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    • 1. 发明授权
    • Antisecretory heterocyclic amidine compounds
    • 防雾杂环脒化合物
    • US4252819A
    • 1981-02-24
    • US934276
    • 1978-08-16
    • Yasufumi HirataIsao YanagisawaToshinari TamuraMasaaki Takeda
    • Yasufumi HirataIsao YanagisawaToshinari TamuraMasaaki Takeda
    • C07D233/64A61K31/40A61K31/4402A61K31/4418A61K31/4427A61K31/455A61P43/00C07D213/30C07D213/32C07D213/68C07D213/86C07D233/54C07D277/26C07D307/52C07D401/12C07D401/14C07D413/12A61K31/34A61K31/38C07D307/54C07D333/24
    • C07D213/30C07D213/32C07D213/68C07D213/86C07D233/64C07D277/26C07D307/52
    • Novel heterocyclic compounds shown by the formula ##STR1## wherein Het represents a 5-membered or 6-membered heterocyclic group which may have substituent(s); Z represents a sulfur atom or oxygen atom; X represents an oxygen atom or the unsubstituted or substituted imino group shown by N--R.sub.1 (wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a cyano group, an unsubstituted or alkyl substituted carbamoyl group, an unsubstituted or lower alkyl substituted thiocarbamoyl group, or a lower alkanoylamino group); Y represents a hydrogen atom, a lower alkyl group which may have substituent(s), a cycloalkyl group of 3-6 carbon atoms, a lower alkenyl group, a lower alkynyl group, an aryl group which may have substituent(s), an aralkyl group which may have substituent(s), a hydroxyl group, a cyano group, a carbamoyl group, an amidino group, an alkanoyl group which may have been substituted by halogen atom(s),an alkanoylamino group, an arylcarbonylamino group, an alkylamino group, an arylamino group, an arylsulfamoyl group, a lower alkoxycarbamoyl group, or an oxamoylamino group; and m and n represent an integer of 1-3; when X is N-R.sub.1, said X and Y may combine with each other to form a 5-membered or 6-membered heterocyclic ring containing 2-3 nitrogen atoms which may have substituent(s), and the pharmaceutically acceptable acid addition salts thereof.The compounds of this invention are useful as gastric acid secretion inhibitors.
    • 式中,Het表示可具有取代基的5元或6元杂环基的新型杂环化合物。 Z表示硫原子或氧原子; X表示氧原子或由N-R 1表示的未取代或取代的亚氨基(其中R 1为氢原子,低级烷基,氰基,未取代或烷基取代的氨基甲酰基,未取代或低级烷基取代的硫代氨基甲酰基 ,或低级烷酰氨基); Y表示氢原子,可具有取代基的低级烷基,3-6个碳原子的环烷基,低级烯基,低级炔基,可具有取代基的芳基, 可以具有取代基的芳烷基,羟基,氰基,氨基甲酰基,脒基,可被卤素原子取代的烷酰基,烷酰基氨基,芳基羰基氨基, 烷基氨基,芳基氨基,芳基氨磺酰基,低级烷氧基氨基甲酰基或氨甲酰基氨基; m和n表示1-3的整数; 当X为N-R 1时,所述X和Y可以彼此结合形成含有2-3个可具有取代基的氮原子的5元或6元杂环,及其药学上可接受的酸加成盐 。 本发明的化合物可用作胃酸分泌抑制剂。
    • 2. 发明授权
    • Antisecretory imidazole amidine compounds, composition and method of use
    • 咪唑咪唑类化合物,组成及使用方法
    • US4379158A
    • 1983-04-05
    • US193742
    • 1980-10-03
    • Yasufumi HirataIsao YanagisawaToshinari TamuraMasaaki Takeda
    • Yasufumi HirataIsao YanagisawaToshinari TamuraMasaaki Takeda
    • C07D213/32C07D213/68C07D213/86C07D233/54C07D233/64C07D277/26C07D277/30C07D307/52A61K31/615C07D401/12
    • C07D213/86C07D213/32C07D213/68C07D233/64C07D277/26C07D307/52
    • Novel heterocyclic compounds shown by the formula ##STR1## wherein Het represents a 5-membered or 6-membered heterocyclic group which may have substituent(s); Z represents a sulfur atom or oxygen atom; X represents an oxygen atom or the unsubstituted or substituted imino group shown by N--R.sub.1 (wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a cyano group, an unsubstituted or alkyl substituted carbamoyl group, an unsubstituted or lower alkyl substituted thiocarbamoyl group, or a lower alkanoylamino group); Y represents a hydrogen atom, a lower alkyl group which may have substituent(s), a cycloalkyl group of 3-6 carbon atoms, a lower alkenyl group, a lower alkynyl group, an aryl group which may have substituent(s), an aralkyl group which may have substituent(s), a hydroxyl group, a cyano group, a carbamoyl group, an amidino group, an alkanoyl group which may have been substituted by halogen atom(s), an alkanoylamino group, an arylcarbonylamino group, an alkylamino group, an arylamino group, an arylsulfamoyl group, a lower alkoxycarbamoyl group, or an oxamoylamino group; and m and n represent an integer of 1-3; when X is N--R.sub.1, said X and Y may combine with each other to form a 5-membered or 6-membered heterocyclic ring containing 2-3 nitrogen atoms which may have substituent(s), and the pharmacologically acceptable acid addition salts thereof.The compounds of this invention are useful as gastric acid secretion inhibitors.
    • 式中,Het表示可具有取代基的5元或6元杂环基的新型杂环化合物。 Z表示硫原子或氧原子; X表示氧原子或由N-R 1表示的未取代或取代的亚氨基(其中R 1为氢原子,低级烷基,氰基,未取代或烷基取代的氨基甲酰基,未取代或低级烷基取代的硫代氨基甲酰基 ,或低级烷酰氨基); Y表示氢原子,可具有取代基的低级烷基,3-6个碳原子的环烷基,低级烯基,低级炔基,可具有取代基的芳基, 可以具有取代基的芳烷基,羟基,氰基,氨基甲酰基,脒基,可被卤素原子取代的烷酰基,烷酰基氨基,芳基羰基氨基, 烷基氨基,芳基氨基,芳基氨磺酰基,低级烷氧基氨基甲酰基或氨甲酰基氨基; m和n表示1-3的整数; 当X是N-R1时,所述X和Y可以彼此结合形成含有2-3个可具有取代基的氮原子的5元或6元杂环,其药理学上可接受的酸加成盐 。 本发明的化合物可用作胃酸分泌抑制剂。
    • 4. 发明授权
    • Guanidinothiazole compounds, and medical compositions containing them
    • 胍基噻唑化合物和含有它们的医药组合物
    • US4362736A
    • 1982-12-07
    • US127902
    • 1980-03-06
    • Yasufumi HirataIsao YanagisawaYoshio IshiiMasaaki Takeda
    • Yasufumi HirataIsao YanagisawaYoshio IshiiMasaaki Takeda
    • C07D277/38C07D277/46C07D277/48C07D277/20A61K31/425
    • C07D277/48C07D277/46
    • Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, Y represents a sulfur atom or a methylene group, m and n each represents an integer of 1-3, A represents the group shown by ##STR2## (wherein R.sub.1 represents a hydrogen atom, a cyano group, a carbamoyl group, a ureido group, a hydroxyl group, a lower alkoxy group, a lower acyl group, an acylamino group, an arylsulfamoyl group, an aralkyl group or a carboxymethyl group, an arylsulfamoyl group, an aralkyl group or a carboxymethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cyano group or a lower acyl group, and R.sub.3 represents a hydrogen atom, a lower alkyl group, a hydroxyl group or a sulfamoyl group), and the pharmacologically acceptable acid addition salts thereof; these compounds are useful as gastric acid secretion inhibitors.
    • 新颖的通式为“IMAGE”的胍基噻唑化合物,其中R表示氢原子或低级烷基,Y表示硫原子或亚甲基,m和n各自表示1-3的整数,A表示由 (其中R 1表示氢原子,氰基,氨基甲酰基,脲基,羟基,低级烷氧基,低级酰基,酰氨基,芳基氨磺酰基,芳烷基或 羧甲基,芳基氨磺酰基,芳烷基或羧甲基,R2表示氢原子,低级烷基,低级烯基,低级炔基,氰基或低级酰基,R3表示氢 原子,低级烷基,羟基或氨磺酰基)及其药理学上可接受的酸加成盐; 这些化合物可用作胃酸分泌抑制剂。