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US 8,013,183 B2Granted
Alpha ketoamide compounds as cysteine protease inhibitors
AssigneeViroBay, Inc.
InventorsMichael Graupe, John O. Link, Michael G. Roepel
Life of this patent
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Abstract
The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
Claims10
A compound of Formula (II):
- wherein:
- R5 is alkyl, cycloalkylalkyl, aralkyl, heteroaralkyl, heterocycloalkylalkyl, -(alkylene)-X—R9 (where X is —S— or —SO2— and R9 is alkyl, cycloalkylalkyl, aryl, aralkyl or heteroaralkyl) or haloalkyl optionally substituted with cycloalkyl, wherein the aromatic or alicyclic ring in R5 is optionally substituted with one, two, or three Ra independently selected from alkyl, haloalkyl, alkoxy, hydroxy, haloalkoxy, cyano, halo or —SO2R11 (where R11 is alkyl, cycloalkyl, aryl, heteroaryl, or heterocycloalkyl);
- R6 is haloalkyl;
- and
- R8 is hydrogen or aryl, wherein the aromatic ring in R8 is optionally substituted with one, two, or three Re independently selected from alkyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, carboxy, cyano, alkylsulfonyl, alkylsulfonylamino, aminocarbonyl, or aminosulfonyl;
- or
- a pharmaceutically acceptable salts thereof.
4 more elements
A compound of Formula (III):
- wherein:
- R1 is hydrogen;
- R2 is cycloalkyl or aralkyl;
- R3 is hydrogen or alkyl;
- R4 is alkyl;
- or
- R3 and R4 together with the carbon atom to which they are attached form cycloalkylene;
- R5 is alkyl, cycloalkylalkyl, aralkyl, heteroaralkyl, heterocycloalkylalkyl, -(alkylene)-X—R9 (where X is —S— or —SO2— and R9 is alkyl, cycloalkylalkyl, aryl, aralkyl or heteroaralkyl) or haloalkyl optionally substituted with cycloalkyl wherein the aromatic or alicyclic ring in R5 is optionally substituted with one, two, or three Ra independently selected from alkyl, haloalkyl, alkoxy, hydroxy, haloalkoxy, cyano, halo or —SO2R11 (where R11 is alkyl, cycloalkyl, aryl, heteroaryl, or heterocycloalkyl);
- R6 is haloalkyl;
- and
- R8 is hydrogen or aryl, wherein the aromatic ring in R8 is optionally substituted with one, two, or three Re independently selected from alkyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, carboxy, cyano, alkylsulfonyl, alkylsulfonylamino, aminocarbonyl, or aminosulfonyl;
- or
- a pharmaceutically acceptable salts thereof.
10 more elements
Dependencies are inferred from the claim text.