EP 2293845 A1 20110316 - DEPSIPEPTIDES AND THEIR THERAPEUTIC USE
Title (en)
DEPSIPEPTIDES AND THEIR THERAPEUTIC USE
Title (de)
DEPSIPEPTIDE UND IHRE THERAPEUTISCHE VERWENDUNG
Title (fr)
DEPSIPEPTIDES ET LEUR UTILISATION THÉRAPEUTIQUE
Publication
Application
Priority
- GB 2009050553 W 20090522
- GB 0809330 A 20080522
- GB 0809326 A 20080522
- US 17409209 P 20090430
Abstract (en)
[origin: GB2460178A] Spiruchostatin derivatives and their therapeutic use Depsipeptide spiruchostatin analogues of the general formula (IX) or (X), isosteres or pharmaceutically acceptable salts thereof, useful in the inhibition of histone deacetylase (HDAC), wherein X is -C(=O)N(R10)-or-CH(OPr3)-; R7and R9are independently hydrogen or a natural or unnatural amino acid side chain moiety; each R10 is independently hydrogen, C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl; Pr1and Pr2are independently hydrogen or a thiol protecting group; Pr3is hydrogen or an alcohol protecting group; R1and R5 are independently Y wherein Y is a substitutent, or a natural or unnatural amino acid side chain moiety provided that R1and R5are not both a natural or unnatural amino acid side chain moiety. The use of such compounds in treatment of cancer, cardiac hypertrophy, chronic heart failure, an inflammatory condition, a cardiovascular disease, a haemoglobinpathy, a thalassemia, a sickle cell disease, a CNS disorder, an autoimmune disease, diabetes, osteoporosis, MDS, benign prostatic hyperplasia, endometriosis, oral leukoplakia, a genetically related metabolic disorder, an infection, Rubens-Taybi, fragile X syndrome or alpha-1 antitrypsin deficiency is also outlined. Methods for assaying HDAC inhibition and pharmaceutical compositions comprising such compounds are also provided.
IPC 8 full level
A61P 35/00 (2006.01); C07K 5/02 (2006.01); C07K 5/10 (2006.01); C07K 5/107 (2006.01); C07K 5/11 (2006.01); C07K 5/113 (2006.01); C07K 5/117 (2006.01)
CPC (source: EP GB)
A61K 38/15 (2013.01 - GB); A61P 3/00 (2018.01 - EP); A61P 7/00 (2018.01 - EP); A61P 9/00 (2018.01 - EP); A61P 15/02 (2018.01 - EP); A61P 17/06 (2018.01 - EP); A61P 17/10 (2018.01 - EP); A61P 19/10 (2018.01 - EP); A61P 25/00 (2018.01 - EP); A61P 29/00 (2018.01 - EP); A61P 35/00 (2018.01 - EP); A61P 37/00 (2018.01 - EP); C07K 5/02 (2013.01 - EP); C07K 5/1016 (2013.01 - EP); C07K 5/1019 (2013.01 - EP); C07K 5/1021 (2013.01 - EP); C07K 5/1024 (2013.01 - EP); C07K 11/02 (2013.01 - GB); Y02P 20/55 (2015.11 - EP)
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA RS
DOCDB simple family (publication)
GB 0908868 D0 20090701; GB 2460178 A 20091125; GB 2460178 B 20100818; EP 2293845 A1 20110316; WO 2009141657 A1 20091126
DOCDB simple family (application)
GB 0908868 A 20090522; EP 09750135 A 20090522; GB 2009050553 W 20090522