SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
申请人:OOST Thorsten
公开号:US20140057916A1
公开(公告)日:2014-02-27
This invention relates to substituted 4-pyridones of formula 1
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
Carbamate compounds having a structure represented by formula I (where R
1
, R
2
, R
3
, R
4
, R
5
and R
6
are as defined herein) are useful as anti-tumor agents.
[EN] 2-CYANOISOINDOLINE DERIVATIVES FOR TREATING CANCER<br/>[FR] DÉRIVÉS DE 2-CYANOISOINDOLINE POUR LE TRAITEMENT DU CANCER
申请人:MISSION THERAPEUTICS LTD
公开号:WO2017158388A1
公开(公告)日:2017-09-21
The invention relates to novel compounds of formula I which are inhibitors of deubiquitylating enzymes (DUBs) and/or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to methods for the preparation of these compounds and to their use in the treatment of cancer.
[EN] NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS<br/>[FR] NOUVEAUX AGONISTES DE RÉCEPTEURS ADRÉNERGIQUES BÊTA 3 DÉRIVÉS DE PYRROLIDINE
申请人:MERCK SHARP & DOHME
公开号:WO2015050798A1
公开(公告)日:2015-04-09
The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.
[EN] BENZOPYRANE AND IMIDAZOLE DERIVATIVES USEFUL FOR THE STABILIZATION OF AMYLOIDOGENIC IMMUNOGLOBULIN LIGHT CHAINS<br/>[FR] DÉRIVÉS DE STABILISATION DE BENZOPYRANE ET D'IMIDAZOLE UTILISÉS POUR LA STABILISATION DE CHAÎNES LÉGÈRES D'IMMUNOGLOBULINES AMYLOÏDOGÉNIQUES
申请人:SCRIPPS RESEARCH INST
公开号:WO2020205683A1
公开(公告)日:2020-10-08
In immunoglobulin light chain amyloidosis (AL), the unique antibody light chain (LC) protein that is secreted by monoclonal plasma cells in each patient misfolds and/or aggregates, a process leading to organ degeneration. For treating AL patients, such as those with substantial cardiac involvement who have difficulty tolerating existing chemotherapy regimens, provided herein are small molecule compounds of Formula Ia, Formula Ib, and Formula II that are kinetic stabilizers of the native dimeric structure of full-length LCs, which compounds can slow or stop the amyloidogenicity cascade at its origin.