Fused tricyclic urea compounds as Raf kinase and/or Raf kinase dimer inhibitors
US-10562899-B2 · Feb 18, 2020 · US
Stable solid dispersion of a B-RAF kinase dimer inhibitor, methods of preparation, and uses therefor
US12582604B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12582604-B2 |
| Application number | US-202017423600-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jan 23, 2020 |
| Priority date | Jan 25, 2019 |
| Publication date | Mar 24, 2026 |
| Grant date | Mar 24, 2026 |
How to read this patent
A practical reading order for non-experts. Skip the full description unless you need deep technical detail.
- Title
What the patent document calls the invention.
- Abstract
A short plain-language summary of the technical disclosure.
- Assignees and inventors
Who owns or filed the patent and who is credited as inventor.
- Key dates
Filing, priority, publication, and grant dates set the timeline.
- First independent claim
The legal scope of protection — read this for what is actually claimed.
- CPC / IPC classifications
Technology tags used to group this patent with similar filings.
- Citations and related patents
Prior art links and similar publications in this corpus.
Abstract
Official abstract text for this publication.
Disclosed herein is a physically stable solid dispersion comprising Compound 1, i.e., the B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-1-yl)-3-(2, 4, 5-trifluorophenyl) urea and a specific stabilizing polymer, the method for preparing the same, and the uses of the solid dispersion. Also disclosed herein is the crystalline form of Compound 1.
First claim
Opening claim text (preview).
What is claimed is: 1 . A stable amorphous solid dispersion comprising Compound 1 and a stabilizing polymer, wherein Compound 1 is 1-((1S,1aS,6bS)-5-((7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-1-yl)-3-(2,4,5-trifluorophenyl) urea, and Compound 1 is molecularly dispersed within a polymer matrix formed by the stabilizing polymer in its solid state, wherein the stabilizing polymer is hydroxypropyl methylcellulose acetate succinate, type LF (HPMCAS-LF), and the weight ratio of Compound 1 in the form of freebase and the polymer is 1:4, and wherein HPMCAS-LF has 5.0-9.0% of acetyl group and 14.0-18.0% of succinoyl group. 2 . The stable amorphous solid dispersion according to claim 1 , wherein the stable amorphous solid dispersion has a drug-loading content of Compound 1 ranging from 10% w/w to 40% w/w. 3 . The stable amorphous solid dispersion according to claim 1 , wherein the stable amorphous solid dispersion has a glass transition temperature ranging from 110-115° C. 4 . The stable amorphous solid dispersion according to claim 1 , wherein the stable amorphous solid dispersion is formulated into an orally administrated formulation.
Assignees
Inventors
Classifications
- C07D471/04Primary
Ortho-condensed systems · CPC title
Crystalline forms, e.g. polymorphs · CPC title
Cellulose; Derivatives thereof · CPC title
the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine · CPC title
Antineoplastic agents · CPC title
Patent family
Related publications grouped by family.
External sources
Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US12582604B2 cover?
- Disclosed herein is a physically stable solid dispersion comprising Compound 1, i.e., the B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-1-yl)-3-(2, 4, 5-trifluorophenyl) urea and a specific stabilizing polymer, the method for preparing the same, and the uses of the solid dispersion. Also disc…
- Who is the assignee on this patent?
- Beigene Ltd
- What technology area does this patent fall under?
- Primary CPC classification C07D471/04. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Mar 24 2026 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 10 related publications on this page (citations in our corpus or others sharing the same primary CPC).