C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/12 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 213/74 (2006.01) C07D 213/82 (2006.01) C07D 213/85 (2006.01) C07D 213/89 (2006.01) C07D 239/42 (2006.01) C07D 295/13 (2006.01) C07D 295/155 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 473/00 (2006.01) C07D 475/00 (2006.01)
Patent
CA 2162089
The present invention relates to novel .alpha.1-adrenoceptor antagonists of Formula I: Image I in which: p is 0 or 1; t is 0, 1 or 2; X is O, S or NR6 (in which R6 is hydro or (C1-6)alkyl); Y and Z are independently CH or N; R1 is hydro, hydroxy, halo, nitro, amino, cyano, (C1-4)- alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl(C1-4)alkyl, heteroaryl(C1-4)alkyl, (C1-6)alkyloxy, (C3-6)cycloalkyloxy, (C3-6)cycloalkyl(C1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl(C1-4) alkyloxy or heteroaryl (C1-4)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano); R2 is hydro, hydroxy, halo, cyano, (C1-6)alkyl or (C1-6)- alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms); R3 is -C(O)R7 (wherein R7 is (C1-6)alkyl, (C3-6)cycloalkyl, di(C1-4)alkylamino, N-(C1-4)alkyl-N-(C1-4)alkyloxyamino, (C1-4)alkyl ((C1-4)alkyloxy)amino, pyrrolidin-1-yl, piperidin- 1-yl, morpholin-4-yl or piperazin-1-yl); R4 is halo, hydroxy, cyano, (C1-6)alkyl or (C1-6)alkyloxy; and R5 is (C1-6)alkyl; and the pharmaceutically acceptable salts and N-oxides thereof.
Clarke David Ernest
Elworthy Todd Richard
Morgans David John Jr.
Pfister Jurg Roland
Repke David Bruce
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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