Pyridazinedione-based heterobicyclic covalent linkers and methods and applications thereof
US-2024425465-A1 · Dec 26, 2024 · US
US9676792B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9676792-B2 |
| Application number | US-201414775897-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 17, 2014 |
| Priority date | Mar 15, 2013 |
| Publication date | Jun 13, 2017 |
| Grant date | Jun 13, 2017 |
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The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.
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What is claimed: 1. A compound of formula V: or a pharmaceutically acceptable salt thereof, wherein, X is hydrogen; R 2 is hydrogen or alkyl; R 3 is —OH or O-(alkyl); R 4 is hydrogen or alkyl; R 6 is hydrogen or alkyl; and R′ is hydrogen. 2. The compound of claim 1 , wherein R 2 is H, methyl, or ethyl. 3. The compound of claim 1 , wherein R 6 is H. 4. The compound of claim 1 , wherein R 3 is —OCH 3 or —OCH 2 CH 3 . 5. The compound of claim 1 , wherein R 4 is methyl or ethyl. 6. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.
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