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US 6,642,386 B2Granted
N-(4-carbamimidoyl-phenyl)-glycine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsLeo Alig, Katrin Groebke Zbinden, Ulrike Obst
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Abstract
The invention is concerned with water soluble N-(4-carbamimidoyl-phenyl)-glycine derivatives of formula (I) wherein R1 to R4 and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.
Claims39
A compound of the formula:
- wherein
- R1 is lower-alkoxy;
- R2 is halogen;
- R3 is piperidinyl or piperidinyl substituted with lower-alkyl, hydroxy-lower-alkyl, carboxy-lower-alkyl or lower-alkoxy-carbonyl-lower-alkyl;
- R4 is hydrogen or lower-alkyl;
- A is —(CH2)n— or —(CH2)n— which is substituted with lower-alkyl;
- and
- n is 0 to 3;
- or a pharmaceutically acceptable salt thereof.
6 more elements
A compound of the formula:
- wherein
- R1 is lower-alkoxy;
- R2 is halogen;
- R3 is piperidinyl or piperidinyl substituted with lower-alkyl, hydroxy-lower-alkyl, carboxy-lower-alkyl or lower-alkoxy-carbonyl-lower-alkyl;
- R4 is hydrogen or lower-alkyl;
- A is —(CH2)n— or —(CH2)n— which is substituted with lower-alkyl;
- and
- n is 0 to 3;
- or a pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.