PEPTIDES, METHOD OF THEIR PRODUCING, THEIR USING AND PHARMACEUTICAL PREPARATION ON THEIR BASE

• Main Authors: GREENGRASS COLIN W, STREET STEPHEN D. A, WHITTLE PETER J
• Format: Patent
• Language: English
• Published: 12.04.1995
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Compounds of formula (I) and pharmaceutically acceptable salts thereof and bioprecursors therefore wherein R is C1-C6 alkyl, C3-C8 cycloalkyl, aryl, heterocyclyl or CONR R ; R is C1-C6 alkyl, C3-C8 cycloalkyl(C1-C4)alkyl, aryl(C1-C4)alkyl or heterocyclyl(C1-C4)alkyl; R 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; R is C1-C6 alkyl, C3-C8 cycloalkyl, aryl or heterocyclyl; each of R , R , R and R is independently H, C1-C6 alkyl or C3-C8 cycloalkyl; or R and R , or R and R 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 -(CR R )m-Het substituent, it may be substituted by up to 4 further substituents independently chosen from F, C1-C6 alkyl, C3-C8 cycloalkyl, OR or NR R ; Het is an imidazolyl or triazolyl group either of which may optionally be substituted by C1-C6 alkyl, C3-C7 cycloalkyl, NR R or CONR R , each of R and R is independently H, C1-C6 alkyl or C3-C8 cycloalkyl, or R and R may be joined together to form, with the nitrogen to which they are attached, a 4 to 8 membered nitrogen-containing heterocyclic group, R is H, C1-C6 alkyl or C3-C8 cycloalkyl; n and m are each independently 0, 1 or 2; 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.