Naphthyloxyacetic acid derivatives
    31.
    发明授权
    Naphthyloxyacetic acid derivatives 失效
    萘氧基乙酸衍生物

    公开(公告)号:US5753700A

    公开(公告)日:1998-05-19

    申请号:US574133

    申请日:1995-12-18

    摘要: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2, therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.

    摘要翻译: (I)的萘氧基乙酸衍生物其中R 1为H,烷基,亚烷基 - ( - COOR 10,-OH,-CONR 4 R 5,-CONR 6 - 亚烷基-OH,-NR 4 R 5 - 氰基或四唑基 ); A是单键,亚烷基,亚烯基,-S-亚烷基,-O-亚烷基; B为NR3CO,CONR3; R2是(1)烷基(2)烯基,(3)被1-3个含氮原子的苯基,环烷基,萘基和杂环取代的烷基或链烯基(所述环可以被1-3个烷基,烷氧基和 卤素等),(4)NR7R8或(5)亚烷基-NR7R8; 其无毒盐,其无毒酸加成盐和其水合物可结合PGE2受体并表现出拮抗或激动PGE2的活性,因此它们可用作PGE2拮抗剂或PGE2激动剂。