Reductive desulfonylation of 2-aryl-2-benzylsulfonylacetates and -propionates with sodium amalgam. A new synthesis of 2-arylacetic and 2-arylpropionic acids.
Azacyclosteroid histamine-3 receptor ligands, pharmaceutical compositions comprising such compounds, and methods for using such compounds and compositions are described herein.
Provided herein is a drug delivery (DD) system for ratiometric luminescence determination of drug release degree in drug delivery monitoring, which includes a drug, a switchable reporter and non-switchable reporter providing two distinguishable signals for detection; or a single switchable reporter providing two distinguishable signals for detection, and a cleavable linker connecting a drug to a switchable reporter, as well as a method for ratiometric luminescence determination of drug release in a target in vivo or in vitro), which is effected by administering the DD system provided herein that is capable of releasing a drug from the DD system, measuring two luminescent signals provided by the switchable reporter and the non-switchable reporter, or the single switchable reporter, determining the ratio between these two luminescence signals, and determining the drug release degree through the ratio between the two luminescence signals.
[EN] SUBSTITUTED AZACYLES AS TRMP8 MODULATORS<br/>[FR] AZACYLES SUBSTITUÉS EN TANT QUE MODULATEURS DE TRPM8
申请人:GIVAUDAN SA
公开号:WO2021074281A1
公开(公告)日:2021-04-22
Disclosed are TRPM8 modulators as defined by formula (I) for achieving a cooling effect on skin and mucousa.
公开的是根据公式(I)定义的TRPM8调节剂,用于实现皮肤和粘膜的冷却效果。
[EN] AZACYCLOSTEROID HISTAMINE-3 RECEPTOR LIGANDS<br/>[FR] LIGANDS DE RECEPTEUR H3 DE L'HISTAMINE AZACYCLOSTEROIDE
申请人:ABBOTT LAB
公开号:WO2005100377A1
公开(公告)日:2005-10-27
Azacyclosteroid histamine-3 receptor ligands, pharmaceutical compositions comprising such compounds, and methods for using such compounds and compositions are described herein.
The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I):
wherein R
1
is optionally substituted C1-C8 alkyl and the like; R
2
is C1-C6 alkyl; R
3
is C1-C6 alkyl and the like; or R
2
and R
3
taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R
4
is hydrogen and the like; G is a group selected from the groups shown by the formula an the like:
wherein R
5
is hydrogen and the like; X
1
is a single bond and the like; X
2
is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R
6
)—, wherein R
6
is hydrogen and the like, and the like; X
3
is a single bond and the like;
a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.