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    • 3. 发明授权
    • Amine derivatives
    • 胺衍生物
    • US4317819A
    • 1982-03-02
    • US213680
    • 1980-12-05
    • John W. ClitherowBarry J. PriceJohn BradshawMichael Martin-Smith
    • John W. ClitherowBarry J. PriceJohn BradshawMichael Martin-Smith
    • A61K31/155A61K31/335A61K31/38A61P1/00C07C67/00C07C209/00C07C211/27C07C213/00C07C217/48C07C239/00C07C275/12C07C279/04C07C279/28C07C301/00C07C311/64C07C325/00C07C335/08C07D233/64C07D295/096C07D307/38C07D307/42C07D307/52C07D333/14A61K31/17C07C127/17C07C129/12
    • C07D295/096C07C279/28C07D307/38C07D307/42C07D307/52C07D333/14Y10S514/886Y10S514/926Y10S514/927
    • The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.6 ;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2 and 5 positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 and 3 or 1 and 4 positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4 and Alk represents a straight chain alkylene group of 1 to 3 carbon atoms,andR.sub.2 represents lower alkyl or the group--(CH.sub.2).sub.y E(CH.sub.2).sub.x Gin whichy represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 -- group, x represents zero, 1 or 2;E represents --CH.sub.2 --, --O-- or --S--; andG represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring, or G represents the group ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; and R.sub.4 ' and R.sub.5 ' which may be the same or different represent any of the groups defined for R.sub.4 or R.sub.5.The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.
    • 本发明提供了通式(I)的化合物及其生理上可接受的盐,水合物和生物前体,其中Y和Z可以相同或不同,各自表示氧,硫,= CHNO 2或= NR 3,其中R 3 是氢,硝基,氰基,低级烷基,芳基,烷基磺酰基或芳基磺酰基; p的值为2到12; R 1表示其中可以相同或不同的R 4和R 5各自表示氢,低级烷基,环烷基,低级烯基,芳烷基或被氧原子间隔的低级烷基或基团> N-R6,其中R 6表示 氢或低级烷基,或R4和R5与它们所连接的氮原子一起形成可含有另外的氧原子或基团> NR 6的5至7元饱和杂环; Q表示呋喃或噻吩环,其中与分子的其余部分结合通过2和5位的键,或苯环,其中结合到分子的其余部分通过1和3或1的键和 4个职位; X表示-CH 2 - , - O-或-S-; n表示0或1; m表示2,3或4,Alk表示1〜3个碳原子的直链亚烷基,R2表示低级烷基或 - (CH2)yE(CH2)xG,y表示2,3或4或可以 当E是-CH 2 - 基时,x代表0或1; E表示-CH 2 - , - O-或-S-; 并且G表示单环5或6元碳环或杂环芳环,或G表示基团,其中Q'表示为Q定义的任何环; Alk'代表为Alk定义的任何组; 和可以相同或不同的R 4'和R 5'表示对于R 4或R 5定义的任何基团。 式(I)化合物具有作为选择性组胺H2拮抗剂的药理学活性。
    • 4. 发明授权
    • Amine derivatives
    • 胺衍生物
    • US4264614A
    • 1981-04-28
    • US95065
    • 1979-11-16
    • John W. ClitherowBarry J. PriceJohn Bradshaw
    • John W. ClitherowBarry J. PriceJohn Bradshaw
    • A61K31/155A61K31/335A61K31/38A61P1/00C07C67/00C07C209/00C07C211/27C07C213/00C07C217/48C07C239/00C07C275/12C07C279/04C07C279/28C07C301/00C07C311/64C07C325/00C07C335/08C07D233/64C07D295/096C07D307/38C07D307/42C07D307/52C07D333/14A61K31/34C07D307/68C07D333/38
    • C07D295/096C07C279/28C07D307/38C07D307/42C07D307/52C07D333/14Y10S514/886Y10S514/926Y10S514/927
    • The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, =CHNO.sub.2 or =NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.6 ;Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2 and 5 positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1 and 3 or 1 and 4 positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero or 1;m represents 2, 3 or 4 andAlk represents a straight chain alkylenegroup of 1 to 3 carbon atoms;and R.sub.2 represents lower alkyl or the group--(CH.sub.2).sub.y E(CH.sub.2).sub.x Gin whichY represents 2, 3 or 4 or can additionallyrepresent zero or 1 when E is a --CH.sub.2 -- group;x represents zero, 1 or 2;E represents --CH.sub.2 --, --0-- or --S--; andG represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring, or G represents the group ##STR3## where Q' represents any of the rings defined for Q;Alk' represents any of the groups defined for Alk;and R.sub.4 ' and R.sub.5 ' which may be the same or different represent any of the groups defined for R.sub.4 or R.sub.5.The compounds of formula (I) have pharmacological activity as selective histamine H.sub.2 -antagonists.
    • 本发明提供了通式(I)的化合物及其生理上可接受的盐,水合物和生物前体,其中Y和Z可以相同或不同,各自表示氧,硫,= CHNO 2或= NR 3,其中R 3 是氢,硝基,氰基,低级烷基,芳基,烷基磺酰基或芳基磺酰基; p的值为2到12; R 1表示其中可以相同或不同的R 4和R 5各自表示氢,低级烷基,环烷基,低级烯基,芳烷基或被氧原子间隔的低级烷基或基团> N-R6,其中R 6表示 氢或低级烷基,或R4和R5与它们所连接的氮原子一起形成可含有另外的氧原子或基团> NR 6的5至7元饱和杂环; Q表示呋喃或噻吩环,其中与分子的其余部分结合通过2和5位的键,或苯环,其中结合到分子的其余部分通过1和3或1的键和 4个职位; X表示-CH 2 - , - O-或-S-; n表示0或1; m表示2,3或4,Alk表示1〜3个碳原子的直链亚烷基; 并且R 2表示低级烷基或基团 - (CH 2)y E(CH 2)x G,其中Y表示2,3或4,或者当E是-CH 2 - 基时,可以另外表示0或1; x表示零,1或2; E表示-CH 2 - , - O-或-S-; 并且G表示单环5或6元碳环或杂环芳环,或G表示基团,其中Q'表示为Q定义的任何环; Alk'代表为Alk定义的任何组; 和可以相同或不同的R 4'和R 5'表示对于R 4或R 5定义的任何基团。 式(I)化合物具有作为选择性组胺H2拮抗剂的药理学活性。