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11. 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.

12. 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。

13. 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.

14. 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。

15. 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。

16. 发明授权

US6012169A Glove made of polyvinyl chloride resin 失效
标题翻译：由聚氯乙烯树脂制成的手套
公开(公告)号：US6012169A
公开(公告)日：2000-01-11
申请号：US248097
申请日：1999-02-11
申请人： Yasutaka Nishi , Akio Miyake
发明人： Yasutaka Nishi , Akio Miyake
IPC分类号： A41D19/00 , A61B19/04 , A61L2/16 , B32B27/18 , B32B27/30 , C09D5/14 , C09D133/06
CPC分类号： A41D19/0058 , A61B42/00 , A41D2400/34
摘要： An object of the invention is to provide a polyvinyl chloride resin-made glove exhibiting an antimicrobial activity both on inner and outer surfaces of the glove which has a simple constitution and is easily fabricated to be cost-competitive. The glove is constituted of a base layer 1 formed of the polyvinyl chloride resin and an antimicrobial agent including layer 2 of which major composition is a polyacrylic resin formed on one of the surfaces of the base layer, no matter what the surface may be the outer one or the inner one of the glove. A base layer thickness of the glove is reduced less than a specified thickness through which the antimicrobial agent can penetrate diffusibly from one of surfaces to the opposite surface of the glove.
摘要翻译：本发明的目的是提供一种在手套的内表面和外表面上具有抗微生物活性的聚氯乙烯树脂制手套，其具有简单的结构并且易于制造成具有成本竞争力。手套由聚氯乙烯树脂形成的基底层1和包含层2的抗微生物剂构成，其中主要成分是在基底层的一个表面上形成的聚丙烯酸树脂，不管表面可以是外部的一个或内部的一个手套。手套的基层厚度减小到比抗微生物剂从表面的一个表面到手套的相对表面可扩散穿透的规定厚度小。

17. 发明授权

US5922712A Eosinophil chemotaxis inhibitor 失效
标题翻译：嗜酸性粒细胞趋化性抑制剂
公开(公告)号：US5922712A
公开(公告)日：1999-07-13
申请号：US070928
申请日：1998-05-01
申请人： Akio Miyake , Yasuko Ashida , Tatsumi Matsumoto
发明人： Akio Miyake , Yasuko Ashida , Tatsumi Matsumoto
IPC分类号： A61K31/50 , A61K31/5025
CPC分类号： A61K31/5025 , A61K31/50
摘要： A method for inhibiting eosinophil infiltration by administrating to a subject in need thereof an effective amount of a compound of the formula: ##STR1## wherein R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-4 group, and R.sup.4a and R.sup.5a independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or a pharmaceutically acceptable salt thereof.
摘要翻译：通过向有需要的受试者施用有效量的下式化合物来抑制嗜酸性粒细胞浸润的方法：其中R2和R3独立地表示氢原子或C1-4基团，并且R4a和R5a独立地表示氢原子或 C 1-4烷基或其药学上可接受的盐。

18. 发明授权

US5703081A Quinolonecarboxylic acid derivatives, their production and use 失效
标题翻译：喹诺酮羧酸衍生物，其生产和使用
公开(公告)号：US5703081A
公开(公告)日：1997-12-30
申请号：US608697
申请日：1996-02-29
申请人： Akio Miyake , Masahira Nakamura , Hideto Fukushi
发明人： Akio Miyake , Masahira Nakamura , Hideto Fukushi
IPC分类号： C07D215/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D513/04 , C07D519/00 , A61K31/495 , A61K31/47 , C07D401/02
CPC分类号： C07D401/04 , C07D215/56 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D513/04
摘要： A composition comprises a 1,7-disubstituted-4-oxo-3-quinolinecarboxylic acid or 1,7-disubstituted-4-oxo-3-naphthyridinecarboxylic acid derivative which is useful as a prophylactic and/or therapeutic agent for peripheral arterial obstruction, acute myocardial infarction, an antitumor agent, and as a prophylactic and/or therapeutic agent for osteoporosis.
摘要翻译：组合物包含可用作外周动脉阻塞的预防和/或治疗剂的1,7-二取代-4-氧代-3-喹啉羧酸或1,7-二取代-4-氧代-3-萘啶羧酸衍生物，急性心肌梗死，抗肿瘤剂，以及作为骨质疏松症的预防和/或治疗剂。

19. 发明授权

US5409919A Pharmaceutically acceptable salt of 7B-[2-(5-amino-1,2,4-thio-diazol-3-yl)-2(Z)-metho-xyiminoacetamido]-3-[( imidazo[1,2-b]pyridazinium-1-yl)methyl]-3-cephem-4-carboxylate and composition comprising same 失效
标题翻译： -3β-[（咪唑并[1,2-b]吡啶-3-基）-2（Z） - 亚氨基亚氨基乙酰氨基] -3 - [（咪唑并[ ]哒嗪鎓-1-基）甲基] -3-头孢烯-4-羧酸钠及其组合物
公开(公告)号：US5409919A
公开(公告)日：1995-04-25
申请号：US41849
申请日：1993-04-02
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.
摘要翻译：下式的化合物：其中R 1为可被保护的氨基，R 3为氢原子或任选取代的烃残基; Z是S，S-> O，O或CH2，R4是氢原子，甲氧基或甲酰氨基，R13是氢原子，甲基，羟基或卤素原子，A（+）是任选取代的咪唑鎓 - 在2,3-或3,4-位上形成稠合环或其药学上可接受的盐或酯是新的，具有优异的抗菌活性。

20. 发明授权

US5369104A Pyridazine compounds, their production and use 失效
标题翻译：哒嗪化合物，其生产和使用
公开(公告)号：US5369104A
公开(公告)日：1994-11-29
申请号：US997538
申请日：1992-12-28
申请人： Akio Miyake , Yasuhiko Kawano , Yasuko Ashida
发明人： Akio Miyake , Yasuhiko Kawano , Yasuko Ashida
IPC分类号： C07D487/04 , A61K31/50 , A61K31/55 , C07D487/14
CPC分类号： C07D487/04
摘要： Novel compound represented by the formula: ##STR1## wherein X stands for a methine (i.e. the group --CH.dbd.) group or a nitrogen atom; R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, or, taken together, may form a 5- to 7-membered ring combined with the adjacent --C.dbd.C--; R.sup.4 and R.sup.5 respectively stands for a hydrogen atom or an optionally substituted lower alkyl group or, taken together, form a 3- to 7-membered homo- or heterocyclic ring combined with the adjacent carbon atom; A stands for an optionally substituted amino group; m and n denote 1 to 4, respectively, or salts thereof which has an antiallergic, antiinflammatory and anti-PAF activity and is useful as an antiasthmatic agent.
摘要翻译：由下式表示的新型化合物：其中X表示次甲基（即基团-CH =）基团或氮原子; R1代表氢原子，任选取代的低级烷基或卤素原子; R2和R3分别表示氢原子或任选取代的低级烷基，或者一起可以形成与相邻-C = C-结合的5-至7-元环; R4和R5分别表示氢原子或任选取代的低级烷基，或者一起形成与相邻碳原子结合的3-至7-元同 - 或杂环; A代表任选取代的氨基; m和n分别表示1至4个或其盐，其具有抗过敏，抗炎和抗PAF活性，并且可用作抗哮喘药。

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