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US 6,617,320 B2Granted
Amino acid derivatives
AssigneeAstraZeneca AB
InventorsDavid Gustafsson, Jan-Erik Nyström
Life of this patent
Estimating the term…
Abstract
There is provided amino acid derivatives of formula I, wherein p, q, R1, R2, R3, R4, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as hirombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
Claims19
A compound of formula I,
- wherein
- p represents 0, 1, 2, 3 or 4;
- q represents 0;
- R1 represents H,
- R2 represents H or C1-4 alkyl (which latter group is optionally substituted or terminated by one or more hydroxy group)
- R3 represents C3-8 cyclohexyl or phenyl (which latter two groups are optionally substituted by one or more of C1-4 alkyl, C1-4 alkoxy, halo, hydroxy, cyano, nitro, methylenedioxy, trifluoromethyl, N(H)R27 or C(O)OR28;
- R27 represents H, C1-4 alkyl or C(O)R29;
- R28 and R29 independently represent H or C1-4 alkyl;
- R4 represents H or C1-4 alkyl;
- Y represents CH2
- n represents 1, 2, 3 or 4;
- and
- B represents a structural fragment of formula IVa
- wherein
- R5 represents H, halo or C1-4 alkyl;
- or a pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.