abstract |
THIS INVENTION RELATES TO COMPOUNDS OF GENERAL FORMULA: IN WHICH R IS A HYDROGEN ATOM, A LOWER ALKYL GROUP, A LOWER ALCOXY, A HALOGEN ATOM, OR A TRIFLUOROMETYL GROUP; R1 IS A HYDROGEN OR HALOGEN ATOM; OR R AND R1 MAY BE TOGETHER -CH = CH-CH = CH-; R2 AND R2 'ARE INDEPENDENTLY FROM ONE ANOTHER HYDROGEN ATOM, ALOGEN A TRIFLUOROMETYL GROUP, A LOWER ALCOXY GROUP OR CYANO; OR R2 AND R2 'MAY BE, TAKEN TOGETHER, -CH = CH- CH = CH-, OPTIONALLY SUBSTITUTED (BY ONE OR MORE SUBSTITUTES SELECTED AMONG THE LOWER ALKYL OR LOWER ALCOXY GROUPS; R3 IS A HYDROGEN ATOM, A GROUP LOWER OR FORM A CYCLOALKYL GROUP; R4 IS A HYDROGEN ATOM, -N (R5) 2 ', -N (R5) (CH2) NOH, - N (R5) S (O) 2 - (LOWER ALKYL), - N (R5) S (O) 2 -PHENYL, -N = CH- N (R5) 2, -N (R5) C (O) R5 OR A CYCLIC TERTIARY AMINE OF THE GROUP. R5 ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN ATOM, A C3 TO C6 CYCLOALKYL GROUP, LOWER BENZYL OR ALKYL; R6 IS A HYDROGEN ATOM, A HYDROXY GROUP, LOWER ALKYL, (CH2) NCOO- (LOWER ALKYLE), -N (R) (LOWER ALKYL), HYDROXY (LOWER ALKYLE), CYANO, - (CH2) NO (CH2) NOH, -CHO OR A HETEROCYCLIC GROUP WITH 5 OR 6 ELEMENTS, POSSIBLY LINKED THROUGH AN ALKYLENE GROUP, X IS - C (O) N 5R5) -, - (CH2) MO-, - (CH2) MN (R5) -, -N (R5) C (O) - , OR -N (R5) (CH2) M; N IS WORTH FROM 0 to 4. AND M IS WORTH 1 OR 2 AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS OF ADDITION. THE FORMULA 1 COMPOUNDS REPRESENT A HIGH AFFINITY TOWARDS THE NK-1 RECEPTOR. THEY CAN BE USED FOR THE TREATMENT OF DISEASES THAT ARE RELATED TO NK-1 RECEPTOR ANTAGONISTS. |