Janssen R&d Ireland

Beate Sabine Hallenberger

Tim Hugo Maria Jonckers

Judith Baumeister

Geerwin Yvonne Paul Haché

Wim Bert Griet Schepens

Gerben Albert Van 't Klooster

Jennifer Chiyomi Sasaki

The present invention relates to compounds of formula (I) that have CYP450 inhibiting properties and are useful as boosting agents when used with HIV treatments. These compounds are represented by formula including the salts and stereoisomeric forms thereof, wherein Ris 5-thiazolyl or 3-pyridinyl; Ris iso-butyl, 2,2-dimethylpropyl; 2-hydroxy-2-methyl-propyl or cyclohexylmethyl; Ris phenyl optionally substituted with one or more halogens, trifluoromethyl, C-alkyl or C-alkoxy wherein optionally two of said alkoxy groups are be linked to each other to form a 5 or 6-membered ring; heteroaryl; Ccycloalkyl optionally substituted with one or more halogens; Calkyl optionally substituted with heteroaryl; &#x2014;O&#x2014;CH&#x2014; (heteroaryl). As boosting agents they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered, or improve the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions comprising these compounds are also provided.

Amide compounds as boosters of antivirals

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.

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Bromskirchen, Germany

Beate Sabine Hallenberger