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US 7,256,194 B2Granted
Compounds that inhibit factor Xa activity
AssigneeMorphochem AG
InventorsSven Nerdinger, Thilo Fuchs, Katrin Illgen, Robert Eckl
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Abstract
The present invention relates to compounds of the Formula or a pharmaceutically acceptable salt, solvate, hydrate or formulation thereof. These compounds can be used for the inhibition of Factor Xa and for the treatment and/or prevention of diseases that are mediated by Factor Xa activity.
Claims10
Compounds of the Formula (I)
- wherein
- X is H, Cl, Br, —C(═NR1)NH2, —CH2NH2, —NH—C(═NR1)NH2, —S—C(═NR1)NH2, —NH—C(═NH)—C(═NH)NH2, —C(═NH)SR1, —NH2, —C(═N—NH2)NH2, wherein R1 is —H, —OH, —C(═O)OR2, alkyl, aralkyl, aralkyloxy, aryloxy or a heteroalkyl group, wherein R2 is alkyl, heteroalkyl, a carbocycle, heterocycloalkyl, aryl, heteroaryl or aralkyl;
- Y is O, S, SO, SO2, SO2NH, PO2NH, NR10, CO or CR8R9 wherein R8, R9 and R10 are independently H, alkyl, heteroalkyl, carbocycle, heterocycloalkyl, aryl, heteroaryl, aralkyl or heteroarylalkyl with the exception, that if Y is NR10, X is not —(═NR1)NH2;
- Ar is aryl, heteroaryl, heteroarylalkyl or aralkyl wherein X is directly attached to the aromatic ring system;
- R3 is H, an alkyl group, a heteroalkyl group, a carbocycle, a heterocycloalkyl group, an aryl group, a heteroaryl, group, a heteroarylalkyl group or an aralkyl group;
- R4 is H, alkyl, heteroalkyl, a carbocycle, heterocycloalkyl, aryl, heteroaryl, heteroarylalkyl or aralkyl;
- R5 is H, an alkyl group, a heteroalkyl group, a carbocycle, a heterocycloalkyl group, an aryl group, a heteroaryl group or an aralkyl group and
- R6 and R7 are independently H, alkyl, heteroalkyl, carbocycle, heterocycloalkyl, aryl, heteroaryl, aralkyl or heteroarylalkyl or are together members of a heterocycloalkyl ring system, or a heteroaryl ring system;
- or a pharmacologically acceptable salt, solvate, hydrate, prodrug or formulation thereof.
6 more elements
Dependencies are inferred from the claim text.