申请人:Glaxo Group Limited
公开号:US04997986A1
公开(公告)日:1991-03-05
The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, wherein Ar represents the group ##STR2## where Q.sup.1 represents a straight or branched C.sub.1-3 alkylene group, ##STR3## where Q.sup.2 represents a group R.sup.3 CO--, R.sup.3 NHCO--, R.sup.3 R.sup.4 NSO.sub.2 -- or R.sup.5 SO.sub.2 --, where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.5 represents a C.sub.1-3 alkyl group, ##STR4## R represents a hydrogen atom or a C.sub.1-3 alkyl group; R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a methyl or ethyl group; and k represents an integer from 1 to 8; m represents zero or an integer from 2 to 7, and; n represents an integer from 1 to 7 with the proviso that the sum total of k, m and n is 4 to 12; X represents an oxygen or sulphur atom, and; Y and Z each represent a bond, or an oxygen or sulphur atom with the proviso that when Y is a bond m is zero, or when Y represents an oxygen or sulphur atom m is an integer from 2 to 7, or when Y and Z each independently represent an oxygen or sulphur atom then n is an integer from 2 to 7; Q represents a naphthalenyl group which may optionally be substituted by one or two groups selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy and halogen. The compounds have a stimulant action at .beta..sub.2 -adrenoreceptors 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(I)的化合物及其生理上可接受的盐和溶剂化物,其中Ar代表基团,其中Q1代表直链或支链C1-3烷基基团,Q2代表基团R3CO-,R3NHCO-,R3R4NSO2-或R5SO2-,其中R3和R4分别代表氢原子或C1-3烷基基团,而R5代表C1-3烷基基团,R代表氢原子或C1-3烷基基团;R1和R2各自独立地代表氢原子或甲基或乙基基团;k表示1到8的整数;m表示零或2到7的整数;n表示1到7的整数,但总和k、m和n为4到12;X表示氧原子或硫原子;Y和Z各自代表键合或氧原子或硫原子,但当Y是键合时,m为零,或当Y代表氧原子或硫原子时,m为2到7的整数,或当Y和Z各自独立地代表氧原子或硫原子时,n为2到7的整数;Q代表萘基团,其可以选择性地被C1-4烷基,C1-4烷氧基,羟基和卤素中的1或2个基团取代。这些化合物在β2-肾上腺素受体上具有兴奋作用,并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。