Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
  • Patent number: 11365190
    Abstract: Disclosed are compounds having the formula: wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Grant
    Filed: January 25, 2021
    Date of Patent: June 21, 2022
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Adam Kenneth Charnley, Gren Z. Wang, Joseph J. Romano
  • Patent number: 11279690
    Abstract: The invention relates to a compound of formula (I): Formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein A is heteraryl selected from 1H-benzimidazolyl and imidazo[1,2-a]pyridine, and R1, R2, R3, R4 and R5 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5) and its isoenzyme glutaminyl-peptide cyclotransferase-like protein (QPCTL). QC and QPCTL catalyze the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: September 20, 2018
    Date of Patent: March 22, 2022
    Inventors: Ulrich Heiser, Robert Sommer
  • Patent number: 11266633
    Abstract: The present invention describes the combination of a NK1-antagonist with pramipexole or a pharmaceutically acceptable salt or solvate thereof, useful for treating depressive disorders, including major depressive disorder.
    Type: Grant
    Filed: June 28, 2018
    Date of Patent: March 8, 2022
    Assignee: CHASE THERAPEUTICS CORPORATION
    Inventors: Thomas N. Chase, Kathleen E. Clarence-Smith
  • Patent number: 11242334
    Abstract: (I) Disclosed herein are compounds of formula I, and/or a stereoisomer, a stable isotope, or a pharmaceutically acceptable salt thereof; and therapeutic uses of these compounds, which are kinase inhibitors potentially useful in the treatment of diseases treatable, such as cancers, as well as pharmaceutical compositions, comprising a compound of formula I, and/or a stereoisomer, a stable isotope, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 15, 2018
    Date of Patent: February 8, 2022
    Assignee: JS Innopharm (Shanghai) Ltd.
    Inventors: Jintao Zhang, Wen Xu, Shanzhong Jian, Qun Li
  • Patent number: 11236089
    Abstract: The disclosure includes compounds of Formula (I) wherein A, W, m, R5, R6, R7, and R8, are defined herein. Also disclosed is a method for treating a neoplastic disease with these compounds.
    Type: Grant
    Filed: February 26, 2020
    Date of Patent: February 1, 2022
    Assignee: BlueValley Pharmaceutical LLC
    Inventor: Xiang Li
  • Patent number: 11197863
    Abstract: Disclosed are methods and compositions for treating pediatric embryonal tumors. The methods and compositions utilize or include an inhibitor of polo-like kinase 4 (PLK4) for treating pediatric embryonal tumors.
    Type: Grant
    Filed: August 29, 2018
    Date of Patent: December 14, 2021
    Assignee: ANN AND ROBERT H. LURIE CHILDREN'S HOSPITAL OF CHICAGO
    Inventors: Simone T. Sredni, Tadanori Tomita
  • Patent number: 11185592
    Abstract: This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
    Type: Grant
    Filed: May 22, 2020
    Date of Patent: November 30, 2021
    Assignee: C4 Therapeutics, Inc.
    Inventors: Andrew J. Phillips, Christopher G. Nasveschuk, James A. Henderson, Yanke Liang, Kiel Lazarski, Ryan E. Michael
  • Patent number: 11180499
    Abstract: Provided herein are compounds and methods for modulating the phosphodiesterase PDE4. More particularly, provided are selective inhibitors PDE4 and the uses of such inhibitors in regulating diseases and disorders, e.g., to treat cancer, inflammatory diseases, neurological diseases, neurodegenerative diseases, and addiction.
    Type: Grant
    Filed: April 12, 2021
    Date of Patent: November 23, 2021
    Assignee: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
    Inventor: Corey Hopkins
  • Patent number: 11104668
    Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: August 31, 2021
    Assignees: Hoffmann-La Roche Inc., Chugai Pharmaceutical Co.
    Inventors: Francisco Javier Lopez-Tapia, Sung-Sau So, Qi Qiao, Romyr Dominique
  • Patent number: 11077101
    Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X1, X2, X3, X4, Y, A, L1, L2, R1, R2, R5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
    Type: Grant
    Filed: July 18, 2019
    Date of Patent: August 3, 2021
    Assignee: Tango Therapeutics, Inc.
    Inventors: Kevin M. Cottrell, John P. Maxwell, Douglas A. Whittington
  • Patent number: 11028079
    Abstract: The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.
    Type: Grant
    Filed: November 15, 2019
    Date of Patent: June 8, 2021
    Assignees: ConverGene, LLC, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Jeffrey William Strovel, Makoto Yoshioka, David J. Maloney, Shyh Yang, Ajit Jadhav, Daniel Jason Urban
  • Patent number: 10981901
    Abstract: Disclosed are compounds having the formula: wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: April 20, 2021
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Joseph J. Romano, Jianxing Kang
  • Patent number: 10973807
    Abstract: The present invention provides a pharmaceutical composition containing a pyrrolo-fused six-membered heterocyclic compound or a pharmaceutically acceptable salt of the compound. Specifically, the invention provides a pharmaceutical composition containing 5-(2-diethylamino-ethyl)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidene-methyl)-3-methyl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one or a pharmaceutically acceptable salt thereof, and at least one water soluble filler. The pharmaceutical composition of the invention features a rapid dissolution and good stability.
    Type: Grant
    Filed: February 28, 2017
    Date of Patent: April 13, 2021
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Yun Lu, Xinhua Zhang, Chenyang Wang, Tonghui Liu
  • Patent number: 10960008
    Abstract: The present invention relates to methods for treating PTEN deficient epithelial cancers using a combination of anti-PI3Kbeta and anti-immune checkpoint agents.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: March 30, 2021
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Jean Zhao, Johann Bergholz, Gordon J. Freeman, Thomas M. Roberts
  • Patent number: 10954217
    Abstract: Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, and neuropathic pain.
    Type: Grant
    Filed: April 29, 2017
    Date of Patent: March 23, 2021
    Assignee: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Stephen F. Martin, James J. Sahn, Kathryn Taylor Linkens
  • Patent number: 10952432
    Abstract: The present invention is directed to use of cannabidiol and compositions thereof as an anti-bacterial agent against multi-drug resistant bacteria such as Pseudomonas aeruginosa.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: March 23, 2021
    Assignee: PHARMOTECH SA
    Inventor: Rodin Aeschbach
  • Patent number: 10919886
    Abstract: A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer.
    Type: Grant
    Filed: November 6, 2019
    Date of Patent: February 16, 2021
    Assignee: UNIVERSITY HEALTH NETWORK
    Inventors: Peter Brent Sampson, Miklos Feher, Heinz W. Pauls
  • Patent number: 10894058
    Abstract: Provided is a method of producing a solid dispersion that can improve solubility of a hardly soluble polyphenol in water. Specifically, provided is a method of producing a solid dispersion containing an amorphous hardly soluble polyphenol, the method including the steps of: mixing (A) a hardly soluble polyphenol, (B) at least one selected from the group consisting of a plant-derived polysaccharide, a seaweed-derived polysaccharide, and a microorganism-derived polysaccharide, a plant-derived polypeptide, and a microorganism-derived polypeptide, and (C) at least one selected from the group consisting of a monosaccharide and a disaccharide, followed by melting of the mixture by heating; and solidifying the molten product by cooling.
    Type: Grant
    Filed: August 19, 2015
    Date of Patent: January 19, 2021
    Assignee: KAO CORPORATION
    Inventors: Masahiro Umehara, Akihiro Uda, Tetsuya Abe, Yasushi Yamada
  • Patent number: 10870627
    Abstract: A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoroanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: December 22, 2020
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Di Li, Ning Zhou, Ao Chen, Liang Zhao, Jiansheng Han, Yanjun Liu
  • Patent number: 10851083
    Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: December 1, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Patent number: 10800774
    Abstract: The present invention relates to heterocyclic compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.
    Type: Grant
    Filed: August 17, 2018
    Date of Patent: October 13, 2020
    Assignees: Board of Regents, The University of Texas System, ChemPartner Corporation
    Inventors: Maria Emilia Di Francesco, Philip Jones, Christopher Lawrence Carroll, Jason Bryant Cross, Zhijun Kang, Michael Garrett Johnson, Sarah Lively
  • Patent number: 10800764
    Abstract: The present invention is directed to substituted pyridine derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives in the treatment of disorders mediated by c-fms kinase. The present invention is further directed to a process for the preparation of said substituted pyridine derivatives.
    Type: Grant
    Filed: August 13, 2018
    Date of Patent: October 13, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jie Chen, Matthew Donahue, Heng-Keang Lim, Ronghui Lin, Rhys Salter, Jiejun Wu, Yong Gong
  • Patent number: 10793549
    Abstract: The present invention relates to a sulfuryl-substituted benzoheterocyclic derivative, a preparation method and medical use thereof. Particularly, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, and a preparation method and application thereof. The definition of each group in the formula can be found in the specification and the claims.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: October 6, 2020
    Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Yunzhou Jin, Xiang Chen, Pengfei Cheng, Ping Bu, Leitao Zhang, Chong Wen, Yingtao Liu, Fusheng Zhou, Ming Weng, Jiong Lan
  • Patent number: 10729670
    Abstract: Compounds of Formula (I), and pharmaceutically effective salts thereof; wherein R1-R14, m, n, o, p, q and r are as defined herein, are provided for treatment of for increasing insulin sensitivity, reducing insulin resistance, preventing insulin resistance and treating insulin resistance disorders.
    Type: Grant
    Filed: September 7, 2017
    Date of Patent: August 4, 2020
    Assignee: Temple University—Of The Commonwealth Systems Of Higher Education
    Inventors: Salim Merali, Carlos A. Barrero, Wayne E. Childers, George C. Morton
  • Patent number: 10730858
    Abstract: The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: August 4, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zilun Hu, Cailan Wang, Mimi L. Quan, Peter W. Glunz
  • Patent number: 10717711
    Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, and Z are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: February 27, 2019
    Date of Patent: July 21, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Adam K. Charnley, Xiaoyang Dong
  • Patent number: 10669251
    Abstract: Compounds of the formula I in which X1, X2, X3, X4, R1, R2, R3, Q and Y have the meanings indicated in Claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: June 2, 2020
    Assignee: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Mathilde Muzerelle, Lars Burgdorf, Margarita Wucherer-Plietker, Paul Czodrowski, Christina Esdar, Christos Tsaklakidis
  • Patent number: 10647693
    Abstract: The invention provides a novel class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the manufacture of medicaments for treating of influenza.
    Type: Grant
    Filed: August 29, 2017
    Date of Patent: May 12, 2020
    Assignee: NORTH & SOUTH BROTHER PHARMACY INVESTMENT COMPANY LIMITED
    Inventors: Changhua Tang, Qingyun Ren, Junjun Yin, Kai Yi, Yingjun Zhang
  • Patent number: 10640491
    Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: June 26, 2018
    Date of Patent: May 5, 2020
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Francisco Javier Lopez-Tapia, Sung-Sau So, Qi Qiao, Romyr Dominique
  • Patent number: 10640487
    Abstract: The present disclosure relates to solid state forms of Nilotinib fumarate and Nilotinib hydrochloride L-tartaric acid co-crystals, processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: March 13, 2017
    Date of Patent: May 5, 2020
    Assignee: Teva Pharmaceuticals USA, Inc.
    Inventors: Helena Ceric, Igor Avdejev, Edi Topic
  • Patent number: 10639313
    Abstract: Tricyclic compounds, including tricyclic iminodibenzylic and tricyclic iminostilbene compounds, are identified as therapeutic agents for inhibition of delta-5-desaturase (D5D) and for treating or preventing cancer and precancerous conditions, as well as autoimmune and inflammatory conditions. Pharmaceutical compositions and dietary supplements are provided, as are methods of administration and treatment.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: May 5, 2020
    Assignee: NDSU RESEARCH FOUNDATION
    Inventors: Yue (Steven) Qian, Pinjing Zhao, Changhui Yan
  • Patent number: 10618897
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: April 14, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Buelent Kocer, Bernd Kuhn, Marco Prunotto, Hans Richter, Martin Ritter
  • Patent number: 10590086
    Abstract: Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises formula (I) wherein X1, and X2 may be the same or different and each is independently selected from C, N, O and S; X3, X4, X5, and X6 may be the same or different and each is independently selected from C and N; each bond represented by a dotted line may be present or absent, provided that at least one such bond is present; R1, R2, R3, R4, R5 and R6 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R1, R2, R3, R4, R5 and R6 groups present is such that the respective valencies of X1, X2, X3, X4, X5, and X6 are maintained; and wherein at least one of R5 and R6 comprises a group Y, wherein Y is a group having a formula selected from (II), (III), (IV), (V), (VI), (VII) wherein L may be present or absent, and may be a substituted or unsub
    Type: Grant
    Filed: November 2, 2015
    Date of Patent: March 17, 2020
    Inventors: Phillip M. Cowley, Alan Wise, Susan Davis, Michael Kiczun
  • Patent number: 10568847
    Abstract: The subject invention pertains to methods and compositions for the treatment of erectile dysfunction (ED) (e.g., impotence) in a subject in need thereof utilizing one or more cannabinoid and one or more anti-ED drug.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: February 25, 2020
    Inventor: James J. Caprio
  • Patent number: 10562890
    Abstract: This invention relates to compounds that bind to wild-type CBF? and inhibit CBF? binding to RUNX proteins. The potent compounds of the invention inhibit this protein-protein interaction at low micromolar concentrations, using allosteric mechanism to achieve inhibition, displace wild-type CBF? from RUNX1 in cells, change occupancy of RUNX1 on target genes, and alter gene expression of RUNX1 target genes. These inhibitors show clear biological effects consistent with on-target RUNX protein activity. Pharmaceutical compositions containing a compound of the invention and a pharmaceutically acceptable carrier represent a separate embodiment of the invention. Another embodiment of the invention are methods of treating a RUNX-signaling-dependent cancer that expresses wild-type CBF? in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: February 18, 2020
    Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: John H. Bushweller, Anuradha Illendula
  • Patent number: 10550121
    Abstract: The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with 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 a kinase, such as a cyclin-dependent kinase (CDK) (e.g.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: February 4, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Nicholas Paul Kwiatkowski
  • Patent number: 10519150
    Abstract: The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene disulfonate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the malate, the hydrochloride, and the acetate each have one crystal salt form; the naphthalene disulfonate is amorphous. When compared to the known morpholine derivative free base, the present invention has one or more improved properties, e.g., a better crystalline state, greatly improved water solubility, light stability and thermal stability, etc. The present invention further provides preparation methods for the salts of morpholine derivative and the crystal forms thereof, pharmaceutical compositions and use thereof.
    Type: Grant
    Filed: December 29, 2016
    Date of Patent: December 31, 2019
    Assignee: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
    Inventors: Guangxin Xia, Jianshu Xie, Guohui Jia, Jiansheng Han, Naoko Ueda, Toru Iijima
  • Patent number: 10517842
    Abstract: Methods of modulating a miRNA level, such as a miR-29c and/or miR-200c level, in a cell are provided. Aspects of the methods include contacting the cell with an anti-fibrotic miRNA modulating active agent, such as a tranilast active agent. Also provided are compositions for use in practicing the methods. The methods and compositions find use in a variety of applications, including the treatment of fibrotic disorders, such as a uterine leiomyoma.
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: December 31, 2019
    Assignee: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center
    Inventors: Omid Khorram, Tsai-Der Chuang
  • Patent number: 10508118
    Abstract: The present invention relates to a compound of formula I, a stereoisomer, a prodrug, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, and a process for preparing the same, a pharmaceutical composition comprising the same, and use of the compound in the preparation of medicine preventing and treating tumors, wherein the substituents are as defined in the specification.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: December 17, 2019
    Assignee: Xiamen University
    Inventors: Xianming Deng, Zhongji Zhuang, Zhou Deng, Xiaoxing Huang, Yan Liu, Ting Zhang, Wei Huang, Qingyan Xu, Zhiyu Hu
  • Patent number: 10507210
    Abstract: Compositions containing and methods of administering TH-4000 are useful in treatment of cancer alone or in combination with other anti-cancer agents.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: December 17, 2019
    Assignee: Auckland UniServices Limited
    Inventors: Adam Vorn Patterson, Jeffrey Bruce Smaill, Shevan Silva, Christopher Paul Guise, Matthew Roy Bull, Victoria Jackson, Tillman Pearce, Nipun Davar
  • Patent number: 10494360
    Abstract: A compound of Formula I: or pharmaceutically acceptable enantiomers, or salts thereof. The present invention also relates to the use of compounds of Formula (I) as selective inhibitors of indoleamine 2,3-dioxygenase. The invention also relates to the use of the compounds of Formula (I) for the treatment or prevention of diseases cancer, infections, central nervous system disease or disorder, and immune-related disorders, either as a single agent or in combination with other therapies.
    Type: Grant
    Filed: March 8, 2017
    Date of Patent: December 3, 2019
    Assignee: NETHERLANDS TRANSLATIONAL RESEARCH CENTER B.V
    Inventors: Adrianus Petrus Antonius De Man, Joost Cornelis Marinus Uitdehaag, Jan Gerard Sterrenburg, Joeri Johannes Petrus De Wit, Nicole Wilhelmina Cornelia Seegers, Antonius Maria Van Doornmalen, Rogier Christian Buijsman, Guido Jenny Rudolf Zaman
  • Patent number: 10472353
    Abstract: A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: November 12, 2019
    Assignee: University Health Network
    Inventors: Peter Brent Sampson, Miklos Feher, Heinz W. Pauls
  • Patent number: 10463610
    Abstract: The present invention relates to novel pharmaceutical formulations. More specifically, the present invention relates to novel pharmaceutical formulations that are suitable for intraocular administration. The present invention also relates to the use of these formulations for the treatment of collagenic eye disorder such as, for example, the treatment of keratoconus.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: November 5, 2019
    Assignee: The University of Liverpool
    Inventors: Rachel L. Williams, Colin E. Willoughby
  • Patent number: 10456407
    Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents (such as tyrosine kinase inhibitors or VEGF/VEGFR inhibitors), particularly anticancer agents such as sunitinib, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: October 29, 2019
    Assignees: Epizyme, Inc., Health Research, Inc.
    Inventors: Heike Keilhack, Roberto Pili
  • Patent number: 10450300
    Abstract: Inhibitors of Wnt signaling pathway with structures of Formula I are disclosed, together with their pharmaceutical salts. Applications of compounds of Formula I in inhibiting or modulating the Wnt signaling pathway are also disclosed. Compounds of Formula I can treat disorders caused by aberrant activation of the Wnt signaling pathway.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: October 22, 2019
    Assignee: Suzhou Yunxuan Yiyao Keji Youxian Gongsi
    Inventor: Xiaohu Zhang
  • Patent number: 10435391
    Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: October 8, 2019
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Linda N. Casillas, John David Harling, Afjal Hussain Miah, Mark David Rackham, Ian Edward David Smith
  • Patent number: 10413540
    Abstract: Methods for treating a subject having a cancerous tumor are disclosed. The methods comprise administering to the subject an effective amount of a non-steroidal selective glucocorticoid receptor modulator (SGRM) and an effective amount of a chemotherapeutic agent. The tumor may be cervical cancer. The SGRM may be a fused azadecalin. In embodiments, the SGRM may be a heteroaryl ketone fused azadecalin or an octahydro fused azadecalin.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: September 17, 2019
    Assignee: Corcept Therapeutics, Inc.
    Inventor: Hazel Hunt
  • Patent number: 10398693
    Abstract: Disclosed herein are pharmaceutical compositions and dosage forms including N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino) benzamide that are useful in the treatment of subjects having cancer. The present disclosure also provides methods for preparing these pharmaceutical compositions and dosage forms, and methods of treating subjects having cancer utilizing the pharmaceutical compositions and dosage forms provided herein.
    Type: Grant
    Filed: July 18, 2018
    Date of Patent: September 3, 2019
    Assignee: IGNYTA, INC.
    Inventors: Daniel Codallos, Jr., Robert Orr, Ching-Yuan Li, Valerie Denise Start
  • Patent number: 10392374
    Abstract: A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: August 27, 2019
    Assignee: University Health Network
    Inventors: Peter Brent Sampson, Miklos Feher, Heinz W. Pauls
  • Patent number: 10370328
    Abstract: Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: August 6, 2019
    Assignee: MUSC Foundation for Research Development
    Inventors: Craig C. Beeson, Christopher C. Lindsey, Baerbel Rohrer, Yuri Karl Peterson