发明公开
EP0278728A2 1-(4-Amino-3,5-dichlorophenyl)-2-(substituted amino)ethanol derivatives and their use in the treatment of respiratory disease
失效
1-(4-氨基-3,5-二氯苯基)-2-(取代的氨基)乙醇衍生物及其在肺部疾病的治疗用途。
- 专利标题: 1-(4-Amino-3,5-dichlorophenyl)-2-(substituted amino)ethanol derivatives and their use in the treatment of respiratory disease
- 专利标题(中): 1-(4-氨基-3,5-二氯苯基)-2-(取代的氨基)乙醇衍生物及其在肺部疾病的治疗用途。
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申请号: EP88301065.4申请日: 1988-02-09
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公开(公告)号: EP0278728A2公开(公告)日: 1988-08-17
- 发明人: Lunts, Lawrence Henry Charles
- 申请人: GLAXO GROUP LIMITED
- 申请人地址: Clarges House 6-12 Clarges Street London W1Y 8DH GB
- 专利权人: GLAXO GROUP LIMITED
- 当前专利权人: GLAXO GROUP LIMITED
- 当前专利权人地址: Clarges House 6-12 Clarges Street London W1Y 8DH GB
- 代理机构: Marchant, James Ian
- 优先权: GB8703007 19870210
- 主分类号: C07D213/80
- IPC分类号: C07D213/80 ; C07D213/79 ; C07D213/73 ; C07D213/81 ; C07D213/74 ; C07D213/82 ; C07D213/76 ; C07D213/71 ; C07D213/65
摘要:
The invention provides compounds of the general formula
wherein
X represents a bond, or a C 1-6 alkylene, C 2 - 6 alkenylene or C 2 - 6 alkynylene chain, and
Y represents a bond, or a C 1-6 alkylene, C 2 - 6 alkenylene or C 2-6 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 10;
R 1 and R 2 each represent a hydrogen atom or a C 1-3 alkyl group, with the proviso that the sum total of carbon atoms in R 1 and R 2 is not more than 4; and
Py represents a pyridyl group substituted by one or two substituents selected from nitro, -(CH 2 ) t R 3 , -NR 4 R 5 , -(CH 2 ) r SO 2 NR 4 R 5 , -NR 6 COR 3 , -NR 6 S0 2 R 7 , -(CH 2 ) r COR 3 , -OCH 2 COR 3 and -O(CH 2 )qR 3 ; where
R 3 represents a hydroxy, C 1 - 3 alkoxy or NR 4 R 6 group;
R 4 and R 5 each represent a hydrogen atom or a C 1-4 alkyl group or -NR 4 R 5 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(CH 3 )-;
R 6 represents a hydrogen atom or a C 1-4 alkyl group;
R 7 represents a C 1-4 alkyl, phenyl or -NR 4 R 6 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 β 2 -adreno receptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
wherein
X represents a bond, or a C 1-6 alkylene, C 2 - 6 alkenylene or C 2 - 6 alkynylene chain, and
Y represents a bond, or a C 1-6 alkylene, C 2 - 6 alkenylene or C 2-6 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 10;
R 1 and R 2 each represent a hydrogen atom or a C 1-3 alkyl group, with the proviso that the sum total of carbon atoms in R 1 and R 2 is not more than 4; and
Py represents a pyridyl group substituted by one or two substituents selected from nitro, -(CH 2 ) t R 3 , -NR 4 R 5 , -(CH 2 ) r SO 2 NR 4 R 5 , -NR 6 COR 3 , -NR 6 S0 2 R 7 , -(CH 2 ) r COR 3 , -OCH 2 COR 3 and -O(CH 2 )qR 3 ; where
R 3 represents a hydroxy, C 1 - 3 alkoxy or NR 4 R 6 group;
R 4 and R 5 each represent a hydrogen atom or a C 1-4 alkyl group or -NR 4 R 5 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(CH 3 )-;
R 6 represents a hydrogen atom or a C 1-4 alkyl group;
R 7 represents a C 1-4 alkyl, phenyl or -NR 4 R 6 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 β 2 -adreno receptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
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