abstract |
Invention Patent: <B> "MONOCYCLIC GASTROKINETIC BENZAMIDES OF 4- (AMINOMETHIL) PIPERIDINE 3 OR 4-SUBSTITUTED DERIVATIVES" <D>. The present invention features compounds of formula (I), a stereochemically isomeric form thereof, an N-oxide form thereof, or a pharmaceutically acceptable acid addition salt thereof, where R 1 1 is C ~ 1-6 ~ alkyloxy , C ~ 2-6 ~ alkenyloxy or C ~ 2-6 ~ alkynyloxy; R 2 is hydrogen, C ~ 1-6 ~ alkyl or C ~ 1-6 ~ alkyloxy; R ^ 3 ^ is hydrogen or halo; R 4 is hydrogen or C 1-6 alkyl; R 5 is hydrogen or C 1-6 alkyl; L is C ~ 3-6 ~ cycloalkyl, C ~ 5-6 ~ cycloalkane or C ~ 2-6 ~ alkenyl; or L is a radical of the formula -Al-R ^ 6 ^ (b-1), -Al-XR ^ 7 ^ (b-2), -Al-YC (= O) -R ^ 9 ^ (b-3) ) or -Al-YC (= O) -NR ^ 11 ^ R ^ 12 ^ (b-4), where each Alk is C ~ 1-12 ~ alkanediyl; and R 6 is hydrogen, cyano, C ~ 1-6 ~ alkylsulfonylamino, C ~ 3-6 ~ cycloalkyl, C ~ 5-6 ~ cycloalkanone or a heterocyclic ring system; R 7 is hydrogen, C ~ 1-6 ~ alkyl, C ~ 1-6 ~ alkyl, C ~ 3-6 ~ cycloalkyl or a heterocyclic ring system; X is O, S, SO ~ 2 ~ or NR ^ 8 ^, with R ^ 8 ^ hydrogen or C ~ 1-6 ~ alkyl; R ^ 9 ^ is hydrogen, C ~ 1-6 ~ alkyl, C ~ 3-6 ~ cycloalkyl, C ~ 1-6 ~ alkyloxy or hydroxy; Y is NR ^ 10 ^ or a direct bond; R ^ 10 ^ hydrogen or C ~ 1-6 ~ alkyl; R ^ 11 ^ and R ^ 12 ^, each independently, are hydrogen, C ~ 1-6 ~ alkyl, C ~ 3-6 ~ cycloalkyl, or R ^ 11 ^ and R ^ 12 ^ combined with the nitrogen atom form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing the products, formulations that comprise the products and their use as a medicine are also presented, in particular to treat conditions that are related to gastric emptying difficulties. |