Aminoalkoxyphenyl derivatives, process of preparation and compositions
containing the same
    17.
    发明授权
    Aminoalkoxyphenyl derivatives, process of preparation and compositions containing the same 失效
    氨基烷氧基苯基衍生物,制备方法和含有它们的组合物

    公开(公告)号:US5215988A

    公开(公告)日:1993-06-01

    申请号:US745268

    申请日:1991-08-14

    摘要: The present invention relates to aminoalkoxyphenyl compounds of formula: ##STR1## in which: B is selected from --S--, --SO-- and --SO.sub.2 --,R.sub.1 and R.sub.2, which are identical or different, are selected from hydrogen, methyl, ethyl and halogen,A is selected from a straight- or branched-alkylene radical having from 2 to 5 carbon atoms, a 2-hydroxypropylene radical, and a 2-(lower alkoxy) propylene radical,R.sub.3 is selected from C.sub.1 -C.sub.8 alkyl and a radical of formula:--Alk--Ar in which Alk is selected from a single bond and a linear- or branched-alkylene radical having from 1 to 5 carbon atoms; and Ar is selected from pyridyl, phenyl, 2-3-methyleneoxyphenyl, 3,4-methylenedioxyphenyl and phenyl substituted with one or more substituents, which may be identical or different, selected from halogen atoms, C.sub.1 -C.sub.8 alkyl groups and C.sub.1 -C.sub.8 alkoxy groups,R.sub.4 is selected from hydrogen and C.sub.1 -C.sub.8 alkyl, orR.sub.3 and R.sub.4, when taken together, denote a 1,4-tetra-methylene, 1,5-pentamethylene, 3-oxa-1,5-pentamethylene, 3-aza-1,5-pentamethylene, 3-methylaza-1,5-pentamethylene, 3-phenylaza-1,5-pentamethylene or --CH.dbd.CH--N.dbd.CH-- radical,R is selected from hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.6, cycloalkyl, benzyl, phenyl optionally substituted with one or more substituents, which may be identical or different, selected from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy as well as a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及下式的氨基烷氧基苯基化合物:其中:B选自-S-,-SO-和-SO 2 - ,R 1和R 2相同或不同,选自氢,甲基,乙基 和卤素,A选自具有2至5个碳原子的直链或支链亚烷基,2-羟基亚丙基和2-(低级烷氧基)丙烯基,R 3选自C 1 -C 8烷基和 其中Alk选自单键和具有1至5个碳原子的直链或支链亚烷基的式:-Alk-Ar的基团; 并且Ar选自吡啶基,苯基,2-3亚甲基氧基苯基,3,4-亚甲二氧基苯基和被一个或多个可以相同或不同的取代基取代的苯基,其可以选自卤素原子,C 1 -C 8烷基和C 1 -C 8 烷氧基,R 4选自氢和C 1 -C 8烷基,或者R 3和R 4一起表示1,4-四亚甲基,1,5-亚戊基,3-氧杂-1,5-五亚甲基,3 1-氮杂-1,5-五亚甲基,3-甲基-1,5-五亚甲基,3-苯基氮杂-1,5-五亚甲基或-CH = CH-N = CH-基,R选自氢,C 1 -C 8烷基 C 3 -C 6,环烷基,苄基,任选被一个或多个选自卤素,C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的苯基以及其药学上可接受的盐。

    4-amidino pyrano (3,2-c) pyridine derivatives, and pharmaceutical
compositions containing them
    18.
    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。

    Use of a statin derivative in the treatment of eye complaints
    19.
    发明授权
    Use of a statin derivative in the treatment of eye complaints 失效
    用于治疗眼睛疾病的染色体衍生物的使用

    公开(公告)号:US5134124A

    公开(公告)日:1992-07-28

    申请号:US532652

    申请日:1990-06-04

    摘要: The invention relates to the use of N-(3-pyridylpropionyl)phenylalanylhistidyl (cyclohexyl)statyl-N-(1,3-dihydroxy-2-methylpropyl)isoleucinamide, which has the formula ##STR1## in which: Phe is the (L)-phenylalanine residue, His is the (L)-histidine residue, Ile is the (L)-isoleucine residue and (cyclohexyl)Sta is the cyclohexylstatin residue, i.e. the (3S, 4S)-4-amino-5-cyclohexyl-3-hydroxypentanoic acid residue, for the preparation of drugs useful in the treatment of eye complaints. Application: treatment of eye complaints.

    摘要翻译: 本发明涉及N-(3-吡啶基丙酰基)苯丙氨酰组氨酰基(环己基)异丙基-N-(1,3-二羟基-2-甲基丙基)异亮氨酰胺,其具有式N-3-(吡啶-3-基) 丙酰基PheHis-(I)其中:Phe是(L) - 苯丙氨酸残基,His是(L) - 组氨酸残基,Ile是(L) - 异亮氨酸残基和(环己基)Sta是环己基 残基,即(3S,4S)-4-氨基-5-环己基-3-羟基戊酸残基,用于制备用于治疗眼睛投诉的药物。 申请:治疗眼睛投诉。