公开(公告)号：US20230399331A1

公开(公告)日：2023-12-14

申请号：US18209674

申请日：2023-06-14

Applicant: Incyte Corporation

Inventor： Zhongjiang Jia ,  Weiguo Liu ,  Pingli Liu ,  David Meloni ,  Yongchun Pan ,  Jiacheng Zhou ,  Travis Houston

IPC: C07D487/04 ,  A61K9/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/36 ,  A61K47/06 ,  A61K47/44 ,  A61K47/32 ,  A61K47/18 ,  A61K47/26 ,  A61K9/107 ,  A61K9/20

CPC classification number: C07D487/04 ,  A61K9/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/36 ,  A61K47/06 ,  A61K47/44 ,  A61K47/32 ,  A61K47/183 ,  A61K47/26 ,  A61K9/107 ,  A61K9/2054 ,  A61K9/2018 ,  A61K9/2009 ,  A61K9/2013 ,  C07B2200/13

Abstract: The present disclosure is related to solid forms of ruxolitinib di-hydrate and ruxolitinib free base, process of preparing the same, and compositions comprising the same.

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：US20230192722A1

公开(公告)日：2023-06-22

申请号：US18085814

申请日：2022-12-21

Applicant: Incyte Corporation

Inventor： Pingli Liu ,  Zhongjiang Jia ,  Qiyan Lin ,  Naijing Su ,  Timothy Martin ,  Michael Xia ,  Jiacheng Zhou ,  Baoyu Mi

IPC: C07D519/00 ,  C07D471/04

CPC classification number: C07D519/00 ,  C07D471/04 ,  C07B2200/13

Abstract: The present invention relates to salts and solid forms of the FGFR inhibitor (7R,8aS)-2-(5-(5-(2,3-Dimethylphenyl)-6-methoxy-1H-pyrazolo[4,3-b]pyridin-3-yl)pyridin-2-yl)octahydropyrrolo[1,2-a]pyrazin-7-ol, including methods of preparation thereof, wherein the compounds, salts, and solid forms are useful in the treatment of FGFR-mediated diseases such as cancer.

公开(公告)号：US20220024934A1

公开(公告)日：2022-01-27

申请号：US17365888

申请日：2021-07-01

Applicant: Incyte Corporation

Inventor： Lei Qiao ,  Lingkai Weng ,  Chongsheng Eric Shi ,  David Meloni ,  Qiyan Lin ,  Michael Xia ,  Vaqar Sharief ,  William Frietze ,  Zhongjiang Jia ,  Yongchun Pan ,  Pingli Liu ,  Tai-Yuen Yue ,  Jiacheng Zhou

IPC: C07D487/04

Abstract: The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ), as well as a salt form and intermediates related thereto.

公开(公告)号：US20210030722A1

公开(公告)日：2021-02-04

申请号：US16849610

申请日：2020-04-15

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： Andrew P. Combs ,  Eddy W. Yue ,  Richard B. Sparks ,  Wenyu Zhu ,  Jiacheng Zhou ,  Qiyan Lin ,  Lingkai Weng ,  Tai-Yuen Yue ,  Pingli Liu

IPC: A61K31/4245 ,  C07D271/08 ,  A61K39/395 ,  C07D413/12 ,  C07D413/04

Abstract: 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.

公开(公告)号：US20170258800A1

公开(公告)日：2017-09-14

申请号：US15355630

申请日：2016-11-18

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： Lingkai Weng ,  Lei Qiao ,  Jiacheng Zhou ,  Pingli Liu ,  Yongchun Pan

IPC: A61K31/53 ,  C07D401/10 ,  C07D487/04 ,  C07D253/07

CPC classification number: A61K31/53 ,  C07D253/07 ,  C07D401/10 ,  C07D487/04

Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.

公开(公告)号：US20170121347A1

公开(公告)日：2017-05-04

申请号：US15337202

申请日：2016-10-28

Applicant: Incyte Corporation

Inventor： Shili Chen ,  William Frietze ,  Zhongjiang Jia ,  Pingli Liu ,  Jiacheng Zhou

IPC: C07D498/04 ,  C07D413/04

CPC classification number: C07D498/04 ,  A61K31/535 ,  C07D413/04

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.

公开(公告)号：US20160347734A1

公开(公告)日：2016-12-01

申请号：US14976583

申请日：2015-12-21

Applicant: Incyte Corporation ,  Incyte Holdings Corporation

Inventor： Pingli Liu ,  Dengjin Wang ,  Yongzhong Wu ,  Ganfeng Cao ,  Michael Xia

IPC: C07D401/14 ,  C07F5/02 ,  C07D403/14

CPC classification number: C07D401/14 ,  C07D403/14 ,  C07D487/04 ,  C07F5/025 ,  C07F5/04

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.

公开(公告)号：US20160257689A1

公开(公告)日：2016-09-08

申请号：US15054474

申请日：2016-02-26

Applicant: Incyte Corporation

Inventor： Lei Qiao ,  Lingkai Weng ,  ChongShen Eric Shi ,  David Meloni ,  Qiyan Lin ,  Michael Xia ,  Vaqar Sharief ,  William Frietze ,  Zhongjiang Jia ,  Yongchun Pan ,  Pingli Liu ,  Tai-Yuen Yue ,  Jiacheng Zhou

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07B2200/13

Abstract: The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ), as well as a salt form and intermediates related thereto.

Abstract translation: 本申请提供了制备（R）-4-（3 - （（S）-1-（4-氨基-3-甲基-1H-吡唑并[3,4-d]嘧啶-1-基）乙基） -5-氯-2-乙氧基-6-氟苯基）吡咯烷-2-酮，其可用作抑制剂磷酸肌醇3-激酶-δ（PI3Kδ），以及与其相关的盐形式和中间体。

公开(公告)号：US12024522B2

公开(公告)日：2024-07-02

申请号：US17365888

申请日：2021-07-01

Applicant: Incyte Corporation

Inventor： Lei Qiao ,  Lingkai Weng ,  Chongsheng Eric Shi ,  David Meloni ,  Qiyan Lin ,  Michael Xia ,  Vaqar Sharief ,  William Frietze ,  Zhongjiang Jia ,  Yongchun Pan ,  Pingli Liu ,  Tai-Yuen Yue ,  Jiacheng Zhou ,  Jianji Wang

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07B2200/13

Abstract: The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3Kδ), as well as a salt form and intermediates related thereto.