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US 7,442,705 B2Granted
HIV replication inhibiting pyrimidines and triazines
AssigneeTibotec Pharmaceuticals Ltd.
InventorsJerôme Emile Georges Guillemont, Elisabeth Thérese Jeanne Pasquier, Jan Heeres, Kurt Hertogs, Eva Bettens, Paulus Joannes Lewi, Marc René De Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers
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Abstract
This invention concerns HIV replication inhibitors of formula (I), The N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
Claims11
A compound of formula (I)
- a pharmaceutically acceptable acid addition salt, or a stereochemically isomeric form thereof, wherein
- -a1=a2-a3=a4- represents a bivalent radical of formula
- —CH═CH—CH═CH— (a-1);
- -b1-b2-b3- represents a bivalent radical of formula
- —O—CH2—CH2— (b-1);
- —O—CH═CH— (b-2);
- —CH2—CH═CH— (b-5);
- n is 1;
- m is 0, 1;
- q is 1,2;
- R1 is hydrogen;
- R2 is halo, nitro, cyano, —CONH2, C1-6alkyl optionally substituted with cyano or with —CONH2;
- X1 is —NH—, —O—;
- R3 is hydrogen, halo, C1-6alkyl;
- R4 is halo, C1-6alkyl;
- R13 and R14 each independently are hydrogen, C1-6alkyl;
- R17 is cyano, halo, C1-6alkyl optionally substituted with cyano;
- C2-6alkenyl optionally substituted with cyano;
- and, where possible, R17 may also be attached to the -b1-b2-b3-moiety by a double bond whereby R17 is ═O;
- the R17 moiety attached to a carbon atom in the -b1-b2-b3 ring;
- Q represents hydrogen;
- Z is C—Y, wherein Y is hydrogen or halo.
19 more elements
Dependencies are inferred from the claim text.