Abstract: The present invention is related to processes for preparing a composition comprising (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile, and related synthetic intermediate compounds. This compound is useful as an inhibitor of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
Type:
Grant
Filed:
October 2, 2019
Date of Patent:
April 13, 2021
Assignee:
Incyte Corporation
Inventors:
Andrew W. Buesking, Richard B. Sparks, Andrew P. Combs, Brent Douty, Nikoo Falahatpisheh, Lixin Shao, Stacey Shepard, Eddy W. Yue, Artem Shvartsbart, David M. Burns, Daniel Levy
Abstract: The present invention relates to processes and intermediates for preparing 3-(cyanomethyl)-3-(4-{[(1R,2S)-2-phenylcyclopropyl]amino}piperidin-1-yl)azetidine-1-sulfonamide, and salts and solid forms thereof, which selectively modulate demethylase. Particular embodiments contemplate compounds and disease indications amenable to treatment by modulation of lysine specific demethylase-1 (LSD1).
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
April 6, 2021
Assignee:
Incyte Corporation
Inventors:
Zhongjiang Jia, Wayne Han, Yongchun Pan, Timothy Martin, Jiacheng Zhou, Qun Li
Abstract: The present invention is directed to [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-a]pyrazine derivatives of Formula IIa, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
Type:
Grant
Filed:
October 3, 2019
Date of Patent:
April 6, 2021
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
Abstract: The present application provides tricyclic heterocyclic compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.
Type:
Grant
Filed:
May 24, 2019
Date of Patent:
March 16, 2021
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Neil Lajkiewicz, Yingda Ye, Zhenwu Li, Wenqing Yao
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
Type:
Grant
Filed:
August 20, 2019
Date of Patent:
March 2, 2021
Assignee:
Incyte Corporation
Inventors:
Oleg Vechorkin, Kai Liu, Alexander Sokolsky, Anlai Wang, Hai Fen Ye, Qinda Ye, Wenqing Yao
Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.
Abstract: The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Type:
Grant
Filed:
March 5, 2020
Date of Patent:
February 2, 2021
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Kaijiong Xiao, Wenqing Yao
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
Type:
Grant
Filed:
August 7, 2019
Date of Patent:
January 26, 2021
Assignee:
Incyte Corporation
Inventors:
Joshua Hummel, Oleg Vechorkin, Alexander Sokolsky, Qinda Ye, Kai Liu, Wenqing Yao
Abstract: This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract: The present application provides heteroaryl amide compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.
Type:
Grant
Filed:
July 31, 2019
Date of Patent:
December 29, 2020
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Neil Lajkiewicz, Wenqing Yao
Abstract: The present invention relates to sustained-release formulations and dosage forms of ruxolitinib, or a pharmaceutically acceptable salt thereof, which are useful in the treatment of Janus kinase-associated diseases such as myeloproliferative disorders.
Abstract: This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.
Abstract: The present invention relates to an amorphous solid form of (4S)-7-(3,5-dimethylisoxazol-4-yl)-4-pyridin-2-yl-4,5-dihydroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-one, and processes for its preparation, which is an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and is useful in the treatment of various diseases such as cancer.
Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer.
Type:
Grant
Filed:
April 23, 2019
Date of Patent:
December 1, 2020
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Liang Lu, Ding-Quan Qian, Bo Shen, Wenqing Yao
Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
Type:
Grant
Filed:
September 4, 2019
Date of Patent:
November 24, 2020
Assignee:
Incyte Corporation
Inventors:
Yun-Long Li, Xiaozhao Wang, Chunhong He
Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.