The Shared Ring Nitrogen Is Bonded Directly To A Ring Nitrogen Of The Second Ring Of The Bicyclo Ring System (e.g., Pyrazolo[1,5-a]pyrimidine, Etc.) Patents (Class 514/259.3)
  • Patent number: 10960007
    Abstract: The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention also relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention also provides a method for manufacture of medicaments useful in the treatment of such disorders.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: March 30, 2021
    Assignee: RICHTER GEDEON NYRT.
    Inventors: István Borza, Viktor Román, János Éles, Zsuzsa Hadady, József Huszár
  • Patent number: 10953012
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: March 23, 2021
    Assignee: BioEnergenix LLC
    Inventors: John M. McCall, Robert C. Kelly, Donna L. Romero
  • Patent number: 10941162
    Abstract: Trisubstituted bicyclic heterocyclic compounds (e.g., pyridopyrimidinones) and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: March 1, 2019
    Date of Patent: March 9, 2021
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Martin R. Tremblay
  • Patent number: 10934298
    Abstract: The invention provides substituted pyrazolo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[1,5-a]pyrimidinyl carboxamide compounds described herein include 2-heterocyclyl-4-alkyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide compounds and variants thereof. The invention provides, in part, a compound of formula (I-A): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein.
    Type: Grant
    Filed: March 18, 2019
    Date of Patent: March 2, 2021
    Assignee: Bial—Biotech Investments, Inc.
    Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury
  • Patent number: 10875867
    Abstract: The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
    Type: Grant
    Filed: October 14, 2019
    Date of Patent: December 29, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christoph Hoenke, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Sara Frattini, Riccardo Giovannini, Scott Hobson
  • Patent number: 10849902
    Abstract: The present invention provides a medicament for preventing or treating heart failure. More specifically, the present invention provides a medicament for preventing or treating heart failure, comprising a compound selected from the group consisting of (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-methoxyphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-5-(2-fluorophenyl)-2,7,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and salts thereof.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: December 1, 2020
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Takahisa Matsuda, Takashi Motoyaji, Shuji Kitamura, Masato Yoshida
  • Patent number: 10813936
    Abstract: A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
    Type: Grant
    Filed: March 27, 2019
    Date of Patent: October 27, 2020
    Assignee: Array BioPharma, Inc.
    Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
  • Patent number: 10799505
    Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: October 13, 2020
    Assignee: Array BioPharma, Inc.
    Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
  • Patent number: 10786506
    Abstract: The present invention provides a medicament for preventing or treating heart failure. More specifically, the present invention provides a medicament for preventing or treating heart failure, comprising a compound selected from the group consisting of (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-methoxyphenyl)propyl]-2,7,7-trimethyl-5-phenyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, (5R)—N-[1-ethyl-1-(4-ethylphenyl)propyl]-5-(2-fluorophenyl)-2,7,7-trimethyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and salts thereof.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: September 29, 2020
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Takahisa Matsuda, Takashi Motoyaji, Shuji Kitamura, Masato Yoshida
  • Patent number: 10781218
    Abstract: The present disclosure provides compounds of Formula (II-A), which inhibit the interaction of menin with one or more of MLL1, MLL2 and MLL-fusion oncoproteins. Also disclosed are methods for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: September 22, 2020
    Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Tao Wu, Liansheng Li, Yi Wang, Pingda Ren, Jolanta Grembecka, Tomasz Cierpicki, Szymon Klossowski, Jonathan Pollock, Dmitry Borkin
  • Patent number: 10774085
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Grant
    Filed: July 25, 2018
    Date of Patent: September 15, 2020
    Assignee: ARRAY BIOPHARMA INC.
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Patent number: 10758542
    Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: April 8, 2019
    Date of Patent: September 1, 2020
    Assignee: Array BioPharma Inc.
    Inventors: Shelley Allen, Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo
  • Patent number: 10759806
    Abstract: Provided are isotopologues of isoquinolinone and quinazolinone compounds of formula (AB?) that modulate PI3 kinase activity, processes for the preparation of the compounds, pharmaceutical compositions comprising the compounds, and methods of treatment of diseases and disorders using the compounds or pharmaceutical compositions.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: September 1, 2020
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventor: Catherine A. Evans
  • Patent number: 10584128
    Abstract: Bicyclic dihydropyrimidine-carboxamide compounds of formula I described herein inhibit Rho Kinase and may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), and pulmonary arterial hypertension (PAH).
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: March 10, 2020
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Alessandro Accetta, Fabio Rancati, Anna Maria Capelli, David Edward Clark, Patrizia Tisselli, Christine Edwards, Gurdip Bhalay
  • Patent number: 10479794
    Abstract: The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: November 19, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christoph Hoenke, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Sara Frattini, Riccardo Giovannini, Scott Hobson
  • Patent number: 10329294
    Abstract: The present invention relates to pyrazolopyrimidine inhibitors of IRAK4 of formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: March 7, 2016
    Date of Patent: June 25, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Michael D. Altman, Jason D. Brubaker, Craig R. Gibeau
  • Patent number: 10285993
    Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: May 14, 2019
    Assignee: Array BioPharma Inc.
    Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
  • Patent number: 10251889
    Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: April 9, 2019
    Assignee: Array BioPharm Inc.
    Inventors: Shelley Allen, Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo
  • Patent number: 10239882
    Abstract: The invention provides a chemical entity of Formula (I): (I), wherein R1, R2, R3, and R4, have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, and dermatological disorders.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: March 26, 2019
    Assignee: DART NEUROSCIENCE (CAYMAN) LTD.
    Inventors: Amy Lynn Allan, James Breitenbucher, Laurent Gomez, Terence Patrick Keenan, Robert Lemus, Kiev Ly, Tami Jo Marrone
  • Patent number: 10172861
    Abstract: A novel crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.
    Type: Grant
    Filed: January 16, 2018
    Date of Patent: January 8, 2019
    Assignee: Array BioPharma Inc.
    Inventors: Alisha B. Arrigo, Derrick Juengst, Khalid Shah
  • Patent number: 10118930
    Abstract: The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: November 6, 2018
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Manuel Ellermann, Gaelle Valot, Yolanda Cancho Grande, Jorma Haßfeld, Tom Kinzel, Johannes Köbberling, Kristin Beyer, Susanne Röhrig, Michael Sperzel, Jan Stampfuß, Imke Meyer, Maria Köllnberger, Nils Burkhardt, Karl-Heinz Schlemmer, Christian Stegmann, Joachim Schuhmacher, Matthias Werner, Jörg Heiermann, Willem Jan Hengeveld
  • Patent number: 10072000
    Abstract: The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.
    Type: Grant
    Filed: August 13, 2013
    Date of Patent: September 11, 2018
    Assignee: FERRER INTERNACIONAL, S.A.
    Inventors: Luis Anglada, Albert Palomer, Antonio Guglietta
  • Patent number: 10005783
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Grant
    Filed: January 5, 2017
    Date of Patent: June 26, 2018
    Assignee: Array BioPharma Inc.
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Patent number: 9963455
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection.
    Type: Grant
    Filed: January 21, 2015
    Date of Patent: May 8, 2018
    Assignee: Curovir AB
    Inventor: Jacob Westman
  • Patent number: 9862707
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are 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 TrkA.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: January 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Harold B. Wood, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • Patent number: 9845327
    Abstract: The present disclosure provides technologies relating to lysosomal activation. The disclosure provides several strategies for increasing level and/or activity of lysosomal enzyme, and furthermore demonstrates the surprising applicability of such strategies in the treatment and/or prophylaxis of certain proteinopathies. Among other things, the present invention provides methods and compositions for the treatment and/or prophylaxis of proteinopathies other than lysosomal storage diseases through lysosomal activation. In particular, the present disclosure provides methods and compositions for the treatment and/or prophylaxis of neurodegenerative proteinopathies, and in particular those associated with accumulation of ?-synuclein. The present disclosure specifically provides methods and compositions for the treatment and/or prophylaxis of Parkinson's disease.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: December 19, 2017
    Assignee: THE GENERAL HOSPITAL CORPORATION
    Inventors: Dmitri Krainc, Joseph R. Mazzulli
  • Patent number: 9840510
    Abstract: The invention provides substituted pyrazolo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[1,5-a]pyrimidinyl carboxamide compounds described herein include 2-heterocyclyl-4-alkyl-pyrazolo[1,5-a]pyrimidine-3-carboxamide compounds and variants thereof.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: December 12, 2017
    Assignee: LYSOSOMAL THERAPEUTICS INC.
    Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury
  • Patent number: 9796724
    Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: October 24, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Shelley Allen, Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo
  • Patent number: 9580431
    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 10, 2014
    Date of Patent: February 28, 2017
    Assignee: ViiV Healthcare UK (No.5) Limited
    Inventors: B. Narasimhulu Naidu, Manoj Patel, Kevin Peese, Zhongyu Wang
  • Patent number: 9573954
    Abstract: The present teachings provide a compound represented by structural formula (1-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: February 21, 2017
    Assignee: University Health Network
    Inventors: Yong Liu, Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Peter Brent Sampson, Miklos Feher, Grace Ng, Narendra Kumar B. Patel, Yunhui Lang
  • Patent number: 9540393
    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 7, 2014
    Date of Patent: January 10, 2017
    Assignee: ViiV HEALTHCARE UK (NO.5) LIMITED
    Inventors: B. Narasimhulu Naidu, Manoj Patel, Stanley D'Andrea, Zhizhen Barbara Zheng
  • Patent number: 9505763
    Abstract: Methods for regulating cancer cell growth and survival, inhibiting cancer cell growth, promoting cancer cell death, and/or treating a cancer make use of antagonists of a type I BMP receptor. In some embodiments the cancer is a lung cancer and the cancer cell is a lung cancer cell.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: November 29, 2016
    Assignees: Vanderbilt University, Rutgers, The State University of new Jersey
    Inventors: Charles C. Hong, John Langenfeld
  • Patent number: 9493476
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: November 15, 2016
    Assignee: Array BioPharma, Inc.
    Inventors: Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, Hong-Woon Yang, Qian Zhao
  • Patent number: 9487519
    Abstract: 5,6-Dialkyl-7-aminotriazolopyrimidines of the formula I in which the substituents are as defined below: R1 is alkyl or alkoxyalkyl, where the aliphatic groups may be substituted as defined in the description; R2 is CHR3CH3, cyclopropyl, CH?CH2 or CH2CH?CH2; R3 is hydrogen, CH3 or CH2CH3; processes for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: November 8, 2016
    Assignee: BASF SE
    Inventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Oliver Wagner, Matthias Niedenbrück, Maria Scherer, Siegfried Strathmann, Ulrich Schöfl, Reinhard Stierl
  • Patent number: 9447106
    Abstract: The invention is substituted 4,5-dihydro- and 4,5,6,7-tetrahydro-pyrazolo[1,5-?]pyrimidine compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor, such as inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: September 20, 2016
    Assignee: BeiGene, Ltd.
    Inventors: Zhiwei Wang, Yunhang Guo
  • Patent number: 9447104
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Grant
    Filed: September 18, 2014
    Date of Patent: September 20, 2016
    Assignee: Array BioPharma, Inc.
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Patent number: 9353063
    Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: May 31, 2016
    Assignee: Bikam Pharmaceuticals, Inc.
    Inventors: David S. Garvey, Jeremy R. Greenwood, Leah L. Frye
  • Patent number: 9278971
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: June 4, 2014
    Date of Patent: March 8, 2016
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
  • Patent number: 9255071
    Abstract: A pharmaceutically acceptable salt, prodrug or derivative compound of the formula I, wherein R1 is selected from H, a (C1-C5) alkyl group and a COR4 group; R2 is selected from H, a (C1-C5) alkyl group and a COR5 group; R3 is selected from H, a (C1-C5) alkyl group, a (C1-C5)-O-alkyl group, a cycloalkyl of (C5-C6) carbon atoms, an aryl group, and an aryl (C1-C5) alkyl group wherein the aryl group can be an unsubstituted aryl or substituted with one or more R6 groups and an NHCOR5 group, or the R2 and R3 groups together with N may form a piperidine, morpholine or piperazine group; R4 is selected from H and a (C1-C5)alkyl group; R5 is selected from an aryl group unsubstituted or substituted with one or more R6, linear or branched(C1-C5) alkyl or pyridyne groups and a pyridine group; R6 is selected from (C1-C5)alkyl groups, halogen and nitro.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: February 9, 2016
    Assignees: Consejo Nacional de Investigaciones Cientificas y Técnicas (CONICET), Laboratorios Richmond Sociedad Anónima Comercial Industrial y Financiera
    Inventors: Gerardo Burton, Fernando Javier Duran, Mario David Martinez, Elvira Zini, Veronica Mora Munoz, Lucila Bertoncello
  • Patent number: 9255103
    Abstract: In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazines analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: February 9, 2016
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor Macdonald, Han Min Tong, Carrie K. Jones
  • Patent number: 9096605
    Abstract: PI3K? selective compounds having the structure
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: August 4, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Hong Lin, Juan Ignacio Luengo, Michael Lee Moore, Junya Qu, Ralph A. Rivero, Rosanna Tedesco, Hongyi Yu
  • Patent number: 9045484
    Abstract: The present invention provides pyridinyl-substituted pyrazolyl pyrimidine small molecule inhibitors of bone morphogenetic protein (BMP) signaling having the structure of formula (I), wherein variables A, B, E, F, X, Y, Z, Ar, L1, R4 and R15 are as defined in the specification. The compounds of the invention are useful in modulating cell growth, differentiation, proliferation, and apoptosis, and thus are useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: June 2, 2015
    Assignees: The Brigham and Women's Hospital, Inc., The General Hospital Corporation
    Inventors: Paul B. Yu, Gregory D. Cuny, Kenneth D. Bloch, Randall T. Peterson, Charles C. Hong
  • 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: 20150126506
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Publication number: 20150126531
    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: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Applicant: Saint Louis College of Pharmacy
    Inventor: John M. Beale
  • Patent number: 9023844
    Abstract: Heterocyclylpyri(mi)dinylpyrazole of the formula (I) in which R1 to R5, X1, U, Q, W, Y, n, a, b have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: May 5, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stefan Hillebrand, Amos Mattes, Alexander Sudau, Pierre Wasnaire, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann, Haruko Sawada, Philippe Desbordes, Anne-Sophie Rebstock, Stéphane Brunet, Hélène Lachaise, Philippe Rinolfi
  • Patent number: 9018219
    Abstract: The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2?X3 is CR5—CR6?CR7, N—CR6?CR7, CR5—N?CR7 or CR5—CR6?N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: April 28, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Moriyasu Masui, Genta Tadano
  • Publication number: 20150111874
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 23, 2015
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Martin R. TREMBLAY
  • Publication number: 20150105377
    Abstract: The invention discloses methods and compositions for treating or preventing RAF kinase mediated diseases or conditions by administering a compound of Formula 1: or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the variables are defined as herein.
    Type: Application
    Filed: March 12, 2013
    Publication date: April 16, 2015
    Inventors: Joseph M. Gozgit, Victor M. Rivera, William C. Shakespeare, Xiaotian Zhu, David C. Dalgarno
  • Patent number: 9006235
    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: April 14, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zhizhen Barbara Zheng, Stanley D'Andrea, David R. Langley, B. Narasimhulu Naidu