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US 7,408,063 B2Granted
1,8-annelated quinoline derivatives substituted with carbon-linked triazoles as farnesyl transferase inhibitors
AssigneeJanssen Pharmaceutica NV
InventorsPatrick René Angibaud, Marc Gaston Venet
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Abstract
This invention comprises the novel compounds of formula (I) wherein r, s, A, X, Y1, Y2, R1, R2, R3, and R4 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
Claims5
A compound of formula (I):
- or a pharmaceutically acceptable salt or N-oxide or stereochemically isomeric form thereof, wherein
- -A- is a bivalent radical of formula selected from the group consisting of
- —CH2—CH2—;
- —CH2—CH2—CH2— and —CH2—O—;
- >Y1—Y2—is >C═CR5— wherein R5 is hydrogen or halo
- R1 is selected from the group consisting of hydrogen or halo;
- R2 is selected from the group consisting of hydrogen, halo, or cyano;
- R3 is selected from the group consisting of hydrogen, N-imidazolyl, —O—R6, and —NHR8;
- wherein
- R6 is selected from the group consisting of hydrogen, C1-6alkyl and hydroxyC1-6alkyl;
- R8 is selected from the group consisting of hydrogen and C1-6alkylcarbonyl;
- and
- R4 is hydrogen or C1-6alkyl.
10 more elements
An intermediate of formula (IVa):
- wherein:
- -A- is a bivalent radical of formula selected from the group consisting of
- —CH2—CH2—;
- —CH2—CH2—CH2—and —CH2—O—;
- >Y1—Y2—is>>C═CR5 is hydrogen or halo;
- R1 is selected from the group consisting of hydrogen or halo;
- R2 is selected from the group consisting of hydrogen, halo, or cyano;
- R4 is C1-6alkyl, and R21 is hydrogen or C1-6alkyl.
5 more elements
Dependencies are inferred from the claim text.