| 摘要 |
4-(AROYLAMINO)PIPERIDINEBUTANAMIDE DERIVATIVES A method of treating warm-blooded animals suffering from diarrhea, which method comprises the administration of particular 4-(aroylamino)piperidinebutanamide derivatives and compositions containing the same. The novel 4 (aroylamino)piperidinebutanamide derivatives have the general formula (I) . wherein R1 is a member selected from the group consisting of hydrogen,C1-6alkyl, arylC1-6alkyl, C1-6alkylcarbonyl, aminoC1-6alkyl and mono- and di(C1-6alkyl)aminoC1-6alkyl; R2 is a member selected from the group consisting of hydrogen and C1-6alkyl; Ar is thienyl, halothienyl, furanyl, halofuranyl, pyridinyl, aminopyridinyl, thiazolyl, imidazolyl or a radical of formula (a-1) wherein R3, R4 and R5 are each independently selected from the group consisting of hydrogen, C1-6alkyl, C1-6alkyloxy. halo, hydroxy, cyano, nitro, amino, mono- and di(C1-6alkyl)amino, aminocarbonyl, arylcarbonylamino, C1-6alkylcarbonylamino. C1-6alkyl-carbonyl, C1-6alkylcarbonyloxy. aminosulfonyl, C1-6alkylsulfinyl, C1-6alkylsulfonyl, C1-6alkylthio, mercapto, C3-6alkynyloxy, C3-6alkenyloxy, arylC1-6alkyloxy, aryloxy and C1-6alkyl substituted with up to 4 halo atoms; Alk is -CH2-CH2- or -CH2-CH(CH3)-; Ar1 and Ar2 are, each independently, phenyl or halophenyl; R6 and R7 are, each independently, hydrogen, Cl-6alkyl, phenylmethyl or 2-propenyl or R6 and R7 combined with the nitrogen atom bearing said R6 and R7 may form a pyrrolidinyl, piperidinyl, Cl-6alkylpiperidinyl, 4-morpholinyl or 2,6-di(C1-6alkyl)-4-morpholinyl radical; wherein aryl is a member selected from the group consisting of phenyl being optionally substituted with up to 3 substituents each independently selected from the group consisting of halo, hydroxy, Cl-6alkyl, Cl-6alkyloxy, aminosulfonyl, Cl-6alkylcarbonyl, nitro, trifluoromethyl, amino. aminocarbonyl and phenylcarbonyl, said phenylcarbonyl being optionally substituted with up to 3 halo atoms; and thienyl being optionally substituted with halo or Cl-6alkyl. |
