1-(4-Amino-3,5-dichlorophenyl)-2-(substituted amino)ethanol derivatives and their use in the treatment of respiratory disease
申请人:GLAXO GROUP LIMITED
公开号:EP0278728A2
公开(公告)日:1988-08-17
The invention provides compounds of the general formula
wherein
X represents a bond, or a C1-6alkylene, C2-6alkenylene or C2-6alkynylene chain, and
Y represents a bond, or a C1-6alkylene, C2-6alkenylene or C2-6alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 10;
R1 and R2 each represent a hydrogen atom or a C1-3alkyl group, with the proviso that the sum total of carbon atoms in R1 and R2 is not more than 4; and
Py represents a pyridyl group substituted by one or two substituents selected from nitro, -(CH2)tR3, -NR4R5, -(CH2)rSO2NR4R5, -NR6COR3, -NR6S02R7, -(CH2)rCOR3, -OCH2COR3 and -O(CH2)qR3; where
R3 represents a hydroxy, C1-3alkoxy or NR4R6 group;
R4 and R5 each represent a hydrogen atom or a C1-4alkyl group or -NR4R5 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from -O- and -S- or a group -NH- or -N(CH3)-;
R6 represents a hydrogen atom or a C1-4alkyl group;
R7 represents a C1-4alkyl, phenyl or -NR4R6 group;
q represents an integer 2 or 3;
r represents an integer from 0 to 3; and
t represents an integer 1, 2 or 3;
and physiologically acceptable salts and solvates (eg. hydrates) thereof.
The compounds have a stimulant action at β2-adreno receptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
本发明提供通式如下的化合物
式中
X 代表键,或 C1-6烷烯、C2-6烯烃或 C2-6 烷炔链,以及
Y 代表键,或 C1-6烷烯、C2-6烯烃或 C2-6 烷炔链,但 X 和 Y 中的碳原子总数不超过 10;
R1 和 R2 各代表一个氢原子或一个 C1-3 烷基,但 R1 和 R2 中的碳原子总数不超过 4 个;以及
Py 代表被一个或两个选自硝基、-(CH2)tR3、-NR4R5、-(CH2)rSO2NR4R5、-NR6COR3、-NR6S02R7、-(CH2)rCOR3、-OCH2COR3 和-O(CH2)qR3 的取代基取代的吡啶基;其中
R3 代表羟基、C1-3 烷氧基或 NR4R6 基团;
R4 和 R5 各代表一个氢原子或一个 C1-4 烷基或-NR4R5 形成一个饱和杂环氨基基团,该基团有 5-7 个环成员,环中可选择包含一个或多个选自-O-和-S-的原子或一个选自-NH-或-N(CH3)-的基团;
R6 代表氢原子或 C1-4 烷基;
R7 代表 C1-4 烷基、苯基或 -NR4R6 基团;
q 代表 2 或 3 的整数
r 代表 0 至 3 的整数;以及
t 代表 1、2 或 3 的整数;
及其生理上可接受的盐和溶液(如水合物)。
这些化合物对 β2-肾上腺素受体有刺激作用,可用于治疗与可逆性气道阻塞有关的疾病,如哮喘和慢性支气管炎。