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US 2003/0166680 A1Published application
Aminopyrrolidine sulfonamides as serine protease inhibitors
AssigneeOrtho-McNeil Pharmaceutical, Inc.
InventorsMichael N. Greco, Bruce E. Maryanoff, Michael J. Hawkins, Robert E. Boyd
Life of this patent
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Abstract
The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.
Claims26
A compound selected from the group consisting of Formula (I) and Formula (II):
- 14
- wherein
- R1 is selected from the group consisting of hydrogen, C1-8alkyl, C3-7cycloalkyl, aryl, aryl(C1-8)alkyl, aryl(C2-8)alkenyl, heteroaryl(C1-8)alkyl, heteroaryl(C2-8)alkenyl and R4C(O)CH2—;
- wherein aryl and heteroaryl are optionally substituted with one to two substituents independently selected from R4;
- R2 is selected from the group consisting of hydrogen, hydroxy, C1-8alkoxy, aryloxy and aryl(C1-8)alkoxy;
- with the proviso that R2 is bonded to the heterocyclyl ring by a single bond;
- alternatively, R2 is oxo;
- with the proviso that R2 is bonded to the heterocyclyl ring by a double bond;
- R3 is selected from the group consisting of aryl, aryl(C1-8)alkyl, aryl(C2-8)alkenyl, heteroaryl(C1-8)alkyl, heteroaryl(C2-8)alkenyl;
- wherein aryl and heteroaryl are optionally substituted with one to three substituents independently selected from the group consisting of halogen, C1-8alkyl, C1-8alkoxy, amino, (C1-4alkyl)amino, di(C1-4alkyl)amino, trihalo(C1-8)alkyl and trihalo(C1-8)alkoxy;
- R4 is selected from the group consisting of hydroxy, amino, C1-8alkyl, (C1-4alkyl)amino, di(C1-4alkyl)amino, C1-8alkoxy, carboxy, carboxy(C1-8)alkyl, carboxy(C1-8)alkoxy, (carboxy)amino, (carboxy(C1-4)alkyl)amino, (carboxyaryl)amino, (carboxyaryl(C1-4)alkyl)amino, (carboxy(C1-4)alkylaryl)amino, aryloxy, aryl(C1-8)alkoxy, (aryl)amino, (aryl(C1-4)alkyl)amino, (C1-4alkylaryl)amino, (arylcarboxy)amino, di(aryl)amino, di(aryl(C1-4)alkyl)amino, C1-8alkoxycarbonyl, C1-8alkoxycarbonyl(C1-8)alkoxy, aminocarbonyl, (C1-8alkyl)aminocarbonyl, (carboxy(C1-8)alkyl)aminocarbonyl, (C1-8alkoxycarbonyl(C1-8)alkyl)aminocarbonyl and guanidino;
- and,
- G is selected from the group consisting of hydrogen, halogen, hydroxy, C1-4alkyl, C1-8alkoxy, aryl, aryloxy, aryl(C1-8)alkyl, aryl(C1-8)alkoxy, amino, carboxy, alkylaminocarbonyl, alkylcarbonylamino, trihalo(C1-8)alkyl and trihalo(C1-8)alkoxy;
- and pharmaceutically acceptable salts thereof.
11 more elements
Dependencies are inferred from the claim text.