5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide...

Details 5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide... 5-amino 4-hydroxy-7-(1H-indolmethyl)-8-methylnonamide...

2005-03-17

2010-12-14

Havlin, Robert (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C514S336000

Reexamination Certificate

active

07851634

ABSTRACT:
The application relates to novel alkanamides of the general formula (I) where X is —CH2— or >CH—OH; (A) R1is e.g. an optionally substituted heterocyclyl radical or an optionally substituted polycyclic, unsaturated hydrocarbon radical where X is hydroxymethylene; R2is C1-C6-alkyl or C3-C6-cydoalkyl; R3are each independently H, C1-C6-alkyl, C1-6-alkoxycarbonyl or C1-C6-alkanoyl; R4is C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl or unsubstituted or substituted arylC1-C6-alkyl; R5is C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkanoyloxy C1-C6-alkyl, C1-C6-aminoalkyl, C1-C6-alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-C1-C6-alkyl, C1-C6-alkanoylamido-C1-C6-alkyl, HO(O)C—C1-C6-alkyl, C1-C6-alkyl-O—(O)C—C1-C6-alkyl, H2N—C(O)—C1-C6-alkyl, C1-C6-alkyl-HN—C(O)—C1-C6-alkyl, (C1,-C6-alkyl)2N—C(O)—C1-C6-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, cyano-C1-C6-alkyl, halo-C1-C6-alkyl, optionally substituted aryl-Co-C6-alkyl, optionally substituted C3-C8-cycloalkyl-Co-C6-alkyl or optionally substituted heterocydyl-Co-C6-alkyl; to a process for their preparation and to the use of these compounds as medicines, especially as renin inhibitors for the treatment of hypertension.

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CAPLUS abstract of WO 9106561.
Goeschke et al. (CAPLUS Abstract Accession No. 1995:995373 (of patent family including EP 678503).
Kubinyi (3D QSAR in Drug Design: Ligand-Protein Interactions and Molecular Similarity, vol. 2-3, Springer, 1998, 800 pages), table of contents and pp. 243-244.

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