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Title:
HISTONE DEACETYLASE INHIBITOR PRODRUG
Document Type and Number:
Japanese Patent JP2012092121
Kind Code:
A
Abstract:

To provide an aqueous prodrug of a histone deacetylase (HDAC) inhibitor of a hydroxamic acid base.

Suberoylanilide hydroxamic acid derivative is expressed by formula (4). In formula (4), Ra is CORb, and Rb is hydrogen, un-substituted or substituted alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclyl, heteroaryl, alkylaryl, alkyl cycloalkyl, alkyl heterocyclyl, alkyl heteroaryl, or an amino acid residue selected from alanine, arginine and asparagine.


Inventors:
MILLER THOMAS A
WITTER DAVID J
BELVEDERE SANDRO
Application Number:
JP2011268666A
Publication Date:
May 17, 2012
Filing Date:
December 08, 2011
Export Citation:
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Assignee:
MERCK HDAC RES LLC
International Classes:
C07D213/80; A61K31/16; A61K31/165; A61K31/167; A61K31/27; A61K31/44; A61K31/455; A61P35/00; A61P43/00; C07C259/06; C07C271/22; C07D213/00; C07D213/82; C07D215/38; C07D215/40; C07D215/42
Domestic Patent References:
JP4993374B22012-08-08
JP2003509343A2003-03-11
JP2003518060A2003-06-03
JP2003226680A2003-08-12
JPH06509338A1994-10-20
JP2002128769A2002-05-09
Foreign References:
GB2279345B
Other References:
JPN6013023560; LEE,M.J. et al: 'Prodrugs of nitroxyl as inhibitors of aldehyde dehydrogenase' Journal of Medicinal Chemistry Vol.35, No.20, 1992, p.3648-52
Attorney, Agent or Firm:
Yoshikazu Iwase
Makoto Ono
Kenkyo Kanayama
Mitsuaki Tsubokura
Kazuki Shigemori
Yasufumi Shiroyama
Kenji Ando