BRM TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
申请人:Arvinas Operations, Inc.
公开号:US20190300521A1
公开(公告)日:2019-10-03
The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau 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] DISUBSTITUTED OCTAHY-DROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS<br/>[FR] OCTAHYDROPYRROLO [3,4-C] PYRROLES DISUBSTITUÉS UTILISÉS COMME MODULATEURS DU RÉCEPTEUR DE L'OREXINE
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2012145581A1
公开(公告)日:2012-10-26
Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
[EN] METHODS FOR TREATING NEUROLOGICAL SYMPTOMS ASSOCIATED WITH LYSOSOMAL STORAGE DISEASES<br/>[FR] MÉTHODES DE TRAITEMENT DE SYMPTÔMES NEUROLOGIQUES ASSOCIÉS À DES MALADIES LYSOSOMALES
申请人:GENZYME CORP
公开号:WO2021156769A1
公开(公告)日:2021-08-12
Methods are provided for treating or preventing neurological symptoms and disorders which are associated with, e.g., lysosomal storage diseases. The methods include enhancing neuronal connectivity within the brain of a subject, increasing brain tissue volume, or preventing or delaying loss of brain tissue volume in a subject. Also provided are methods for monitoring the progression or regression of a neurological disorder, or assessing the onset of a neurological disorder, associated with a lysosomal storage disease, in which brain tissue volume of the subject is measured.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND OR SALT THEREOF
申请人:FUJIFILM Corporation
公开号:US20150322063A1
公开(公告)日:2015-11-12
A compound represented by Formula [1] (in the formula, Z
1
represents N, CH, or the like; X
1
represents NH or the like; R
1
represents a heteroaryl group or the like; each of R
2
, R
3
, and R
4
represents a hydrogen atom, a halogen atom, an alkoxy group, or the like; and R
5
represents a heteroaryl group or the like) or salt thereof.
[EN] PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE<br/>[FR] COMPOSÉS DE PYRIMIDINE, COMPOSITIONS ET PROCÉDÉS D'UTILISATION
申请人:GENENTECH INC
公开号:WO2010014939A1
公开(公告)日:2010-02-04
Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).