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US 5,057,525 AGranted
Novel N-(3-hydroxy-4-piperidinyl) benzamide derivatives
AssigneeJanssen Pharmaceutica NV
InventorGeorges Van Daele
Life of this patent
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Abstract
Novel N-(3-hydroxy-4-pipridinyl)benzamides and derivatives thereof, said compounds being used as stimulators of the motility of the gastro-intestinal system.
Claims15
A compound of the formula:
- ##STR59## the pharmaceutically acceptable acid addition salts thereof, the stereochemically isomeric forms, and the pharmaceutically acceptable quaternary ammonium salts thereof, wherein:
- the substituents in the 3 and 4 positions in the piperidine ring have the cis configuration;
- R.sup.1 represents a member selected from the group consisting of hydrogen, lower alkyl, (Ar.sup.1)lower alkyl, and lower alkylcarbonyl;
- R.sup.2 represents hydrogen;
- R.sup.3, R.sup.4, and R.sup.5 each independently represent hydrogen, lower alkyl, lower alkyloxy, halo, hydroxy, amino, nitro, mono- or di(lower alkyl)amino, lower alkylcarbonylamino, lower alkylcarbonyl, lower alkylcarbonyloxy, aminosulfonyl, and lower alkylsulfonyl;
- and
- L represents a group of the formula:
- --C.sub.r H.sub.2r --Ar.sup.2
- wherein r represents an integer of from 1 to 6 inclusive and Ar.sup.2 represents a member selected from the group consisting of naphthalenyl and pyridinyl,
- wherein in the foregoing Ar.sup.1 represents 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, lower alkyl, lower alkyloxy, aminosulfonyl, lower alkylcarbonyl, nitro, trifluoromethyl, amino, aminocarbonyl, phenylcarbonyl wherein said phenyl may be optionally substituted with up to 3 halo atoms, and thienyl substituted with halo or lower alkyl.
7 more elements
Dependencies are inferred from the claim text.