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11. 发明授权

US4234735A Guanidino imidazoles and thiazoles 失效
标题翻译：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。

12. 发明授权

US4165377A Guanidino imidazoles and thiazoles 失效
标题翻译：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。

13. 发明授权

US4374836A Antisecretory heterocyclic derivatives, process for their manufacture and pharmaceutical compositions containing them 失效
标题翻译：抗菌杂环衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4374836A
公开(公告)日：1983-02-22
申请号：US83479
申请日：1979-10-10
申请人： Tobias O. Yellin , Derrick F. Jones
发明人： Tobias O. Yellin , Derrick F. Jones
IPC分类号： C07D417/12 , A61K31/425 , A61K31/505 , A61P1/00 , A61P1/04 , C07D213/58 , C07D239/47 , C07D253/06 , C07D277/48 , C07D417/00 , C07D417/14
CPC分类号： C07D417/12
摘要： The invention relates to a heterocyclic derivative of the formula: ##STR1## 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.sub.2, SO or a direct bond; m is 0 to 4 and n is 1 to 4, provided that when Y is S, O or SO m is 1 to 4, when Y is O or SO, n is 2 to 4; A is C.sub.(3-4) chain comprising at least one C and also optionally S, N, 2N or N and S, and also comprising C.dbd.O or C.dbd.S or where possible SO.sub.2, the chain optionally substituted by 1 or 2 C.sub.(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.
摘要翻译：本发明涉及下式的杂环衍生物：其中D是O，S或NH; E为CH或当D为O或S时，E为N; Y是S，O，CH2，SO或直接键; m为0〜4，n为1〜4，条件是当Y为S时，O或SO m为1〜4，当Y为O或SO时，n为2〜4; A是包含至少一个C并且还任选地S，N，2N或N和S，且还包含C = O或C = S的C（3-4）链，或者在可能的情况下，SO 2，任选被1或2取代的链每个任选在芳环体系上被1至3个卤素原子取代的甲基，甲氧基，苯基，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，，三氟甲基，二甲基氨基，苯基或苯氧基; 及其盐。

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