首页>
外国专利>
8-(omega,omega-diphenylalkenyl)-4-hydroxy-4-methyl-2-oxo-1-oxa-3,8-diazaspiro 4,5 decane derivatives,their preparation and pharmaceutical compositions containing them
8-(omega,omega-diphenylalkenyl)-4-hydroxy-4-methyl-2-oxo-1-oxa-3,8-diazaspiro 4,5 decane derivatives,their preparation and pharmaceutical compositions containing them
4,4-disubstd piperidine derivs of formula (I) and their acid addn and quaternary ammonium salts are new. In (I) R1 = H or C0NHR; R = H, 1-12C alkyl, 3-6C cycloalkyl or a carboxyclic 6-10C aryl or carbocycline (6-10C aryl) 1-4C alkyl opt ring substd by one or more halo, 1-4C alkyl or 1-4C alkoxy; R2 = ethynyl or C0CH3; Ph1 and Ph2 = phenyl opt substd by one or more halo, 1-4C alkyl, 1-4C alkoxy, trihalo or 0H opt esterified by a 1-4C alkansic acid; n = 1-2. - 3 Cpds (I) ie 1-(3,3-bis(4-fluorophenyl)-2-propenyl)-4 ethynyl-4-hydroxypiperidine hydrochloride, (Ib) 1-(4,4-bis(4-fluorophenyl)-3- butenyl)-4-ethynyl-4-hydroxy piperidine hydrochloride (Ia) and 1-(4,4-bis(4-fluorophenyl)-3- butenyl)-4-benzylcarbamoyloxy-4 ethynylpiperidine are specifically claimed.
展开▼
机译:式(I)的4,4-二取代哌啶衍生物及其酸加成盐和季铵盐是新的。在(I)中,R1 = H或C0NHR; R = H,1-12C烷基,3-6C环烷基或羧基的6-10C芳基或碳环素(6-10C芳基)1-4C烷基opt环,该环由一个或多个卤素,1-4C烷基或1-4C烷氧基取代; R2 =乙炔基或CO3; Ph1和Ph2 =苯基被一个或多个卤素,1-4C烷基,1-4C烷氧基,三卤或0H取代,并被1-4C链烷酸酯化; n = 1-2。 -3 Cpds(I),即1-(3,3-双(4-氟苯基)-2-丙烯基)-4乙炔基-4-羟基哌啶盐酸盐,(Ib)1-(4,4-双(4-氟苯基)特别要求保护的是-3-丁烯基)-4-乙炔基-4-羟基哌啶盐酸盐(Ia)和1-(4,4-双(4-氟苯基)-3-丁烯基)-4-苄基氨甲酰氧基-4乙炔基哌啶。
展开▼