Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.
Type:
Grant
Filed:
May 27, 2020
Date of Patent:
March 16, 2021
Assignee:
NOVARTIS AG
Inventors:
Luca Arista, Sreehari Babu, Jianwei Bian, Kai Cui, Michael Patrick Dillon, Rene Lattmann, Jialiang Li, Lv Liao, Dimitrios Lizos, Rita Ramos, Nikolaus Johannes Stiefl, Thomas Ullrich, Peggy Usselmann, Xiaoyang Wang, Liladhar Murlidhar Waykole, Sven Weiler, Yubo Zhang, Yizong Zhou, Tingying Zhu
Abstract: An embodiment of the present invention provides a method of preparing 2,5-furandimethylcarboxylate (FDMC), including preparing 2,5-furandimethylcarboxylate (FDMC) by subjecting a reaction mixture including 5-hydroxymethylfurfural (HMF), air, and an alcohol solvent to oxidative esterification in the presence of a gold (Au)-nanoparticle-supported catalyst, in which the gold (Au)-nanoparticle-supported catalyst includes a support and gold (Au) nanoparticles supported on the support.
Type:
Grant
Filed:
June 29, 2018
Date of Patent:
March 16, 2021
Assignees:
Korea Institute of Industrial Technology, SK CHEMICALS CO., LTD.
Inventors:
Yong Jin Kim, Dinesh Kumar Mishra, Jin Ku Cho, Yong Jin Yi, Han Seok Kim, Jong Ryang Kim
Abstract: The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor.
Type:
Grant
Filed:
March 26, 2020
Date of Patent:
March 16, 2021
Assignee:
CuraSen Therapeutics, Inc.
Inventors:
Anthony P. Ford, Wei Chen, David Scott Carter, Jiaxin Yu
Abstract: The present application describes deuterium-enriched pioglitazone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: The present invention relates to compound of Formula (I) containing carbon-carbon linker, a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a prodrug, a polymorph, N-oxide, S-oxide, or a carboxylic acid isostere thereof; processes for their preparation; pharmaceutical compositions comprising said compounds; and their use for the treatment of the diseases or disorders mediated by GPR120 receptor.
Abstract: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
Inventors:
Stephen John Atkinson, Emmanuel Hubert Demont, Lee Andrew Harrison, Etienne Levernier, Alexander G. Preston, Jonathan Thomas Seal, Ian David Wall, Robert J. Watson, James Michael Woolven
Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
Type:
Grant
Filed:
July 29, 2020
Date of Patent:
March 2, 2021
Assignees:
Aragon Pharmaceuticals, Inc., Sloan-Kettering Institute For Cancer Research
Inventors:
Anna Dihas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
Abstract: The present invention relates to the improved synthesis of noroxymorphone of formula (III). Particularly, the invention shows a way how to reduce the impurity level in the product avoiding lengthy purification steps.
Type:
Grant
Filed:
November 29, 2018
Date of Patent:
February 23, 2021
Assignee:
SIEGFRIED AG
Inventors:
Ernesto Santandrea, Beat Theodor Weber, Andreas Boudier, Oliver Geiseler, Patrick Jeger
Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein Z, L, R1a, R1b, R1c, R1d, 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:
July 27, 2018
Date of Patent:
February 16, 2021
Assignee:
ChemoCentryx, Inc.
Inventors:
Christopher Lange, Viengkham Malathong, Venkat Reddy Mali, Jeffrey McMahon, Darren J. McMurtrie, Sreenivas Punna, Howard S. Roth, Rajinder Singh, Yu Wang, Ju Yang, Penglie Zhang
Abstract: Disclosed are a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.
Type:
Grant
Filed:
April 30, 2020
Date of Patent:
February 9, 2021
Assignees:
SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
Abstract: Compounds having formula (I) (IX), and enantiomers, and diastereomers, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
Type:
Grant
Filed:
February 12, 2018
Date of Patent:
February 9, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Junqing Guo, Amy C. Hart, John E. Macor, Michael E. Mertzman, William J. Pitts, Steven H. Spergel, Scott Hunter Watterson, Murugaiah Andappan Murugaiah Subbaiah, Jie Chen, Carolyn Diane Dzierba, Guanglin Luo, Jianliang Shi, Sing-Yuen Sit
Abstract: Compounds of the formula (I) wherein Q1, Q2, Y—X, R1, R2, R3, R4, Rb, Rc, Rd, R5, R6, R7, Ra, m and n 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 8, 2016
Date of Patent:
February 2, 2021
Assignee:
Syngenta Participations AG
Inventors:
Laura Quaranta, Stephan Trah, Matthias Weiss, Farhan Bou Hamdan
Abstract: Disclosed is a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.
Type:
Grant
Filed:
April 30, 2020
Date of Patent:
January 26, 2021
Assignees:
SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
Abstract: Provided is a production method of a thiazole derivative represented by the formula (I), which has an adenosine A2A receptor antagonistic action and is useful as a therapeutic agent for, for example, Parkinson's disease, sleep disorder, analgesic resistance to opioid, migraine, movement disorder, depression, anxiety disorder and the like. Also provided is a production method of a compound represented by the formula (C), which contains (i) a step of reacting a compound represented by the formula (A) and a compound represented by the formula (B), and the like: (wherein R1 represents furyl, R4, R5 and R6 are the same or different and each represents lower alkyl or aryl, R2 represents pyridyl or tetrahydropyranyl, and X1 represents halogen).
Abstract: Disclosed is a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.
Type:
Grant
Filed:
April 30, 2020
Date of Patent:
December 29, 2020
Assignees:
SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
Abstract: The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.
Type:
Grant
Filed:
March 16, 2020
Date of Patent:
December 22, 2020
Assignee:
CELGENE QUANTICEL RESEARCH, INC.
Inventors:
Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
Abstract: The application describes methods for making a deuterated dextromethorphan of Formula (I), deuterated dextromethorphan produced by these methods, and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
June 24, 2020
Date of Patent:
December 15, 2020
Assignee:
Avanir Pharmaceuticals, Inc.
Inventors:
Matt Johnson, Cunxiang Zhao, Weihua Meng, Zhijun Lu, Yan Li
Abstract: The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with orotic acid are described. The invention further provides methods of preparation and characterization of such nicotine salts. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided.