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19 条记录 (耗时 0.017 秒)

    Guanidino-substituted heterocyclic derivatives having histamine H-2 antagonist activity
    5.
    发明公开
    Guanidino-substituted heterocyclic derivatives having histamine H-2 antagonist activity 失效
    胍类取代基杂环衍生物组蛋白-H-2拮抗剂Wirkung。

    公开(公告)号：EP0059597A2

    公开(公告)日：1982-09-08

    申请号：EP82300946.9

    申请日：1982-02-24

    申请人： IMPERIAL CHEMICAL INDUSTRIES PLC ,  ICI AMERICAS INC.

    发明人： Yellin, Tobias Oregon ,  Gilman, David John ,  Edwards, Philip Neil ,  Large, Michael Stewart ,  Jones, Derrick Fleet ,  Oldham, Keith

    IPC分类号： C07D239/42 ,  C07D239/46 ,  C07D251/16 ,  C07D277/48 ,  C07D249/04 ,  C07D417/12 ,  C07D405/12 ,  C07D401/12 ,  C07D403/12 ,  A61K31/425

    CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D249/04 ,  C07D251/16 ,  C07D277/48

    摘要： The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I:-
    in which R' and R 2 , same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R 1 and R 2 is halogen substituted, or R 2 is hydrogen and R 1 is R 5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO. SO 2 or NR 6 in which R 6 is H or 1-6C alkyl, R 5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R 5 and R 6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R 2 is H and R 1 is H, 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups: D is O or S; R 4 is H or 1-6C alkyl; R 3 is H or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

    摘要翻译： 本发明涉及作为组胺H-2拮抗剂并抑制胃酸分泌的羰基衍生物。 根据本发明，其中提供了式I的胍衍生物：其中R1和R2相同或不同，为氢或1-10C烷基，3-8C环烷基或4-14C环烷基烷基，每个烷基， 任选地携带一个或多个F，Cl或Br原子的环烷基或环烷基烷基，条件是R 1和R 2中的一个是卤素取代的，或者R 2是氢，R 1是其中W是任选被1或2取代的2-6C亚烷基的R 5-EW 1-4C烷基，E是O，S，SO，SO2或NR6，其中R6是H或1-6C烷基，R5是H或任选被1或2个1-4C烷基取代的1-6C烷基，或R5和R6 连接形成吡咯烷，哌啶，吗啉，哌嗪或N-甲基哌嗪环，或R 2为H，R 1为H，1-10C烷基，3-8C环烷基，4-14C环烷基烷基，3-6C烯基，3-6C 炔基，1-6C烷酰基，6-10C芳基，7-11C芳烷基或7-11C芳酰基; 环X是说明书中定义的杂环; A是亚苯基或5-7C亚环烷基，或其中任选插入一个或两个基团的1-8C亚烷基; D为O或S; R4是H或1-6C烷基; R3是H或本说明书中描述的各种基团及其药学上可接受的酸加成盐。 还描述了制造方法和药物组合物。

    Antisecretory branched-chain heterocyclic guanidine derivatives, processes for their manufacture, intermediates, and pharmaceutical compositions containing said derivatives
    6.
    发明公开
    Antisecretory branched-chain heterocyclic guanidine derivatives, processes for their manufacture, intermediates, and pharmaceutical compositions containing said derivatives 失效
    支链的具有抗分泌活性的含氮杂环胍衍生物，它们的制备方法，中间体和列出的衍生物的药物组合物。

    公开(公告)号：EP0010893A1

    公开(公告)日：1980-05-14

    申请号：EP79302211.2

    申请日：1979-10-15

    申请人： IMPERIAL CHEMICAL INDUSTRIES PLC ,  ICI AMERICAS INC.

    发明人： Yellin, Tobias Oregon ,  Gilman, David John ,  Jones, Derrick Fleet

    IPC分类号： C07D277/48 ,  A61K31/425

    CPC分类号： C07D209/48 ,  C07D277/14 ,  C07D277/48

    摘要： Heterocyclic guanidine derivatives of the formula:
    in which D is O, S or NH; E is CH or when D is O or S, E is N; Y is S, O, CH 2 , SO or a direct bond; P is a direct bond or C (1-4) unbranched alkylene optionally substituted by 1 or 2 C (1-4) alkyls and Q is C (1-4) unbranched alkylene optionally substituted by 1 or 2 C( 1 - 4 )alkyls, provided total number of alkyls in P and Q is 1 or 2, that when Y is S, 0 or SO, P is alkylene and that when Y is O or SO, Q is C (2-4) alkylene; R 1 is H or C (1-10) alkyl; A is 3,4-dioxocyclo- buten-1,2-diyl or C=Z where Z is S, O, NCN, NNO 2 , CHNO 2 , NCONH 2 , C(CN) 2 , NCOR 2 , NCO 2 R 2 , NSO 2 R 2 or NR 3 where R 3 is C (1-6) alkyl or C (6-12) aryl and R 3 is H or C (1-6) alkyl; B is C( 1 - 6 )alkoxy, C (1-6) alkylthio or NR 4 R 5 where R 4 and R 5 are H, C (1-10) alkyl, C (3-6) alkenyl, C (3-6) alkynyl, C( 2 - 6 )(primary,OH)alkyl, C (2-6) primary NH 2 )alkyl, C (3-6) cycloalkyl, or R 4 and R 5 together are a 5- or 6-membered saturated ring which may contain an additional O or NH: and the salts thereof. A process for the manufacture of said compounds is described; e.g. 2-guanidino-4-(5-amino-2-methylpentyl)-thiazole gives by reaction with dimethyl(cyanimido)dithio- carbonate and then methylamine 2-guanidino-4-[5-(2-cyano-3-methylguanidino)-2-methylpentyl]thiazole.

    摘要翻译： 式杂环胍衍生物：其中D是O，S或NH; E为CH或当D是O或S，E为N; Y是S，O，CH 2，SO或直接键; P为直接键或C（1-4）直链亚被1或2个C（1-4）烷基，且Q是C（1-4）直链亚被1或2个C任选取代的（1-4）任选被取代的 烷基，提供P中的烷基的总数，并且q是1或2，做当Y是S，O或SO，P是亚烷基并且做了当Y是O或SO，Q是C（2-4）亚烷基; [R <1>是H或C（1-10）烷基; A为3,4- dioxocyclobuten -1,2-二基或C = Z，其中Z为S，O，NCN，NNO2，CHNO 2，NCONH2，C（CN）2，NCOR <2>，NCO2R <2> NSO2R < 2>或NR <3>，其中R <3>是C（1-6）烷基或C（6-12）芳基并且R <3>是H或C（1-6）烷基; B是C（1-6）烷氧基，C（1-6）烷硫基或NR <4> - [R <5>，其中R <4>和R <5>为H，C（1-10）烷基，C（3 -6）链烯基C（3-6）炔基，C（2-6）（初级OH）烷基，C（2-6）（伯NH 2）烷基，C（3-6）环烷基，或R <4> 且R <5>一起是5-或6-元饱和环，该环可含有额外O或NH：和它们的盐。 一种用于所述化合物的制备方法进行说明; E.G. 2-胍基-4-（5-氨基-2-甲基戊基）-thiazoles通过与二甲基（cyanimido）二硫代碳酸酯反应，然后甲基胺2-胍基-4- [5-（2-氰基-3-甲基胍基）-2-甲基戊基给出， ]噻唑。

    Antisecretory heterocyclic guanidine derivatives, process for their manufacture and pharmaceutical compositions containing them
    7.
    发明公开
    Antisecretory heterocyclic guanidine derivatives, process for their manufacture and pharmaceutical compositions containing them 失效
    抗分泌有效杂环胍衍生物，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0010894A1

    公开(公告)日：1980-05-14

    申请号：EP79302212.0

    申请日：1979-10-15

    申请人： IMPERIAL CHEMICAL INDUSTRIES PLC ,  ICI AMERICAS INC.

    发明人： Yellin, Tobias Oregon ,  Jones, Derrick Fleet

    IPC分类号： C07D417/12 ,  A61K31/425

    CPC分类号： C07D417/12

    摘要： Heterocyclic antisecretory derivatives of the formula:
    where D is O, S or NH; E is CH or when D is O or S, E is N; Y is S, O, CH 2 , SO or a direct bond; m is O to 4 and n is 1 to 4, provided that when Y is S, O or SO m is 1 to 4, and when Y is O or SO, n is 2 to 4; A is a chain of 3 or 4 atoms comprising at least one C and also optionally S, N, 2N, or N and S, and also comprising C=O or C=S or where possible S0 2 and chain optionally substituted by 1 or 2 C (1-6) alkyl, benzyl, naphthylmethyl, 2-phenethyl, 4-phenylbutyl, pyridylmethyl, thiazolylmethyl, thienylmethyl, benzyloxy, pyridylmethoxy or phenoxymethyl radicals each optionally substituted on the aromatic ring system by 1 to 3 halogen atoms or methyl, methoxy, trifluoromethyl, dimethylamino, phenyl or phenoxy radicals; and the salts thereof. A process for the manufacture of said compounds is described; e.g. 2-guanidino-4[(2-aminomethyl)-thiomethyl]-thiazole gives by reaction with 5-(4-chlorobenzyl)-2-methyl- thiopyrimid-4-one 5-(4-chlorobenzyl)-2-[2-(2-guanidinothia- zol-4-ylmethylthio)ethylamino]pyrimid-4-one.

    摘要翻译： 式杂环抗分泌衍生物：... ...其中D是O，S或NH; E为CH或当D是O或S，E为N; Y是S，O，CH 2，SO或直接键; m是0〜4，n为1至4，条件没当Y是S，O或SO m是1至4，并且当Y是O或SO，n为2至4; A是3或4原子的含有至少一个C，因此，S，N，2N，或N和S，和因此包括C = O或C = S或在可能的情况SO2和链被1或2个任意性任选地取代的链 C（1-6）烷基，苄基，萘基甲基，2-苯乙基，4-苯基丁基，吡啶基甲基，噻唑基甲基，噻吩基甲基，苄氧基，吡啶基甲氧基或苯氧基甲基自由基各自任选的芳族环系上被1至3个卤素原子或甲基，甲氧基substituiertem 甲基，三氟甲基，二甲氨基，苯基或苯氧基自由基; 和它们的盐。 一种用于所述化合物的制备方法进行说明; E.G. 2-胍基-4-〔（2-氨基甲基）硫代甲基] -thiazoles通过用5-4氯苄反应得到）-2- methylthiopyrimid -4-酮5-（4-氯苄基）-2- [2-（2- 胍基 - 噻唑-4-基甲硫基）乙基氨基]嘧啶-4-酮。

    Guanidine derivatives
    8.
    发明公开
    Guanidine derivatives 失效
    胍的衍生物。

    公开(公告)号：EP0045155A1

    公开(公告)日：1982-02-03

    申请号：EP81303222.4

    申请日：1981-07-14

    申请人： IMPERIAL CHEMICAL INDUSTRIES PLC ,  ICI AMERICAS INC.

    发明人： Yellin, Tobias Oregon ,  Gilman, David John ,  Jones, Derrick Fleet ,  Oldham, Keith

    IPC分类号： C07D521/00 ,  C07D277/48 ,  C07D239/42 ,  A61K31/425

    CPC分类号： C07D239/42 ,  C07D277/48

    摘要： The invention relates to a guanidine derivative of the formula:
    in which W is a 2-6C alkylene chain optionally substituted by 1 or 21-4C alkyls; E is O, S, SO, S0 2 or NR 3 in which R 3 is H or 1-6C alkyl; R 1 is H or a straight chain 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls; or R 1 and R 3 are joined to form a morpholine, pyrrolidine, piperidine or piperazine; ring X, P, Y, Q and R 2 are as defined in the specification, and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing process, pharmaceutical compositions and intermediates are also described. The compounds of the formula I are histamine H-2 antagonists.

    Amidine derivatives
    9.
    发明公开
    Amidine derivatives 失效
    衍生销售。

    公开(公告)号：EP0067508A1

    公开(公告)日：1982-12-22

    申请号：EP82302092.0

    申请日：1982-04-23

    申请人： IMPERIAL CHEMICAL INDUSTRIES PLC

    发明人： Jones, Derrick Fleet ,  Oldham, Keith

    IPC分类号： A61K31/505 ,  C07D239/46 ,  C07D239/42 ,  C07D249/04 ,  C07D249/08 ,  C07D403/12

    CPC分类号： C07D239/42 ,  C07D239/47 ,  C07D249/04 ,  C07D249/08

    摘要： This invention relates to amidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I:-
    in which R' is hydrogen or a 1-10C alkyl, 3-8C cycloalkyl, 4.14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl radical, the latter three being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; and R 2 and R 3 are a variety of radicals described in the specification: and the pharmaceutically-acceptabie acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.