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COMBINATIONS INCLUDING SEFR RECEPTOR INHIBITOR (VASCULAR ENDOTHELIAL GROWTH FACTOR) AND AGENT INCREASING PERMEABILITY

机译:包括SEFR受体抑制剂(血管内皮生长因子)和增加通透性的组合

摘要

1. A composition comprising an inhibitor of a VEGF receptor (vascular endothelial growth factor) and an agent that increases permeability. ! 2. The composition according to claim 1, in which the inhibitor of the VEGF receptor is a compound of the formula! ! wherein ! R1 is H; halogen; - (C0-C7) -R3; - (C0-C7) -NR4R5; or -C (= O) -R6; ! R2 is substituted (C3-C8) cycloalkyl; substituted aryl; or substituted heterocyclyl; ! R3 is H or unsubstituted or substituted (C1-C4) alkyl; ! R4 and R5 are independently selected from the group consisting of H; unsubstituted or substituted (C1-C4) alkyl; (C1-C4) alkylcarbonyl in which the (C1-C4) alkyl moiety is optionally substituted; and (C1-C4) alkoxycarbonyl in which the (C1-C4) alkyl moiety is optionally substituted; R6 is H; unsubstituted or substituted (C1-C4) alkyl; A (C1-C4) alkoxy group in which the (C1-C4) alkyl moiety is optionally substituted; or an unsubstituted, mono- or disubstituted amino group; ! A, B and X are independently selected from the group consisting of = C (R7) - and N; ! E, G and T are independently selected from the group consisting of = C (R8) - and N; ! R7 and R8 are independently selected from the group consisting of H, halogen, and unsubstituted or substituted (C1-C4) alkyl; ! Y is —O—, —S—, —S (O) -, —S (O) 2-, —CH 2 - or —CH 2 —CH 2 -; ! Z is CH or N and Q is (C1-C4) alkylene or (C2-C4) alkenylene in which (C1-C4) alkylene or (C2-C4) alkenylene may optionally be substituted and in which one or more carbon atoms said (C1-C4) alkylene or (C2-C4) alkenylene chain may optionally be replaced with a heteroatom independently selected from the group consisting of nitrogen, oxygen and sulfur; and the relationship between Q and Z, shown by a dashed line, is an ordinary relationship; provided that,
机译:1.一种组合物,其包含VEGF受体的抑制剂(血管内皮生长因子)和增加通透性的试剂。 ! 2.根据权利要求1的组合物,其中所述VEGF受体的抑制剂是下式的化合物: !其中! R1是H;卤素; -(C0-C7)-R3; -(C0-C7)-NR4R5;或-C(= O)-R6; ! R2是取代的(C3-C8)环烷基;取代的芳基;或取代的杂环基; ! R3是H或未取代或取代的(C1-C4)烷基; ! R4和R5独立地选自由H组成的组;未取代的或取代的(C1-C4)烷基; (C1-C4)烷基羰基,其中(C1-C4)烷基部分任选被取代; (C1-C4)烷氧基羰基,其中(C1-C4)烷基部分被任选取代; R6为H;未取代的或取代的(C1-C4)烷基; (C1-C4)烷氧基,其中(C1-C4)烷基部分被任选取代;或未取代的,单取代或二取代的氨基; ! A,B和X独立地选自= C(R7)-和N; ! E,G和T独立地选自= C(R8)-和N; ! R7和R8独立地选自H,卤素和未取代或取代的(C1-C4)烷基; ! Y为-O-,-S-,-S(O)-,-S(O)2-,-CH 2-或-CH 2 -CH 2-; ! Z是CH或N,Q是(C1-C4)亚烷基或(C2-C4)亚烯基,其中(C1-C4)亚烷基或(C2-C4)亚烯基可以任选被取代,并且其中一个或多个碳原子表示( C1-C4)亚烷基或(C2-C4)亚烯基链可以任选地被杂原子取代,所述杂原子独立地选自氮,氧和硫;用虚线表示的Q和Z之间的关系是普通关系;前提是

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