4-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders

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United States of America Patent

PATENT NO 6544997
SERIAL NO

09857905

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The present invention of compounds of formula (I) ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, --R.sup.1 --R.sup.2 -- is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl or hydroxy; R.sup.3 is hydrogen or halo; R.sup.4 is hydrogen or C.sub.1-6 alkyl; R.sup.5 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, oxoC.sub.5-6 cycloalkyl, C.sub.2-6 alkenyl, or L is a radical of formula --Alk--R.sup.6 --, Alk--X--R.sup.7, --Alk--Y--C(.dbd.O)--R.sup.9, or --Alk--Y--C(.dbd.O)--NR.sup.11 R.sup.12 wherein each Alk is C.sub.1-12 alkanediyl; and R.sup.6 is hydrogen, amino, cyano, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, oxoC.sub.5-6 cycloalkyl, aryl or a heterocyclic ringsystem; R.sup.7 is hydrogen, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO.sub.2 or NR.sup.8 ; said R.sup.8 being hydrogen or C.sub.1-6 alkyl; R.sup.9 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-6 alkyloxy, hydroxy or aryl; Y is a direct bond or NR.sup.10 ; said R.sup.10 being hydrogen, or C.sub.1-6 alkyl; R.sup.11 and R.sup.12 each independently are hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or R.sup.11 and R.sup.12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating or preventing gastrointestinal disorders.

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Patent Owner(s)

Patent OwnerAddress
JANSSEN PHARMACEUTICA N VBEERSE

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bosmans, Jean-Paul Rene Marie Andre Rijkevorsel, BE 23 86
De, Cleyn Michel Anna Jozef Mekrplas, BE 24 100
Gijsen, Henricus Jacobus Maria Breda, NL 50 129
Meulemans, Ann Louise Gabrielle Mol, BE 5 89

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