abstract |
THIS INVENTION CONCERNS THE COMPOUNDS OF FORMULA FORMULA I THE N-OXIDE FORMS, THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS AND THE STEREOCHEMICALLY ISOMERIC FORMS THEREOF, WHEREIN RL IS CL-6ALKYLOXY, C2-6ALKENYLOXY OR C2-6ALKYNYLOXY; R2 IS HYDROGEN OR CL-6ALKYLOXY, OR WHEN TAKEN TOGETHER RL AND R2 MAY FORM A BIVALENT RADICAL OF FORMULA WHEREIN IN SAID BIVALENT RADICALS ONE OR TWO HYDROGEN ATOMS MAY BE SUBSTITUTED WITH CL-6ALKYL, R3 IS HYDROGEN OR HALO; L IS C3-6CYCLOALKYL, C5-6CYCLOALKANONE, C2-6ALKENYL OPTIONALLY SUBSTITUTED WITH ARYL, OR L IS A RADICAL OF FORMULA -ALK-R4, -ALK-NR5R6, L-R6-4-PIPERIDINYL, ALK-X-R7, -ALK- Y -C(=0)-R9 , OR -ALK- Y -C(=O)-NR11R12 WHEREIN EACH ALK IS C1-12ALKANEDIYL; R4 IS HYDROGEN, C1-6ALKYLSULFONYLAMINO, C 3-6CYCLOALKYL, C5-6 CYCLOALKANONE, AR-, DI(AR)METHYL, AR-OXY- OR HET1 R5 IS HYDROGEN OR C1-6ALKYL; R6 IS HET2; R7 IS HYDROGEN, C1-6ALKYL, HYDROXYCL-6ALKYL, C3-6CYCLOALKYL, AR OR HET2; X IS O, S, SO2 OR NR8; SAID R8 BEING HYDROGEN, CL-6ALKYL OR AR; R9 IS HYDROGEN, CL-6ALKYL,C3-6CYCLO-ALKYL, AR, ARC1-6ALKYL, DI(AR)METHYL, C1-6ALKYLOXY OR HYDROXY; Y IS NR10 OR A DIRECT BOND; SAID R10 BEING HYDROGEN, CL-6ALKYL OR AR; R11 AND R12 EACH INDEPENDENTLY ARE HYDROGEN, C1-6ALKYL, C3-6CYCLOALKYL, AR OR ARC1-6ALKYL, OR R11 AND R12 COMBINED WITH THE NITROGEN ATOM BEARING R11 AND R12 MAY FORM A PYRROLIDINYL OR PIPERIDINYL RING BOTH BEING OPTIONALLY SUBSTITUTED WITH CL-6ALKYL, AMINO OR MONO OR DI(C1-6ALKYL)AMINO, OR SAID R11 AND R12 COMBINED WITH THE NITROGEN BEARING R11 AND R12 MAY FORM A PIPERAZINYL OR 4-MORPHOLINYL RADICAL BOTH BEING OPTIONALLY SUBSTITUTED WITH C1-6ALKYL. PROCESSES FOR PREPARING SAID PRODUCTS, FORMULATIONS COMPRISING SAID PRODUCTS AND THEIR USE AS A MEDICINE ARE DISCLOSED, IN PARTICULAR FOR TREATING CONDITIONS WHICH ARE RELATED TO IMPAIRMENT OF GASTRIC EMPTYING. |