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4-(aroylamino)piperidine-butanimide derivatives

  • US 4,990,521 A
  • Filed: 09/08/1989
  • Issued: 02/05/1991
  • Est. Priority Date: 07/03/1986
  • Status: Expired due to Fees
First Claim
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1. A method of treating warm-blooded animals suffering from diarrhea, which method comprises the systemic administration to warm-blooded animals of an amount effective in treating diarrhea of a compound having the formula:

  • ##STR22## an N-oxide form, a pharmaceutically acceptable acid-solution salt, or a possible stereoisomeric form thereof, whereinR1 is a member selected from the group consisting of hydrogen, C1-6 alkyl, aryl C1-6 alkyl;

    C1-6 alkylcarbonyl, aminoC1-6 alkyl, and mono- and di(C1-6 alkyl)aminoC1-6 alkyl;

    R2 is a member selected from the group consisting of hydrogen and C1-6 alkyl;

    Ar is a radical of the formula;

    ##STR23## wherein R3, R4, and R5 are each independently selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 alkyloxy, halo, hydroxy, cyano, nitro, amino, mono- and di(C1-6 alkyl)amino, aminocarbonyl, arylcarbonylamino, C1-6 alkylcarbonylamino, C1-6 alkylcarbonyl, C1-6 alkylcarbonyloxy, aminosulfonyl, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, CI-6 alkylthio, mercapto, C3-6 alkynyloxy, C3-6 alkenyloxy, aryl C1-6 alkyloxy, aryloxy, and C1-6 alkyl 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, C1-6 alkyl, phenylmethyl, or 2-propenyl;

    wherein aryl is 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, C1-6 alkyl, C1-6 alkyloxy, aminosulfonyl, C1-6 alkylcarbonyl, nitro, trifluoromethyl, amino, aminocarboxyl, and phenylcarbonyl, said phenylcarbonyl being optionally substituted with up to 3 halo atoms.

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