NK-1 receptor active amine oxide prodrugs

A compound of the formula

• 24
• wherein
• R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl;
• R1 is hydrogen or halogen;
• or
• R and R1 when adjacent, together with the ring carbon atoms to which they are attached are —CH═CH—CH═CH—;
• R2 and R2′ are hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano;
• or
• R2 and R2′ when adjacent, together with the ring carbons to which they are attached are —CH═CH—CH═CH—, unsubsituted or substituted by one or two substituents selected from lower alkyl or lower alkoxy;
• R3, R3′ are hydrogen, lower alkyl or cycloalkyl;
• R4, R4′ are —(CH2)mOR6 or lower alkyl;
• or
• R4 and R4′ together with the N-atom to which they are attached form a 5 or 6 member nitrogen containing heterocyclic ring of the structure
• 25
• said heterocyclic ring having 0 or 1 additional hetero-atoms selected from sulfur, nitrogen and oxygen, said additional hetero-sulfur atom being a sulfonyl moiety;
• R5 is hydrogen, hydroxy, lower alkyl, -lower alkoxy, —(CH2)mOH, —COOR3, —CON(R3)2, —N(R3)CO-lower alkyl or —C(O)R3;
• R6 is lower alkyl;
• X is —C(O)N(R6)—;
• n is 0, 1, 2, 3 or 4;
• and
• m is 1, 2 or 3;
• or a pharmaceutically acceptable acid addition salt thereof.