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11. 发明授权

US5948774A Cephem compounds, their production and use 失效
标题翻译：头孢烯化合物，其生产和使用
公开(公告)号：US5948774A
公开(公告)日：1999-09-07
申请号：US836424
申请日：1997-07-29
申请人： Keiji Kamiyama , Kenji Okonogi , Akio Miyake
发明人： Keiji Kamiyama , Kenji Okonogi , Akio Miyake
IPC分类号： C07D501/00 , C07D501/24 , A61K31/545
CPC分类号： C07D501/00
摘要： Cephem compounds of the formula: ##STR1## wherein R.sup.1 is an optionally protected amino group; R.sup.2 is a fluoro-lower alkyl group; and the ring A may have further substituent(s), or their esters or salts, show broad and excellent antibacterial activities and are useful as antibacterial agents.
摘要翻译： PCT No.PCT / JP96 / 01436 Sec。 371日期1997年7月29日第 102（e）日期1997年7月29日PCT提交1996年5月28日PCT公布。 WO96 / 34851 PCT出版物日期：1996年12月5日化学式：其中R1为任选保护的氨基; R2是氟代低级烷基; 并且环A可以具有其它取代基或其酯或盐，显示出广泛和优异的抗菌活性并且可用作抗菌剂。

12. 发明授权

US4962100A 3-Condensed imidazolium-cephem compounds 失效
标题翻译： 3-缩合咪唑 - 头孢烯化合物
公开(公告)号：US4962100A
公开(公告)日：1990-10-09
申请号：US331192
申请日：1989-03-28
申请人： Akio Miyake , Masahiro Kondo , Masahiko Fujino
发明人： Akio Miyake , Masahiro Kondo , Masahiko Fujino
IPC分类号： C07D501/06 , A61K31/545 , A61K31/546 , C07D277/20 , C07D285/08 , C07D463/00 , C07D471/04 , C07D487/04 , C07D498/04 , C07D501/46 , C07D505/00 , C07D519/00
CPC分类号： C07D277/587 , C07D285/08 , C07D463/20 , C07D463/22 , C07D471/04 , C07D487/04 , C07D505/00
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sup..sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.

13. 发明授权

US4725592A 1-Acyloxyalkyl esters of cephalosporin 失效
标题翻译：头孢菌素的1-芳氧基烷基酯
公开(公告)号：US4725592A
公开(公告)日：1988-02-16
申请号：US637138
申请日：1984-08-03
申请人： Akio Miyake , Masayoshi Yamaoka , Mitsuo Numata
发明人： Akio Miyake , Masayoshi Yamaoka , Mitsuo Numata
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36 , C07D501/56
CPC分类号： C07D501/36
摘要： A compound of the formula: ##STR1## wherein R.sub.1 stands for n-propyl or isopropyl; and R.sub.2 stands for n-butyl, isobutyl, n-pentyl, n-hexyl or 2-ethylbutyl, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.
摘要翻译：下式的化合物：其中R 1代表正丙基或异丙基; R2代表正丁基，异丁基，正戊基，正己基或2-乙基丁基，或其药学上可接受的盐，其制备方法及其药物组合物。该化合物可口服施用，具有改善生物利用度的抗生素。

14. 发明授权

US4665065A 3-pyrazolo(1,5-a.alpha.pyridinium cephem compounds 失效
标题翻译： 3-吡唑并（1,5-aα吡啶鎓头孢烯化合物
公开(公告)号：US4665065A
公开(公告)日：1987-05-12
申请号：US739440
申请日：1985-05-30
申请人： Akio Miyake , Masahiro Kondo , Masahiko Fujino
发明人： Akio Miyake , Masahiro Kondo , Masahiko Fujino
IPC分类号： C07D463/00 , C07D501/46 , C07D505/00 , C07D519/00 , A61K31/545
CPC分类号： C07D519/00 , C07D463/16 , C07D463/22 , C07D505/00 , Y02P20/55
摘要： A compound of the formula; ##STR1## wherein R.sup.0 stands for hydrogen atom, nitrogen-containing heterocyclic group, acyl group or amino-protecting group, Z stands for S, S.fwdarw.O, O or CH.sub.2, R.sup.4 stands for hydrogen atom, methoxy group or formamido group, R.sup.13 stands for hydrogen atom, methyl group, hydroxyl group or halogen atom and A stands for an optionally substituted pyrazol-2-yl group forming a fused ring at the 1,5-position or a physiologically or pharmaceutically acceptable salt or ester thereof.This compound is novel and has excellent antibacterial activity.
摘要翻译：式的化合物; 其中R 0表示氢原子，含氮杂环基，酰基或氨基保护基，Z表示S，S-> O，O或CH2，R4表示氢原子，甲氧基或甲酰氨基， R13表示氢原子，甲基，羟基或卤素原子，A表示在1,5-位上形成稠环的任选取代的吡唑-2-基，或其生理或药学上可接受的盐或酯。该化合物新颖，抗菌活性优异。

15. 发明授权

US5098892A Process for preparation of bicyclic compounds 失效
标题翻译：制备双相化合物的方法
公开(公告)号：US5098892A
公开(公告)日：1992-03-24
申请号：US302940
申请日：1989-01-30
申请人： Yoshikazu Oka , Kohei Nishikawa , Akio Miyake
发明人： Yoshikazu Oka , Kohei Nishikawa , Akio Miyake
IPC分类号： C07C213/08 , A61K38/00 , C07K5/02
CPC分类号： C07K5/022 , A61K38/00
摘要： New bicyclic compounds, inclusive of salts thereof, of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, hydroxyl or lower alkoxy, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is hydrogen, lower alkyl, amino-lower-alkyl or acylamino-lower-alkyl, R.sup.5 is hydrogen, lower alkyl or aralkyl which may be substituted, R.sup.6 is hydroxyl, lower alkoxy, amino or lower alkylamino, and m and n each means 1 or 2, have inhibitory activities of angiotensin converting enzyme and bradykinin decomposing enzyme, and are useful as antihypertensive agents.

16. 发明授权

US4921851A Cephem compounds, their production and use 失效
标题翻译：头孢烯化合物，其生产和使用
公开(公告)号：US4921851A
公开(公告)日：1990-05-01
申请号：US396758
申请日：1989-08-22
申请人： Shoji Kishimoto , Kiminori Tomimatsu , Akio Miyake , Yoshinobu Yoshimura
发明人： Shoji Kishimoto , Kiminori Tomimatsu , Akio Miyake , Yoshinobu Yoshimura
IPC分类号： C07D501/00 , C07D501/46 , C07D519/00
CPC分类号： C07D501/46 , C07D501/00 , C07D519/00
摘要： This invention relates to a compound of the formula: ##STR1## wherein Q is nitrogen or CH; R.sup.1 is hydrogen or a lower alkyl group which may be substituted; and ring A is a pyridine or pyridazine ring which is substituted at the ring-constituting carbon atom by a group of the formula:--E--(CH.sub.2).sub.n --R.sup.2in which E is sulfur or NH; R.sup.2 is an amino, carbamoylamino, formylamino, acetylamino, N-formimidoylamino, N-acetimidoylamino, lower alkylamino, hydroxyl or carbamoyloxy group; and n is an integer of 2 to 4, or a pharmaceutically acceptable salt thereof. The compound (I) or a pharmaceutically acceptable sale thereof has excellent antibacterial activity and is used as antibiotics.
摘要翻译：本发明涉及下式的化合物：其中Q是氮或CH; R1是氢或可被取代的低级烷基; 环A为吡啶或哒嗪环，其在环的构成碳原子上被下列基团取代：其中E为硫或NH的-E-（CH2）n-R2; R2是氨基，氨基甲酰基氨基，甲酰氨基，乙酰氨基，N-甲脒基氨基，N-亚氨代乙酰氨基，低级烷基氨基，羟基或氨基甲酰氧基; n为2〜4的整数，或其药学上可接受的盐。化合物（I）或其药学上可接受的销售具有优异的抗菌活性并用作抗生素。

17. 发明授权

US4873172A Process for forming a superhigh contrast negative image 失效
标题翻译：用于形成超高对比度负像的过程
公开(公告)号：US4873172A
公开(公告)日：1989-10-10
申请号：US229796
申请日：1988-08-08
申请人： Shoji Ishiguro , Shigeo Hirano , Tadao Shishido , Akio Miyake
发明人： Shoji Ishiguro , Shigeo Hirano , Tadao Shishido , Akio Miyake
IPC分类号： G03C1/06
CPC分类号： G03C1/061
摘要： A process for forming a superhigh contrast negative image with a stable developer is disclosed, which comprises development processing a silver halide photographic material in the presence of a compound of formula (I) and a compound of formula (II) as defined in the specification.
摘要翻译：公开了一种用稳定显影剂形成超高对比度负像的方法，其包括在本说明书中定义的式（I）化合物和式（II）化合物存在下显影处理卤化银照相材料。

18. 发明授权

US4822818A Bicycle compounds, their production and use 失效
标题翻译：自行车化合物，其生产和使用
公开(公告)号：US4822818A
公开(公告)日：1989-04-18
申请号：US312639
申请日：1981-10-19
申请人： Yoshikazu Oka , Kohei Nishikawa , Akio Miyake
发明人： Yoshikazu Oka , Kohei Nishikawa , Akio Miyake
IPC分类号： C07C213/08 , A61K38/00 , C07K5/02 , A61K37/43 , C07C101/02 , C07C101/30 , C07C101/72
CPC分类号： C07K5/022 , A61K38/00
摘要： New bicyclic compounds, inclusive of salts thereof, of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, hydroxyl or lower alkoxy, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is hydrogen, lower alkyl, amino-lower-alkyl or acylamino-lower-alkyl, R.sup.5 is hydrogen, lower alkyl or aralkyl which may be substituted, R.sup.6 is hydroxyl, lower alkoxy, amino or lower alkylamino, and m and n each means 1 or 2, have inhibitory activities of angiotensin converting enzyme and bradykinin decomposing enzyme, and are useful as antihypertensive agents.

19. 发明授权

US4797395A 1-Acyloxyalkyl esters of cephalosporin 失效
标题翻译：头孢菌素的1-芳氧基烷基酯
公开(公告)号：US4797395A
公开(公告)日：1989-01-10
申请号：US886814
申请日：1986-07-18
申请人： Akio Miyake , Yoshinobu Yoshimura , Mitsuo Numata
发明人： Akio Miyake , Yoshinobu Yoshimura , Mitsuo Numata
IPC分类号： A61K31/545 , C07D501/36 , C07D501/56
CPC分类号： C07D501/36
摘要： A compound of the formula ##STR1## wherein (1) R.sub.1 is a lower alkyl group of 2 to 6 carbon atoms or a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a cycloalkyl group of 5 to 7 carbon atoms or a lower alkyl group of 1 to 3 carbon atoms which is substituted by a cycloalkyl group of 5 to 7 carbon atoms or by a phenyl group, or (2) R.sub.1 is a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a lower alkyl group of 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.
摘要翻译：式（Ⅰ）化合物其中（1）R 1为2〜6个碳原子的低级烷基或5〜7个碳原子的环烷基，R 2为5〜7个碳原子的环烷基原子或碳原子数为5〜7的环烷基取代的1〜3个碳原子的低级烷基或苯基，或（2）R 1为5〜7个碳原子的环烷基，R 2为提供1〜5个碳原子的低级烷基或其药学上可接受的盐，其制备方法及其药物组合物。该化合物可口服施用，具有改善生物利用度的抗生素。

20. 发明授权

US4521607A Chromanyl glycines 失效
标题翻译：色甘氨酸甘氨酸
公开(公告)号：US4521607A
公开(公告)日：1985-06-04
申请号：US365038
申请日：1982-04-02
申请人： Yoshikazu Oka , Kohei Nishikawa , Akio Miyake
发明人： Yoshikazu Oka , Kohei Nishikawa , Akio Miyake
IPC分类号： C07D215/42 , C07D311/68 , C07D317/70 , C07D339/04 , C07D307/82
CPC分类号： C07D311/68 , C07D215/42 , C07D317/70 , C07D339/04
摘要： New bicyclic compounds, inclusive of salts thereof, of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, each represent hydrogen, halogen, lower alkyl, hydroxyl, lower alkyloxy or aralkyloxy, or R.sup.1 and R.sup.2 jointly represent lower alkylenedioxy; R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl or --CH.sub.2 SR.sup.7 (R.sup.7 represents hydrogen or acyl); R.sup.6 represents hydrogen or acyl, or R.sup.6 and R.sup.7 jointly represent a single bond; X represents --CH.sub.2 --, --O-- or >N--R.sup.8 (R.sup.8 represents hydrogen, acyl or lower alkyl); and n represents 2, 3 or 4, have inhibitory activities of angiotensin converting enzyme and bradykinin decomposing enzyme, and are useful as antihypertensive agents.
摘要翻译：新的双环化合物，包括其盐，其具有下式：其中R 1和R 2可以相同或不同，各自代表氢，卤素，低级烷基，羟基，低级烷氧基或芳烷氧基，或R 1和R 2共同代表低亚烷基二氧基; R3和R4各自表示氢或低级烷基; R5代表氢，低级烷基或-CH2SR7（R7代表氢或酰基）; R6表示氢或酰基，或R6和R7共同表示单键; X表示-CH 2 - ， - O-或> N-R 8（R 8表示氢，酰基或低级烷基）。 n代表2,3或4，具有血管紧张素转换酶和缓激肽分解酶的抑制活性，可用作抗高血压药。

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