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1. 发明授权

US4937268A Chemical compounds 失效
标题翻译：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.

2. 发明授权

US5109023A Phenethanolamine derivatives 失效
公开(公告)号：US5109023A
公开(公告)日：1992-04-28
申请号：US622505
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 a method of treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis, utilizing the compounds of the formula ##STR1## or a physiological acceptable salt or solvate thereof, wherein Q represents a 1- or 2- naphthalenyl group.

3. 发明授权

US5099068A 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.

4. 发明授权

US4997986A Phenethanolamine derivatives 失效
标题翻译：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.

5. 发明授权

US5283262A Phenethanolamine derivatives 失效
标题翻译：苯乙醇胺衍生物
公开(公告)号：US5283262A
公开(公告)日：1994-02-01
申请号：US812757
申请日：1991-12-23
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 , A61K31/135
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## or a physiologically acceptable salt or solvate thereof, wherein Q represents a 1- or 2-naphthalenyl group.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.
摘要翻译：本发明提供通式（I）的化合物或其生理学上可接受的盐或溶剂化物，其中Q表示1-或2-萘基。化合物在β2肾上腺素受体具有刺激作用，可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。

6. 发明授权

US5066678A Phenethandamine derivatives and pharmaceutical use thereof 失效
标题翻译：苯并咪唑衍生物及其药物用途
公开(公告)号：US5066678A
公开(公告)日：1991-11-19
申请号：US512874
申请日：1990-04-23
申请人： Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor , Ian B. Campbell , Charles Willbe , William L. Mitchell , Stephen Swanson , Brian D. Judkins
发明人： Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor , Ian B. Campbell , Charles Willbe , William L. Mitchell , Stephen Swanson , Brian D. Judkins
IPC分类号： C07C307/06 , A61K31/135 , A61K31/18 , C07C213/00 , C07C217/08 , C07C217/46 , C07C233/36 , C07C233/43 , C07C275/10 , C07C275/14 , C07C311/04 , C07C311/08 , C07C311/35
CPC分类号： C07C217/08 , C07C311/35 , C07C2101/08 , C07C2101/14
摘要： The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof; wherein;R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a C.sub.1-3 -alkyl group with the proviso that the sum total of carbon atom in R.sup.1 and R.sup.2 is not more than 4;X represents a direct bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene group and Y represents a direct bond or a C.sub.1-6 alkylene C.sub.2-6 alkenylene or C.sub.2-6 alknylene group with the proviso that the sum total of carbon atoms in X and Y is not more than 10;W represents a group ##STR2## wherein Z represents a group R.sup.3 (CH.sub.2).sub.q where q is 0, 1 or 2 and R.sup.3 is a group R.sup.4 CONH--, R.sup.4 NHCONH--, R.sup.4 R.sup.5 NSO.sub.2 NH--, R.sup.6 SO.sub.2 NH-- or --OH;R.sup.4 and R.sup.5 each represent a hydrogen atom or a C.sub.1-3 alkyl group;R.sup.6 represents a C.sub.1-3 alkyl group;R.sup.7 represents a chlorine atom or the group --CF.sub.3 ;A represents a straight or branched C.sub.1-6 alkyl group, a C.sub.3-8 cycloalkyl group, either of which may be saturated or unsaturated, or a C.sub.1-6 alkoxy group, with the proviso that the sum total of carbon atoms in A and Y is not less than 5;having a stimulant action at .beta..sub.2 -adrenoreceptors and are useful in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

7. 发明授权

US5039697A Ethanolamine derivatives 失效
标题翻译：乙醇胺衍生物
公开(公告)号：US5039697A
公开(公告)日：1991-08-13
申请号：US521107
申请日：1990-05-09
申请人： Ian F. Skidmore , Harry Finch , Alan Naylor , Lawrence H. C. Lunts , Charles Willbe , David Middlemiss
发明人： Ian F. Skidmore , Harry Finch , Alan Naylor , Lawrence H. C. Lunts , Charles Willbe , David Middlemiss
IPC分类号： C07D307/81 , A61K31/34 , A61K31/38 , A61P11/08 , C07D307/42 , C07D307/68 , C07D307/80 , C07D333/16 , C07D333/20 , C07D333/34 , C07D333/38 , C07D333/56 , C07D333/58
CPC分类号： C07D307/42 , C07D307/68 , C07D307/80 , C07D333/16 , C07D333/34 , C07D333/38 , C07D333/56
摘要： The invention relates to compounds of general formula (I) and physiologically acceptable salts and solvates thereof, methods for their preparation and pharmaceutical formulations thereof. ##STR1## wherein Ar represents a substituted phenyl or nitrogen-containing heterocyclic ring;X and Y represent alkylene, alkenylene or alkynylene chains;R.sup.1, R.sup.2 and R.sup.18 each represent hydrogen or alkyl groups; andQ represents an optionally substituted furan or thiophene ring.The compounds of the invention have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
摘要翻译：本发明涉及通式（I）的化合物及其生理学上可接受的盐和溶剂合物，其制备方法及其药物制剂。（I）其中Ar表示取代的苯基或含氮杂环; X和Y表示亚烷基，亚烯基或亚炔基链; R1，R2和R18各自表示氢或烷基; Q表示任选取代的呋喃或噻吩环。本发明的化合物在β2-肾上腺素受体具有刺激作用，并且可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。

8. 发明授权

US4992474A Phenethanolamine derivatives 失效
标题翻译：苯乙醇胺衍生物
公开(公告)号：US4992474A
公开(公告)日：1991-02-12
申请号：US397664
申请日：1989-08-23
申请人： Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor
发明人： Ian F. Skidmore , Lawrence H. C. Lunts , Harry Finch , Alan Naylor
IPC分类号： C07C217/48 , A61K31/135 , A61K31/335 , A61K31/357 , A61K31/36 , A61P11/00 , A61P25/02 , C07C33/46 , C07C43/174 , C07C43/178 , C07C43/225 , C07C45/00 , C07C45/30 , C07C47/277 , C07C49/255 , C07C59/13 , C07C59/66 , C07C67/00 , C07C213/00 , C07C213/02 , C07C217/10 , C07C217/14 , C07C217/28 , C07C217/64 , C07C229/38 , C07D303/40 , C07D309/12 , C07D309/18 , C07D317/54 , C07D317/58 , C07D319/06 , C07D319/08 , C07D319/18
CPC分类号： C07C45/004 , C07C229/38 , C07C309/00 , C07C33/46 , C07C43/174 , C07C43/1742 , C07C43/1782 , C07C43/225 , C07C45/30 , C07C47/277 , C07C49/255 , C07C59/66 , C07D303/40 , C07D309/12 , C07D317/54 , C07D319/06 , Y02P20/55 , Y10S514/826 , Y10S514/863 , Y10S514/886 , Y10S514/887 , Y10S514/906 , Y10S514/913 , Y10S514/925 , Y10S514/926 , Y10S514/927 , Y10S514/928
摘要： Phenethanolamine derivatives are disclosed of formula ##STR1## wherein m is 2 to 8; n is 1 to 7 provided that m+n is 4 to 12;Ar is phenyl or phenyl substituted by one or two halogen atoms, alkyl or alkoxy groups or by an alkylenedioxy group;R.sup.1 and R.sup.2 are hydrogen or alkyl provided that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4;and the 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 obstructions such as asthma and chronic bronchitis. The compounds may be formulated in conventional manner as pharmaceutical compositions with physiologically acceptable carriers or excipients.The compounds may be prepared, for example by alkylation of an amine: ##STR2## where R.sup.3, R.sup.5 and R.sup.6 is hydrogen or a protecting group, followed by removal of any protecting group.
摘要翻译：公开了苯甲醇胺衍生物，其中m为2至8; n为1〜7，条件是m + n为4〜12; Ar是被一个或两个卤素原子，烷基或烷氧基或亚烷基二氧基取代的苯基或苯基; R1和R2是氢或烷基，条件是R1和R2中碳原子的总和不大于4; 及其生理上可接受的盐和溶剂化物。所述化合物在β2肾上腺素受体具有选择性兴奋剂作用，并且可以特别用于治疗与可逆气道阻塞物如哮喘和慢性支气管炎相关的疾病。化合物可以以常规方式配制成具有生理上可接受的载体或赋形剂的药物组合物。化合物可以例如通过烷基化胺制备：其中R 3，R 5和R 6是氢或保护基，然后除去任何保护基。

9. 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.

10. 发明授权

US5006556A Dichloroaniline derivatives for the therapy or prophylaxysis of a disease associated with reversible airway obstruction 失效
标题翻译：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.

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