Amide compounds as boosters of antivirals
AssigneeTibotec BVBA
InventorsTim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
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Abstract
The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions are also provided.
Claims16
A compound of the formula
- the salts and stereoisomeric forms thereof, wherein
- R is H, phenyl, pyridyl, C1-6alkyl or
- wherein A and B are independently from each other H;
- C1-6alkyl optionally substituted with alkynyl, heteroaryl or a heteroatom selected from nitrogen, oxygen or sulfur which is optionally substituted with C1-6alkyl;
- or wherein A and B together with the nitrogen to which they are attached form a 5 or 6 membered saturated, partially or completely unsaturated heterocyclic ring containing 1 to 4 hetero atoms each independently selected from nitrogen, oxygen or sulfur, said heteroatoms are optionally substituted with C1-6alkyl;
- R1 is selected from the group comprising
- R2 is C1-6alkyl optionally substituted with OH, aminoalkyl, pyrrolidinyl, morpholinyl, alkynyl or C3-7cycloalkyl optionally substituted with halogen;
- R3 is OH;
- R4 is H or alkyl;
- R5 is pyridyl or phenyl optionally substituted with halogen;
- X is O, S or N optionally substituted with C1-6alkyl.
5-6. (canceled)
11-12. (canceled)
Dependencies are inferred from the claim text.