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21. 发明公开

EP0220054A3 Ethanolamine derivatives 失效
公开(公告)号：EP0220054A3
公开(公告)日：1987-12-02
申请号：EP86307974
申请日：1986-10-15
申请人： GLAXO GROUP LIMITED
发明人： Finch, Harry , Lunts, Lawrence Henry Charles , Naylor, Alan , Skidmore, Ian Frederick , Campbell, Ian Baxter , Middlemiss, David , Willbe, Charles
IPC分类号： C07D213/38 , C07C143/75 , C07C93/00 , C07C93/08 , C07C127/17 , C07C93/14 , C07C125/065 , C07C103/76 , C07C103/38 , C07D295/08 , A61K31/135
CPC分类号： C07D295/096 , C07D213/65 , Y10S514/826
摘要： The present invention provides compounds of the general formula (I)
wherein
Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C 1-6 alkyl, nitro, -(CH 2 )qR, [where R is hydroxy, C 1-6 alkoxy, -NR3R4 (where R3 and R 4 each represents a hydrogen atom, or a C 1-4 alkyl group, or -NR 3 R 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 3 )-), -NR 5 COR 6 (where R 5 represents a hydrogen atom or a C 1-4 alkyl group, and R 6 represents a hydrogen atom or a C 1-4 alkyl, Ci- 4 alkoxy, phenyl or -NR 3 R 4 group), -NR S S0 2 R 7 (where R 7 represents a C 1-4 alkyl, phenyl or -NR3R4 group), -COR 8 (where R 8 represents hydroxy, C 1-4 alkoxy or-NR 3 R 4 ), -SR 9 (where R 9 is a hydrogen atom, or a C 1-4 alkyl or phenyl group), -SOR 9 , -S0 2 R 9 , or -CN, and q represents an integer from 0 to 3], or -O(CH 2 ) 1 R 10 [where R 10 represents a hydroxy or C 1-4 alkoxy group, and t is an integer 2 or 3], or Ar is a phenyl group substituted by an alkylenedioxy group of formula -O(CH 2 )pO-, where p represents an integer 1 or 2: R 1 and R 2 each represents 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; X represents a bond or a C 1-7 alkylene, C 2 - 7 alkynylene or C 2 - 7 alkenylene 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 2-10; Q represents the group
[where Q 1 represents C 1-3 alkoxy, methanesulphonyl or cyano) or the group -CH 2 NHR 11 (where R 11 represents R 12 CO-. R 12 NHCO-. R 12 R 13 NSO 2 - or R 14 SO 2 -, where R 12 and R 13 each represent a hydrogen atom or a C 1-3 alkyl group, and R 14 represents a C 1-3 alkyl group), or the group -NR 15 R 16 (where R 15 represents a hydrogen atom or a C 1-4 alkyl group, and R 16 represents a hydrogen atom or a C 1-4 alkyl group or, when R 15 is a hydrogen atom. R 16 also represents a C 1-4 alkoxycarbonyl group)]. or Q represents the group
or Q represents a phenyl group substituted by a hydroxy group and optionally also by a halogen atom; and physiologically acceptable salts and solvates (e.g. hydrates)thereof. The compounds have a stimulant action at β2-adrenorecep- tors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

22. 发明公开

EP0220878A2 Ethanolamine compounds 失效
标题翻译： Ethanolaminverbindungen。
公开(公告)号：EP0220878A2
公开(公告)日：1987-05-06
申请号：EP86307975.2
申请日：1986-10-15
申请人： GLAXO GROUP LIMITED
发明人： Finch, Harry , Naylor, Alan , Lunts, Lawrence Henry Charles , Skidmore, Ian Frederick
IPC分类号： C07C93/08 , C07C93/10 , C07C93/14 , A61K31/135 , C07D213/18 , C07D295/08 , C07C103/76 , C07C103/38 , C07C125/065 , C07C127/17 , C07C143/75
CPC分类号： C07D213/65
摘要： he invention provides compounds of the general formula
wherein

Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C 1-6 alkyl, nitro. -(CH 2 ) q R, [where R is hydroxy, C 1-6 alkoxy, -NR 3 R 4 (where R 3 and R 4 each represents a hydrogen atom, or a C 1-4 alkyl group, or -NR 3 R 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 3 )-), -NR 5 COR 6 (where R 6 represents a hydrogen atom or a C 1-4 alkyl group, and R 6 represents a hydrogen atom or a C 1-4 alkyl, C 1-4 alkoxy, phenyl or -NR 3 R 4 group). -NR 5 S0 2 R 7 (where R 7 represents a C 1-4 alkyl, phenyl or -NR 3 R 4 group), -COR 8 (where R 8 represents hydroxy, C 1-4 alkoxy or -NR 3 R 4 ), -SR 9 (where R 9 is a hydrogen atom, or a C 1-4 alkyl or phenyl group). -SOR 9 , -S0 2 R 9 , or -CN, and q represents an integer from 0 to 3], or -O(CH 21 R 11 [where R" represents a hydroxy or C 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 2 )pO-, where p represents 1 or 2;
R' 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;
R 20 represents a C 1-3 alkyl group;
X represents a C 2-8 alkylene C 2-8 alkenylene or C 2-8 alkynylene chain, and
Y represents a C 1-7 alkylene C 2-7 alkenylene or C 2-7 alkynylene chain. with the proviso that the sum total of carbon atoms in X
and Y is 4 to 12; Q represents (a)
EMI PA=2 FR= 1 HE=30 WI=40 TI=CHE (where R' 2 is a straight or branched C 1-3 alkylene group).
(where one of R 13 and R 14 is a hydroxy group and the other is a hydrogen or halogen atom or a hydroxy group),
[where R 15 is a group R 16 CO-, R 16 NHCO-, R 16 R 17 NSO 2 - or R 18 SO 2 - (where R' 6 and R 17 is each a hydrogen atom or a C 1-3 alkyl group and R 18 is a C 1-3 alkyl group) and p is an integer 0 or 1],
(where R 26 and R 27 is each a hydrogen atom or a C 1-3 alkyl group or. when R 26 is a hydrogen atom, R 27 may also be a C 1-4 alkoxycarbonyl group),
(where R 19 is a C 1-3 alkyl group),

or (i)
and physiologically acceptable salts and solvates (e.g. hydrates) thereof.

The compounds have a stimulant action at β 2 -adrenorecep- tors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
摘要翻译：本发明提供了通式（I）的化合物，其中Ar表示任选被一个或多个选自卤原子的取代基取代的苯基，或基团C 1-6烷基，硝基， - （CH 2）q R [其中 R是羟基，C 1-6烷氧基，-NR 3 R 4（其中R 3和R 4各自表示氢原子或C 1-4烷基或-NR 3 R 形成饱和杂环氨基，其具有5-7个环成员并且任选在环中含有一个或多个选自-O-或-S-或-NH-或-N（CH 3） - 基团的原子）， -NR 5 COR 6（其中R 6表示氢原子或C 1-4烷基，R 6表示氢原子或C 1-4烷基，C 1-4烷氧基，苯基或 -NR 3 R 4基团），-NR 5 SO 2 R 7（其中R 7表示C 1-4烷基，苯基或-NR 3 R 4基团），-COR <8>（其中R 8表示羟基，C 1-4烷氧基或-NR 3 R 4），-SR 9（其中R 9为氢原子或C 1-4烷基或苯基），-SOR 9，-SO 2 R 9或-CN，q表示0〜3的整数] 或-O（CH 2 t R 1）其中R 1表示羟基或C 1-4烷氧基，t为2或3]，或Ar为被亚烷基二氧基取代的苯基式-O（CH 2）p O-，其中p表示1或2; R 1和R 2各自表示氢原子或C 1-3烷基，条件是R 1和R 2中的碳原子总和不大于4; R 2表示C 1-3烷基; X表示C2-8亚烷基C2-8亚烯基或C2-8亚炔基链，Y表示C1-7亚烷基C2-7亚烯基或C2-7亚炔基链，条件是X和 Y为4〜12; Q表示（a）（其中R 1> 2是直链或支链C 1-3亚烷基），（其中R 1> 3和R 1> 4 >是羟基，另一个是氢或卤素原子或羟基）， [其中R 1'5是基团R 1 -C 6 - ，R 1' NCO 2 - 或R 1 SO 2 - （其中R 1〜6和R 1〜7）分别为氢原子或C 1-3烷基，R 1是C 1-3烷基），p是整数0或1]，（其中R 2＆lt; 6＆gt;和R R 2为氢原子或C 1-3烷基，或者当R 2为6时，R 2为氢原子时，R 2也可为C 1-4烷氧基羰基），（其中R 1 <9>为C 1-3烷基），及其生理上可接受的盐和溶剂合物（例如水合物）。这些化合物在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。

23. 发明公开

EP0017623A3 Dimethylamino derivatives and their use 有权
标题翻译：二甲基胺衍生物及其用途
公开(公告)号：EP0017623A3
公开(公告)日：1981-07-15
申请号：EP80810110
申请日：1980-04-02
申请人： CIBA-GEIGY AG
发明人： Zondler, Helmut, Dr. , Moser, Roland
IPC分类号： C07C93/04 , C07C93/08 , C07C93/12 , C07C93/16 , C07C93/187 , C07C93/20 , C07C121/34 , C07C125/065 , C07C125/073 , C07C127/15 , C07C127/19
CPC分类号： C07C275/28 , C07C275/14 , C07C275/16 , C08G59/4014 , C08G59/50 , C08G59/52

24. 发明公开

EP0021079A1 Tert. Aminogruppen aufweisende Orthocarbonsäureester, ihre Herstellung und Verwendung als Katalysatoren 失效
标题翻译：叔。 Aminogruppen aufweisendeOrthocarbonsäureester，ihre Herstellung und Verwendung als Katalysatoren。
公开(公告)号：EP0021079A1
公开(公告)日：1981-01-07
申请号：EP80102946.3
申请日：1980-05-27
申请人： BAYER AG
发明人： Meyborg, Holger, Dr. , Illger, Hans-Walter, Dr. , König, Klaus, Dr. , Seifert, Peter, Dr. , Rabe, Hans-Jürgen, Dr.
IPC分类号： C07C93/04 , C07C93/08 , C08G18/18
CPC分类号： C08G18/1833
摘要： Orthocarbonsäureester der allgemeinen Formel
in der

R H, C1-C 19 -Alkyl, Aryl, vorzugsweise H, Methyl oder Phenyl,
R I , R II H, C 1 -C 4 -Alkyl, vorzugsweise H und/oder Methyl, Ethyl,
R III , R IV C 1 -C 6 -Alkyl, zusammen mit N fünf- oder sechsgliedriger Heterocyclus, vorzugsweise Methyl, Ethyl,
n eine ganze Zahl von 1-5, bedeuten.
摘要翻译：其中R表示H，C 1 -C 19 - 烷基，芳基，优选H，甲基或苯基，R 1和R II的通式为“IMAGE”的正己酯代表H，C 1 -C 4烷基，优选H和 /或甲基或乙基，R III和R IV表示C 1 -C 6 - 烷基，或与N一起为五或六元杂环，优选甲基或乙基，n表示1的整数 -5。

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