abstract |
Compounds of general formula (I) ** (See formula) ** in which R1: means H, C1-C2 alkyl or C1-C2 alkyloxy; 5 wherein C1-C2 alkyl and C1-C2 alkyloxy can be substituted simply or multiplely with fluorine, R2: is H or methyl; subject to the condition that one of the two residues R1 or R2 is H; X: is - (CH2) l-, - (CH2) kO-, -CH2-S-, CH2-S (O) 2-, -CH (CH3) -, -CH (CH3) -O- or -C (CH3) 2-O-; k: is 1 or 2; l: is 0, 1 or 2; R4: H, C1-C4 alkyl, C3-C4 cycloalkyl, wherein C1-C4 alkyl and C3-C4 cycloalkyl can optionally be substituted simply or multiple with fluorine; or CH2-C3-C4 cycloalkyl, in which the cycloalkyl may optionally be substituted simply or multiple with fluorine; and in the case that X: -CH2- or -CH (CH3) -R4: additionally means a 4-6 membered heterocyclyl residue that can be substituted simply or multiplely with fluorine, hydroxy, methoxy or with oxo; and in the case that X: - (CH2) l- or -CH (CH3) - R4: additionally means CN; X together with R4 form a 4-6 membered heterocyclyl residue by means of a ring carbon ligation, which can be optionally substituted in a single or multiple manner with fluorine, hydroxy, methoxy or with oxo; m: is 1 or 2; n: is 1 or 2; Ar: is an aryl residue of 6-10 or heteroaryl of 5-10, each of which can optionally be simply substituted with a fluorine, chlorine or methyl group, R3: is halogen, CN, SF5, C1 alkyl -C4, which can be optionally substituted simply or multiplely with fluorine; C3-C6 cycloalkyl, which can be substituted single or multiple with fluorine; C4-C6 heterocyclyl, which can be optionally substituted in single or multiple form with fluorine, hydroxy, methoxy or with oxo; O-C1-C4 alkyl, which can be optionally substituted in a single or multiple form with fluorine; C3-C6 O-cycloalkyl, in which the cycloalkyl can optionally be substituted simply or multiplely with fluorine; C4-C6 O-heterocyclyl, wherein the heterocyclyl can be optionally substituted in a single or multiple manner with fluorine, hydroxy, methoxy or with oxo; S-C1-C4 alkyl, in which the alkyl can optionally be substituted simply or multiple with fluorine; S (O) 2-C1-C4 alkyl, wherein the alkyl may optionally be substituted simply or multiple with fluorine; Ar ', O-Ar', C (CH3) 2-CN or C (CH3) 2-OH; and Ar ': is an optionally substituted or doubly substituted 6-membered aryl residue or 5- to 6-membered heteroaryl; wherein the substituents are selected from C1-C4 alkyl, O-C1-C4 alkyl, each of which can optionally be substituted simply or multiple with fluorine, C (CH3) 2-CN, C (CH3) 2- OH, F, Cl, CN, and C (O) NH2; and their diastereomers, enantiomers and cyclodextrin salts or clathrates thereof. |