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    2'-MODIFIED ERYTHROMYCIN OR DERIVATIVE THEREOF
    2.
    发明公开
    2'-MODIFIED ERYTHROMYCIN OR DERIVATIVE THEREOF 失效
    2-MODIFIZIERTES ERYTHROMYCIN ODER DERIVAT DAVON。

    公开(公告)号：EP0553353A1

    公开(公告)日：1993-08-04

    申请号：EP91917071.2

    申请日：1991-10-08

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： ASAKA, Toshifumi ,  MISAWA, Yoko ,  KASHIMURA, Masato ,  MORIMOTO, Shigeo ,  WATANABE, Yoshiaki ,  HATAYAMA, Katsuo

    IPC分类号： C07H17/08 ,  A61K31/71

    CPC分类号： C07H17/08

    摘要： Modified erythromycin having remarkably alleviated bitterness and improved bioabsorbability, comprising a compound prepared by introducing a group represented by the formula: -O-CO-O-[(CH₂) m -O] n -R (wherein R represents C₁ to C₁₂ alkyl, m represents an integer of 2 to 4, and n represents an integer of 1 to 7), into the 2'-position of an erythromycin, or its salt.

    摘要翻译： 改进的红霉素具有显着缓解的苦味和改善的生物吸收性，包括通过引入由下式表示的基团制备的化合物：-O-CO-O - [（CH2）mO] nR（其中R表示C1至C12烷基，m表示整数 2〜4，n表示1〜7的整数），进入红霉素或其盐的2'-位。

    AMINOALKYLTHIAZOLE DERIVATIVE
    4.
    发明公开
    AMINOALKYLTHIAZOLE DERIVATIVE 失效
    氨基烷基噻唑衍生物

    公开(公告)号：EP0641788A1

    公开(公告)日：1995-03-08

    申请号：EP92910766.2

    申请日：1992-05-29

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： NAKAZATO, Atsuro ,  SEKIGUCHI, Yoshinori ,  KAWASHIMA, Yutaka ,  HATAYAMA, Katsuo

    IPC分类号： C07D277/40

    CPC分类号： C07D277/40

    摘要： Object to provide an antipsychotic having a mechanism of action different from that of a dopamine autoreceptor agonist, that is, an antipsychotic having a specific affinity for a sigma receptor and not causing extrapyramidal disorder. Constitution: an aminoalkylthiazole derivative represented by general formula (I) and a salt thereof, wherein R¹ represents halogenated phenyl; R² and R³ may be the same or different from each other and each represents C₄ to C₁₀ alkyl; and n represents 2 or 3.

    摘要翻译： 目的是提供具有不同于多巴胺自身受体激动剂作用机制的抗精神病药物，即对σ受体具有特异性亲和力并且不引起锥体束外疾病的抗精神病药物。 组成：由通式（Ⅰ）表示的氨烷基噻唑衍生物及其盐，其中R 1代表卤代苯基; R 2和R 3可以相同或不同，各自代表C 4至C 10烷基; 并且n代表2或3。

    ANILIDE DERIVATIVE
    5.
    发明公开
    ANILIDE DERIVATIVE 失效
    ANILINDERIVAT。

    公开(公告)号：EP0559898A1

    公开(公告)日：1993-09-15

    申请号：EP92902521.1

    申请日：1991-11-21

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： SATO, Masakazu ,  KAWASHIMA, Yutaka ,  HATAYAMA, Katsuo

    IPC分类号： C07C317/44 ,  C07C323/60 ,  C07C327/32 ,  A61K31/16 ,  A61K31/255

    CPC分类号： C07C317/44 ,  C07C323/60 ,  C07C327/32

    摘要： An anilide derivative useful for treating arteriosclerosis, represented by general formula (I), wherein X represents C₁ to C₄ alkyl or C₁ to C₄ alkoxy; Y represents hydrogen or C₁ to C₄ alkoxy; Z represents C₁ to C₄ alkyl or C₁ to C₄ alkoxy; A represents C₁ to C₄ alkylene, R represents C₆ to C₂₀ alkyl, C₂ to C₂₀ alkanoyl, or benzyl which may be substituted with C₁ to C₄ alkyl; and n represents 0, 1 or 2.

    摘要翻译： 用于治疗由通式（I）表示的动脉硬化的苯胺衍生物，其中X表示C1-C4烷基或C1-C4烷氧基; Y表示氢或C1至C4烷氧基; Z表示C1-C4烷基或C1-C4烷氧基; A表示C1至C4亚烷基，R表示C6至C20烷基，C2至C20链烷酰基或可被C1至C4烷基取代的苄基; n表示0,1或2.

    5-0-DESOSAMINYLERYTHRONOLIDE DERIVATIVE
    6.
    发明授权
    5-0-DESOSAMINYLERYTHRONOLIDE DERIVATIVE 失效
    5-0-去氧苯甲酰甲基丙烯酸酯衍生物

    公开(公告)号：EP0619319B1

    公开(公告)日：1997-03-05

    申请号：EP93900446.1

    申请日：1992-12-25

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： ASAKA, Toshifumi ,  MISAWA, Yoko ,  KASHIMURA, Masato ,  MORIMOTO, Shigeo ,  HATAYAMA, Katsuo

    IPC分类号： C07H17/08 ,  A61K31/70

    CPC分类号： C07H17/08

    摘要： A 3-carbamoylated 5-O-desosaminyl-6-O-methylerythronolide derivative represented by general formula (I) and a pharmaceutically acceptable acid addition salt thereof, which are novel macrolide antibiotics with a potent antibacterial power, wherein R?1 and R2¿ each represent hydrogen, phenyl optionally substituted by halogen, nitro or amino, alkyl optionally containing nitrogen, oxygen or sulfur, or aralkyl, or alternatively R?1 and R2¿ are combined together with the nitrogen atom to form a nitrogenous ring; Z represents oxo or hydroxyimino; V represents hydroxy; W represents hydrogen or hydroxy, or alternatively V and W are combined together to form a cyclic carbonate group or an oxazoline ring; and R represents hydrogen or acyl.

    摘要翻译： 由通式（I）表示的3-氨基甲酰基化5-O-德糖胺基-6-O-甲基赤藓糖酸内酯衍生物及其药学上可接受的酸加成盐，它们是具有强效抗菌力的新型大环内酯类抗生素，其中R 1和R 2' 各自代表氢，任选被卤素，硝基或氨基取代的苯基，任选含有氮，氧或硫的烷基或芳烷基，或者R 1和R 2与氮原子一起形成含氮环; Z代表氧代或羟基亚氨基; V代表羟基; W表示氢或羟基，或者V和W结合在一起形成环状碳酸酯基团或恶唑啉环; 和R代表氢或酰基。

    5-O-DESOSAMINYLERYTHRONOLIDE DERIVATIVE
    9.
    发明公开
    5-O-DESOSAMINYLERYTHRONOLIDE DERIVATIVE 失效
    5-O-脱氧胞嘧啶核赖脯氨酸衍生物

    公开(公告)号：EP0682038A1

    公开(公告)日：1995-11-15

    申请号：EP94904756.7

    申请日：1994-01-24

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： MISAWA, Yoko ,  ASAKA, Toshifumi ,  KASHIMURA, Masato ,  MORIMOTO, Shigeo ,  HATAYAMA, Katsuo

    IPC分类号： C07H17/08

    CPC分类号： C07H17/08

    摘要： A novel macrolide antibiotic having a potent antimicrobial activity, represented by general formula (1), which is produced by introducing a specified aryloxy or alkyloxy group into the 3-position of a 5-O-desosaminylerythronolide derivative, wherein Y represents oxygen-containing C₄-C₆ cycloalkyl, optionally substituted phenyl, glucopyranosyl, ribopyranosyl, benzyl or methyl; U represents hydrogen or acyl; Z represents oxygen or N-OR₁ wherein R₁ represents hydrogen, alkanoyl or optionally substituted benzyl; and A represents a group that forms an erythronolide which may form a cyclic carbonate group between the 11- and the 12-positions or a double bond between the 10- and 11-positions.

    摘要翻译： 一种通式（1）所示的具有有效抗微生物活性的新型大环内酯类抗生素，它是通过在5-O-去杂氨基红霉素衍生物的3位引入一个特定的芳氧基或烷氧基得到的，其中Y代表含氧C 4 任选取代的苯基，吡喃葡萄糖基，核糖吡喃糖基，苄基或甲基; U代表氢或酰基; Z代表氧或N-OR 1，其中R 1代表氢，链烷酰基或任意取代的苄基; A表示形成可在11位和12位之间形成环状碳酸酯基或10位和11位之间的双键的乙交酯（erythronolide）的基团。

    ANILIDE DERIVATIVE
    10.
    发明公开
    ANILIDE DERIVATIVE 失效
    ANILID衍。

    公开(公告)号：EP0619312A1

    公开(公告)日：1994-10-12

    申请号：EP93900418.0

    申请日：1992-12-18

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： SATO, Masakazu ,  KAWASE, Masahiro ,  MANAKA, Akira ,  KAWASHIMA, Yutaka ,  HATAYAMA, Katsuo

    IPC分类号： C07D295/08 ,  C07D213/74 ,  C07D239/42 ,  C07D295/18

    CPC分类号： C07D239/42 ,  C07D213/74 ,  C07D295/088 ,  C07D295/112 ,  C07D295/185

    摘要： To provide a compound with a potent ACAT inhibiting activity. An anilide derivative represented by general formula (I) and a salt thereof, wherein R¹ and R² may be the same or different from each other and each represents C₁-C₄ alkyl; n represents 0, 1 or 2; A represents C₁-C₁₄ alkylene or -CH₂CO-; and Ar represents phenyl or benzyl each of which may be substituted by halogen, nitro, C₁-C₄ alkyl, C₁-C₄ alkoxy, C₂-C₅ alkanoyl or trifluoromethyl, or pyridyl or pyrimidyl each of which may be substituted by halogen or trifluoromethyl.

    摘要翻译： 提供具有强效ACAT抑制活性的化合物。 由通式（I）表示的苯胺衍生物及其盐，其中R 1和R 2可以相同或不同，各自表示C1-C4烷基; n表示0,1或2; A表示C1-C14亚烷基或-CH2CO-; 并且Ar表示可被卤素，硝基，C 1 -C 4烷基，C 1 -C 4烷氧基，C 2 -C 5烷酰基或三氟甲基取代的苯基或苄基，或各自可被卤素或三氟甲基取代的吡啶基或嘧啶基。