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US 2013/0172327 A1Published application
Substituted n- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin c
AssigneeBoehringer Ingelheim International GmbH
InventorsMarc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Doris RIETHER, Wolfgang WIENEN
Life of this patent
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Abstract
Disclosed are N-1-cyano-2-(phenyl)ethyl)-2-azabicyclo[2.2.1]heptane-3-carboxamides of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory diseases.
Claims9
A compound of the formula I
- wherein
- n is 0, 1, 2, 3 or 4;
- R1 is C1-6-alkyl-, halogen, HO—, C1-6-alkyl-O—, H2N—, (C1-6-alkyl)2N—, C1-6-alkyl-C(O)HN—;
- R2 is H, halogen or selected from the group consisting of
- C1-6-alkyl-, C2-6-alkenyl-, C2-6-alkinyl-, C3-6-cycloalkyl- or C3-6-cycloalkenyl- each optionally substituted independently from each other with one, two, three or four R2.1;
- a monocyclic C5-7-heterocyclyl-, wherein one or two carbon atoms are replaced by heteroatoms selected from —S—, —S(O)—, —S(O)2—, —O— or —N— and the ring is fully or partially saturated, optionally substituted independently from each other with one, two, is three or four R2.1;
- a bicyclic C8-10-heterocyclyl-, wherein one, two, three or four carbon atoms are replaced by heteroatoms selected from —S—, —S(O)—, —S(O)2—, —O— or —N— and the ring is fully or partially saturated, optionally substituted independently from each other with one, two, three or four R2.1;
- a C5-10-heteroaryl-, wherein one, two, three or four carbon atoms are replaced by heteroatoms selected from —S—, —S(O)—, —S(O)2—, —O— or —N— and the ring is aromatic, optionally substituted independently from each other with one, two, three or four R2.1;
- aryl-, optionally substituted independently from each other with one, two, three or four R2.1;
- aryl-(O)C—HN—, optionally substituted independently from each other with one, two, three or four R2.1;
- R2.1 is halogen, C1-6-alkyl-, C3-6-cycloalkyl-, HO—, O═, C1-6-alkyl-O—, C1-6-alkyl-(O)C—, C1-6-alkyl-O(O)C—, C1-6-alkyl-HN—, (C1-6-alkyl)2N—, C1-6-alkyl-S—, C1-6-alkyl-(O)S—, C1-6-alkyl-(O)2S—, C1-6-alkyl-(O)2SO—, (C1-6-alkyl)2N(O)C—, C1-6-alkyl-HN(O)C—, C1-6-alkyl-(O)CHN—, C1-6-alkyl-(O)C(C1-6-alkyl)N—, C3-6-cycloalkyl-HN—, C3-6-cycloalkyl-(O)C—, HO—C1-6-alkyl-, MeO—C1-6-alkyl-, NC—, (C1-6-alkyl)2N(O)2S—, C1-6-alkyl-HN(O)2S—, (C1-6-alkyl)2(HO)C— or R2.1.1—, R2.1.1—C1-6-alkyl-O(O)C—,
- R2.1.1 is phenyl-, pyridinyl-, C3-6-cycloalkyl-, each optionally substituted with one, two or three halogen, HO—, NC—, C1-6-alkyl-, C1-6-alkyl-O—;
- or a salt thereof.
10 more elements
Dependencies are inferred from the claim text.