Two Of The Ring Nitrogens Are Bonded Directly To Each Other Patents (Class 546/119)
  • Patent number: 10662195
    Abstract: The invention relates to protein conjugates that contain a protein kinase containing a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.
    Type: Grant
    Filed: July 18, 2016
    Date of Patent: May 26, 2020
    Assignee: Celgene CAR LLC
    Inventors: Juswinder Singh, Russell Colyn Petter, Deqiang Niu, Lixin Qiao, Arthur Kluge, Roy Lobb, Shomir Ghosh, Zhendong Zhu
  • Patent number: 10544143
    Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: December 17, 2018
    Date of Patent: January 28, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Sreekantha Ratna Kumar
  • Patent number: 10519151
    Abstract: This application relates to substituted [1,2,4]triazolo[4,3-a]pyridines of formula (I), compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to substituted [1,2,4]triazolo[4,3-a]pyridines and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: December 31, 2019
    Assignee: Neomed Institute
    Inventors: Malken Bayrakdarian, Stephen Claridge, Andrew Griffin
  • Patent number: 10478425
    Abstract: Provided is a compound which is useful as an AMPK activator. The compound is represented by formula: wherein the symbols are defined in the specification.
    Type: Grant
    Filed: February 24, 2017
    Date of Patent: November 19, 2019
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Yuusuke Tamura, Hiroki Ozasa
  • Patent number: 10472357
    Abstract: The invention relates to a compound of Formula I or IA and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: November 12, 2019
    Assignee: Flatley Discovery Lab, LLC
    Inventors: Bridget M. Cole, Richard A. Nugent, Paul T. Smith, Jr.
  • Patent number: 10414764
    Abstract: The present invention relates to a process for the preparation substantially pure propane-1-sulfonicacid-{3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide or Vemurafenib of Formula (I).
    Type: Grant
    Filed: November 19, 2015
    Date of Patent: September 17, 2019
    Assignee: SHILPA MEDICARE LIMITED
    Inventors: Purohit Prashant, Nagnnath Kokare, Veera Reddy Yenireddy, Chaturvedi Akshay Kant
  • Patent number: 10377754
    Abstract: An object of the present invention is to develop and provide a novel agricultural and horticultural insecticide in view of the still immense damage caused by insect pests etc. and the emergence of insect pests resistant to existing insecticides in crop production in the fields of agriculture, horticulture and the like.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: August 13, 2019
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Yusuke Sano, Ikki Yonemura, Shunpei Fujie, Akiyuki Suwa
  • Patent number: 10285982
    Abstract: 6-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 6-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: May 14, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10285983
    Abstract: 7-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 7-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: May 14, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10206908
    Abstract: 6-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 6-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: February 19, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10206909
    Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: February 19, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10195185
    Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: February 5, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, Joseph Timothy Marakovits, Venkataiah Bollu, John Hood
  • Patent number: 10188634
    Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: January 29, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, Joseph Timothy Marakovits, Venkataiah Bollu, John Hood
  • Patent number: 10166218
    Abstract: 6-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 6-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: January 1, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10155728
    Abstract: The present invention relates to colchicine-binding site compounds having anti-cancer activity, compositions comprising the same, and their use for treating various forms of cancer.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: December 18, 2018
    Assignees: GTX INC., UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Yan Lu, James T Dalton, Wei Li, Duane D Miller
  • Patent number: 10138237
    Abstract: The present invention relates to novel 1,2,4-triazolo[4,3-a]pyridine compounds as positive allosteric modulators (PAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which mGluR2 subtype of metabotropic receptors is involved.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: November 27, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventor: José Maria Cid-Núñez
  • Patent number: 10104893
    Abstract: Compounds of formula (I) wherein Q is (Q1) or (Q2); and wherein the other substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: April 18, 2016
    Date of Patent: October 23, 2018
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph Marcel Jung, Andrew Edmunds, Michel Muehlebach, Peter Renold, Roger Graham Hall, Jerome Yves Cassayre
  • Patent number: 10087192
    Abstract: The invention relates to novel compounds of the formula (I) in which the R1, R2a, R2b, R3, A1, A2, A3, A4 and n radicals are each as defined above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: October 2, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Ruediger Fischer, David Wilcke, Kerstin Ilg, Ulrich Goergens, Daniela Portz, Sascha Eilmus, Andreas Turberg
  • Patent number: 10053471
    Abstract: The present invention relates to compounds of general formula (I), wherein R1, R2, R3, A1, A2, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: August 21, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf
  • Patent number: 10052331
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 10, 2017
    Date of Patent: August 21, 2018
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10035797
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: July 31, 2018
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Patent number: 10005775
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 12, 2015
    Date of Patent: June 26, 2018
    Assignee: Syngenta Participations, AG
    Inventors: Pierre Joseph Marcel Jung, Andrew Edmunds, Andre Jeanguenat, Michel Muehlebach, Andre Stoller, Daniel Emery, Roger Graham Hall
  • Patent number: 9994565
    Abstract: Compounds of formula (I) defined herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: June 12, 2018
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Carmelida Capaldi, Elisabetta Armani, Andrew Steven Robert Jennings, Christopher Hurley
  • Patent number: 9981915
    Abstract: The present invention relates to colchicine-binding site compounds having anti-cancer activity, compositions comprising the same, and their use for treating various forms of cancer.
    Type: Grant
    Filed: May 5, 2015
    Date of Patent: May 29, 2018
    Assignees: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION, GTx, INC
    Inventors: Yan Lu, James T Dalton, Wei Li, Duane D Miller
  • Patent number: 9980945
    Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: May 29, 2018
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Corey R. Hopkins, Craig W. Lindsley, Colleen M. Niswender, Darren W. Engers, Joe Panarese, Sean Bollinger, Julie Engers
  • Patent number: 9981988
    Abstract: Provided herein are novel polymorphic forms and co-crystals of a compound useful in the treatment, prevention, or amelioration of cancer. In particular, the invention provides polymorphs and co-crystals of 6-{(1R)-1-[8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl}-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, which is an inhibitor of c-Met.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: May 29, 2018
    Assignee: AMGEN INC.
    Inventors: David Bauer, Matthew Bio, Melanie Cooke, Katrina W. Copeland, Matthew Peterson, Michele Potashman, Roman Shimanovich, Helming Tan
  • Patent number: 9951067
    Abstract: A method for producing an optically active ?-trifluoromethyl-?-amino acid derivative, the method including: allowing a compound represented by the following General Formula (1) and a compound represented by the following General Formula (2) to react in the presence of a copper-optically active phosphine complex obtained from a copper compound and an optically active phosphine compound, to thereby obtain an optically active ?-trifluoromethyl-?-amino acid derivative represented by the following General Formula (3):
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: April 24, 2018
    Assignee: Microbial Chemistry Research Foundation
    Inventors: Masakatsu Shibasaki, Naoya Kumagai, Liang Yin
  • Patent number: 9944603
    Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof.
    Type: Grant
    Filed: April 10, 2017
    Date of Patent: April 17, 2018
    Assignee: FLATLEY DISCOVERY LAB, LLC
    Inventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
  • Patent number: 9932336
    Abstract: The present invention relates to an improved process for the preparation of Apixaban and intermediates thereof. Further the present invention also relates to novel intermediate of Formula V and its process for the preparation.
    Type: Grant
    Filed: October 20, 2015
    Date of Patent: April 3, 2018
    Assignee: JUBILANT GENERICS LIMITED
    Inventors: Khushwant Singh, Amit Kumar Srivastava, Ratnakar Tripathi, Jai Prakash Verma, Dharam Vir, Lalit Kumar, Mukesh Masand, Rajendra Singh Shekhawat, Rakesh Tiwari, Sujay Biswas
  • Patent number: 9926315
    Abstract: The invention relates to a compound of Formula I or IA and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: March 27, 2018
    Assignee: Flatley Discovery Lab, LLC
    Inventors: Bridget M. Cole, Richard A. Nugent, Paul T. Smith, Jr.
  • Patent number: 9901571
    Abstract: The present invention relates to novel compounds of a formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, pharmaceutical compositions comprising them and their use in therapy, for example as modulators of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR-1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
    Type: Grant
    Filed: November 2, 2015
    Date of Patent: February 27, 2018
    Assignee: RaQualia Pharma Inc.
    Inventors: Yasuhiro Iwata, Kiyoshi Kawamura, Masaki Sudo, Kaoru Shimada, Shinichi Koizumi, Nobuyuki Takahashi, Keiko Obata, Makiko Kuroda
  • Patent number: 9890163
    Abstract: Protein kinases are regulators of cellular signaling and their functional dysregulation is common in carcinogenesis and many other disease states or disorders. The present invention relates to novel chemical entities that have biological activity to modulate mammalian protein kinase enzymes. In particular, compounds of the invention display potent inhibition of breast tumor related kinase (BRK).
    Type: Grant
    Filed: October 11, 2016
    Date of Patent: February 13, 2018
    Assignee: Princeton Drug Discovery Inc
    Inventors: Kan He, Lining Cai
  • Patent number: 9884825
    Abstract: Compounds having Formula I or II, and methods of making and using thereof, are described herein:
    Type: Grant
    Filed: August 1, 2013
    Date of Patent: February 6, 2018
    Assignees: Georgia State University Research Foundation, Inc., University of Delhi
    Inventors: Diwan S. Rawat, Binghe Wang, Nitin Kumar, Sunny Manohar, Xiaochuan Yang, Guojing Sun, Nanting Ni
  • Patent number: 9845314
    Abstract: The invention relates to new substituted heteroaryls of formula 1 or of formula 1? wherein A is either N or CH, wherein R2 is selected from the group consisting of —C1-3-alkyl, —C1-3-haloalkyl, F, Br, Cl, wherein Y is selected from —O— or —CH2—, and wherein R3 is defined as in claim 1, and the pharmaceutically acceptable salts thereof, and the use of these aforementioned compounds for the treatment of diseases such as asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: December 19, 2017
    Assignee: Boehrnger Ingelheim International GmbH
    Inventors: Matthias Hoffmann, Georg Dahmann, Christian Gnamm, Daniel Fandrick, John Scott, Clive McCarthy
  • Patent number: 9809587
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 18, 2015
    Date of Patent: November 7, 2017
    Assignee: Syngenta Participations AG
    Inventors: Andre Stoller, Andre Jeanguenat, Andrew Edmunds, Pierre Joseph Marcel Jung, Daniel Emery, Michel Muehlebach, Peter Renold
  • Patent number: 9782392
    Abstract: A method for treating rheumatoid arthritis, multiple sclerosis, or a disease involving JAK3, including administering a compound of the formula (I) or a salt thereof to a subject
    Type: Grant
    Filed: January 12, 2017
    Date of Patent: October 10, 2017
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masayuki Nakamura, Hiroyoshi Yamanaka, Kazuaki Shibata, Morihiro Mitsuya, Takafumi Harada
  • Patent number: 9763951
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: September 6, 2016
    Date of Patent: September 19, 2017
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9758521
    Abstract: Compounds of formulae (I), (II), and (III), defined herein, are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: September 12, 2017
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Carmelida Capaldi, Elisabetta Armani, Andrew Steven Robert Jennings, Christopher Hurley
  • Patent number: 9758520
    Abstract: The present invention relates to substituted fused heterocyclic compounds. The substituted fused heterocyclic compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heterocyclic compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: October 3, 2016
    Date of Patent: September 12, 2017
    Assignee: SANOFI
    Inventors: Lothar Schwink, Christian Buning, Heiner Glombik, Matthias Gossel, Dieter Kadereit, Nis Halland, Matthias Lohmann, Christoph Pöverlein, Kurt Ritter
  • Patent number: 9676773
    Abstract: Provided is a novel compound having a selective JAK3-inhibitory effect and also having excellent oral absorbability. Also provided is a pharmaceutical agent, which is based on a JAK3-inhibitory effect and is useful for preventing and/or treating a disease involving the JAK3, and in particular, rheumatoid arthritis or multiple sclerosis. An azaindole derivative having a cycloalkenyl group, which is represented by the following formula (I), or a salt thereof, and a pharmaceutical composition containing the same: where R1 to R4, m and n have the same meanings as those defined in the description.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: June 13, 2017
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masayuki Nakamura, Hiroyoshi Yamanaka, Kazuaki Shibata, Morihiro Mitsuya, Takafumi Harada
  • Patent number: 9675594
    Abstract: The present invention is directed to arylpyrrolopyridine derivatives of Formula A: The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Lewy body dementia, Parkinson's disease or cancer.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: June 13, 2017
    Assignee: H. Lundbeck A/S
    Inventors: Simon Timothy Bedford, I-Jen Chen, Yikang Wang, Douglas Stewart Williamson
  • Patent number: 9643984
    Abstract: Disclosed herein are methods for preparing [1,2,4]triazolo[4,3-a]pyridines, particularly (R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one, and precursors thereof, such as a method comprising reacting (R)—N-(3-fluoro-5-(1methyl-1H-pyrazol-4-yl) pyridin-2-yl)-2-(3-(2-methoxyethoxy)-5-oxo-1,6-naphthyridin-6(5H)yl) propanehydrazide (“HYDZ”): (HYDZ) under conditions sufficient to form (R)-6-(1-(8-fluoro-6-(1-methyl-IH-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (“A”): (A)
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: May 9, 2017
    Assignee: AMGEN INC.
    Inventors: Matthew Bio, Eric Fang, Jacqueline E. Milne, Sean Wiedemann, Ash Wilsily
  • Patent number: 9637483
    Abstract: Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: May 2, 2017
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masato Yoshida, Hiroyuki Nagamiya, Yusuke Ohba, Masaki Seto, Takatoshi Yogo, Satoshi Sasaki, Norihito Tokunaga, Kazuyoshi Aso
  • Patent number: 9617263
    Abstract: The present invention provides a compound of the Formula (I) below: wherein R1 is selected from the group consisting of H, CH3, CN, —CH2CN, —C(CH3)2CN, F, Cl, and Br; R2 is selected from the group consisting of H, —O(C1-C3alkylene)R4, —CH2CN, CN, —OCH3, CF2, —C(CH3)2CN, —C(CH3)2, —S(O)2CH3, —S(O)2NH2, and —OCF2; R3 is selected from the group consisting of H, CH3, and —OCH3; and R4 is selected from the group consisting of H, —C(CH3)2CN, —OCH3, —S(O)2CH3, CN, and —C(CH3)2OH; or a pharmaceutical salt thereof, methods of treating type two diabetes using the compound and a process for preparing the compound.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: April 11, 2017
    Assignee: Eli Lilly and Company
    Inventors: Chafiq Hamdouchi, Pranab Maiti
  • Patent number: 9586958
    Abstract: The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: March 7, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Volker Schulze, Hans-Georg Lerchen, Donald Bierer, Antje Margret Wengner, Gerhard Siemeister, Philip Lienau, Ursula Krenz, Dirk Kosemund, Detlef Stöckigt, Michael Brüning, Ulrich Lücking, Ildikó Terebesi
  • Patent number: 9580421
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Grant
    Filed: November 12, 2015
    Date of Patent: February 28, 2017
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim
  • Patent number: 9573949
    Abstract: Mitogen activated protein kinase (MAPK) inhibitors disclosed herein are useful for the treatment of diseases of the respiratory tract, such as chronic eosinophilic pneumonia, asthma, COPD, adult respiratory distress syndrome (ARDS), exacerbation of airways hyper-reactivity consequent to other drug therapy, and airways disease that is associated with pulmonary hypertension.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: February 21, 2017
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Andrew Peter Cridland, Christopher Hurley
  • Patent number: 9573948
    Abstract: The invention relates to a compound of Formula I or IA and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
    Type: Grant
    Filed: October 6, 2015
    Date of Patent: February 21, 2017
    Assignee: Flatley Discovery Lab
    Inventors: Bridget M. Cole, Richard A. Nugent, Paul T. Smith, Jr.
  • Patent number: 9527846
    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: Grant
    Filed: April 18, 2016
    Date of Patent: December 27, 2016
    Assignee: 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
  • Patent number: 9493487
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: November 15, 2016
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar Kc, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood