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    Use of imidazolinylaminoisoindolines and related compounds in the treatment of hyperglycaemia
    3.
    发明公开
    Use of imidazolinylaminoisoindolines and related compounds in the treatment of hyperglycaemia 失效
    Verwendung von Imidazolinylaminoindindenen und verwandten Verbindungen zur Behandlung vonHyperglykämie。

    公开(公告)号：EP0212783A2

    公开(公告)日：1987-03-04

    申请号：EP86303828.7

    申请日：1986-05-20

    申请人： BEECHAM GROUP PLC

    发明人： Cawthorne, Michael Anthony

    IPC分类号： A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/435 ,  A61K31/47 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

    CPC分类号： A61K31/425 ,  A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/435 ,  A61K31/47 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

    摘要： A method for the treatment and/or prophylaxis of hyperglycaemia in human or non-human mammals which comprises administering to the mammal in need of such treatment and/or prophylaxis an effective non-toxic amount of: a compound of formula (I):
    or a pharmaceutically acceptable acid addition salt thereof, wherein each of R' and R 2 , which may be the same or different, represents a hydrogen or halogen atom, or an alkyl or alkoxy group containing 1 to 4 carbon atoms, X represents an oxygen or sulphur atom, an imino group, an acylimino group containing 2 to 4 carbon atoms in the acyl group, or a methylene group, each of n and m, which may be the same or different, represents the number 1, 2 or 3, and p represents the number 2 or 3; with the proviso that when the moiety
    is present in formula (I), then either R 1 or R 2 must represent hydrogen; or a compound of formula (II):
    or a pharmaceutically exeptable add addition saft thereof, wherein each of R 3 and R 4 may be either a hydrogen or halogen atom; or an alkyl or alkoxy group either of which groups may have from 1 to 4 carbon atoms; providing that either R 3 or R 4 must be hydrogen; R 5 and R 6 can be identical or different and either a hydrogen or an alkyl with 1 to 4 carbon atoms, and R 7 , R 8 , R 9 and R 10 can be identical or different and either hydrogen or an alkyl with 1 to 4 carbon atoms, or in which R 7 and R 8 together represent an ethylene group with the further proviso that when R and R 8 represent an ethylene group then at least one of R 5 , R 6 , R 9 and R 10 represents an alkyl group with 1 to 4 carbon atoms; and compositions for use in such method.

    摘要翻译： 一种用于治疗和/或预防人或非人哺乳动物高血糖症的方法，其包括向需要这种治疗和/或预防有效的无毒量的哺乳动物施用：式（I）的化合物： CHEM>或其药学上可接受的酸加成盐，其中R 1和R 2各自可以相同或不同，表示氢或卤素原子，或含有1至4个碳原子的烷基或烷氧基 原子，X表示氧或硫原子，酰亚胺基，亚氨基，酰基中含有2至4个碳原子的酰亚胺基或可以相同或不同的n和m各自的亚甲基表示数 1,2或3，p表示数字2或3; 条件是当式（I）中存在部分时，R 1或R 2必须表示氢; 或式（II）的化合物：或其药学上可接受的酸加成盐，其中R 3和R 4各自可以是氢或卤素原子; 或者这些基团可以具有1至4个碳原子的烷基或烷氧基; 条件是R 3或R 4必须是氢; R 5和R 6可以相同或不同，可以是氢或具有1至4个碳原子的烷基，R 7，R 8，R 9和R 1 <0 >可以是相同或不同的，氢或具有1至4个碳原子的烷基，或其中R 7和R 8一起代表乙烯基，另外条件是当R 7和R 8 >表示亚乙基，则R 5，R 6，R 9和R 1至少有一个表示具有1至4个碳原子的烷基; 和用于这种方法的组合物。

    Use of imidazolinylaminoisoindolines and related compounds in the treatment of hyperglycaemia
    4.
    发明公开
    Use of imidazolinylaminoisoindolines and related compounds in the treatment of hyperglycaemia 失效
    咪唑啉氨基吲哚和相关化合物在治疗高血压中的应用

    公开(公告)号：EP0212783A3

    公开(公告)日：1989-12-13

    申请号：EP86303828.7

    申请日：1986-05-20

    申请人： BEECHAM GROUP PLC

    发明人： Cawthorne, Michael Anthony

    IPC分类号： A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/435 ,  A61K31/47 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

    CPC分类号： A61K31/425 ,  A61K31/40 ,  A61K31/415 ,  A61K31/42 ,  A61K31/435 ,  A61K31/47 ,  A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

    摘要： A method for the treatment and/or prophylaxis of hyperglycaemia in human or non-human mammals which comprises administering to the mammal in need of such treatment and/or prophylaxis an effective non-toxic amount of: a compound of formula (I):
    or a pharmaceutically acceptable acid addition salt thereof, wherein each of R' and R 2 , which may be the same or different, represents a hydrogen or halogen atom, or an alkyl or alkoxy group containing 1 to 4 carbon atoms, X represents an oxygen or sulphur atom, an imino group, an acylimino group containing 2 to 4 carbon atoms in the acyl group, or a methylene group, each of n and m, which may be the same or different, represents the number 1, 2 or 3, and p represents the number 2 or 3; with the proviso that when the moiety
    is present in formula (I), then either R 1 or R 2 must represent hydrogen; or a compound of formula (II):
    or a pharmaceutically exeptable add addition saft thereof, wherein each of R 3 and R 4 may be either a hydrogen or halogen atom; or an alkyl or alkoxy group either of which groups may have from 1 to 4 carbon atoms; providing that either R 3 or R 4 must be hydrogen; R 5 and R 6 can be identical or different and either a hydrogen or an alkyl with 1 to 4 carbon atoms, and R 7 , R 8 , R 9 and R 10 can be identical or different and either hydrogen or an alkyl with 1 to 4 carbon atoms, or in which R 7 and R 8 together represent an ethylene group with the further proviso that when R and R 8 represent an ethylene group then at least one of R 5 , R 6 , R 9 and R 10 represents an alkyl group with 1 to 4 carbon atoms; and compositions for use in such method.

    2-Hydroxy-3-aryloxypropyl or 2-hydroxy-2-benzofuranyl ethyl tertiary amine having an anti-hyperglycaemic and/or anti-obesity activity
    5.
    发明公开
    2-Hydroxy-3-aryloxypropyl or 2-hydroxy-2-benzofuranyl ethyl tertiary amine having an anti-hyperglycaemic and/or anti-obesity activity 失效
    2-羟基-3-芳氧基丙基醚2-羟基-2-苯并呋喃基乙基叔胺Amin mit antihyperglycemischer und / oderAntiobesitäts-Wirkung。

    公开(公告)号：EP0170121A1

    公开(公告)日：1986-02-05

    申请号：EP85108609.0

    申请日：1985-07-10

    申请人： BEECHAM GROUP PLC

    发明人： Ainsworth, Anthony Trevor ,  Cawthorne, Michael Anthony

    IPC分类号： C07C217/04 ,  C07C229/38 ,  C07C311/16 ,  C07D307/80 ,  A61K31/135 ,  A61K31/34

    CPC分类号： C07D307/81 ,  C07C217/62 ,  C07C229/38

    摘要： A compound of formula (A):

    wherein

    X' represents a 2-hydroxy-3-aryloxypropyl radical unsubstituted or substituted in the aryl moiety or a 2-hydroxy-2-benzofuranylethyl group; and
    X 2 represents a 2-hydroxy-3-aryloxypropyl or 2-hydroxy-2-arylethyl radical unsubstituted or substituted in the aryl moiety or a 2-hydroxy-2-benzofuranylethyl group; and
    X 3 represents a 2- or 3-arylpropyl or 2-aryloxyethyl radical substituted in the aryl moiety and unsubstituted or methyl-substituted in the aryl chain; or a compound of formula (A) wherein one of the -CHOH- moieties in any one of the 2-hydroxyethyl or 2-hydroxypropyl moieties is present as a carbonyl group and/or a compound of formula (A) wherein up to two of the aforementioned -CHOH- moieties may be present in the form of a pharmaceutically acceptable in-vivo hydrolysable ester; or a pharmaceutically acceptable salt thereof; a process for preparing such compounds and pharmaceutical compositions containing them and their use in medicine and agriculture.

    摘要翻译： 式（A）的化合物：其中X 1表示在芳基部分未取代或取代的2-羟基-3-芳氧基丙基或2-羟基-2-苯并呋喃基乙基; X 2表示在芳基部分或2-羟基-2-苯并呋喃基乙基中未取代或取代的2-羟基-3-芳氧基丙基或2-羟基-2-芳基乙基; 并且X 3表示在芳基中被取代的未取代或甲基取代的2-或3-芳基丙基或2-芳氧基乙基; 或其中一个2-羟乙基或2-羟丙基部分中的一个-CHOH-部分作为羰基存在的式（A）化合物和/或式（A）的化合物，其中至多两个 上述-CHOH-部分可以以药学上可接受的体内可水解的酯的形式存在; 或其药学上可接受的盐; 制备这种化合物的方法和含有它们的药物组合物及其在医药和农业中的应用。