Astinova Blog
Working notes from the Astinova chemistry team — synthesis case studies, modality deep dives, and observations from real drug discovery programs.
Patent / Application Type Assignee Filed Expiry (~) WO 2007/058338 A1 (US 7,919,617 B2; EP 1,953,148 B1; JP 4,975,757 B2) Composition of matter (originator) Otsuka Pharmaceutical Co., Ltd. 2006-11-16 (priority 2005-11-15, JP 2005-330289) ~Nov 2026 nominal (US 7,919,617…
Read article →Patent Landscape & Exclusivity 2.1 Key patent filings Synthesis Route of the Originator Convergent synthesis disclosed in WO 2014/135561 (Roche). Eastern fragment: 1-methyl-6-bromo-3,4-dihydroquinolin-2(1H)-one (INT-2) → pinacolboronate (INT-3, via Pd/B2pin2 Miyaura). Western fragment: (R)-8-aminotetrahydroisoquinoline scaffold, Boc-protected (INT-5), 4-bromide for…
Read article →In the conventional ADC narrative, the antibody picks the cell, the payload kills it, and the linker just holds them together until they get there. The picture is wrong in roughly the same way that calling a fuel…
Read article →In the last five years, targeted protein degradation has gone from an academic curiosity to an industry-wide drug discovery priority. Roughly thirty PROTACs are in human clinical trials as of early 2026. Several are deep into Phase 2…
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