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1. 发明申请

WO2021007269A1 BICYCLIC HETEROCYCLES AS FGFR INHIBITORS 审中-公开
公开(公告)号：WO2021007269A1
公开(公告)日：2021-01-14
申请号：PCT/US2020/041104
申请日：2020-07-08
申请人： INCYTE CORPORATION
发明人： VECHORKIN, Oleg , QI, Chao , NGUYEN, Minh , WANG, Anlai , YAO, Wenqing
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P35/00
摘要： The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 enzyme and are useful in the treatment of FGFR3-associated diseases such as cancer, Formula (I).

2. 发明申请

WO2014113388A1 THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS 审中-公开
标题翻译：作为PIM激酶抑制剂有用的噻唑并恶唑和吡啶甲酰胺化合物
公开(公告)号：WO2014113388A1
公开(公告)日：2014-07-24
申请号：PCT/US2014/011486
申请日：2014-01-14
申请人： INCYTE CORPORATION
发明人： XUE, Chu-Biao , LI, Yun-Long , FENG, Hao , PAN, Jun , WANG, Anlai , ZHANG, Ke , YAO, Wenqing , ZHANG, Fenglei , ZHUO, Jincong
IPC分类号： C07D401/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , A61K31/4355 , A61K31/4365 , A61K31/4427 , A61K31/4709 , A61K31/497 , A61P35/00
CPC分类号： A61K31/444 , C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The present disclosure describes thiazole and pyridine carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is C or N; A, B and D are rings; the bond— represents a normalized bond within the aromatic ring containing both an N and X, which formally is represented by a C=C bond when X is C and a single bond when X is N; ring A is of the formula (A-l) or (A-2): wherein El and E2 are rings; their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
摘要翻译：本公开描述了式（I）的噻唑和吡啶甲酰胺衍生物或其药学上可接受的盐，其中：X是C或N; A，B和D是环; 该键 - 表示包含N和X的芳环中的归一化键，当X是C时，正式地由C = C键表示，当X是N时，其表示单键; 环A具有式（A-1）或（A-2）：其中E1和E2是环; 它们的组成和使用方法。所述化合物抑制Pim激酶的活性，并且可用于治疗与Pim激酶的活性相关的疾病，包括例如癌症和其它疾病。

3. 发明申请

WO2007150025A2 PURINONE DERIVATIVES AS HM74A AGONISTS 审中-公开
标题翻译：作为HM74A激动剂的嘌呤衍生物
公开(公告)号：WO2007150025A2
公开(公告)日：2007-12-27
申请号：PCT/US2007/071891
申请日：2007-06-22
申请人： INCYTE CORPORATION , ZHENG, Changsheng , XUE, Chu-Biao , CAO, Ganfeng , XIA, Michael , WANG, Anlai , YE, Hai, Fen , METCALF, Brian
发明人： ZHENG, Changsheng , XUE, Chu-Biao , CAO, Ganfeng , XIA, Michael , WANG, Anlai , YE, Hai, Fen , METCALF, Brian
CPC分类号： C07D487/14
摘要： The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.
摘要翻译：本发明涉及作为HM74a受体激动剂的嘌呤酮衍生物。进一步提供了使用本文化合物及其可药用盐治疗疾病的组合物和方法。

4. 发明申请

WO2016196244A1 PYRIDINEAMINE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS 审中-公开
标题翻译：吡啶胺化合物可用作PIM激酶抑制剂
公开(公告)号：WO2016196244A1
公开(公告)日：2016-12-08
申请号：PCT/US2016/034520
申请日：2016-05-27
申请人： INCYTE CORPORATION
发明人： VECHORKIN, Oleg , FENG, Hao , LI, Yun-Long , MEI, Song , WANG, Anlai , ZHU, Wenyu , ZHUO, Jincong
IPC分类号： C07D401/14 , C07D213/74 , C07D401/04 , C07D417/14 , C07D471/04 , C07D491/048 , A61P35/00 , A61P37/00 , A61K31/444
CPC分类号： C07D401/14 , C07D213/74 , C07D401/04 , C07D401/12 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present disclosure describes pyridineamine compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer, immune disorders and other diseases. Formula (I).
摘要翻译：本公开内容描述吡啶胺化合物及其组合物和使用方法。所述化合物抑制Pim激酶的活性，并且可用于治疗与Pim激酶活性相关的疾病，包括例如癌症，免疫疾病和其它疾病。式（I）。

5. 发明申请

WO2013056015A1 ISOINDOLINONE AND PYRROLOPYRIDINONE DERIVATIVES AS AKT INHIBITORS 审中-公开
标题翻译：作为AKT抑制剂的异吲哚酮和吡咯烷酮衍生物
公开(公告)号：WO2013056015A1
公开(公告)日：2013-04-18
申请号：PCT/US2012/059905
申请日：2012-10-12
申请人： INCYTE CORPORATION
发明人： HUANG, Taisheng , FENG, Hao , KONG, Lingquan , WANG, Anlai , YE, Hai Fen , XUE, Chu-Biao
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D417/14 , C07D471/02 , C07D487/02 , A61K31/4155 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D409/14 , C07D417/14 , C07D471/02 , C07D487/02
摘要： The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.
摘要翻译：本发明提供异吲哚啉酮和吡咯并吡喃酮衍生物及其组合物和使用方法，其抑制丝氨酸/苏氨酸激酶Akt的活性，并且可用于治疗与Akt活性相关的疾病，包括例如，癌症等疾病。

6. 发明申请

WO2011112662A1 PIPERIDIN-4-YL AZETIDINE DERIVATIVES AS JAK1 INHIBITORS 审中-公开
标题翻译：作为JAK1抑制剂的哌啶-4-基亚氨基衍生物
公开(公告)号：WO2011112662A1
公开(公告)日：2011-09-15
申请号：PCT/US2011/027665
申请日：2011-03-09
申请人： INCYTE CORPORATION , HUANG, Taisheng , XUE, Chu-Biao , WANG, Anlai , KONG, Ling , YE, Hai Fen , YAO, Wenqing , RODGERS, James D. , SHEPARD, Stacey , WANG, Haisheng , SHAO, Lixin , LI, Hui-Yin , LI, Qun
发明人： HUANG, Taisheng , XUE, Chu-Biao , WANG, Anlai , KONG, Ling , YE, Hai Fen , YAO, Wenqing , RODGERS, James D. , SHEPARD, Stacey , WANG, Haisheng , SHAO, Lixin , LI, Hui-Yin , LI, Qun
IPC分类号： C07D401/14 , C07D405/14 , A61K31/4155 , A61K31/437 , A61K31/4468 , A61P29/00
CPC分类号： A61K31/4545 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/0048 , A61K31/519 , A61P1/00 , A61P11/00 , A61P11/06 , A61P27/02 , A61P35/00 , C07B2200/13 , C07D401/14 , C07D405/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要： 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.
摘要翻译：本发明提供哌啶-4-基氮杂环丁烷衍生物及其组合物和使用方法，其调节Janus激酶1（JAK1）的活性，并且可用于治疗与JAK1的活性相关的疾病，包括对于例如炎症性疾病，自身免疫性疾病，癌症和其它疾病。

7. 发明申请

WO2021076602A1 BICYCLIC HETEROCYCLES AS FGFR INHIBITORS 审中-公开
公开(公告)号：WO2021076602A1
公开(公告)日：2021-04-22
申请号：PCT/US2020/055547
申请日：2020-10-14
申请人： INCYTE CORPORATION , XU, Yao
发明人： VECHORKIN, Oleg , NGUYEN, Minh , QI, Chao , WANG, Anlai , WITTEN, Michael , YE, Hai FEN , ZHANG, Ke , ZHAO, Peng , YAO, Wenqing
IPC分类号： A61P35/00 , C07D471/04 , A61K31/437
摘要： The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR enzyme and are useful in the treatment of FGFR-associated diseases such as cancer. Formula (I).

8. 发明申请

WO2019164847A1 INDAZOLE COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2019164847A1
公开(公告)日：2019-08-29
申请号：PCT/US2019/018609
申请日：2019-02-19
申请人： INCYTE CORPORATION
发明人： SOKOLSKY, Alexander , VECHORKIN, Oleg , WANG, Anlai , YE, Qinda , YAO, Wenqing
IPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D471/08 , C07D487/08 , C07D487/10 , A61K31/506 , A61P35/00
摘要： Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.

9. 发明申请

WO2015027124A1 FURO- AND THIENO-PYRIDINE CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS 审中-公开
标题翻译：作为PIM激酶抑制剂有用的呋喃和三苯基吡啶酰胺化合物
公开(公告)号：WO2015027124A1
公开(公告)日：2015-02-26
申请号：PCT/US2014/052214
申请日：2014-08-22
申请人： INCYTE CORPORATION
发明人： LI, Yun-Long , BURNS, David M. , FENG, Hao , HUANG, Taisheng , MEI, Song , PAN, Jun , VECHORKIN, Oleg , YE, Hai Fen , ZHU, Wenyu , RAFALSKI, Maria , WANG, Anlai , XUE, Chu-Biao
IPC分类号： C07D491/048 , C07D495/04 , A61K31/4355 , A61K31/4365 , A61K31/5025 , A61P35/00 , A61P37/02 , A61P37/08 , A61P9/10
CPC分类号： C07D495/04 , C07D491/048
摘要： The present disclosure describes furo-and thieno-pyridine carboxamide compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: X is S or 0; A 5 is N or C-R 5 . Cy A is a 5 to 6 membered monocyclic heteroaryl group, wherein the ring atoms of the heteroaryl group forming Cy A consist of carbon atoms and 1, 2, or 3 heteroatoms selected from N, 0 and S, and wherein the 5 to 6 membered monocyclic heteroaryl group forming Cy A is unsubstituted or substituted with 1, 2, or 3 R A ; Cy B is C 6-10 aryl, C 3-7 cycloalkyl, 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl wherein the ring atoms of the ring atoms of the heteroaryl or heterocycloalkyl forming Cy B consist of carbon atoms and 1, 2 or 3 heteroatoms selected from 0, N and S, and wherein each of said C 6-10 aryl, C 3-7 cycloalkyl, 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl forming Cy B is unsubstituted or substituted with 1, 2, 3, 4 or 5 R B ; R 2 is H, halogen or NH 2 ; and R 5 , R 6 and R 7 are as defined in claim 1; The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
摘要翻译：本公开描述了式（I）的呋喃并噻吩并吡啶甲酰胺化合物或其药学上可接受的盐，其中：X为S或0; A5是N或C-R5。 CyA是5至6元单环杂芳基，其中形成CyA的杂芳基的环原子由碳原子和1,2或3个选自N，O和S的杂原子组成，其中5至6元单环杂芳基基团形成CyA未被取代或被1,2或3个RA取代; CyB是C6-10芳基，C3-7环烷基，5-10元杂芳基或4-10元杂环烷基，其中形成CyB的杂芳基或杂环烷基的环原子的环原子由碳原子和1,2或3个选自0的杂原子组成，N和S，并且其中形成CyB的所述C6-10芳基，C3-7环烷基，5-10元杂芳基或4-10元杂环烷基中的每一个是未取代的或被1,2,3,4或5个RB取代; R2是H，卤素或NH2; R5，R6和R7如权利要求1所定义; 该化合物抑制Pim激酶的活性，并且可用于治疗与Pim激酶活性相关的疾病，包括例如癌症和其它疾病。

10. 发明申请

WO2014110574A1 BICYCLIC AROMATIC CARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS 审中-公开
标题翻译：双相芳族羧酰胺化合物有用作PIM激酶抑制剂
公开(公告)号：WO2014110574A1
公开(公告)日：2014-07-17
申请号：PCT/US2014/011487
申请日：2014-01-14
申请人： INCYTE CORPORATION
发明人： LI, Yun-Long , BURNS, David M. , FENG, Hao , XUE, Chu-Biao , WANG, Anlai , PAN, Jun
IPC分类号： C07D401/14 , C07D471/04 , C07D491/048 , A61K31/444 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D491/048 , C07D498/04 , C07D498/22
摘要： The present disclosure describes bicyclic aromatic carboxamide derivatives of formula (I), as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
摘要翻译：本公开描述了式（I）的双环芳族甲酰胺衍生物及其组合物和使用方法。该化合物抑制Pim激酶的活性，并且可用于治疗与Pim激酶活性相关的疾病，包括例如癌症和其它疾病。

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