160727
    Abstract: The present invention relates to a compound represented by Formula (I): wherein -L- is —C(?X)—, or the like, —Z— is —NR5—, or the like, —ZA— is —NR5A—, or the like, —W— is —C(R8R9)n-, —WA— is —C(R3R4)m-, B is substituted or unsubstituted aromatic carbocyclyl, or the like, Y is a bond, or the like, the ring C is a substituted or unsubstituted aromatic heterocycle, or the like, R2 is a hydrogen atom, or the like, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: December 25, 2018
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenichiroh Nakamura, Takatsugu Inoue
  • Patent number: 10138208
    Abstract: Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: November 27, 2018
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: David J. Daniels, Ian F. Parney, Timothy E. Peterson
  • Patent number: 10072003
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: September 11, 2018
    Inventors: Ashok Arasappan, Christopher James Bungard, Jessica L. Frie, Yongxin Han, Scott B. Hoyt, Peter J. Manley, Robert S. Meissner, James J. Perkins, Iyassu K. Sebhat, Robert R. Wilkening, Kenneth J. Leavitt
  • Patent number: 10022354
    Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylases, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: July 17, 2018
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS INC.
    Inventors: Kwong Wah Lai, Jun Liang, Birong Zhang, Sharada Labadie, Daniel Ortwine, Peter Dragovich, James Kiefer, Victor S. Gehling, Jean-Christophe Harmange
  • Patent number: 9974775
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Grant
    Filed: July 6, 2016
    Date of Patent: May 22, 2018
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus Maria Gijsen, Saravanan Vadivelu, Mark Wall, Christopher Flores
  • Patent number: 9975886
    Abstract: Provided are compounds of the formula: and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels.
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: May 22, 2018
    Assignee: Cadent Therapeutics, Inc.
    Inventors: Dipak Vasantrao Amrutkar, Kelly Foster, Thomas Amos Jacobsen, Martin R. Jefson, Gregg F. Keaney, Janus Schreiber Larsen, Karin Sandager Nielsen
  • Patent number: 9932314
    Abstract: The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
    Type: Grant
    Filed: June 2, 2015
    Date of Patent: April 3, 2018
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Romain Siegrist, Bibia Heidmann, Simon Stamm, John Gatfield, Olivier Bezencon
  • Patent number: 9896447
    Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: February 20, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Chun Sing Li, Qinghua Mao
  • Patent number: 9890127
    Abstract: Disclosed are compounds, such as pyridazinones, that can be, inter alia, used for treating cancer.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: February 13, 2018
    Assignees: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Timothy A. Lewis, Benito Munoz, Lucian De Waal, Heidi Greulich, Matthew Meyerson, Lara Nicole Gechijian
  • Patent number: 9850216
    Abstract: Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of Ack1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new Ack1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I through IV are disclosed.
    Type: Grant
    Filed: August 6, 2014
    Date of Patent: December 26, 2017
    Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Nupam P. Mahajan, Kiran N. Mahajan, Nicholas J. Lawrence, Harshani R. Lawrence
  • Patent number: 9802960
    Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: January 13, 2015
    Date of Patent: October 31, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
  • Patent number: 9771353
    Abstract: Compounds are of formula (I): The compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: April 1, 2014
    Date of Patent: September 26, 2017
    Assignees: TOPIVERT PHARMA LIMITED, RESPIVERT LIMITED
    Inventor: Matthew Colin Thor Fyfe
  • Patent number: 9730914
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula I, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: August 15, 2017
    Assignee: Axikin Pharmaceuticals
    Inventor: Tai Wei Ly
  • Patent number: 9718841
    Abstract: The present invention provides substituted bicyclic pyrazolone compounds, which are used to inhibit or modulate the activity of receptor tyrosine kinases, especially Axl, Mer, c-Met and Ron. The invention also provides pharmaceutical compositions comprising the compound disclosed herein, and a method of preventing, treating or lessening the severity of a proliferative disorder in a patient with the compounds or the pharmaceutical compositions disclosed herein.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: August 1, 2017
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Yanjun Wu
  • Patent number: 9670182
    Abstract: The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) in which R1, R2, R3 and R4 are each as defined in the description, by conversion of compounds of the general formula (IV) in the presence of a palladium catalyst and carbon monoxide. The present invention likewise relates to compounds of the general formula (IV).
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: June 6, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Thomas Himmler, Sergii Pazenok, Frank Volz, Norbert Lui
  • Patent number: 9592237
    Abstract: Use of a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for the preparation of drugs useful for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level, as well as a method for increasing motor neuron excitability through the administration of a CB1 antagonist/ inverse agonist receptors, and to the use of a pharmaceutical composition which comprises a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: March 14, 2017
    Assignee: Fundacion Del Hospital Nacional De Paraplejicos Para La Investigacion Y La Integracion (FUHNPAIIN)
    Inventors: Antonio Oliviero, Juan de Los Reyes Aguilar Lepe, Mario Rotondi, Eduardo Molina Holgado, Luca Chiovato, Guglielmo Foffani, Laura Mordillo Mateos, Angel Lozano Sicilia, Daniel Garcia Ovejero, Angel Arevalo Martin, Yolanda Perez Borrego
  • Patent number: 9556149
    Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: January 31, 2017
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
  • Patent number: 9546163
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula I, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: January 17, 2017
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventor: Tai Wei Ly
  • Patent number: 9527819
    Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: December 27, 2016
    Assignees: NORTHWESTERN UNIVERSITY, UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: D. Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdalena Zasadzki
  • Patent number: 9517227
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: June 10, 2014
    Date of Patent: December 13, 2016
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste Deselm, Andreas Goutopoulos
  • Patent number: 9493438
    Abstract: The invention, in a first aspect relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered aromatic ring, or a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, or a 6-membered benzocondensed heteroaromatic ring containing N as heteroatom, optionally each of said rings being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, cyano, trifluoromethyl, dimethylamino, or phenyl which optionally is substituted with one or more halogen atoms, or a 5- or 6-membered heterocycle containing from one to three nitrogen atoms; X is O or N; P is pyridyl, pyrimidyl, pyrazyl, or pyridazyl, each being optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, and cyano, and use thereof as pharmaceuticals.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: November 15, 2016
    Assignee: Rottapharm S.R.L.
    Inventors: Luigi Piero Stasi, Lucio Rovati, Roberto Artusi, Clara Bovino, Fabrizio Colace, Stefano Mandelli
  • Patent number: 9469634
    Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: October 18, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yongxin Han, Chun Sing Li
  • Patent number: 9458112
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: October 4, 2016
    Assignee: NOVARTIS AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Patent number: 9453002
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: September 27, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus Maria Gijsen, Saravanan Vadivelu, Mark Wall
  • Patent number: 9428460
    Abstract: The invention relates to N-[4-(quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides, intermediates and methods for their production, use thereof for treating and/or preventing diseases and use thereof for producing medicinal products and use thereof for treating and/or preventing diseases, especially of hyperproliferative diseases.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: August 30, 2016
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Duy Nguyen, Hermann Künzer, Hortensia Faus Gimenez, Benjamin Bader, Silke Köhr, Martin Fritsch
  • Patent number: 9403799
    Abstract: Compounds selected from the group according to claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: August 2, 2016
    Assignee: MERCK PATENT GMBH
    Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
  • Patent number: 9346792
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: May 24, 2016
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Patent number: 9321757
    Abstract: The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: April 26, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masato Yoshida, Kazuaki Takami, Yusuke Tominari, Zenyu Shiokawa, Akito Shibuya, Yusuke Sasaki, Tony Gibson, Terufumi Takagi
  • Patent number: 9289365
    Abstract: Cosmetic compositions comprising substituted carbamoyl heterocyclic analogs and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The substituted carbamoyl heterocyclic analogs are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: March 22, 2016
    Assignee: Avon Products, Inc.
    Inventors: Cheng Hwang, John Lyga, Hong Hu
  • Patent number: 9260410
    Abstract: There is provided inter alia a compound of formula (I): wherein R1, J, Ar, L, X, R3 and R4 are as defined in the specification, for use in the treatment of inflammatory disorders.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: February 16, 2016
    Assignee: Respivert Ltd.
    Inventors: John King-Underwood, Kazuhiro Ito, Peter Strong, William Garth Rapeport, Catherine Elisabeth Charron, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
  • Patent number: 9242960
    Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers and tautomers, which is an inhibitor of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: January 26, 2016
    Assignee: Respivert, Ltd.
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Onions, Catherine Elisabeth Charron
  • Patent number: 9233957
    Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide of Formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.
    Type: Grant
    Filed: June 11, 2012
    Date of Patent: January 12, 2016
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
  • Patent number: 9216991
    Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: December 22, 2015
    Assignee: Ares Trading S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
  • Patent number: 9113631
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z1, Z2, J1, J2, M, R1a, R1b, R2a, R2b, R2c, R2d and R14 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: August 25, 2015
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Thomas Francis Pahutski, Jr., George Philip Lahm, Moumita Kar, Omar Khaled Ahmad
  • Patent number: 9056853
    Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is A1 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.
    Type: Grant
    Filed: June 2, 2014
    Date of Patent: June 16, 2015
    Assignee: BASF SE
    Inventors: Thomas Schmidt, Michael Puhl, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Toni Bucci, Henry Van Tuyl Cotter, David G. Kuhn, Hassan Oloumi-Sadeghi
  • Patent number: 9051313
    Abstract: The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: June 9, 2015
    Assignee: Gildead Sciences, Inc.
    Inventor: Gregory Notte
  • Patent number: 9040516
    Abstract: The present invention provides: an uracil derivative represented by general formula (I) or a physiologically acceptable salt thereof (in the formula, R1 represents a hydrogen atom, a C1-10 alkyl group, a C2-6 alkene group or a 3- to 6-membered saturated or 4- to 6-membered unsaturated aliphatic ring group which may contain 1 to 2 hetero atoms independently selected from the group consisting of N, O and S; R2 represents a hydrogen atom, a halogen atom, a cyano group, —NRcRd, —N?CHN(CH3)2, or an C1-3 alkyl group; Ar1 and Ar2 independently represent a 5- to 6-membered aromatic ring group which may contain 1 to 3 hetero atoms independently selected from the group consisting of N, O and S; and L represents a 6-membered aromatic ring group which may contain 1 to 4 nitrogen atoms, a pyrazole group, a triazole group, or an imidazole group); and a therapeutic agent or prophylactic agent for various inflammatory diseases associated with elastase, comprises the compound or the like as an active ingredient.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: May 26, 2015
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Tomoya Shiro, Masanori Tobe, Katsumi Kubota, Yosuke Takanashi, Tomoaki Nakamura, Toshihiko Sone
  • Publication number: 20150133451
    Abstract: The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 14, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masato Yoshida, Kazuaki TAKAMI, Yusuke TOMINARI, Zenyu SHIOKAWA, Akito SHIBUYA, Yusuke SASAKI, Tony GIBSON, Terufumi TAKAGI
  • Publication number: 20150133452
    Abstract: Compounds selected from the group according to claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: January 22, 2015
    Publication date: May 14, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Oliver SCHADT, Dieter DORSCH, Frank STIEBER, Andree BLAUKAT
  • Publication number: 20150126485
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150126364
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z1, Z2, J1, J2, M, R1a, R1b, R2a, R2b, R2c, R2d, R14 and R14a are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Applicant: E I Du Pont de Nemours and Company
    Inventors: Thomas Francis Pahutski, JR., Matthew James Campbell, Dominic Ming-Tak Chan, Jeffrey Keith Long, Thomas Martin Stevenson
  • Publication number: 20150105389
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
  • Publication number: 20150105388
    Abstract: This invention relates to new carboxamide-substituted heteroaryl-pyrazoles, method for their production, their use for the treatment and/or prophylaxis of diseases, as well as their use for the production of pharmaceutical agents for the treatment and/or prophylaxis of diseases, in particular retroviral diseases, in humans and/or animals.
    Type: Application
    Filed: November 29, 2012
    Publication date: April 16, 2015
    Applicant: AICURIS GMBH & CO. KG
    Inventors: Steffen Wildum, Burkhard Klenke, Astrid Wendt
  • Publication number: 20150105390
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Applicant: IRM LLC, a Delaware Limited Liability Company
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Publication number: 20150080397
    Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 19, 2015
    Inventors: Tai Wei LY, Erik Dean RAAUM
  • Publication number: 20150080375
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: October 14, 2014
    Publication date: March 19, 2015
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Monique Bodil Van Niel, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley