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1. 发明公开

EP0286242A2 Ethanolamine derivates, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：乙醇胺衍生物，它们的制备方法和含有它们的化合物的药物组合物。
公开(公告)号：EP0286242A2
公开(公告)日：1988-10-12
申请号：EP88302151.1
申请日：1988-03-11
申请人： GLAXO GROUP LIMITED
发明人： Skidmore, Ian Frederick , Finch, Harry , Mitchell, William Leonard , Naylor, Alan , Lunts, Lawrence Henry , Hartley, David
IPC分类号： C07C93/08 , C07C149/32 , C07C143/75 , C07C127/17 , C07C103/76 , C07D213/65 , C07D215/52 , A61K31/10 , A61K31/135 , A61K31/165
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 where Ar represents
where

R 3 is a bond or a straight or branched C 1 2 alkylene group,
R 4 is a hydroxy group or a group R 5 NH-where
R 5 represents a group CH 3 SO 2 -, HCO-or NH 2 CO-,

where R 6 is a chlorine atom or the group F 3 C-,

k represents an integer from 1 to 8,
m represents zero or an integer from 2 to 7 and
n represents an integer from 2 to 7 with the proviso that the sum total of k. m and n is 4 to 12;
R 1 and R 2 each represents a hydrogen atom or a methyl or ethyl group with the proviso that the sum total of carbon atoms in R 1 and R 2 is not more than 2;
R 30 represents hydrogen or C 12 alkyl;
X represents an oxygen or sulphur atom: and
Y 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 otionally substituted by one or more substituents selected from halogen atoms, or the groups C 1 3 alkyl, C 1 3 alkoxy, hydroxy, -CH 2 OH-, -(CH 2 ) 2 OH, -CO 2 H. -CO 2 CH 3 , ·CO 2 (CH 2 )- 2 CH 3 , -R 7 , COR 7 , -NHCOR s and ·NR 9 SO 2 R 10 ; where
R 7 represents an amino, aminoC 1 3 alkyl, aminoC, 3 dialkyl, pyrrolidino. piperidino. hexamethyleneimino, piperazino, N-methylpiperazino or morpholino group;
R 8 represents a hydrogen atom or a C, 4 alkyl, C, 4 alkoxy, phenyl or amino group;
R 9 represents a hydrogen atom or a methyl group;
R 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, 3 alkyl and C 1 3 alkoxy groups.
The compounds have a stimulant action at β 2 -adrenoreceptors and are useful, in particular, 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）生理学上可接受的盐的化合物和和它们的溶剂合物，其中Ar darstellt 其中R <3>是一个键或直链或支链的C 1-2亚烷基团，R <4> 为羟基或基团R <5> NH，其中R <5> darstellt的基团CH 3 SO 2，HCO或NH 2 CO--，其中R <6>是氯原子或基团F3C ，ķdarstellt在整数从1到8，M darstellt为零或整数2至在整数7和n darstellt从2至7，条件的总和K，M没有和n是4到12; [R <1>和R <2>每一个darstellt氢原子或甲基或乙基，条件的总和中的R的碳原子的那样<1>和R <2>不大于2; [R <3> <0> darstellt氢或C1-2烷基; X darstellt到氧或硫原子; 和Y和Q可以各自代表一个键或氧或硫原子，条件没有氧或硫原子的Y和Q darstellt中的至少一个，并且当Y是键，m是零，或当氧或硫Y的darstellt 原子，m为2至7的整数; P表示被选自卤素原子中的一种或多种取代基，或基团C 1-3烷基，C 1-3烷氧基，羟基，-CH2OH-，otionally取代的苯基 - （CH 2）2 OH，-CO 2 H，-CO 2 CH 3，-CO 2（CH 2 ）2 CH 3，-R <7>，COR <7>，-NHCOR <8>和-NR <9> SO 2 <1> <0>; 其中R <7> darstellt氨基的，aminoC1-3alkyl，aminoC1-3dialkyl，吡咯烷基，哌啶子基，六亚甲基亚，哌嗪子基，N-甲基哌嗪基或吗啉代基团; [R <8>表示一个氢原子或一个C 1-4烷基，C 1-4烷氧基，苯基或氨基; [R <9>代表氢原子或甲基; [R <1> <0>表示一个甲基，苯基，氨基或二甲基氨基; 或P被选自卤素原子或羟基，C 1-3烷基C 1-3烷氧基和基团的一个或两个取代基darstellt吡啶基，任选substituiertem。所述化合物具有在β-2肾上腺素能受体兴奋剂作用和是有用的，特别是，在与可逆气道阻塞相关的疾病的治疗：如哮喘和慢性支气管炎。

2. 发明公开

EP0278727A2 1-(4-Amino-3-chloro-5-trifluoromethylphenyl)-2-(substituted amino)ethanol derivatives and their use in the treatment of respiratory disease 失效
标题翻译： 1-（4-氨基-3-氯-5-三氟甲基苯基）-2-（取代的氨基）乙醇衍生物及其在肺部疾病的治疗中的用途。
公开(公告)号：EP0278727A2
公开(公告)日：1988-08-17
申请号：EP88301064.7
申请日：1988-02-09
申请人： GLAXO GROUP LIMITED
发明人： Lunts, Lawrence Henry Charles , Skidmore, Ian Frederick , Finch, Harry , Naylor, Alan , Campbell, Ian Baxter
IPC分类号： C07C93/08 , C07D213/30 , A61K31/135 , A61K31/44
CPC分类号： C07D213/30
摘要： The present invention provides compounds of the general formula (I)
wherein
X represents a bond, or a C 1-6 alkylene, C 2-6 alkenylene or C 2-6 alkynylene chain, and
Y represents a bond, or a C 1-4 alkylene, C 2-4 alkenylene or C 2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;
R¹ and R² each represent a hydrogen atom or a C 1-3 alkyl group, with the proviso that the sum total of carbon atoms in R¹ and R² is not more than 4; and
Ar represents a pyridyl group optionally substituted by one or two substituents selected from halogen atoms or hydroxy, C 1-3 alkyl and C 1-3 alkoxy groups, or
Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups hydroxy, hydroxyC 1-3 alkyl, C 1-3 alkyl, C 1-3 alkoxy, -NR³R⁴ and -NR⁵COR⁶,
or Ar is a phenyl group substituted by an alkylenedioxy group of formula -O(CH₂) p O-; where
R³ and R⁴ each represent a hydrogen atom or a C 1-4 alkyl group or -NR³R⁴ 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- and -S- or a group -NH- or -N(CH₃)-;
R⁵ represents a hydrogen atom or a C 1-4 alkyl group;
R⁶ represents a hydrogen atom or a C 1-4 alkyl, C 1-4 alkoxy, phenyl or -NR³R⁴ group;
p is an integer 1 or 2;
and physiologically acceptable salts and solvates (eg. hydrates) thereof.
The compounds have a stimulant action at β₂-adreno receptors 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worin X darstellt一个键，或一个C1-6alkylene，C2-6alkenylene或C2-6alkynylene链，和Y darstellt一个键，或一个C 1-4亚烷基，C 2 -C 4alkenylene或C2-4alkynylene链，条件总和碳原子的那样在X和Y不超过8; [R <1>和R <2>分别表示氢原子或C 1-3烷基，条件总和碳原子的R中做<1>和R <2>不大于4; 和Ar darstellt被选自卤素原子或羟基，C 1-3烷基和C 1-3烷氧基，或Ar的一个或两个取代基任选取代的吡啶基表示被一个或多个取代基任选地取代的苯基基团：卤素原子或基团选择羟基，hydroxyC1-3alkyl，C 1-3烷基，C 1-3烷氧基，-NR <3> [R <4>和-NR <5> COR <6>，或Ar是取代的苯基（下式的亚烷基二氧基-O CH 2）p O-; 其中R <3>和R <4>各自表示氢原子或C 1-4烷基或-NR <3> [R <4>形成其中具有5-7个环成员并且任选地在环中含有一个饱和杂环氨基的一个或多个原子选自-O-和-S-或基团-NH-或-N（CH 3）选择 - ; [R <5> darstellt氢原子或C 1-4烷基; [R <6>表示一个氢原子或一个C 1-4烷基，C 1-4烷氧基，苯基或-NR <3> [R <4>基; p是整数1或2; 和生理上可接受的盐和溶剂化物（例如水合物）。所述化合物具有于β-2肾上腺受体兴奋剂动作，并且可以在与可逆气道阻塞相关的疾病的治疗中：如哮喘和慢性支气管炎。

3. 发明公开

EP0162576A1 Ethanolamine compounds 有权
标题翻译： Ethanolamin-Verbindungen。
公开(公告)号：EP0162576A1
公开(公告)日：1985-11-27
申请号：EP85302708.4
申请日：1985-04-17
申请人： GLAXO GROUP LIMITED
发明人： Skidmore, Ian Frederick , Naylor, Alan , Lunts, Lawrence henry Charles , Finch, Harry
IPC分类号： C07D215/26 , C07C93/08 , A61K31/135 , A61K31/47
CPC分类号： C07D215/26 , C07C45/673 , C07C45/68 , C07C49/255 , C07C49/82
摘要： The invention provides compounds of the general formula (I)
wherein

Ar represents a phenyl group optionally substituted by one or two substituents selected from halogen atoms, or C 1-3 alkyl or C 1-3 alkoxy groups, or by an alkylenedioxy group of formula -O(CH 2 ) p O- where p is 1 or 2;
R, and R 2 each represents a hydrogen atom or C 1-3 alkyl group with the proviso that the sum total of carbon atoms in R, and R 2 is not more than 4;
m is an integer from 2 to 8 and
n is an integer from 1 to 7 with the proviso that the sum total of m + n is 4 to 12;
Q represents a group of formula
where
R 3 represents a hydrogen atom or a C 1-3 alkyl group, R a represents:
and R b represents:

where F 4 represents a straight or branched C 2-3 alkylene chain: and physiologically acceptable salts and solvates thereof.

The compounds of formula (l) have a selective stimulant action at (β 2 -adrenoreceptors and are useful, in particular 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表示任选被一个或两个选自卤素原子或C 1-3烷基或C 1-3烷氧基的取代基取代的苯基，或者被亚烷基二氧基式-O（CH 2）p O-，其中p是1或2; R1和R2各自表示氢原子或C1-3烷基，条件是R1和R2中的碳原子总数不大于4; m是2至8的整数，n是1至7的整数，条件是m + n的总和为4至12; Q表示式CHEM的基团，其中R 3表示氢原子或C 1-3烷基，R a表示：CHEM，R b表示：其中R 4表示：代表直链或支链C 2-3亚烷基链; 及其生理上可接受的盐和溶剂合物。式（I）化合物在β2-肾上腺素受体中具有选择性刺激作用，并且特别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。

4. 发明公开

EP0041476A3 Aryl-phenyl-acetylene compounds 有权
标题翻译：芳基 - 苯乙烯化合物
公开(公告)号：EP0041476A3
公开(公告)日：1982-02-24
申请号：EP81810195
申请日：1981-05-22
申请人： CIBA-GEIGY AG
发明人： Brunner, Hans-Georg, Dr. , Schurter, Rolf, Dr. , Szczepanski, Henry, Dr.
IPC分类号： C07C93/08 , C07D295/08 , C07C103/28 , C07D213/30 , C07D213/61 , C07D333/16 , C07C125/065 , C07C123/00 , C07C103/38 , A01N33/04 , A01N43/10
CPC分类号： C07D213/30 , C07D213/61 , C07D213/73 , C07D213/76 , C07D213/80 , C07D213/85 , C07D239/26 , C07D239/30 , C07D251/16 , C07D251/18 , C07D251/20 , C07D263/32 , C07D277/24 , C07D285/08 , C07D295/088 , C07D307/42 , C07D333/16

5. 发明公开

EP0017217A2 Diphenylalkanoether and diphenylalkanone oximeether derivatives, a process for their production, pharmaceutical compositions and their use 有权
标题翻译： Diphenylalkanäther-和Diphenylalkanonoximäther衍生物，它们的制备方法，药物组合物和它们的用途。
公开(公告)号：EP0017217A2
公开(公告)日：1980-10-15
申请号：EP80101748.4
申请日：1980-04-01
申请人： SUMITOMO CHEMICAL COMPANY, LIMITED
发明人： Ono, Keiichi , Kawakami, Hajime , Katsube, Junki
IPC分类号： C07C93/08 , C07C93/14 , C07C131/00 , C07D213/30 , C07D295/08 , C07D307/42 , C07D333/16 , A61K31/13 , A61K31/15 , A61K31/34 , A61K31/38
CPC分类号： C07D213/30 , C07D295/088 , C07D307/42 , C07D333/16 , Y10S514/929
摘要： Diphenylalkanoether and diphenylalkanone oxime-ether derivatives are described of the formula:
wherein R 1 and R 2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, nitro, cyano, di(C 1 -C 4 )alkylamino, amino, benzyloxy, hydroxyl, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfinyl, C 1 -C 4 alkylsulfonyl, C 1 -C 4 alkanoylamino, C 1 -C 4 alkylamino and N-(C 1 -C 4 )alkyl-N-(C 1 -C 4 )alkanoylamino, Z 1 is a group of the formula:
(wherein R 3 and R 4 are each independently a hydrogen atom, a C 1 -C 4 alkyl group or an ar(C 1 -C 4 )alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a nitrogen-containing 5 to 7-membered saturated heterocyclic group optionally having an oxygen atom or an additional nitrogen atom as the hetero atom in addition to the said nitrogen atom and, if having the additional nitrogen atom, bearing a hydrogen atom, a C 1 -C 4 alkyl group, an ar(C,-C 4 )alkyl group or a phenyl group thereon),
is a group of the formula:
or the formula:
A' is a C 2 -C 6 alkylene group and A 2 is a C 2 -C 4 alkylene group, and acid addition salts thereof, which have cerebral vasodilating activity and antihypoxic activity.

6. 发明公开

EP0014017A1 1-(Omega-aminoalkoxy)-3,3,5-trimethylcyclohexanes, processes for their preparation and pharmaceutical compositions containing same 失效
标题翻译： 1-（ω-Aminoalcoxy）-3,3,5-三甲基环己烷，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0014017A1
公开(公告)日：1980-08-06
申请号：EP80200045.5
申请日：1980-01-18
申请人： Chem. Pharmaz. Fabrik Dr. Hermann Thiemann GmbH
发明人： Cambanis, Anton , Mayer, Dieter , Bohn, Helmut , Magda, Stephan , Schmitz, Dieter
IPC分类号： C07C93/08 , A61K31/13
CPC分类号： C07C217/12 , C07C2601/14
摘要： The invention relates to novel 1-(ω-aminoalkoxy)-3,3,5-trimethylcyclohexanes and their salts of the general formula:
where

R, denotes a straight chain or branched alkyl, or an aryl or aralkyl-residue, which may be substituted by alkyl residues or halogen atoms;
R 2 and R 3 denote a straight chain or branched alkyl residue and
n represents 2, 3, or 4,

having valuable cardiovascular properties.
摘要翻译：本发明涉及新的1-（氨基烷氧基的ω）3,3,5- trimethylcyclohexanes及其如下通式的盐：其中R 1表示直链或支链烷基或芳基或芳烷基，以 - 残基，其可以通过烷基残基或卤原子substituiertem; R2和R3表示直链或支链烷基残基，n darstellt 2，3，或4，具有有价值的心血管性能。 Ť

7. 发明公开

EP0278727A3 1-(4-Amino-3-chloro-5-trifluoromethylphenyl)-2-(substituted amino)ethanol derivatives and their use in the treatment of respiratory disease 失效
标题翻译： 1-（4-氨基-3-氯代-5-三氟甲基苯基）-2-（取代的氨基）乙醇衍生物及其在治疗呼吸道疾病中的用途
公开(公告)号：EP0278727A3
公开(公告)日：1990-03-14
申请号：EP88301064.7
申请日：1988-02-09
申请人： GLAXO GROUP LIMITED
发明人： Lunts, Lawrence Henry Charles , Skidmore, Ian Frederick , Finch, Harry , Naylor, Alan , Campbell, Ian Baxter
IPC分类号： C07C93/08 , C07D213/30 , A61K31/135 , A61K31/44
CPC分类号： C07D213/30
摘要： The present invention provides compounds of the general formula (I)
wherein
X represents a bond, or a C 1-6 alkylene, C 2-6 alkenylene or C 2-6 alkynylene chain, and
Y represents a bond, or a C 1-4 alkylene, C 2-4 alkenylene or C 2-4 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is not more than 8;
R¹ and R² each represent a hydrogen atom or a C 1-3 alkyl group, with the proviso that the sum total of carbon atoms in R¹ and R² is not more than 4; and
Ar represents a pyridyl group optionally substituted by one or two substituents selected from halogen atoms or hydroxy, C 1-3 alkyl and C 1-3 alkoxy groups, or
Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms or the groups hydroxy, hydroxyC 1-3 alkyl, C 1-3 alkyl, C 1-3 alkoxy, -NR³R⁴ and -NR⁵COR⁶,
or Ar is a phenyl group substituted by an alkylenedioxy group of formula -O(CH₂) p O-; where
R³ and R⁴ each represent a hydrogen atom or a C 1-4 alkyl group or -NR³R⁴ 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- and -S- or a group -NH- or -N(CH₃)-;
R⁵ represents a hydrogen atom or a C 1-4 alkyl group;
R⁶ represents a hydrogen atom or a C 1-4 alkyl, C 1-4 alkoxy, phenyl or -NR³R⁴ group;
p is an integer 1 or 2;
and physiologically acceptable salts and solvates (eg. hydrates) thereof. The compounds have a stimulant action at β₂-adreno receptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

8. 发明公开

EP0219350A3 Ethanolamine compounds 失效
标题翻译：乙醇胺化合物乙醇胺化合物
公开(公告)号：EP0219350A3
公开(公告)日：1988-06-08
申请号：EP86307976
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
IPC分类号： C07C93/08 , C07C93/10 , A61K31/135 , C07D213/18 , C07C93/14 , C07C103/76 , C07C103/38 , C07C125/065 , C07C127/17 , C07C143/75 , C07D295/08
CPC分类号： A61K31/135
摘要： The 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 )qR, [where R is hydroxy, C 1-6 alkoxy. -NR 3 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 I - 4 alkyl, C I - 4 alkoxy, phenyl or -NR 3 R 4 group), -NR 5 SO 2 R (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 , -SR9 (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 ) t R 11 [where R 11 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 1 and R 2 each represent a hydrogen atom or a C I - 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 30 represents a hydrogen atom or a C 1-3 alkyl group; X represents a C 2 - 8 alkylene chain optionally substituted by one or two C 1-3 alkyl groups, or, when one carbon atom is substituted by two methyl groups, they may be linked to form an ethylene group, and Y represents a C 1-7 alkylene chain optionally substituted by one or two C 1-3 alkyl groups, or, when one carbon atom is substituted by two alkyl groups, they may be linked to form an alkylene group; with the proviso that the sum total of carbon atoms in X and Y is 4 to 12; and with the further proviso that at least one of X and Y is substituted by one or two C 1-3 alkyl groups or an alkylene group; Q represents (where R 12 is a straight or branched Ci.3 alkylene group).

(where one or R 13 and R 14 is a hydroxy group and the other is a hydrogen or halogen atom or a hydroxy group).

[where R' 5 is a group R 16 CO-, R 16 NHCO-, R 16 R 17 NS0 2 - or R 18 SO 2 - (where R 16 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 I - 3 alkyl group),
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.

9. 发明公开

EP0196849A3 Aminohydroxyalkylbenzene anti-obesity and/or anti-hyperglycaemic agents 失效
标题翻译：氨基甲基苯乙酮抗体和/或抗高血压药物
公开(公告)号：EP0196849A3
公开(公告)日：1988-01-07
申请号：EP86302145
申请日：1986-03-24
申请人： BEECHAM GROUP PLC
发明人： Smith, David Glynn , White, Susan Mary
IPC分类号： C07C91/18 , C07C93/06 , C07C91/34 , C07C91/40 , A61K31/135 , C07C87/18 , C07C93/08
CPC分类号： A61K31/135 , A23K20/111 , A61K31/165
摘要： A compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein R A is a group of formula (a):
wherein T represents a group of formula (b):
wherein Q is
, and where
R' is a hydrogen or halogen atom or a -CF 3 , OR 4 , NHR 4 , -NHCOR 4 , -NHCONH 2 , NHSO 2 R 4 , CH 2 OR 4 or -CH 2 SO 2 R 4 group: R 2 is a hydrogen or halogen atom or an -OR 4 group; R 3 is a hydrogen or halogen atome; and R 4 is hydrogen, C 1-6 alkyl or benzyl; X' is a bond or -OCH 2 -; X 2 is a group of formula -CR 5 R 6 -CH 2 -A-wherein R 5 and R 6 are independently hydrogen or methyl; and A is a bond, -CH 2 -, or O; T' represents a hydrogen atom or a group of formula (b) as defined above in respect of T, such that T' and T may be the same or different; R C represents a group (a) as defined above in respect of R A , such that R C and R A may be the same or different; provided that when R A and R C each represent a group of formula:
wherein R is oH or -O-benzyl; then when A is a bond, -CH 2 - or -0, R' is not -CH 2 OH or NHSO 2 -C 1-4 alkyl; processes for the preparation of such compounds and their use in medicine and agriculture.

10. 发明公开

EP0223410A3 Ethanolamine Derivatives 失效
标题翻译：乙醇胺衍生物
公开(公告)号：EP0223410A3
公开(公告)日：1987-11-19
申请号：EP86307981
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
IPC分类号： C07C93/08 , C07C93/14 , C07C149/36 , C07C143/75 , C07D215/22 , C07D295/08 , A61K31/135 , A61K31/16 , A61K31/40 , A61K31/47
CPC分类号： C07D295/096 , C07D215/26
摘要： The 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, C 1-6 alkoxy, nitro, -(CH 2 )qR [where R is hydroxy, -NR 3 R 4 (where R 3 and R 4 each represent 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, C 1-4 alkoxy, phenyl or -NR 3 R 4 group), -NR 5 SO 2 R 7 (where R' 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' is a hydrogen atom, or a C 1-4 alkyl or phenyl group), -SOR 9 , -SO 2 R 9 or -CN, and q represents an integer from 0 to 3], -(CH2) r R'° (where R 10 is a C 1-4 alkoxy group and r represents an integer from 1 to 3) or -O(CH 2 ) t R 11 (where R" represents a hydroxy or C 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 2 ) p O-where p represents an integer 1 or 2; Q represents a group of formula
where R a represents a hydrogen atom or a C 1-3 alkyl group, R b represents
and R c represents
where R represents a straight or branched C 2 . 3 alkylene chain; 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' and R 2 is not more than 4; X represents a C 1-7 alkylene, C 2-7 alkenylene or C 2 . 7 alkynylene chain; and Y represents a bond or a C 1-6 alkylene, C 2 . 6 alkenylene or C26 alkynylene chain with the proviso that the sum total of carbon atoms in X and Y is 2-10, and when X represents C 1-7 alkylene and Y represents a bond or C 1- 6 alkylene, then the group Ar does not represent an unsubstituted phenyl group or a phenyl group substituted by one or two substituents selected solely from halogen atoms or C 1-3 alkyl or C 1-3 alkoxy groups or an alkylenedioxy group -O(CH 2 )pO-;
and physiologically acceptable salts and solvates e.g. hydrates thereof. The compounds have a selective stimulant action at β 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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