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    Substituted ureas
    5.
    发明授权
    Substituted ureas 有权
    取代尿素

    公开(公告)号：US06620832B2

    公开(公告)日：2003-09-16

    申请号：US10002747

    申请日：2001-11-02

    申请人： Paul Robert Eastwood

    发明人： Paul Robert Eastwood

    IPC分类号： A61K3140

    CPC分类号： C07D401/12 ,  C07D209/08

    摘要： The invention is directed to physiologically active compounds of general formula (I): wherein R1 is lower alkyl, R2 is aryl, arylalkyl, heteroaryl or heteroarylalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a cyclic amine, Ar1 is aryldiyl or heteroaryldiyl, Ar2 is optionally substituted phenylene or heteroaryldiyl, L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z1)—NR4—, —NR4—C(═Z1)—, —Z1—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z1)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—, —NR4—C(═O)—O— or —O—C(═O)—NR4—, L2 is a direct bond, an optionally substituted alkylene, alkenylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or aryldiyl linkage, a —[C(═O)—N(R9)—C(R4)(R10)]p— linkage, a —Z3—R11— linkage, a —C(═O)—CH2—C(═O)— linkage or a —R11—Z3—R11— linkage, and Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

    摘要翻译： 本发明涉及通式（I）的生理活性化合物：其中R 1是低级烷基，R 2是芳基，芳烷基，杂芳基或杂芳基烷基，或者R 1和R 2与它们所连接的氮原子一起形成环状胺， Ar 1是芳基或杂芳基二，Ar 2是任选取代的亚苯基或杂芳基二基，L1是一个-R5-R6-键，其中R5是亚烷基，亚烯基或亚炔基，R6是直接键，亚环烷基，亚杂环亚烷基，亚芳基，杂芳基二基，-C（ = Z1）-NR4-，-NR4-C（= Z1） - ，-Z1，-C（= O） - ， - （= NOR4） - ，-NR4-，-NR4-C（= NR4-，-SO2-NR4-，-NR4-SO2-，-OC（= O） - ， - C（= O）-O-，-NR4-C（= O）-O-或-OC ） - NR 4 - ，L 2是直接键，任选取代的亚烷基，亚烯基，亚炔基，亚环烯基，亚环烷基，杂芳基二基，杂环亚烷基或芳基二键，a- [C（= O）-N（R 9）-C（R 4） R 10）] p键，-Z 3 -R 11键，-C（= O）-CH 2 -C（= O） - 键或-R 11 -Z 3 -R 11键，Y是羧基或酸 生物电子 和相应的N-氧化物及其前药; 和这些化合物的药学上可接受的盐和溶剂合物（例如水合物）及其N-氧化物和前药。这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1 ）。