公开(公告)号：US20240287100A1

公开(公告)日：2024-08-29

申请号：US18411493

申请日：2024-01-12

申请人： NIKANG THERAPEUTICS, INC. ,  SHANGHAI BLUERAY BIOPHARMA CO., LTD.

发明人： Jiping FU ,  Yan LOU ,  Yongfeng SUN

IPC分类号： C07D519/00 ,  A61K31/519 ,  A61K45/06

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K45/06

摘要： The present disclosure provides certain alkylidenyl derivatives that inhibit certain K-Ras proteins and are therefore useful for the treatment of cancers mediated by such proteins. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US20230303509A1

公开(公告)日：2023-09-28

申请号：US18189380

申请日：2023-03-24

申请人： NiKang Therapeutics, Inc.

发明人： Yan LOU

IPC分类号： C07D331/04 ,  A61P35/00

CPC分类号： C07D331/04 ,  A61P35/00

摘要： The present disclosure provides certain sulfonamido derivatives that are Cyclin-dependent kinase 2 (CDK2) inhibitors of Formula (I):




for the treatment of diseases treatable by inhibition of CDK2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US20230115881A1

公开(公告)日：2023-04-13

申请号：US17963926

申请日：2022-10-11

申请人： NiKang Therapeutics, Inc.

发明人： Charles M. COOK ,  Jiping FU ,  Yigang HE ,  Yan LOU ,  Rongzhen CHEN ,  Yan DONG

IPC分类号： C07C255/54 ,  C07C253/34 ,  A61K9/20 ,  A61K9/48 ,  A61K9/00 ,  A61K47/26 ,  A61K47/38 ,  A61K47/12 ,  A61K9/06 ,  A61K47/10 ,  A61K47/14 ,  C07C253/30 ,  A61K9/08

摘要： The present disclosure provides certain processes of making 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)-benzonitrile (Compound 1) and certain polymorphs thereof. Also provided are pharmaceutical compositions comprising a crystalline polymorph form of Compound 1 and processes for preparing such polymorph forms.

公开(公告)号：US20220162158A1

公开(公告)日：2022-05-26

申请号：US17670423

申请日：2022-02-11

申请人： NIKANG THERAPEUTICS, INC.

发明人： Jiping FU ,  Yan LOU ,  Yigang HE

IPC分类号： C07C255/54 ,  A61P35/00 ,  C07C313/06 ,  C07D213/63 ,  C07D233/60

摘要： The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US11420936B2

公开(公告)日：2022-08-23

申请号：US17686385

申请日：2022-03-03

申请人： NIKANG THERAPEUTICS, INC.

发明人： Jiping Fu ,  Yan Lou ,  Yigang He

IPC分类号： C07C255/54 ,  A61P35/00

摘要： The present disclosure is directed certain Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and their use in the treatment of diseases mediated by HIF-2α such as cancer. Also provided is the use of HIF-2α inhibitors in combination with a poly (ADP-ribose) polymerase (PARP) inhibitor. In particular, the present disclosure is directed to methods for the treatment of cancers using a HIF-2α inhibitor in combination with a PARP inhibitor and pharmaceutical compositions comprising the same.

公开(公告)号：US20220177487A1

公开(公告)日：2022-06-09

申请号：US17600587

申请日：2020-03-31

申请人： NIKANG THERAPEUTICS, INC.

发明人： Jiping FU ,  Yigang HE ,  Yan LOU

IPC分类号： C07D491/22 ,  C07D471/22 ,  A61K45/06 ,  A61P31/16

摘要： Provided are compounds of Formula (IA) that inhibit orthomyxovirus replication such as Influenza viruses and are accordingly useful for treatment of viral infections caused by orthomyxoviruses. Also provided are pharmaceutical compositions containing these compounds and methods of using these compounds to treat or prevent viral infections caused by orthomyxovirus such as Influenza viruses.

公开(公告)号：US20220119345A1

公开(公告)日：2022-04-21

申请号：US17503176

申请日：2021-10-15

申请人： Nikang Therapeutics, Inc.

发明人： Jiping FU ,  Yan LOU ,  Yigang HE ,  Yuetao SHI ,  Peng ZHOU ,  Xingxing LI

IPC分类号： C07C253/30 ,  C07C45/27 ,  C07C29/00 ,  C07C29/143 ,  C07C45/66 ,  C07C67/307 ,  C07C45/00 ,  C07C67/343

摘要： Disclosed herein are processes for preparing certain intermediates useful in the synthesis of 3-fluoro-5-(((1S,2aR)-1,3,3,4,4-pentafluoro-2a-hydroxy-2,2a,3,4-tetrahydro-1H-cyclopenta[cd]inden-7-yl)oxy)benzonitrile or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20210380536A1

公开(公告)日：2021-12-09

申请号：US17286818

申请日：2019-10-16

申请人： NiKang Therapeutics, Inc.

发明人： Jiping FU ,  Yan LOU ,  Yigang HE

IPC分类号： C07D221/04 ,  C07C255/54 ,  C07D213/85 ,  C07D213/65 ,  C07C43/295 ,  A61K45/06

摘要： The present disclosure provides certain indane compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US20210347729A1

公开(公告)日：2021-11-11

申请号：US17377356

申请日：2021-07-15

申请人： Nikang Therapeutics, Inc.

发明人： Jiping FU ,  Yan Lou ,  Yigang He

IPC分类号： C07C255/54 ,  A61P35/00 ,  C07C313/06 ,  C07D213/63 ,  C07D233/60

摘要： The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US12077506B2

公开(公告)日：2024-09-03

申请号：US17286818

申请日：2019-10-16

申请人： NiKang Therapeutics, Inc.

发明人： Jiping Fu ,  Yan Lou ,  Yigang He

IPC分类号： C07D221/04 ,  A61K45/06 ,  C07C43/295 ,  C07C255/54 ,  C07D213/65 ,  C07D213/85

CPC分类号： C07D221/04 ,  A61K45/06 ,  C07C43/295 ,  C07C255/54 ,  C07D213/65 ,  C07D213/85 ,  C07B2200/05

摘要： The present disclosure provides certain indane compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.