Additional Hetero Ring Attached Directly Or Indirectly To The Four-membered Hetero Ring By Nonionic Bonding Patents (Class 514/210.18)
  • Patent number: 10993939
    Abstract: The present disclosure is directed to compositions and methods for treating or preventing vasomotor symptoms such as hot flashes, comprising a Transient Receptor Potential Melastatin 8 (TRPM8) antagonist and administering a TRPM8 antagonist, respectively.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: May 4, 2021
    Assignee: Mitsubishi Tanabe Pharmaceutical Company
    Inventor: Joseph M. Palumbo
  • Patent number: 10975287
    Abstract: Disclosed are compounds having the formula: wherein Ra, R1, R2, R3, R4, R5, R6, R7, and R8, are as defined herein, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: April 13, 2021
    Inventors: Adam Kenneth Charnley, Michael G. Darcy, Jason W. Dodson, Terry V. Hughes, Yue Li, Yiqian Lian, Neysa Nevins, Joshi M. Ramanjulu
  • Patent number: 10935558
    Abstract: Provided are methods of detecting the presence or amount of a vitamin D metabolite in a sample using mass spectrometry. The methods generally directed to ionizing a vitamin D metabolite in a sample and detecting the amount of the ion to determine the presence or amount of the vitamin D metabolite in the sample. Also provided are methods to detect the presence or amount of two or more vitamin D metabolites in a single assay.
    Type: Grant
    Filed: April 22, 2019
    Date of Patent: March 2, 2021
    Assignee: Quest Diagnostics Investments Incorporated
    Inventors: Nigel J. Clarke, Brett Holmquist, Gloria Kwang-Ja Lee, Richard E. Reitz
  • Patent number: 10906924
    Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: February 2, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Martha Alicia De La Rosa, Hongfeng Deng, Ghotas Evindar, Wieslaw Mieczyslaw Kazmierski, John Franklin Miller, Vicente Samano, Yoshiaki Washio, Bing Xia
  • Patent number: 10899737
    Abstract: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: January 26, 2021
    Assignee: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
    Inventors: Cheryl A. Grice, Daniel J. Buzard, Michael B. Shaghafi, Olivia D. Weber
  • Patent number: 10899695
    Abstract: The present invention relates to a process for the manufacturing of 1-aryl-1-trifluoromethylcyclopropanes, which serve as intermediates for the manufacturing of calcium T channel blockers of the general formula (A) which are described in WO 2015/186056.
    Type: Grant
    Filed: February 5, 2018
    Date of Patent: January 26, 2021
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Lee McLaren, Daniel To, David Tovell, Stefan Abele
  • Patent number: 10882830
    Abstract: The present disclosure relates to crystalline form CS3 of ozanimod hydrochloride which can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis and preparation method thereof.
    Type: Grant
    Filed: September 14, 2017
    Date of Patent: January 5, 2021
    Assignee: RECEPTOS LLC
    Inventors: Minhua Chen, Yanfeng Zhang, Xiaoting Zhai, Kaiqiang Yan, Chaohui Yang, Xiaoyu Zhang
  • Patent number: 10874743
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: December 29, 2020
    Assignee: KYMERA THERAPEUTICS, INC.
    Inventors: Nello Mainolfi, Nan Ji, Arthur F. Kluge, Matthew M. Weiss, Yi Zhang
  • Patent number: 10865181
    Abstract: The present technology relates to compounds of any one of Formula I, II, IIa, III, IV, and/or V as described herein and their tautomers and/or pharmaceutically acceptable salts, compositions, and methods of uses thereof.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: December 15, 2020
    Assignees: UNIVERSITY OF KANSAS, Oregon Health & Science University
    Inventors: Sudeshna Roy, Paolo Bernardi, Michael Forte, Frank Schoenen, Justina Sileikyte
  • Patent number: 10857140
    Abstract: Provided herein, inter alia, are methods and compounds of formula (I) for inhibiting K-Ras and for treating cancer.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: December 8, 2020
    Assignees: The Regents of the University of California, Leidos Biomedical Research, Inc.
    Inventors: Frank McCormick, Adam R. Renslo, David Turner, Stephan Gysin, Anna E. Maciag, Oleg Chertov
  • Patent number: 10851053
    Abstract: The invention is directed to substituted pyrrolidine derivatives. Specifically, the invention is directed to compounds according to Formula III: wherein A, B, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, R10, R30, Y1, Y2, z2, z4, z5, and z6 are as defined herein, and salts thereof.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: December 1, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Jeffrey Michael Axten, Mui Cheung, Anthony William Dean, Michael P. DeMartino, Hilary Schenck Eidam, Biswajit Kalita, Raghava Reddy Kethiri, Rajendra Kristam
  • Patent number: 10835536
    Abstract: The problem to be solved by the present invention is to provide an anticancer agent for treating tumors resistant to other antitumor agents that inhibit FGFR, and a method for treating such tumors. The present invention provides an antitumor agent for administration to a tumor patient resistant to an FGFR inhibitor, the antitumor agent comprising a 3,5-disubstituted benzene alkynyl compound represented by Formula (I) below or a salt thereof. The present invention also provides a therapeutic method using the anticancer agent.
    Type: Grant
    Filed: October 2, 2018
    Date of Patent: November 17, 2020
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Hiroshi Sootome
  • Patent number: 10822339
    Abstract: The present invention relates to a pyrrolopyrimidine five-membered azacyclic derivative as a novel JAK kinase inhibitor, and use thereof in a preparation of a pharmaceutical product for preventing and/or treating an indication related to a JAK kinase function. The pyrrolopyrimidine five-membered azacyclic derivative of the invention is an ideal JAK kinase inhibitor with a high potency, and can be used to treat or prevent diseases such as rheumatoid arthritis, polycythemia vera, psoriasis, primary thrombocytosis, myelofibrosis, and the like.
    Type: Grant
    Filed: January 25, 2017
    Date of Patent: November 3, 2020
    Assignees: HANGZHOU HUADONG MEDICINE GROUP BIOPHARMACEUTICAL CO. LTD
    Inventors: Jianming Yin, Yubin Lv, Bangliang Li
  • Patent number: 10815213
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: October 27, 2020
    Assignee: Pfizer Inc.
    Inventors: John Robert Springer, Balekudru Devadas, Danny James Garland, Margaret Lanahan Grapperhaus, Seungil Han, Susan Landis Hockerman, Robert Owen Hughes, Eddine Saiah, Mark Edward Schnute, Shaun Raj Selness, Daniel Patrick Walker, Zhao-Kui Wan, Li Xing, Christoph Wolfgang Zapf, Michelle Ann Schmidt
  • Patent number: 10793544
    Abstract: The present disclosure provides compounds that may be useful for inhibiting Wnt pathway comprising compounds of the formula: (Ia) or (Ib) wherein the variables are as defined herein. In some aspects, the compounds may be used to inhibit the Wnt pathway and used to treat cancer, myocardial infarction, osteopetrosis, or used in the maturation of a precursor cell to a mature cell. Also provided herein in are pharmaceutical compositions of the compounds described herein.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: October 6, 2020
    Inventors: Nageswari Yarravarapu, Chuo Chen, Lawrence Lum, Lin You, Chengwei Zhang, Xiaolei Wang, Lishu Zhang
  • Patent number: 10765676
    Abstract: The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
    Type: Grant
    Filed: April 5, 2019
    Date of Patent: September 8, 2020
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Jun Takeuchi, Satoshi Itadani, Kazuya Hashimura, Masahiro Ikura, Masato Higashino, Tetsuya Yasuhiro, Takeshi Nagaura
  • Patent number: 10745364
    Abstract: The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: August 18, 2020
    Assignees: Lycera Corporation, Merck Sharp & Dohme Corp.
    Inventors: Thomas D. Aicher, Chad A. VanHuis, William D. Thomas, John K. MacLean, Brian M. Andresen, Kenneth J. Barr, Corey E. Bienstock, Neville J. Anthony, Matthew Daniels, Kun Liu, Yuan Liu, Catherine M. White, Blair T. Lapointe, Nunzio Sciammetta, Vladimir Simov
  • Patent number: 10729688
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: March 27, 2019
    Date of Patent: August 4, 2020
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Jorden Kass, Byung-Chul Suh, Hui Cao, Wei Li, Xiaowen Peng, Xuri Gao, Yat Sun Or
  • Patent number: 10724102
    Abstract: Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.
    Type: Grant
    Filed: October 26, 2016
    Date of Patent: July 28, 2020
    Assignees: Loxo Oncology, Inc., Array BioPharma, Inc.
    Inventors: Nisha Nanda, Joshua H. Bilenker, James F. Blake, Gabrielle R. Kolakowski, Barbara J. Brandhuber, Steven W. Andrews
  • Patent number: 10723700
    Abstract: The present disclosure relates to tosylate salts 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the LSD1-associated or mediated diseases such as cancer.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: July 28, 2020
    Assignee: Incyte Corporation
    Inventors: Yongchun Pan, Wayne Han, Ganfeng Cao, Zhongjiang Jia, Jiacheng Zhou
  • Patent number: 10696661
    Abstract: Anti-angiogenic treatments, for example treatment of ocular neovascularization or cancer, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of treating or preventing fibrosis and compounds for use in such methods are described.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: June 30, 2020
    Assignee: Exonate Limited
    Inventors: David Bates, Jonathan Morris, Hamish Toop, Jennifer Batson, Andrew David Morley
  • Patent number: 10683269
    Abstract: The invention relates to novel compounds of formula I which are inhibitors of deubiquitylating enzymes (DUBs) and/or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to methods for the preparation of these compounds and to their use in the treatment of cancer.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: June 16, 2020
    Assignee: MISSION THERAPEUTICS LIMITED
    Inventors: Karl Richard Gibson, Alison Jones, Mark Ian Kemp, Andrew Madin, Martin Lee Stockley, Gavin Alistair Whitlock, Michael D Woodrow, Keith Allan Menear
  • Patent number: 10676472
    Abstract: The invention relates to crystalline salts of a compound having the structure of formula (I), methods for their preparation, and related pharmaceutical compositions comprising the crystalline salt. The invention further relates to methods of treating or preventing cancer or an immunological or neurological disease comprising administering a crystalline salt of the invention.
    Type: Grant
    Filed: June 7, 2019
    Date of Patent: June 9, 2020
    Assignee: Calithera Biosciences, Inc.
    Inventors: Timothy F. Stanton, James J. Springer, Jacqueline N. Williams
  • Patent number: 10662159
    Abstract: Provided herein are compounds and pharmaceutical compositions for selectively inhibiting serine hydrolase a/b-hydrolase domain 6 (ABHD6) and dually inhibiting ABHD6 and monoacylglycerol lipase (MGL). The compounds and pharmaceutical compositions disclosed herein are useful for treating a number of therapeutic conditions related to cannabinergic receptor function such as pain, inflammation, neuropathy, neurodegenerative diseases, anxiety disorders, motor function disorder, metabolic disorder, glaucoma and chemotherapy-induced nausea and vomiting and cancer.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: May 26, 2020
    Assignee: MAKSCIENTIFIC, LLC
    Inventors: Alexandros Makriyannis, Michael Malamas, Manjunath Lamani, Shrouq I. Farah
  • Patent number: 10654837
    Abstract: Potent 5-HT2B antagonist of Formula (A), including stereochemically isomeric forms, and salts, hydrates, solvates thereof and their use wherein R1 to R4 and Ar have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them, alone or in combination with other drugs, in fibrosis and/or cirrhosis prevention or therapy.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: May 19, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Zhao-Kui Wan, Haibing Guo, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
  • Patent number: 10647708
    Abstract: A compound of formula (I) wherein: R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: May 12, 2020
    Assignee: CTXT PTY. LTD
    Inventors: Richard Charles Foitzik, Michelle Ang Camerino, Scott Raymond Walker, H. Rachel Lagiakos
  • Patent number: 10647696
    Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: May 12, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
  • Patent number: 10626112
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: April 21, 2020
    Assignee: EA PHARMA CO., LTD.
    Inventors: Kaori Kobayashi, Tamotsu Suzuki, Tomohiro Fujii, Tatsuya Okuzumi
  • Patent number: 10555941
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: March 14, 2016
    Date of Patent: February 11, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Patent number: 10512638
    Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine 5 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: December 24, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael T. Rudd, David M. Tellers, Jenny Miu-Chun Wai
  • Patent number: 10493074
    Abstract: N-{(R)-1-[8-Chloro-2-(1-oxypyridin-3-yl)-quinolin-3-yl]-2,2,2-trifluoroethyl}-pyrido[3,2-d]pyrimidin-4-ylamine is effective in the treatment and/or prevention of Sjögren's syndrome.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: December 3, 2019
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Rodger Anthony Allen, Francesca Barone, William Anthony Fahy, Saba Nayar
  • Patent number: 10487045
    Abstract: The present invention provides a pharmaceutical composition for treating or preventing a cognitive disease or disorder, containing a compound represented by Formula (I), an enantiomer thereof, a diastereomer thereof, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 26, 2017
    Date of Patent: November 26, 2019
    Assignees: Tohoku University, Brain Innovation Co., Inc.
    Inventors: Shigeki Moriguchi, Koji Fukunaga, Yoshiharu Iwabuchi
  • Patent number: 10487068
    Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, n, A, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: November 26, 2019
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Monique Bodil van Niel, Andrew Cridland, Christopher Hurley, Jonathan Killen, Stuart Ward
  • Patent number: 10463671
    Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents, particularly anticancer agents such as prednisone, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: November 5, 2019
    Assignee: Epizyme, Inc.
    Inventors: Heike Keilhack, Sarah K. Knutson, Kevin W. Kuntz
  • Patent number: 10464956
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Grant
    Filed: February 14, 2019
    Date of Patent: November 5, 2019
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Venkat Rao Gadhachanda, Qiuping Wang, Godwin Pais, Akihiro Hashimoto, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash S. Phadke
  • Patent number: 10457655
    Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: October 29, 2019
    Assignee: FORMA THERAPEUTICS, INC.
    Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E.R. Schiller, Mark J. Tebbe
  • Patent number: 10407445
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: January 27, 2016
    Date of Patent: September 10, 2019
    Assignees: Enanta Pharmaceuticals, Inc., Novartis AG
    Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Xuri Gao, Yat Sun Or, Zachary Kevin Sweeney
  • Patent number: 10392401
    Abstract: The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.
    Type: Grant
    Filed: February 3, 2016
    Date of Patent: August 27, 2019
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jiang Wang, Jian Li, Jia Li, Jingya Li, Shengbin Zhou, Mingbo Su, Hualiang Jiang, Xiaomin Luo, Kaixian Chen
  • Patent number: 10377753
    Abstract: Substituted 4-azaindoles as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.
    Type: Grant
    Filed: March 20, 2018
    Date of Patent: August 13, 2019
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Christa C. Chrovian, Michael A. Letavic, Jason C. Rech, Akinola Soyode-Johnson, Jessica L. Wall
  • Patent number: 10377759
    Abstract: The present invention relates to a compound represented by general formula (I) (wherein, all symbols represent the same meanings as the symbols set forth in the specification), a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug of any of these. Since the compound has a Brk inhibitory activity, the compound is useful as a drug ingredient for the prevention and/or treatment of Brk-related diseases such as cancer, for example.
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: August 13, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shingo Yamamoto, Hiroshi Tokura, Masakuni Kurono, Yoshinori Nomura, Shingo Hotta
  • Patent number: 10370727
    Abstract: Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.
    Type: Grant
    Filed: October 16, 2017
    Date of Patent: August 6, 2019
    Assignees: Loxo Oncology, Inc., Array BioPharma, Inc.
    Inventors: Nisha Nanda, Joshua H. Bilenker, James F. Blake, Gabrielle R. Kolakowski, Barbara J. Brandhuber, Steven W. Andrews
  • Patent number: 10329297
    Abstract: The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of IDO, and for the treatment of IDO-related disorders.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: June 25, 2019
    Assignee: Merck Patent GmbH
    Inventor: Brian A. Sherer
  • Patent number: 10329288
    Abstract: The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: June 25, 2019
    Assignees: Genentech, Inc., Array BioPharma Inc.
    Inventors: Chong Han, Keena Green, Francis Gosselin, Michelangelo Scalone, Paul J. Nichols, Weidong Liu, Keith L. Spencer, Zackary D. Crane, Peter J. Stengel, Sagar Shakya
  • Patent number: 10323019
    Abstract: The present invention provides compounds of the formula below (I?): where R, and R1-R3 are as described herein, methods of treating patients for certain types of autoimmune diseases and cancer, and processes for preparing the compounds.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: June 18, 2019
    Assignee: Eli Lilly and Company
    Inventors: Jolie Anne Bastian, Joshua Ryan Clayton, David Andrew Coates, Daniel Jon Sall, Timothy Andrew Woods
  • Patent number: 10316030
    Abstract: The invention relates to crystalline salts of a heterocyclic compound, methods of their preparation, and related pharmaceutical preparations thereof. The invention further relates to methods of treatment using the crystalline salts of the invention.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: June 11, 2019
    Assignee: Calithera Biosciences, Inc.
    Inventors: Timothy F. Stanton, James J. Springer, Jacqueline N. Williams
  • Patent number: 10314844
    Abstract: Inhibitors for Bruton's Tyrosine Kinase (BTK) are disclosed as are compositions thereof, methods for their preparation, and methods for their use.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: June 11, 2019
    Assignees: GILEAD SCIENCES, INC., ONO PHARMACEUTICAL CO., LTD.
    Inventors: Seung H. Lee, Shingo Yamamoto
  • Patent number: 10301318
    Abstract: The invention described herein relates generally to neuroactive compounds and compositions for the treatment psychotic disorders, methods for treating psychosis using these neuroactive compounds, and methods for screening for novel neuroactive compounds. Certain aspects are directed to a family of compounds called “finazines.” Certain aspects are directed to in vivo screening methods using high-through-put behavioral assays in zebrafish.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: May 28, 2019
    Assignee: The General Hospital Corporation
    Inventors: Randall T. Peterson, Andrew J. Rennekamp, David Kokel, You Wang
  • Patent number: 10294202
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof: wherein R1, R2, R3, R4, R5, R6, Q1, Q2, Y1, and Y2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: May 21, 2019
    Assignee: FMC CORPORATION
    Inventors: Andrew Duncan Satterfield, Thomas Paul Selby, David Andrew Travis, Kanu Maganbhai Patel, Andrew Edmund Taggi
  • Patent number: 10294223
    Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: May 21, 2019
    Assignee: PRINCIPIA BIOPHARMA, INC.
    Inventors: Erik Verner, Kenneth Albert Brameld
  • Patent number: 10287295
    Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
    Type: Grant
    Filed: January 2, 2018
    Date of Patent: May 14, 2019
    Assignees: Rigel Pharmaceuticals, Inc., Bristol-Meyers Squibb Company
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Padmakar Darne, Hasibur Rahaman, Jayakumar Sankara Warrier