Title:
NF-kappaB INHIBITORS
Document Type and Number:
WIPO Patent Application WO/2017/122209
Kind Code:
A3
Abstract:
Disclosed herein are compounds capable of inhibiting dimerization of NF- KB, for example, p65-p65 homodimerization and/or p50-p65 heterodimerization, the compounds being represented by formula I: X-L2-L1-L'2-Y Formula I wherein X, Y, Li, L 2and L' 2are as defined herein, the compound being for use in inhibiting dimerization of NF- KB. Further disclosed are compounds capable of disrupting a hydrophobic core domain of p65, for use in inhibiting dimerization of NF- KB comprising p65. Further disclosed herein is a method of identifying an inhibitor of NF- KB dimerization, utilizing a first NF- KB monomer attached to a first fragment of a luciferase protein and a second NF- KB monomer attached to a second fragment of a luciferase protein, wherein dimerization of the first NF- KB monomer and the second NF- KB monomer increases luciferase activity.
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Inventors:
DIKSTEIN RIVKA (IL)
ASHKENAZI SHAKED (IL)
ASHKENAZI SHAKED (IL)
Application Number:
PCT/IL2017/050043
Publication Date:
November 02, 2017
Filing Date:
January 12, 2017
Export Citation:
Assignee:
YEDA RES & DEV (IL)
International Classes:
C07D403/12; A61K31/41; A61K31/4192; A61K31/422; A61K31/4436; A61K31/4439; A61K31/444; A61K31/519; A61K31/5355; A61K31/5375; A61K31/542; C07D401/04; C07D401/14; C07D407/14; C07D413/14
Domestic Patent References:
| WO2011062955A2 | 2011-05-26 | |||
| WO2007073503A2 | 2007-06-28 | |||
| WO1997009315A1 | 1997-03-13 | |||
| WO1999065449A2 | 1999-12-23 | |||
| WO2006032322A1 | 2006-03-30 |
Foreign References:
| US20080227784A1 | 2008-09-18 | |||
| EP1535609A1 | 2005-06-01 |
Attorney, Agent or Firm:
EHRLICH, Gal et al. (IL)
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