Piperidine derivatives as antagonists of the NK1 receptor (Neuropeptide Neurokinin - 1) antagonist activity higher in treatments of Physiological Disorders and reduced side effects

摘要

1.A compound of the formula (i) or a Salt for pharmaceutical use of the same, wherein aR1 and ar2 are each independently selected from the group consisting of R17 - heteroaryl and X1 is - O -, - S -, so nh34 - SO2 -, -, -, - N (cor12) - O - n - (so2r15); when X1 is - So - SO2 -, -, - N (cor12) - N - (so2r15) Then: R1 and R2 are each independently selected from the group consisting of H,Alkyl of C1 - C6 Hydroxy alkyl, cycloalkyl C1 - C3) C1 C8 -, - and - and - CHF2 CH2f, CF3, R1 and R2, together with the carbon Atom to which they are both together form a Ring alquileno from C3 to C6; or when X1 is or - -, - S - O - nr34 then: R1 and R2 are each independently selected from Group consisting of H, alkyl of C1 - C6 Hydroxy alkyl, cycloalkyl C1 - C3) of C3, C8, CH2f,- and CHF2 - Cf3; R1 and R2, together with the carbon Atom to which they are both together form a Ring alquileno from C3 to C6 Chemically feasible; R1 and R2, between themselves and with the carbon Atom to which they are both together form a Group c = o; R3 is selected from the group consisting of h, alq Uilo of C1 - C6 Hydroxy alkyl, cycloalkyl C1 - C3) of C3, C8, CH2f,- CHF2 and R6 - Cf3; each is selected regardless of the group consisting of H, alkyl of C1 - C6 and - Oh; each R7 is selected regardless of the group consisting of H, alkyl of C1 - C6; n2 is 1 to 4; R4 and R5 are selected irrespective of the group that is in - cr28r29 N1 - (g), where N1 is 0, 5, and G - H, - CF3, CHF2 CH2f, -, -, - or - (alkyl of C1 - C6), och2f ochf2 ocf3 - -,,,Och2cf3, - O - (cycloalkyl of C3, C6) - or - (C1 - C6 (cycloalkyl) alkyl C8 - C3 -), nr13r14 so2nr13r14 nr12so2r13, -, -, - nr12c R14 (OR), (OR) - nr12c OR13, nr12 (- C (o) nr13r14),...