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    • 3. 发明申请
    • VASCULAR SMOOTH MUSCLE CELL MIGRATION INHIBITOR
    • 血管平滑肌细胞移植抑制剂
    • WO1996004903A1
    • 1996-02-22
    • PCT/JP1995001492
    • 1995-07-27
    • TEIJIN LIMITEDMASEGI, TsukioTOMIMORI, KojiWATANABE, Kunihito
    • TEIJIN LIMITED
    • A61K31/215
    • A61K31/5575
    • A vascular smooth muscle cell migration inhibitor and a preventive or remedy for post-PTCA restenosis, each containing an isocarbacyclin represented by general formula (1) and/or an enantiomer thereof as the active ingredient, wherein W represents o-, m- or p-phenylene, C3-C7 cycloalkylene or thiophenediyl; R represents hydrogen, methyl, ethyl or vinyl; R represents optionally substituted linear or branched C3-C9 alkyl, alkenyl or alkynyl, or C3-C7 cycloalkyl; R represents hydrogen, C1-C10 alkyl, phenyl, naphthyl, benzyl or a mono-equivalent cation; Z and Z represent each independently hydrogen, tri(C1-C7 hydrocarbyl)silyl or a group that forms an acetal or ester linkage together with the oxygen atom to which it is bonded; n represents 0 or 1; and m represents an integer of 0 to 4.
    • 血管平滑肌细胞迁移抑制剂和用于PTCA后再狭窄的预防或治疗,每种含有由通式(1)表示的异卡巴环素和/或其对映异构体作为活性成分,其中W表示o-,m-或p 亚苯基,C3-C7亚环烷基或噻吩二基; R 1表示氢,甲基,乙基或乙烯基; R 2表示任选取代的直链或支链C 3 -C 9烷基,烯基或炔基或C 3 -C 7环烷基; R 30表示氢,C 1 -C 10烷基,苯基,萘基,苄基或单当量阳离子; Z 10和Z 20各自独立地表示氢,三(C 1 -C 7烃基)甲硅烷基或与其键合的氧原子一起形成缩醛或酯键的基团; n表示0或1; m表示0〜4的整数。
    • 6. 发明申请
    • POWDERY MEDICINE DOSING DEVICE
    • 粉末药物剂量设备
    • WO1997004826A1
    • 1997-02-13
    • PCT/JP1996002097
    • 1996-07-25
    • TEIJIN LIMITEDMATSUGI, HideoKAWABE, HiroyukiMAKINO, YujiSUZUKI, YoshikiFUJII, Takao
    • TEIJIN LIMITED
    • A61M13/00
    • A61M15/0028A61M11/00A61M2202/06A61M2202/064
    • A powdery medicine dosing device which achieves portability, simplicity and rapidity of operation, simplicity of a manufacturing process, rigidity of construction, and economy such as minimization of the number of parts and low costing. The device comprises a medicine holding section, which defines therein a powder medicine storing space doubling as an air reservoir and of which at least a portion of a wall is flexible, and a medicine leading-out section which allows an inner space of the medicine holding section to communicate with the outside. The inner space of the medicine holding section communicates with the outside only through the medicine leading-out section, and the medicine leading-out section is of a tubular construction which includes at one end thereof a medicine spraying port disposed outside of the medicine holding section and at the other end thereof a medicine suction port disposed in the inner space of the medicine holding section. Disposed substantially immediately below the medicine suction port of the medicine leading-out section is a bottom of the inner space of the medicine holding section, and disposed close to the bottom is the medicine suction port, so that a powder medicine is jetted outside through the medicine leading-out section by pressing and loosening the flexible wall portion of the medicine holding section.
    • 实现便携性,操作简单性和快速性,制造过程简单,结构刚性和经济性的粉末药物计量装置,例如零件数量的最小化和低成本。 该装置包括:药剂保持部,其在其中限定作为空气储存器加倍的粉末药物储存空间,壁的至少一部分是柔性的;以及药物引出部,其允许药剂保持的内部空间 部分与外界沟通。 药剂保持部的内部空间仅通过药物引出部与外部连通,药物导出部为管状结构,其一端包括设置在药剂保持部的外侧的药剂喷出口 另一端设置在药剂保持部的内部空间中的吸药口。 在药物引出部的药液吸入口的下方大致立即设置在药剂保持部的内部空间的底部,并且靠近底部设置有药物吸入口,从而将粉末药物通过 通过按压和松开药物保持部的柔性壁部来进行药物导出部。
    • 7. 发明申请
    • POWDERY COMPOSITION FOR NASAL ADMINISTRATION
    • 粉末成分为NASAL管理
    • WO1997031626A1
    • 1997-09-04
    • PCT/JP1997000541
    • 1997-02-26
    • TEIJIN LIMITEDDOHI, MasahikoNISHIBE, YoshihisaMAKINO, YujiFUJII, Takao
    • TEIJIN LIMITED
    • A61K09/14
    • A61K9/0043
    • A powdery composition for nasal administration wherein: (1) the composition comprises (i) a medicament, (ii) a water-absorbent, gel-forming base such as hydroxypropylcellulose or hydroxypropylmethylcellulose, and (iii) a water-absorbent, sparingly water-soluble base such as crystalline cellulose or alpha -cellulose; (2) the amount of the water-absorbent, gel-forming base is about 5 to 40 % by weight of the sum of the amounts of the water-absorbent, gel-forming base and the water-absorbent, sparingly water-soluble base; and (3) the medicament is unevenly dispersed in the water-absorbent, sparingly water-soluble base rather than in the water-absorbent, gel-forming base. The composition is advantageous in that an excellent absorption via the nasal cavity can be offered even in the case of a highly water-soluble medicament, a highly liposoluble medicament, and a high-molecular weight peptide or protein medicament and the maximum blood level is much larger than that for the conventional compositions for nasal administration.
    • 一种用于鼻内给药的粉末状组合物,其中:(1)组合物包含(i)药物,(ii)吸水性凝胶形成碱如羟丙基纤维素或羟丙基甲基纤维素,和(iii)吸水性, 可溶性碱如结晶纤维素或α-纤维素; (2)吸水性凝胶形成基质的量为吸水性凝胶形成基质和吸水性微溶水性基质的总量的5〜40重量% ; 和(3)药物不均匀地分散在吸水性微水溶性基质中而不是在吸水凝胶形成基质中。 该组合物的优点在于,即使在高度水溶性药物,高度脂溶性药物和高分子量肽或蛋白质药物的情况下也可以提供通过鼻腔的优异吸收,并且最大血液水平是多 大于用于鼻腔给药的常规组合物。
    • 9. 发明申请
    • 7-THIAPROSTAGLANDIN E1'S AND PROCESS FOR THEIR PREPARATION
    • 7-THIAPROSTAGLANDIN E1及其制备方法
    • WO1985003936A1
    • 1985-09-12
    • PCT/JP1985000110
    • 1985-03-05
    • TEIJIN LIMITEDTANAKA, ToshioBANNAI, KiyoshiHAZATO, AtsuoKUROZUMI, Seiji
    • TEIJIN LIMITED
    • C07C177/00
    • C07C405/0033
    • 7-thiaprostaglandin E1's represented by formula (I): (wherein R1 represents H, C1 to C10 alkyl, C2 to C20 alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted C3 to C10 cycloalkyl, substituted or unsubstituted phenyl(C1 to C2)alkyl, or mono-equivalent cation, R2 and R3, which may be the same or different, each represents H, tri(C1 to C7)-hydrocarbylsilyl or a group forming an acetal bond with the oxygen atom of the hydroxy group, R4 represents H, methyl or vinyl, R5 represents straight or branched C3 to C8 alkyl, straight or branched C3 to C8 alkenyl, straight or branched C3 to C8 alkynyl, optionally substituted phenyl, optionally substituted phenoxy, optionally substituted C3 to C10 cycloalkyl, or straight or branched C1 to C5 alkyl substituted by C1 to C6 alkoxy, optionally substituted phenyl, optionally substituted phenoxy or optionally substituted C3 to C10 cycloalkyl, X represents ethylene, vinylene or ethynylene, n represents 0 or 1,$(1,6)$represents ethylene or vinylene, provided that, when n represents 0 and X represents ethylene, R5 does not represent straight or branched C3 to C8 alkyl, nor optionally substituted C3 to C10 cycloalkyl), enantiomers thereof, and mixtures thereof in arbitrary ratios are useful for treating and/or preventing diseases of digestive organs such as duodenum or stomach.