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US 10,537,652 B2Granted
Cyclic urea compounds as granzyme B inhibitors
AssigneeviDA Therapeutics Inc.
InventorDale R. Cameron
Life of this patent
Estimating the term…
Abstract
Cyclic urea compounds as Granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Methods for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.
Claims18
A compound having Formula (I):
- or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein:
- R1 is a heteroaryl group selected from
- (a) 1,2,3-triazolyl, and
- (b) 1,2,3,4-tetrazolyl;
- n is 1 or 2;
- R2 is selected from
- (a) hydrogen,
- (b) C1-C6 alkyl, and
- (c) C3-C6 cycloalkyl;
- R3 is selected from
- (a) hydrogen,
- (b) C1-C4 alkyl optionally substituted with a carboxylic acid, carboxylate, or carboxylate C1-C8 ester group, an amide optionally substituted with an alkylheteroaryl group, or a heteroaryl group;
- Z is an acyl group selected from the group
- wherein
- Y is hydrogen, heterocycle, —NH2, or C1-C4 alkyl;
- R4 is selected from
- (i) C1-C12 alkyl,
- (ii) C1-C6 heteroalkyl optionally substituted with C1-C6 alkyl,
- (iii) C3-C6 cycloalkyl,
- (iv) C6-C10 aryl,
- (v) heterocyclyl,
- (vi) C3-C10 heteroaryl,
- (vii) aralkyl, and
- (viii) heteroalkylaryl;
- R5 is heteroaryl or —C(═O)—R10,
- wherein R10 is selected from
- (i) C1-C12 alkyl optionally substituted with C6-C10 aryl, C1-C10 heteroaryl, amino, or carboxylic acid,
- (ii) C1-C10 heteroalkyl optionally substituted with C1-C6 alkyl or carboxylic acid,
- (iii) C3-C6 cycloalkyl optionally substituted with C1-C6 alkyl, optionally substituted C6-C10 aryl, optionally substituted C3-C10 heteroaryl, amino, or carboxylic acid,
- (iv) C6-C10 aryl optionally substituted with C1-C6 alkyl, optionally substituted C6-C10 aryl, optionally substituted C3-C10 heteroaryl, amino, or carboxylic acid,
- (v) heterocyclyl,
- (vi) C3-C10 heteroaryl,
- (vii) aralkyl, and
- (viii) heteroalkylaryl.
31 more elements
Dependencies are inferred from the claim text.