Additional Hetero Ring Attached Directly Or Indirectly To The Four-membered Hetero Ring By Nonionic Bonding Patents (Class 514/210.18)
  • Patent number: 11365189
    Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of HER2 or EGFR for the treatment or prevention of disease, including cancer.
    Type: Grant
    Filed: April 24, 2020
    Date of Patent: June 21, 2022
    Assignee: Board of Regents, The University of Texas System
    Inventors: John Heymach, Jacqulyne Robichaux, Monique Nilsson, Philip Jones, Jason Cross, Jay Theroff
  • Patent number: 11359037
    Abstract: The present invention relates to a modifier represented by Formula 1, a method of preparing the same, a modified conjugated diene-based polymer having a high modification ratio which includes a modifier-derived functional group, and a method of preparing the polymer.
    Type: Grant
    Filed: August 14, 2020
    Date of Patent: June 14, 2022
    Inventors: Seung Ho Choi, Dae June Joe, Won Taeck Lim, Won Mun Choi
  • Patent number: 11345702
    Abstract: Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.
    Type: Grant
    Filed: September 24, 2021
    Date of Patent: May 31, 2022
    Assignee: MYOFORTE THERAPEUTICS, INC.
    Inventors: Roopa Rai, Robert Booth, Michael J. Green
  • Patent number: 11318205
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 16, 2020
    Date of Patent: May 3, 2022
    Assignee: KYMERA THERAPEUTICS, INC.
    Inventors: Nello Mainolfi, Nan Ji, Arthur F. Fluge, Matthew M. Weiss, Yi Zhang
  • Patent number: 11304947
    Abstract: The present invention provides methods and compositions for treating and preventing lung injuries due to or associated with coronavirus infections that cause Severe Acute Respiratory Syndrome, including COVID-19. More specifically the present invention provides methods for treating or preventing the lung injuries associated with SARS-CoV-2 infections, such as acute lung injury (ALI), lung fibrosis, and acute respiratory distress syndrome (ARDS). The methods comprise administering a therapeutically effective amount of a pharmaceutical composition comprising a protein kinase inhibitor compound having MAP3K2/MAP3K3 inhibition activity, such as pazopanib or nintedanib, or a pharmaceutically acceptable salt, solvate, or prodrug thereof, to a patient in need thereof. The present invention also provides devices for administering the compositions.
    Type: Grant
    Filed: May 20, 2021
    Date of Patent: April 19, 2022
    Assignees: Qx Therapeutics Inc., Yale University
    Inventors: Dianqing Wu, Ho Yin Lo
  • Patent number: 11278526
    Abstract: Methods for treatment of systemic lupus erythematosus (SLE” or “Lupus”) by administration of a modulator of sphingosine-1-phosphate receptor subtype 1 (S1P1), as well as compositions and methods related to the same, wherein such S1P1 modulators have the following general structure and wherein X and Y are as defined herein.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: March 22, 2022
    Assignee: RECEPTOS LLC
    Inventors: Fiona Lorraine Scott, Kristen R. Taylor Meadows, Robert Peach
  • Patent number: 11267825
    Abstract: The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: March 8, 2022
    Assignee: AICURIS GMBH & CO. KG
    Inventors: Alastair Donald, Andreas Urban, Susanne Bonsmann, Anita Wegert, Christiaan Gremmen, Jasper Springer
  • Patent number: 11261184
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R5, A and q have the meanings given in the claims and specification, their use as inhibitors of CDK8/19, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: March 1, 2022
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Heribert Arnhof, Sebastian Carotta, Marco Hofmann, Marc Kerenyi, Dirk Scharn
  • Patent number: 11236088
    Abstract: This invention relates to heterocyclic compounds and their use in medicine. In particular, the present invention discloses heterocyclic compound of formula I, or an isotopically labeled compound thereof, or an optical isomer thereof, a geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. The invention also relates to the use of these compounds in medicine.
    Type: Grant
    Filed: November 13, 2018
    Date of Patent: February 1, 2022
    Assignee: KIND PHARMACEUTICAL
    Inventor: Dong Liu
  • Patent number: 11236086
    Abstract: Described herein are compounds that inhibit ALK2 and its mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: February 1, 2022
    Assignee: Blueprint Medicines Corporation
    Inventors: Jason D. Brubaker, Paul E. Fleming, Joseph L. Kim, Brett Williams, Brian L. Hodous
  • Patent number: 11203586
    Abstract: An iridinesulfonamide compound having isocitrate dehydrogenase 1 (IDH1) inhibitory activity, pharmaceutically acceptable salts, solvates or hydrates thereof, a pharmaceutical composition, as well as use of the compound or the pharmaceutically acceptable salts, solvates or hydrates thereof, and the pharmaceutical composition thereof in treating IDH1 mutation induced cancer.
    Type: Grant
    Filed: March 22, 2017
    Date of Patent: December 21, 2021
    Assignees: Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Lianyungang Runzhong Pharmaceutical Co., Ltd., Centaurus Biopharma Co., Ltd.
    Inventors: Li Zhu, Yanqing Yang, Liguang Dai, Xiaowei Duan, Zhao Yang, Hui Zhang, Yuandong Hu, Yong Peng, Yongxin Han, Rui Zhao, Xin Tian, Shanchun Wang
  • Patent number: 11191732
    Abstract: Currently available glutaminase inhibitors are generally poorly soluble, metabolically unstable, and/or require high doses, which together reduce their efficacy and therapeutic index. These can be formulated into nanoparticles and delivered safely and effectively for treatment of pancreatic cancer and other glutamine addicted cancers. Studies demonstrate that nanoparticle delivery of BPTES, relative to use of BPTES alone, can be safely administered and provides dramatically improved tumor drug exposure, resulting in greater efficacy. GLS inhibitors can be administered in higher concentrations with sub-100 nm nanoparticles, since the nanoparticles package the drug into “soluble” colloidal nanoparticles, and the nanoparticles deliver higher drug exposure selectively to the tumors due to the enhanced permeability and retention (EPR) effect. These factors result in sustained drug levels above the IC50 within the tumors for days, providing significantly enhanced efficacy compared to unencapsulated drug.
    Type: Grant
    Filed: April 20, 2020
    Date of Patent: December 7, 2021
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Barbara S. Slusher, Anne Le, Takashi Tsukamoto
  • Patent number: 11186554
    Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: November 30, 2021
    Assignee: VIVACE THERAPEUTICS, INC.
    Inventors: Andrei W. Konradi, Tracy Tzu-Ling Tang Lin
  • Patent number: 11168086
    Abstract: The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R4 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: November 9, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Taishan Hu, Xingchun Han, Buyu Kou, Hong Shen, Shixiang Yan, Zhisen Zhang
  • Patent number: 11111223
    Abstract: The present disclosure is directed to novel crystalline forms of ozanimod and ozanimod hydrochloride, as well as preparation method thereof. Said crystalline forms of ozanimod and ozanimod hydrochloride can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis. The crystalline forms of the present disclosure have one or more advantages in solubility, melting point, stability, dissolution, bioavailability and processability and provide new and better choices for the preparation of ozanimod drug product, and are very valuable for drug development.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: September 7, 2021
    Assignee: RECEPTOS LLC
    Inventors: Minhua Chen, Yanfeng Zhang, Xiaoting Zhai, Kaiqiang Yan, Chaohui Yang, Xiaoyu Zhang
  • Patent number: 11103508
    Abstract: In one aspect, compounds and compositions that inhibit TXNIP expression and/or that lower hepatic glucose production and methods of identifying, making, and using same are disclosed. The disclosed compounds and compositions can be useful for disorders associated with elevated TXNIP and/or elevated glucagon levels such as, for example, diabetes and associated disorders. Further provided are methods for treating hyperlipidemia or fatty liver disease, optionally associated with elevated TXNIP and/or elevated glucagon levels.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: August 31, 2021
    Assignees: SOUTHERN RESEARCH INSTITUTE, THE UAB RESEARCH FOUNDATION
    Inventors: Corinne E. Augelli-Szafran, Omar Moukha-Chafiq, Mark J. Suto, Anath Shalev, Lance Thielen, Junqin Chen, Gu Jing
  • Patent number: 11098368
    Abstract: Novel ALK and NTRK1 fusion molecules and uses are disclosed.
    Type: Grant
    Filed: May 14, 2018
    Date of Patent: August 24, 2021
    Assignee: FOUNDATION MEDICINE, INC.
    Inventors: Maureen T. Cronin, Doron Lipson, Roman Yelensky
  • Patent number: 11087354
    Abstract: The present invention relates generally to the fields of molecular biology and growth factor regulation. More specifically, the invention relates to therapies for the treatment of pathological conditions, such as cancer.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: August 10, 2021
    Assignee: Genentech, Inc.
    Inventors: Gordon Bray, Iris Chan
  • Patent number: 11084780
    Abstract: The present disclosure relates to a) crystalline forms of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising one or more crystalline forms of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, one or more pharmaceutically acceptable carriers; c) methods of treating a tumor a cancer, or a Rasopathy disorder by administering one or more crystalline forms of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof, and methods of producing essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide.
    Type: Grant
    Filed: February 17, 2021
    Date of Patent: August 10, 2021
    Assignee: SpringWorks Therapeutics, Inc.
    Inventors: Kristin Patterson, Jiping Liu, Ricky Wayne Couch, Peter Gregory Varlashkin, Mai Li, Yonghong Gan
  • Patent number: 11066358
    Abstract: The present disclosure relates to: a) a crystalline composition of essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising the crystalline composition of essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, a pharmaceutically acceptable carrier; and c) methods of treating a tumor, a cancer, or a Rasopathy disorder by administering the crystalline composition of essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof.
    Type: Grant
    Filed: February 17, 2021
    Date of Patent: July 20, 2021
    Assignee: WARNER-LAMBERT COMPANY LLC
    Inventor: Erwin Irdam
  • Patent number: 11053260
    Abstract: Disclosed in the present invention are a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt, and applications thereof in the preparation of drugs for treating HBV-related diseases.
    Type: Grant
    Filed: February 9, 2018
    Date of Patent: July 6, 2021
    Assignee: FUJIAN COSUNTER PHARMACEUTICAL CO., LTD.
    Inventors: Haiying He, Jing Wang, Zhigan Jiang, Yaxun Yang, Peng Shao, Chen Zhang, Jian Li, Shuhui Chen
  • 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: 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: 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: 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