Abstract: Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.
Abstract: The disclosure provides for compounds having immunoproteasome inhibitory activity, and pharmaceutical compositions made thereof. The disclosure further provides for the use of the compounds and compositions in treating various diseases and disorders in a subject that are associated with immunoproteasome activity, including inflammatory disorders, autoimmune disorders, hematological disorders, and neurodegenerative disorders.
Type:
Grant
Filed:
March 10, 2017
Date of Patent:
March 10, 2020
Assignees:
The Regents of the University of California, Board of Trustees of the Michigan State University
Inventors:
Michael C. Pirrung, Nicole A. Bakas, Andre Bachmann
Abstract: The various aspects present inventions provide various crystalline forms of (S)-(?)-amisulpride, (R)-(+)-amisulpride, and solvates thereof and methods of making same. In various aspects, the inventions also provide methods of resolving racemic amisulpride.
Type:
Grant
Filed:
June 21, 2019
Date of Patent:
March 3, 2020
Assignee:
Sunovion Pharmaceuticals Inc.
Inventors:
John R. Snoonian, Harold Scott Wilkinson
Abstract: The disclosure provides compounds of formula (I) or pharmaceutically acceptable salts thereof: The disclosure also provides processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them, and their use as modulators of dopamine D3 receptors, such as treating substance abuse or psychiatric diseases.
Type:
Grant
Filed:
October 13, 2016
Date of Patent:
March 3, 2020
Assignee:
INDIVIOR UK LIMITED
Inventors:
Susana Cremonesi, Fabrizio Micheli, Teresa Semeraro, Luca Tarsi
Abstract: A process for preparing aminothiol ester compounds and salts thereof. The present invention relates to a process for preparing compounds of formula (I), (I) comprising the following steps: a) reacting a compound of formula (II) with an inorganic acid or an organic acid, (II) b) reacting the compound obtained in step a) with a base; c) reacting the compound obtained in step b) with CO2; d) reacting the compound obtained in step c) with an alkyl chloroformate, a reagent capable of forming, with the compound obtained in step c), an acid halide, or a reagent capable of forming, with the compound obtained in step c), a mixed anhydride; e) reacting the compound obtained in step d) with an SMe anion precursor compound.
Type:
Grant
Filed:
February 16, 2017
Date of Patent:
February 25, 2020
Assignee:
ADVANCED BIODESIGN
Inventors:
Patrice Rool, Benoit De Carne-Carnavalet
Abstract: Phenylimidazole compounds of formula (1) shown below and pharmaceutically acceptable salts thereof: Also disclosed are a pharmaceutical composition and a lipoprotein lipase activator, each containing one of the phenylimidazole compounds.
Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.
Type:
Grant
Filed:
November 14, 2016
Date of Patent:
February 18, 2020
Assignees:
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, NEW YORK UNIVERSITY
Inventors:
Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika Elaine Englund
Abstract: Embodiments of the present disclosure relate generally to novel achiral and chiral sulfur-, nitrogen- and phosphorus-containing ligands, designated as NNS-type, P(O)NS-type, PNS-type, SNNS-type, SNNP(O)-type, or SNNP-type polydentate ligands and transition metal complexes of these ligands, including iridium complexes having PNS-type and NNS-type ligands. The catalysts derived from these ligands and transition metal complexes may be used in a wide range of catalytic reactions, including hydrogenation and transfer hydrogenation of unsaturated organic compounds, dehydrogenation of alcohols and boranes, various dehydrogenative couplings, chemoselective hydrogenation of ?,?-unsaturated alcohols, and other catalytic transformations.
Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the prevention and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, autoimmune diseases, metabolic diseases, and neurodegenerative diseases (e.g. autism, autism spectrum disorders, Alzheimer's disease)), as well as methods of treating these diseases.
Type:
Grant
Filed:
December 29, 2017
Date of Patent:
January 28, 2020
Assignee:
Agency for Science, Technology and Research
Abstract: Disclosed are amino triazole compounds substituted with a piperidinyl ring that is itself substituted with a heterocyclic ring. These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.
Type:
Grant
Filed:
February 15, 2019
Date of Patent:
January 21, 2020
Assignee:
OncoArendi Therapeutics S.A.
Inventors:
Marzena Mazur, Robert Koralewski, Bartlomiej Borek, Sylwia Olejniczak, Wojciech J. Czestkowski, Michal C. Piotrowicz, Jacek P. Olczak, Adam A. Golebiowski, Agnieszka Bartoszewicz, Elzbieta Maziarz, Michal L. Kowalski
Abstract: The present invention discloses an ?-silane coupling agent and application thereof. The ?-silane coupling agent has a structure formula of formula (I): R1 is alkyl with 1 to 6 carbon atoms; R2 is alkyl with 1 to 6 carbon atoms; R3 is alkyl with 1 to 6 carbon atoms; R4 or R5 is selected from one of hydrogen, alkyl with 1 to 18 carbon atoms, aryl, benzyl, ester-containing group, carbamido-containing group or heterocyclic alkane; R4 and R5 are the same or different. The ?-silane coupling agent is applied to silicone rubber, which can be cured without adding a catalyst, and the curing speed is fast; the ?-silane coupling agent has strong reactivity, the surface curing time is less than 2 minutes; and the ?-silane coupling agent has good stability, which can be stored stably under conditions at room temperature for 6 months, and does not easily turn yellow.
Abstract: The present invention provides polymeric pegylated carfilzomib compounds, and pharmaceutically acceptable salts thereof, of Formula I wherein R1, R2, linker, PEG, n and o are as defined herein. The invention also provides methods of making and using these compounds to treat cancer, and particularly to treat hematological malignancies including multiple myeloma.
Type:
Grant
Filed:
May 23, 2017
Date of Patent:
December 31, 2019
Assignee:
Amgen Inc.
Inventors:
Gary Luehr, Shabbir T. Anik, Ge Peng, Irina Dotsenko, Pasit Phiasivongsa, Dante Romanini
Abstract: This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.
Type:
Grant
Filed:
October 9, 2018
Date of Patent:
December 31, 2019
Assignee:
COMPASS Pathways Limited
Inventors:
Derek John Londesbrough, Christopher Brown, Julian Scott Northen, Gillian Moore, Hemant Kashinath Patil, David E. Nichols
Abstract: A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is LY; each L is a direct bond, C1-C10 alkylene, C2-C10 alkenylene or C2-C10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R3 is independently H, C1-C10 alkyl, halogen, fluoro C1-C10 alkyl, O— C1-C10 alkyl, NH—C1-C10 alkyl, S—C1-C10 alkyl, O-fluoro C1-C10 alkyl, NH-acyl, NH—C(O)—NH—C1-C10 alkyl, C(O)—NH—C1-C10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110?, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.
Type:
Grant
Filed:
April 24, 2018
Date of Patent:
December 24, 2019
Assignee:
Karus Therapeutics Limited
Inventors:
Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Franck Alexandre Silva
Abstract: A thiazole derivative compound includes a compound having the following structural formula: or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
January 11, 2019
Date of Patent:
December 10, 2019
Assignee:
King Saud University
Inventors:
Yahia Nasser Mabkhot, Jamal Mohammed Ali Khaled, Naiyf Sultan Helial Alaloi Alharbi, Fahd Ali Nasr Mohammed, Fahd Abdo Almekhlafi, Nael Mahmmoud Abutaha, Salim S. Al-Showiman
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110?, and therefore have utility in therapy.
Type:
Grant
Filed:
March 1, 2018
Date of Patent:
December 10, 2019
Assignee:
Karus Therapeutics Limited
Inventors:
Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Thomas James Hill, Franck Alexandre Silva
Abstract: Provided are compounds of formula I and formula II or pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The compounds of formula I and formula II or the pharmaceutically acceptable salts of the compounds provide indole 2,3-dioxygenase (IDO) inhibitory activity and are capable of treating IDO-mediated immunosuppressive diseases, such as infectious diseases or cancer.
Type:
Grant
Filed:
February 20, 2017
Date of Patent:
November 26, 2019
Assignees:
Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Medshine Discovery Inc.
Abstract: The present invention deals with novel bis-triazole compounds, compositions comprising these compounds, and their uses as a medicament, an antibacterial agent, an anti-biofilm agent, an anti-fouling agent and/or an anti-corrosion agent.
Type:
Grant
Filed:
December 14, 2016
Date of Patent:
November 26, 2019
Assignee:
Universite de Toulon
Inventors:
Sofyane Andjouh, Francois-Xavier Perrin, Yves Guy Blache