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US 6,476,264 B2Granted
N-(4-carbamimidoyl-phenyl)-glycine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsJean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
Life of this patent
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Abstract
The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
Claims3
A compound of the formula:
- wherein R1 is hydrogen;
- E is hydrogen;
- X1 is the group C(Ra);
- X2 is the group C(Rb);
- X3 is the group C(Rc);
- X4 is the group C(Rdd);
- Ra is hydrogen, carbanoylalkoxy, hydroxyalkoxy, or halogen;
- Rb is hydrogen, alkenyl, alkynyl, alkoxy, or alkyl;
- Rc is hydrogen, alkoxy, mono- or di-alkylaminoalkoxy, or hydroxyalkoxy;
- Rd is hydrogen, alkoxy, hydroxycycloalkoxy, mono- or di-alkylaminoalkoxy, or an unsubstituted or substituted heterocyclic substituent selected from the group of morpholinylalkyl, piperidinyloxy, pyridinylaminoalkyl, pyrrolidinylalkyl and tetrahydropyranyloxy, with the subtituent on the substituted heterocyclic substituent being alkyl or alkylsulphonyl;
- and G1 and G2 are each hydrogen.
8 more elements
A compound of the formula:
- wherein R1 is hydrogen or the residue of an ester group that is cleavable under physiological conditions;
- E is hydrogen;
- X1 is the group C(Ra);
- X2 is the group C(Rb);
- X3 is the group C(Rc);
- X4 is the group C(Rdd);
- Ra is hydrogen, carbanoylalkoxy, hydroxyalkoxy, or halogen;
- Rb is hydrogen, alkenyl, alkynyl, alkoxy, or alkyl;
- Rc is hydrogen, alkoxy, mono- or di-alkylaminoalkoxy, or hydroxyalkoxy;
- Rd is hydrogen, alkoxy, hydroxycycloalkoxy, mono- or di-alkylaminoalkoxy, or an unsubstituted or substituted heterocyclic substituent selected from the group of morpholinylalkyl, piperidinyloxy, pyridinylaminoalkyl, pyrrolidinylalkyl and tetrahydropyranyloxy, with the subtituent on the substituted heterocyclic substituent being alkyl or alkylsulphonyl;
- and one of G1 and G2 is hydrogen or hydroxy and the other is hydrogen.
8 more elements
Dependencies are inferred from the claim text.