| abstract |
THE PRESENT INVENTION REFERS TO COMPOUNDS OF THE GENERAL FORMULA WHERE R IS HYDROGEN, LOWER ALKYL, LOWER ALCOXY, HALOGEN OR TRIFLUOROMETILE; R1 IS HYDROGEN OR HALOGEN; OR R AND R1 CAN BE TOGETHER -CH = CH-CH = CH-; R2 AND R2 ', ARE INDEPENDENTLY, HYDROGEN, HALOGEN, TRIFLUOROMETILE, CYAN, OR LOWER ALCOXY; OR R2 AND R2', MAY BE TOGETHER -CH = CH-CH = CH-, OPTIONALLY REPLACED BY ONE OR TWO SELECTED SUBSTITUTES FROM THE OTHER FROM THE LOWER ALCOXY; R3 IS HYDROGEN, LOWER ALKYL OR FORM A CYCLOALKYL GROUP; R4 IS HYDROGEN, -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 CYCLICAL TERTIARY AMINE OF GROUP R5 IS INDEPENDENTLY, HYDROGEN, C3-6-CYCLLOALKYL, BENZYL OR LOWER ALKYL; R6 IS HYDROGEN, HYDROXY, LOWER RENT, - (CH2) nCOO-RENT LOWER, -N (R5) CO-RENT LOWER, HYDROXY-RENT-LOWER, CYAN, - (CH2) nO (CH2) nOH, -CHO OR ONE HETERO-CYCLE GROUP OF 5 OR 6 MEMBERS, OPTIONALLY UNITED BY AN ALKYLENE GROUP, X ES -C (O) N (R5) -, - (CH2) mO -, - (CH2) mN (R5) -, - N (R5) C (O) -, or -N (R5) (CH2) m-; N IS 0-4; Y M IS 1 or 2; AND SALTS DERIVED FROM A PHARMACEUTICALLY ACCEPTABLE ACID ADDITION. THE COMPOUNDS OF FORMULA 1 SHOW A GREATER AFFINITY FOR THE NK-1 RECEPTOR. THESE MAY BE USED FOR THE TREATMENT OF DISEASES THAT ARE RELATED TO NK-1 RECEPTOR ANTAGONISTS. |