AMINO- AND AMIDO-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
申请人:Trapp Sean G.
公开号:US20090247627A1
公开(公告)日:2009-10-01
The invention provides amino- and amido-aminotetralin compounds of formula (I):
wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst, wherein the catalytically active mass of the catalyst contains, after its preparation and before the treatment with hydrogen, 22 to 45% by weight of oxygen-containing compounds of zirconium, calculated as ZrO
2
,
1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO,
5 to 50% by weight of oxygen-containing compounds of nickel, calculated as Nio, where the molar ratio of nickel to copper is greater than 1,
5 to 50% by weight of oxygen-containing compounds of cobalt, calculated as CoO,
0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO
3
, and 0 to 10% by weight of oxygen-containing compounds of aluminum and/or manganese, calculated as Al
2
O
3
or MnO
2
.
2-Arylhydrazino-2-imidazoline, deren Acylderivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Bekämpfung von Endo- und Ektoparasiten
申请人:BAYER AG
公开号:EP0073960A1
公开(公告)日:1983-03-16
Imidazolinverbindungen der Formel
in der
Y für -
- steht und
R' und R2 Wasserstoff oder Acyl bedeuten,
Ar einen mit identischen Substituenten disubstituierten oder mit einem weiteren Ring anellierten Phenylrest bedeutet und
R für Wasserstoff, C1-C4-Alkyl oder einen Acyirest steht,
Verfahren zu ihrer Herstellung und ihre Verwendung zur Bekämpfung von Ektoparasiten und Endoparasiten.
式中的咪唑啉化合物
中的
Y 代表
- 和
R' 和 R2 表示氢或酰基、
Ar 表示被相同取代基取代或与另一个环融合的苯基,以及
R 是氢、C1-C4 烷基或酰基、
其制备方法及其在防治外寄生虫和内寄生虫中的用途。
2 -AMINOTETRALIN DERIVATIVES AS MU OPIOID RECEPTOR ANTAGONISTS