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US 2003/0166577 A1Published application
Inhibitors for the blood-clotting factor xa
AssigneeCuracyte AG
InventorsJorg Sturzebecher, Torsten Steinmetzer, Sebastian Kunzel, Andreas Schweinitz
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Abstract
The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for treating cardiovascular diseases and thrombotic events.
Claims5
Inhibitors for the coagulation factor Xa of the general formula I:
- 1
- in which the substituent Y occurs in the 3- or 4-position and is an amidino group
- 2
- in which R5 has an H, an OH or a carbonyl residue —CO—R or oxycarbonyl residue —COO—R, where R can be a branched or unbranched alkyl having 1-16 C atoms, a substituted or unsubstituted aryl or heteroaryl residue or a substituted or unsubstituted aralkyl or heteroaralkyl residue,
- X is a CH group or N,
- R1 is H or a branched or unbranched alkyl having 1-8 C atoms or (CH2)n—OH where n=1-5,
- R2 is an H or a branched or unbranched alkyl having 1-8 C atoms,
- R3 is a branched or unbranched alkyl having 1-8 C atoms or a (CH2)n—O—R6, (CH2)n—S—R6 or (CH2)n—NH—R6 where n=1-5 and R6 is a branched or unbranched alkyl having 1-16 C atoms, a substituted or unsubstituted aryl or heteroaryl residue or a substituted or an unsubstituted aralkyl or heteroaralkyl residue and
- R4 is a sulfonyl residue —SO2—R, a carbonyl residue —CO—R, an oxycarbonyl residue —COO—R or an H, where R is a branched or unbranched alkyl having 1-16 C atoms, a substituted or an unsubstituted aryl or heteroaryl residue, a substituted or unsubstituted aralkyl or heteroaralkyl residue, an adamantyl residue, a camphor residue or a cyclohexylmethyl residue.
6 more elements
Dependencies are inferred from the claim text.