| 摘要 |
THE PRESENT INVENTION CONCERNS COMPOUNDS OF FORMULA THE N-OXIDE FORMS, THE PHARMACEUTICALLY ACCEPTABLE ADDITION SALTS AND STEREOCHEMICALLY ISOMERIC FORMS THEREOF, WHEREIN N IS 0, 1 OR 2; M IS 1 OR 2, PROVIDED THAT IF M IS 2, THEN N IS 1; P IS 0, 1 OR 2; =Q IS =O OR =NR3; X IS A COVALENT BOND OR A BIVALENT RADICAL OF FORMULA -O-, -S-, -NR3-; R1 IS ARL; AR1C1-6ALKYL OR DI(AR1)C1-6ALKYL, WHEREIN EACH C1-6ALKYL GROUP IS OPTIONALLY SUBSTITUTED WITH HYDROXY, C1-4ALKYLOXY, OXO OR A KETALIZED OXO SUBSTITUENT OF FORMULA -O-CH2-CH2-O- OR -O-CHZ-CHZ-CH2-O-; R2 IS AR2; AR2C1-6ALKYL; HET OR HETC1-6ALKYL; R3 IS HYDROGEN OR C1-6ALKYL; R4 IS HYDROGEN; C1-4A1KY1; C1-4ALKYLOXYC1-4ALKYL; HYDROXYC1-4ALKYL; CARBOXYL; C1-4ALKYLOXYCARBONYL OR AR3; R5 IS HYDROGEN; HYDROXY; AR3; AR3C1-6ALKYLOXY; DI(AR3)C1-6ALKYLOXY; AR3C1-6ALKYLTHIO; DI(AR3)C1-6ALKYLTHIO; AR3C1-6ALKYLSULFOXY; DI(AR3)C1-6ALKYLSULFOXY; AR3C1-6ALKYLSULFONYL; DI(AR3)C1-6ALKYLSULFONYL; -NR7R8; C1-6A1KY1 SUBSTITUTED WITH -NR7R8; OR A RADICAL OF FORMULA (A-1) OR (A-2); R4 AND R5 MAY ALSO BE TAKEN TOGETHER; R6 IS HYDROGEN; HYDROXY; C1-6ALKYLOXY; C1-6ALKYL OR AR3C1-6ALKYL; AR1, AR2 AND AR3 ARE PHENYL OR SUBSTITUTED PHENYL; AR2 IS ALSO NAPHTALENYL; AND HET IS AN OPTIONALLY SUBSTITUTED MONOCYCLIC OR BICYCLIC HETEROCYCLE; AS SUBSTANCE P ANTAGONISTS; THEIR PREPARATION, COMPOSITIONS CONTAINING THEM AND THEIR USE AS A MEDICINE.
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