, I can generate a high-quality, professional report tailored to your needs. For example: What is the general field?
– The core scaffold is patented globally (CN, US, EP, JP). Companies wishing to develop analogues must either license the core or design around the protected substitution pattern (e.g., varying the phenyl‑pyridine linkers). The patents have a typical 20‑year term; the earliest expiration is projected for 2042 (US filing). JUFE-448
| Target | Assay | IC₅₀ / K D | Selectivity | |--------|-------|----------------------|------------| | | AlphaScreen competition | 48 nM | ≥ 30‑fold vs. BRD2/3 | | BRD4 (bromodomain‑2) | SPR | 62 nM | 20‑fold vs. BRD2/3 | | CREBBP/EP300 bromodomain | FP assay | >10 µM (inactive) | — | | Off‑target kinases (e.g., CDK9, AURKA) | Kinome scan (KINOMEscan®) | >5 µM | — | , I can generate a high-quality, professional report
| Strategy | Rationale | Current status | |----------|-----------|----------------| | | Improves solubility, enables controlled release; protects from rapid metabolism. | Pre‑clinical PK shows 2‑fold increase in AUC. | | Lipid‑based SMEDDS (self‑micelle forming) | Enhances oral absorption (bioavailability ↑ ~30 %). | Pilot mouse study completed; scale‑up pending. | | Pro‑drug (tert‑butyl‑carbamate cleavage) | In vivo esterases convert to active free amine; improves stability in formulation. | Demonstrated in vitro; in vivo data still limited. | | Crystal polymorph optimization (Form B) | Higher melting point, lower hygroscopicity, better processability for solid dosage forms. | GMP‑grade batches manufactured for IND‑enabling studies. | Companies wishing to develop analogues must either license