即使在今天,组胺H 2受体(H 2 R)在中枢神经系统(CNS)中的作用仍然广为人知。在先前的研究中,许多二聚体,高亲和力和亚型选择性的氨基甲酰基胍型配体,例如UR-NK22(5,p K i = 8.07)被报道为H 2 R激动剂。但是,它们在中枢神经系统中研究H 2 R的适用性因其分子和药代动力学特性(例如高分子量)而受到限制,因此其生物利用度有限。满足对更多类似毒品的H 2的需求R激动剂具有高亲和力,我们合成了一系列含有各种间隔基和侧链部分的单体(硫代)氨基甲酰基胍型配体。这种结构上的简化导致了有效的(部分)激动剂(豚鼠右心房,[ 35 S]GTPγS和β-arrestin2募集试验),其人类(h)H 2 R亲和力在一位纳摩尔范围内(p K i(139,UR-KAT523):8.35; p K i(157,UR-MB-69):8.69)。本文介绍的大多数化合物对hH 2 R表现出出色
3,4-DISUBSTITUTED 3-CYCLOBUTENE-1,2-DIONES AND USE THEREOF
申请人:ALLERGAN, INC.
公开号:US20190047947A1
公开(公告)日:2019-02-14
Described herein are compounds, or pharmaceutically acceptable salts thereof, of the following formula:
The compounds are useful for treating inflammatory and autoimmune diseases.
N-(Diethoxyphosphoryl)Aldimines as Synthetic Equivalents of A<sup>1</sup> Type Synthons
作者:Andrzej Zwierzak、Anna Napieraj
DOI:10.1080/10426509908546190
日期:1999.1.1
Novel organophosphorus reagents useful for convergent synthesis of primary amines are presented.
介绍了可用于伯胺会聚合成的新型有机磷试剂。
Catalytic Hydrochlorination System and Process for Manufacturing Vinyl Chloride from Acetylene and Hydrogen Chloride in the Presence of this Catalytic System
申请人:Petitjean Andre
公开号:US20100063333A1
公开(公告)日:2010-03-11
Catalytic hydrochlorination system comprising at least one amine hydrochloride and at least one group VIII metal compound chosen from the group composed of mixtures of a platinum (IV) compound with tin (II) chloride, mixtures of a platinum (II) compound with triphenylphosphine oxide and mixtures of a palladium (II) compound with triphenylphosphine. This catalytic system is suitable for preparing vinyl chloride by reaction of acetylene with hydrogen chloride.
Pyrazolo [3,4-B] pyridine Compounds and Their Use as Phosphodiesterase Inhibitors
申请人:Allen George David
公开号:US20070111995A1
公开(公告)日:2007-05-17
The invention provides pyrazolo[3,4-b]pyridine compounds of formula (I) having a —C(O)—NH—C(R
4
)(R
5
)-aryl substituent at the 5-position of the pyrazolo[3,4-b]pyridine ring system wherein at least one of R
4
and R
5
is not a hydrogen atom (H) compound or a salt thereof:
wherein Ar has the sub-formula (x) or (z).
These compounds are useful as inhibitors of PDE4.