Invention Grant
- Patent Title: Amide compounds as boosters of antivirals
- Patent Title (中): 酰胺化合物作为抗病毒药物的助剂
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Application No.: US13122817Application Date: 2009-10-07
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Publication No.: US08664391B2Publication Date: 2014-03-04
- Inventor: Tim 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
- Applicant: Tim 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
- Applicant Address: IE Little Island Co, Cork
- Assignee: Janssen R&D Ireland Ltd
- Current Assignee: Janssen R&D Ireland Ltd
- Current Assignee Address: IE Little Island Co, Cork
- Agent Michael J. Atkins
- Priority: EP08166004 20081007
- International Application: PCT/EP2009/062996 WO 20091007
- International Announcement: WO2010/040762 WO 20100415
- Main IPC: C07D241/36
- IPC: C07D241/36

Abstract:
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 R1 is 5-thiazolyl or 3-pyridinyl; R2 is iso-butyl, 2,2-dimethylpropyl; 2-hydroxy-2-methyl-propyl or cyclohexylmethyl; R3 is phenyl optionally substituted with one or more halogens, trifluoromethyl, C1-6-alkyl or C1-6-alkoxy wherein optionally two of said alkoxy groups are be linked to each other to form a 5 or 6-membered ring; heteroaryl; C3-7cycloalkyl optionally substituted with one or more halogens; C1-6alkyl optionally substituted with heteroaryl; —O—CH2— (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.
Public/Granted literature
- US20110195969A1 AMIDE COMPOUNDS AS BOOSTERS OF ANTIVIRALS Public/Granted day:2011-08-11
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