5-(substituted amino)-1,2,4-triazolo (1,5-A) pyrimidine derivatives
    4.
    发明授权
    5-(substituted amino)-1,2,4-triazolo (1,5-A) pyrimidine derivatives 失效
    5-(取代氨基)-1,2,4-三唑并(1,5-A)嘧啶衍生物

    公开(公告)号:US5478825A

    公开(公告)日:1995-12-26

    申请号:US261214

    申请日:1994-06-15

    摘要: The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.9 is alkyl substituted by alkoxy-carbonyl and possess inotropic and antianginal effects, complemented by antiinflammatory, ulcus, and gastric acid secretion inhibiting, and by weaker tranquillant, spasmolytic, and analgesic properties.

    摘要翻译: 所公开的化合物具有式“IMAGE”,其中Q为6元饱和杂环基团或S(O)pR 3基团,其中p为0,1或2,R 3为烷基,烯基或苯基,其中 可以具有卤素或硝基取代基,或任选取代的苯基; 或NR4R5,其中R4和R5是氢,烷基,烯基,苯基 - 烷基或二 - 烷基 - 氨基 - 烷基; 或者一起形成基团(CH 2)n -Y-(CH 2)m,其中Y是CH 2或NR 6,其中R 6是苯基 - 烷基,n和m是0或1至5; Z是NR7R8,其中R7和R8各自是氢,烯基,环烷基,金刚烷基或苯基 - 烷基,其可以具有一个或多个取代基或一起形成(CH 2)j W-(CH 2)k的基团,其中j和k 各自为1至3,W为氧,CH 2,CHOH或NR 10,其中R 10为氢,烷氧基羰基或烷基,后者可以被取代。 - 或SR9,其中R9是被烷氧基 - 羰基取代的烷基,并且具有各向同性和抗心绞痛作用,由抗炎,溃疡和胃酸分泌抑制以及较弱的镇静剂,解痉药和镇痛药物补充。

    Aminopropanol derivatives, process for their preparation and
pharmaceutical compositions comprising the same
    6.
    发明授权
    Aminopropanol derivatives, process for their preparation and pharmaceutical compositions comprising the same 失效
    氨基丙醇衍生物,其制备方法和包含其的药物组合物

    公开(公告)号:US5234934A

    公开(公告)日:1993-08-10

    申请号:US876091

    申请日:1992-04-30

    摘要: The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6,acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.

    摘要翻译: 本发明涉及式I的新型外消旋或光学活性氨基丙醇衍生物其中R和R 1独立地为氢原子,卤素原子,低级烷氧基或一起代表亚甲基二氧基,R2和R3一起表示化学键或 独立地代表氢原子,R4和R5独立地是氢原子,C3-7环烷基或任选被一个或多个二烷基氨基烷基,二甲氧基苯基或苯基取代的直链或支链,饱和或不饱和的C 1-12烷基,或R 4 和R5与相邻的氮原子一起形成任选地包含氧,硫或另外的氮原子的4至7元环,该环任选被苯基,苄基或C 1-3烷基取代,所述取代基可以携带 羟基,一个或两个甲氧基,卤素原子或三氟甲基,或R4和R5与相邻的氮原子一起形成哌啶环,其任选地是 由苯基或苄基构成,如果需要,它包含双键,R6代表氢原子或苯甲酰基,n代表3-6的整数,其酸加成盐和季铵衍生物。 本发明还涉及制备这些化合物的方法。 本发明的化合物发挥心脏循环控制和/或改善,中枢神经系统镇定和/或消化系统不调节改善作用。