TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
申请人:Arvinas, Inc.
公开号:US20180125821A1
公开(公告)日:2018-05-10
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
Provided is a cephem compound which has a wide antimicrobial spectrum, and in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical composition comprising the same.
A Compound of the formula (I):
wherein
W and U are as defined in the specification;
R
1
is as defined in the specification;
R
2A
and R
2B
are as defined in the specification, provided that R
2A
and R
2B
are not taken together to form an optionally substituted oxime group when R
1
is aminothiazole or aminothiadiazole optionally protected at the amino group;
ring A is a benzene ring or a 6-membered aromatic heterocyclic group having 1-3 nitrogen atoms;
R
3
is a hydrogen atom, —OCH
3
or —NH—CH(═O);
k is an integer from 0 to 2;
R
4
is as defined in the specification; and
D and E are as defined in accordance with a) or b) described in the specification.
Provided is a compound comprising a first ligand L
A
of
提供一个包含第一配体L的化合物。
[EN] LINKED DIBENZIMIDAZOLE DERIVATIVES<br/>[FR] DÉRIVÉS DU DIBENZIMIDAZOLE LIÉS
申请人:ENANTA PHARM INC
公开号:WO2010091413A1
公开(公告)日:2010-08-12
The present invention discloses linked dibenzimidazole derivatives, or pharmaceutically acceptable salts, esters, or prodrugs thereof, which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.