Azacyclic compounds

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 211/42 (2006.01) A61K 31/40 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 207/12 (2006.01) C07D 211/54 (2006.01) C07D 401/02 (2006.01) C07D 401/12 (2006.01) C07D 403/02 (2006.01) C07D 405/02 (2006.01) C07D 405/12 (2006.01) C07D 409/02 (2006.01) C07D 413/02 (2006.01) C07D 417/02 (2006.01)

Patent

CA 2138650

Compounds of Formula (I), and salts and prodrugs thereof, wherein n is 1, 2 or 3; X represents O or S; R1 is optionally substituted phenyl; R2 is aryl or heteroaryl; R4 and R5 are independently H, halo, C1-6alkyl, oxo, CH2ORa, CO2Ra or CON- RaRb; R8 represents C(COORa)2, C(CONRaRb)2 or C1-6alkyl substituted by C(=NRa)NRbNRcCO2Rd, CONHNRaRb, C(S)NRaRb, CONRaC1-6alkylR12, CONR13C2-6alkynyl, CONR13C2-6alkenyl, COCONRaRb, CONRaC(NRb)NRcRd, CONR13SO2Ra, SO2NRI3CORa, CONRaheteroaryl or CORq; Ra, Rb, Rc and Rd are each H, C1-6alkyl, phenyl or trifluor- omethyl. R12 represents ORa, CONRaRb or heteroaryl; R13 represents H or C1-6alkyl; and Rq represents a group (a) where Q represents the residue of a non-aromatic azacyclic or azabicyclic ring system; are tachykinin antagonists useful in ther- apy.

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