Depsipeptide Derivatives and their Therapeutic Use

Steven Joseph Shuttleworth; A. Ganesan; Alexander Richard Liam Cecil; Thomas Hill; Cyril Tomassi; Franck Alexandre Silva

Depsipeptide Derivatives and their Therapeutic Use

Steven Joseph Shuttleworth (Inventor), A. Ganesan (Inventor), Alexander Richard Liam Cecil (Inventor), Thomas Hill (Inventor), Cyril Tomassi (Inventor), Franck Alexandre Silva (Inventor)

Research output: Patent

Abstract

A compound of structure VII, VIII, IX or X wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 9 are the same or different and each represents an amino-acid side- chain moiety; each R 10 is the same or different and represents hydrogen or C 1 -C 6 alkyl, C 2 - C 6 alkenyl, C 2 -C 6 alkynyl or 5- or 6-membered aryl or heteroaryl; Pr is hydrogen or an alcohol protecting group; X1 and X2 _are the same or different and each represents a non-peptide moiety; and R 8 is a metallophile capable of binding with zinc in the active site of HDAC; with the proviso that X1 is not the group -CHR 1 -CH(OPr-)-CHR 9 -, wherein R 1 , Pr and R 9 are as defined above; and pharmaceutically acceptable salts thereof.

Original language	English
Patent number	WO/2009/022182
Publication status	Published - 2009

Cite this

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title = "Depsipeptide Derivatives and their Therapeutic Use",

abstract = "A compound of structure VII, VIII, IX or X wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 9 are the same or different and each represents an amino-acid side- chain moiety; each R 10 is the same or different and represents hydrogen or C 1 -C 6 alkyl, C 2 - C 6 alkenyl, C 2 -C 6 alkynyl or 5- or 6-membered aryl or heteroaryl; Pr is hydrogen or an alcohol protecting group; X1 and X2 _are the same or different and each represents a non-peptide moiety; and R 8 is a metallophile capable of binding with zinc in the active site of HDAC; with the proviso that X1 is not the group -CHR 1 -CH(OPr-)-CHR 9 -, wherein R 1 , Pr and R 9 are as defined above; and pharmaceutically acceptable salts thereof.",

author = "Shuttleworth, {Steven Joseph} and A. Ganesan and Cecil, {Alexander Richard Liam} and Thomas Hill and Cyril Tomassi and Silva, {Franck Alexandre}",

year = "2009",

language = "English",

type = "Patent",

note = "WO/2009/022182",

}

TY - PAT

T1 - Depsipeptide Derivatives and their Therapeutic Use

AU - Shuttleworth, Steven Joseph

AU - Ganesan, A.

AU - Cecil, Alexander Richard Liam

AU - Hill, Thomas

AU - Tomassi, Cyril

AU - Silva, Franck Alexandre

PY - 2009

Y1 - 2009

N2 - A compound of structure VII, VIII, IX or X wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 9 are the same or different and each represents an amino-acid side- chain moiety; each R 10 is the same or different and represents hydrogen or C 1 -C 6 alkyl, C 2 - C 6 alkenyl, C 2 -C 6 alkynyl or 5- or 6-membered aryl or heteroaryl; Pr is hydrogen or an alcohol protecting group; X1 and X2 _are the same or different and each represents a non-peptide moiety; and R 8 is a metallophile capable of binding with zinc in the active site of HDAC; with the proviso that X1 is not the group -CHR 1 -CH(OPr-)-CHR 9 -, wherein R 1 , Pr and R 9 are as defined above; and pharmaceutically acceptable salts thereof.

AB - A compound of structure VII, VIII, IX or X wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 9 are the same or different and each represents an amino-acid side- chain moiety; each R 10 is the same or different and represents hydrogen or C 1 -C 6 alkyl, C 2 - C 6 alkenyl, C 2 -C 6 alkynyl or 5- or 6-membered aryl or heteroaryl; Pr is hydrogen or an alcohol protecting group; X1 and X2 _are the same or different and each represents a non-peptide moiety; and R 8 is a metallophile capable of binding with zinc in the active site of HDAC; with the proviso that X1 is not the group -CHR 1 -CH(OPr-)-CHR 9 -, wherein R 1 , Pr and R 9 are as defined above; and pharmaceutically acceptable salts thereof.

M3 - Patent

M1 - WO/2009/022182

ER -