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US 2006/0211656 A1Published application
Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators
AssigneeNovartis AG
InventorsRainer Albert, Claus Ehrhardt, Peter Ettmayer, Klaus Hinterding, Klemens Högenauer, Peter Nussbaumer
Life of this patent
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Abstract
Compounds of formula I, wherein X, a, b, R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
Claims10
A compound of formula I
- wherein
- R1 is C1-6alkyl;
- C1-6alkyl substituted by hydroxy, C1-2alkoxy, or 1 to 6 fluorine atoms;
- C2-6alkenyl;
- or C2-6alkynyl;
- X is O, CH2, C═O or direct bond;
- R2 is optionally substituted C1-7alkyl, optionally substituted C1-7alkenyl, optionally substituted C1-7alkinyl, optionally substituted C3-6cycloalkyl, optionally substituted phenyl, or optionally substituted heteroaryl,
- wherein the substituted C1-7alkyl, C1-7alkenyl, C1-7alkinyl or C3-6cycloalkyl has 1 to 5 substitutents selected from hydroxyl, halogen, C1-4alkyl, C1-4alkoxy, C1-4alkoxy substituted by 1 to 5 halogen atoms, C3-6cycloalkyl, C3-6cycloalkoxy, C3-6cycloalkylC1-5alkyl, C3-6cycloalkoxyC1-5alkyl, cyano, optionally substituted phenyl, optionally substituted phenyloxy, optionally substituted heteroaryl, optionally substituted heteroaryloxy, optionally substituted heterocyclic residue optionally attached via oxygen;
- and wherein each of phenyl, phenyloxy, heteroaryl, heteroaryloxy, heterocyclic residue optionally attached via oxygen, independently may be substituted with 1 to 5 substituents selected from hydroxyl, halogen, C1-4alkyl, C1-4alkyl substituted by 1 to 5 fluorine atoms, C1-4alkoxy, C1-4alkoxy substituted by 1 to 5 fluorine atoms, cyano, phenyl, and phenyl substituted by 1 to 5 substituents selected from hydroxyl, halogen, C1-4alkyl, C1-4alkyl substituted by 1 to 5 fluorine atoms, C1-4alkoxy, C1-4alkoxy substituted by 1 to 5 fluorine atoms, and cyano;
- or each of phenyl, phenyloxy, heteroaryl, heteroaryloxy, heterocyclic residue optionally attached via oxygen independently may be fused to a heterocyclic residue;
- R3 is Z-X2 wherein Z is CH2, CHF or CF2 and X2 is OH or a residue of formula (a)
- wherein Z1 is a direct bond, CH2, CHF, CF2 or O, and each of R6 and R7, independently is H, C1-4alkyl optionally substituted by 1, 2 or 3 halogen atoms, or benzyl;
- and
- each of R4 and R5, independently, is H, C1-4alkyl optionally'substituted by 1, 2 or 3 halogen atoms, or acyl;
- each of anellated rings a and b is independently C5-6cycloalkyl, aryl, a heterocyclic residue, or heteroaryl;
- in free form or in salt form.
13 more elements
Dependencies are inferred from the claim text.