Abstract: The invention relates to the field of prevention and treatment of cancer, in particular suppression of tumor manifestation. The invention also relates to compounds for use in this field. A novel tumor manifestation suppression (TMS) regulation in a mammalian brain is recognized. The invention relates to compounds, pharmaceutical preparations, in particular medicaments for use in the prevention and treatment of cancer, in particular suppression of tumor manifestation based on said TMS regulation as well as methods for the same.
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X1, X2, X3, X4, Y, Z, A, Het, R1, R2, R3, R4, R5 R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.
Type:
Grant
Filed:
December 19, 2017
Date of Patent:
April 16, 2019
Assignee:
Genentech, Inc.
Inventors:
Benjamin Fauber, Emanuela Gancia, Tammy Ladduwahetty, David Vesey, Paul Winship, Olivier Rene
Abstract: This invention concerns pyrrolo[3,2-d]pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treatment and/or therapy of diseases.
Type:
Grant
Filed:
October 25, 2016
Date of Patent:
April 16, 2019
Assignee:
Janssen Sciences Ireland UC
Inventors:
David Craig McGowan, Stefaan Julien Last, Serge Maria Aloysius Pieters, Werner Embrechts, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson
Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
Abstract: An OLED device includes, in order, an electron blocking layer, an organic emissive layer, and a hole blocking layer. Its organic emissive layer contains at least four components: an electron transporting compound, a host, a hole transporting compound, and an emitting compound capable of phosphorescence emission at room temperature. The emitting compound has HOMO energy level of 5.2 eV or lower and a LUMO energy level of 2.5 eV or higher.
Type:
Grant
Filed:
April 15, 2014
Date of Patent:
April 9, 2019
Assignee:
UNIVERSAL DISPLAY CORPORATION
Inventors:
Vadim Adamovich, James Esler, Jason Brooks, Michael S. Weaver, Julia J. Brown
Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their use and production.
Type:
Grant
Filed:
July 17, 2015
Date of Patent:
April 2, 2019
Assignee:
BIOGEN MA INC.
Inventors:
Timothy Chan, Kevin Guckian, Tracy Jenkins, Jermaine Thomas, Jeffery Vessels, Gnanasambandam Kumaravel, Robert Meissner, Joseph Lyssikatos, Brian Lucas, Irina Leaf, Jeremy Duffield
Abstract: The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.
Type:
Grant
Filed:
September 29, 2016
Date of Patent:
April 2, 2019
Assignees:
Bristol-Myers Squibb Company, Syngene International Limited, Bristol-Myers Squibb Company
Inventors:
Joanne J. Bronson, Ling Chen, Jonathan L. Ditta, Carolyn Diane Dzierba, Prasada Rao Jalagam, Guanglin Luo, John E. Macor, Tarun Kumar Maishal, Susheel Jethanand Nara, Ramkumar Rajamani, Ramesh Kumar Sistla, Soodamani Thangavel
Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.
Abstract: Compounds and methods for treating diseases or conditions affected by the activity or expression of genes/proteins related to human GH, GHR, STAT5, SOCS, IGF-1, insulin are provided. Monoclonal antibodies for treating diseases or conditions related to growth hormone and growth hormone receptor activity are also provided.
Type:
Grant
Filed:
February 12, 2016
Date of Patent:
April 2, 2019
Assignee:
University of Southern California
Inventors:
Valter D. Longo, Priya Balasubramanian, Nouri Neamati, Min Wei
Abstract: Indazole sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma ROR?t are described. Pharmaceutical compositions including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.
Abstract: The invention relates to thiocarbamate prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: wherein R1, R2, R3, R4 and n are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.
Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, R3, Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.
Type:
Grant
Filed:
June 23, 2017
Date of Patent:
March 12, 2019
Assignee:
Polaris Pharmaceuticals, Inc.
Inventors:
Stephen E. Webber, Xueliang Tao, Elena Brin
Abstract: The present disclosure relates to the field of nucleic acid chemistry, specifically to 5-position modified uridines as well as phosphoramidite and triphosphate derivatives thereof. The present disclosure also relates to methods of making and using the same.
Type:
Grant
Filed:
July 14, 2017
Date of Patent:
March 5, 2019
Assignee:
SomaLogic, Inc.
Inventors:
John Rohloff, Nebojsa Janjic, Jeffrey D. Carter, Catherine Fowler
Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:
Type:
Grant
Filed:
April 22, 2016
Date of Patent:
March 5, 2019
Assignee:
VIIV HEALTHCARE UK (NO.5) LIMITED
Inventors:
John A. Bender, Robert G. Gentles, Annapurna Pendri, Alan Xiangdong Wang, Nicholas A. Meanwell, Brett R. Beno, Robert A. Fridell, Makonen Belema, Van N. Nguyen, Zhong Yang, Gan Wang, Selvakumar Kumaravel, Srinivasan Thangathirupathy, Rajesh Onkardas Bora, Shilpa Maheshwarappa Holehatti, Mallikarjuna Rao Mettu, Manoranjan Panda
Abstract: The invention concerns novel substituted pyrazolo- and triazolo-pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.
Type:
Grant
Filed:
April 27, 2016
Date of Patent:
February 19, 2019
Assignee:
Janssen Sciences Ireland UC
Inventors:
David Francis Alain Lançois, Jérôme Émile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Dirk André Emmy Roymans, Boris Rogovoy, Vadim Bichko, Delphine Yvonne Raymonde Lardeau, Antoine Benjamin Michaut, Anil Koul
Abstract: Disclosed are adsorption complexes that include 1-methylcyclopropene (1-MCP) and a metal coordination polymer network (MCPN), wherein the MCPN is a porous material, and the 1-MCP is adsorbed into the MCPN. Also disclosed are kits for containing 1-MCP that include the adsorption complex in a 1-MCP-impermeable package. Also disclosed are methods of releasing 1-methylcyclopropene (1-MCP) from the kit that include the application of aqueous fluids, heat, and/or pressure.
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of one or both of ERK1 and ERK2.
Type:
Grant
Filed:
June 14, 2018
Date of Patent:
February 12, 2019
Assignee:
CELGENE CAR LLC
Inventors:
Antonio Christian Ferretti, Lianfeng Huang, Ying Li, John Traverse, Jean Xu, Kelvin Hin-Yeong Yong, Daozhong Zou
Abstract: We disclose novel asymmetric bis-acridines with antitumor activity. These compounds are useful for use in pharmaceuticals, particularly in the treatment or the prevention of neoplasms.
Type:
Grant
Filed:
March 17, 2016
Date of Patent:
February 12, 2019
Assignee:
Gdansk University of Technology
Inventors:
Jerzy Kazimierz Konopa, Barbara Horowska, Ewa Maria Paluszkiewicz, Barbara Borowa-Mazgaj, Ewa Anna Augustin, Anna Skwarska, Zofia Mazerska