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    • 1. 发明申请
    • THIAZOLE DERIVATIVES HAVING VAP-1 INHIBITORY ACTIVITY
    • 具有VAP-1抑制活性的噻唑衍生物
    • WO2006028269A2
    • 2006-03-16
    • PCT/JP2005/016984
    • 2005-09-08
    • Astellas Pharma Inc.INOUE, TakayukiTOJO, TakashiMORITA, Masataka
    • INOUE, TakayukiTOJO, TakashiMORITA, Masataka
    • C07D417/06A61K31/427A61P27/02C07D277/46A61K31/426C07D417/10C07D417/12
    • C07D417/10C07D277/46C07D417/06C07D417/12
    • A compound of the formula (I): U-V-W-X-Y-Z (I) wherein U is lower alkyl; V is -CONH- or -NR 1 CO- wherein R 1 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: or wherein R 2 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 -SO 2 -; and G is lower alkyl, optionally protected amino, -OH, phenyl, or ; and R 3 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.
    • 式(I)的化合物:U-V-W-X-Y-Z(I)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:或其中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是一个键,-NH-或; D是键,-CS-或-CO-; E是键或-NH-; F是键,-CO - , - O-或-SO 2 - 。 且G为低级烷基,任选保护的氨基,-OH,苯基或 并且R 3为低级烷基,条件是当Z为下式基团时,则当Z为下式基团时,G不应为氨基,则G不应为 Z是下式的基团:G是任选保护的氨基,则D应为-CS-,或者A应为低级亚烷基,B或E应为-NH-,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。
    • 8. 发明申请
    • THIAZOLE DERIVATIVES HAVING VAP-1 IHIBITORY ACTIVITY
    • 具有VAP-1 IHIBITORY活性的噻唑衍生物
    • WO2006028269A3
    • 2006-06-29
    • PCT/JP2005016984
    • 2005-09-08
    • ASTELLAS PHARMA INCINOUE TAKAYUKITOJO TAKASHIMORITA MASATAKA
    • INOUE TAKAYUKITOJO TAKASHIMORITA MASATAKA
    • C07D417/06A61K31/426A61K31/427A61P27/02C07D277/46C07D417/10C07D417/12
    • C07D417/10C07D277/46C07D417/06C07D417/12
    • A compound of the formula (I): U-V-W-X-Y-Z (I) wherein U is lower alkyl; V is -CONH- or -NR 1 CO- wherein R 1 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: (a) wherein R 2 is a group of the formula: -A-B-D-E-F-G wherein A is a bond or lower alkylene; B is a bond, (b); D is a bond, -CS- or -CO-; E is a bond or -NH-; F is a bond, -CO-, -O- or -SO 2 -; and G is lower alkyl, optionally protected amino, -OH, phenyl, (c); and R 3 is lower alkyl, provided that when Z is a group of the formula: (d), then G should not be amino, when Z is a group of the formula: (e), then G should not be (f), when Z is a group of the formula: (g) 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.
    • 式(I)的化合物:U-V-W-X-Y-Z(I)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:(a)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是债券,(b); D是键,-CS-或-CO-; E是键或-NH-; F是键,-CO - , - O-或-SO 2 - 。 和G是低级烷基,任选保护的氨基,-OH,苯基,(c); 并且R 3为低级烷基,条件是当Z为式(d)的基团时,则当Z为下列基团时,G不应为氨基,则 G不应该是(f),当Z是下列基团时:(g)和G是任选保护的氨基,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 - 和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。