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公开(公告)号：US4546187A
公开(公告)日：1985-10-08
申请号：US507203
申请日：1983-06-23
申请人： Roger Crossley , Kay H. Dickinson
发明人： Roger Crossley , Kay H. Dickinson
IPC分类号： C07D213/70 , C07D233/84 , C07D401/12
CPC分类号： C07D213/70 , C07D233/84 , Y10S514/926 , Y10S514/927
摘要： The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinium radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, e.g. where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.
摘要翻译： 本发明涉及式I XASY（I）的新化合物，其中X是选自咪唑基，吡啶基，喹啉基，四氢吡啶基或哌啶基中的任何一个可以被取代，Y是任何上述基团或吡啶鎓基，A是亚烷基 1-6个碳原子。 大多数化合物是抗溃疡剂，但有些具有抗高血压活性，例如， 其中X是喹啉基。 还描述了治疗溃疡和抗溃疡组合物的方法。
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2.发明授权
公开(公告)号：US4440773A
公开(公告)日：1984-04-03
申请号：US350442
申请日：1982-02-19
申请人： Roger Crossley , Kay H. Dickinson
发明人： Roger Crossley , Kay H. Dickinson
IPC分类号： C07D213/70 , C07D233/84 , C07D213/32 , A61K31/44
CPC分类号： C07D213/70 , C07D233/84 , Y10S514/926 , Y10S514/927
摘要： The invention provides a compound of the formula I ##STR1## wherein Y is a heterocyclic radical of formula ##STR2## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, hydroxy, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, loweralkoxy, halogen, formyl, phenyl, phenylalkyl, halophenyl, or acetal [CH(OR.sup.4).sub.2 where R.sup.4 is lower alkyl or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, the dotted lines in formula V represent an optional double bond in one of the indicated positions, A is a saturated or unsaturated alkylene radical having from 1 to 6 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and R.sup.3 is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms and Z.sup.- is an anion, and acid addition salts thereof, with the provisos that (1) when more than one R.sup.1 radical is present in the molecule then the R.sup.1 radicals may be the same or different and (2) A is linked to the 2 or 3 position of the pyridine ring.The compounds are useful as anti-ulcer or anti-secretory agents. Methods of treating ulcers and anti-ulcer compositions are described.
摘要翻译： 本发明提供了式I化合物，其中Y是式IMA的杂环基，其中R是氢或低级烷基，R 1是氢，羟基，低级烷基，羟基低级烷基，低级烷氧基低级烷基，低级烷氧基，卤素，甲酰基 ，苯基，苯基烷基，卤代苯基或缩醛[CH（OR 4）2，其中R 4是低级烷基或两个R 4基团连接形成低级亚烷基链]，m为1或2，式V中的虚线表示任选的双 在一个指定位置键合，A是具有1至6个碳原子的饱和或不饱和亚烷基，其可以被1至6个碳原子的低级烷基取代，S是硫，R3是低级烷基，苯基或芳烷基 7至12个碳原子，Z-为阴离子，及其酸加成盐，条件是（1）当分子中存在多于一个R 1基团时，则R 1基团可以相同或不同，并且（2 ）A与吡啶环的2或3位相连。 该化合物可用作抗溃疡或抗分泌剂。 描述了治疗溃疡和抗溃疡组合物的方法。
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公开(公告)号：US4350703A
公开(公告)日：1982-09-21
申请号：US222282
申请日：1981-01-05
IPC分类号： C07D205/08 , C07D205/12 , C07D477/08 , C07F9/535 , C07F9/54 , C07F9/568 , C07F9/6561 , C07D487/04 , A61K37/40
CPC分类号： C07F9/5352 , C07D205/08 , C07D205/12 , C07D477/08 , C07F9/5442 , C07F9/5683 , C07F9/65613
摘要： Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.
摘要翻译： 化合物描述为式（II）：其中R 1是使CO 2 R 1是酯基的基团; A1是氢原子; A2为基团CR2R3R4，其中R2为氢原子或羟基; R3是氢原子或低级烷基; R4为氢原子或低级烷基，苄基，苯基或与R3结合形成C5-7羧酸环的一部分，或为式CH（OH）R5或CHX的基团，其中R5 是氢原子或低级烷基，X是氧原子或其中R6是氢原子或低级烷基，苯基，CN，CO2R8的CR6R7基团，其中R8是低级烷基，苯基或苄基，R7是氢 原子或低级烷基，或者连接到R6以形成C5-7碳环的一部分。 已经发现这些化合物具有抗菌性质。 描述了这些化合物的制备。
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公开(公告)号：US4431587A
公开(公告)日：1984-02-14
申请号：US330656
申请日：1981-12-14
IPC分类号： C07D205/08 , C07D205/12 , C07D477/08 , C07F9/535 , C07F9/54 , C07F9/568 , C07F9/6561 , C07D487/04 , A61K31/40 , C07D403/12
CPC分类号： C07F9/5352 , C07D205/08 , C07D205/12 , C07D477/08 , C07F9/5442 , C07F9/5683 , C07F9/65613
摘要： Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.
摘要翻译： 化合物描述为式（II）：其中R 1是使CO 2 R 1是酯基的基团; A1是氢原子; A2为基团CR2R3R4，其中R2为氢原子或羟基; R3是氢原子或低级烷基; R4为氢原子或低级烷基，苄基，苯基或与R3结合形成C5-7羧酸环的一部分，或为式CH（OH）R5或CHX的基团，其中R5 是氢原子或低级烷基，X是氧原子或其中R6是氢原子或低级烷基，苯基，CN，CO2R8的CR6R7基团，其中R8是低级烷基，苯基或苄基，R7是氢 原子或低级烷基，或者连接到R6以形成C5-7碳环的一部分。 已经发现这些化合物具有抗菌性质。 描述了这些化合物的制备。
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公开(公告)号：US4415582A
公开(公告)日：1983-11-15
申请号：US351837
申请日：1982-02-24
申请人： Roger Crossley , Kay H. Dickinson
发明人： Roger Crossley , Kay H. Dickinson
IPC分类号： C07D213/70 , C07D233/84 , A61K31/445
CPC分类号： C07D213/70 , C07D233/84 , Y10S514/926 , Y10S514/927
摘要： The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinium radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, e.g. where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.
摘要翻译： 本发明涉及式I XASY（I）的新化合物，其中X是选自咪唑基，吡啶基，喹啉基，四氢吡啶基或哌啶基中的任何一个可以被取代，Y是任何上述基团或吡啶鎓基，A是亚烷基 1-6个碳原子。 大多数化合物是抗溃疡剂，但有些具有抗高血压活性，例如， 其中X是喹啉基。 还描述了治疗溃疡和抗溃疡组合物的方法。
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公开(公告)号：US4419362A
公开(公告)日：1983-12-06
申请号：US351836
申请日：1982-02-24
申请人： Roger Crossley , Kay H. Dickinson
发明人： Roger Crossley , Kay H. Dickinson
IPC分类号： C07D213/70 , C07D233/84 , A61K31/415 , C07D403/12
CPC分类号： C07D213/70 , C07D233/84 , Y10S514/926 , Y10S514/927
摘要： The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinum radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, e.g. where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.
摘要翻译： 本发明涉及式I XASY（I）的新化合物，其中X是选自咪唑基，吡啶基，喹啉基，四氢吡啶基或哌啶基的基团，其中任何一个可以被取代，Y是上述基团中的任何一个或吡啶基，A是亚烷基 1-6个碳原子。 大多数化合物是抗溃疡剂，但有些具有抗高血压活性，例如， 其中X是喹啉基。 还描述了治疗溃疡和抗溃疡组合物的方法。
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公开(公告)号：US4343805A
公开(公告)日：1982-08-10
申请号：US217925
申请日：1980-12-18
申请人： Roger Crossley , Kay H. Dickinson
发明人： Roger Crossley , Kay H. Dickinson
IPC分类号： C07D213/70 , C07D233/84 , C07D401/12 , A61K31/435
CPC分类号： C07D213/70 , C07D233/84 , Y10S514/926 , Y10S514/927
摘要： The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinium radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, eg where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.
摘要翻译： 本发明涉及式I XASY（I）的新化合物，其中X是选自咪唑基，吡啶基，喹啉基，四氢吡啶基或哌啶基中的任何一个可以被取代，Y是任何上述基团或吡啶鎓基，A是亚烷基 1-6个碳原子。 大多数化合物是抗溃疡剂，但有些具有抗高血压活性，例如其中X是喹啉基。 还描述了治疗溃疡和抗溃疡组合物的方法。
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公开(公告)号：US4576955A
公开(公告)日：1986-03-18
申请号：US541921
申请日：1983-10-13
申请人： Roger Crossley , Kay H. Dickinson
发明人： Roger Crossley , Kay H. Dickinson
IPC分类号： C07D213/70 , C07D233/84 , C07D401/12 , A61K31/44
CPC分类号： C07D213/70 , C07D233/84 , Y10S514/926 , Y10S514/927
摘要： The invention provides a compound of the formula I ##STR1## wherein Y is a heterocyclic radical of formula ##STR2## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, hydroxy, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, loweralkoxy, halogen, formyl, phenyl, phenylalkyl, halophenyl, or acetal [CH(OR.sup.4).sub.2 where R.sup.4 is lower alkyl or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, the dotted lines in formula V represent an optional double bond in one of the indicated positions, A is a saturated or unsaturated alkylene radical having from 1 to 6 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and R.sup.3 is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms and Z.sup.- is an anion, and acid addition salts thereof, with the provisos that (1) when more than one R.sup.1 radical is present in the molecule then the R.sup.1 radicals may be the same or different and (2) A is linked to the 2 or 3 position of the pyridine ring.The compounds are useful as anti-ulcer or anti-secretory agents. Methods of treating ulcers and anti-ulcer compositions are described.
摘要翻译： （VII）其中R是氢或低级烷基，R 1是氢的式（I）的化合物，其中Y是式 ，羟基，低级烷基，羟基低级烷基，低级烷氧基低级烷基，低级烷氧基，卤素，甲酰基，苯基，苯基烷基，卤代苯基或缩醛[CH（OR 4）2，其中R 4是低级烷基或两个R 4基团连接形成低级亚烷基链] 是1或2，式V中的虚线表示在指定位置之一中任选的双键，A是具有1至6个碳原子的饱和或不饱和亚烷基，其可以被1至6的低级烷基取代 碳原子，S是硫，R3是7-12个碳原子的低级烷基，苯基或芳烷基，Z-是阴离子，其酸加成盐，条件是（1）当多于一个R 1基团存在于 该分子然后R1基团可以相同或不同，并且（2）A与2或3位相连 n的吡啶环。 该化合物可用作抗溃疡或抗分泌剂。 描述了治疗溃疡和抗溃疡组合物的方法。
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公开(公告)号：US4405637A
公开(公告)日：1983-09-20
申请号：US306535
申请日：1981-09-28
IPC分类号： C07D205/08 , C07D205/12 , C07D477/08 , C07F9/535 , C07F9/54 , C07F9/568 , C07F9/6561 , C07D487/04 , A61K31/40
CPC分类号： C07F9/5352 , C07D205/08 , C07D205/12 , C07D477/08 , C07F9/5442 , C07F9/5683 , C07F9/65613
摘要： Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.
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