公开(公告)号：US20230167129A1

公开(公告)日：2023-06-01

申请号：US18045149

申请日：2022-10-08

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Bing Zhou ,  Wei Tang ,  Xiangbo Yang ,  Huimin Lu ,  Mengying Gao ,  Yaxi Yang ,  Huijin Feng

IPC: C07D513/04 ,  A61P37/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

CPC classification number: C07D513/04 ,  A61P37/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

Abstract: The present invention relates to a heterocyclic amide inhibiting RIP1 kinase and the use thereof, and specifically, to a compound of formula I, its pharmaceutically acceptable salts, stereoisomers, enantiomers, diastereomers, atropisomers, optical isomers, racemates, polymorphs, solvates or isotopically labeled compounds, a pharmaceutical composition comprising the compound, and the pharmaceutical use thereof. The compound is particularly effective for treatment of diseases or disorders mediated by RIP1 kinase.

公开(公告)号：US12145923B2

公开(公告)日：2024-11-19

申请号：US16967721

申请日：2019-02-03

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Yechun Xu ,  Hong Liu ,  Wei Tang ,  Xianglei Zhang ,  Zhanni Gu ,  Heng Li ,  Xu Han ,  Fenghua Zhu ,  Chunlan Feng ,  Guangyu Dong ,  Tiantian Chen ,  Wuyan Chen ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D401/14 ,  C07D217/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14

Abstract: Disclosed are a novel tetrahydroisoquinoline compound, a method for preparing intermediates thereof, a pharmaceutical composition thereof and the use thereof. The tetrahydroisoquinoline compound of the present invention has a good inhibitory effect on phosphodiesterase (PDE4), and can be used in the prevention, treatment or auxiliary treatment of multiple diseases associated with the activity or expression of phosphodiesterase, especially PDE4-associated immune and inflammatory diseases, such as psoriasis and arthritis.

公开(公告)号：US12065447B2

公开(公告)日：2024-08-20

申请号：US18045149

申请日：2022-10-08

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Bing Zhou ,  Wei Tang ,  Xiangbo Yang ,  Huimin Lu ,  Mengying Gao ,  Yaxi Yang ,  Huijin Feng

IPC: C07D513/04 ,  A61P37/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

CPC classification number: C07D513/04 ,  A61P37/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

Abstract: The present invention relates to a heterocyclic amide inhibiting RIP1 kinase and the use thereof, and specifically, to a compound of formula I, its pharmaceutically acceptable salts, stereoisomers, enantiomers, diastereomers, atropisomers, optical isomers, racemates, polymorphs, solvates or isotopically labeled compounds, a pharmaceutical composition comprising the compound, and the pharmaceutical use thereof. The compound is particularly effective for treatment of diseases or disorders mediated by RIP1 kinase.

公开(公告)号：US11498927B2

公开(公告)日：2022-11-15

申请号：US17289642

申请日：2019-10-08

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Bing Zhou ,  Wei Tang ,  Xiangbo Yang ,  Huimin Lu ,  Mengying Gao ,  Yaxi Yang ,  Huijin Feng

IPC: C07D513/04 ,  A61P37/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

Abstract: The present invention relates to a heterocyclic amide inhibiting RIP1 kinase and the use thereof, and specifically, to a compound of formula I, its pharmaceutically acceptable salts, stereoisomers, enantiomers, diastereomers, atropisomers, optical isomers, racemates, polymorphs, solvates or isotopically labeled compounds, a pharmaceutical composition comprising the compound, and the pharmaceutical use thereof. The compound is particularly effective for treatment of diseases or disorders mediated by RIP1 kinase.

公开(公告)号：US11045475B2

公开(公告)日：2021-06-29

申请号：US16314024

申请日：2017-06-29

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  NINGBO ZIYUAN PHARMACEUTICALS INC.

Inventor： Jianping Zuo ,  Wei Tang ,  Zemin Lin ,  Chongsheng Yuan

IPC: A01N37/00 ,  A61K31/215 ,  A01N37/12 ,  A01N37/44 ,  A61K31/24 ,  A01N25/00 ,  A61K31/52 ,  A61P17/06 ,  A61P17/00 ,  A61K9/00 ,  A61K9/06 ,  A61K47/42

Abstract: Provided in the present invention is a use of methyl 4-[9-(6-aminopuryl)]-2(s)-hydroxybutyrate in the preparation of a medicament for treating psoriasis and vitiligo. More specifically, the present invention uses mice whose psoriasis is induced by an imiquimod cream to observe a changing condition in skin lesions on the psoriasis-like mice, according to a psoriasis skin lesion area of the mice and grading standards for disease severity; the present invention also observes a proportion of lymphocytes in the spleens and cytokines in skin lesion tissues of the mice. A good therapeutic effect may be obtained by treating typical cases of vitiligo with an ointment of methyl 4-[9-(6-aminopuryl)]-2(s)-hydroxybutyrate. Results show that methyl 4-[9-(6-aminopuryl)]-2(s)-hydroxybutyrate used in the present invention has a good therapeutic effect on psoriasis and vitiligo, as well as a favorable prospect in clinical application.