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New tetralone derivs. - used for treating e.g. hypertension, asthma, angina, congestive heart failure, epilepsy, irritable bowel syndrome and incontinence

机译:新的四氢萘酮衍生物。 -用于治疗例如高血压,哮喘,心绞痛,充血性心力衰竭,癫痫,肠易激综合征和失禁

摘要

Tetralones of formula (I) and their salts are new. In (I) R1 and R2 are H, alkyl, hydroxy, alkoxy, formyl, alkylcarbonyl, alkylthiocarbonyl, carboxyl, alkoxycarbonyl, alkoxythiocarbonyl, alkylcarbonyloxy, alkylthiocarbonyloxy, hydroxyalkyl, mercaptoalkyl, perfluoroalkyl, nitro, amino, cyano, halo, trifluoromethoxy, ethynyl, etc.; R3 is H or alkyl; R4 is alkyl; or R3 + R4 are 2-5C polymethylene; alkyl is 1-4C alkyl; R5 is hydroxy, acetoxy or formyloxy; R6 is H; or R5 + R6 is a bond; Z is O or NR8; R7 is a gp. R9 when Z is O; or a radical R9 or C(=X)R10 when Z = NR8; R8 is H, 1-6C alkyl, 1-6C alkoxy, aryloxy, arylmethyloxy, 1-6C alkoxycarbonyloxy, arylcarbonyloxy, 1-6C alkylcarbonylamino or aryl carbonylamino; X is O, S or NCN; R9 is 3-6C cycloalkyl, 3-6C cycloalkenyl, phenyl or heteroaryl, all opt. substd. by 1 or 2 halo and/or 1-6C alkyl, 2-4C alkenylmethyl, 2-4C alkynylmethyl or R11; R10 is H, 1-6C alkyl opt. substd. by hydroxy, 1-6C alkoxy or 1-6C alkoxycarbonyl, 2-6C alkenyl, 3-6C cycloalkyl, 3-6C cycloalkenyl, and phenyl or heteroaryl opt. substd. by halo, 1-6C alkyl or R11; and R11 is 1-6C alkoxy, thioalkoxy, alkylcarbonyloxy, alkylcarbonyl, alkylthiocarbonyl or alkoxycarbonyl, hydroxy, oxo, nitro, cyano, trifluoromethyl, carboxyl, mercapto, amino (opt. substd. by 1 or 2 1-4C alkyl or aryl).
机译:式(I)的四氢萘酮及其盐是新的。在(I)中,R1和R2为H,烷基,羟基,烷氧基,甲酰基,烷基羰基,烷基硫羰基,羧基,烷氧基羰基,烷氧基硫羰基,烷基羰氧基,烷基硫羰氧基,羟烷基,巯基烷基,全氟烷基,硝基,氨基,氰基,卤素,三氟甲氧基,乙炔基,等等。; R3是H或烷基; R4是烷基;或R 3 + R 4为2-5C的聚亚甲基;或烷基是1-4C烷基; R5是羟基,乙酰氧基或甲酰氧基; R6为H;或者R5 + R6是键; Z为O或NR 8; R7是gp。当Z为O时为R9;当Z = NR8时,基团R9或C(= X)R10; R8是H,1-6C烷基,1-6C烷氧基,芳氧基,芳基甲氧基,1-6C烷氧基羰氧基,芳基羰氧基,1-6C烷基羰基氨基或芳基羰基氨基; X是O,S或NCN; R 9是3-6C环烷基,3-6C环烯基,苯基或杂芳基,全部选择。取代1或2个卤素和/或1-6C烷基,2-4C烯基甲基,2-4C炔基甲基或R 11; R 10是H,1-6C烷基。取代由羟基,1-6C烷氧基或1-6C烷氧基羰基,2-6C烯基,3-6C环烷基,3-6C环烯基和苯基或杂芳基选择。取代通过卤素,1-6C烷基或R 11; R11是1-6C烷氧基,硫代烷氧基,烷基羰氧基,烷基羰基,烷基硫羰基或烷氧基羰基,羟基,氧代,硝基,氰基,三氟甲基,羧基,巯基,氨基(优选被1或2个1-4C烷基或芳基取代)。

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