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US 2006/0223795 A1Published application
Novel diazabicyclononene derivatives
OwnerOliver Bezencon, Daniel Bur +5inventors
InventorsOliver Bezencon, Daniel Bur, Walter Fischli, Lubos Remen, Sylvia Richard-Bildstein, Thomas Weller, Thierry Sifferlen
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Abstract
The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
Claims12
A compound of formula I
- wherein
- W is a six-membered, non benzofused, phenyl or heteroaryl ring, substituted by V in meta or para position;
- V represents —O—CH2—CH(OCH3)—CH2—O:
- —O—CH2—CH(CH3)—CH2—O—1;
- —O—CH2—CH(CF3)—CH2—O—;
- —O—CH2—C(CH3)2—O—;
- —O—C(CH3)2—CH2—1O—;
- —O—CH2—CH(CH3)—O—;
- —O—CH(CH3)—CH2—O—;
- —O—CH2—C(CH2CH2)—O—;
- or —O—C(CH2CH2)—CH12—O—;
- U represents aryl;
- or heteroaryl;
- T represents —CONR1—;
- —(CH2)pOCO—;
- —(CH2)pN(R1)CO—;
- —(CH2)pN(R1)SO2—;
- or —COO—;
- Q represents lower alkylene;
- or lower alkenylene;
- M represents hydrogen;
- cycloalkyl;
- aryl;
- heterocyclyl;
- or heteroaryl;
- L represents —R3;
- —COR3;
- —COOR3;
- —CONR2R3;
- —SO2R3;
- —SO2NR2R3;
- or —COCH(Aryl)2;
- R1 represents hydrogen;
- lower alkyl;
- lower alkenyl;
- lower alkinyl;
- cycloalkyl;
- aryl;
- or cycloalkyl-lower alkyl;
- R2 and R2′ independently represent hydrogen;
- lower alkyl;
- lower alkenyl;
- cycloalkyl;
- or cycloalkyl-lower alkyl;
- R3 represents hydrogen;
- lower alkyl;
- lower alkenyl;
- cycloalkyl;
- aryl;
- heteroaryl;
- heterocyclyl;
- cycloalkyl-lower alkyl;
- aryl-lower alkyl;
- heteroaryl-lower alkyl;
- heterocyclyl-lower alkyl;
- aryloxy-lower alkyl;
- or heteroaryloxy-lower alkyl, whereby these groups may be unsubstituted or mono- di- or trisubstituted with hydroxy, —OCOR2, —COOR2, lower alkoxy, cyano, —CONR2R2′, —CO-morpholin-4-yl, —CO-((4-loweralkyl)piperazin-1-yl), —NH(NH)NH2, —NR4R4′ or lower alkyl with the proviso that a carbon atom is attached at the most to one heteroatom in case this carbon atom is sp3-hybridized;
- R4 and R4′ independently represent hydrogen;
- lower alkyl;
- cycloalkyl;
- cycloalkyl-lower alkyl;
- hydroxy-lower alkyl;
- —COOR2;
- or —CONH2;
- k is the integer 0 or 1;
- m and n represent the integer 0 or 1, with the proviso that in case m represents the integer 1, n is the integer 0, in case n represents the integer 1, m is the integer 0;
- and in case k represents the integer 0, n represents the integer 0;
- and
- p is the integer 1, 2, 3 or 4;
- or optically pure enantiomers, racemates, diastereomers, mixtures of diastereomers, diastereomeric racemates, mixtures of diastereomeric racemates, or the meso-form of the compound:
- or pharmaceutically acceptable salts, solvent complexes or morphological forms of the compound.
68 more elements
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(canceled)
Dependencies are inferred from the claim text.