[EN] PSMA-TARGETING AMANITIN CONJUGATES<br/>[FR] CONJUGUÉS D'AMANITINE CIBLANT LE PSMA
申请人:HEIDELBERG PHARMA RES GMBH
公开号:WO2019057964A1
公开(公告)日:2019-03-28
The invention relates to a PSMA-targeting conjugate comprising (a) an amatoxin; (b) a small molecule PSMA-targeting moiety; and (c) optionally a linker linking said amatoxin and said small molecule PSMA-targeting moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate.
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
申请人:Arvinas, Inc.
公开号:US20190151295A1
公开(公告)日:2019-05-23
The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
[EN] FARNESOID X RECEPTOR AGONISTS AND USES THEREOF<br/>[FR] AGONISTES DU RÉCEPTEUR FARNÉSOÏDE X ET LEURS UTILISATIONS
申请人:METACRINE INC
公开号:WO2018170166A1
公开(公告)日:2018-09-20
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
[EN] A THIONATION PROCESS AND A THIONATING AGENT<br/>[FR] PROCÉDÉ DE THIONATION ET AGENT DE THIONATION
申请人:VIRONOVA AB
公开号:WO2012104415A1
公开(公告)日:2012-08-09
A process for transforming a group >C=O (I) in a compound into a group >C=S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5·2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5·2 C5H5N