Arylalkoxythiocoumarins, the preparation thereof and therapeutic
compositions containing these
    5.
    发明授权
    Arylalkoxythiocoumarins, the preparation thereof and therapeutic compositions containing these 失效
    芳基烷氧基硫香环素,其制备方法和含有它们的治疗组合物

    公开(公告)号:US5414006A

    公开(公告)日:1995-05-09

    申请号:US136033

    申请日:1993-10-14

    摘要: Arylalkoxythiocoumarins of the formula ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, C.sub.1 -C.sub.5 -alkyl, trifluoromethyl, phenyl or halogen, or together are a C.sub.3 -C.sub.5 -alkylene chain, andX is oxygen or sulfur,R.sup.3 is C.sub.1 -C.sub.5 -alkyl or halogen,n is an integer from 0 to 3,R.sup.4 is hydrogen or C.sub.1 -C.sub.4 -alkyl andAr is phenyl, which can be mono- or disubstituted by halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.6 -alkoxy, nitro, cyano, trifluoromethyl or a combination of these substituents or is a heteraromatic ring which has from one to three heteroatoms which can, independently of one another, be N, O or S, and which can be substituted by C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.4 -alkoxy-substituted C.sub.1 -C.sub.6 -alkyl, 5-6-membered oxacycloalkyl, benzyl, C.sub.1 -C.sub.5 -alkoxycarbonyl, perfluoro-C.sub.1 -C.sub.2 -alkyl, phenyl or halogen, are prepared as described and used in therapeutic compositions, especially for treating disorders of the central nervous system.

    摘要翻译: 其中R 1和R 2各自独立地为氢,C 1 -C 5 - 烷基,三氟甲基,苯基或卤素,或一起为C 3 -C 5 - 亚烷基链,并且X为氧或芳基烷氧基, 硫,R3是C1-C5-烷基或卤素,n是0-3的整数,R4是氢或C1-C4-烷基,Ar是可以被卤素单 - 或二取代的苯基,C1-C6-烷基 C 3 -C 7 - 环烷基,C 1 -C 6 - 烷氧基,硝基,氰基,三氟甲基或这些取代基的组合,或者是具有1至3个杂原子的杂芳环,它们可以彼此独立地为N,O或S 可以被C 1 -C 6 - 烷基,C 3 -C 7 - 环烷基,C 1 -C 6 - 烷氧基,C 1 -C 4 - 烷氧基取代的C 1 -C 6 - 烷基,5-6元氧杂环烷基,苄基,C 1 -C 5 - 烷氧基羰基,全氟-C 1 - C 2 - 烷基,苯基或卤素,如治疗组合物中所述和使用,特别是用于治疗中枢神经系统疾病。

    Arylalkoxycoumarins
    8.
    发明授权
    Arylalkoxycoumarins 失效
    ARYLALKOXYCOUMARINS

    公开(公告)号:US5100914A

    公开(公告)日:1992-03-31

    申请号:US414307

    申请日:1989-09-29

    CPC分类号: C07D311/16

    摘要: Arylalkoxycoumarins of the general formula I ##STR1## where R.sup.1 and R.sup.2 independently of one another are each hydrogen, lower alkyl, phenyl or halogen, or the two radicals together form an alkylene bridge of 3 to 5 carbon atoms, R.sup.3 is lower alkyl or halogen, n is an integer of from 0 to 3, m is an integer of from 0 to 4, R.sup.4 is hydrogen or lower alkyl and Ar is a phenyl ring which is monosubstituted to trisubstituted by halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy or monosubstituted by nitro, cyano or trifluoromethyl or is a naphthyl ring, with the proviso that m is not 0 when Ar is unsubstituted phenyl, processes for their preparation, and drugs prepared therefrom.

    摘要翻译: 其中R 1和R 2彼此独立地为氢,低级烷基,苯基或卤素,或两个基团一起形成3至5个碳原子的亚烷基桥,R 3为低级烷基或 卤素,n为0〜3的整数,m为0〜4的整数,R4为氢或低级烷基,Ar为被卤素,C1-C6烷基或C1-C6烷基单取代为三取代的苯基环, C6烷氧基或被硝基,氰基或三氟甲基单取代或是萘环,条件是当Ar是未取代的苯基时m不为0,制备方法及由其制备的药物。

    Aminoalkyl-substituted 2-aminothiazoles and therapeutic agents
containing them
    9.
    发明授权
    Aminoalkyl-substituted 2-aminothiazoles and therapeutic agents containing them 失效
    氨基取代的2-氨基丁酸和含有它们的治疗剂

    公开(公告)号:US5071864A

    公开(公告)日:1991-12-10

    申请号:US544900

    申请日:1990-06-28

    摘要: Aminoalkyl-substituted 2-aminothiazole derivatives of the general formula I ##STR1## where R.sup.1 and R.sup.2, which may be identical or different, are each hydrogen, C.sub.1 -C.sub.5 -alkyl, phenyl or C.sub.1 -C.sub.5 -alkanoyl, R.sup.3 is C.sub.1 -C.sub.5 -alkyl, phenyl which is unsubstituted or monosubstituted by halogen, C.sub.1 -C.sub.5 -alkyl or C.sub.1 -C.sub.5 -alkoxy, or thienyl,n is an integer of from 2 to 6, andNR.sup.4 R.sup.5 is one of the groups a, b, c or d ##STR2## where Ar is a phenyl ring which is unsubstituted or monosubstituted by C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, halogen, hydroxyl, nitro or trifluoromethyl, or is pyridyl, pyrimidinyl or thienyl, R.sup.5 is H or C.sub.1 -C.sub.5 -alkyl and R.sup.7 is phenyl which is unsubstituted or monosubstituted by C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, halogen, hydroxyl or trifluoromethyl, or R.sup.7 is thienyl, with the proviso that R.sup.3 is C.sub.1 -C.sub.5 alkyl only when either R.sup.1 and R.sup.2 are not both simultaneously H or when NR.sup.4 R.sup.5 is the group d, and their salts with physiologically tolerated acids, their preparation, their use for the preparation of a drug, and the drugs.

    摘要翻译: 通式I的氨基烷基取代的2-氨基噻唑衍生物其中R 1和R 2可以相同或不同,各自为氢,C 1 -C 5 - 烷基,苯基或C 1 -C 5 - 烷酰基,R 3为C1- C 5 - 烷基,未被卤素,C 1 -C 5 - 烷基或C 1 -C 5 - 烷氧基或噻吩基单取代的苯基,n为2至6的整数,并且NR 4 R 5为a,b,c之一 或者其中Ar是未被取代或被C 1 -C 5 - 烷基,C 1 -C 5 - 烷氧基,卤素,羟基,硝基或三氟甲基单取代的苯环,或者是吡啶基,嘧啶基或噻吩基,R 5是 H或C1-C5-烷基,R7是未被取代或被C1-C5-烷基,C1-C5-烷氧基,卤素,羟基或三氟甲基单取代的苯基,或R7是噻吩基,条件是R3仅为C1-C5烷基 当R 1和R 2不同时为H时,或当NR4R5为基团d时,及其与生理上耐受的酸的盐,其制备方法,其用于制备药物的用途, 和药物。