Back to results
US 2006/0235056 A1Published application
Novel 3,4-disubstituted 1,2,3,6-tetrahydropyridine derivatives
OwnerOlivier Bezencon, Daniel Bur +4inventors
InventorsOlivier Bezencon, Daniel Bur, Walter Fischli, Lubos Remen, Sylvia Richard-Bildstein, Thomas Weller
Life of this patent
Estimating the term…
Abstract
The invention relates to novel 3,4-disubstituted 1,2,3,6-tetrahydropyridine 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
- X and W represent independently a nitrogen atom or a CH-group;
- V represents —(CH2)r—;
- -A-(CH2)s—;
- —CH2-A-(CH2)t;
- —(CH2)s-A-;
- —(CH2)2-A-(CH2)u—;
- -A-(CHF)v—B—;
- —CH2—CH2—CH2-A-CH2—;
- -A-CH2—CH2—B—CH2—;
- —CH2-A-CH2—CH—B—;
- —CH2—CH2—CH2-A-CH2—CH2—;
- —CH-2-CH2—CH2—C12-A-CH2—;
- -A-CH2—CH2—B—CH2—CH2—;
- —CH2-A-CH2—CH2—B—CH2—;
- —CH2-A-CH2—CH2—CH2—B—;
- or —CH2—CH2-A-CH2—CH2—B—;
- A and B independently represent —O—;
- —S—;
- —SO—;
- or —SO2—;
- U represents aryl;
- or heteroaryl;
- T represents —CONR1—;
- —(CFL)pOCO—;
- —(CH2)pN(R1)CO—;
- —(CH2)pN(R1)SO2—;
- —COO—;
- —(CH2)pOCONR1—;
- or —(CH2)pN(R1′)CONR1—;
- Q represents lower alkylene;
- or lower alkenylene;
- M represents hydrogen;
- cycloalkyl;
- aryl;
- heterocyclyl;
- heteroaryl;
- aryl-O(CH2)vR2;
- heteroaryl-O(CH2)vR2;
- aryl-O(CH2)2O(CH2)wR2;
- heteroaryl-(CH)2O(CH)wR2;
- aryl-OCH2CH(R5)CH2;
- or heteroaryl-OCHCH(R5)CH2R2;
- R1 and R1′ independently represent hydrogen;
- lower alkyl;
- lower alkenyl;
- lower alkinyl;
- cycloalkyl;
- aryl;
- or cycloalkyl-lower alkyl;
- R2 represents —OH, lower alkoxy, —OCOR3, —COOR3, —NR3R3, —OCONR3R3′, —NCONR3R3′, cyano, —CONR3R3′, SO3H, —SONR3R31, —CO-morpholin-4-yl, —CO-((4-loweralkyl)piperazin-1-yl), —NH(NH)NH2, or —NR4R4′, with the proviso that a carbon atom is attached at the most to one heteroatom in case this carbon atom is sp3-hybridized;
- R3 and R3′ independently represent hydrogen;
- lower alkyl;
- lower alkenyl;
- cycloalkyl;
- or cycloalkyl-lower alkyl;
- R4 and R4′ independently represent hydrogen;
- lower alkyl;
- cycloalkyl;
- cycloalkyl-lower alkyl;
- hydroxy-lower alkyl;
- —COOR2;
- or —CONe;
- R5 represents —OH, —OR2;
- —OCOR2;
- —OCOOR2;
- or R5 and R2 form together with the carbon atoms to which they are attached a 1,3-dioxolane ring which is substituted in position 2 with R3 and R3′;
- or R5 and R2 form together with the carbon atoms to which they are attached a 1,3-dioxolan-2-one ring;
- p is the integer 1, 2, 3 or 4;
- r is the integer 3, 4, 5, or 6;
- s is the integer 2, 3, 4 or 5;
- t is the integer 1, 2, 3 or 4;
- u is the integer 1, 2 or 3;
- v is the integer 2, 3 or 4;
- and
- w is the integer 1 or 2L
- 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.
75 more elements
(canceled)
(canceled)
Dependencies are inferred from the claim text.