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US 8,283,356 B2Granted
2,4- Di(hetero)-arylamino-pyrimidine derivatives as ZAP-70 and/or SYK inhibitors
AssigneeNovartis AG
InventorsRolf Baenteli, Marie Claude Bernhard, Peter Buehlmayer, Nigel Graham Cooke, Rudolf Duthaler, Klaus Hinterding, Gebhard Thoma, Maurice Van Eis, Anette Von Matt, Louis Walliser, Gerhard Zenke
Life of this patent
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Abstract
Disclosed are pyrimidine derivatives of formula wherein R0, R1, R3 to R9, and Z have a signification as indicated in claim 1, which have interesting pharmaceutical properties.
Claims11
A compound of formula I
- wherein
- Z is ═CR2;
- R0 is hydrogen;
- R1 and R2 form together with the C-atoms to which they are attached a 5 to 15 membered non-aromatic carbocyclyl or heterocyclyl, wherein said heterocyclyl contains 1 to 5 heteroatoms selected from N, O and S;
- or R1 is hydrogen;
- and R2 is C1-4-alkoxy;
- R3 is —SO2NH2;
- R4 and R6 are hydrogen;
- R5 is hydrogen;
- halogen;
- C1-4alkyl;
- or CF3;
- one of R7, R8 and R9 is NR10R11 and one of the two others is hydrogen, halogen, COOH, CF3 or C1-4 alkyl;
- and the third one is H;
- one of R10 and R11, is hydrogen or C1-4alkyl and the other is hydrogen;
- C1-8-alkyl, C1-8-alkyl terminally substituted by OH, C3-6-cycloalkyl or a heterocyclic ring;
- C2-8alkenyl;
- C3-8-cycloalkyl;
- C1-8alkoxyC1-4-alkyl;
- hydroxyC1-8alkoxyC1-8alkyl;
- or a 5 membered heterocyclic ring;
- or a salt thereof.
19 more elements
A compound of formula X1
- wherein R5, R7, R8, R9 and R14 are as defined in Table 1:
- TABLE 1
- R5
- R7
- R8
- R9
- R14
- H
- —NHCH3
- H
- H
- H
- H
- —CH3
- —NHCH3
- H
- H
- H
- —NH—(CH2)2—OCH3
- —CH3
- H
- H
- H
- —NHCH3
- —CH2—CH3
- H
- H
- H
- —NHCH3
- F
- H
- H
- H
- —NHCH3
- Cl
- H
- H
- H
- —NHCH3
- Br
- H
- H
- H
- —CF3
- NH2
- H
- H
- H
- —CF3
- —NHCH3
- H
- H
- H
- —COOH
- —NH2
- H
- H
- H
- —NHCH2CH3
- —CH3
- H
- H
- H
- —NHCH2CH2CH3
- —CH3
- H
- H
- H
- —NHCH2CH2CH2OCH3
- —CH3
- H
- H
- H
- —CH3
- —NH—CH2CH3
- H
- H
- H
- —CH3
- —NH—CH2CH2CH3
- H
- H
- or a salt thereof.
80 more elements
A compound of formula X7
- wherein R7, R8, R9 and R16 are as defined in Table 6:
- TABLE 6
- R16
- R7
- R8
- R9
- —CH3
- —NHCH3
- H
- H
- —CH3
- NHCH2CH2OCH3
- CH3
- H
- —CH3
- —NHCH3
- F
- H
- —CH3
- —NHCH3
- Cl
- H
- —CH3
- —NHCH3
- Br
- H
- —CH3
- CF3
- NH2
- H
- —CH3
- COOH
- NH2
- H
- —CH3
- NHCH2CH3
- CH3
- H
- —CH3
- NHCH2CH2CH3
- CH3
- H
- —CH3
- NHCH2CH2CH2OCH3
- CH3
- H
- —CH3
- CH3
- NHCH2CH3
- H
- —CH3
- CH3
- —NHCH2CH2CH3
- H
- or a salt thereof.
52 more elements
Dependencies are inferred from the claim text.