Pyridazinedione-based heterobicyclic covalent linkers and methods and applications thereof
US-2024425465-A1 · Dec 26, 2024 · US
US9045484B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9045484-B2 |
| Application number | US-201313940641-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 12, 2013 |
| Priority date | Mar 13, 2008 |
| Publication date | Jun 2, 2015 |
| Grant date | Jun 2, 2015 |
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The present invention provides pyridinyl-substituted pyrazolyl pyrimidine small molecule inhibitors of bone morphogenetic protein (BMP) signaling having the structure of formula (I), wherein variables A, B, E, F, X, Y, Z, Ar, L 1 , R 4 and R 15 are as defined in the specification. The compounds of the invention are useful in modulating cell growth, differentiation, proliferation, and apoptosis, and thus are useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.
Opening claim text (preview).
The invention claimed is: 1. A method of inhibiting BMP-induced phosphorylation of SMAD1/5/8, comprising contacting the cell with a compound having a structure of Formula I: wherein: X and Y are each N; Z is CR 3 ; Ar is selected from substituted or unsubstituted aryl and heteroaryl; L 1 is absent or selected from substituted or unsubstituted alkyl and heteroalkyl…
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