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1. 发明授权

US4857527A Morpholine containing pyridine compounds, compositions and use 失效
标题翻译：含有吡啶化合物的吗啉，组成和用途
公开(公告)号：US4857527A
公开(公告)日：1989-08-15
申请号：US184195
申请日：1988-04-21
申请人： Takao Takaya , Hisashi Takasugi , Kimio Esumi , Atsushi Kuno , Hiroyoshi Sakai , Kazuhiro Maeda , Yoshie Sakamoto
发明人： Takao Takaya , Hisashi Takasugi , Kimio Esumi , Atsushi Kuno , Hiroyoshi Sakai , Kazuhiro Maeda , Yoshie Sakamoto
IPC分类号： C07D213/82
CPC分类号： C07D213/82
摘要： An N-containing heterocyclic compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl optionally substituted with hydroxy, halogen or a heterocyclic group, carboxy, esterified carboxy, carbamoyl optionally substituted with heterocyclic(lower)alkyl or lower alkylamino(lower)alkyl, N-containing heterocycliccarbonyl optionally substituted with lower alkyl, or ureido optionally substituted with lower alkylamino(lower)alkyl, andR.sup.3 is hydrogen or halogen;R.sup.2 is phenyl substituted with nitro, andX is .dbd.N--or ##STR2## in which R.sup.4 is lower alkyl or halo(lower)alkyl, or is taken together with R.sup.1 to form an N-containing heterocyclic group optionally substituted with oxo and lower alkylamino(lower)alkyl; orR.sup.2 is lower alkyl, andX is ##STR3## in which R.sup.4 is phenyl substituted with nitro; and a pharmaceutically acceptable salt thereof, processes for the preparation thereof and pharmaceutical (e.g. antihypertension) compositions comprising the same.
摘要翻译：含有下式的杂环化合物：其中R 1为任选被羟基，卤素或杂环基取代的低级烷基，羧基，酯化羧基，任选被杂环（低级）烷基或低级烷基氨基（低级）烷基取代的氨基甲酰基，任选被低级烷基取代的含N杂环羰基或任选被低级烷基氨基（低级）烷基取代的脲基，R 3为氢或卤素; R 2为被硝基取代的苯基，X为= N-或其中R 4为低级烷基或卤代（低级）烷基），或与R 1一起形成任选被氧代取代的含氮杂环基烷基氨基（低级）烷基; 或R2是低级烷基，X是其中R4是被硝基取代的苯基; 和其药学上可接受的盐，其制备方法和包含其的药物（例如抗高血压）组合物。

2. 发明授权

US4990507A N-containing heterocyclic compounds, and composition comprising the same 失效
标题翻译：含氮杂环化合物及其组合物
公开(公告)号：US4990507A
公开(公告)日：1991-02-05
申请号：US294743
申请日：1989-01-09
申请人： Takao Takaya , Hisashi Takasugi , Kimio Esumi , Atsushi Kuno , Hiroyoshi Sakai , Kazuhiro Maeda , Yoshie Sakamoto
发明人： Takao Takaya , Hisashi Takasugi , Kimio Esumi , Atsushi Kuno , Hiroyoshi Sakai , Kazuhiro Maeda , Yoshie Sakamoto
IPC分类号： C07D213/26 , C07D213/30 , C07D213/36 , C07D213/75 , C07D213/80 , C07D213/82 , C07D237/08 , C07D237/24 , C07D413/12 , C07D471/04 , C07D401/12 , A61K31/44
CPC分类号： C07D213/30 , C07D213/26 , C07D213/36 , C07D213/75 , C07D213/80 , C07D213/82 , C07D237/08 , C07D237/24 , C07D413/12 , C07D471/04
摘要： The invention relates to a pharmaceutical composition as a therapeutic agent for ischemic disease comprising a compound of the formula ##STR1## wherein R.sup.1 is carbamoyl substituted with morpholino (lower) alkyl, thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl; andR.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substituted with nitro;with proviso that R.sup.1 is carbamoyl substituted with thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl when R.sup.4 is lower alkyl; or its salt, as an active ingredient, in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.
摘要翻译：本发明涉及作为缺血性疾病治疗剂的药物组合物，其包含下式化合物其中R 1是被吗啉代（低级）烷基，硫代吗啉代（低级）烷基或低级烷基氨基（低级）烷基取代的氨基甲酰基）或被低级烷基氨基（低级）烷基取代的脲基; R2是被硝基取代的苯基，R4是低级烷基; 或R 2为低级烷基，R 4为被硝基取代的苯基; 条件是R1是被硫代吗啉代（低级）烷基或低级烷基氨基（低级）烷基取代的氨基甲酰基; 或当R 4为低级烷基时被低级烷基氨基（低级）烷基取代的脲基; 或其盐作为活性成分，与药学上可接受的，基本上无毒的载体或赋形剂结合。

3. 发明授权

US4931453A Di phenylpyridazine compounds, processes for the preparation thereof and pharmaceutical compositions comprising the same 失效
标题翻译：二苯基哒嗪化合物，其制备方法和包含其的药物组合物
公开(公告)号：US4931453A
公开(公告)日：1990-06-05
申请号：US286169
申请日：1988-12-19
申请人： Hisashi Takasugi , Atsushi Kuno , Hiroyoshi Sakai , Yoshie Sugiyama , Takao Takaya
发明人： Hisashi Takasugi , Atsushi Kuno , Hiroyoshi Sakai , Yoshie Sugiyama , Takao Takaya
IPC分类号： C07D237/10 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/445 , A61K31/455 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/54 , A61P9/00 , A61P25/28 , C07D211/78 , C07D213/26 , C07D213/30 , C07D213/36 , C07D213/38 , C07D213/80 , C07D213/82 , C07D237/04 , C07D237/08 , C07D237/24 , C07D471/04
CPC分类号： C07D213/30 , C07D211/78 , C07D213/26 , C07D213/36 , C07D213/80 , C07D213/82 , C07D237/04 , C07D237/08 , C07D237/24 , C07D471/04
摘要： The invention relates to diphenylpyridazine compounds useful in the treatment of cerebrovascular disease, of the formula: ##STR1## wherein R.sup.1 is piperazinyl(lower)alkyl, carbamoyl substituted with piperazinyl(lower)alkyl, or piperazinylcarbonyl, in each of which a piperazinyl group may be substituted with lower alkyl,R.sup.2 is phenyl substituted with nitro, andR.sup.3 is hydrogen or halogen, or a pharmaceutically acceptable salt thereof.

4. 发明授权

US4831030A Diphenylpyridine compounds, processes for the preparation thereof and composition comprising the same 失效
标题翻译：二苯基吡啶化合物，其制备方法和包含其的组合物
公开(公告)号：US4831030A
公开(公告)日：1989-05-16
申请号：US940923
申请日：1986-12-12
申请人： Hisashi Takasugi , Atsushi Kuno , Hiroyoshi Sakai , Yoshie Sugiyama , Takao Takaya
发明人： Hisashi Takasugi , Atsushi Kuno , Hiroyoshi Sakai , Yoshie Sugiyama , Takao Takaya
IPC分类号： C07D237/10 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/445 , A61K31/455 , A61K31/495 , A61K31/50 , A61K31/535 , A61K31/54 , A61P9/00 , A61P25/28 , C07D211/78 , C07D213/26 , C07D213/30 , C07D213/36 , C07D213/38 , C07D213/80 , C07D213/82 , C07D237/04 , C07D237/08 , C07D237/24 , C07D471/04
CPC分类号： C07D213/30 , C07D211/78 , C07D213/26 , C07D213/36 , C07D213/80 , C07D213/82 , C07D237/04 , C07D237/08 , C07D237/24 , C07D471/04
摘要： The invention relates to compounds for treatment of hypertension, and cardiovascular and cerebrovascular diseases, which compounds are of the formula: ##STR1## wherein R.sup.1 is piperazinyl(lower)alkyl, carbamoyl substituted with piperazinyl(lower)alkyl, or piperazinylcarbonyl, in each of which a piperazinyl group may be substituted with lower alkyl, andR.sup.3 is hydrogen or halogen;R.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl or halo(lower)alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substitured with nitro;and a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及用于治疗高血压和心血管和脑血管疾病的化合物，其化合物具有下式：其中R 1是哌嗪基（低级）烷基，被哌嗪基（低级）烷基或哌嗪基羰基取代的氨基甲酰基，哌嗪基可以被低级烷基取代，R3是氢或卤素; R2是被硝基取代的苯基，R4是低级烷基或卤代（低级）烷基; 或R2是低级烷基，R4是被硝基取代的苯基; 及其药学上可接受的盐。

5. 发明授权

US4698340A Pyrimidine derivatives, processes for preparation thereof and composition containing the same 失效
标题翻译：嘧啶衍生物，其制备方法和含有它们的组合物
公开(公告)号：US4698340A
公开(公告)日：1987-10-06
申请号：US753912
申请日：1985-07-11
申请人： Takao Takaya , Hisashi Takasugi , Atsushi Kuno , Yoshie Sugiyama
发明人： Takao Takaya , Hisashi Takasugi , Atsushi Kuno , Yoshie Sugiyama
IPC分类号： C07D213/50 , A61K31/505 , A61P9/00 , A61P25/28 , C07C205/56 , C07D213/55 , C07D239/20 , C07D239/26 , C07D239/28 , C07D239/30 , C07D239/34 , C07D239/42 , C07D333/00 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D491/04 , C07D491/048 , C07D491/052
CPC分类号： C07D239/26 , C07C205/45 , C07C205/56 , C07D239/20 , C07D239/30 , C07D239/42 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D491/04
摘要： The invention relates to pyrimidine derivatives and their pharmaceutically acceptable salts which are useful in the treatment of cerebrovascular diseases, to processes for preparation thereof and to the composition containing the same, said pyrimidine derivatives being represented by the following formula: ##STR1## wherein Ar, R.sup.1, R.sup.2 and R.sup.3 are as defined in the disclosure.
摘要翻译：本发明涉及可用于治疗脑血管疾病的嘧啶衍生物及其药学上可接受的盐，其制备方法和含有该嘧啶衍生物的组合物，所述嘧啶衍生物由下式表示：其中Ar， R1，R2和R3如本公开中所定义。

6. 发明授权

US4727073A Pyrimidine derivatives and composition of the same 失效
标题翻译：嘧啶衍生物及其组成相同
公开(公告)号：US4727073A
公开(公告)日：1988-02-23
申请号：US779043
申请日：1985-09-23
申请人： Takao Takaya , Hisashi Takasugi , Atsushi Kuno , Yoshie Sugiyama
发明人： Takao Takaya , Hisashi Takasugi , Atsushi Kuno , Yoshie Sugiyama
IPC分类号： A61K31/505 , C07C205/56 , C07D239/20 , C07D239/26 , C07D239/30 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D487/04 , C07D491/04
CPC分类号： C07D239/26 , C07C205/45 , C07C205/56 , C07D239/20 , C07D239/30 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/04 , C07D487/04 , C07D491/04
摘要： The invention relates to new pyrimidine derivatives, useful in the treatment of cerebrovascular disease, of the formula: ##STR1## wherein Ar, R.sup.1, R.sup.2 and R.sup.3 are defined in the specification.
摘要翻译：本发明涉及可用于治疗脑血管疾病的新的嘧啶衍生物，具有下式：其中Ar，R 1，R 2和R 3在说明书中定义。

7. 发明授权

US5037824A N-containing heterocyclic compounds, compositions and use 失效
标题翻译：含氮杂环化合物，组合物和用途
公开(公告)号：US5037824A
公开(公告)日：1991-08-06
申请号：US489536
申请日：1990-03-07
申请人： Hisashi Takasugi , Atsushi Kuno , Hiroyoshi Sakai
发明人： Hisashi Takasugi , Atsushi Kuno , Hiroyoshi Sakai
IPC分类号： C07D213/73 , C07D213/75 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/85 , C07D405/04 , C07D409/04 , C07D413/04
CPC分类号： C07D213/73 , C07D213/75 , C07D213/80 , C07D213/82 , C07D213/84 , C07D213/85 , C07D405/04 , C07D409/04 , C07D413/04
摘要： The invention relates to cardioprotective compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2 R.sup.3 and R.sup.4 are moieties as described in the specification.

8. 发明授权

US4925948A 2 amino 5 chloro thiazol-4-yl cycloalkenoxy imino acetic derivatives 失效
标题翻译： 2氨基-5-氯噻唑-4-基环烯氧基亚氨基乙酸衍生物
公开(公告)号：US4925948A
公开(公告)日：1990-05-15
申请号：US845526
申请日：1986-03-28
申请人： Takao Takaya , Hisashi Takasugi , Masayoshi Murata , Akiteru Yoshioka
发明人： Takao Takaya , Hisashi Takasugi , Masayoshi Murata , Akiteru Yoshioka
IPC分类号： C07D277/20 , C07D277/38 , C07D277/40 , C07D277/46 , C07D501/20 , C07D501/22 , C07D501/36 , C07D501/59
CPC分类号： C07D277/587
摘要： Compounds of the formula ##STR1## wherein r.sup.1 is amino or protected amino R.sup.2 is cycloalkenyl X is halogen and Y is carboxy or protected carboxy, or salts useful as intermediates for cephalosporin antibiotics.

9. 发明授权

US4822888A New cepham compounds and processes for the production thereof 失效
标题翻译：新的头孢烯化合物及其制备方法
公开(公告)号：US4822888A
公开(公告)日：1989-04-18
申请号：US830973
申请日：1986-02-19
申请人： Takao Takaya , Hisashi Takasugi , Kiyosha Tsuji , Toshiyuki Chiba
发明人： Takao Takaya , Hisashi Takasugi , Kiyosha Tsuji , Toshiyuki Chiba
IPC分类号： C07C251/38 , A61K31/545 , A61K31/546 , A61P31/04 , C07C251/52 , C07C251/60 , C07D277/20 , C07D277/38 , C07D277/40 , C07D277/44 , C07D285/06 , C07D501/14 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/59 , C07D277/48
CPC分类号： C07D277/20 , C07D277/587 , C07D285/06 , C07D501/20
摘要： A compound of the formula: ##STR1## wherein R.sup.2 is halo(lower)alkyl, andR.sup.6 is amino or protected amino, its reactive derivative at the carboxy group or its lower alkyl ester, is disclosed, having utility as an intermediate for producing cephems or cephams.
摘要翻译：公开了下式的化合物，其中R 2是卤代（低级）烷基，R 6是氨基或被保护的氨基，其在羧基或其低级烷基酯上的反应性衍生物，可用作生产cephems的中间体或cephams。

10. 发明授权

US4639448A 7-amino-3-[substituted vinyl]-3-cephem-4-carboxylates having antimicrobial activity 失效
标题翻译：具有抗菌活性的7-氨基-3- [取代的乙烯基] -3-头孢烯-4-羧酸酯
公开(公告)号：US4639448A
公开(公告)日：1987-01-27
申请号：US741267
申请日：1985-06-04
申请人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka , Kenji Miyai , Yoshikazu Inoue
发明人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka , Kenji Miyai , Yoshikazu Inoue
IPC分类号： A61K20060101 , A61K31/54 , A61K31/545 , C07D20060101 , C07D501/00 , C07D501/04 , C07D501/14 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/48
CPC分类号： C07D501/24 , C07D501/18
摘要： The invention relates to cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or acylamino,R.sup.2 is lower alkyl, andY is CH or N.

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