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    • 6. 发明申请
    • NEW COMPOUND AND ITS PREPARATION
    • 新化合物及其制备
    • WO1995000537A1
    • 1995-01-05
    • PCT/JP1994001042
    • 1994-06-28
    • FUJISAWA PHARMACEUTICAL CO., LTD.HEMMI, KeijiNEYA, MasahiroFUKAMI, NaokiKAYAKIRI, NatsukoTANAKA, Hirokazu
    • FUJISAWA PHARMACEUTICAL CO., LTD.
    • C07K05/08
    • C07K5/0808A61K38/00C07K5/0207C07K5/0827Y02P20/55
    • A compound of formula (1) in which R is acyl, R is lower alkyl, R is optionally substituted ar(lower)alkyl or optionally substituted heterocyclic-(lower)alkyl, R is lower alkyl or lower alkylthio(lower)alkyl, R is carboxy or protected carboxy, A is lower alkylene, Z is a group of formula (2) wherein R is hydrogen, lower alkyl, common amino-protective group or optionally substituted ar(lower)alkyl, R is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, optionally substituted heterocyclic-(lower)alkyl, optionally substituted cyclo(lower)alkyl(lower)alkyl, common amino-protective group, amino(or protected amino)(lower)alkyl, optionally substituted heterocyclic-carbonyl or cyclo(lower)alkyl, and R is optionally substituted heterocyclic(lower)alkyl, and m is an integer of 0 to 2, or pharmaceutically acceptable salts thereof, useful as endothelin antagonist.
    • 式(1)的化合物,其中R 4是酰基,R 5是低级烷基,R 6是任选取代的芳(低级)烷基或任选取代的杂环 - (低级)烷基,R 7是 是低级烷基或低级烷硫基(低级)烷基,R 8是羧基或保护的羧基,A是低级亚烷基,Z是式(2)的基团,其中R 1是氢,低级烷基,常见的氨基保护基 基团或任选取代的芳(低级)烷基,R 2是氢,低级烷基,任选取代的芳(低级)烷基,任选取代的杂环 - (低级)烷基,任选取代的环(低级)烷基 氨基(或保护的氨基)(低级)烷基,任选取代的杂环 - 羰基或环(低级)烷基,R 3是任选取代的杂环(低级)烷基,m是0至 2或其药学上可接受的盐,其可用作内皮素拮抗剂。