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    • 7. 发明申请
    • SUSPENSION OF SPARINGLY WATER-SOLUBLE ACIDIC DRUG
    • 悬浮性水溶性酸性药物
    • WO1997041832A1
    • 1997-11-13
    • PCT/JP1997001496
    • 1997-05-01
    • TAISHO PHARMACEUTICAL CO., LTD.NAITO, MayumiNAKANO, HiroshiHASEGAWA, KazuoNAKAJIMA, ToshiakiOKUDAIRA, IchiroTSUNODA, Kenji
    • TAISHO PHARMACEUTICAL CO., LTD.
    • A61K09/107
    • A61K9/0095
    • A suspension of a sparingly water-soluble acidic drug especially, a nonsteroidal anti-inflammatory analgetic agent, which is stable for a prolonged period of time and is highly dissolvable; and a process for simply and easily producing the suspension. This suspension has a pH value of 2 to 5 and comprises a sparingly water-soluble acidic drug whose average particle size ranges from 1 to 15 mu m, a polyglycerol fatty acid ester, a water-soluble polyhydric alcohol and water, optionally, together with an inorganic powder having an average particle size of 1 to 15 mu m. This process is characterized by carrying out pulverization and dispersion of sparingly water-soluble acid drug, a polyglycerol fatty acid ester, a water-soluble polyhydric alcohol and water by means of a pulverizer comprising a main shaft adapted to rotate in a casing and a plurality of layshafts adapted to revolve in relationship interlocked with the rotation of the main shaft, each of the layshafts being fitted with a multiplicity of annular grinding media.
    • 一种微溶水性酸性药物,特别是非甾体类消炎镇痛药的悬浮液,它是长时间稳定且高度可溶的; 以及简单且容易地制造悬浮液的方法。 该悬浮液的pH值为2〜5,包含平均粒径为1〜15μm的微溶水性酸性药物,聚甘油脂肪酸酯,水溶性多元醇和水,以及 平均粒径为1〜15μm的无机粉末。 该方法的特征在于通过粉碎机进行微水溶性酸性药物,聚甘油脂肪酸酯,水溶性多元醇和水的粉碎和分散,该粉碎机包括适于在壳体中旋转的主轴和多个 的副轴适于以与主轴的旋转互锁的关系旋转,每个副轴装配有多个环形研磨介质。
    • 9. 发明申请
    • AMINO COMPOUNDS AND ANGIOTENSIN IV RECEPTOR AGONISTS
    • 氨基化合物和血管紧张素Ⅱ受体激动剂
    • WO1998005624A1
    • 1998-02-12
    • PCT/JP1997002716
    • 1997-08-05
    • TAISHO PHARMACEUTICAL CO., LTD.SAGAMI CHEMICAL RESEARCH CENTERKOBORI, TakeoGODA, KenichiSUGIMOTO, KikuoOTA, TomomiTOMISAWA, Kazuyuki
    • TAISHO PHARMACEUTICAL CO., LTD.SAGAMI CHEMICAL RESEARCH CENTER
    • C07C211/13
    • C07D213/40C07C237/20C07D215/12
    • Amino compounds represented by general formula (1) or pharmaceutically acceptable salts thereof: (wherein X represents CH2NH or CONH; Y represents CH2NH or CONH, provided that X and Y do not represent CONH at the same time; Z represents CH=C(R )R , CH2CH(R )R or alkoxycarbonyl (wherein R and R independently represent each hydrogen or optionally substituted alkyl, aralkyl, aryl or heteroaryl); R represents hydrogen or optionally substituted lower alkyl, cycloalkyl, cycloalkyl-substituted alkyl, aralkyl or aryl; and R and R independently represent each optionally substituted lower alkyl or aralkyl); drugs composed of the amino compounds of general formula (1) or pharmaceutically acceptable salts thereof; and angiotensin receptor agonists containing the same as the active ingredient. These drugs are useful as remedies such as antagonists or agonists for various pathological states in which angiotensin IV participates, for example, accelerated renal blood flow, cerebral vasodilation, cell proliferation inhibition or hypermnesia.
    • 由通式(1)表示的氨基化合物或其药学上可接受的盐:(其中X表示CH 2 NH或CONH; Y表示CH 2 NH或CONH,条件是X和Y不同时表示CONH; Z表示CH = C R 5),CH 2 CH(R 4)R 5或烷氧基羰基(其中R 4和R 5独立地表示各个氢或任选取代的烷基,芳烷基,芳基或杂芳基); R R 1和R 3独立地代表各个任选被取代的低级烷基或芳烷基); R 2和R 3独立地表示任意取代的低级烷基或芳烷基。 由通式(1)的氨基化合物或其药学上可接受的盐组成的药物; 和含有与活性成分相同的血管紧张素受体激动剂。 这些药物可用作诸如血管紧张素IV参与的各种病理状态的拮抗剂或激动剂,例如加速肾血流量,脑血管扩张,细胞增殖抑制或高血症。