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    Histamine H2-antagonists
    1.
    发明授权
    Histamine H2-antagonists 失效
    组胺H2拮抗剂

    公开(公告)号：US4496571A

    公开(公告)日：1985-01-29

    申请号：US353422

    申请日：1982-03-01

    申请人： Tobias O. Yellin ,  David J. Gilman ,  Philip N. Edwards ,  Michael S. Large ,  Derrick F. Jones ,  Keith Oldham

    发明人： Tobias O. Yellin ,  David J. Gilman ,  Philip N. Edwards ,  Michael S. Large ,  Derrick F. Jones ,  Keith Oldham

    IPC分类号： C07D239/42 ,  C07D239/46 ,  C07D249/04 ,  C07D249/10 ,  C07D251/16 ,  C07D277/48 ,  C07D401/12

    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: ##STR1## in which R.sup.1 and R.sup.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.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.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.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.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.sup.4 is H or 1-6C alkyl; R.sup.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。

    Guanidino imidazoles and thiazoles
    2.
    发明授权
    Guanidino imidazoles and thiazoles 失效
    胍基咪唑和噻唑

    公开(公告)号：US4234735A

    公开(公告)日：1980-11-18

    申请号：US65801

    申请日：1979-08-13

    申请人： Derrick F. Jones ,  Tobias O. Yellin

    发明人： Derrick F. Jones ,  Tobias O. Yellin

    IPC分类号： A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61P1/04 ,  A61P43/00 ,  C07C277/08 ,  C07D209/48 ,  C07D233/88 ,  C07D277/20 ,  C07D277/38 ,  C07D277/42 ,  C07D277/48

    CPC分类号： C07D209/48 ,  C07D233/88 ,  C07D277/48

    摘要： The invention relates to guanidine derivatives of imidazoles and thiazoles which are histamine H-2 antagonists and which inhibit the secretion of gastric acid, to methods for their manufacture, to pharmaceutical compositions containing them and to methods of using such guanidine derivatives and compositions. The guanidine derivatives are of the general formula I: ##STR1## in which X is S or NH, Y is CH.sub.2, a direct bond or a vinylene radical, m is 0 to 4 and n is 1 to 4, R.sup.1 is hydrogen, halogen or alkyl, R.sup.2 is hydrogen, alkyl, alkanoyl or aroyl, A is a 3,4-dioxocyclobuten-1,2-diyl radical or C.dbd.Z in which Z is O, S, NCN, NNO.sub.2, CHNO.sub.2, NCONH.sub.2, C(CN).sub.2, NCOR.sup.3, NCO.sub.2 R.sup.3, NSO.sub.2 R.sup.3 or NR.sup.4 in which R.sup.3 is alkyl or aryl and R.sup.4 is hydrogen or alkyl, B is alkoxy or alkylthio or NR.sup.5 R.sup.6 in which R.sup.5 and R.sup.6 are independently hydrogen, alkyl, alkenyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, alkylaminoalkyl or dialkylaminoalkyl; and the salts thereof.

    摘要翻译： 本发明涉及作为组胺H-2拮抗剂的咪唑和噻唑的胍衍生物，其抑制胃酸的分泌，其制备方法，含有它们的药物组合物以及使用这种胍衍生物和组合物的方法。 胍衍生物具有通式I：其中X为S或NH，Y为CH 2，直接键或亚乙烯基，m为0至4，n为1至4，R 1为氢， 卤素或烷基，R 2是氢，烷基，烷酰基或芳酰基，A是3,4-二氧杂环丁烯-1,2-二基或C = Z，其中Z是O，S，NCN，NNO 2，CHNO 2，NCONH 2，C （CN）2，NCOR3，NCO2R3，NSO2R3或NR4，其中R3是烷基或芳基，R4是氢或烷基，B是烷氧基或烷硫基或NR5R6，其中R5和R6独立地是氢，烷基，烯基，环烷基，羟基烷基， 烷氧基烷基，烷基氨基烷基或二烷基氨基烷基; 及其盐。

    Amidine derivatives
    3.
    发明授权
    Amidine derivatives 失效
    脒衍生物

    公开(公告)号：US4748165A

    公开(公告)日：1988-05-31

    申请号：US377137

    申请日：1982-05-11

    申请人： Derrick F. Jones ,  Keith Oldham

    发明人： Derrick F. Jones ,  Keith Oldham

    IPC分类号： A61K31/41 ,  A61K31/505 ,  A61P1/04 ,  A61P43/00 ,  C07D239/42 ,  C07D239/46 ,  C07D239/47 ,  C07D249/04 ,  C07D249/08 ,  C07D249/14 ,  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: ##STR1## in which R.sup.1 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.sup.2 and R.sup.3 are 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： 本发明涉及组胺H-2拮抗剂的脒衍生物，其抑制胃酸分泌。 根据本发明，提供了式I的胍衍生物：其中R 1是氢或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，后三个任选被取代; 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1-8C亚烷基链，其中任选地插入一个或两个基团; 并且R 2和R 3是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。

    Nitrogen heterocycles
    5.
    发明授权
    Nitrogen heterocycles 失效
    氮杂环

    公开(公告)号：US4460584A

    公开(公告)日：1984-07-17

    申请号：US356503

    申请日：1982-03-09

    申请人： Derrick F. Jones ,  Keith Oldham

    发明人： Derrick F. Jones ,  Keith Oldham

    IPC分类号： C07D239/47 ,  A61K31/505 ,  A61P1/04 ,  A61P43/00 ,  C07D239/46 ,  C07D249/12 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D521/00 ,  A61K31/44

    CPC分类号： C07D239/47 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D249/12

    摘要： The invention relates to nitrogen heterocycles 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: ##STR1## in which R.sup.1 and R.sup.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.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.3 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.4 in which R.sup.4 is H or 1-6C alkyl, R.sup.3 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.3 R.sup.4 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.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; ring Y is a heterocyclic ring 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氮杂环。 根据本发明，提供了式I的胍衍生物：其中R 1和R 2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R 3-EW，其中W是任选被1或2取代的2-6C亚烷基 1-4C烷基，E是O，S，SO，SO2或NR4，其中R4是H或1-6C烷基，R3是H或任选被1或2个1-4C烷基取代的1-6C烷基，或R3R4是 连接形成吡咯烷，哌啶，吗啉，哌嗪或N-甲基哌嗪环，或者R2是H，R1是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; 环Y是说明书中描述的杂环：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。

    Heterocyclic derivatives
    7.
    发明授权
    Heterocyclic derivatives 失效
    杂环衍生物

    公开(公告)号：US4795755A

    公开(公告)日：1989-01-03

    申请号：US353384

    申请日：1982-03-01

    申请人： Derrick F. Jones ,  Keith Oldham

    发明人： Derrick F. Jones ,  Keith Oldham

    IPC分类号： C07D213/73 ,  C07D213/75 ,  C07D231/16 ,  C07D231/40 ,  C07D239/42 ,  C07D239/46 ,  C07D239/54 ,  C07D239/545 ,  C07D249/04 ,  C07D249/08 ,  C07D249/14 ,  C07D257/06 ,  A61K31/495 ,  C07D403/04

    CPC分类号： C07D213/73 ,  C07D213/75 ,  C07D231/16 ,  C07D231/40 ,  C07D239/42 ,  C07D239/47 ,  C07D239/545 ,  C07D249/04 ,  C07D249/08 ,  C07D249/14 ,  C07D257/06

    摘要： This invention relates to heterocyclic 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: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen-substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W- in which W is 2-6 alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O,S,SO,SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring; 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; and R.sup.3 and R.sup.4 are 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： 本发明涉及组胺H-2拮抗剂并抑制胃酸分泌的杂环衍生物。 根据本发明，提供了式I的胍衍生物：其中R 1和R 2相同或不同，为氢或1-10C烷基，3-8C环烷基，4-14C环烷基烷基，各烷基， 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R 5 -WW-，其中W是2-6个亚烷基， 或2 1-4C烷基，E是其中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烷基的O，S，SO，SO2或NR6，或R5 R 6连接形成吡咯烷，哌啶，吗啉，哌嗪或N-甲基哌嗪环; 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; R3和R4是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 guanidine derivatives and pharmaceutical compositions containing them
    9.
    发明授权
    Antisecretory guanidine derivatives and pharmaceutical compositions containing them 失效
    反分子胍衍生物和含有它们的药物组合物

    公开(公告)号：US4315009A

    公开(公告)日：1982-02-09

    申请号：US4531

    申请日：1979-01-18

    申请人： Derrick F. Jones ,  Keith Oldham

    发明人： Derrick F. Jones ,  Keith Oldham

    IPC分类号： C07D277/20 ,  A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61K31/535 ,  A61K31/5377 ,  A61P1/04 ,  C07C335/28 ,  C07D263/48 ,  C07D271/06 ,  C07D271/07 ,  C07D277/48 ,  C07D285/08 ,  C07D417/10 ,  C07D417/12

    CPC分类号： C07D271/07 ,  C07C335/28 ,  C07D263/48 ,  C07D277/48 ,  C07D285/08

    摘要： The guanidine derivative has the formula: ##STR1## where X is O or S: Y is N, CH or CCH.sub.3 : m is 0 or 1: R.sup.1 is hydrogen and R.sup.2 cyano, trifluoroacetyl, C.sub.1-6 alkanoyl, 4,5-dihydro-4-oxothiazol-2-yl or A-B where A is 3,4-dioxocyclobutene-1,2-diyl or C.dbd.Z where Z is oxygen, sulphur, NCN, NNO.sub.2, CHNO.sub.2, NCONH.sub.2, C(CN).sub.2, NCOR.sup.6, NCO.sub.2 R.sup.6, NSO.sub.2 R.sup.6 or NR.sup.7 where R.sup.6 is C.sub.1-6 alkyl and R.sup.7 is hydrogen or C.sub.1-6 alkyl and B is C.sub.1-6 alkyl, alkoxy or alkylthio or NR.sup.8 R.sup.9 where R.sup.8 and R.sup.9 are hydrogen, C.sub.1-10 alkyl, C.sub.3-10 -alkenyl, alkynyl or alkoxyalkyl, C.sub.2-6 (primary hydroxy)alkyl, or, when R.sup.9 is hydrogen, R.sup.8 is 2-[[5-dimethylaminomethylfuran-2-yl]methylthio]-ethylamino or R.sup.8 and R.sup.9 are together a 5- or 6-membered non-aromatic ring optionally containing an additional N or O; or R.sup.1 and R.sup.2 are together imidazolidin-2-ylidene: R.sup.3 is hydrogen or fluorine: R.sup.4 is halogen or methyl: R.sup.5 is hydrogen, C.sub.1-6 alkyl or C.sub.3-10 alkoxyalkyl: and the salts thereof.

    摘要翻译： 胍衍生物具有下式：其中X是O或S：Y是N，CH或CCH 3：m是0或1：R 1是氢，R 2是氰基，三氟乙酰基，C 1-6烷酰基， 二氢-4-氧代噻唑-2-基或AB，其中A是3,4-二氧环戊烯-1,2-二基或C = Z，其中Z是氧，硫，NCN，NNO 2，CHNO 2，NCONH 2，C（CN）2， NCOR6，NCO2R6，NSO2R6或NR7，其中R6是C1-6烷基，R7是氢或C1-6烷基，B是C1-6烷基，烷氧基或烷硫基或NR8R9，其中R8和R9是氢，C1-10烷基，C3-10-烯基， 炔基或烷氧基烷基，C2-6（伯羟基）烷基，或当R9为氢时，R8为2 - [[5-二甲氨基甲基呋喃-2-基]甲硫基] - 乙氨基或R8和R9一起为5-或6- 任选地含有另外的N或O的非芳族环; 或R 1和R 2一起是咪唑烷-2-亚基：R 3是氢或氟：R 4是卤素或甲基：R 5是氢，C 1-6烷基或C 3-10烷氧基烷基：及其盐。

    Guanidino imidazoles and thiazoles
    10.
    发明授权
    Guanidino imidazoles and thiazoles 失效
    胍基咪唑和噻唑

    公开(公告)号：US4165377A

    公开(公告)日：1979-08-21

    申请号：US897910

    申请日：1978-04-19

    申请人： Derrick F. Jones ,  Tobias O. Yellin

    发明人： Derrick F. Jones ,  Tobias O. Yellin

    IPC分类号： A61K31/415 ,  A61K31/425 ,  A61K31/426 ,  A61P1/04 ,  A61P43/00 ,  C07C277/08 ,  C07D209/48 ,  C07D233/88 ,  C07D277/20 ,  C07D277/38 ,  C07D277/42 ,  C07D277/48

    CPC分类号： C07D209/48 ,  C07D233/88 ,  C07D277/48

    摘要： The invention relates to guanidine derivatives of imidazoles and thiazoles which are histamine H-2 antagonists and which inhibit the secretion of gastric acid, to methods for their manufacture, to pharmaceutical compositions containing them and to methods of using such guanidine derivatives and compositions. The guanidine derivatives are of the general formula I: ##STR1## in which X is S or NH, Y is CH.sub.2, a direct bond or a vinylene radical, m is 0 to 4 and n is 1 to 4, R.sup.1 is hydrogen, halogen or alkyl, R.sup.2 is hydrogen, alkyl, alkanoyl or aroyl, A is a 3,4-dioxocyclobuten-1,2-diyl radical or C.dbd.Z in which Z is O, S, NCN, NNO.sub.2, CHNO.sub.2, NCONH.sub.2, C(CN).sub.2, NCOR.sup.3, NCO.sub.2 R.sup.3, NSO.sub.2 R.sup.3 or NR.sup.4 in which R.sup.3 is alkyl or aryl and R.sup.4 is hydrogen or alkyl, B is alkoxy or alkylthio or NR.sup.5 R.sup.6 in which R.sup.5 and R.sup.6 are independently hydrogen, alkyl, alkenyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, alkylaminoalkyl or dialkylaminoalkyl; and the salts thereof.

    摘要翻译： 本发明涉及作为组胺H-2拮抗剂的咪唑和噻唑的胍衍生物，其抑制胃酸的分泌，其制备方法，含有它们的药物组合物以及使用这种胍衍生物和组合物的方法。 胍衍生物具有通式I：其中X为S或NH，Y为CH 2，直接键或亚乙烯基，m为0至4，n为1至4，R 1为氢， 卤素或烷基，R 2是氢，烷基，烷酰基或芳酰基，A是3,4-二氧杂环丁烯-1,2-二基或C = Z，其中Z是O，S，NCN，NNO 2，CHNO 2，NCONH 2，C （CN）2，NCOR3，NCO2R3，NSO2R3或NR4，其中R3是烷基或芳基，R4是氢或烷基，B是烷氧基或烷硫基或NR5R6，其中R5和R6独立地是氢，烷基，烯基，环烷基，羟基烷基， 烷氧基烷基，烷基氨基烷基或二烷基氨基烷基; 及其盐。