Ammonium salts of 3-(3,5-dibromo-4-hydroxybenzyliden)-5-indo-1,3-dihydroindol-2-one and uses thereof
US11304930B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 24, 2019 |
| Grant date | Apr 19, 2022 |
| Priority date | — |
| Expiry date | Jul 24, 2039 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D209/34
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Disclosed herein is a compound of formula (I), which is ammonium salt of GW5074, wherein R1, R2, and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; or R1, R2, R3 and the nitrogen are taken together to form a 6-membered heterocyclyl; and the alkyl, the alkenyl, the alkynyl, the aryl, the heteroaryl, or the 6-membered heterocyclyl is optionally substituted with at least one substituent selected from the group consisting of, —OH, —NH2, and —NRaRb, in which Ra and Rb are independently alkyl, aryl, or heteroaryl. Also disclosed herein is a pharmaceutical kit for the treatment of cancers. The pharmaceutical kit includes, a first formulation comprising a c-Raf inhibitor and a pharmaceutically acceptable carrier; and a second formulation comprising the compound of formula (I) and a pharmaceutically acceptable carrier. Also encompasses herein is a method of treating a subject having a cancer. The method comprises: (a) detecting whether the cancer cells of the subject has phosphorylation on serine 308 of death-associated protein kinase (DAPK); and (b) treating the subject based on the detection of the step (a) by, administering to the subject (i) an effective am…
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