940890-90-4Relevant articles and documents
Tumor-Cell-Specific Targeting of Ibrutinib: Introducing Electrostatic Antibody-Inhibitor Conjugates (AiCs)
B?umer, Nicole,B?umer, Sebastian,Becht, Manuel,Berdel, Wolfgang E.,Dersch, Petra,Faust, Andreas,Geyer, Christiane,Greune, Lilo,Lenz, Georg,Margeta, Renato,Rüter, Christian,Schlütermann, Alina,Wittmann, Lisa
supporting information, (2021/12/09)
Ibrutinib is an inhibitor of Bruton's tyrosine kinase that has been approved for the treatment of patients with chronic lymphocytic leukemia, mantle cell lymphoma and Waldenstrom's macroglobulinemia and is connected with toxicities. To minimize its toxicities, we linked ibrutinib to a cell-targeted, internalizing antibody. To this end, we synthesized a poly-anionic derivate, ibrutinib-Cy3.5, that retains full functionality. This anionic inhibitor is complexed by our anti-CD20-protamine targeting conjugate and free protamine, and thereby spontaneously assembles into an electrostatically stabilized vesicular nanocarrier. The complexation led to an accumulation of the drug driven by the CD20 antigen internalization to the intended cells and an amplification of its pharmacological effectivity. In vivo, we observed a significant enrichment of the drug in xenograft lymphoma tumors in immune-compromised mice and a significantly better response to lower doses compared to the original drug.
BTK Inhibitors and uses thereof
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Paragraph 0448; 0453-0455; 1480; 1494-1496; 1726; 1731-1733, (2020/05/02)
The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
ANTITUMOR-EFFECT ENHANCER USING PYRAZOLO[3,4-D]PYRIMIDINE COMPOUND
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Paragraph 0286, (2020/01/22)
To provide a method for treating cancer using a pyrazolo[3,4-d]pyrimidine compound or a salt thereof. The present invention provides an antitumor agent comprising a pyrazolo[3,4-d]pyrimidine compound of formula (I) wherein X, Y, Z1, Z2/su
PROCESS FOR THE SYNTHESIS OF STABLE AMORPHOUS IBRUTINIB
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, (2017/09/05)
Disclosed herein is a new route of synthesis and a new stable amorphous form of ibrutinib. Also disclosed are pharmaceutical compositions, oral dosage forms and the use of the amorphous ibrutinib in the treatment of mantle cell lymphoma or chronic lymphocytic leukemia.
AN IMPROVED PROCESS FOR THE PREPARATION OF IBRUTINIB
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Page/Page column 12, (2018/02/28)
The present invention relates to an improved process for the preparation of Ibrutinib with high purity and high yields. The present process is cost effective and feasible in large scale production also. The present process avoids the mitsunobu reagent conditions also. The present Invention also relates to a process for the preparation of Crystalline form A and Crystalline form C of Ibrutinib.
NOVEL SALT OF FUSED PYRIMIDINE COMPOUND AND CRYSTAL THEREOF
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Paragraph 0187, (2017/04/11)
Provided is a salt having a high selectivity to BTK and is useful as a drug ingredient for a pharmaceutical product. It has been found that fumarate of Compound A is free of a characteristic of channel hydrate and is stable and excellent in absorptive property, compared to Compound A or other salts thereof.
NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUND OR SALT THEREOF
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Paragraph 0335, (2017/08/26)
To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 i
Preventive and/or therapeutic agent of immune disease
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Page/Page column 40, (2017/10/28)
Provided is a preventive and/or therapeutic agent for immune diseases containing a compound having a BTK inhibitory activity or a salt thereof, as an active ingredient. A preventive and/or therapeutic agent of immune diseases, comprising a compound repres
TYROSINE KINASE INHIBITORS
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Page/Page column 76, (2017/04/19)
The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase ("BTK") inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, au