Abstract: The present disclosure discusses salt forms of 4-cyano-N-[2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl]-1H-imidazole-2-carboxamide.
Abstract: A method for purifying a crude 2,5-furandicarboxylic acid composition including 2,5-furandicarboxylic acid and 5-formylfuran-2-carboxylic acid is disclosed. The method includes the steps of: (a) subjecting the crude 2,5-furandicarboxylic acid composition to complete dissolution in a solvent solution to obtain a mixture, the solvent solution including an organic solvent and water; (b) subjecting 5-formylfuran-2-carboxylic acid in the mixture to an addition reaction with sodium hydrogen sulfite to obtain an addition product; and (c) subjecting 2,5-furandicarboxylic acid to precipitation after step (b) to obtain purified 2,5-furandicarboxylic acid.
Abstract: Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.
Type:
Grant
Filed:
April 26, 2017
Date of Patent:
November 24, 2020
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Stefan Werner, Stefanie Mesch, Arwed Cleve, Nico Bräuer, Simon Anthony Herbert, Markus Koch, Henrik Dahllöf, Maren Osmers, Elizabeth Hardaker, Anton Lishchynskyi
Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.
Abstract: The present invention provides novel crystalline forms of 4-[3-Chloro-4-(N?-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, as well as methods for their preparation.
Type:
Grant
Filed:
September 15, 2017
Date of Patent:
November 17, 2020
Assignee:
Indena S.P.A.
Inventors:
Nicola Sardone, Stefano Luca Giaffreda, Andrea Gambini, Alex Petrolati, Pietro Allegrini, Enrico Modena
Abstract: The present invention provides a cocrystal of (S)-3-(1-((1-acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-1H-1,2,4-triazol-5(4H)-one and an organic acid capable of forming a cocrystal with the compound.
Abstract: There is a demand for the development of a technique according to which sodium 2,2,6,6-tetramethylpiperidides (Na-TMPs) can be economically and efficiently synthesized through simple operations including a small number of steps under mild conditions in a short period of time. Also, there is a demand for the development of a technique according to which high-quality Na-TMPs that do not contain lithium or lithium compounds such as Li-TMP can be synthesized. The method for synthesizing sodium 2,2,6,6-tetramethylpiperidides includes a step of obtaining sodium 2,2,6,6-tetramethylpiperidides by reacting, in a reaction solvent, 2,2,6,6-tetramethylpiperidines with a dispersion product obtained by dispersing sodium in a dispersion solvent or an organosodium compound having an aromatic ring obtained through a reaction with a dispersion product obtained by dispersing sodium in a dispersion solvent.
Abstract: The present disclosure provides, inter alia, Compounds of Formula (I) or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.
Type:
Grant
Filed:
December 20, 2018
Date of Patent:
November 10, 2020
Assignee:
ChemoCentryx, Inc.
Inventors:
Pingchen Fan, Christopher W. Lange, Viengkham Malathong, Venkat Reddy Mali, Sreenivas Punna, Hiroko Tanaka, Yibin Zeng, Penglie Zhang
Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate are also disclosed.
Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I? and I?? or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
Type:
Grant
Filed:
February 26, 2018
Date of Patent:
October 20, 2020
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
Abstract: The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.
Type:
Grant
Filed:
May 28, 2019
Date of Patent:
October 20, 2020
Assignee:
Pliva Hrvatska D.O.O.
Inventors:
Tomislav Biljan, Jasna Dogan, Leonid Metsger, Sara Morasi Pipercic, Marina Ratkaj, Maja Matanovic Skugor, Yi Wang
Abstract: The present invention relates to a method for preparing a tyrosine kinase inhibitor and a derivative thereof. The present method has a short synthesis route, low costs, easy operation, and is suitable for large-scale production.
Type:
Grant
Filed:
April 27, 2017
Date of Patent:
October 6, 2020
Assignee:
Jiangsu Hengrui Medicine Co., Ltd.
Inventors:
Guaili Wu, Quanliang Zhang, Yongxing Cao
Abstract: The present invention provides a compound represented by formula (I), or a pharmaceutically acceptable salt, a solvate, an ester, an acid, a metabolite or a prodrug thereof. The compound itself in the present invention or in combination with at least one therapeutic agent can be used for preventing or treating diseases, disorders or symptoms caused by the adjustment of the activity of tyrosine kinase C-KIT, or affected by the activity of the tyrosine kinase C-KIT or involving in the activity of the tyrosine kinase C-KIT, especially cancers or other cell proliferation diseases.
Abstract: This invention relates to compounds of formula (I), a process for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions having an association with the orexin sub-type 1 receptor. Ar, R1, R2, R3, R4, R5, R6 and R7 have meanings given in the description.
Type:
Grant
Filed:
April 7, 2017
Date of Patent:
September 29, 2020
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec
Abstract: Provided herein is a process for the preparation of 4-((6-(2-(2,4-difluorophenyl)-1,1-difluoro-2-hydroxy-3-(5-mercapto-1H-1,2,4-triazol-1-yl)propyl)pyridin-3-yl)oxy)benzonitrile.
Type:
Grant
Filed:
November 17, 2017
Date of Patent:
September 29, 2020
Assignee:
Dow AgroSciences LLC
Inventors:
Nicholas R. Babij, Qiang Yang, Sarah Ryan, Yan Hao, Gary Roth, Kaitlyn Gray
Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate are also disclosed.
Abstract: The present invention provides a cocrystal of (S)-3-(1-((1-acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-1H-1,2,4-triazol-5(4H)-one and an organic acid capable of forming a cocrystal with the compound.
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:
December 11, 2019
Date of Patent:
September 8, 2020
Assignees:
Aragon Pharmaceuticals, Inc., Sloan-Kettering Institute for Cancer Research
Inventors:
Anna Dihas, Mark R. Herbert, Ouathek Ouerfelli, Nicholas D. Smith
Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.
Type:
Grant
Filed:
March 3, 2016
Date of Patent:
September 8, 2020
Assignee:
PHARMAKEA, INC.
Inventors:
Martin W. Rowbottom, John Howard Hutchinson, David Lonergan