C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/03 (2006.01) A61K 31/395 (2006.01) A61K 38/05 (2006.01) C07D 205/04 (2006.01) C07D 205/08 (2006.01) C07D 207/14 (2006.01) C07D 207/404 (2006.01) C07D 211/26 (2006.01) C07D 211/58 (2006.01) C07D 211/74 (2006.01) C07D 307/33 (2006.01) C07D 401/02 (2006.01) C07D 401/12 (2006.01) C07D 403/02 (2006.01) C07D 405/10 (2006.01) C07D 405/12 (2006.01) C07D 407/10 (2006.01) C07D 409/12 (2006.01) C07D 413/02 (2006.01) C07F 7/18 (2006.01)
Patent
CA 2133583
2133583 9323373 PCTABScor01 Compounds of formula (I) wherein R1 is C1-C6 alkyl, C3-C8 cycloalkyl, aryl, heterocyclyl, or R7R8NCO; R2 is C1-C6 alkyl, C3-C8 cycloalkyl(C1-C4)alkyl, aryl(C1-C4)alkyl, or heterocyclyl(C1-C4)alkyl; R3 is C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl(C1-C4)alkyl, aryl(C1-C4)alkyl, aryl(C2-C4)alkenyl, heterocyclyl(C1-C4)alkyl or heterocyclyl(C2-C4)alkenyl; R4 is C1-C6 alkyl, C3-C8 cycloalkyl, aryl or heterocyclyl; R5 and R6 are each independently H, C1-C6 alkyl, C3-C7 cycloalkyl, or C1-C6 alkyl substituted by C1-C4 alkoxy, hydroxy or NR7R8; or R5 and R6 are linked to form, together with the nitrogen atom to which they are attached, a pyrrolidine, piperidine, morpholine, piperazine or N-(C1-C4 alkyl) piperazine group; each of R7 and R8 is independently H, C1-C6 alkyl or C3-C8 cycloalkyl or R7 and R8 may be joined together to form, with the nitrogen to which they are attached, a 4 to 8 membered nitrogen-containing heterocyclic group; each of R9, R10, R11 and R12 is independently H, C1-C6 alkyl or C3-C8 cycloalkyl; or R9 and R10, or R11 and R12 may be joined together to form a 3 to 8 membered carbocyclic ring; X is a 4-10 membered mono- or bicyclic heterocyclic group containing carbon ring atoms and one ring nitrogen atom through which the group is attached to the adjacent carbonyl group; the group may be saturated or partially unsaturated and, in addition to the -(CR11R12)m -NR5R6 substituent, it may be substituted by up to 4 further substituents each independently chosen from F, C1-C6 alkyl, C3-C8 cycloalkyl, OH, C1-C6 alkoxy or NR7R8; and n and m are each independently 0, 1 or 2; and wherein any alkyl or cycloalkyl group included in the aforementioned definitions may optionally be fully or partially substituted by fluorine; are inhibitors of retroviral proteases of utility in the treatment and prophylaxis of human retroviral infections.
Greengrass Colin W.
Gymer Geoffrey E.
Hoople David W. T.
Street Stephen D. A.
Whittle Peter J.
Limited Pfizer
Smart & Biggar
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