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    • 9. 发明授权
    • 1-Benzoxepin-5 (2H)-one derivatives and pharmaceutical compositions
    • 1-苯并恶庚英-5(2H) - 酮衍生物和药物组合物
    • US4279905A
    • 1981-07-21
    • US173076
    • 1980-07-28
    • Heinrich-Wilhelm OhlendorfKlaus-Ullrich WolfWilhelm Kaupmann
    • Heinrich-Wilhelm OhlendorfKlaus-Ullrich WolfWilhelm Kaupmann
    • A61K31/335A61K31/37A61P1/00A61P1/14C07D313/08
    • C07D313/08
    • Novel, 3-amino-1-benzoxepin-5 (2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.5 R.sub.6 ;R.sub.5 and R.sub.6 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.5 and R.sub.6 are together a 5 to 7 member ring, orR.sub.5 and R.sub.6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen;R.sub.1 and R.sub.2 are together a 5 to 7 member ring, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or NR.sub.7 ;R.sub.7 is hydrogen, methyl, benzyl or phenyl;R.sub.3 and R.sub.4 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; orone of R.sub.3 and R.sub.4 is trifluoromethyl or nitro and the other is hydrogen;and the acid addition salts thereof. These compounds have a favorable effect on the treatment of spasms of the stomach-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of disorders of the stomach and intestinal tract. Processes for the preparation of the derivatives and their acid addition salts and intermediate products for their preparation are also descrived.
    • 公开了3-氨基-1-苯并氧杂-5(2H) - 酮衍生物及其生产方法。 这些衍生物对应于式I:其中:R 1和R 2彼此独立地是氢,C 1 -C 5烷基,被末端苯基取代的C 1 -C 5烷基或含有一个或两个卤素的苯基,甲基或 甲氧基,3,4-亚甲二氧基或3,4-亚乙二氧基,被末端羟基或甲氧基取代的C 2 -C 5烷基或C 3 -C 4烯基; 或R 1和R 2中的一个为氢或C 1 -C 5烷基,另一个为被末端NR 5 R 6取代的C 2 -C 5烷基; R 5和R 6彼此独立地是氢或C 1 -C 5烷基; 或R 5和R 6一起为5至7元环,或者R 5和R 6一起为具有异质的氧,硫或氮的5至7元环; R 1和R 2一起为5至7元环,或者R 1和R 2一起为具有异质氧,硫或NR 7的5至7元环; R7是氢,甲基,苄基或苯基; R 3和R 4彼此独立地是氢,卤素,C 1 -C 4烷基,C 1 -C 4烷氧基或C 1 -C 4烷硫基; 或者R 3和R 4中的一个是三氟甲基或硝基,另一个是氢; 及其酸加成盐。 这些化合物对胃肠道痉挛的治疗具有有利的作用,因此构成了用于治疗胃肠道疾病的药物组合物和方法的活性成分。 还描述了制备衍生物及其酸加成盐和中间产物用于其制备的方法。