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    MACROLIDE DERIVATIVE
    2.
    发明公开
    MACROLIDE DERIVATIVE 审中-公开
    MACROLIDE衍生物

    公开(公告)号：EP2077271A1

    公开(公告)日：2009-07-08

    申请号：EP07742762.3

    申请日：2007-05-01

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： KASHIMURA, Masato ,  KAWAMURA, Madoka ,  ASAKA, Toshifumi ,  TAKAYAMA, Kiyoshi ,  OGITA, Haruhisa

    IPC分类号： C07H17/08 ,  A61K31/7048 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00

    CPC分类号： C07H17/08 ,  A61K31/7048 ,  A61K31/7052 ,  C07H17/00

    摘要： Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

    摘要翻译： 由式（I）和式（IV）表示的化合物具有MMP-9产生的抑制活性，因此可用作副作用小于传统MMP酶活性抑制剂的药物，作为致癌的预防和治疗药物 血管生成，慢性风湿性关节炎，经皮冠状动脉腔内血管成形术后血管内膜增厚，血管动脉硬化，出血性中风，急性心肌梗塞，慢性心力衰竭，动脉瘤，肺癌转移，成人呼吸窘迫综合征，哮喘，间质性肺纤维化，慢性鼻窦炎， 支气管炎或慢性阻塞性肺病（COPD）。

    5-0-DESOSAMINYLERYTHRONOLIDE DERIVATIVE
    3.
    发明公开
    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：EP0619319A1

    公开(公告)日：1994-10-12

    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 R¹ and R² each represent hydrogen, phenyl optionally substituted by halogen, nitro or amino, alkyl optionally containing nitrogen, oxygen or sulfur, or aralkyl, or alternatively R¹ 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与氮原子结合在一起形成含氮环; 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
    5.
    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。

    5-0-DESOSAMINYLERYTHRONOLIDE DERIVATIVE
    7.
    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。

    PROCESS FOR PRODUCING ERYTHROMYCIN DERIVATIVE
    10.
    发明公开
    PROCESS FOR PRODUCING ERYTHROMYCIN DERIVATIVE 审中-公开
    生产红霉素衍生物的方法

    公开(公告)号：EP1310506A1

    公开(公告)日：2003-05-14

    申请号：EP01955675.2

    申请日：2001-08-10

    申请人： TAISHO PHARMACEUTICAL CO., LTD

    发明人： KASHIMURA, Masato ,  KAMIYAMA, Hiroaki ,  KUWADA, Takeshi ,  SUZUKI, Nobuyuki ,  ADACHI, Takashi

    IPC分类号： C07H17/08 ,  C07H1/00

    CPC分类号： C07H17/08

    摘要： There is provided a preparation process useful for an efficient synthesis of 6-O-substituted ketolide derivatives by combining a characterized step of introduction of a substituent at the 6-position by selective cleavage of a C-O bond of the cyclic acetal at the 9-position side via 6,9-cyclic acetal 5-O-desosaminyl erythronolide derivative, a step of conversion into carbonyl groups at the 9- and 3-positions, and a step of 11,12-cyclic carbamation to lead to 6-O-substituted ketolide derivatives.

    摘要翻译： 提供了一种用于有效合成6-O-取代的酮内酯衍生物的制备方法，其通过组合在6位上引入取代基的特征化步骤通过选择性裂解9-位环状缩醛的CO键 通过6,9-环缩醛5-O-德糖胺基赤藓糖酸内酯衍生物，在9位和3位转化成羰基的步骤，以及11,12-环状氨基甲酸酯化步骤以产生6-O-取代 酮内酯衍生物。