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    ベンズイミダゾール誘導体及びその医薬用途
    5.
    发明申请
    ベンズイミダゾール誘導体及びその医薬用途 审中-公开
    苯并咪唑衍生物及其医学用途

    公开(公告)号：WO2005063788A1

    公开(公告)日：2005-07-14

    申请号：PCT/JP2004/019290

    申请日：2004-12-16

    Applicant: キッセイ薬品工業株式会社 ,  菊地 紀彦 ,  野中 義功 ,  田谷 和也 ,  平栃 正博 ,  倉持 有 ,  伊佐治 正幸 ,  清水 和夫 ,  宮城 貴史

    Inventor： 菊地 紀彦 ,  野中 義功 ,  田谷 和也 ,  平栃 正博 ,  倉持 有 ,  伊佐治 正幸 ,  清水 和夫 ,  宮城 貴史

    IPC: C07H19/052

    CPC classification number: C07H19/052

    Abstract: The invention provides benzimidazole derivatives represented by the general formula (I) or pharmacologically acceptable salts or prodrugs thereof which exhibit inhibitory activities against sodium-dependent nucleoside transporter 2 and are efficacious against diseases caused by abnormality in plasma uric acid level: (I) (wherein n is 1 or 2; R and R are each H, halogeno, cyano, optionally substituted alkyl, optionally substituted aryl, or the like; R is H, halogeno, optionally substituted alkyl, or the like; R and R are each H, halogeno, OH, or the like; R and R are each H or OH; and R is F or OH). The compounds are useful in the prevention or treatment of gout, hyperuricemia, urolithiasis, hyperuricemic nephropathy, and so on.

    Abstract translation: 本发明提供通式（I）表示的苯并咪唑衍生物或其药理学上可接受的盐或前体药物，它们对钠依赖性核苷转运蛋白2表现出抑制活性，对抗血浆尿酸水平异常引起的疾病有效（I）（其中 n为1或2; R 1和R 2各自为H，卤代，氰基，任选取代的烷基，任选取代的芳基等; R 3为H，卤代，任选取代的烷基或 R 4和R 5各自为H，卤素，OH等; R 6和R X各自为H或OH; R Y为F或OH）。 该化合物可用于预防或治疗痛风，高尿酸血症，尿石症，高尿酸血症等。

    LYXOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS
    7.
    发明申请
    LYXOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS 审中-公开
    苯氧基苯甲酸钠作为抗病毒剂

    公开(公告)号：WO99006424A1

    公开(公告)日：1999-02-11

    申请号：PCT/US1998/015722

    申请日：1998-07-29

    IPC: A61K31/7042 ,  A61K31/7052 ,  A61K31/7056 ,  A61P31/12 ,  A61P31/22 ,  C07H19/052 ,  A61K31/70

    CPC classification number: C07H19/052 ,  Y02P20/55

    Abstract: The present invention pertains to D- and L-lyxofuranosyl benzimidazole compounds. In one embodiment, the present invention pertains to D- and L-lyxofuranosyl benzimidazole compounds selected from the group consisting of compounds having a formula selected from the following: (beta-D), (beta-L), (alpha-L) and (alpha-D) wherein R , R , R , R , and R are independently the same or different and independently selected from the group consisting of: -H, -F, -Cl, -Br, -I, -NO2, -N(R )2, -OR , -SR , and -CF3, wherein R is independently -H or an alkyl group having 1-6 carbon atoms and wherein R is independently -H or a hydrocarbyl group having 1-10 carbon atoms; and R , R and R are independently the same or different and are H or a hydroxyl protecting group; anomeric and optical isomers thereof; and pharmaceutically acceptable salts and prodrug derivatives thereof. The present invention also pertains to antiviral compositions using these compounds, methods of treating a viral infection using these compounds, and the use of these compounds in the preparation of a medicament for use in the treatment of a viral infection.

    Abstract translation: 本发明涉及D-和L-赖索呋喃基苯并咪唑化合物。 在一个实施方案中，本发明涉及选自下列化学式的化合物的D-和L-赖索呋喃基苯并咪唑化合物：（β-D），（β-L），（α-L）和 （α-D）其中R 2，R 4，R 5，R 6和R 7独立地相同或不同并且独立地选自：-H， - F，-Cl，-Br，-I，-NO 2，-N（R 8）2，-OR 8，-SR 12和-CF 3，其中R 8独立地为-H或 具有1-6个碳原子的烷基，其中R 12独立地是-H或具有1-10个碳原子的烃基; R 9，R 10和R 11独立地相同或不同，为H或羟基保护基; 其异头和旋光异构体; 及其药学上可接受的盐和前药衍生物。 本发明还涉及使用这些化合物的抗病毒组合物，使用这些化合物治疗病毒感染的方法，以及这些化合物在制备用于治疗病毒感染的药物中的用途。

    CYTOKINE RELATED TREATMENTS OF DISEASE
    8.
    发明申请
    CYTOKINE RELATED TREATMENTS OF DISEASE 审中-公开
    细胞因子相关疾病治疗

    公开(公告)号：WO98030223A1

    公开(公告)日：1998-07-16

    申请号：PCT/US1998/000634

    申请日：1998-01-13

    IPC: C07H19/167 ,  A61K31/52 ,  A61K31/522 ,  A61K31/56 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7056 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/7115 ,  A61K45/06 ,  A61P1/16 ,  A61P3/10 ,  A61P17/00 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/00 ,  A61P37/04 ,  A61P37/08 ,  A61P43/00 ,  C07H19/00 ,  C07H19/04 ,  C07H19/052 ,  C07H19/056 ,  C07H19/16 ,  C07H19/24

    CPC classification number: C07H19/16 ,  A61K31/52 ,  A61K31/522 ,  A61K31/70 ,  A61K31/7056 ,  A61K31/7076 ,  A61K31/7115 ,  A61K45/06 ,  C07H19/00 ,  C07H19/04 ,  C07H19/052 ,  C07H19/056 ,  C07H19/24

    Abstract: Nucleosides and other compounds to selectively modulate Th1 and Th2 responses relative to each other in the treatment of disease. In one aspect of the invention, administration of a nucleoside or other compound reduces the dosage at which a primary drug is administered. In another aspect of the invention, an abnormality reflected in increased response in one group of cytokines is treated by administering a nucleoside or other compound which increases response in another group of cytokines. In yet another aspect of the invention, a patient is prophylactically treated by administering a nucleoside or other compound which selectively reduces Th1 activity without significantly reducing Th2 activity. In yet another aspect of the invention, a nucleoside or other compound is administered to a patient at a dose which reduces the patient's GTP pool to a degree that selectively reduces one of the Th1 or Th2 response without significantly reducing the other response. Controlled release dosage forms are particularly contemplated to achieve that result.

    Abstract translation: 核苷和其他化合物，用于在疾病治疗中相对于彼此选择性调节Th1和Th2应答。 在本发明的一个方面，核苷或其它化合物的施用降低了施用初次药物的剂量。 在本发明的另一方面，通过施用增加另一组细胞因子中的应答的核苷或其它化合物来治疗反映在一组细胞因子中的增加的反应中的异常。 在本发明的另一方面，通过施用选择性降低Th1活性而不显着降低Th2活性的核苷或其它化合物来预防性地治疗患者。 在本发明的又一个方面中，将核苷或其它化合物以一定剂量施用于患者，其剂量可以将患者的GTP池降低至选择性降低Th1或Th2反应之一而不显着降低其他反应的程度。 特别考虑到控制释放剂型以实现该结果。

    IMIDAZO[1,2-A]PYRIDINE C-NUCLEOSIDES AS ANTIVIRAL AGENTS
    9.
    发明申请
    IMIDAZO[1,2-A]PYRIDINE C-NUCLEOSIDES AS ANTIVIRAL AGENTS 审中-公开
    咪唑并[1,2-A]吡啶C - 核苷酸作为抗病毒剂

    公开(公告)号：WO1997027205A1

    公开(公告)日：1997-07-31

    申请号：PCT/US1997001602

    申请日：1997-01-22

    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  TOWNSEND, Leroy, B. ,  DRACH, John, C.

    Inventor： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

    IPC: C07H19/052

    CPC classification number: C07D471/04 ,  C07H7/06 ,  C07H9/04 ,  C07H11/00 ,  C07H19/052

    Abstract: This invention pertains to nucleoside analogs which have antiviral activity and improved metabolic stability, compositions comprising them, and methods of antiviral treatment employing them. More particularly, this invention pertains to imidazo [1,2-a]pyridine C-nucleosides, as exemplified by compounds such imidazo[1,2-a]pyridine C5-nucleosides and imidazo[1,2-a]pyridine C3-nucleosides, and may be represented by formula (I), wherein exactly one of Q and Q is a sugar-like moiety; exactly one of Q and Q is -H; and Q , Q , Q and Q are independently imidazo[1,2-a]pyridine substituents, such as -H, -F, -Cl, -Br, and -I.

    Abstract translation: 本发明涉及具有抗病毒活性和改善的代谢稳定性的核苷类似物，包含它们的组合物以及使用它们的抗病毒治疗方法。 更具体地，本发明涉及咪唑并[1,2-a]吡啶C-核苷，例如咪唑并[1,2-a]吡啶C5-核苷和咪唑并[1,2-a]吡啶C 3 - 核苷 并且可以由式（I）表示，其中Q 3和Q 5中的仅一个是糖状部分; Q 3和Q 5中的正好一个是-H; 和Q 2，Q 6，Q 7和Q 8独立地是咪唑并[1,2-a]吡啶取代基，例如-H，-F，-Cl，-Br和-I 。

    ANTITUMOR INDOLOPYRROLOCARBAZOLES
    10.
    发明申请
    ANTITUMOR INDOLOPYRROLOCARBAZOLES 审中-公开
    抗肿瘤剂吲哚酚

    公开(公告)号：WO1996004293A1

    公开(公告)日：1996-02-15

    申请号：PCT/JP1995001490

    申请日：1995-07-26

    Applicant: BANYU PHARMACEUTICAL CO., LTD. ,  KOJIRI, Katsuhisa ,  SHIMOKAWA, Haruki ,  OHKUBO, Mitsuru ,  KAWAMURA, Kenji ,  KONDO, Hisao ,  ARAKAWA, Hiroharu ,  SUDA, Hiroyuki

    Inventor： BANYU PHARMACEUTICAL CO., LTD.

    IPC: C07H19/23

    CPC classification number: C07H19/04 ,  C07H19/052 ,  C12P19/26

    Abstract: A compound represented by general formula [1] or a pharmaceutically acceptable salt thereof, having an excellent antitumor effect, and hence being useful as an antitumor agent, wherein X and X represent each independently hydrogen, halogen, amino, mono(lower alkyl)amino, di(lower alkyl)amino, hydroxy, lower alkoxy, aralkoxy, carboxy, lower alkoxycarbonyl, lower alkanoyloxy, or lower alkyl which may be substituted by one or two hydroxy groups; R represents hydrogen, amino, formylamino, lower alkanoylamino, mono(lower alkyl)amino, di(lower alkyl)amino, hydroxy, lower alkoxy, aralkoxy, aralkyl, lower alkylcarbonyl, arylcarbonyl or lower alkyl (wherein the lower alkanoylamino, mono(lower alkyl)amino, di(lower alkyl)amino, lower alkoxy, aralkoxy, aralkyl, lower alkylcarbonyl, arylcarbonyl and lower alkyl may be substituted by one to five groups selected from among carboxy, carbamoyl, sulfo, amino, cyano, mono(lower alkyl)amino, di(lower alkyl)amino, hydroxy, heterocycle which may be substituted by one to three hydroxy groups or by lower alkyl which may be substituted by one to three hydroxy groups, and halogen atoms); and R represents a disaccharide group.

    Abstract translation: 由通式[1]表示的化合物或其药学上可接受的盐，具有优异的抗肿瘤效果，因此可用作抗肿瘤剂，其中X 1和X 2各自独立地表示氢，卤素，氨基， 单（低级烷基）氨基，二（低级烷基）氨基，羟基，低级烷氧基，芳烷氧基，羧基，低级烷氧基羰基，低级烷酰氧基或可被一个或两个羟基取代的低级烷基; R 1表示氢，氨基，甲酰氨基，低级烷酰氨基，单（低级烷基）氨基，二（低级烷基）氨基，羟基，低级烷氧基，芳烷氧基，芳烷基，低级烷基羰基，芳基羰基或低级烷基（其中低级烷酰基氨基， 单（低级烷基）氨基，二（低级烷基）氨基，低级烷氧基，芳烷氧基，芳烷基，低级烷基羰基，芳基羰基和低级烷基可以被一至五个选自羧基，氨基甲酰基，磺基，氨基，氰基， （低级烷基）氨基，二（低级烷基）氨基，羟基，可被一至三个羟基取代的杂环或被一至三个羟基取代的低级烷基和卤素原子）。 R 2表示二糖基。

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