Indol-2-one derivatives
    11.
    发明授权
    Indol-2-one derivatives 失效
    吲哚-2-酮衍生物

    公开(公告)号:US5773612A

    公开(公告)日:1998-06-30

    申请号:US640080

    申请日:1996-04-30

    摘要: A compound of formula II' ##STR1## in which R.sub.I is an ethoxy group or a chlorine atom; R.sub.II is hydrogen, a chlorine atom or a methyl group; R.sub.III is a chlorophenyl group or a methoxyphenyl group; R.sub.IV is an amino group, a group NR.sub.9 R.sub.10 or NR.sub.9 R.sub.XI, or a piperazin-1-yl radical substituted in the 4-position by a (C.sub.2 -C.sub.10)alkylene group substituted by an amino group which is free or carries a protective group; R.sub.10 is (CH.sub.2).sub.p R.sub.35 or a (C.sub.2 -C.sub.10)alkylene group substituted by R.sub.21 ; R.sub.XI is a (C.sub.1 -C.sub.12)alkyl group or a group .omega.-R.sub.32 R.sub.33 N(C.sub.1 -C.sub.4)-alkylcarbonyl; and R.sub.21 is R.sub.36 ; a group OR.sub.37 ; a group NR.sub.32 R.sub.33 ; a cyano group; a group S(C.sub.1 -C.sub.7)alkyl; a group SO(C.sub.1 -C.sub.7)alkyl; or a group SO.sub.2 (C.sub.1 -C.sub.7)alkyl; R.sub.35 is a piperid-4-yl group which is unsubstituted or substituted in the 1-position by a (C.sub.1 -C.sub.7)alkoxycarbonyl group or by a (C.sub.1 -C.sub.7)alkyl group; or a pyrid-2-yl group; R.sub.37 is R.sub.13 ; a (C.sub.3 -C.sub.7)cycloalkyl group; a (C.sub.1 -C.sub.6)alkylene group substituted by R.sub.24 ; a (C.sub.2 -C.sub.6)alkylene group substituted by a hydroxyl or a (C.sub.1 -C.sub.7)alkoxy group; or a (C.sub.2 -C.sub.6)alkylene group substituted by an amino group which is free or substituted by one or two (C.sub.1 -C.sub.7)alkyl groups or by a protective group; R.sub.24 is a carboxyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl group; a benzyloxycarbonyl group; or a carbamoyl group which is free or substituted by one or two (C.sub.1 -C.sub.7)alkyl groups.

    摘要翻译: 其中RI是乙氧基或氯原子的式II'化合物(II'); RII是氢,氯原子或甲基; RIII是氯苯基或甲氧基苯基; RIV是被无取代或携带保护基团的氨基取代的(C2-C10)亚烷基在4-位取代的氨基,NR9R10或NR9RXI基团或哌嗪-1-基; R 10为被R 21取代的(CH 2)p R 35或(C 2 -C 10)亚烷基; RXI是(C 1 -C 12)烷基或ω-R 32 R 33 N(C 1 -C 4) - 烷基羰基; R21为R36; 一组OR37; 一组NR32R33; 氰基; S(C 1 -C 7)烷基; SO(C 1 -C 7)烷基; 或基团SO 2(C 1 -C 7)烷基; R35是未被取代的或被(C1-C7)烷氧基羰基或(C1-C7)烷基取代在1位的哌啶-4-基; 或吡啶-2-基; R37是R13; (C 3 -C 7)环烷基; 被R24取代的(C1-C6)亚烷基; 被羟基或(C 1 -C 7)烷氧基取代的(C 2 -C 6)亚烷基; 或被一个或两个(C 1 -C 7)烷基或保护基取代的氨基取代的(C 2 -C 6)亚烷基; R24是羧基; (C1-C7)烷氧基羰基; 苄氧基羰基; 或不含或被一个或两个(C 1 -C 7)烷基取代的氨基甲酰基。

    4-amidino pyrano (3,2-c) pyridine derivatives, and pharmaceutical
compositions containing them
    15.
    发明授权
    4-amidino pyrano (3,2-c) pyridine derivatives, and pharmaceutical compositions containing them 失效
    4-脒基吡喃并(3,2-c)吡啶衍生物,以及含有它们的药物组合物

    公开(公告)号:US5185345A

    公开(公告)日:1993-02-09

    申请号:US850994

    申请日:1992-03-12

    CPC分类号: C07D405/04 C07D491/04

    摘要: The present invention deals with 4-amidino chroman and 4-amidino pyrano (3,2-c) pyridine derivatives, a process for their preparation and pharmaceutical compositions containing them. Said derivatives have antihypertensive and antiarythmic activities. They respond to formula ##STR1## in which: A+B.dbd.--CH.dbd.CH--CH.dbd.N-- ou --CH.dbd.CR.sub.4 --CR.sub.5 .dbd.CH--; X.dbd.N,N.fwdarw.O, C--Z;R.sub.1 .dbd.H, CN, NO.sub.2, C.sub.1 -C.sub.4, alkyl, OH, C.sub.1 -C.sub.4 alkoxy, CF.sub.3 CO--, CH.sub.3 --SO.sub.2 --, .rho.--SO.sub.2 --;R.sub.2 .dbd.H;R.sub.3 .dbd.OH ou OCOCH.sub.3 ou R.sub.2 +R.sub.3 .dbd.double bond.

    摘要翻译: 本发明涉及4-脒基色满和4-脒基吡喃(3,2-c)吡啶衍生物,其制备方法和含有它们的药物组合物。 所述衍生物具有抗高血压和抗血栓活性。 它们响应式(I)其中:A + B = -CH = CH-CH = N-O -CH = CR4-CR5 = CH-; X = N,N-> O,C-Z; R1 = H,CN,NO2,C1-C4,烷基,OH,C1-C4烷氧基,CF3CO-,CH3-SO2-, R2 = H; R3 = OH o OCOCH3 ou R2 + R3 =双键。