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    Thiazole Derivatives Having Vap-1 Inhibitory Activity
    1.
    发明申请
    Thiazole Derivatives Having Vap-1 Inhibitory Activity 审中-公开
    具有Vap-1抑制活性的噻唑衍生物

    公开(公告)号：US20080015202A1

    公开(公告)日：2008-01-17

    申请号：US11574946

    申请日：2005-09-08

    Applicant: Takayuki Inoue ,  Takashi Tojo ,  Masataka Morita

    Inventor： Takayuki Inoue ,  Takashi Tojo ,  Masataka Morita

    IPC: A61K31/426 ,  A61K31/445 ,  A61K31/497 ,  A61P27/02 ,  C07D411/00

    CPC classification number: C07D417/10 ,  C07D277/46 ,  C07D417/06 ,  C07D417/12

    Abstract: A compound of the formula (I): U-V-W-X-Y-Z  (I) wherein U is lower alkyl; V is —CONH— or —NR1CO— wherein R1 is a hydrogen or lower alkyl; W is a bond or lower alkylene; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond or lower alkylene; and Z is a group of the formula: wherein R2 is a group of the formula: -A-B-D-E-F-G wherein A is a bond or lower alkylene; B is a bond, —NH— or D is a bond, —CS— or —CO—; E is a bond or —NH—; F is a bond, —CO—, —O— or —SO2—; and G is lower alkyl, optionally protected amino, —OH, phenyl, R3 is lower alkyl, provided that when Z is a group of the formula: then G should not be amino, when Z is a group of the formula: then G should not be when Z is a group of the formula: and G is optionally protected amino, then D should be —CS—, or then A should be lower alkylene, B or E should be —NH— and F should be —CO—; or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor as well as a pharmaceutical composition and a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.

    Abstract translation: 式（I）的化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> UVWXYZ（I）<？in-line-formula description =“In-line Formulas” end =“tail”？>其中U是低级烷基; V是-CONH-或-NR 1 CO-，其中R 1是氢或低级烷基; W是键或低级亚烷基; X是衍生自任选取代的噻唑的二价残基; Y是键或低级亚烷基; 并且Z是下式的基团：其中R 2是下列基团：-A-B-D-E-F-G其中A是键或低级亚烷基; B是键，-NH-或D是键，-CS-或-CO-; E是键或-NH-; F是键，-CO - ， - O-或-SO 2 - 。 并且G为低级烷基，任意保护的氨基，-OH，苯基，R 3为低级烷基，条件是当Z为下式基团时，则G不应为氨基，当Z为 组式为：那么G不应该是当Z是下式的基团时：G是任意保护的氨基，那么D应该是-CS-，或者A应该是低级亚烷基，B或E应该是-NH- 而F应为-CO-; 或其药学上可接受的盐可用作血管粘附蛋白-1（VAP-1）抑制剂，以及用于预防或治疗VAP-1相关疾病，特别是黄斑水肿的药物组合物和方法，该方法包括施用有效的 化合物或其药学上可接受的盐对受试者的量等。

    New compound
    7.
    发明申请
    New compound 审中-公开
    新化合物

    公开(公告)号：US20050004014A1

    公开(公告)日：2005-01-06

    申请号：US10860508

    申请日：2004-06-04

    Applicant: Takahiro Matsuya ,  Hiroaki Mizuno ,  Takashi Tojo ,  Hiroshi Matsuda ,  David Barrett

    Inventor： Takahiro Matsuya ,  Hiroaki Mizuno ,  Takashi Tojo ,  Hiroshi Matsuda ,  David Barrett

    IPC: A61K38/00 ,  C07K7/56 ,  A61K38/12 ,  C07K7/64

    CPC classification number: C07K7/56 ,  A61K38/00

    Abstract: This invention relates to new lipopeptide compound represented by the following general formula (I): wherein R1, R2, R3, R4 and R5 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.

    Abstract translation: 本发明涉及由以下通式（I）表示的新的脂肽化合物：其中R 1，R 2，R 3，R 4和R 5如说明书中所定义或 其具有抗微生物活性（特别是抗真菌活性），对β-1,3-葡聚糖合酶的抑制活性，其制备方法，包含其的药物组合物，以及预防和/或治疗方法 的感染性疾病，包括人或动物中的卡氏肺囊虫感染（例如肺孢子虫肺炎）。

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