公开(公告)号：WO2022099071A1

公开(公告)日：2022-05-12

申请号：PCT/US2021/058334

申请日：2021-11-05

申请人： INCYTE CORPORATION

发明人： WANG, Dengjin ,  CARPER, Daniel ,  JIA, Zhongjiang ,  SHEN, Bo ,  SCLAFANI, Joseph A. ,  WILSON, Robert ,  ZHOU, Jiacheng ,  SULEIMAN, Osama ,  WRIGHT, Mark

IPC分类号： C07D413/14 ,  C07C237/46 ,  C07C255/53 ,  C07C255/60 ,  C07D211/34 ,  C07D471/04

摘要： 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.

公开(公告)号：WO2019213544A3

公开(公告)日：2019-11-07

申请号：PCT/US2019/030633

申请日：2019-05-03

申请人： INCYTE CORPORATION

发明人： BURN, Timothy C. ,  LIU, Phillip C. ,  FRIETZE, William ,  JIA, Zhongjiang ,  TAO, Ming ,  WANG, Dengjin ,  ZHOU, Jiacheng ,  LI, Qun

IPC分类号： C07D471/14 ,  A61K31/519 ,  A61P35/00

摘要： The present disclosure relates to solid forms and polymorphs of compound (1): 3-(2,6-difluoro-3,5-dimethoxyphenyl) -l-ethyl-8-(morpholin-4-ylmethyl)-l,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one, 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：WO2019213544A2

公开(公告)日：2019-11-07

申请号：PCT/US2019/030633

申请日：2019-05-03

申请人： INCYTE CORPORATION

发明人： BURN, Timothy C. ,  LIU, Phillip C. ,  FRIETZE, William ,  JIA, Zhongjiang ,  TAO, Ming ,  WANG, Dengjin ,  ZHOU, Jiacheng ,  LI, Qun

IPC分类号： C07D471/14 ,  A61K31/519 ,  A61P35/00

摘要： 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：WO2015168246A1

公开(公告)日：2015-11-05

申请号：PCT/US2015/028224

申请日：2015-04-29

申请人： INCYTE CORPORATION

发明人： ZHOU, Jiacheng ,  LIU, Pingli ,  CHEN, Shili ,  WU, Yongzhong ,  WANG, Dengjin ,  JIA, Zhongjiang ,  QIAO, Lei ,  FRIETZE, William ,  XIA, Michael ,  DAI, Yingrui

IPC分类号： C07D495/14 ,  A61K31/437 ,  A61P25/00 ,  A61P35/00 ,  A61P37/00

CPC分类号： C07D495/14 ,  C07D309/14 ,  C07D495/04

摘要： This invention relates to processes for preparing a JAKl inhibitor having Formula la: as well as new forms of the inhibitor.

摘要翻译： 本发明涉及制备具有式Ia的JAK1抑制剂的方法：以及抑制剂的新形式。

公开(公告)号：WO2019152374A1

公开(公告)日：2019-08-08

申请号：PCT/US2019/015582

申请日：2019-01-29

申请人： INCYTE CORPORATION

发明人： WANG, Dengjin ,  LIU, Pingli ,  WU, Yongzhong ,  ZHOU, Jiacheng

IPC分类号： C07D401/04 ,  C07D213/61

CPC分类号： C07D401/06 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P27/02 ,  A61P35/00 ,  C07D213/61 ,  C07D213/803 ,  C07D401/04 ,  C07D487/04

摘要： This invention relates to processes and intermediates for making {1- {l-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H- pyrrolo[2,3-d]pyrimidin-4-yl)-IH-pyrazol-l-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. The invention is specifically directed to processes for making the intermediate (l-(3-fluoro-2- (trifluoromethyl)isonicotinyl)piperidine-4-one) from l-(3-fluoro-2- (trifluoromethyl)isonicotinoyl chloride and 4-hydroxypiperidine or 4- piperidone as well as to the intermediate l-(3-fluoro-2-(trifluoromethyl)isonicotinoyl chloride.

公开(公告)号：WO2018218100A1

公开(公告)日：2018-11-29

申请号：PCT/US2018/034559

申请日：2018-05-25

申请人： INCYTE CORPORATION

发明人： PAN, Yongchun ,  SHI, Chongsheng Eric ,  TAO, Ming ,  HAN, Wayne ,  XIA, Michael ,  WANG, Dengjin ,  JIA, Zhongjiang ,  ZHOU, Jiacheng ,  LI, Qun

IPC分类号： C07D471/04 ,  A61K31/438 ,  A61P35/00

摘要： The present disclosure relates to solid forms of N-{[2'-(2,6-difluoro-3,5-dimethoxyphenyl)-3'-oxo-2',3'-dihydro-1'H-spiro[cyclopropane-1,4'-[2,7]naphthyridin]-6'-yl]methyl}acrylamide, 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：WO2014138168A1

公开(公告)日：2014-09-12

申请号：PCT/US2014/020554

申请日：2014-03-05

申请人： INCYTE CORPORATION

发明人： LIU, Pingli ,  WANG, Dengjin ,  WU, Yongzhong ,  CAO, Ganfeng ,  XIA, Michael

IPC分类号： C07D487/04 ,  C07F5/04 ,  C07D401/14

CPC分类号： C07D401/14 ,  C07D403/14 ,  C07D487/04 ,  C07F5/025 ,  C07F5/04

摘要： 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.

摘要翻译： 本发明涉及制备{1- {1- [3-氟-2-（三氟甲基）异烟酰基]哌啶-4-基} -3- [4-（7H-吡咯并[2,3-d] 嘧啶-4-基）-1H-吡唑-1-基]氮杂环丁烷-3-基}乙腈，可用于治疗与包括炎症性疾病，自身免疫性疾病，癌症等的Janus激酶（JAK）的活性相关的疾病 疾病。