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71. 发明公开

EP0852233A1 CYCLOSPORIN PHOSPHATE DERIVATIVES AND MEDICINAL COMPOSITION 失效
标题翻译： CYCLOSPORIN-PHOSPHAT-DERIVATE UND MEDIZINISCHE ZUSAMMENSETZUNGEN
公开(公告)号：EP0852233A1
公开(公告)日：1998-07-08
申请号：EP95932203.3
申请日：1995-09-21
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： KONNO, Kiyotaka , SETO, Takashi , YOSHIFUSA, Hiroto , EZURE, Yoji
IPC分类号： C07K7/64 , A61K38/13
CPC分类号： C07K7/645 , A61K38/00
摘要： The invention provides a novel cyclosporin compound which is water-soluble, improved in the amount of absorption and absorption rate after oral administration, with low nephrotoxicity, and a pharmaceutical composition comprising the same compound.
The compound of the invention includes such cyclosporin phosphate derivatives as [phosphonothreonine 2 ]cyclosporin A, [phosphono-4-hydroxynorvaline 2 ]cyclosporin A, [phosphono-D-serine 8 ]cyclosporin A, [phosphonothreonine 2 , phosphono-D-serine 8 ]cyclosporin A, etc. or salts thereof, and solvates thereof.
摘要翻译：本发明提供了一种新型的环孢菌素化合物，其具有水溶性，口服给药后的吸收和吸收量的量增加，肾毒性低，以及包含相同化合物的药物组合物。本发明的化合物包括这种环磷酰胺磷酸酯衍生物，如亚膦酸二环素环孢菌素A，亚膦酰基-4-羟基诺维定2环孢菌素A，亚膦酰-D-丝氨酸8环孢菌素A，亚膦酸腺嘌呤2，膦酰-D-丝氨酸 <8>环孢菌素A等，或其盐，及其溶剂合物。

72. 发明公开

EP0821961A1 NEOVASCULARIZATION INHIBITOR 失效
标题翻译：抑制剂DER NEOVASKULARISATION
公开(公告)号：EP0821961A1
公开(公告)日：1998-02-04
申请号：EP96910205.2
申请日：1996-04-19
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： UEDA, Fusao , KATOH, Fumitaka
IPC分类号： A61K31/53
CPC分类号： A61K31/53
摘要： The invention relates to a neovascularization inhibitor composition comprising a compound of the following general formula [I] or a salt thereof, or a solvate thereof, as an active ingredient,
wherein R 1 represents hydrogen, optionally substituted alkyl, aralkyl, arylalkenyl, or aryl; R 2 represents optionally substituted alkyl, aralkyl, arylalkenyl, or aryl; or R 1 and R 2 conjoinedly and taken together with the adjacent N atom, i.e. in the form of NR 1 R 2 , represent a 4- through 8-membered cyclic amino group optionally containing nitrogen, oxygen, or sulfur as a ring member in addition to said N atom and optionally being further substituted.
摘要翻译：本发明涉及一种新生血管形成抑制剂组合物，其包含作为活性成分的下列通式ⅪI或其盐或其溶剂化物的化合物：其中R 1表示氢，任选取代的烷基，芳烷基，芳基烯基，或芳基; R 2表示任选取代的烷基，芳烷基，芳基烯基或芳基; 或R 1和R 2连接并与相邻的N原子一起，即以NR 1 R 2的形式，代表任选含有氮，氧的4-至8-元环氨基，或除了所述N原子之外的硫作为环成员，并且任选地被进一步取代。

73. 发明授权

EP0319986B1 Anti-plasmin depressant 失效
标题翻译：抗纤溶酶抑制剂
公开(公告)号：EP0319986B1
公开(公告)日：1997-03-12
申请号：EP88120564.5
申请日：1988-12-08
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： Yoshikuni, Yoshiaki , Ojima, Nobutoshi , Mori, Kazuya
IPC分类号： A61K31/445 , A61K31/70 , A61K31/435
CPC分类号： A61K31/7004 , A61K31/435 , A61K31/445 , A61K31/70

74. 发明公开

EP0729748A1 PROCESS FOR PRODUCING STABLE MEDICINAL COMPOSITION, AND PHARMACEUTICAL PREPARATION 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG STABILER ARZNEIMITTEL UND PHARMAZEUTISCHE ZUBEREITUNG
公开(公告)号：EP0729748A1
公开(公告)日：1996-09-04
申请号：EP95900907.7
申请日：1994-11-17
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： NAKAMICHI, Kouichi , IZUMI, Shougo , YASUURA, Hiroyuki
IPC分类号： A61K9/00
CPC分类号： A61K9/2095 , A61K9/1694
摘要： An object of the invention is to provide a technique whereby medicines and pharmaceutical preparations can readily be stabilized by a more practicable and economical process than before. The process comprises processing 1 part by weight of a physiologically inactive powdery additive, 0.001-1 part by weight of a high-molecular-weight additive and, for example, a sublimable medicine as the essential starting materials in one batch on a multi-screw extruder. This process enables a physicochemically stable medicinal composition to be produced readily and rapidly in a large quantity and in a fundamentally continuous manner.
摘要翻译：本发明的目的是提供一种技术，其中药物和药物制剂可以通过比以前更可行和经济的方法容易地稳定。该方法包括加工1重量份的生理惰性粉末状添加剂，0.001-1重量份的高分子量添加剂和例如作为主要原料的可升华药物，在一个批次中多重螺杆挤出机。该方法使得物理化学稳定的药物组合物能够以大量和基本上连续的方式容易且快速地生产。

75. 发明授权

EP0598116B1 FAT EMULSION 失效
标题翻译： FETTEMULSION
公开(公告)号：EP0598116B1
公开(公告)日：1996-07-24
申请号：EP90917270.2
申请日：1990-11-26
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： SEKI, Junzo , USHIMARU, Kouichi , SUGIYAMA, Makoto
IPC分类号： A61K9/107 , A61K31/71
CPC分类号： A61K9/1075 , A61K31/7048
摘要： A fat emulsion developed to solve the problems of polyene antifungal antibiotics that they have such a severe toxicity as to limit the administration range thereof by suitably designing the administration form, thereby reducing the hemolytic toxicity and nephrotoxicity and facilitating the migration of a drug toward infected parts without adversely affecting the pharmacological action (antifungal action) on a molecular level. The emulsion comprises 0.005 to 5 % of a polyene antifungal antibiotic, 0.5 to 30 % of a simple lipid, and a phospholipid in an amount 0.15 to 2 times as large as that of the simple lipid, wherein the relative proportion of each ingredient is controlled to give a fine microemulsion of a mean particle diameter of at least 10 nm up to 100 nm. This emulsion can remarkably enhance the efficacy of polyene antifungal antibiotics such as Amphotericin B and is very useful for the development of medicines.

76. 发明公开

EP0685457A1 GLYCEROL DERIVATIVE, DEVICE AND PHARMACEUTICAL COMPOSITION 失效
标题翻译： GLYCEROLDERIVAT，VORRICHTUNG UND PHARMAZEUTISCHE ZUSAMMENSETZUNG。
公开(公告)号：EP0685457A1
公开(公告)日：1995-12-06
申请号：EP94907060.1
申请日：1994-02-17
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： YANO, Junichi , OHGI, Tadaaki
IPC分类号： C07C229/06 , C07C237/08 , C07C271/16 , C07C279/04 , C07C307/02 , C07D207/08 , C07D211/08 , C07D241/04 , C07D265/30 , C07F9/40
CPC分类号： A61K31/70 , A61K9/1272 , C07C229/12 , C07C237/08 , C07C271/16 , C07C271/20 , C07C279/20 , C07C333/04 , C07D295/13 , C07F9/4075
摘要： The invention aims at providing a device comprising lipids that act like the so-called cationic liposome and are reduced in toxicity and the lipids as the constituent of the device. The invention compounds are exemplified by 3-0-(4-dimethylaminobutanoyl)-1,2-0-dioleylglycerol, 3-0-(2-dimethylaminoethyl)carbamoyl-1,2-0-dioleylglycerol, 3-0-(2-diethylaminoethyl)carbamoyl-1,2-0-dioleylglycerol, and 2-0-(2-diethylaminoethyl)-carbamoyl-1,3-0-dioleylglycerol. The device comprises these lipids and phospholipids. The device enables, when administered together with, for example, a double-stranded RNA, the RNA to migrate to the action site safely.
摘要翻译：本发明的目的在于提供一种装置，其包含像所谓的阳离子脂质体那样起作用并且毒性降低的脂质和作为装置成分的脂质。本发明化合物的实例是3-0-（4-二甲基氨基丁酰基）-1,2-二油基甘油，3-0-（2-二甲基氨基乙基）氨基甲酰基-1,2-二油基甘油，3-0-（2- 二乙基氨基乙基）氨基甲酰基-1,2-二油基甘油和2-0-（2-二乙基氨基乙基） - 氨基甲酰基-1,3-0-二油基甘油。该装置包括这些脂质和磷脂。当与例如双链RNA一起施用时，该装置能够安全地迁移到作用部位的RNA。

77. 发明公开

EP0665009A1 CRYSTALLINE CONDITION DISLOCATING METHOD 失效
标题翻译： VERFAHREN ZUR VERSCHIEBUNG EINES KRISTALLZUSTANDES。
公开(公告)号：EP0665009A1
公开(公告)日：1995-08-02
申请号：EP93922625.4
申请日：1993-10-13
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： NAKAMICHI, Kouichi , IZUMI, Shougo , OKA, Masaaki
IPC分类号： A61K9/00 , A61K9/14
CPC分类号： A61K9/14
摘要： An object of this invention is to provide a method of dislocating the crystalline condition of crystalline medicine simply, speedily and homogeneously, and, moreover, in large quantities at once. This invention is directed to a method using an extruder when crystalline medicine in a certain crystalline condition (△ is dislocated to another crystalline condition (○), i.e., when the dislocation of crystalline condition (△->○) is carried out.
摘要翻译：本发明的一个目的是提供一种简单，快速和均匀的脱色结晶状态的方法，此外大量地提供一种方法。本发明涉及一种在某种结晶状态（INCREMENT被脱位到另一种结晶状态（即，当进行结晶状态的位错）时，使用挤出机的方法。

78. 发明公开

EP0598116A1 FAT EMULSION 失效
标题翻译： FETTEMULSION。
公开(公告)号：EP0598116A1
公开(公告)日：1994-05-25
申请号：EP90917270.2
申请日：1990-11-26
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： SEKI, Junzo , USHIMARU, Kouichi , SUGIYAMA, Makoto
IPC分类号： A61K9/107 , A61K31/71
CPC分类号： A61K9/1075 , A61K31/7048
摘要： A fat emulsion developed to solve the problems of polyene antifungal antibiotics that they have such a severe toxicity as to limit the administration range thereof by suitably designing the administration form, thereby reducing the hemolytic toxicity and nephrotoxicity and facilitating the migration of a drug toward infected parts without adversely affecting the pharmacological action (antifungal action) on a molecular level. The emulsion comprises 0.005 to 5 % of a polyene antifungal antibiotic, 0.5 to 30 % of a simple lipid, and a phospholipid in an amount 0.15 to 2 times as large as that of the simple lipid, wherein the relative proportion of each ingredient is controlled to give a fine microemulsion of a mean particle diameter of at least 10 nm up to 100 nm. This emulsion can remarkably enhance the efficacy of polyene antifungal antibiotics such as Amphotericin B and is very useful for the development of medicines.
摘要翻译：为了解决多烯抗真菌抗生素的问题，开发了一种脂肪乳剂，它们具有如此严重的毒性，通过适当地设计给药形式来限制其给药范围，从而降低溶血毒性和肾毒性并促进药物向感染部位的迁移而不会对分子水平的药理作用（抗真菌作用）产生不利影响。乳液含有0.005〜5％的多烯抗真菌抗生素，0.5〜30％的单一脂质，磷脂的量为单质脂质量的0.15〜2倍，其中各成分的相对比例被控制得到至少10nm至100nm的平均粒径的微细微乳液。该乳液可以显着提高多烯抗真菌抗生素如两性霉素B的功效，对于药物的开发是非常有用的。

79. 发明公开

EP0555478A4 PYRIMIDINE DERIVATIVE AND MEDICINE 失效
标题翻译：吡嗪衍生物和药物
公开(公告)号：EP0555478A4
公开(公告)日：1993-11-18
申请号：EP91915722
申请日：1991-08-29
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： CHOKAI, SHOICHI , AOKI, TOMIYOSHI , KIMURA, KIYOSHI
IPC分类号： C07D239/34 , C07D239/42 , C07D401/12 , C07D453/02
CPC分类号： C07D453/02 , C07D239/34 , C07D239/42 , C07D401/12
摘要： The invention aims at obtaining a novel compound which is excellent in central nervous system selectivity and reduced in side effects and has an activity of improving the function of learning and memory, thus providing an excellent medicine for dementia. The invention relates to a compound represented by general formula (I), a pharmacologically acceptable salt thereof, and an agent for remedying the disturbance of learning and memory containing the same as the active ingredient of formula (I), wherein R?1 and R2¿ may be the same or different from each other and each represents hydrogen, hydroxy, alkoxy, trifluoromethyl or halogen; A represents methyl, trifluoromethyl or tertbutyl; and Y represents O or NH.

80. 发明公开

EP0558750A4 DISPERSION PREPARATION 失效
标题翻译：分散制剂
公开(公告)号：EP0558750A4
公开(公告)日：1993-10-20
申请号：EP91919697
申请日：1991-11-15
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： SEKI, JUNZO, 6-16, SHIROGANE 3-CHOME INAGAWACHO , YAMAMOTO, HIROFUMI, NIPPONSHINYAKU CO., LTD.
IPC分类号： A61K9/107 , A61K31/70 , A61K31/7048
CPC分类号： A61K31/7048

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