[EN] BIFUNCTIONAL COMPOUNDS FOR THE TREATMENT OF CANCER<br/>[FR] COMPOSÉS BIFONCTIONNELS POUR LE TRAITEMENT DU CANCER
申请人:HOFFMANN LA ROCHE
公开号:WO2021083949A1
公开(公告)日:2021-05-06
The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).
[EN] PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND METHODS OF USE THEREOF<br/>[FR] AGENTS DE DÉGRADATION DE PROTÉINE TYROSINE PHOSPHATASE ET LEURS MÉTHODES D'UTILISATION
申请人:CALICO LIFE SCIENCES LLC
公开号:WO2021127586A1
公开(公告)日:2021-06-24
Provided herein are compounds, compositions, and methods useful for degrading protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer 5 or a metabolic disease.
[EN] N/O-LINKED DEGRONS AND DEGRONIMERS FOR PROTEIN DEGRADATION<br/>[FR] DÉGRONS ET DÉGRONIMÈRES À LIAISON N/O POUR LA DÉGRADATION DE PROTÉINES
申请人:C4 THERAPEUTICS INC
公开号:WO2018237026A1
公开(公告)日:2018-12-27
This invention provides Degronimers that have E3 Ubiquitin Ligase targeting moieties (Degrons) that can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation. The invention also provides Degrons that can be used to treat disorders mediated by cereblon or an Ikaros family protein, and methods of use and compositions thereof as well as methods for their preparation.
[EN] COMPOUND FOR TARGETING AND DEGRADING PROTEIN, AND PREPARATION METHOD THEREFOR AND USE THEREOF<br/>[FR] COMPOSÉ PERMETTANT DE CIBLER ET DE DÉGRADER UNE PROTÉINE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION<br/>[ZH] 靶向蛋白降解化合物及其制备方法和应用
A herbicidal composition which comprises at least one carrier and, as active ingredient, a compound of the general formula ##STR1## in which each of n and m independently is 0 or 1; each of Ar.sup.1 and Ar.sup.2 independently is an aryl group, at least one of Ar.sup.1 and Ar.sup.2 being substituted by one or more of the same or different substituents selected from halogen atoms, alkyl groups, alkoxy groups, haloalkyl groups and haloalkoxy groups; and R.sup.1 is hydrogen, or an alkyl, alkylthio or haloalkyl group having from 1 to 4 carbon atoms, and R.sup.2 is hydrogen or a halogen atom provided that at least one of R.sup.1 and R.sup.2 represents a hydrogen atom. Certain compounds of formula I are novel.