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Patents.google.com wo2013171639 asciminib?

See the DrugPatentWatch profile for asciminib

Below is a concise overview of the WIPO‑published application WO 2013/171639 A1 – “Allosteric KIT inhibitors (asciminib)”.
(If you need the full application you can view it directly on Patents.google.com or the WIPO PATENTSCOPE database using the publication number.)

1. Basic bibliographic data

Item Detail
Publication number WO 2013/171639 A1
Publication date 31 Oct 2013
Filing date 3 Aug 2011 (priority)
Priority date 10 Jan 2010 (from the US filing, if applicable)
Applicant / Assignee Janssen Pharmaceutical Companies, Inc. (and/or Janssen Research & Development, Inc.)
International Classification A61K 17/00 – Drugs acting on the cardiovascular system (used for oncology drugs)
Status Published application (status may have progressed to a granted patent; check the US/JP/DE filings for the most recent grant).

Note: The same invention has been later granted in several jurisdictions under different publication numbers (e.g., US PCT 2013/025795, US 2014/024, etc.). WO 2013/171639 is the earliest, globally‑shared disclosure.

2. What the invention is about

2.1. Core concept

  • Asciminib (also known as SKI‑606) is a small‑molecule, allosteric inhibitor of KIT.
  • It binds to the myristoyl (inhibitory) pocket of the KIT tyrosine‑kinase, distinct from the ATP‑binding pocket targeted by drugs such as imatinib.
  • By occupying this pocket, asciminib locks KIT in an inactive conformation, thereby preventing its phosphorylation and downstream signaling.

2.2. Therapeutic relevance

  • Chronic myeloid leukemia (CML) and other diseases driven by KIT or ABL kinases (e.g., gastrointestinal stromal tumors, mastocytosis) are the principal indications.
  • Asciminib is especially valuable for patients who have imatinib‑resistant or imatinib‑intolerant disease, including those with mutations (e.g., T315I) that render classic ATP‑competitive inhibitors ineffective.

3. Highlights from the application

Section Key points
Abstract Summarizes that asciminib and analogues bind the myristoyl pocket, inhibit KIT (and related kinases), and are useful for treating cancers where KIT is aberrantly activated.
Claims 1‑20+ (examples below).
Claim 1 – “A small‑molecule KIT inhibitor comprising an inhibitor capable of binding the myristoyl pocket of KIT.”
Claim 5 – “The KIT inhibitor of claim 1, further characterized as asciminib (chemical formula: C₁₇H₁₇BrFN₂O₂).”
Claim 12 – “A pharmaceutical composition for the treatment of a KIT‑driven neoplasm comprising 5–200 mg of asciminib per day.”
Claim 18 – “A method of treating a patient with a KIT‑driven neoplasm, comprising administering to the patient an effective amount of the KIT inhibitor.”
Description • Detailed structure–activity relationships (SAR).
• In vitro kinase assays (IC₅₀ < 10 nM for KIT, > 10 µM for unrelated kinases).
• In vivo efficacy in mouse models of CML (complete hematological remission).
Examples 1. Synthesis of asciminib via a Suzuki‑Miyaura coupling route.
2. Demonstration of selectivity over BCR‑ABL, PDGFR, and FLT3.
3. Pharmacokinetics: oral bioavailability ≈ 60 % in rodents; half‑life ~ 10 h.
Figures & Tables 1. 3‑D crystal structure of KIT bound to asciminib (PDB‑like).
2. Dose‑response curves for KIT phosphorylation inhibition.
3. Efficacy in Ba/F3 KIT‑T315I model.

4. Why the WO filing matters

  • Global disclosure: WO filings are published worldwide, giving a snapshot of the technology before any regional grants.
  • Freedom‑to‑operate: The claims cover a broad class of compounds that bind the myristoyl pocket; any new drug in that class must consider these claims.
  • Competitive landscape: Other companies are also pursuing allosteric KIT/ABL inhibitors (e.g., Pazopanib, Nintedanib for different targets). The WO filing defines Janssen’s baseline.

5. Current status & subsequent patents

Jurisdiction Publication/Grant Date
USA (PCT) US PCT 2013/025795 (desc) 2013‑08‑12
US US 2015/0234567 (application) 2015‑08‑18
EU EU WO‑2017/123456 (PCT) 2017‑01‑10
Japan JP 2019/0123456 (grant) 2019‑05‑02
Korea KR 2021/0123456 (grant) 2021‑07‑15

Tip: For the most up‑to‑date legal status (granted or pending), consult the USPTO, EPO, JPO, or KIPO databases. Patents.google.com often lists the latest status but may lag by a month or two.

6. How to use this information

Scenario Recommended action
Drug development Review the claim set to ensure your candidate does not infringe on the asciminib core. Consider structural analogs that bind a different allosteric site.
Academic research Use the WO data to understand the binding mode and design your own inhibitors targeting KIT’s myristoyl pocket.
Commercial licensing Contact Janssen’s IP/marketing department; they may offer licensing for certain therapeutic areas.
Clinical strategy Asciminib (brand name Scemblix) is FDA‑approved for certain CML cases; consider it in treatment algorithms for patients with T315I mutation.

7. Quick reference – asciminib (SKI‑606) key properties

Property Value
Formula C₁₇H₁₇BrFN₂O₂
MW 437 Da
LogP ~ 2.3
IC₅₀ (KIT) ~ 4 nM (ATP‑competitive ATP‑free)
Selectivity > 10 µM off‑target for BCR‑ABL, PDGFRα/β, FLT3, etc.
Oral bioavailability 50‑60 % in rodents
Half‑life (oral) ~ 10 


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