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US 2003/0153510 A1Published application
Novel compounds inhibiting factor xa activity
AssigneeMorphochem AG
InventorsMichael W Cappi, Thilo Fuchs, Robert Eckl, Silke Schabbert
Life of this patent
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Abstract
The present invention relates to compounds of formula (I): 1 or a pharmaceutically acceptable salt, solvate, hydrate or a pharmaceutically acceptable formulation thereof. Those compounds can be used for inhibiting factor Xa and for the prevention and/or treatment of thromboembolic conditions.
Claims15
Compounds of formula (I):
- 8
- wherein
- X is Cl, Br or R1—N═CH(—NH2)— wherein
- R1 is H, —OH, —C(═O)OR2, alkyl, aralkyl, aralkyloxy or a heteroalkyl group, such as, for example, alkoxy, acyl or acyloxy, wherein
- R2 is alkyl, heteroalkyl, a carbocyclic group, heterocycloalkyl, aryl, heteroaryl, heteroarylalkyl or aralkyl;
- Ar is arylene, heteroarylene, heteroarylalkylene or aralkylene, X being bonded directly to the aromatic ring system;
- R3 is H, alkyl, heteroalkyl or aralkyl;
- the groups R4 independently of one another are alkyl groups that may be substituted by one or more —OH or —NH2 radicals, or are heteroalkyl groups, carbocyclic groups, heterocycloalkyl groups, aryl groups, heteroaryl groups or aralkyl groups, it being possible for those groups to be substituted by one or more unsubstituted groups selected from alkyl, heteroalkyl, such as, for example, alkoxy, acyl or acyloxy, a carbocyclic group, heterocycloalkyl, aryl, heteroaryl and aralkyl, or are hydroxyl groups or glycosyloxy groups;
- n is an integer from 0 to 5;
- R5 is H, alkyl, heteroalkyl, a carbocyclic group, heterocycloalkyl, aryl, heteroaryl, heteroarylalkyl or aralkyl;
- R6 and R7 independently of each other are H, alkyl, heteroalkyl, a carbocyclic group, heterocycloalkyl, such as, for example, aryl-heterocycloalkyl, aryl, heteroaryl, aralkyl or heteroarylalkyl, it being possible for those groups to be substituted by one or more groups selected from alkyl, heteroalkyl, such as, for example, alkoxy, acyl or acyloxy, a carbocyclic group, heterocycloalkyl, aryl, heteroaryl, heteroarylalkyl, aralkyl, —OH and —NH2,
- or together form part of a heterocycloalkyl ring system, especially an arylheterocycloalkyl ring system, such as, for example, aryl-piperazinyl, or of a heteroaryl ring system, it being possible for those systems to be substituted by one or more groups selected from alkyl, heteroalkyl, such as, for example, alkoxy, acyl or acyloxy, a carbocyclic group, heterocycloalkyl, aryl, heteroaryl, heteroarylalkyl, aralkyl, —OH and —NH2;
- and
- R8 is H, alkyl, heteroalkyl, a carbocyclic group, heterocycloalkyl, aryl, heteroaryl, heteroarylalkyl or aralkyl or, together with R5, forms part of a heterocycloalkyl ring system;
- or a pharmacologically acceptable salt, solvate, hydrate or a pharmacologically acceptable formulation thereof.
12 more elements
Dependencies are inferred from the claim text.