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Novel compoundsNovel compounds description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20080125426, Novel compounds. Brief Patent Description - Full Patent Description - Patent Application Claims
The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors. BACKGROUND OF THE INVENTIONCathepsin S is a member of the papain superfamily of cysteine proteases which also encompasses Cathepsins B, H, L, O and K. Cathepsin S plays a key role in the processing of invariant chain in MHC class II complexes allowing the complex to associate with antigenic peptides. MHC class II complexes are then transported to the surface of the cell for presentation to effector cells such as T cells. The process of antigen presentation is a fundamental step in initiation of the immune response. In this respect inhibitors of cathepsin S could be useful agents in the treatment of inflammation and immune disorders such as, but not limited to, asthma, rheumatoid arthritis, multiple sclerosis and Crohn's disease. Cathepsin S has also been implicated in a variety of other diseases involving extracellular proteolysis such as the development of emphysema in COPD through degradation of elastin and in Alzheimers disease. Other Cathepsins notably K and L have been shown to degrade bone collagen and other bone matrix proteins. Inhibitors of these cysteine proteases would be expected to be useful in the treatment of diseases involving bone resorption such as osteoporosis. The present invention therefore provides a compound of formula (I)
in which: X is N, NH, :CH or CH2;Y is N, :CH, CO, CH2 or :CNR2R3, where R2 and R3 are independently hydrogen, C1-6 alkyl or C3-6 cycloalkyl;
R is aryl or heteroaryl optionally substituted by halogen, amino, hydroxy, cyano, nitro, trifluoromethyl, carboxy, CONR5R6, SO2NR5R6, SO2R4, NHSO2R4, NHCOR4, ethylenedioxy, methylenedioxy, C1-6 alkyl, C1-6 alkoxy, SR4 or NR5R6 where R4 is hydrogen, C1-6 alkyl or C3-6 cycloalkyl, R5 and R6 are independently hydrogen, C1-6 alkyl or together with the nitrogen atom to which they are attached form a 5- or 6-membered saturated ring optionally containing a further O, S or NR4 group;
or R is hydrogen, C1-6 alkyl or C3-6 cycloalkyl both of which can optionally contain one or more O, S or NR4 groups,
R1 is a group Y(CH2)pR7 where p is 0, 1 or 2 and Y is O or NR8 where R8 is hydrogen, C1-6 alkyl or C3-6 cycloalkyl;
and R7 is a 5- or 6-membered saturated ring containing one or more O, S or N atoms, aryl or a heteroaryl group containing one to four heteroatoms selected from O, S or N, the saturated ring, aryl and heteroaryl groups all being optionally substituted by halogen, amino, hydroxy, cyano, nitro, trifluoromethyl, carboxy, CONR5R6, SO2NR5R6, SO2R4, NHSO2R4, NHCOR4, C1-6 alkyl, C1-6 alkoxy, SR4 or NR5R6 where R4 is hydrogen, C1-6 alkyl or C3-6 cycloalkyl, R5 and R6 are independently hydrogen, C1-6 alkyl or together with the nitrogen atom to which they are attached form a 5- or 6-membered saturated ring optionally containing a further O, S or NR4 group;
or R1 is a group NR9R10 where R9 and R10 are independently hydrogen or C1-6 alkyl optionally containing one or more O, S or NR4 groups, or R9 and R10 together with the nitrogen atom to which they are attached form a 5 or 6-membered saturated ring optionally containing a further O, S or N atom and optionally substituted by NR9R10, CO2C1-6 alkyl, CONR11R12 where R11 and R12 are independently hydrogen or C1-6 alkyl, aryl or heteroaryl group optionally substituted by halogen, amino, hydroxy, cyano, nitro, trifluoromethyl, carboxy, CONR5R6, SO2NR5R6, SO2R4, NHSO2R4, NHCOR4, C1-6 alkyl, C1-6 alkoxy, SR4 or NR5R6 where R4 is hydrogen, C1-6 alkyl or C3-6 cycloalkyl, R5 and R6 are independently hydrogen, C1-6 alkyl or together with the nitrogen atom to which they are attached form a 5- or 6-membered saturated ring optionally containing a further O, S or NR4 group;
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