516 patents
Page 10 of 26
Utility
Solid Forms of an HPK1 Inhibitor
26 May 22
The present invention relates to salt forms of the hematopoietic progenitor kinase 1 (HPK1) inhibitors N-(2-((2S,4S)-4-Amino-2-(hydroxymethyl)pyrrolidin-1-yl)-5-fluorophenyl)-2-(2-fluoro-6-methoxyphenyl)pyrimidine-4-carboxamide and N-(2-((2S,4S)-4-Amino-2-(hydroxymethyl)pyrrolidin-1-yl)-4-(4-cyanopyridin-3-yl)phenyl)-2-(2-fluoro-6-methoxyphenyl)pyrimidine-4-carboxamide, including methods of preparation thereof, where the compounds are useful in the treatment of HPK1 mediated diseases such as cancer.
Zhongjiang Jia, William Frietze
Filed: 25 Jun 21
Utility
Sustained-release dosage forms of ruxolitinib
24 May 22
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.
Yong Ni, Bhavnish Parikh, Krishnaswamy Yeleswaram, Susan Erickson-Viitanen, William V. Williams
Filed: 16 Nov 20
Utility
Heterocyclic compounds as immunomodulators
24 May 22
Liangxing Wu, Jingwei Li, Wenqing Yao, Chao Qi, Ding-Quan Qian, Fenglei Zhang
Filed: 18 Aug 20
Utility
Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
17 May 22
The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
James D. Rodgers, Stacey Shepard
Filed: 17 Mar 20
Utility
Process of Preparing a PD-1/PD-L1 Inhibitor
12 May 22
The present invention relates to processes of preparing PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3′-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2′-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, or salts thereof, related synthetic intermediates, and salts of the intermediates, where the PD-1/PD-L1 inhibitor is useful in the treatment of various diseases including infectious diseases and cancer.
Jiacheng Zhou, Shili Chen, Zhongjiang Jia, Yi Li, Qiyan Lin, Pingli Liu, Yongchun Pan, Timothy Martin, Bo Shen, Chongsheng Eric Shi, Naijing Su, Yongzhong Wu, Michael Xia
Filed: 5 Nov 21
Utility
Process for Making a PD-1/PD-L1 Inhibitor and Salts and Crystalline Forms Thereof
12 May 22
This application relates to processes and intermediates for the preparation of the PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3′-((2-(difluoromethyl)-7-((3-hydroxypyrrolidin-1-yl)methyl)pyrido[3,2-d]pyrimidin-4-yl)amino)-2,2′-dimethyl-[1,1′-biphenyl]-3-yl)benzo[d]oxazol-5-yl)methyl)piperidine-4-carboxylic acid, and salts and crystalline forms thereof, where the PD-1/PD-L1 inhibitor and solid forms and salt forms thereof are useful in the treatment of various diseases including infectious diseases and cancer.
Dengjin Wang, Daniel Carper, Zhongjiang Jia, Bo Shen, Joseph A. Sclafani, Robert Wilson, Jiacheng Zhou, Osama Suleiman, Mark Wright
Filed: 5 Nov 21
Utility
Crystalline Form of a PD-1/PD-L1 Inhibitor
12 May 22
The present invention relates to crystalline forms of the PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3′-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2′-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, including methods of preparation thereof, and related synthetic intermediates, where the compound is useful in the treatment of various diseases including infectious diseases and cancer.
Zhongjiang Jia, Shili Chen, Mei Li, Pingli Liu, Yongchun Pan, Yongzhong Wu, Jiacheng Zhou
Filed: 5 Nov 21
Utility
Combination therapy for treatment of hematological diseases
10 May 22
The present application relates to treatment of a hematological disease selected from leukemia, lymphoma, and multiple myeloma in a patient in need thereof, comprising administering to the patient: (a) a therapeutically effective amount of a selective JAK1 inhibitor; (b) a therapeutically effective amount of an immunomodulatory agent, and (c) a therapeutically effective amount of a steroid.
Albert Assad
Filed: 31 Oct 19
Utility
Fused Pyrazine Derivatives As A2A / A2B Inhibitors
5 May 22
Xiaozhao Wang, Peter Niels Carlsen, Pei Gan, Gia Hoang, Yong Li, Chao Qi, Liangxing Wu, Wenqing Yao, Zhiyong Yu, Wenyu Zhu
Filed: 13 Oct 21
Utility
Use of Pyrazolopyrimidine Derivatives for the Treatment of PI3K-DELTA Related Disorders
21 Apr 22
Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Song Mei, Brent Douty
Filed: 30 Jun 21
Utility
Treatment of hidradenitis suppurativa using JAK inhibitors
19 Apr 22
The present application provides methods of treating hidradenitis suppurativa in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound which inhibits JAK1 and/or JAK2, or a pharmaceutically acceptable salt thereof.
Michael D. Howell, Paul Smith
Filed: 29 Mar 19
Utility
3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors
19 Apr 22
Artem Shvartsbart, Andrew P. Combs, Nikoo Falahatpisheh, Padmaja Polam, Lixin Shao, Stacey Shepard
Filed: 20 Dec 18
Utility
Crystalline Forms of a Phosphoinositide 3-KINASE (PI3K) Inhibitor
14 Apr 22
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: 27 Oct 21
Utility
Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
29 Mar 22
The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Taisheng Huang, Chu-Biao Xue
Filed: 19 May 20
Utility
Heterocyclic Compounds As Immunomodulators
24 Mar 22
Liangxing Wu, Fenglei Zhang, Song Mei, Wenqing Yao
Filed: 4 May 21
Utility
Low dose combination therapy for treatment of myeloproliferative neoplasms
22 Mar 22
The present application relates to treatment of myeloproliferative neoplasms using the JAK1/JAK2 inhibitor, ruxolitinib, in combination with a low dose of a Pim inhibitor, N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, wherein the combination is unexpectedly synergistic at a very low dose of the Pim inhibitor.
Holly Koblish, Gary Reuther
Filed: 6 Feb 20
Utility
Tricyclic Heterocyclic Compounds As Sting Activators
10 Mar 22
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.
Liangxing Wu, Neil Lajkiewicz, Yingda Ye, Zhenwu Li, Wenqing Yao
Filed: 2 Mar 21
Utility
Tricyclic Urea Compounds As JAK2 V617F Inhibitors
3 Mar 22
The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
Kai Liu, Brent Douty, Daniel Levy, Liangxing Wu, Wenqing Yao, Eddy W. Yue
Filed: 26 Aug 21
Utility
Vinyl Imidazole Compounds As Inhibitors of Kras
3 Mar 22
Peter Carlsen, Xiaozhao Wang, Alexander Sokolsky, Pei Gan, Rocco Policarpo, Wenqing Yao
Filed: 27 Aug 21
Utility
Imidazotriaines and imidazopyrimidines as kinase inhibitors
1 Mar 22
The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
Jincong Zhuo, Meizhong Xu, Chunhong He, Colin Zhang, Ding-Quan Qian, David M. Burns, Yun-Long Li, Brian Metcalf, Wenqing Yao
Filed: 23 Jun 20