公开(公告)号：US10662186B2

公开(公告)日：2020-05-26

申请号：US16067158

申请日：2016-12-30

Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.

Inventor： Guangxin Xia ,  Qian Wang ,  Chen Shi ,  Xiong Zhai ,  Hui Ge ,  Xuemei Liao ,  Yu Mao ,  Zhixiong Xiang ,  Yanan Han ,  Guoyong Huo ,  Yanjun Liu

IPC: A61K31/506 ,  C07D239/30 ,  C07D471/04 ,  A61P35/00 ,  C07F5/02 ,  C07F7/08 ,  C07F9/6561 ,  C07F9/6584

Abstract: The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.

公开(公告)号：US20240317686A1

公开(公告)日：2024-09-26

申请号：US18270664

申请日：2021-12-29

Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.

Inventor： Qian Wang ,  Bingbin Zhang ,  Guangxin Xia ,  Sijie Shu ,  Guoyong Huo ,  Zhijun Xiang ,  Guosheng Wu ,  Tao Liang ,  Chen Shi ,  Yongxin Zhao ,  Lingwen Li ,  Ying Ke

IPC: C07D213/75 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

CPC classification number: C07D213/75 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

Abstract: Provided are an RORγt modulator, and a preparation method therefor and an application thereof. The RORγt modulator is selected from a compound represented by formula I, and a pharmaceutically acceptable salt, solvate, solvate of pharmaceutically acceptable salt, metabolite or prodrug thereof. The compound has inhibitory activity on RORγt, and can effectively inhibit an RORγt protein receptor, thereby regulating the differentiation of Th17 cells, inhibiting generation of IL-17, and then treating RORγt-mediated relevant autoimmune diseases.

公开(公告)号：US10988476B2

公开(公告)日：2021-04-27

申请号：US16848942

申请日：2020-04-15

Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.

Inventor： Guangxin Xia ,  Qian Wang ,  Chen Shi ,  Xiong Zhai ,  Hui Ge ,  Xuemei Liao ,  Yu Mao ,  Zhixiong Xiang ,  Yanan Han ,  Guoyong Huo ,  Yanjun Liu

IPC: A61K31/506 ,  C07D239/30 ,  C07D471/04 ,  A61P35/00 ,  C07F5/02 ,  C07F7/08 ,  C07F9/6561 ,  C07F9/6584

Abstract: The present invention discloses a substituted pyridine compound represented by formula I, and a pharmaceutically acceptable salt, stereoisomer and tautomer thereof. The compounds of the present invention are useful in the treatment of cancers.