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 -