Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility
摘要:
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the entrance channel of the NNRTI binding site. Compound 4d shows low-nanomolar activity similar to etravirine towards wild-type HIV-1 and key viral variants. (C) 2013 Elsevier Ltd. All rights reserved.
BICYCLIC HETEROCYCLE DERIVATIVES AND THEIR USE AS MODULATORS OF THE ACTIVITY OF GPR119
申请人:Xia Yan
公开号:US20110212938A1
公开(公告)日:2011-09-01
The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
The invention relates to antibacterial and anti-mycobacterial drug compounds of formula I. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections, and methods of treating bacterial infections. The invention is also directed to antibacterial drug compounds capable of treating bacterial infections that are currently hard to treat with existing drug compounds, e.g., those caused by resistant bacterial or mycobacterial strains.
本发明涉及式 I 的抗菌和抗霉菌药物化合物,还涉及抗菌药物化合物的药物制剂。 本发明还涉及这些衍生物在治疗细菌感染中的用途,以及治疗细菌感染的方法。 本发明还涉及能够治疗目前难以用现有药物化合物治疗的细菌感染的抗菌药物化合物,例如由抗药性细菌或分枝杆菌菌株引起的细菌感染。
ANTIBACTERIAL COMPOUNDS
申请人:REDX PHARMA PLC
公开号:US20170158708A1
公开(公告)日:2017-06-08
The invention relates to antibacterial and anti-mycobacterial drug compounds of formula I. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections, and methods of treating bacterial infections. The invention is also directed to antibacterial drug compounds capable of treating bacterial infections that are currently hard to treat with existing drug compounds, e.g., those caused by resistant bacterial or mycobacterial strains.
PHOTOAFFINITY PROBES
申请人:Promega Corporation
公开号:US20200340982A1
公开(公告)日:2020-10-29
Provided herein are compositions and methods for photoaffinity labeling of molecular targets. In particular, probes that specifically interact with cellular targets based on their affinity and are then covalently linked to the cellular target via a photoreactive group (PRG) on the probe.