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US 7,732,464 B2Granted
Heterocyclic substituted 4-(aminomethyl)-piperidine benzamides as 5HT4-antagonists
AssigneeJanssen Pharmaceutica NV
InventorsJean-Paul René Marie André Bosmans, Henricus Jacobus Maria Gijsen, Laurence Anne Mevellec
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Abstract
The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine of said compounds.
Claims10
A compound of formula (I)
- a stereochemically isomeric form thereof, an N-oxide form thereof, or a pharmaceutically acceptable acid or base addition salt thereof, wherein
- —R1—R2— is a bivalent radical of formula
- —O—CH2—CH2—O— (a-3), or
- —O—CH2—CH2—CH2—O— (a-5),
- wherein in said bivalent radicals optionally one or two hydrogen atoms on the same or a different carbon atom may be replaced by C1-6alkyl or hydroxy,
- R3 is hydrogen, halo, C1-6alkyl or C1-6alkyloxy;
- R4 is hydrogen, halo, C1-6alkyl;
- C1-6alkyl substituted with cyano, or C1-6alkyloxy;
- C1-6alkyloxy;
- cyano;
- amino or mono or di(C1-6alkyl)amino;
- R5 is hydrogen or C1-6alkyl, and the —OR5 radical is situated at the 3- or 4-position of the piperidine moiety;
- L is a radical of formula
- -Alk-R6 (b-1),
- -Alk-X—R7 (b-2),
- wherein each Alk is C1-12alkanediyl;
- and
- R6 is Het;
- R7 is Het;
- X is O, S, SO2 or NR8;
- said R8 being hydrogen or C1-6alkyl;
- and
- Het is morpholinyl;
- morpholinyl substituted with C1-6alkyl;
- tetrazolyl;
- tetrazolyl substituted with halo, hydroxy, or C1-6alkyl;
- pyrazolyl;
- pyrazolyl substituted with halo, hydroxy, or C1-6alkyl;
- isoxazolyl;
- isoxazolyl substituted with halo, hydroxy, or C1-16alkyl;
- isothiazolyl;
- isothiazolyl substituted with halo, hydroxy, or C1-6alkyl;
- 2,4-dioxo-imidazolidinyl;
- 2,4-dioxo-imidazolidinyl substituted with one or two substitutents each independently selected from halo, or C1-6alkyl;
- oxazolyl;
- oxazolyl substituted with halo, hydroxy, or C1-6alkyl;
- thiazolyl;
- thiazolyl substituted with halo, hydroxy, or C1-6alkyl;
- or
- pyranyl;
- pyranyl substituted with halo, hydroxy, or C1-6alkyl.
38 more elements
Dependencies are inferred from the claim text.