NOVEL CONJUGATES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
申请人:BOUCHARD Hervé
公开号:US20120225089A1
公开(公告)日:2012-09-06
Provided herein are cryptophycin conjugates and compositions containing them. Methods of making and using such compounds also are provided.
本发明提供了隐藻素偶联物及其包含它们的组合物。还提供了制备和使用此类化合物的方法。
Carbon dioxide utilization in the efficient synthesis of carbamates by deep eutectic solvents (DES) as green and attractive solvent/catalyst systems
作者:Iman Dindarloo Inaloo、Sahar Majnooni
DOI:10.1039/c9nj02810b
日期:——
green and eco-friendly solvent/catalyst system based on a deep eutectic solvent (DES) was devised and developed for the simple synthesis of carbamates through three-component coupling of amines, alkyl halides and carbon dioxide (CO2). It was found that choline chloride:zinc(II) chloride ([ChCl][ZnCl2]2) was very proficient and effective for the activation and utilization of CO2 in carbamate formation
Triazole-Containing Releasable Linkers, Conjugates Thereof, and Methods of Preparation
申请人:Beusker Patrick Henry
公开号:US20080311136A1
公开(公告)日:2008-12-18
This invention relates to compounds comprising one or more therapeutic and/or diagnostic moieties and one or more functional moieties linked together via one or more triazole-containing linkers and to their intermediates and methods of their preparation. The triazole-containing linker may optionally contain one or more conditionally-cleavable or conditionally-transformable moieties and one or more spacer systems in between said moiety/moieties and the one or more therapeutic and/or diagnostic moieties.
The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula:
wherein R
1
represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R
2
represents a group —OR
3
or the like, and R
3
represents a hydrogen atom, C1-C6 alkyl group or the like, or R
1
and —(CH
2
)
n
R
2
may bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H):
wherein R
41
is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against
Mycobacterium tuberculosis
, multi-drug-resistant
Mycobacterium tuberculosis
, and atypical acid-fast bacteria.
The invention provides a compound or its pharmaceutically-acceptable salt of formula
wherein A
1
is a hydrogen, etc.; j and k are 0 or 1;
is a double bond, etc.;
is a double bond, etc.;
one of W
1
and W
2
is E-O—W, etc., and the other is a hydrogen atom, etc.; E is a divalent group derived from a benzene ring, etc., by removing two hydrogen atoms therefrom; W is a group of formula (II-1):
which has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for prevention or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.