1-Acyl-7-nitroindoline derivatives, their preparation and their use as photocleavable precursors

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United States of America Patent

PATENT NO 6765014
SERIAL NO

09936975

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Photoreleasable compounds comprising a caging moiety linked to an effector moiety represented by structural formula (I) wherein R.sub.1 is hydrogen; C.sub.1-10 alkyl or substituted alkyl; O(CH.sub.2).sub.n --Y; N(COZ)(CH.sub.2).sub.m Y; or N[(CH.sub.2).sub.m Y'[(CH.sub.2).sub.N Y]; R.sub.2 and R.sub.3 are independently selected from: hydrogen; C.sub.1-10 alkyl or substituted alkyl; or R.sub.2 and R.sub.3 together are cycloalkyl; R.sub.4 is hydrogen; C.sub.1-10 alkyl or substituted alkyl; phenyl or substituted phenyl; (CH.sub.2).sub.n Y; or (CH.sub.2).sub.m O(CH.sub.2).sub.n Y; wherein m and n are independently between 1 and 10; Y and Y' are independently selected from hydrogen, CO.sub.2 H or salts thereof or OPO.sub.3.sup.2-, Z is hydrogen or C.sub.1-10 alkyl or substituted alkyl; and, X is an effector moiety or a group capable of being coupled or converted to an effector moiety, which are capable of releasing the effector moiety on irradiation, typically by flash irradiation with UV light. The photoreleasable compounds can therefor be used to deliver biologically active effector moieties such as neuroactive amino acids or metal chelators to sites where their activity is required. ##STR1##

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Patent Owner(s)

  • MEDICAL RESEARCH COUNCIL

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Corrie, John Edgar Thomas Knebworth, GB 5 8
Papageorgiou, George New Barnet, GB 11 124

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