Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond Patents (Class 514/275)
  • Patent number: 10730859
    Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: August 4, 2020
    Assignee: Laurus Labs Limited
    Inventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Sunil Kumar Indukuri, Sanjay Kumar Dehury, Nagaraju Mekala, Jahangeer Baba Shaik, Durga Prasad Kuchipudi
  • Patent number: 10722512
    Abstract: The invention relates to combinations comprising an HDAC inhibitor and a Her2 inhibitor for the treatment of breast cancer in a subject in need thereof. The invention also relates to combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of breast cancer in a subject in need thereof. Also provided herein are methods for treating breast cancer in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations. Further provided are methods for inhibiting migration and/or invasion of a breast cancer cell in a subject by administering to the subject a HDAC6 specific inhibitor.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: July 28, 2020
    Assignee: Acetylon Pharmaceuticals, Inc.
    Inventors: David Lee Tamang, Min Yang, Simon S. Jones
  • Patent number: 10717725
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: December 6, 2018
    Date of Patent: July 21, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Elizabeth Anne Jurica, Zhenqiu Hong
  • Patent number: 10710983
    Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 ?M to 3.7 ?M; a TAK1 IC50 of from 0.008 ?M to 132 ?M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
    Type: Grant
    Filed: June 26, 2017
    Date of Patent: July 14, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Patent number: 10709705
    Abstract: The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, and R7 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to inhibition of ALK such as cancer.
    Type: Grant
    Filed: August 28, 2017
    Date of Patent: July 14, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Jianyong Chen
  • Patent number: 10710979
    Abstract: The present invention provides an EGFR kinase inhibitor and a preparation method and use thereof. Specifically, the present invention provides a compound as shown in formula (I), the definition of each group therein being as described in the description. Said compound is an efficient EGFR inhibitor.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: July 14, 2020
    Assignee: ZHEJIANG BOSSAN PHARMACEUTICAL CO. LTD.
    Inventors: Dawei Ma, Qiang Yu, Junying Yuan, Hongguang Xia, Dongpo Cai, Kailiang Wang, Chen Zhang, Shanghua Xia
  • Patent number: 10702527
    Abstract: The present disclosure provides combination therapy of a transcription inhibitor and a kinase inhibitor. The combination of the transcription inhibitor and the kinase inhibitor may be useful in treating and/or preventing in a subject a proliferative disease, such as proliferative a disease that is resistant to the transcription inhibitor alone or the kinase inhibitor alone. In certain embodiments, the proliferative disease is a cancer. The combination of the transcription inhibitor and the kinase inhibitor is expected to be synergistic.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: July 7, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Peter Hammerman, Kwok-kin Wong, Nathanael S. Gray
  • Patent number: 10682352
    Abstract: Provided in the present invention are a compound having the effects of preventing and treating diseases related to IDH mutation, and a preparation method and use thereof.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: June 16, 2020
    Assignees: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Lei Jiang, Meiyu Geng, Qiangang Zheng, Min Huang, Huixin Wan, Shuai Tang, Xianlei Fu, Xiaojing Lan, Jianhua Cao, Feifei Liu, Jian Ding
  • Patent number: 10662186
    Abstract: The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.
    Type: Grant
    Filed: December 30, 2016
    Date of Patent: May 26, 2020
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Qian Wang, Chen Shi, Xiong Zhai, Hui Ge, Xuemei Liao, Yu Mao, Zhixiong Xiang, Yanan Han, Guoyong Huo, Yanjun Liu
  • Patent number: 10647686
    Abstract: The present invention relates to compounds represented by Formula 1 or a pharmaceutically acceptable salt thereof, wherein: R1 is chloro or methyl; R2 is hydrogen or chloro; R3 is hydrogen, fluoro, chloro, bromo, methyl, ethyl, isopropyl, pentyl, hexyl, octyl, methoxy, phenoxy, (4-nitrophenyl)sulfonyl, piperidin-4-yl, or piperazin-1-yl; R4 is hydrogen, chloro, methyl or trifluoromethyl, phenoxy, (4-nitrophenyl)sulfonyl or piperidin-4-yl; or R3 and R4, together with the carbons to which they are attached, form a fused ring selected form the group consisting of: n is 1 or 2. These compounds according to the present invention remarkably inhibits activity of DRAK that inhibits signal systems of TGF-?, which is known to suppress cancer growth, and thus the novel pyrimidine compounds can be used as a pharmaceutical composition for preventing or treating cancer and can be used as a pharmaceutical composition for preventing or treating inflammatory disease.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: May 12, 2020
    Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Kwangho Lee, Gildon Choi, Na Ri Lee, Sang Jun Park, Myoung Eun Jung, Seong Jin Kim, Kyung-Min Yang, Jihee Lee
  • Patent number: 10632120
    Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
    Type: Grant
    Filed: August 26, 2019
    Date of Patent: April 28, 2020
    Assignee: Emory University
    Inventors: Michael G. Natchus, Richard Arrendale, Dennis Liotta, Ketan Desai, Hyunsuk Shim
  • Patent number: 10632192
    Abstract: The present invention provides a compound of the formula (1): wherein X, R1, R2, R3, R4, R5, R6, Y1, Y2, L, and m are as defined in the description, and a pharmaceutically acceptable salt thereof, which are useful as a vaccine adjuvant.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: April 28, 2020
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Hidenori Kimura, Hitoshi Ban, Yoshiaki Isobe, Hitoshi Watanabe
  • Patent number: 10633413
    Abstract: This invention relates to methods of stimulating the activity of the human and animal enteric nervous system. The method comprises orally administering an aminosterol, such as squalamine, a naturally occurring aminosterol isolated from Squalus acanthias, or derivatives thereof, to a subject in need.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: April 28, 2020
    Assignee: ENTERIN, INC.
    Inventor: Michael Zasloff
  • Patent number: 10618887
    Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: March 5, 2018
    Date of Patent: April 14, 2020
    Assignees: Sunesis Pharmaceuticals, Inc., Biogen MA Inc.
    Inventors: Brian T. Hopkins, Timothy R. Chan, Tracy J. Jenkins, Patrick Conlon, Xiongwei Cai, Michael Humora, Xianglin Shi, Ross A. Miller, Andrew Thompson
  • Patent number: 10570122
    Abstract: The present invention relates to compounds of general formula (I). wherein A represents an optionally substituted heterocycle group, B represents an aryl or heteroaryl group and wherein X, R1, R2, R3, R4 and R5 are as defined in the description. Compounds of formula (I) are useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: February 25, 2020
    Assignee: AB Science
    Inventors: Alain Moussy, Abdellah Benjahad, Didier Pez, Franck Sandrinelli, Jason Martin, Willy Picoul, Emmanuel Chevenier
  • Patent number: 10562894
    Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
    Type: Grant
    Filed: April 22, 2019
    Date of Patent: February 18, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Jennifer Kozak, Ryan Hudson, Gary E. L. Brandt, Robert Murray McKinnell
  • Patent number: 10537574
    Abstract: This disclosure relates to the use of kinase inhibitor to treat or prevent infectious diseases such as tuberculosis. In certain embodiments, this disclosure relates to treating or preventing an infectious disease comprising administering an effective amount of a kinase inhibitor or other compound disclosed herein to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating or preventing tuberculosis comprising administering a kinase inhibitor to a subject in need thereof. In certain embodiments, the subject is diagnosed with Mycobacterium tuberculosis (Mtb) that is resistant to multiple antibiotic agents.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: January 21, 2020
    Assignee: Emory University
    Inventor: Daniel Kalman
  • Patent number: 10526345
    Abstract: The present invention relates to novel compounds of formula (I) as GPR119 agonist, composition compositions containing such compounds and method of preparation thereof.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: January 7, 2020
    Assignee: MANKIND PHARMA LTD.
    Inventors: Rakesh Ishwar Patil, Jeevan Verma, Dharmesh Shah, Sazid Ali, Srinivasa Reddy Bapuram, Santosh Kumar Rai, Anil Kumar
  • Patent number: 10527633
    Abstract: Use of prostacyclin or an analogue thereof for treatment of a new medical indication in acute critically ill patients, in particular acute critically ill patients with systemic endothelial damage, a biomarker for identifying individuals that have a new medical indication, and a method for identifying a new medical indication.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: January 7, 2020
    Assignee: ENDOTHEL PHARMA APS
    Inventors: Sisse Rye Ostrowski, Pär Ingemar Johansson
  • Patent number: 10519169
    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: December 31, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10519107
    Abstract: The present disclosure relates to compounds having the Formula (Formula (I)) which are inhibitors of STAT5.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: December 31, 2019
    Assignee: The Governing Council of the University of Toronto
    Inventors: Patrick Thomas Gunning, Abbarna A. Cumaraswamy, Andrew Martin Lewis, Mulu Geletu-Heye
  • Patent number: 10519135
    Abstract: The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: December 31, 2019
    Assignee: Syros Pharmaceuticals, Inc.
    Inventors: Kevin Sprott, Jason J. Marineau, Darby Schmidt, Michael Bradley, Stephane Ciblat, M. Arshad Siddiqui, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Stephanie Roy, Dana K. Winter, Tom Miller, Amy Ripka, Dansu Li
  • Patent number: 10501461
    Abstract: Tyrosine amide compounds of formula I described herein inhibit Rho Kinase and may be used for the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Type: Grant
    Filed: January 30, 2018
    Date of Patent: December 10, 2019
    Assignee: CHIESI FARMACEUTICI S.P.A.
    Inventors: Alessandro Accetta, Fabio Rancati, Anna Maria Capelli, David Edward Clark, Patrizia Tisselli, Christine Edwards, Gurdip Bhalay, Arnaud Jean Francois Auguste Cheguillaume
  • Patent number: 10494378
    Abstract: Disclosed area fused ring pyrimidine compound, and an intermediate, a preparation method, a composition and a use thereof. The fused ring pyrimidine compound is a compound as shown in formula I, a tautomer, an enantiomer, a diastereoisomer, a pharmaceutically acceptable salt, a metabolite, a metabolic precursor or a prodrug thereof, wherein the above-mentioned compound is used for the preparation of a medicine for preventing, remitting or treating one or more of immune system diseases, autoimmune diseases, cell proliferative diseases, allergic disorders and cardiovascular diseases, and the compound has a strong inhibitory effect on the Janues kinase, FGFR kinase, FLT3 kinase and Src family kinase.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: December 3, 2019
    Assignee: GUANGZHOU MAXINOVEL PHARMACEUTICALS CO., LTD.
    Inventors: Zusheng Xu, Nong Zhang, Tinghan Wang, Qingrui Sun, Yuguang Wang
  • Patent number: 10479785
    Abstract: A novel class of inhibitors of protein kinases that are useful in the treatment of cell proliferative diseases and conditions, and especially those characterised by over-expression of CDK4, CDK6 and/or cyclin D, including certain cancers of lung, breast, brain, central nervous system, colorectal cancer and leukaemias.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: November 19, 2019
    Assignee: AUCENTRA THERAPEUTICS PTY LTD
    Inventors: Shudong Wang, Solomon Tadesse Zeleke, Mingfeng Yu
  • Patent number: 10463641
    Abstract: The disclosure includes a method of inducing direct reprogramming (transdifferentiation) into non-oncogenic cells accompanied by tumor cell apoptosis in human tumor cells using a small molecule composition, based on the mechanism of chemical-induction of direct cellular reprogramming. The disclosure also includes a small molecule composition used for the method, and culture media and agents prepared from the composition.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: November 5, 2019
    Assignee: Transcend Cytotherapy Co., Ltd
    Inventors: Pei-Lin Zhang, Hong-Yang Wang
  • Patent number: 10464927
    Abstract: The present disclosure relates to a 2,4-disubstituted pyrimidine derivative and the use thereof as a therapeutically effective cyclin-dependent kinase (CDK) inhibitor. In particular, the present disclosure relates to the use of a new 2,4-disubstituted pyrimidine derivatives shown in formula (I) and a pharmaceutical composition thereof as a selective CDK4/6 inhibitor in preventing or treating diseases related to CDK4/6.
    Type: Grant
    Filed: October 9, 2018
    Date of Patent: November 5, 2019
    Assignee: Shanghai Xunhe Pharmaceutical Technology Co. Ltd.
    Inventors: Yongyong Zheng, Hua Jin, Feng Zhou, Meihua Huang, Xin Meng
  • Patent number: 10428062
    Abstract: The present invention relates to novel geminal substituted aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of ?7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: October 1, 2019
    Assignee: Axovant Sciences GmbH
    Inventors: Raksha Acharya, Duane A. Burnett, Matthew Gregory Bursavich, Andrew Simon Cook, Bryce Alden Harrison, Andrew J. McRiner
  • Patent number: 10420761
    Abstract: The current invention is directed to a class of compounds that inhibit the function of Thymidylate synthase. Thymidylate synthase inhibition was noted to result in inhibition of tumor cell grow and killing of tumor cells. Thymidylate synthase inhibition is, thus, useful for treatment of various types of cancers, including but not limited to, acute lymphoblatic leukemia (ALL), acute myelogenous leukemia (AML), acute promyelocytic leukemia, chronic lymphocytic leukemia (CLL), chronic myelogenous leukemia (CML), acute monocytic leukemia (AMOL), hairy cell leukemia, large cell immunoblastic lymphoma, plasmacytoma, multiple myeloma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, leukemia, brain cancer, lung cancer, central nervous system (CNS) cancer, melanoma, renal cancer, prostate cancer, colon cancer, ovarian cancer and breast cancer. The compounds disclosed herein can be used alone or in combination with other cancer treatment regimens (e.g.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: September 24, 2019
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Maria Zajac-Kaye, Lidia Kulemina
  • Patent number: 10385342
    Abstract: The present invention relates to oligomeric compounds and conjugates thereof that target Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) PCSK9 mRNA in a cell, leading to reduced expression of PCSK9. Reduction of PCSK9 expression is beneficial for a range of medical disorders, such as hypercholesterolemia and related disorders.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: August 20, 2019
    Assignee: ROCHE INNOVATION CENTER COPENHAGEN A/S
    Inventors: Nanna Albæk, Maj Hedtjärn, Marie Wickstrom Lindholm, Niels Fisker Nielsen, Andreas Petri, Jacob Ravn
  • Patent number: 10369129
    Abstract: Disclosed herein is a long acting pharmaceutical composition for treating or preventing human immunodeficiency virus (HIV) infection. The pharmaceutical composition comprises a suspension of a lysine-based aspartyl protease inhibitor or salt thereof, a surface modifier, and a pharmaceutically acceptable carrier; wherein the lysine-based aspartyl protease inhibitor or salt thereof has an average effective particle size of less than about 500 nm. A method for treating or preventing HIV infection with the pharmaceutical composition is also disclosed.
    Type: Grant
    Filed: May 31, 2016
    Date of Patent: August 6, 2019
    Assignee: TaiMed Biologics, Inc.
    Inventors: James Nienyuan Chang, Hsiang-Fa Liang, Meng-Hsin Chen, Kuei-Ling Kuo, An-Chieh Li
  • Patent number: 10370341
    Abstract: The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: August 6, 2019
    Assignee: NEOCULI PTY LTD
    Inventors: Stephen Page, Sanjay Garg, Martine Keenan, Adam McCluskey, Andrew Stevens
  • Patent number: 10363255
    Abstract: The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and/or an amorphous form.
    Type: Grant
    Filed: January 25, 2018
    Date of Patent: July 30, 2019
    Assignee: FORSIGHT VISION4, INC.
    Inventors: Judit Horvath, Irina Astafieva, Signe Erickson, Kathleen Cogan Farinas
  • Patent number: 10350195
    Abstract: Compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, disclosed are combined therapies that modulate synapse function for treating the disease.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: July 16, 2019
    Assignee: Pharnext
    Inventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko, Nathalie Cholet
  • Patent number: 10351560
    Abstract: The invention relates to a crystalline form of (S)-2-(8-((5-chloropyrimidin-2-yl)(methyl)amino)-2-fluoro-6,7,8,9-tetrahydro-5H-pyrido[3,2-b]indol-5-yl)acetic acid, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as a medicament, especially as CRTH2 receptor modulators.
    Type: Grant
    Filed: September 14, 2016
    Date of Patent: July 16, 2019
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Hamed Aissaoui, Christoph Boss, Patrick Bouis, Julien Hazemann, Romain Siegrist, Markus Von Raumer
  • Patent number: 10342766
    Abstract: Derivatives of 6-shogaol are described herein. Also described herein are methods of preparing the derivatives, as well as methods of using the derivatives to activate Nrf2 and to treat diseases associated with inflammation and/or oxidative stress.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: July 9, 2019
    Assignees: North Carolina Agricultural and Technical State University, North Carolina Central University
    Inventors: Shengmin Sang, Yingdong Zhu, TinChung Leung
  • Patent number: 10329261
    Abstract: A method of preparing 6-chloro-5-nitro-2,4-diaminopyrimidine includes: reacting guanidine hydrochloride with ethyl carbamoylacetate and sodium hypochlorite in the presence of a metal nitrate salt and acetate anhydride in an organic solvent.
    Type: Grant
    Filed: July 18, 2018
    Date of Patent: June 25, 2019
    Assignee: XI'AN TAIKOMED PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Yonghong Tang, Minghui Chang, Chengyuan Liang, Danni Tian, Juan Xia, Kaiqi Shi, Han Li, Xuechuan Wang
  • Patent number: 10329278
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where X1; X2; R1 and R4 are as defined herein.
    Type: Grant
    Filed: June 18, 2018
    Date of Patent: June 25, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Benjamin Gerald Tehan, Barry John Teobald
  • Patent number: 10308646
    Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
    Type: Grant
    Filed: October 26, 2018
    Date of Patent: June 4, 2019
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Jennifer Kozak, Ryan Hudson, Gary E. L. Brandt, Robert Murray McKinnell, Marta Dabros, Jerry Nzerem
  • Patent number: 10301260
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: May 28, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiang-Yang Ye, Bruce A. Ellsworth, Elizabeth A. Jurica
  • Patent number: 10287253
    Abstract: The present disclosure relates to a class of pyrimidine derivatives having immunomodulating properties that act via TLR7 which are useful in the treatment of viral infections and cancers.
    Type: Grant
    Filed: December 4, 2017
    Date of Patent: May 14, 2019
    Assignee: APROS THERAPEUTICS, INC.
    Inventor: Tom Yao-Hsiang Wu
  • Patent number: 10280154
    Abstract: Provided are a pyrimidine compound represented by Formula 1, a method of preparing the same, and a pharmaceutical use of the pyrimidine compound for the prevention or treatment of cancer.
    Type: Grant
    Filed: September 11, 2018
    Date of Patent: May 7, 2019
    Assignee: HANMI PHARM. CO., LTD.
    Inventors: Young Jin Ham, Seok Jong Kang, Jae Yul Choi, Seo Hee Kim, Tae Woo Kim, In Hwan Bae, Young Gil Ahn, Kwee Hyun Suh
  • Patent number: 10272084
    Abstract: Disclosed are methods for treating cisplatin-induced peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a histone deacetylase 6 selective inhibitor.
    Type: Grant
    Filed: June 1, 2016
    Date of Patent: April 30, 2019
    Assignees: Regenacy Pharmaceuticals, LLC, Board of Regents, The University of Texas System
    Inventors: Annemieke Kavelaars, Cobi J. Heijnen, Karen Krukowski, Matthew B. Jarpe
  • Patent number: 10266521
    Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: April 23, 2019
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Minxiong Li, Xiaobo Li, Wuhong Chen, Tao Zhang, Haiyang Hu, Weilong Dai, Yanjun Wu
  • Patent number: 10233178
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
    Type: Grant
    Filed: June 15, 2017
    Date of Patent: March 19, 2019
    Assignee: Oryzon Genomics, S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez De La Cuesta, Maria de los Ángeles Estiarte Martinez
  • Patent number: 10213511
    Abstract: The present invention relates to compositions and methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: February 26, 2019
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Will McLean, Megan Harrison, Michael R. Jirousek
  • Patent number: 10201540
    Abstract: The present invention relates to compositions and methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: February 12, 2019
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Will McLean, Megan Harrison, Michael R. Jirousek
  • Patent number: 10189833
    Abstract: Solid forms of the compound, [5-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(6-trifluoromethyl-pyridin-3-ylmethyl)-amine HCl salt (Compound I) and its free base, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3, were prepared and characterized: Also provided are methods of using the solid forms.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: January 29, 2019
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Gary Conard Visor
  • Patent number: 10150743
    Abstract: The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.
    Type: Grant
    Filed: May 11, 2016
    Date of Patent: December 11, 2018
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Seiji Hori, Futoshi Hasegawa, Daisuke Urabe, Hirotaka Kurebayashi
  • Patent number: 10131639
    Abstract: Provided are pharmaceutical compositions and dosage forms of 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, or a pharmaceutically acceptable stereoisomer, tautomer, solid form, polymorph, salt, hydrate, clathrate, or solvate thereof. Also provided are methods of treating, managing, or preventing various disorders, such as diseases or disorders treatable or preventable by inhibition of a JNK pathway in mammals using such pharmaceutical compositions or dosage forms. Further provided are salts of 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide and methods of preparation of such salts.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: November 20, 2018
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Nathan Andrew Boersen, Indrajit Ghosh, Lianfeng Huang, Daozhong Zou