Abstract: In one aspect, the present invention provides a method for treating or ameliorating the effects of a HER2 positive cancer in a subject. In some embodiments, the method comprises administering a combination therapy comprising an anti-HER2 antibody and tucatinib. In some embodiments, the method further comprises administering a chemotherapeutic agent (e.g., an antimetabolite) to the subject. Pharmaceutical compositions and kits are also provided herein.
Abstract: This application relates to compounds and methods of treating retinal degeneration associated with inherited rhodopsin mutations in the ocular tissue of a subject. The retinal degeneration, can include, for example, macular degeneration, a including age-related macular degeneration, Stargardt disease, and retinitis pigmentosa. The retinitis pigmentosa can include autosomal dominate retinitis pigmentosa associated with a P23H RHO mutation. A method of treating retinal degeneration in a subject includes administering to the subject a therapeutically effective amount of a compound of formula (I), wherein the compound of formula (I) acts as a chaperone of rhodopsin.
Type:
Grant
Filed:
April 30, 2018
Date of Patent:
December 7, 2021
Assignees:
CASE WESTERN RESERVE UNIVERSITY, UNIVERSITY OF PITTSBURGH—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
Type:
Grant
Filed:
August 16, 2018
Date of Patent:
November 30, 2021
Assignee:
SYNGENTA PARTICIPATIONS AG
Inventors:
Matthias Weiss, Laura Quaranta, Farhan Bou Hamdan
Abstract: Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.
Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
Type:
Grant
Filed:
September 11, 2018
Date of Patent:
November 30, 2021
Assignee:
SYNGENTA PARTICIPATIONS AG
Inventors:
Farhan Bou Hamdan, Matthias Weiss, Laura Quaranta
Abstract: Compounds of the formula (I) wherein the subsitiuents are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
Type:
Grant
Filed:
September 11, 2018
Date of Patent:
November 23, 2021
Assignee:
SYNGENTA PARTICIPATIONS AG
Inventors:
Laura Quaranta, Matthias Weiss, Farhan Bou Hamdan
Abstract: The present invention relates to a novel 1H-pyrazolopyridine derivative and a pharmaceutical composition containing the same. The 1H-pyrazolopyridine derivative and the pharmaceutical composition containing the same can be usefully used for the prevention or treatment of autoimmune diseases or cancer.
Type:
Grant
Filed:
July 12, 2018
Date of Patent:
November 23, 2021
Assignee:
Daewoong Pharmaceutical Co., Ltd.
Inventors:
Keuk-Chan Bang, Deok Ki Eom, Joon Seok Park
Abstract: The present disclosure describes novel IDO inhibitors and methods for preparing them. The pharmaceutical compositions comprising such IDO inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders are also described.
Type:
Grant
Filed:
September 5, 2018
Date of Patent:
November 23, 2021
Assignee:
ANGEX PHARMACEUTICAL, INC.
Inventors:
Wen-Lian Wu, Zhiqiang Yang, Francis Lee, John Qiang Tan
Abstract: The present invention relates to a process for the preparation of migalastat of formula (I) and intermediates useful in the synthesis thereof. The process comprises the double reductive amination reaction of a compound of formula (VI).
Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
Type:
Grant
Filed:
April 23, 2020
Date of Patent:
November 2, 2021
Assignee:
Anacor Pharmaceuticals, Inc.
Inventors:
Tsutomu Akama, Eric Easom, Yvonne Freund, Jacob J. Plattner, Jessica Sligar, Daitao Chen, Jennifer Freeman, Joe Perales
Abstract: The present disclosure provides a method for producing tetrahydrofuran (THF). The method includes: feeding 1,4-butanediol into a reactive distillation apparatus; performing the dehydration reaction in the presence of an acidic catalyst; and producing the top stream containing product THF and the bottom stream from the reactive distillation apparatus, wherein a weight ratio of a water content in the bottom stream to a water content in the top stream is 0.05 to 2.4, thereby providing a high conversion rate and more cost-effectiveness, and enhancing the value of the industrial application.
Abstract: The present disclosure relates to a novel phenylpyridine derivative represented by Chemical Formula 1 and a pharmaceutical composition comprising the same, and the compound according to the present disclosure can be usefully used for the prevention or treatment of autoimmune diseases or cancers.
Type:
Grant
Filed:
October 11, 2018
Date of Patent:
October 19, 2021
Assignee:
Daewoong Pharmaceutical Co., Ltd.
Inventors:
Wol-Young Kim, Jung-eun Park, Keuk-Chan Bang, Joon-Seok Park
Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
January 14, 2020
Date of Patent:
October 5, 2021
Assignee:
ChemoCentryx, Inc.
Inventors:
Christopher Lange, Sreenivas Punna, Rajinder Singh, Ju Yang, Penglie Zhang
Abstract: The present disclosure is directed to disclosed compounds that modulate, e.g., address underlying defects in cellular processing of CFTR activity.
Type:
Grant
Filed:
December 17, 2019
Date of Patent:
October 5, 2021
Assignee:
Proteostasis Therapeutics, Inc.
Inventors:
Benito Munoz, Cecilia M. Bastos, Daniel Parks, David Kombo
Abstract: Aminoquinoline compounds useful for treating chronic pain, addiction, and other conditions are provided. The aminoquinoline compound is represented by Formula (I): in which the substituents thereof are defined as set forth in the specification.
Abstract: The present invention relates to a method of preparing Cabozantinib (Cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylo]amide(4-fluoro-phenyl)amide) and 18F labeled Cabozantinib.
Type:
Grant
Filed:
July 31, 2015
Date of Patent:
September 21, 2021
Assignee:
Exelixis, Inc.
Inventors:
Wei Xu, David J. Donnelly, Patrick L. Chow, Benjamin J. Henley
Abstract: High-potential photo-oxidants are provided with a supermolecule structure at least including a conjugated macrocycle linked to a metal complex. The conjugated macrocycle is electron-accepting relative to hydrogen or bears electron withdrawing substituents such as fluoroalkyl, fluoroaryl, fluoro, halo, cyano, or nitro. The metal complex is also electron-accepting relative to hydrogen or bears electron withdrawing substituents such as fluoroalkyl, fluoroaryl, fluoro, halo, cyano, or nitro. The linker can be thynyl, vinyl, thiophenyl, diethynylaryl, divinylaryl, diethynyl(unsaturated heterocycloalkenyl), divinyl(unsaturated heterocycloalkenyl), diethynyl(unsaturated heterocycloalkynyl), or divynyl(unsaturated heterocycloalkynyl). A specific implementation is an ethyne-bridged eDef-Rutpy-(porphinato)Zn(II) (eDef-RuPZn) supermolecule.
Type:
Grant
Filed:
June 5, 2018
Date of Patent:
September 14, 2021
Assignee:
DUKE UNIVERSITY
Inventors:
Michael Therien, Ting Jiang, Nicholas Polizzi, Jeffrey Rawson
Abstract: The present invention provides a compound of Formula II wherein X is selected from the group consisting of CH and N; Q is selected from the group consisting of CH3 and H; R is selected from the group consisting of and; or a pharmaceutically acceptable salt thereof, compositions, methods to treat liver disease and NASH.
Type:
Grant
Filed:
February 21, 2018
Date of Patent:
September 14, 2021
Assignee:
Eli Lilly and Company
Inventors:
Hui Lei, Gang Liu, Yuan Tian, Haizhen Zhang
Abstract: Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, and the other is hydrogen, and methods for their use are provided.
Type:
Grant
Filed:
May 18, 2020
Date of Patent:
September 14, 2021
Assignee:
Eli Lilly and Company
Inventors:
Jolie Anne Bastian, Jeffrey Daniel Cohen, Almudena Rubio, Daniel Jon Sall, Jennifer Anne McMahon