Back to results
US 12,371,400 B2Granted
Cathepsin inhibitors
AssigneeAcademisch Ziekenhuis Leiden (H.O.D.N. Lumc)
InventorsHuib Ovaa, Maria Wilhelmina Elisabeth Mons, Stan Van Boeckel
Life of this patent
Estimating the term…
Abstract
This invention relates to compounds that are useful as inhibitors, in particular as inhibitors of Cathepsin K (CatK), and to a method of inhibiting cathepsin activity, comprising administering a compound or formulation comprising a compound according to the invention.
Claims20
A compound of formula I:
- wherein:
- R1 is —S(O)2Ra, —C(O) Ra, —H, —X, —CN, —C1-C6 substituted or unsubstituted alkyl, —C3-C6 substituted or unsubstituted cycloalkyl, —C1-C6 alkoxy, —C3-C6 cycloalkoxy, —NHC(O) Ra, —NHC(O) NHRa, —C2-C5 lactam, or —C1-C4 cyclourea;
- and R1 is located para or meta to the phenylene moiety;
- R2 is —C1-C4 alkyl, —C1-C4 haloalkyl, or ═O;
- R3 is —C2-C6 alkyl, or —C2-C6 haloalkyl;
- R4 and R5 are independently selected from —H, —C1-C3 alkyl, or —C1-C3 haloalkyl, or R4 and R5 together with the carbon atom to which they are attached form a C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, or C3-C6 cyclohaloalkyl;
- R6 is —H, —Y, —CH3, —CY3, —CHY2, or —CH2Y;
- each R7 is independently selected from —H, —X, —CN, —C1-C4 alkyl, —C1-C4 haloalkyl, or —C1-C3 alkoxy;
- each R8 is independently selected from —X, —C1-C4 alkyl, or —C1-C4 haloalkyl;
- Ra is —H, —C1-C6 substituted or unsubstituted alkyl, —NH2, or —NR9R10;
- each X is independently selected from —F, —Cl, —Br, or —I;
- R9 and R10 are independently selected from —H, —C1-C3 alkyl, or —C1-C3 haloalkyl;
- or R9 and R10 together with the nitrogen atom to which they are attached form a C3-C6 heterocycloalkyl or C3-C6 heterocyclohaloalkyl;
- Y is —F, —Cl, —Br, or —I;
- m is 0, 1, 2, 3, or 4;
- and
- n is 0, 1 or 2,
- or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof.
15 more elements
Dependencies are inferred from the claim text.