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    Dichloroaniline derivatives for the therapy or prophylaxysis of a disease associated with reversible airway obstruction
    1.
    发明授权
    Dichloroaniline derivatives for the therapy or prophylaxysis of a disease associated with reversible airway obstruction 失效
    用于治疗或预防与可逆性气道阻塞相关的疾病的二氯苯胺衍生物

    公开(公告)号：US5006556A

    公开(公告)日：1991-04-09

    申请号：US524141

    申请日：1990-05-15

    申请人： Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  Ian B. Campbell

    发明人： Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  Ian B. Campbell

    IPC分类号： C07C45/00 ,  C07D295/096 ,  C07D295/192

    CPC分类号： C07D295/192 ,  C07C45/004 ,  C07D295/096 ,  Y10S514/826

    摘要： The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2)qR [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent 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 or --NR.sup.3 R.sup.4 group), and q represents an integer from 0 to 3], --NR.sup.5 COR.sup.19 (where R.sup.5 is as defined above and R.sup.19 represents a phenyl group), --(CH.sub.2).sub.r R.sup.7 [where R.sup.7 represents --NR.sup.5 SO.sub.2 R.sup.8 (where R.sup.8 represents a C.sub.1-4 alkyl, phenyl or --NR.sup.3 R.sup.4 group), --NR.sup.5 COCH.sub.2 N(R.sup.5).sub.2 (where each of the groups R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group), --COR.sup.9 (where R.sup.9 represents hydroxy, C.sub.1-4 alkoxy or NR.sup.3 R.sup.4), --SR.sup.10 (where R.sup.10 is a hydrogen atom, or a C.sub.1-4 alkyl group optionally substituted by hydroxy, C.sub.1-4 alkoxy or NR.sup.3 R.sup.4), --SOR.sup.10, --SO.sub.2 R.sup.10, --CN, or --NR.sup.11 R.sup.12 (where R.sup.11 and R.sup.12 represent a hydrogen atom or a C.sub.1-4 alkyl group, at least one of which is C.sub.2-4 alkyl substituted by a hydroxy, C.sub.1-4 alkoxy or NR.sup.3 R.sup.4 group), and r represents an integer from 0 to 3], --O(CH.sub.2).sub.q COR.sup.9 (where q and R.sup.9 are as defined above), or --O(CH.sub.2).sub.t R.sup.13 [where R.sup.13 represents hydroxy, NR.sup.3 R.sup.4, NR.sup.11 R.sup.12 or a C.sub.1-4 alkoxy group optionally substituted by hydroxy, C.sub.1-4 alkoxy or NR.sup.3 R.sup.4, and t is an integer 2 or 3], or Ar is a phenyl group substituted by an alkylenedioxy group --O(CH.sub.2).sub.p O-- where p is 1 or 2; R.sup.1 and R.sup.2 each represents 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;and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds of formula (I) have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful, in particular, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    Ethanolamine derivatives
    5.
    发明授权
    Ethanolamine derivatives 失效

    公开(公告)号：US4990664A

    公开(公告)日：1991-02-05

    申请号：US230357

    申请日：1988-08-10

    申请人： Ian F. Skidmore ,  Alan Naylor ,  Harry Finch ,  Lawrence H. C. Lunts ,  Ian B. Campbell ,  Peter C. North

    发明人： Ian F. Skidmore ,  Alan Naylor ,  Harry Finch ,  Lawrence H. C. Lunts ,  Ian B. Campbell ,  Peter C. North

    IPC分类号： C07D295/18 ,  A61K31/135 ,  A61K31/165 ,  A61K31/18 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61K31/47 ,  A61P5/38 ,  C07C67/00 ,  C07C231/00 ,  C07C237/30 ,  C07C301/00 ,  C07C303/34 ,  C07C309/66 ,  C07C313/00 ,  C07C323/25 ,  C07C323/27 ,  C07C323/41 ,  C07C323/42 ,  C07C323/43 ,  C07C323/44 ,  C07C323/49 ,  C07C323/60 ,  C07C323/62 ,  C07C323/65 ,  C07C325/00 ,  C07D213/32 ,  C07D213/65 ,  C07D215/26

    CPC分类号： C07C323/62 ,  C07C323/25 ,  C07D213/32

    摘要： The invention provides compounds of the general formula ##STR1## and physiologically acceptable salts and solvates thereof, wherein Z represents the group ##STR2## where A represents a group selected from HOR.sup.3 --, R.sup.6 NH(CH.sub.2)p--, R.sup.10 R.sup.11 N--, R.sup.12 OCH.sub.2 --, CH.sub.3 SO.sub.2 CH.sub.2 -- or NCCH.sub.2 --;where R.sup.3 is a C.sub.1-3 alkylene group,R.sup.6 is a group selected from R.sup.7 CO--, R.sup.7 NHCO--, R.sup.7 R.sup.8 NSO.sub.2 -- orR.sup.9 SO.sub.2 --, and p is zero or 1,R.sup.7 and R.sup.8 each represent a hydrogen atom or a C.sub.1-3 alkyl group,R.sup.9 is a C.sub.1-3 alkyl group,R.sup.10 and R.sup.11 each represent a hydrogen atom or a C.sub.1-4 alkyl group or, when R.sup.10 is a hydrogen atom, R.sup.11 may also be a C.sub.1-4 alkoxycarbonyl group, andR.sup.12 is a C.sub.1-3 alkyl group; ##STR3## where one of R.sup.4 and R.sup.5 is a hydroxy group and the other is a hydrogen or halogen atom or a hydroxy group; ##STR4## where A.sup.1 is either a chlorine atom or a --CF.sub.3 group; ##STR5## X represents a bond or a C.sub.1-7 alkenylene or C.sub.2-7 alkynylene chain, andY 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;R represents a hydrogen atom or a C.sub.1-3 alkyl group;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group; with the proviso that the sum total of carbon atoms inR.sup.1 and R.sup.2 is not more than 4;Q represents a pyridyl group optionally substituted by one or two substituents selected from halogen atoms or hydroxy, C.sub.1-3 alkyl or C.sub.1-3 alkoxy groups, or Q represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-6 alkyl, nitro, --(CH.sub.2).sub.q R.sup.13 or --O(CH.sub.2).sub.r R.sup.14, or Q represents a phenyl group substituted by an alkylenedioxy group of formula --O(CH.sub.2).sub.t O--; whereR.sup.13 represents hydroxy, C.sub.1-6 alkoxy, cyano, --NR.sup.15 R.sup.16, --NR.sup.17 COR.sup.18, --NR.sup.17 SO.sub.2 R.sup.19, --COR.sup.20, --SR.sup.21, --SOR.sup.22 or --SO.sub.2 R.sup.22 ;R.sup.14 represents hydroxy or C.sub.1-4 alkoxy;R.sup.15 and R.sup.16 each represent a hydrogen atom or a C.sub.1-4 alkyl group or --NR.sup.15 R.sup.16 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)--;R.sup.17 represents a hydrogen atom or a C.sub.1-4 alkyl group;R.sup.18 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or --NR.sup.15 R.sup.16 group;R.sup.19 represents C.sub.1-4 alkyl, phenyl or --NR.sup.15 R.sup.16 ;R.sup.20 represents hydroxy, C.sub.1-4 alkoxy or --NR.sup.15 R.sup.16 ;R.sup.21 represents a hydrogen atom or a C.sub.1-4 alkyl or phenyl group;R.sup.22 represents a C.sub.1-4 alkyl or phenyl group;q represents an integer from 0 to 3;r represents 2 or 3; andt represents 1 or 2.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.

    Ethanolamine derivatives
    7.
    发明授权
    Ethanolamine derivatives 失效
    乙醇胺衍生物

    公开(公告)号：US4908386A

    公开(公告)日：1990-03-13

    申请号：US287441

    申请日：1988-12-20

    申请人： Harry Finch ,  Lawrence H. C. Lunts ,  Alan Naylor ,  Ian F. Skidmore ,  Ian B. Campbell ,  David Middlemiss ,  Charles Willbe

    发明人： Harry Finch ,  Lawrence H. C. Lunts ,  Alan Naylor ,  Ian F. Skidmore ,  Ian B. Campbell ,  David Middlemiss ,  Charles Willbe

    IPC分类号： C07D213/65 ,  C07D295/096 ,  C07C143/74 ,  A61K31/18

    CPC分类号： C07D295/096 ,  C07D213/65 ,  Y10S514/826

    摘要： The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene 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;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    摘要翻译： 本发明提供通式（I）的化合物，其中Ar表示未取代或取代的苯基; R1和R2各自表示氢原子或C1-3烷基; X表示键或C 1-7亚烷基，C 2-7亚烯基或C 2-7亚炔基链; Y表示键或C 1-6亚烷基，C 2-6亚烯基或C 2-6亚炔基链; Q表示取代的苯基或吡啶环; 以及其可用作2-肾上腺素受体的兴奋剂的生理上可接受的盐和溶剂合物，特别是用于治疗与可逆气道阻塞如哮喘和慢性支气管炎相关的疾病。

    Ethanolamine compounds
    8.
    发明授权
    Ethanolamine compounds 失效

    公开(公告)号：US4853381A

    公开(公告)日：1989-08-01

    申请号：US919122

    申请日：1986-10-15

    申请人： Harry Finch ,  Lawrence H. C. Lunts ,  Alan Naylor ,  Ian F. Skidmore ,  Ian B. Campbell

    发明人： Harry Finch ,  Lawrence H. C. Lunts ,  Alan Naylor ,  Ian F. Skidmore ,  Ian B. Campbell

    IPC分类号： C07C45/67 ,  C07C45/68 ,  C07C49/255 ,  C07C49/82 ,  C07D215/26 ,  C07D295/096

    CPC分类号： C07D295/096 ,  C07C45/673 ,  C07C45/68 ,  C07C49/255 ,  C07C49/82 ,  C07D215/26 ,  Y10S514/826

    摘要： The invention provides compounds of the general formula (I) ##STR1## whereinAr 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 represent 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 an integer 2 or 3), or Ar is a phenyl ring substituted by an alkylenedioxy group of formula --O(CH.sub.2).sub.p O-- where p represents an integer 1 or 2;Q represents a group of formula ##STR2## where R.sup.a represents a hydrogen atom or a C.sub.1-3 alkyl group,R.sup.b represents ##STR3## and Rc represents ##STR4## where R.sup.d represents a straight or branched C.sub.2-3 alkylene chain; 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 alkenylene or C.sub.2-7 alkynylene chain; andY 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 2-10,and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds of formula (I) have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful, in particular, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    Dichloroaniline derivatives
    10.
    发明授权
    Dichloroaniline derivatives 失效

    公开(公告)号：US4943591A

    公开(公告)日：1990-07-24

    申请号：US918317

    申请日：1986-10-14

    申请人： Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  Ian B. Campbell

    发明人： Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  Ian B. Campbell

    IPC分类号： C07C45/00 ,  C07D295/096 ,  C07D295/192

    CPC分类号： C07D295/192 ,  C07C45/004 ,  C07D295/096 ,  Y10S514/826

    摘要： The invention provides compounds of the general formula (I) ##STR1## wherein X represents a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain andY represents a bond, or a C.sub.1-4 alkylene, C.sub.2-4 alkenylene or C.sub.2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups C.sub.1-3 alkyl, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, C.sub.1-3 alkoxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent 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 or --NR.sup.3 R.sup.4 group), and q represents an integer from 0 to 3], --NR.sup.5 COR.sup.19 (where R.sup.5 is as defined above and R.sup.19 represents a phenyl group), --(CH.sub.2).sub.r R.sup.7 [where R.sup.7 represents --NR.sup.5 SO.sub.2 R.sup.8 (where R.sup.8 represents a C.sub.1-4 alkyl, phenyl or --NR.sup.3 R.sup.4 group), --NR.sup.5 COCH.sub.2 N(R.sup.5).sub.2 (where each of the groups R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group), --COR.sup.9 (where R.sup.9 represents hydroxy, C.sub.1-4 alkoxy or NR.sup.3 R.sup.4), --SR.sup.10 (where R.sup.10 is a hydrogen atom, or a C.sub.1-4 alkyl group optionally substituted by hydroxy, C.sub.1-4 alkoxy or NR.sup.3 R.sup.4), --SOR.sup.10, --SO.sub.2 R.sup.10, --CN, or --NR.sup.11 R.sup.12 (where R.sup.11 and R.sup.12 represent a hydrogen atom or a C.sub.1-4 alkyl group, at least one of which is C.sub.2-4 alkyl substituted by a hydroxy, C.sub.1-4 alkoxy or NR.sup.3 R.sup.4), and r represents an integer from 0 to 3], --O(CH.sub.2).sub.q COR.sup.9 (where q and R.sup.9 are as defined above), or --O(CH.sub.2).sub.t R.sup.13 [where R.sup.13 represents hydroxy, NR.sup.3 R.sup.4, NR.sup.11 R.sup.12 or a C.sub.1-4 alkoxy group optionally substituted by hydroxy, C.sub.1-4 alkoxy or NR.sup.3 R.sup.4, and t is an integer 2 or 3], or Ar is a phenyl group substituted by an alkylenedioxy group --O(CH.sub.2).sub.p O-- where p is 1 or 2;R.sup.1 and R.sup.2 each represents 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;and physiologically acceptable salts and solvates (e.g. hydrates) thereof.The compounds of formula (I) have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful, in particular, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.