Patent(s) and the Corresponding Patented Drug(s) |
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World Intellectual Property Organization (WIPO) |
Patent ID |
WO2010043866 |
Title |
Histone Lysine Demethylase Inhibitors. |
Abstract |
The invention provides a compound which is an iV-oxalylglycine derivative of formula (I): a hydroxamic acid derivative of formula (II): or a heteroaryl derivative of fomula (III): wherein n; Z1; Z2; Y1; Y2; A; p; X1; X2; m; R4; B; R5; R6; R7; R8; R9; X3; R10; R11 and R12 are as defined herein, or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of the human 2-oxoglutarate-dependant JMJD2 subfamily of histone demethylases, in particular JMJD2E. Such inhibitors are useful in changing the epigenetic state of cells resulting in the inhibition / activation of chromatin remodelling, multiple gene activation / deactivation, and in treating cancer and other conditions characterised by undesirable cellular proliferation, and psychiatric disorders including depression. |
Applicant(s) |
Isis Innovation Limited |
Representative Drug(s) |
D02URA |
Drug Info
|
IC50 = 1400 nM |
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[1] |
2
|
D0R1OG
|
Drug Info
|
IC50 = 1500 nM
|
[1] |
3
|
D0K2OT
|
Drug Info
|
IC50 = 3600 nM
|
[1] |
4
|
D0G8SB
|
Drug Info
|
IC50 = 3800 nM
|
[1] |
5
|
D0ZW5H
|
Drug Info
|
IC50 = 4500 nM
|
[1] |
6
|
D0J1OK
|
Drug Info
|
IC50 = 4800 nM
|
[1] |
7
|
D0B5WF
|
Drug Info
|
IC50 = 6600 nM
|
[1] |
8
|
D0B7GQ
|
Drug Info
|
IC50 = 8000 nM
|
[1] |
9
|
D0C1CV
|
Drug Info
|
IC50 = 27000 nM
|
[1] |
10
|
D01IYF
|
Drug Info
|
N.A.
|
[1] |
11
|
D07GAP
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2014053491 |
Title |
Inhibitors of Histone Demethylases. |
Abstract |
The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form (I). |
Applicant(s) |
Epither Apeutics Aps |
Representative Drug(s) |
D05YBG |
Drug Info
|
N.A. |
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[1] |
2
|
D06XXJ
|
Drug Info
|
N.A.
|
[1] |
3
|
D0EY9Y
|
Drug Info
|
N.A.
|
[1] |
4
|
D0J6OC
|
Drug Info
|
N.A.
|
[1] |
5
|
D0YZ1B
|
Drug Info
|
N.A.
|
[1] |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US20130137720 |
Title |
Histone Demethylase Inhibitors and Methods for Using The Same. |
Representative Drug(s) |
D0B4VO |
Drug Info
|
N.A. |
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[1] |
2
|
D0TH2W
|
Drug Info
|
N.A.
|
[1] |
Japan Patent Office (JPO) |
Patent ID |
JP2011168581 |
Title |
Preparation of Hydroxamic Acid Derivatives As Jhdm Inhibitors. |
Representative Drug(s) |
D05HBS |
Drug Info
|
N.A. |
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[1] |
2
|
D0K1PP
|
Drug Info
|
N.A.
|
[1] |