| Patent Application Title: | Bruton’s Tyrosine Kinase Inhibitors | ||
| Patent Application Number: | WO 2017127371 A1 | Publication date: | July 27, 2017 |
| Priority Application: | US62/281,252 | Priority date: | January 21, 2016 |
| Inventors: | Liao, X.; Li, J.; Lu, Z.; Zhou, Y.; Gao, A. | ||
| Applicant(s): | Sunnylife Pharma Inc. and Shanghai Institute of Materia Medica, Chinese Academy of Sciences | ||
| Disease Area: | Autoimmune diseases, cancers, inflammatory diseases, thromboembolic diseases, and allergic diseases | Biological Target: | Bruton’s Tyrosine Kinase |
| Summary: | Bruton’s tyrosine kinase (BTK) is a kinase that plays a critical role in B lymphocytes (B-cell) development. In mammals, the B-cells mature in the bone marrow. In addition, most B-cell lymphomas express a B-cell receptor (BCR), which is critical for their proliferation and survival. Aberrant BCR signal in the tumor microenvironment has adverse effects to the survival, proliferation, differentiation, and activation of B-cells. Lymphoma is the fifth most common cancer in the U.S., and most treatments carry significant side effects, which are poorly tolerable by the elderly. BTK inhibitors are effective therapeutics in which B-cells with aberrant signaling pathways exist. The present BTK inhibitors (Formula I) described herein are potential therapeutics for the treatment of ailment such as inflammatory diseases, allergic diseases, cancers, autoimmune diseases, and thromboembolic diseases. |
| Important Compound Classes: |  |
| Key Structures: |  |
| Biological Assay: | The BTK activity was determined by a homogeneous time-resolved fluorescence (HTRF) methodology. The HTRF signal was measured on a multimode plate reader with detection wavelengths of 330, 615, and 665 nm. The activity was determined by the ratio of the fluorescence at 665 nm to that of 615 nm, and enzyme activity was measured at various concentrations. The table below shows the activity of selected compounds (shown in key structures) in the BTK inhibition assay. |
| Biological Data: |  |
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| Claims: | 13 Total claims |
| 8 Composition of matter claims | |
| 5 Method of use claims | |
| Recent Review Articles: | Chiappella A.; Santambrogio E.; Castellino A.; Nicolosi M.; Vitolo U.. Expert Review of Hematology 2017, 10, 697–705. |
| Seiler T.; Dreyling M.. Expert Opinion on Investigational Drugs 2017, 26, 909–915. | |
| Molina-Cerrillo J.; Alonso-Gordoa T.; Gajate P.; Grande E.. Cancer Treatment Reviews 2017, 58, 41–50. |
The author declares no competing financial interest.