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1. 发明授权

US5496564A Suspendible composition and process for preparing the same 失效
标题翻译：可混合组合物及其制备方法
公开(公告)号：US5496564A
公开(公告)日：1996-03-05
申请号：US296403
申请日：1994-08-26
申请人： Sotoo Asakura , Yasuto Koyama , Youhei Kiyota , Kiyoko Akashi , Akira Kagayama , Yoshio Murakami , Toshiomi Nakate
发明人： Sotoo Asakura , Yasuto Koyama , Youhei Kiyota , Kiyoko Akashi , Akira Kagayama , Yoshio Murakami , Toshiomi Nakate
IPC分类号： A61K9/107 , A61K9/00 , A61K31/40 , A61K31/435 , A61K31/55 , A61K47/26 , A61P27/02 , A61P31/04 , A61P37/06 , C07D498/18 , A61K9/10 , A61K9/14 , A61K47/00
CPC分类号： A61K31/70 , A61K47/26 , A61K9/0048 , Y10S514/885 , Y10S514/912 , Y10S514/937 , Y10S514/951 , Y10S514/952 , Y10S514/97 , Y10S514/975
摘要： A suspendible composition comprising a tricyclic compound such as FK 506 substance which is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo-[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, or the like, and a pharmaceutically acceptable surfactant, which can be used as an orally administrable agent or eye drops and is useful for treating various diseases.
摘要翻译：含有17-烯丙基-1,14-二羟基-12- [2-（4-羟基-3-甲氧基环己基）-1-甲基乙烯基] -23,25-二甲氧基 - 环己基的三环化合物如FK 506物质的悬浮组合物， 13,19,21,27-四甲基-11,28-二氧杂-4-氮杂三环[22.3.1.04,9]二十八烷-18-烯-2,3,10,16-四酮等，和药学上可接受的表面活性剂，其可用作口服给药剂或滴眼剂，并且可用于治疗各种疾病。

2. 发明授权

US4772594A Prodrug compounds, process for the preparation thereof and sustained release preparation comprising the same 失效
标题翻译：前药化合物，其制备方法和包含其的缓释制剂
公开(公告)号：US4772594A
公开(公告)日：1988-09-20
申请号：US26530
申请日：1987-03-16
申请人： Masashi Hashimoto , Hidekazu Takeno , Hiroshi Kayakiri , Akira Kagayama , Yuji Tokunaga , Tomoaki Iwasa
发明人： Masashi Hashimoto , Hidekazu Takeno , Hiroshi Kayakiri , Akira Kagayama , Yuji Tokunaga , Tomoaki Iwasa
IPC分类号： C07H21/00 , C07J43/00 , A61K31/56 , C07J9/00
CPC分类号： C07H21/00 , C07J43/003
摘要： The invention relates to a novel prodrug compound useful in the treatment of tumors, of the formula:A--CO(CH.sub.2).sub.m (NHCO).sub.n --RwhereinA is a residue of an antitumor substance having >NH or --NH.sub.2 group in the molecule,R is a residue of cholesterol,m is an integer of 1 or 2 andn is 0 or 1,and its salts.
摘要翻译：本发明涉及一种可用于治疗肿瘤的新型前体药物化合物，具有下式：A-CO（CH 2）m（NHCO）n R，其中A是分子中具有> NH或-NH2基团的抗肿瘤物质的残基， R为胆固醇残基，m为1或2的整数，n为0或1，及其盐。

3. 发明授权

US6019752A Fluid vessel 失效
标题翻译：流体容器
公开(公告)号：US6019752A
公开(公告)日：2000-02-01
申请号：US894087
申请日：1997-08-13
申请人： Seizo Sunago , Akira Kagayama , Osamu Takahata , Hitoshi Futagawa , Mitsuo Murakami , Tomohiko Kubo
发明人： Seizo Sunago , Akira Kagayama , Osamu Takahata , Hitoshi Futagawa , Mitsuo Murakami , Tomohiko Kubo
IPC分类号： A61J1/00 , A61J1/20 , A61B19/00
CPC分类号： A61J1/2093 , A61J1/1462 , A61J1/201 , A61J1/2013 , A61J1/2027 , A61J1/2075 , A61J1/2086
摘要： A fluid vessel which include a drug storing chamber, a capping member for hermetically sealing the mouth portion of the drug storing chamber, and a solvent chamber joined to the bottom of the drug storing chamber, wherein the drug storing chamber is provided with a communication hole at the bottom thereof for communicating with the solvent chamber and includes a protruding piece which hermetically seals the communication hole, protrudes into the drug storing chamber, and is movable so as to open the communication hole, while the capping member has an engaging portion to be engaged with the tip of the protruding piece whereby the protruding piece is moved to open the communication hole by rotation of the capping member. This vessel serves to simplify the manufacturing process and reduces the number of components, is readily disposed of, facilitates mixing the drug with the solvent, and is easy to store and handle in hospitals and other facilities.
摘要翻译： PCT No.PCT / JP96 / 00308 Sec。 371日期1997年8月13日 102（e）日期1997年8月13日PCT 1996年2月9日PCT公布。 WO96 / 25136 PCT公开号日期：1996年8月22日包括药物储存室的流体容器，用于气密地密封药物储存室的口部的封盖构件和与药物储存室的底部连接的溶剂室，其中药物储存室在其底部设置有与溶剂室连通的连通孔，并且包括密封连通孔的突出片，突出到药物储存室中，并且可移动以打开连通孔，同时封盖构件具有与突出片的前端接合的接合部，由此突出片移动以通过盖帽构件的旋转来打开连通孔。该容器用于简化制造过程并减少部件数量，容易处理，便于药物与溶剂混合，并且易于在医院和其他设施中储存和处理。

4. 发明授权

US5939427A Lotion for FK 506 失效
标题翻译： FK 506的乳液
公开(公告)号：US5939427A
公开(公告)日：1999-08-17
申请号：US2887
申请日：1998-01-05
申请人： Akira Kagayama , Sachiyo Tanimoto , Saburo Murata , Takehisa Hata
发明人： Akira Kagayama , Sachiyo Tanimoto , Saburo Murata , Takehisa Hata
IPC分类号： A61K9/107 , A61K9/00 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/436 , A61K31/55 , A61K47/00 , A61K47/10 , A61K47/14 , A61K47/18 , A61K47/24 , A61K47/32 , A61K47/44 , A61P17/00 , A61P29/00 , C07D498/18 , A61K31/44
CPC分类号： A61K9/0014 , A61K31/407 , A61K31/436 , A61K31/55 , A61K31/70 , A61K47/00 , A61K47/10 , A61K47/14 , A61K47/32 , A61K47/44
摘要： A lotion comprising a tricyclic compound, typically 17-allyl-1,14-dihydroxy-12-�2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl!-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo �22.3.1.0.sup.4,9 !octacos-18-ene-2,3,10,16-tetraone, or a pharmaceutically acceptable salt thereof, a solubilizing and/or absorption-promoting agent, a liquid medium, and optionally an emulsifier and/or a viscosity increasing agent. The lotion is stable, excellent in absorption and has less irritation against the skin and sustained release. Also, the lotion is effective for the treatment and/or prophylaxis of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.
摘要翻译：包含三环化合物，通常为17-烯丙基-1,14-二羟基-12- [2-（4-羟基-3-甲氧基环己基）-1-甲基乙烯基] -23,25-二甲氧基-13,19,21， 27-二甲基-11,28-二氧杂-4-氮杂三环[22.3.1.04,9]二十八碳-18-烯-2,3,10,16-四酮或其药学上可接受的盐，增溶和/ 促进剂，液体介质和任选的乳化剂和/或增粘剂。洗剂稳定，吸收性好，对皮肤刺激性好，持续释放。此外，洗剂对于治疗和/或预防炎性和过度增生性皮肤病以及免疫介导的疾病的皮肤表现是有效的。

5. 发明授权

US5601844A Sustained release medicinal preparation 失效
标题翻译：持续释放药用制剂
公开(公告)号：US5601844A
公开(公告)日：1997-02-11
申请号：US424498
申请日：1995-05-18
申请人： Akira Kagayama , Sumihisa Kimura , Saburo Murata , Sachiyo Tanimoto , Takehisa Hata
发明人： Akira Kagayama , Sumihisa Kimura , Saburo Murata , Sachiyo Tanimoto , Takehisa Hata
IPC分类号： A61K9/16 , A61K9/52 , A61K31/436 , C07D498/18 , A61K9/48 , A61K9/50 , A61K31/44
CPC分类号： C07D498/18 , A61K31/436 , A61K9/1647
摘要： A sustained release medicinal preparation is produced by enclosing a macrocyclic compound represented by 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl)-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone or 17-ethyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, into the fine particles generally called microspheres which arc made of biodegradable polymer. This preparation, when, for example, given by injection, appreciably improves the transferance of said macrocyclic compound into the blood. Further, this is also used as an agent suitable for topical administration.
摘要翻译： PCT No.PCT / JP93 / 01672 Sec。 371日期1995年5月18日 102（e）日期1995年5月18日PCT提交1993年11月11日PCT公布。公开号WO94 / 10981 日期1994年5月26日缓释药物制剂是通过将由17-烯丙基-1,14-二羟基-12- [2-（4-羟基-3-甲氧基环己基）-1-甲基乙烯基）-23表示的大环化合物， 25-二甲氧基-13,19,21,27-四甲基-11,28-二氧杂-4-氮杂三环[22.3.1.04,9]二十八-18-烯-2,3,10,16-四酮或17-乙基 - 1,14-二羟基-12- [2-（4-羟基-3-甲氧基环己基）-1-甲基乙烯基] -23,25-二甲氧基-13,19,21,27-四甲基-11,28-二氧杂-4- 氮杂三环[22.3.1.04,9]二十八烷-18-烯-2,3,10,16-四酮，形成由可生物降解的聚合物制成的通常称为微球的细颗粒。当通过注射给予时，该制剂明显地改善了所述大环化合物向血液中的转移。此外，这也用作适合局部给药的药剂。

6. 发明授权

US5368865A Suspendible composition and process for preparing the same 失效
标题翻译：可混合组合物及其制备方法
公开(公告)号：US5368865A
公开(公告)日：1994-11-29
申请号：US97617
申请日：1993-07-27
申请人： Sotoo Asakura , Yasuto Koyama , Youhei Kiyota , Kiyoko Akashi , Akira Kagayama , Yoshio Murakami , Toshiomi Nakate
发明人： Sotoo Asakura , Yasuto Koyama , Youhei Kiyota , Kiyoko Akashi , Akira Kagayama , Yoshio Murakami , Toshiomi Nakate
IPC分类号： A61K9/107 , A61K9/00 , A61K31/40 , A61K31/435 , A61K31/55 , A61K47/26 , A61P27/02 , A61P31/04 , A61P37/06 , C07D498/18 , A61K9/10 , A61K9/14
CPC分类号： A61K31/70 , A61K47/26 , A61K9/0048 , Y10S514/885 , Y10S514/912 , Y10S514/937 , Y10S514/951 , Y10S514/952 , Y10S514/97 , Y10S514/975
摘要： A suspendible composition comprising a tricyclic compound such as FK 506 substance which is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny1]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, or the like, and a pharmaceutically acceptable surfactant, which can be used as an orally administrable agent or eye drops and is useful for treating various diseases.
摘要翻译：包含17-烯丙基-1,14-二羟基-12- [2-（4-羟基-3-甲氧基环己基）-1-甲基乙烯基] -23,25-二甲氧基 - 13,19,21,27-四甲基-11,28-二氧杂-4-氮杂三环[22.3.1.04,9]二十八-18-烯-2,3,10,16-四酮等，以及药学上可接受的表面活性剂，其可以用作口服给药剂或滴眼剂，并且可用于治疗各种疾病。

7. 发明授权

US06391851B1 Hydrochlorides of vancomycin antibiotics and process for producing the same 失效
标题翻译：万古霉素抗生素的盐酸盐及其制备方法
公开(公告)号：US06391851B1
公开(公告)日：2002-05-21
申请号：US09508528
申请日：2000-04-03
申请人： Seiji Sawai , Kenji Nishiwaki , Kazumi Ohtomo , Akira Kagayama
发明人： Seiji Sawai , Kenji Nishiwaki , Kazumi Ohtomo , Akira Kagayama
IPC分类号： A61K3816
CPC分类号： C07K9/008 , A61K38/14
摘要： Process for producing a hydrochloride of a vancomycin antibiotic, comprising subjecting an aqueous solution of a hydrochloride of a vancomycin antibiotic to a primary freezing at from −1° C. to −20° C. for a time sufficient to grow ice crystals, to form a primarily frozen substance, then subjecting said primarily frozen substance to a secondary freezing at from −25° C. to −80° C. to form a completely frozen solid, and then drying the resulting frozen solid in vacuo; and product obtained by the process.
摘要翻译：制备万古霉素抗生素的盐酸盐的方法，包括使万古霉素抗生素的盐酸盐水溶液在-1℃至-20℃下进行一次冰冻，持续足够的时间生长冰晶，形成然后将所述主要冷冻物质在-25℃至-80℃下进行二次冷冻，以形成完全冷冻的固体，然后真空干燥所得冷冻固体; 和通过该方法获得的产品。

8. 发明授权

US5826713A Fluid vessel 失效
标题翻译：流体容器
公开(公告)号：US5826713A
公开(公告)日：1998-10-27
申请号：US817649
申请日：1997-04-30
申请人： Seizo Sunago , Osamu Takahata , Akira Kagayama , Hitoshi Futagawa , Tetsuji Miyamoto , Mitsuo Murakami
发明人： Seizo Sunago , Osamu Takahata , Akira Kagayama , Hitoshi Futagawa , Tetsuji Miyamoto , Mitsuo Murakami
IPC分类号： A61J1/05 , A61J1/00 , A61J1/20 , A61J3/00 , B65D25/08
CPC分类号： A61J1/2089 , A61J1/1462 , A61J1/201 , A61J1/2017 , A61J1/2051
摘要： A fluid vessel including a drug vessel with a mouth portion sealed with a penetrable plug, a vial guide which holds the drug vessel and a flexible solvent vessel. The flexible solvent vessel has a drug solution outlet port and a communication port to the drug vessel, and an integrally molded tubular guide portion concentrically surrounding the communication port. Also included is a slidable communication mechanism housed in the tubular guide portion for communicating an inside of the solvent vessel and an inside of the drug vessel. Furthermore, also included is a cap for housing the vial guide and for rotatably sealing an opening of the guide portion, and a drug vessel push-down mechanism for moving the drug vessel down towards the communication port of the solvent vessel. The fluid vessel further includes a communication sequence control device for controlling a communication sequence so that, when the cap is rotated, the vial guide is moved down, without rotating, and the plug of the drug vessel is first pierced, and then a thin film of the communication port of the solvent vessel is pierced, thus communicating the drug vessel with the solvent vessel.
摘要翻译： PCT No.PCT / JP95 / 02215 Sec。 371日期1997年04月30日 102（e）1997年4月30日PCT PCT 1995年10月27日PCT公布。公开号WO96 / 13241 日期1996年5月9日一种流体容器，包括具有用可穿透塞子密封的口部的药物容器，容纳药物容器的小瓶引导件和柔性溶剂容器。柔性溶剂容器具有药液出口和与药物容器连通的连通口，以及整体模制的管状引导部分，同心地围绕连通口。还包括容纳在管状引导部分中用于使溶剂容器内部和药物容器内部连通的可滑动连通机构。此外，还包括用于容纳小瓶引导件并用于可旋转地密封引导部分的开口的盖，以及用于将药物容器朝向溶剂容器的连通口向下移动的药物容器下推机构。流体容器还包括用于控制通信顺序的通信顺序控制装置，使得当盖旋转时，小瓶引导件向下移动而不旋转，并且首先刺穿药物容器的塞子，然后将薄膜的溶剂容器的通信口被刺穿，从而使药物容器与溶剂容器连通。

9. 发明授权

US5817333A Liposome preparation containing a tricyclic compound 失效
标题翻译：含有三环化合物的脂质体制剂
公开(公告)号：US5817333A
公开(公告)日：1998-10-06
申请号：US446305
申请日：1995-05-22
申请人： Akira Kagayama , Yuji Tokunaga , Atsunori Kaibara , Sachiyo Tanimoto , Takehisa Hata
发明人： Akira Kagayama , Yuji Tokunaga , Atsunori Kaibara , Sachiyo Tanimoto , Takehisa Hata
IPC分类号： A61K31/435 , A61K9/127
CPC分类号： B82Y5/00 , A61K31/435 , Y10S514/885
摘要： A liposome preparation containing an immunosuppresive tricylic compound or a pharmaceutically acceptable salt thereof. Since the tricyclic compound is entrapped stably and quantitatively into the liposomes, a broad variety of drug forms and pharmaceutical preparations insuring a long duration of efficacy can be provided.
摘要翻译：含有免疫抑制性三环化合物或其药学上可接受的盐的脂质体制剂。由于三环化合物被稳定并定量地包埋在脂质体中，所以可以提供确保长期疗效的多种药物形式和药物制剂。

10. 发明授权

US5654009A Delayed action preparation 失效
标题翻译：延迟行动准备
公开(公告)号：US5654009A
公开(公告)日：1997-08-05
申请号：US635556
申请日：1996-04-22
申请人： Takehisa Hata , Akira Kagayama , Sumihisa Kimura , Satoshi Ueda , Saburo Murata
发明人： Takehisa Hata , Akira Kagayama , Sumihisa Kimura , Satoshi Ueda , Saburo Murata
IPC分类号： A61K9/16 , A61K9/50 , A61K9/52
CPC分类号： A61K9/1658 , A61K9/1652 , A61K9/5031 , A61K9/5078
摘要： The invention relates to a delayed action preparation which comprises a core comprising a drug and a swelling agent and an outer membrane comprising a biodegradable high molecular weight substance characterized in that the swelling agent is contained in a sufficient amount to cause a explosion of the outer membrane of biodegradable high molecular weight substance at a definite time after administration. This preparation provides for free control over the timing of drug release and is suited for administration not only by the oral route but also by the intramuscular, subcutaneous and other routes.
摘要翻译：本发明涉及延迟作用制剂，其包括包含药物和溶胀剂的核心和包含可生物降解的高分子量物质的外膜，其特征在于包含足够量的溶胀剂以引起外膜爆炸的生物降解性高分子量物质。该制剂提供了对药物释放时间的自由控制，并且不仅通过口服途径而且通过肌内，皮下和其它途径进行给药。

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