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    Chemical compounds
    1.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号：US4937268A

    公开(公告)日：1990-06-26

    申请号：US166975

    申请日：1988-03-11

    申请人： Ian F. Skidmore ,  Harry Finch ,  Alan Naylor ,  Lawrence H. C. Lunts ,  David Hartley ,  William L. Mitchell

    发明人： Ian F. Skidmore ,  Harry Finch ,  Alan Naylor ,  Lawrence H. C. Lunts ,  David Hartley ,  William L. Mitchell

    IPC分类号： A61K31/395 ,  A61K31/135 ,  A61K31/165 ,  A61K31/18 ,  A61K31/19 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/47 ,  A61P1/04 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/24 ,  A61P25/26 ,  A61P27/02 ,  A61P27/14 ,  A61P29/00 ,  A61P37/08 ,  C07D213/30 ,  C07D213/32 ,  C07D213/63 ,  C07D213/65 ,  C07D215/26 ,  C07D295/18

    CPC分类号： C07D213/30 ,  C07D213/32 ,  C07D213/63

    摘要： This invention relates to compounds of the general formula (I) and physiologically acceptable salts and solvates thereof whereinAr represents ##STR1## where R.sup.3 is a bond or a straight or branched C.sub.1-2 alkylene group,R.sup.4 is a hydroxy group or a group R.sup.5 NH-- whereR.sup.5 represents a group CH.sub.3 SO.sub.2 --, HCO-- or NH.sub.2 CO--, ##STR2## where R.sup.6 is a chlorine atom or the group F.sub.3 C--, ##STR3## k represents an integer from 1 to 8, m represents zero or an integer from 2 to 7 andn represents an integer from 2 to 7 with the proviso that the sum total of k, m and n is 4 to 12;R.sup.1 and R.sup.2 each represents a hydrogen atom or a methyl or ethyl group with the proviso that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 2;R.sup.30 represents hydrogen or C.sub.1-2 alkyl;X represents an oxygen or sulphur atom; andY and Q may each represent a bond or an oxygen or sulphur atom with the provisos that at least one of Y and Q represents an oxygen or sulphur atom and 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;P represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C.sub.1-3 alkyl, C.sub.1-3 alkoxy, hydroxy, --CH.sub.2 OH--, --(CH.sub.2).sub.2 OH, --CO.sub.2 H, --CO.sub.2 CH.sub.3, --CO.sub.2 (CH.sub.2).sub.2 CH.sub.3, --R.sup.7, COR.sup.7, --NHCOR.sup.8 and --NR.sup.9 SO.sub.2 R.sup.10 ; whereR.sup.7 represents an amino, aminoC.sub.1-3 alkyl, aminoC.sub.1-3 dialkyl, pyrrolidino, piperidino, hexamethyleneimino, piperazino, N-methylpiperazino or morpholino group;R.sup.8 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or amino group;R.sup.9 represents a hydrogen atom or a methyl group;R.sup.10 represents a methyl, phenyl, amino or dimethylamino group;or P represents a pyridyl group optionally substituted by one or two substitutents selected from halogen atoms or hydroxy, C.sub.1-3 alkyl and C.sub.1-3 alkoxy groups.The compounds 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.

    Phenethanolamine derivatives
    3.
    发明授权
    Phenethanolamine derivatives 失效

    公开(公告)号：US5099068A

    公开(公告)日：1992-03-24

    申请号：US622549

    申请日：1990-12-05

    申请人： William L. Mitchell ,  Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  David Hartley

    发明人： William L. Mitchell ,  Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  David Hartley

    IPC分类号： C07C307/10 ,  C07C65/11 ,  C07C217/08 ,  C07C231/12 ,  C07C233/43 ,  C07C275/34 ,  C07C311/08 ,  C07C323/12 ,  C07C323/16 ,  C07C323/25

    CPC分类号： C07C65/11 ,  Y10S514/819 ,  Y10S514/826 ,  Y10S514/886 ,  Y10S514/887 ,  Y10S514/913 ,  Y10S514/925 ,  Y10S514/927

    摘要： 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; andk 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 wich 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.

    Phenethanolamine derivatives
    4.
    发明授权
    Phenethanolamine derivatives 失效
    苯乙醇胺衍生物

    公开(公告)号：US4997986A

    公开(公告)日：1991-03-05

    申请号：US270945

    申请日：1988-11-14

    申请人： William L. Mitchell ,  Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  David Hartley

    发明人： William L. Mitchell ,  Ian F. Skidmore ,  Lawrence H. C. Lunts ,  Harry Finch ,  Alan Naylor ,  David Hartley

    IPC分类号： C07C307/10 ,  C07C65/11 ,  C07C217/08 ,  C07C231/12 ,  C07C233/43 ,  C07C275/34 ,  C07C311/08 ,  C07C323/12 ,  C07C323/16 ,  C07C323/25

    CPC分类号： C07C65/11 ,  Y10S514/819 ,  Y10S514/826 ,  Y10S514/886 ,  Y10S514/887 ,  Y10S514/913 ,  Y10S514/925 ,  Y10S514/927

    摘要： 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.

    Aminophenol derivatives
    9.
    发明授权
    Aminophenol derivatives 失效
    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.

    Dichloroaniline derivatives for the therapy or prophylaxysis of a disease associated with reversible airway obstruction
    10.
    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.