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US 2011/0034516 A1Published application
Aminopyrazole derivatives
AssigneeActelion
InventorsDaniel Bur, Olivier Corminboeuf, Sylvaine Cren, Heinz Fretz, Corinna Grisostomi, Xavier Leroy, Julien Pothier, Sylvia Richard-Bildstein
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Abstract
The invention relates to aminopyrazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
Claims17
A compound of formula (I),
- wherein
- A represents a phenyl- or a monocyclic heterocyclyl-group including two substituents, wherein the two substituents are in a 1,3-arrangement;
- or A represents propan-1,3-diyl;
- E represents *-(C1-C4)alkyl-O—, —CH═CH— or
- wherein the asterisks indicate the bond which is linked to R1;
- Q represents O, or S;
- R3 represents hydrogen, (C1-C4)alkyl, cyclopropyl, (C1-C4)alkoxy-(C1-C2)alkyl, —CH2NH2, —CH2NHBoc, —CH2CH2C(O)OtBu or benzyl;
- R1 represents a heterocyclyl- or an aryl-group, which group is unsubstituted, mono-, di- or tri-substituted with
- halogen, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)fluoroalkyl, (C1-C4)fluoroalkoxy, phenyl, cyano, di-[(C1-C3)alkyl]-amino, —C(O)—NH2, —C(O)OtBu, (C1-C4)alkoxy-(C1-C2)alkyl, hydroxy-(C1-C2)alkyl or dimethylamino-(C1-C2)alkyl;
- and
- R2 represents —CO—(C1-C3)alkyl, —CO-cyclopropyl, —CF2—(C1-C3)alkyl, —CHF—(C1-C3)alkyl or —SO2—(C1-C3)alkyl;
- or a salt thereof.
9 more elements
(canceled)
Dependencies are inferred from the claim text.