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US 2007/0179151 A1Published application
Isoquinoline aminopyrazole derivatives
AssigneeHoffmann-La Roche Inc.
InventorsLi Chen, Guy Georges, Alfred Mertens, Xihan Wu
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Abstract
The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of such compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
Claims75
Compounds of formula I and all pharmaceutically acceptable salts or esters thereof wherein formula I is:
- wherein:
- (a) R1 is hydrogen, alkyl or cycloalkyl;
- (b) R2 is hydrogen or alkyl;
- (c) R3 is selected from the group consisting of:
- (1) unsubstituted alkyl,
- (2) alkyl which is substituted one or two times with —C(O)O-alkyl, heteroaryl, phenyl, heterocyclyl or cycloalkyl,
- (3) alkyl wherein one or more —CH2-groups are replaced by oxygen,
- (4) aryl which is optionally substituted one or more times with halogen, alkyl, halogenated alkyl, halogenated alkoxy, cyano, —C(O)-alkyl, —NH—C(O)-alkyl, —C(O)OH, —C(O)O-alkyl, unsubstituted alkoxy, alkoxy substituted by heterocyclyl, or —NR2,
- (5) heteroaryl which is optionally substituted one or more times with alkyl,
- (6) cycloalkyl, and
- (7) heterocyclyl;
- (d) R3a is hydrogen, alkyl or alkoxy;
- (e) R4 is hydrogen, alkyl, alkoxy, halogen, cyano, —C(O)NR2,
- —(CH2)n—Y—R7 or -Z-R8;
- (f) R5 is hydrogen, alkyl, alkoxy, halogen, cyano, —C(O)NR2, —(CH2)n—Y—R7 or -Z-R8;
- and R6 is hydrogen, alkyl, alkoxy, halogen or cyano;
- or alternatively R5 and R6 form together with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring;
- (g) X is a single bond, —NR—, —O—, —S—, —C(O)— or —C(O)NR—;
- (h) Y is —O—, —NR—, —S—, —S(O)2NR—, —NRC(O)—, —NRC(O)O— or —C(O)NR—;
- (i) Z is —C(O)—, —O—, a single bond or alkylene;
- (j) R7 is cycloalkyl;
- or alkyl, which is optionally substituted one or more times by alkoxy, hydroxy, alkylsulfonyl, heterocyclyl or —NR2;
- (k) R8 is heterocyclyl;
- (l) R is hydrogen or alkyl;
- and
- (m) n is 0, 1, 2 or 3.
23 more elements
Dependencies are inferred from the claim text.