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FormulaC25H22N6O3. HCl
CAS1439901-97-9 HCL1351636-18-4FREE FORM
Mol weight490.9415

JAPAN APPROVED 2020/3/25 Velexbru

Antineoplastic, Bruton’s tyrosine kinase inhibitor



Tirabrutinib (Velexbru®) is an orally administered, small molecule, Bruton’s tyrosine kinase (BTK) inhibitor being developed by Ono Pharmaceutical and its licensee Gilead Sciences for the treatment of autoimmune disorders and haematological malignancies. Tirabrutinib irreversibly and covalently binds to BTK in B cells and inhibits aberrant B cell receptor signalling in B cell-related cancers and autoimmune diseases. In March 2020, oral tirabrutinib was approved in Japan for the treatment of recurrent or refractory primary central nervous system lymphoma. Tirabrutinib is also under regulatory review in Japan for the treatment of Waldenström’s macroglobulinemia and lymphoplasmacytic lymphoma. Clinical development is underway in the USA, Europe and Japan for autoimmune disorders, chronic lymphocytic leukaemia, B cell lymphoma, Sjogren’s syndrome, pemphigus and rheumatoid arthritis. This article summarizes the milestones in the development of tirabrutinib leading to the first approval of tirabrutinib for the treatment of recurrent or refractory primary central nervous system lymphoma in Japan.

The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review - ScienceDirect


WO 2011152351

Example 19 (2) : 6-amino-9-[(3R) -1- (2-butinoyl) -3-pyrrolidinyl] -7- (4-phenoxyphenyl) -7,9-dihydro-8H-purine- 8-on

Figure JPOXMLDOC01-appb-C000034

TLC: Rf 0.68 (ethyl acetate: methanol = 9: 1);
1 H-NMR (CDCl 3 ): δ 1.94-2.03, 2.23-2.39, 2.80-3.01, 3.50-3.63, 3.67-3.80, 3.86-4.02, 4.03-4.18, 4.23-4.33, 4.42-4.51, 5.11-5.25, 7.04-7.23, 7.34-7.45, 8.20-8.23.


WO 2013081016

WO 2015193740

WO 2015181633

WO 2015185998

WO 2016024228

WO 2016024231

WO 2016163531

WO 2016024227

WO 2017033113


US 20170035881

PATENT WO 2017033113

///////Tirabrutinib, japan 2020, 2020 approvals, Velexbru , チラブルチニブ塩酸塩  , GS 4059, ONO 4059,


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