516 patents
Page 12 of 26
Utility
Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
4 Jan 22
The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Wenqing Yao, David M. Burns, Jincong Zhuo
Filed: 13 Nov 19
Utility
1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
28 Dec 21
The present invention is directed to 1, 2, 5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2, 3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1, 2, 5-oxadiazole derivatives.
Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu, Jiacheng Zhou, Qiyan Lin, Lingkai Weng, Tai-Yuen Yue, Pingli Liu
Filed: 15 Apr 20
Utility
ALK2 Inhibitors for the Treatment of Anemia
23 Dec 21
Provided herein are methods of treating anemia in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an ALK2 inhibitor.
Francis Séguy, Ekaterine Asatiani, Yaoyu Chen
Filed: 15 Jun 21
Utility
Pyrrolotriazine Compounds As JAK2 V617F Inhibitors
23 Dec 21
The present application provides pyrrolotriazine compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
Zhiyong Yu, Liangxing Wu, Wenqing Yao
Filed: 17 Jun 21
Utility
Bicyclic Heterocycles As FGFR Inhibitors
23 Dec 21
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.
Yaping Sun, Liang Lu, Wenqing Yao, Jincong Zhuo, Liangxing Wu, Meizhong Xu, Ding-Quan Qian, Chunhong He, Fenglei Zhang
Filed: 28 Jan 21
Utility
Heterocyclic Derivatives As PI3K Inhibitors
23 Dec 21
Stacey Shepard, Yanran Ai, Andrew P. Combs, Nikoo Falahatpisheh, Lixin Shao, Artem Shvartsbart
Filed: 24 Jun 21
Utility
Naphthyridinone Compounds As JAK2 V617F Inhibitors
23 Dec 21
The present application provides naphthyridinone compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
Stacey Shepard, Lixin Shao, Liangxing Wu, Wenqing Yao
Filed: 17 Jun 21
Utility
Tricyclic Fused Thiophene Derivatives As Jak Inhibitors
16 Dec 21
The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Yun-Long Li, Wenyu Zhu, Song Mei, Joseph Glenn
Filed: 12 Aug 21
Utility
Imidazopyridazine Compounds and Uses Thereof
16 Dec 21
Jun Pan, Yu Bai, Liangxing Wu, Wenqing Yao
Filed: 10 Jun 21
Utility
Combination Therapy for Treatment of Myeloproliferative Neoplasms
9 Dec 21
The present application relates to treatment of myeloproliferative neoplasms using the JAK1/JAK2 inhibitor, ruxolitinib, in combination with a BET protein inhibitor, 2,2,4-trimethyl-8-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-6-(methylsulfonyl)-2H-1,4-benzoxazin-3(4H)-one, wherein the combination is unexpectedly synergistic.
Matthew Stubbs, Phillip C. Liu
Filed: 2 Jun 21
Utility
Processes of Preparing a JAK1 Inhibitor
9 Dec 21
The present application provides processes for preparing 4-[3-(cyanomethyl)-3-(3′,5′-dimethyl-1H, 1′H-4,4′-bipyrazol-1-yl)azetidin-1-yl]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]benzamide, and phosphoric acid salt thereof, which is useful as a selective (Janus kinase 1) JAK1 inhibitor, as well as salt forms and intermediates related thereto.
Jiacheng Zhou, Yingrui Dai, Zhongjiang Jia, Yongchun Pan, James M. Parks, Anthony J. Tomaine, Jianji Wang, Aibin Zhang
Filed: 2 Jun 21
Utility
Heterocyclic Compounds As Immunomodulators
9 Dec 21
Liangxing Wu, Jingwei Li, Wenqing Yao
Filed: 18 Aug 21
Utility
Substituted Tricyclic Compounds As FGFR Inhibitors
9 Dec 21
The present invention relates to tricyclic compounds, 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.
Liangxing Wu, Colin Zhang, Chunhong He, Liang Lu, Wenqing Yao
Filed: 2 Jun 21
Utility
Pyrazolopyridine Compounds and Uses Thereof
9 Dec 21
Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds.
Oleg Vechorkin, Jun Pan, Kai Liu, Alexander Sokolsky, Anlai Wang, Hai Fen Ye, Qinda Ye, Wenqing Yao
Filed: 7 Jan 21
Utility
Modulators of indoleamine 2,3-dioxygenase and methods of using the same
7 Dec 21
The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
Andrew P. Combs, Eddy W. Yue
Filed: 10 Jan 19
Utility
Pyrazolopyrimidine Compounds and Uses Thereof
2 Dec 21
Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds.
Oleg Vechorkin, Kai Liu, Jun Pan, Alexander Sokolsky, Hai Fen Ye, Qinda Ye, Wenqing Yao, Joshua Hummel
Filed: 23 Apr 21
Utility
Crystalline forms of a phosphoinositide 3-kinase (PI3K) inhibitor
30 Nov 21
The present invention relates to salts and crystalline forms of 2-(3-(8-Amino-6-(trifluoromethyl)imidazo[1,2-a]pyrazin-3-yl)-4-methylphenyl)-3,3,3-trifluoro-2-hydroxypropanamide, crystalline forms of 8-amino-N-(2-hydroxy-2-methylpropyl)-3-(2-methyl-5-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide, and crystalline forms of 8-amino-N-(2-hydroxy-2-methylpropyl)-3-(2-(methyl-d3)-5-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide, which are PI3K inhibitors useful in the treatment of cancer and other diseases.
Brent Douty, David M. Burns, Andrew P. Combs, Zhongjiang Jia, Daniel Levy, Eddy W. Yue
Filed: 4 Sep 19
Utility
Heterocyclic Compounds As Immunomodulators
25 Nov 21
Liangxing Wu, Zhiyong Yu, Fenglei Zhang, Wenqing Yao
Filed: 17 Dec 20
Utility
Fused Tricyclic Kras Inhibitors
18 Nov 21
Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds.
Wenyu ZHU, Xiaozhao WANG, Artem SHVARTSBART, Chao Qi, Rocco Policarpo, Wenqing Yao
Filed: 15 Apr 21
Utility
Fused Pyrimidine Compounds As Kras Inhibitors
18 Nov 21
Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds.
Gia Hoang, Xiaozhao Wang, Wenqing Yao
Filed: 12 May 21