SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
申请人:GLAXOSMITHKLINE LLC
公开号:US20150152108A1
公开(公告)日:2015-06-04
The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
[EN] IRAK DEGRADERS AND USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION D'IRAK ET LEURS UTILISATIONS
申请人:KYMERA THERAPEUTICS INC
公开号:WO2020264490A1
公开(公告)日:2020-12-30
The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.
[EN] SMARCA DEGRADERS AND USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION DE SMARCA ET LEURS UTILISATIONS
申请人:KYMERA THERAPEUTICS INC
公开号:WO2020251972A1
公开(公告)日:2020-12-17
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same for the modulation of one or more SWI/SNF-related matrix associated actin dependent regulator of chromatin subfamily A (SMARCA) and/or polybromo-1 (PB-1) protein via ubiqitination and/or degradation by compounds. The compounds are bifunctional molecules that link a cereblon-binding moiety to a ligand that binds SMARCA and/or PB1 proteins.
A compound of formula (I) or its enantiomers or diastereoisomers thereof:
wherein: A, X, W, R
1
, Y; R
3
; and R
4
are as defined herein.
The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.
COMPOUNDS AND METHODS FOR MODULATING COMMUNICATION AND VIRULENCE IN QUORUM SENSING BACTERIA
申请人:BLACKWELL Helen E.
公开号:US20100305182A1
公开(公告)日:2010-12-02
The present invention provides compositions and methods for modulating the communication and virulence of quorum sensing bacteria. In various exemplary embodiments, the invention provides a combinatorial library of quorum sensing compounds including synthetic analogs of naturally occurring and non-naturally occurring acyl-homoserine lactone (AHL) analogs, and methods of synthesizing and using these compounds.