IP Library Granted Patent US 8,664,391
Granted Patent B2
US 8,664,391 · App. 13/122,817 · Granted Mar 4, 2014

Amide compounds as boosters of antivirals

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Quick Facts
Patent No.
US 8,664,391
App. No.
13/122,817
Granted
Mar 4, 2014
Kind
B2
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 R 1 is 5-thiazolyl or 3-pyridinyl; R 2 is iso-butyl, 2,2-dimethylpropyl; 2-hydroxy-2-methyl-propyl or cyclohexylmethyl; R 3 is phenyl optionally substituted with one or more halogens, trifluoromethyl, C 1-6 -alkyl or C 1-6 -alkoxy wherein optionally two of said alkoxy groups are be linked to each other to form a 5 or 6-membered ring; heteroaryl; C 3-7 cycloalkyl optionally substituted with one or more halogens; C 1-6 alkyl optionally substituted with heteroaryl; —O—CH 2 — (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.

Claims (2)

1. A compound having the formula (II)

or pharmaceutically acceptable salts and stereoisomers thereof.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 24, 2015
From: JANSSEN R & D IRELAND
To: JANSSEN SCIENCES IRELAND UC
Reel/Frame 035496/0382 →
CHANGE OF NAME Recorded Aug 21, 2013
From: TIBOTEC PHARMACEUTICALS LTD.
To: JANSSEN R&D IRELAND
Reel/Frame 031049/0748 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 6, 2011
From: JONCKERS, TIM HUGO MARIA; SCHEPENS, WIM BERT GRIET; HACHE, GEERWIN YVONNE PAUL; HALLENBERGER, BEATE SABINE; SASAKI, JENNIFER CHIYOMI; BAUMEISTER, JUDITH EVA; VAN'T KLOOSTER, GERBEN ALBERT ELEUTHERIUS
To: TIBOTEC BVBA
Reel/Frame 026083/0526 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 6, 2011
From: TIBOTEC BVBA
To: TIBOTEC PHARMACEUTICALS LTD.
Reel/Frame 026084/0065 →