公开(公告)号：US20190337948A1

公开(公告)日：2019-11-07

申请号：US16402955

申请日：2019-05-03

Applicant: Incyte Corporation

Inventor： William Frietze ,  Zhongjiang Jia ,  Ming Tao ,  Dengjin Wang ,  Jiacheng Zhou ,  Qun Li ,  Timothy C. Burn ,  Phillip C. Liu

IPC: C07D471/14 ,  C07D471/04 ,  A61K9/00 ,  A61P35/00

Abstract: The present disclosure relates to 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4, 7-tetrahydro-2H-pyrrolo[3′,2′: 5,6]pyrido[4,3-d]pyrimidin-2-one, solid forms and polymorphs thereof, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.

公开(公告)号：US20190112313A1

公开(公告)日：2019-04-18

申请号：US16142514

申请日：2018-09-26

Applicant: Incyte Corporation

Inventor： Zhongjiang Jia ,  Yongzhong Wu ,  Yongchun Pan ,  Jiacheng Zhou ,  Qun Li

IPC: C07D487/04 ,  A61P35/00

Abstract: The present application provides salt forms of N-(4-(4-Amino-7-(1-isobutyrylpiperidin-4-yl)pyrrolo[1,2-f][1,2,4]triazin-5-yl)phenyl)-1-isopropyl-2,4-dioxo-3-(pyridin-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide and N-(4-(4-Amino-7-(1-isobutyrylpiperidin-4-yl)pyrrolo[1,2-f][1,2,4]triazin-5-yl)phenyl)-1-isopropyl-2,4-dioxo-3-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxamide, which are useful as inhibitors of TAM kinases, as well as processes and intermediates related thereto.

公开(公告)号：US20170362229A1

公开(公告)日：2017-12-21

申请号：US15626539

申请日：2017-06-19

Applicant: Incyte Corporation

Inventor： Shili Chen ,  Zhongjiang Jia ,  Pingli Liu ,  Lei Qiao ,  Yongzhong Wu ,  Jiacheng Zhou ,  Qun Li

IPC: C07D471/04 ,  C07F5/02

CPC classification number: C07D471/04 ,  C07B2200/13 ,  C07D471/02 ,  C07F5/025

Abstract: The present application relates to crystalline solid forms of an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of diseases such as cancer.

公开(公告)号：US20170121310A1

公开(公告)日：2017-05-04

申请号：US15260695

申请日：2016-09-09

Applicant: Incyte Corporation

Inventor： Zhongjiang Jia ,  Ganfeng Cao ,  Qiyan Lin ,  Yongchun Pan ,  Lei Qiao ,  Vaqar Sharief ,  Chongsheng Eric Shi ,  Michael Xia ,  Changsheng Zheng ,  Jiacheng Zhou ,  Qun Li

IPC: C07D401/14

CPC classification number: C07D401/14 ,  A61K31/4545 ,  C07B2200/13 ,  C07D401/12 ,  C07F7/1804

Abstract: The present invention relates to salt forms of the Pim kinase 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, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.

公开(公告)号：US20250051328A1

公开(公告)日：2025-02-13

申请号：US18671458

申请日：2024-05-22

Applicant: Incyte Corporation

Inventor： Zhongjiang Jia ,  Jiacheng Zhou ,  Qun Li

IPC: C07D471/14 ,  A61P35/00

Abstract: The present invention relates to salt forms of the Fibroblast Growth Factor Receptors (FGFR) inhibitor 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3′,2′:5,6]pyrido[4,3-d] pyrimidin-2-one, including methods of preparation thereof, where the compound is useful in the treatment of FGFR mediated diseases such as cancer.

公开(公告)号：US12043614B2

公开(公告)日：2024-07-23

申请号：US17981887

申请日：2022-11-07

Applicant: Incyte Corporation

Inventor： Zhongjiang Jia ,  Ganfeng Cao ,  Qiyan Lin ,  Yongchun Pan ,  Lei Qiao ,  Vaqar Sharief ,  Chongsheng Eric Shi ,  Michael Xia ,  Changsheng Zheng ,  Jiacheng Zhou ,  Qun Li

IPC: C07D401/14 ,  A61K31/4545 ,  C07D401/12 ,  C07F7/18

CPC classification number: C07D401/14 ,  A61K31/4545 ,  C07D401/12 ,  C07F7/1804 ,  C07B2200/13

Abstract: The present invention relates to salt forms of the Pim kinase 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, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.

公开(公告)号：US11753406B2

公开(公告)日：2023-09-12

申请号：US16987557

申请日：2020-08-07

Applicant: Incyte Corporation

Inventor： Zhongjiang Jia ,  Pingli Liu ,  David J. Meloni ,  Yongchun Pan ,  Yongzhong Wu ,  Jiacheng Zhou ,  Qun Li

IPC: C07D471/04 ,  A61K9/00

CPC classification number: C07D471/04 ,  A61K9/0053 ,  C07B2200/13

Abstract: The present invention relates to salt 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, where the compound is useful in the treatment of various diseases including infectious diseases and cancer.

公开(公告)号：US11512064B2

公开(公告)日：2022-11-29

申请号：US17200082

申请日：2021-03-12

Applicant: Incyte Corporation

Inventor： Zhongjiang Jia ,  Wayne Han ,  Yongchun Pan ,  Timothy Martin ,  Jiacheng Zhou ,  Qun Li

IPC: C07D401/04 ,  A61K9/00

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).

公开(公告)号：US11001571B2

公开(公告)日：2021-05-11

申请号：US16555620

申请日：2019-08-29

Applicant: Incyte Corporation

Inventor： Yun-Long Li ,  Jincong Zhuo ,  Ding-Quan Qian ,  Song Mei ,  Ganfeng Cao ,  Yongchun Pan ,  Qun Li ,  Zhongjiang Jia

IPC: C07D403/14 ,  A61P37/06

Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit 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.

公开(公告)号：US20200071289A1

公开(公告)日：2020-03-05

申请号：US16555907

申请日：2019-08-29

Applicant: Incyte Corporation

Inventor： Zhongjiang Jia ,  Wayne Han ,  Yongchun Pan ,  Timothy Martin ,  Jiacheng Zhou ,  Qun Li

IPC: C07D401/04 ,  A61K9/00

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).