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1. 发明授权

US4562261A 2-Guanidinothiazoline compounds, and process for preparing them 失效
标题翻译： 2-胍基噻唑啉化合物及其制备方法
公开(公告)号：US4562261A
公开(公告)日：1985-12-31
申请号：US597234
申请日：1984-04-05
申请人： Yasufumi Hirata , Isao Yanagisawa
发明人： Yasufumi Hirata , Isao Yanagisawa
IPC分类号： C07D277/10 , C07D277/18 , C07D277/20 , C07D277/46 , C07D277/48
CPC分类号： C07D277/18 , C07D277/48
摘要： Novel 2-guanidinothiazoline compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, and the acid addition salts thereof; they are important intermediate compounds for preparing famotidine and thiotidine which are medicaments useful as gastric acid secretion inhibitors.
摘要翻译：其中R代表氢原子或低级烷基，X代表卤素原子及其酸加成盐的通式为“IMAGE”的新型2-胍基噻唑啉化合物，它们是制备作为胃酸分泌抑制剂的药物的法莫替丁和硫代替丁的重要中间体化合物。

2. 发明授权

US4379158A Antisecretory imidazole amidine compounds, composition and method of use 失效
标题翻译：咪唑咪唑类化合物，组成及使用方法
公开(公告)号：US4379158A
公开(公告)日：1983-04-05
申请号：US193742
申请日：1980-10-03
申请人： Yasufumi Hirata , Isao Yanagisawa , Toshinari Tamura , Masaaki Takeda
发明人： Yasufumi Hirata , Isao Yanagisawa , Toshinari Tamura , Masaaki Takeda
IPC分类号： C07D213/32 , C07D213/68 , C07D213/86 , C07D233/54 , C07D233/64 , C07D277/26 , C07D277/30 , C07D307/52 , A61K31/615 , C07D401/12
CPC分类号： C07D213/86 , C07D213/32 , C07D213/68 , C07D233/64 , C07D277/26 , C07D307/52
摘要： Novel heterocyclic compounds shown by the formula ##STR1## wherein Het represents a 5-membered or 6-membered heterocyclic group which may have substituent(s); Z represents a sulfur atom or oxygen atom; X represents an oxygen atom or the unsubstituted or substituted imino group shown by N--R.sub.1 (wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a cyano group, an unsubstituted or alkyl substituted carbamoyl group, an unsubstituted or lower alkyl substituted thiocarbamoyl group, or a lower alkanoylamino group); Y represents a hydrogen atom, a lower alkyl group which may have substituent(s), a cycloalkyl group of 3-6 carbon atoms, a lower alkenyl group, a lower alkynyl group, an aryl group which may have substituent(s), an aralkyl group which may have substituent(s), a hydroxyl group, a cyano group, a carbamoyl group, an amidino group, an alkanoyl group which may have been substituted by halogen atom(s), an alkanoylamino group, an arylcarbonylamino group, an alkylamino group, an arylamino group, an arylsulfamoyl group, a lower alkoxycarbamoyl group, or an oxamoylamino group; and m and n represent an integer of 1-3; when X is N--R.sub.1, said X and Y may combine with each other to form a 5-membered or 6-membered heterocyclic ring containing 2-3 nitrogen atoms which may have substituent(s), and the pharmacologically acceptable acid addition salts thereof.The compounds of this invention are useful as gastric acid secretion inhibitors.
摘要翻译：式中，Het表示可具有取代基的5元或6元杂环基的新型杂环化合物。 Z表示硫原子或氧原子; X表示氧原子或由N-R 1表示的未取代或取代的亚氨基（其中R 1为氢原子，低级烷基，氰基，未取代或烷基取代的氨基甲酰基，未取代或低级烷基取代的硫代氨基甲酰基，或低级烷酰氨基）; Y表示氢原子，可具有取代基的低级烷基，3-6个碳原子的环烷基，低级烯基，低级炔基，可具有取代基的芳基，可以具有取代基的芳烷基，羟基，氰基，氨基甲酰基，脒基，可被卤素原子取代的烷酰基，烷酰基氨基，芳基羰基氨基，烷基氨基，芳基氨基，芳基氨磺酰基，低级烷氧基氨基甲酰基或氨甲酰基氨基; m和n表示1-3的整数; 当X是N-R1时，所述X和Y可以彼此结合形成含有2-3个可具有取代基的氮原子的5元或6元杂环，其药理学上可接受的酸加成盐。本发明的化合物可用作胃酸分泌抑制剂。

3. 发明授权

US4197243A N-1-Benzyl-3-pyrrolidinyl-4-dimethylamino benzamide derivatives 失效
标题翻译： N-1-苄基-3-吡咯烷基-4-二甲基氨基苯甲酰胺衍生物
公开(公告)号：US4197243A
公开(公告)日：1980-04-08
申请号：US906079
申请日：1978-05-15
申请人： Masuo Murakami , Kozo Takahashi , Yasufumi Hirata , Mutsuo Takashima , Sumio Iwanami , Osamu Hasegawa , Yoshihisa Nozaki , Shiro Tachikawa , Masaaki Takeda , Shinji Usuda
发明人： Masuo Murakami , Kozo Takahashi , Yasufumi Hirata , Mutsuo Takashima , Sumio Iwanami , Osamu Hasegawa , Yoshihisa Nozaki , Shiro Tachikawa , Masaaki Takeda , Shinji Usuda
IPC分类号： C07D207/08 , C07D209/14 , C07D211/26 , C07D213/53 , C07D217/14 , C07D307/52 , C07D207/14
CPC分类号： C07D213/53 , C07D207/08 , C07D209/14 , C07D211/26 , C07D217/14 , C07D307/52
摘要： The compounds of this invention are strong central nervous system depressants, in particular strong antipsychotics.
摘要翻译：其中R表示氢原子或低级烷基; X表示低级烷氧基; Y表示氢原子，氨基或单 - 或二 - 低级烷基氨基; Z表示卤素原子，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，氨磺酰基或低级烷基氨磺酰基; 所述Y和Z可以结合形成-N = N-NH-; W表示由下式表示的基团：其中A表示苯基，环己基，呋喃基或吡啶基; R 1，R 2和R 4可以相同或不同，不同的是，各自表示氢原子，低级烷基或苯基; R 3表示低级烷基，苯基低级烷基或二低级烷基氨基低级烷基; R 5，R 6和R 7可以相同或不同，各自表示氢原子，卤素原子，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基或三氟甲基; R8表示低级烷基; n表示代表1或2），1-乙基-5-苯基-2-吡咯烷基甲基，1-乙基-2-异吲哚啉基甲基，2-乙基-1,2,3,4-四氢-4-异喹啉基， 2-（2-苯基吡咯烷子基）乙基，2-（2-异吲哚啉基）乙基或2-（1,2,3,4-四氢-2-异喹啉基）乙基及其药学上可接受的无毒盐。本发明的化合物是强中枢神经系统抑制剂，特别是强抗精神病药。

4. 发明授权

US4609737A Novel 2-guanidinothiazoline compounds, and process for preparing them 失效
标题翻译：新型2-胍基噻唑啉化合物及其制备方法
公开(公告)号：US4609737A
公开(公告)日：1986-09-02
申请号：US742581
申请日：1985-06-07
申请人： Yasufumi Hirata , Isao Yanagisawa
发明人： Yasufumi Hirata , Isao Yanagisawa
IPC分类号： C07D277/10 , C07D277/18 , C07D277/20 , C07D277/46 , C07D277/48
CPC分类号： C07D277/18 , C07D277/48
摘要： Novel 2-guanidinothiazoline compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, and the acid addition salts thereof; they are important intermediate compounds for preparing famotidine and thiotidine which are medicaments useful as gastric acid secretion inhibitors.

5. 发明授权

US4283408A Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them 失效
标题翻译：胍基噻唑化合物，制备方法和含有它们的胃抑制组合物
公开(公告)号：US4283408A
公开(公告)日：1981-08-11
申请号：US107629
申请日：1979-12-27
申请人： Yasufumi Hirata , Isao Yanagisawa , Yoshio Ishii , Shinichi Tsukamoto , Noriki Ito , Yasuo Isomura , Masaaki Takeda
发明人： Yasufumi Hirata , Isao Yanagisawa , Yoshio Ishii , Shinichi Tsukamoto , Noriki Ito , Yasuo Isomura , Masaaki Takeda
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61P1/00 , A61P1/04 , A61P43/00 , C07D277/40 , C07D277/48 , C07D277/38
CPC分类号： C07D277/48 , C07D277/40
摘要： Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a substituted- or unsubstituted-aryl group, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof, they are useful as gastric acid secretion inhibitors.
摘要翻译：新型的胍基噻唑化合物，其通式为：其中R表示氢原子或低级烷基，R1表示氨基，低级烷基，卤代低级烷基，取代或未取代的芳基，单 - 或二 - 低级烷基氨基，芳基氨基或芳烷基氨基，R 2表示氢原子，低级烷基，低级烯基或低级炔基，Y表示硫原子或亚甲基，m和n 各自表示1-3的整数，其药理学上可接受的酸加成盐可用作胃酸分泌抑制剂。

6. 发明授权

US4252819A Antisecretory heterocyclic amidine compounds 失效
标题翻译：防雾杂环脒化合物
公开(公告)号：US4252819A
公开(公告)日：1981-02-24
申请号：US934276
申请日：1978-08-16
申请人： Yasufumi Hirata , Isao Yanagisawa , Toshinari Tamura , Masaaki Takeda
发明人： Yasufumi Hirata , Isao Yanagisawa , Toshinari Tamura , Masaaki Takeda
IPC分类号： C07D233/64 , A61K31/40 , A61K31/4402 , A61K31/4418 , A61K31/4427 , A61K31/455 , A61P43/00 , C07D213/30 , C07D213/32 , C07D213/68 , C07D213/86 , C07D233/54 , C07D277/26 , C07D307/52 , C07D401/12 , C07D401/14 , C07D413/12 , A61K31/34 , A61K31/38 , C07D307/54 , C07D333/24
CPC分类号： C07D213/30 , C07D213/32 , C07D213/68 , C07D213/86 , C07D233/64 , C07D277/26 , C07D307/52
摘要： Novel heterocyclic compounds shown by the formula ##STR1## wherein Het represents a 5-membered or 6-membered heterocyclic group which may have substituent(s); Z represents a sulfur atom or oxygen atom; X represents an oxygen atom or the unsubstituted or substituted imino group shown by N--R.sub.1 (wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a cyano group, an unsubstituted or alkyl substituted carbamoyl group, an unsubstituted or lower alkyl substituted thiocarbamoyl group, or a lower alkanoylamino group); Y represents a hydrogen atom, a lower alkyl group which may have substituent(s), a cycloalkyl group of 3-6 carbon atoms, a lower alkenyl group, a lower alkynyl group, an aryl group which may have substituent(s), an aralkyl group which may have substituent(s), a hydroxyl group, a cyano group, a carbamoyl group, an amidino group, an alkanoyl group which may have been substituted by halogen atom(s),an alkanoylamino group, an arylcarbonylamino group, an alkylamino group, an arylamino group, an arylsulfamoyl group, a lower alkoxycarbamoyl group, or an oxamoylamino group; and m and n represent an integer of 1-3; when X is N-R.sub.1, said X and Y may combine with each other to form a 5-membered or 6-membered heterocyclic ring containing 2-3 nitrogen atoms which may have substituent(s), and the pharmaceutically acceptable acid addition salts thereof.The compounds of this invention are useful as gastric acid secretion inhibitors.
摘要翻译：式中，Het表示可具有取代基的5元或6元杂环基的新型杂环化合物。 Z表示硫原子或氧原子; X表示氧原子或由N-R 1表示的未取代或取代的亚氨基（其中R 1为氢原子，低级烷基，氰基，未取代或烷基取代的氨基甲酰基，未取代或低级烷基取代的硫代氨基甲酰基，或低级烷酰氨基）; Y表示氢原子，可具有取代基的低级烷基，3-6个碳原子的环烷基，低级烯基，低级炔基，可具有取代基的芳基，可以具有取代基的芳烷基，羟基，氰基，氨基甲酰基，脒基，可被卤素原子取代的烷酰基，烷酰基氨基，芳基羰基氨基，烷基氨基，芳基氨基，芳基氨磺酰基，低级烷氧基氨基甲酰基或氨甲酰基氨基; m和n表示1-3的整数; 当X为N-R 1时，所述X和Y可以彼此结合形成含有2-3个可具有取代基的氮原子的5元或6元杂环，及其药学上可接受的酸加成盐。本发明的化合物可用作胃酸分泌抑制剂。

7. 发明授权

US4362736A Guanidinothiazole compounds, and medical compositions containing them 失效
标题翻译：胍基噻唑化合物和含有它们的医药组合物
公开(公告)号：US4362736A
公开(公告)日：1982-12-07
申请号：US127902
申请日：1980-03-06
申请人： Yasufumi Hirata , Isao Yanagisawa , Yoshio Ishii , Masaaki Takeda
发明人： Yasufumi Hirata , Isao Yanagisawa , Yoshio Ishii , Masaaki Takeda
IPC分类号： C07D277/38 , C07D277/46 , C07D277/48 , C07D277/20 , A61K31/425
CPC分类号： C07D277/48 , C07D277/46
摘要： Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, Y represents a sulfur atom or a methylene group, m and n each represents an integer of 1-3, A represents the group shown by ##STR2## (wherein R.sub.1 represents a hydrogen atom, a cyano group, a carbamoyl group, a ureido group, a hydroxyl group, a lower alkoxy group, a lower acyl group, an acylamino group, an arylsulfamoyl group, an aralkyl group or a carboxymethyl group, an arylsulfamoyl group, an aralkyl group or a carboxymethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cyano group or a lower acyl group, and R.sub.3 represents a hydrogen atom, a lower alkyl group, a hydroxyl group or a sulfamoyl group), and the pharmacologically acceptable acid addition salts thereof; these compounds are useful as gastric acid secretion inhibitors.
摘要翻译：新颖的通式为“IMAGE”的胍基噻唑化合物，其中R表示氢原子或低级烷基，Y表示硫原子或亚甲基，m和n各自表示1-3的整数，A表示由（其中R 1表示氢原子，氰基，氨基甲酰基，脲基，羟基，低级烷氧基，低级酰基，酰氨基，芳基氨磺酰基，芳烷基或羧甲基，芳基氨磺酰基，芳烷基或羧甲基，R2表示氢原子，低级烷基，低级烯基，低级炔基，氰基或低级酰基，R3表示氢原子，低级烷基，羟基或氨磺酰基）及其药理学上可接受的酸加成盐; 这些化合物可用作胃酸分泌抑制剂。

8. 发明授权

US4097487A Pyrrolidinyl and piperidinyl benzamide derivatives 失效
标题翻译：吡咯烷基和哌啶基苯甲酰胺衍生物
公开(公告)号：US4097487A
公开(公告)日：1978-06-27
申请号：US671583
申请日：1976-03-29
申请人： Masuo Murakami , Kozo Takahashi , Yasufumi Hirata , Mutsuo Takashima , Sumio Iwanami , Osamu Hasegawa , Yoshihisa Nozaki , Shiro Tachikawa , Masaaki Takeda , Shinji Usuda
发明人： Masuo Murakami , Kozo Takahashi , Yasufumi Hirata , Mutsuo Takashima , Sumio Iwanami , Osamu Hasegawa , Yoshihisa Nozaki , Shiro Tachikawa , Masaaki Takeda , Shinji Usuda
IPC分类号： C07D207/09 , C07D209/14 , C07D211/26 , C07D213/53 , C07D217/14 , C07D307/52 , C07D207/16 , C07D211/60
CPC分类号： C07D213/53 , C07D207/09 , C07D209/14 , C07D211/26 , C07D217/14 , C07D307/52
摘要： The compounds of this invention are strong central nervous system depressants, in particular strong antipsychotics.
摘要翻译：其中R表示氢原子或低级烷基; X表示低级烷氧基; Y表示氢原子，氨基或单 - 或二 - 低级烷基氨基; Z表示卤素原子，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，氨磺酰基或低级烷基氨磺酰基; 所述Y和Z可以组合形成-N = N-NH-; W表示由下式表示的基团：其中A表示苯基，环己基，呋喃基或吡啶基; R 1，R 2和R 4可以相同或不同，不同的是，各自表示氢原子，低级烷基或苯基; R 3表示低级烷基，苯基低级烷基或二低级烷基氨基低级烷基; R 5，R 6和R 7可以相同或不同，各自表示氢原子，卤素原子，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基或三氟甲基; R8表示低级烷基; n表示代表1或2），1-乙基-5-苯基-2-吡咯烷基甲基，1-乙基-2-异吲哚啉基甲基，2-乙基-1,2,3,4-四氢-4-异喹啉基， 2-（2-苯基吡咯烷子基）乙基，2-（2-异二氢吲哚基）乙基或2-（1,2,3,4-四氢-2-异喹啉基） - 乙基和药学上可接受的无毒盐其中。

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