US2018153830A1PendingUtilityA1
Selective inhibitors of undifferentiated cells
Assignee: YISSUM RES DEV CO OF HEBREW UNIV JERUSALEM LTDPriority: May 22, 2012Filed: Feb 1, 2018Published: Jun 7, 2018
Est. expiryMay 22, 2032(~5.8 yrs left)· nominal 20-yr term from priority
A61K 31/513A61K 31/341A61K 31/15A61K 31/4453A61K 31/451A61K 31/4545A61K 31/343A61K 31/404A61K 31/4409A61K 31/34G01N 33/5073A61K 31/381A61P 35/00A61K 31/136G01N 33/502G01N 2500/10A61K 31/4015A61K 31/403A61K 31/4985A61P 43/00A61K 31/166A61K 31/165A61K 31/155A61P 35/02G01N 2500/02A61K 31/407
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Claims
Abstract
Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A method of inhibiting undifferentiated cells, the method being effected by contacting undifferentiated cells with a compound selected from the group consisting of:
a compound of Formula I
a compound of Formula II
a compound of Formula III
a compound of Formula IV
a compound of Formula V
and
a compound of Formula VI
wherein:
R 1 is hydrogen, and
R 2 is selected from the group consisting of:
hydrogen,
2,4-dioxo-5-fluoropyrimidin-1-ylcarbonyl,
2-methylbenzofuran-3-ylmethyleneamino,
and
—NH—R 5 , wherein R 5 is selected from the group consisting of:
pyridinylcarbonyl,
2-hydroxyl-2-phenyl-2-thiophen-2-yl-acetyl,
(C 1-6 )alkyl-carbonyl,
N-(ethoxycarbonylmethyl)-2,4-dioxo-pyrrolidine-3-ylidene-methyl,
naphthylsulfonyl, and
N-hydroxy-acetimidoyl;
or wherein:
R 1 is benzoyl and R 2 is 4-chlorobenzamido; and
R 3 and R 4 are independently selected from the group consisting of hydrogen, halo, NH 2 , biphenyloxymethyl and (C 1-4 )alkyl,
with the proviso that at least one of R 1 , R 2 , R 3 and R 4 is not hydrogen, halo, NH 2 or (C 1-4 )alkyl.
2 . The method of claim 1 , wherein said compound is of Formula I.
3 . The method of claim 2 , wherein:
R 1 is hydrogen, and R 2 is selected from the group consisting of:
2,4-dioxo-5-fluoropyrimidin-1-ylcarbonyl,
2-methylbenzofuran-3-ylmethyleneamino, and
—NH—R 5 , wherein R 5 is selected from the group consisting of:
pyridinylcarbonyl,
2-hydroxyl-2-phenyl-2-thiophen-2-yl-acetyl,
(C 1-6 )alkyl-carbonyl,
N-(ethoxycarbonylmethyl)-2,4-dioxo-pyrrolidine-3-ylidene-methyl,
naphthylsulfonyl, and
N-hydroxy-acetimidoyl;
or wherein: R 1 is benzoyl and R 2 is 4-chlorobenzamido; and R 3 and R 4 are independently selected from the group consisting of hydrogen, chloro, NH 2 , and methyl.
4 . The method of claim 1 , wherein said compound is of formula II:
5 . The method of claim 1 , wherein said compound is of formula III:
6 . The method of claim 1 , wherein said compound is of formula IV:
7 . The method of claim 1 , wherein said compound is of formula V:
8 . The method of claim 1 , wherein said compound is of formula VI:
9 . The method of claim 1 , wherein said undifferentiated cells comprise pluripotent stem cells.
10 . The method of claim 1 , wherein said undifferentiated cells comprise undifferentiated cancer cells.
11 . The method of claim 10 , wherein said undifferentiated cancer cells comprise cancer stem cells and/or Grade 4 undifferentiated cancer cells.
12 . A method of treating a proliferative disease or disorder associated with proliferation of undifferentiated cells in a subject in need thereof, said undifferentiated cells being selected from the group consisting of pluripotent stem cells, cancer stem cells and Grade 4 undifferentiated cancer cells, the method comprising administering to the subject a therapeutically effective amount of a compound selected from the group consisting of:
a compound of Formula I
a compound of Formula II
a compound of Formula III
a compound of Formula IV
a compound of Formula V
and
a compound of Formula VI
thereby treating the proliferative disease or disorder.
13 . The method of claim 12 , wherein said proliferative disease or disorder is selected from the group consisting of a teratoma, an undifferentiated cancer, a leukemia, a brain cancer, a breast cancer, a colon cancer, an ovarian cancer, a pancreatic cancer, a prostate cancer, a melanoma, a liver cancer, a lung cancer, a head and neck cancer, a mesenchymal cancer and a multiple myeloma.
14 . The method of claim 12 , wherein said compound is of Formula I.
15 . The method of claim 14 , wherein:
R 1 is hydrogen, and R 2 is selected from the group consisting of:
2,4-dioxo-5-fluoropyrimidin-1-ylcarbonyl,
2-methylbenzofuran-3-ylmethyleneamino, and
—NH—R 5 , wherein R 5 is selected from the group consisting of:
pyridinylcarbonyl,
2-hydroxyl-2-phenyl-2-thiophen-2-yl-acetyl,
(C 1-6 )alkyl-carbonyl,
N-(ethoxycarbonylmethyl)-2,4-dioxo-pyrrolidine-3-ylidene-methyl,
naphthylsulfonyl, and
N-hydroxy-acetimidoyl;
or wherein: R 1 is benzoyl and R 2 is 4-chlorobenzamido; and R 3 and R 1 are independently selected from the group consisting of hydrogen, chloro, NH 2 , and methyl.
16 . The method of claim 12 , wherein said compound is of formula II:
17 . The method of claim 12 , wherein said compound is of formula III:
18 . The method of claim 12 , wherein said compound is of formula IV:
19 . The method of claim 12 , wherein said compound is of formula V:
20 . The method of claim 12 , wherein said compound is of formula VI:Join the waitlist — get patent alerts
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