Synergistic compositions of N-acylhomoserine lactones and 4-quinolones

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United States of America Patent

PATENT NO 7371779
APP PUB NO 20040198978A1
SERIAL NO

10481373

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A composition having immunosuppressant activity comprises at least one compound of the formula (I) in which R is an acyl group of the formula (II) wherein one of R.sup.1 and R.sup.2 is H and the other is selected from OR.sup.4, SR.sup.4 and NHR.sup.4, wherein R.sup.4 is H or 1-6C alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are joined form a keto group, and R.sup.3 is a straight or branched chain, saturated or unsaturated aliphatic hydrocarbyl group containing from 8 to 11 carbon atoms and is optionally substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR.sup.5R.sup.6 wherein each of R.sup.5 and R.sup.6 is selected from H and 1-6C alkyl or R.sup.5 and R.sup.6 together with the N atom form a morpholino or piperazino group, or any enantiomer thereof; and at least one compound of the formula (III): wherein R.sup.7 is a straight or branched chain, saturated or ethylenically-unsaturated aliphatic hydrocarbyl group containing from 1 to 18 carbon atoms which may optionally be substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR.sup.12R.sup.13, wherein each of R.sup.12 and R.sup.13 is independently selected from H and 1-6C alkyl or R.sup.12 and R.sup.13 together with the N atom to which they are attached form a saturated heterocyclic group selected from piperidino, piperazino and morpholino; R.sup.8 is a group selected from H, --OH, halo, --CHO, --CO.sub.2H and CONHR.sup.14 wherein R.sup.14 is H or a 1-6C alkyl; each of R.sup.9, R.sup.10 and R.sup.11 is independently selected from H, --CH.sub.3, --OCH.sub.3 and halo; or a non-toxic pharmaceutically-acceptable salt thereof. The determined immunosuppressant activity of the composition is greater than the sum of the activities of the individual components of the composition when determined separately ##STR00001##

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Patent Owner(s)

  • SECRETARY OF STATE FOR DEFENCE, THE;THE SECRETARY OF STATE FOR DEFENSE SCIENCE AND TECHNOLOGY

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Pritchard, David Idris Leicestershire, GB 18 26

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