[EN] SMALL MOLECULE ANDROGEN RECEPTOR PROTEIN DEGRADERS<br/>[FR] AGENTS DE DÉGRADATION DES PROTÉINES DU RÉCEPTEUR DES ANDROGÈNES À PETITES MOLÉCULES
申请人:UNIV MICHIGAN REGENTS
公开号:WO2022011204A1
公开(公告)日:2022-01-13
The present disclosure provides compounds represented by Formula I: A-L-B1 I, and the salts or solvates thereof, wherein A, L, and B1 are as defined in the specification. Compounds having Formula I are androgen receptor degraders useful for the treatment of cancer and other diseases.
The present invention is directed to a new class of 4-cycloalkoxy benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.
[EN] ANDROGEN RECEPTOR PROTEIN DEGRADERS<br/>[FR] AGENTS DE DÉGRADATION DE PROTÉINE DE RÉCEPTEUR DES ANDROGÈNES
申请人:UNIV MICHIGAN REGENTS
公开号:WO2022011205A1
公开(公告)日:2022-01-13
The present disclosure provides compounds represented by Formula I: A-L-B1 and the salts or solvates thereof, wherein A, L, and B1 are as defined in the specification. Compounds having Formula I are androgen receptor degraders useful for the treatment of cancer and other diseases.
[EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR PROTEIN<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION CIBLÉE DE PROTÉINE DU RÉCEPTEUR DES ANDROGÈNES
申请人:ARVINAS OPERATIONS INC
公开号:WO2022087125A1
公开(公告)日:2022-04-28
Bifunctional compounds, which find utility as modulators of androgen receptor (AR), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds AR, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
The present invention is directed to a new class of 4-cycloalkoxy benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.