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US 2006/0142339 A1Published application
Aminosulfonyl substituted 4-(aminomethyl)-piperidine benzamides as 5ht 4-antagonists
AssigneeJanssen Pharmaceutica NV
InventorsJean-Paul Bosmans, Henricus Gijsen, Laurence 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.
Claims13
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—O— (a-1),
- —O—CH2—CH2— (a-2),
- —O—CH2—CH2—O— (a-3),
- —O—CH2—CH2—CH2— (a-4),
- —O—CH2—CH2—CH2—O— (a-5),
- —O—CH2—CH2—CH2—CH2— (a-6),
- —O—CH2—CH2—CH2—CH2—O— (a-7),
- —O—CH2—CH2—CH2—CH2—CH2— (a-8),
- 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),
- -Alk-Y—C(═O)—R9 (b-3),
- -Alk-C(═O)—NH—C(═O)—R11 (b-4),
- -Alk-C(═O)—NH—SO2—R11 (b-5),
- -Alk-SO2—NH—C(═O)—R11 (b-6),
- -Alk-SO2—NH—SO2—R11 (b-7),
- wherein each Alk is C1-12alkanediyl;
- and
- R6 is aminosulfonyl optionally substituted with C1-4alkyl, C3-6cycloalkyl or phenyl;
- R7 is C1-6alkylsulfonyl;
- X is NR8;
- said R8 being C1-6alkyl;
- R9 is C1-6alkylsulfonylamino;
- Y is a O, S, or NR10 wherein R10 is hydrogen or C1-6alkyl;
- and
- R11 is C1-6alkyl or phenyl.
33 more elements
(canceled)
(canceled)
Dependencies are inferred from the claim text.