| abstract |
This refers to quinoline derivatives, their obtaining, pharmaceutical compositions containing them and their use as medicaments, as 5-HTsa receptor agonists. Claim 1: A compound of the formula (1), wherein R1 is -NRa-Ar1, -NRbCH2-Ar1, -CH2NRb-Ar1, -NRcC (O) -Ar1, -OCH2-Ar1, -CH2O-Ar1, -CH2CH2-Ar1, -CH = CH-Ar1, -NHC (O) NH-Ar1, -NHSO2NH-Ar1, -NRcC (O) O-Ar1, -C (O) NRcCH2-Ar1, -CH2NRbCH2-Ar1, - NHC (= N-Ar1) -Ar1, -NRbCH2CH2CH2-Ar1 or -NRbCH2CH2O-Ar1, R2 is -Ar2, -CHRd-Ar2 or -CH2CH2O-Ar2, R3 is hydrogen, phenyl or pyridinyl, optionally substituted by one or more alkyl C1-4, halogen or C1-4 alkoxy, -NReRf, in which Re and Rf independently of each other are hydrogen or - (CH2) m-ORg, in which m is a number from 2 to 6, Ar1 and Ar2 independently of each other they are aryl or heteroaryl, each of them is optionally substituted by one or more B, B is C1-7 alkoxy, C1-7 haloalkoxy, hydroxy, halogen, C1-7 alkyl optionally substituted by one or more halogen, hydroxy or cyano, -S (O) 2-C1-7 alkyl, -NRiRii, -NRiiiS (O) 2Riv, -NRiiiC (O) Riv, -C (O) NRiiiRiv, -S (O) 2-NRiiiRiv, - CH2-O-Rv, - (OCH2CH2) n-ORv, in which n is a number from 1 to 3, -CH2- OCH2CH2) nOPv, in which n is a number from 1 to 3, -C (O) Rv, cyano, nitro, allyl, C3-7 cycloalkyl, monocyclic heterocycloalkyl of 5 to 7 links, or two moieties B which are in ortho position between if they form a bridge with 3 or 4 links of the formula -CH2CH2CH2-, -CH2CH2CH2CH2-, -OC (Rvi) 2-O-, -OCH2CH2O-, -OCH (Rvii) -CH (Rviii) -, Ra, Rb, Rc, Rd and Rg, independently of each other are hydrogen, C1-7 alkyl; Ri, Rii, Riii, Riv and Rv independently of one another are hydrogen or C1-7 alkyl or - (CH2) n-C3-7 cycloalkyl, in which n is a number from 0 to 3; Rvi, Rvii and Rviii, independently of each other are hydrogen, C1-4 alkyl or halogen; or a pharmaceutically acceptable salt thereof. |