首页> 外国专利> NOVEL 33AMINOO11BENZOXEPINN5*2H**ONE DERIVATIVE* ITS MANUFACTURE* DRUG CONTAINING IT AND ACTIVE TO GASTRIC MOVEMENT FUNCTION* NOVEL 2*3*4*55 TETRAHYDROO11BENZOXEPINN3*55DIONE DERIVATIVE AND ITS MANUFA

NOVEL 33AMINOO11BENZOXEPINN5*2H**ONE DERIVATIVE* ITS MANUFACTURE* DRUG CONTAINING IT AND ACTIVE TO GASTRIC MOVEMENT FUNCTION* NOVEL 2*3*4*55 TETRAHYDROO11BENZOXEPINN3*55DIONE DERIVATIVE AND ITS MANUFA

机译:新型33 AMINOO11BENZOXEPINN5*2H**一种衍生物*包含它的药物*并具有胃运动功能*新型2 * 3 * 4 * 55四羟基11BENZOXEPINN3 * 55DIONE衍生物及其制造

摘要

Novel, 3-amino-1-benzoxepin-5 (2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: IMAGE I wherein: R1 and R2 independently of one another are hydrogen, C1-C5 alkyl, C1-C5 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, C2-C5 alkyl substituted with terminal hydroxy or methoxy or, C3-C4 alkenyl; or one of R1 and R2 are hydrogen or a C1-C5 alkyl and the other is a C2-C5 alkyl substituted with a terminal NR5R6; R5 and R6 independently of one another are hydrogen or C1-C5 alkyl; or R5 and R6 are together a 5 to 7 member ring, or R5 and R6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen; R1 and R2 are together a 5 to 7 member ring, or R1 and R2 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or NR7; R7 is hydrogen, methyl, benzyl or phenyl; R3 and R4 independently of one another are hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy or C1-C4 alkylthio; or one of R3 and R4 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.
机译:公开了新颖的3-氨基-1-苯并氧杂-5(2H)-一衍生物及其生产方法。这些衍生物对应于式I:<图像> I其中:R1和R2彼此独立地是氢,C1-C5烷基,被末端苯基取代的C1-C5烷基,或包含一个或两个卤素,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C2-C5烷基或C3-C4烯基; R 1和R 2之一为氢或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;或R5和R6彼此独立地是氢或C1-C5烷基;或R 5和R 6一起为5至7元环,或R 5和R 6一起为5至7元环,它们具有不均匀的氧,硫或氮; R 1和R 2一起是5至7元环,或者R 1和R 2一起是5至7元环,它们具有不均匀的氧,硫或NR 7; R7是氢,甲基,苄基或苯基; R3和R4彼此独立地是氢,卤素,C1-C4烷基,C1-C4烷氧基或C1-C4烷硫基; R3和R4之一为三氟甲基或硝基,另一个为氢;或及其酸加成盐。这些化合物对胃-肠痉挛的治疗具有有利的作用,因此构成用于治疗胃和肠疾病的药物组合物和方法的活性成分。还描述了用于制备衍生物及其酸加成盐的方法以及用于其制备的中间产物。

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