公开(公告)号：US4590192A

公开(公告)日：1986-05-20

申请号：US537048

申请日：1983-09-29

申请人： Charles S. Fake ,  Gordon Burrell

发明人： Charles S. Fake ,  Gordon Burrell

IPC分类号： C07D275/04 ,  C07D275/06 ,  C07D285/24 ,  C07D285/32 ,  C07D417/12 ,  A61K31/38

CPC分类号： C07D275/04 ,  C07D275/06 ,  C07D285/24 ,  C07D285/32 ,  C07D417/12

摘要： Compounds of formula (I), or a pharmaceutically acceptable salt, quaternized derivative, N-oxide or solvate thereof:R.sub.1 --Ar--(CH.sub.2).sub.a --X--(CH.sub.2).sub.b --NH--Het (I)wherein: the substituents are defined in the specification.The compounds are useful in treating excess gastric acid secretions such as peptic ulcers.

摘要翻译： 式（I）化合物或其药学上可接受的盐，季铵化衍生物，N-氧化物或其溶剂合物：R1-Ar-（CH2）aX-（CH2）b-NH-Het（I）其中：取代基定义在 规格。 该化合物可用于治疗过量的胃酸分泌物如消化性溃疡。

公开(公告)号：US4363811A

公开(公告)日：1982-12-14

申请号：US186708

申请日：1980-09-12

申请人： John M. Evans ,  Graham A. Showell ,  Charles S. Fake

发明人： John M. Evans ,  Graham A. Showell ,  Charles S. Fake

IPC分类号： C07D311/22 ,  C07D311/68 ,  C07D493/04 ,  A61K31/445 ,  C07D405/04

CPC分类号： C07D493/04 ,  C07D311/22 ,  C07D311/68

摘要： Compounds of the formula (I): ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a hydrogen atom or a lower alkyl group;R.sub.3 is a hydrogen atom or a lower alkyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a lower alkyl or a substituted alkyl group;or R.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is an electron donating group;R.sub.7 is an electron withdrawing group; andthe NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans having antihypertensive activity, pharmaceutical compositions containing them and processes for their preparation.

摘要翻译： 式（I）化合物：其中R 1为氢原子或低级烷基; R2是氢原子或低级烷基; R3是氢原子或低级烷基; R4是氢原子或烷基; R5是低级烷基或取代的烷基; 或R 4和R 5连接，使得它们与它们所连接的氮原子一起形成任选含有氧或硫原子的5-，6-或7-元环; R6是给电子基团; R7是吸电子基团; 并且NR4R5和OR3部分是具有抗高血压活性的反式，含有它们的药物组合物及其制备方法。

公开(公告)号：US4366163A

公开(公告)日：1982-12-28

申请号：US186709

申请日：1980-09-12

申请人： John M. Evans ,  Graham A. Showell ,  Charles S. Fake

发明人： John M. Evans ,  Graham A. Showell ,  Charles S. Fake

IPC分类号： C07D311/22 ,  C07D311/58 ,  C07D311/68 ,  C07D311/70 ,  A61K31/445 ,  C07D405/04

CPC分类号： C07D311/70 ,  C07D311/22 ,  C07D311/58 ,  C07D311/68

摘要： Compounds of the formula (I) ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a hydrogen atom or a lower alkyl group;R.sub.3 is a hydrogen atom or a lower alkyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a lower alkyl or a substituted alkyl group;or R.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is an electron donating group;R.sub.7 is an electron withdrawing group; andthe NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans having compositions containing them and processes for their preparation.

摘要翻译： 式（I）化合物及其盐及其前药，其中：R1为氢原子或低级烷基; R2是氢原子或低级烷基; R3是氢原子或低级烷基; R4是氢原子或烷基; R5是低级烷基或取代的烷基; 或R 4和R 5连接，使得它们与它们所连接的氮原子一起形成任选含有氧或硫原子的5-，6-或7-元环; R6是给电子基团; R7是吸电子基团; 并且NR4R5和OR3部分是反式含有它们的组合物及其制备方法。

公开(公告)号：US4224331A

公开(公告)日：1980-09-23

申请号：US570015

申请日：1975-04-21

申请人： Charles S. Fake

发明人： Charles S. Fake

IPC分类号： C07D213/75 ,  A61K31/44

CPC分类号： C07D213/75

摘要： Orally administrable pharmaceutical compositions for reducing the rate of gastric acid secretion and acid addition salts thereof containing an effective amount of halo-substituted 2-pyridyl thioureas and a pharmaceutical carrier and a method of treating gastric ulcers and reducing gastric acid secretion with such compositions.

摘要翻译： 用于降低胃酸分泌速率的口服给药药物组合物及其含有有效量的卤代-2-吡啶基硫脲和其药物载体的酸加成盐，以及用这些组合物治疗胃溃疡并减少胃酸分泌的方法。

公开(公告)号：US4320128A

公开(公告)日：1982-03-16

申请号：US131236

申请日：1980-03-17

申请人： Charles S. Fake

发明人： Charles S. Fake

IPC分类号： C07D311/22 ,  A61K31/44 ,  C07D405/12 ,  C07D405/14

CPC分类号： C07D311/22

摘要： Compounds of the formula (II): ##STR1## and pharmaceutically acceptable acid-addition salts thereof wherein Ar is a pyridyl or optionally substituted phenyl group of the sub-formula --C.sub.6 H.sub.3 R.sub.1 R.sub.2 wherein R.sub.1 is a hydrogen, fluorine, chlorine or bromine atom or a lower alkyl, lower alkoxyl, lower acyl, lower acyloxyl or lower alkoxycarbonyl group; and R.sub.2 is a hydrogen, fluorine or chlorine atom or a lower alkyl or lower alkoxy group having useful anti-hypertension activity, their preparation, and pharmaceutical compositions containing them.

摘要翻译： 式（II）化合物：其中Ar是吡啶基或任意取代的亚式-C 6 H 3 R 1 R 2的苯基，其中R 1是氢，氟，氯或溴 低级烷基，低级烷氧基，低级酰基，低级酰氧基或低级烷氧基羰基; R2为氢，氟或氯原子或具有有效抗高血压活性的低级烷基或低级烷氧基，其制备方法和含有它们的药物组合物。