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101. 发明授权

US4853382A Aminophenol derivatives 失效
标题翻译：氨基苯酚衍生物
公开(公告)号：US4853382A
公开(公告)日：1989-08-01
申请号：US124601
申请日：1987-11-24
申请人： Ian F. Skidmore , Harry Finch , Alan Naylor , Lawrence H. C. Lunts , Ian B. Campbell
发明人： Ian F. Skidmore , Harry Finch , Alan Naylor , Lawrence H. C. Lunts , Ian B. Campbell
IPC分类号： A61K31/165 , A61K31/17 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/235 , A61K31/27 , A61K31/275 , A61K31/335 , A61K31/357 , A61K31/445 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P11/08 , A61P25/02 , C07C67/00 , C07C231/00 , C07C233/43 , C07C233/78 , C07C253/00 , C07C255/37 , C07C255/54 , C07C275/24 , C07C275/32 , C07C275/40 , C07C301/00 , C07C303/40 , C07C307/10 , C07C311/00 , C07C313/00 , C07C315/04 , C07C317/18 , C07D295/08 , C07D317/54 , C07D319/18
CPC分类号： C07C275/40
摘要： The invention provides compounds of the general formula (I) ##STR1## wherein Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, --(CH.sub.2).sub.q R, [where R is hydroxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represents a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 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-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or --NR.sup.3 R.sup.4 group), --NR.sup.5 SO.sub.2 R.sup.7 (where R.sup.7 represents a C.sub.1-4 alkyl, phenyl or --NR.sup.3 R.sup.4 group), --COR.sup. 8 (where R.sup.8 represents hydroxy, C.sub.1-4 alkoxy or --NR.sup.3 R.sup.4), --SR.sup.9 (where R.sup.9 is a hydrogen atom, or a C.sub.1-4 alkyl or phenyl group), --SOR.sup.9, --SO.sub.2 R.sup.9, or --CN, and q represents an integer from 0 to 3], --(CH.sub.2).sub.r R.sup.10, [where R.sup.10 is a C.sub.1-4 alkoxy group and r represents an integer from 1 to 3] or --O(CH.sub.2).sub.t R.sup.11 [where R.sup.11 represents a hydroxy or C.sub.1-4 alkoxy group and t is 2 or 3] or Ar is a phenyl group substituted by an alkylenedioxy group of formula --O(CH.sub.2).sub.p O--, where p represents 1 or 2;R.sup.1 and R.sup.2 each represent a hydrogen atom or a C.sub.1-3 alkyl group with the proviso that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4;X represents a C.sub.1-7 alkylene, C.sub.2-7 alkylene or C.sub.2-7 alkynylene chain;Y represents a bond, or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is 2 to 10;Q represents a group R.sup.12 CO--, R.sup.12 NHCO--, R.sup.12 R.sup.13 NSO.sub.2 -- or R.sup.14 SO.sub.2, where R.sup.12 and R.sup.13 each represent a hydrogen atom or a C.sub.1-3 alkyl group, and R.sup.14 represents a C.sub.1-4 alkyl group, with the proviso that when X represents C.sub.1-7 alkylene, and Y represents a bond or C.sub.1-6 alkylene, then the group Ar does not represent an unsubstituted phenyl group or a phenyl group substituted by one or more substituents selected solely from halogen atoms or C.sub.1-6 alkyl or C.sub.1-6 alkoxy groups or an alkylenedioxy group --O(CH.sub.2).sub.p O--;and physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used, inter alia, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

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