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US 2015/0031915 A1Published application
Compositions and Methods for Inhibition of Cathepsins
AssigneesOXiGENE, Inc., Baylor University
InventorsDavid J. Chaplin, Kishore Kumar Gaddale Devanna, Erica Parker, Kevin G. Pinney, Jiangli Song, Mary L. Trawick
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Abstract
This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful.
Claims3
A compound of formula I:
- or a solvate or pharmaceutically acceptable salt thereof, wherein
- X is selected from the group consisting of C(═O), CH(OR6) and
- n is 0, 1, 2 or 3;
- m is 0, 1, 2 or 3;
- p is 0, 1, 2 or 3;
- R1 is hydrogen, C1-C3 alkyl, aryl and arylalkyl;
- R2 is hydrogen or C1-C3 alkyl;
- each R3 and R5 independently is selected from the group consisting of hydroxyl, C1-C3 alkyl, C1-C2 alkoxy, fluoro, and chloro;
- each R4 independently is selected from the group consisting of hydroxyl, C1-C6 alkyl, C1-C6 alkoxy, halo, amino, nitro, nitroso and acyl;
- and
- R6 is selected from the group consisting of hydrogen and methyl.
8 more elements
2-20. (canceled)
A compound selected from the group consisting of:
- 1,4-dibenzoylbenzene (1),
- 3-benzoyl benzophenone thiosemicarbazone (3),
- 4-Benzoyl benzophenone thiosemicarbazone (4),
- 3-Benzoyl benzhydrol thiosemicarbazone (6),
- 1-(3-methylbenzoyl),3-(3-methylbenzoyl)benzene thisosemicarbazone (9),
- 1,3-bis(2-fluoro-benzoyl)-5-bromobenzene thiosemicarbazone (11),
- 1,3-bis-(4-fluorobenzoyl)benzene thiosemicarbazone (13),
- 1-(4-hydroxybenzoyl)-3-(4-methoxybenzoyl)benzene thiosemicarbazone (17),
- 1-(4-methoxybenzoyl)-3-(4-hydroxybenzoyl)benzene thiosemicarbazone (18),
- 1-(4-hydroxybenzoyl)-3-(4-methoxybenzoyl)benzene di-thiosemicarbazone (19),
- 1,3-bis-(4-isopropoxybenzoyl)benzene thiosemicarbazone (22),
- 1,3-bis-(4-isopropoxybenzoyl)benzene dithiosemicarbazone (23),
- 1,3-bis-(4-bromobenzoyl)benzene thiosemicarbazone (24),
- 1,3,5-Tribenzoyl benzene thiosemicarbazone (25),
- 2-[(3-benzoylphenyl)(phenyl)methylene]-N-methylhydrazinecarbothioamide (27),
- 2-[(3-benzoylphenyl)(phenyl)methylene]-1-methylhydrazinecarbothioamide (28), and
- 1,3-bis-(4-methoxybenzoyl)benzene dithiosemicarbazone (33).
14 more elements
Dependencies are inferred from the claim text.