首页> 外国专利> METHOD OF OBTAINING NOVEL DERIVATIVES OF 1,2,3,5-TETRAHYDROIMIDAZO(2,1-B)QUINAZOLINE

METHOD OF OBTAINING NOVEL DERIVATIVES OF 1,2,3,5-TETRAHYDROIMIDAZO(2,1-B)QUINAZOLINE

机译:获得1,2,3,5-四氢咪唑啉(2,1-B)喹唑啉的新衍生物的方法

摘要

Compounds according to the formula IMAGE (I) and the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer of 1 to 6; R1 is hydrogen or alkyl of 1 to 4 carbons; R2 is hydrogen or R1 and R2 are combined to form an oxo group; R3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl or hydroxy lower alkyl; R4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl; Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy; A is an amide forming group wherein the nitrogen substituents are: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms; cycloalkyl of 3 to 7 carbon atoms or cycloalkyl lower alkyl of 4 to 11 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, OH, -OCOR5, halo, -NH2, -N(R5)2, -NHCOR5, -COOH, or -COO(R5) group wherein R5 is lower alkyl; phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with 1 or more lower alkyl, halo or lower alkoxy groups or an NH2, -N(R5)2, -NHCOR5, -COOH, or -COOR5 group wherein R5 is lower alkyl; morpholinyl; piperidinyl; perhexylenyl; N-loweralkylpiperazinyl; tetrahydroquinolinyl; tetrahydroisoquinolinyl; (+/-)-decahydroquinolinyl or indolinyl. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic agents and the like in mammals.
机译:根据式(I)的化合物及其药学上可接受的酸加成盐,其中:n为1至6的整数; R1是氢或1-4个碳的烷基; R 2为氢或R 1和R 2结合形成氧代基; R3是氢,1-6个碳的烷基,苯基,苄基或羟基低级烷基; R4是氢,1-6个碳的烷基,苄基或羟基低级烷基; Y是氢,1-4个碳原子的烷基,卤素或低级烷氧基; A是酰胺形成基团,其中氮取代基是:氢;和1-6个碳原子的烷基; 1至6个碳原子的羟烷基及其1至6个碳原子的脂族酰化物或7至12个碳原子的芳基酰化物;具有3至7个碳原子的环烷基或具有4至11个碳原子的环烷基低级烷基,其中环烷基环未被取代或被低级烷基,低级烷氧基,OH,-OCOR5,卤素,-NH2,-N(R5)2取代, -NHCOR5,-COOH或-COO(R5)基团,其中R5是低级烷基;苯基或苯基低级烷基,其中苯基未被取代或被1个或多个低级烷基,卤代或低级烷氧基或NH 2,-N(R 5)2,-NHCOR 5,-COOH或-COOR 5基取代,其中R 5为低级烷基;吗啉基哌啶基;过己烯基; N-低级烷基哌嗪基;四氢喹啉基;四氢异喹啉基; (+/-)-十氢喹啉基或茚满基。这些化合物是在哺乳动物中用作抗血栓形成剂等的环状AMP磷酸二酯酶抑制剂。

著录项

  • 公开/公告号PL142959B1

    专利类型

  • 公开/公告日1987-12-31

    原文格式PDF

  • 申请/专利权人

    申请/专利号PL19840253009

  • 发明设计人

    申请日1984-02-15

  • 分类号C07D487/04;

  • 国家 PL

  • 入库时间 2022-08-22 06:59:10

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