US2021317107A1PendingUtilityA1
Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase
Est. expiryMar 2, 2037(~10.6 yrs left)· nominal 20-yr term from priority
C07D 209/34A61K 45/06C07D 401/06C07D 403/12A61K 31/496C07D 405/06C07D 401/14C07D 401/12C07D 403/04C07D 413/14C07D 413/04C07D 405/14
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Claims
Abstract
The present disclosure relates to indolinone compounds, compositions, and methods for the inhibition of maternal embryonic leucine zipper kinase (MELK). The present disclosure further relates to indolinone compounds, compositions, and methods for the treatment or prevention of a cancer (for example, triple negative breast cancer).
Claims
exact text as granted — not AI-modified1 .- 11 . (canceled)
12 . A method for the treatment of a cancer, comprising:
administering an effective amount of a compound of Formula I to a host in need thereof:
wherein:
R 1 is hydrogen;
R 2 is selected from carboxylic acid, ester, amide, acyl, alkoxy, sulfonamide, alkylamino, aminoacyl, or amino; and
R 3 is selected from aryl or heteroaryl;
or a pharmaceutically acceptable salt thereof.
13 . The method of claim 12 , wherein the compound comprises the formula:
wherein:
R 1 is hydrogen; and
R 2 is selected from carboxylic acid, ester, amide, acyl, alkoxy, sulfonamide, alkylamino, aminoacyl, or amino;
or a pharmaceutically acceptable salt thereof.
14 . The method of claim 12 , wherein R 2 is ester.
15 . The method of claim 12 , wherein R 3 is selected from phenyl, benzyl, pyridine, or furan.
16 . The method of claim 12 , wherein R 3 is unsubstituted aryl.
17 . The method of claim 12 , wherein R 3 is phenyl.
18 . The method of claim 12 , wherein R 3 is substituted aryl.
19 . The method of claim 12 , wherein R 3 is pyridine.
20 . The method of claim 12 , wherein R 3 is furan.
21 . The method of claim 12 , wherein the compound is
22 . The method of claim 12 , wherein the compound is
23 . (canceled)
24 . The method of claim 12 , wherein the cancer is triple negative breast cancer.
25 . The method of claim 12 , wherein the cancer is glioblastoma multiforme.
26 . The method of claim 12 , wherein the compound is administered in combination with an additional chemotherapeutic agent.
27 . A method for the treatment of a cancer, comprising:
administering an effective amount of a compound of Formula III to a host in need thereof:
wherein:
R 1 is hydrogen;
R 2 is selected from carboxylic acid, ester, amide, acyl, alkoxy, sulfonamide, alkylamino, aminoacyl, amino, nitro, aryl, or heteroaryl;
each R 4 is independently selected from hydrogen, alkyl, carboxylic acid, ester, amide, acyl, alkoxy, hydroxyl, hydroxyalkyl, sulfonamide, alkylamino, aminoacyl, amino, nitro, heterocycloalkyl, heterocycloalkylalkyl, or NR 5 R 6 ; or
two R 4 come together to form a carbocyclic ring or a heterocyclic ring;
R 5 and R 6 are independently selected from hydrogen, alkyl, alkylamino, heterocycloalkyl, acyl, or ester; and
x is selected from 1 or 2;
or a pharmaceutically acceptable salt thereof.
28 . The method of claim 27 , wherein R 2 is ester.
29 . The method of claim 27 , wherein R 4 is selected from hydrogen or alkyl.
30 . The method of claim 27 , wherein x is 1.
31 . The method of claim 27 , wherein the cancer is triple negative breast cancer.
32 . The method of claim 27 , wherein the cancer is glioblastoma multiforme.Join the waitlist — get patent alerts
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