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    • 5. 发明授权
    • Arylalkoxythiocoumarins, the preparation thereof and therapeutic
compositions containing these
    • 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
    • US5414006A
    • 1995-05-09
    • US136033
    • 1993-10-14
    • Beatrice Rendenbach-MuellerUlrich KarlHarald Weifenbach
    • Beatrice Rendenbach-MuellerUlrich KarlHarald Weifenbach
    • C07D311/16C07D405/12C07D409/12C07D413/12C07D413/14C07D417/12A61K31/37
    • C07D405/12C07D311/16C07D409/12C07D413/12C07D413/14C07D417/12
    • 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.
    • 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。
    • 9. 发明授权
    • Aminoalkyl-substituted 2-aminothiazoles and therapeutic agents
containing them
    • 氨基取代的2-氨基丁酸和含有它们的治疗剂
    • US5071864A
    • 1991-12-10
    • US544900
    • 1990-06-28
    • Beatrice Rendenbach-MuellerLiliane UngerHans-Juergen Teschendorf
    • Beatrice Rendenbach-MuellerLiliane UngerHans-Juergen Teschendorf
    • C07D277/20A61K31/44A61K31/445A61K31/495A61K31/505A61P25/00A61P43/00C07D277/38C07D277/40C07D277/42C07D277/46C07D417/00C07D417/06C07D417/12C07D417/14
    • C07D417/06C07D277/40C07D277/42C07D417/12
    • 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.
    • 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。