1351636-18-4

Basic information

• Product Name: Btk Kinase inhibitor
• Synonyms: Btk Kinase inhibitor;ONO BTK;ONO-4059(GS-4059,Tirabrutinib) free base;6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one;Tirabrutinib (ONO-4059)
• CAS NO: 1351636-18-4
• Molecular Formula: C₂₅H₂₂N₆O₃
• Molecular Weight: 454.48058
• Mol File: 1351636-18-4.mol
• Article Data: 10

Chemical Properties

• Boiling Point: 672.0±65.0 °C(Predicted)
• Appearance: /
• Density: 1.412±0.06 g/cm3(Predicted)
• PKA: 3.16±0.20(Predicted)
• CAS DataBase Reference: Btk Kinase inhibitor(CAS DataBase Reference)
• NIST Chemistry Reference: Btk Kinase inhibitor(1351636-18-4)
• EPA Substance Registry System: Btk Kinase inhibitor(1351636-18-4)

Safety Data

• Hazardous Substances Data: 1351636-18-4(Hazardous Substances Data)

Usage

General Description

Btk Kinase inhibitors are specialized drugs used in the treatment of several conditions, especially B-cell cancers and autoimmune diseases. Btk, or Bruton’s tyrosine kinase, is a type of enzyme responsible for transmitting crucial signals in B cells for their expansion and survival. When overexpressed or mutated, they can lead to various malignancies or immune disorders. Hence, Btk kinase inhibitors work by blocking this enzyme's activity, thus dampening B cell responses in diseases such as chronic lymphocytic leukemia, mantle cell lymphoma, and non-Hodgkin lymphoma. The inhibitors effectively control the progression of these diseases and enhance patient survival rates. Notable Btk inhibitors include Ibrutinib, Acalabrutinib, and Tirabrutinib.

Upstream product

• 590-93-2 2-Butynoic acid 
• 1439901-94-6 tert-butyl (3R)-3-(6-amino-8-oxo-7, 8-dihydro-9H-purin-9-yl)pyrrolidine-1-carboxylate 
• 1351636-74-2 tert-butyl (3R)-3-{[6-(dibenzylamino)-5-nitropyrimidin-4-yl]amino} pyrrolidine-1-carboxylate 

Relevant articles and documents

PROCESS FOR PRODUCING PURINONE DERIVATIVE

According to the present invention, differently from well-known production methods, with the use of a different starting material, Ullmann condensation which may decrease the yield with an increase of a production scale can be avoided and thus 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one can be provided safely and stably with high reaction yield.

BTK INHIBITORS TO TREAT SOLID TUMORS THROUGH MODULATION OF THE TUMOR MICROENVIRONMENT

In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat solid tumor cancers by modulation of the tumor microenvironment, including macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells, and fibroblasts.

METHODS OF TREATING CANCERS, IMMUNE AND AUTOIMMUNE DISEASES, AND INFLAMMATORY DISEASES BASED ON BTK OCCUPANCY AND BTK RESYNTHESIS RATE

In an embodiment, therapeutic methods and use of a Bruton's Tyrosine Kinase (BTK) inhibitor for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are described. In an embodiment, dosing regimens for a BTK inhibitor for treatment of cancer, inflammation, immune disorders, and autoimmune disorders, and for transplantation prophylaxis, based on BTK occupancies and/or BTK resynthesis rates for B cells in various diseases, tissue compartments, including bone marrow and lymph nodes, are described.