- CRYSTALLINE FORM OF BTK KINASE INHIBITOR AND PREPARATION METHOD THEREOF
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The present invention relates to a crystalline form of a BTK kinase inhibitor and the preparation method thereof. In particular, the present invention relates to a crystal form I of (R)-4-amino-1-(1-(but-2-ynoyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1H-pyrrolo[2,3-d]pyridazin-7(6H)-one (the compound of formula (I)) and the preparation method thereof. The crystal form I of the compound of formula (I) obtained by the present invention has a good crystalline stability and chemical stability, and the crystallization solvent used has a low toxicity and low residue, thus making it more suitable for use in clinical treatment.
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Paragraph 0033; 0035-0037
(2019/01/24)
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- Crystallization form of BTK inhibitor, and preparation method thereof
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The invention relates to a crystallization form of a BTK inhibitor, and a preparation method thereof, and concretely relates to a type I crystal of (R)-1-(3-(4-amino-3-(4-(2,6-difluorophenoxy)phenyl)-7-hydroxy-1H-pyrrolo[2,3-d]pyridazine-1-yl)piperidine-1-yl)propyl-2-ene-1-one (compound of formula (I)), and a preparation method thereof. The type I crystal of the compound (I) obtained in the invention has the advantages of good chemical stability and crystal form stability, and a crystallization solvent used in the invention has low toxicity and low residual, so the type I crystal of the compound (I) can be well used in clinic treatment.
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Paragraph 0047; 0048; 0049
(2017/08/31)
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- AMINOPYRIDAZINONE COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.
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Paragraph 00179; 00180
(2016/01/25)
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- TREATMENT OF DRY EYE
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The present disclosure provides a method of treating dry eye by inhibition of Bruton's tyrosine kinase (hereinafter "BTK") inhibitors, pharmaceutical formulations comprising the same, and processes for preparing such compounds.
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Page/Page column 60
(2014/02/16)
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- Tyrosine kinase inhibitors
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The present disclosure provides compounds such as pyrazolpyrimidine compounds, and pharmaceutically acceptable salts thereof, that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Page/Page column 210; 211
(2014/03/26)
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- Purinone Derivatives as Tyrosine Kinase Inhibitors
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The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as autoimmune diseases, cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Paragraph 0198
(2014/05/25)
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- REVERSIBLE COVALENT PYRROLO- OR PYRAZOLOPYRIMIDINES USEFUL FOR THE TREATMENT CANCER AND AUTOIMMUNE DISEASES
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Oral pharmaceutical formulations comprising reversible covalent compounds having a Michael acceptor moiety, a process of their production, and use of these formulations for the treatment of diseases treatable by such compounds such as cancer and autoimmune diseases.
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Page/Page column 165
(2014/01/09)
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- PYRAZOLOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, Jak3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.
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Page/Page column 83-84
(2012/12/13)
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- TYROSINE KINASE INHIBITORS
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The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
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Page/Page column 177
(2012/12/13)
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- A NOVEL, SIMPLE METHOD FOR THE PREPARATION OF HINDERED DIPHENYL ETHERS
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The displacement of the nitro group from substituted nitrobenzenes is used for the synthesis of diphenyl ethers. 1,4-Dinitrobenzene has been converted into a variety of hindered diphenyl ethers using 2,6-disubstituted phenoxides and studies show that the mechanism of formation of the ether (5a) is radical in nature.
- Sammes, Peter G.,Thetford, Dean,Voyle, Martyn
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p. 3229 - 3232
(2007/10/02)
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- Displacement of an Aromatic Nitro Group using Phenoxides
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1,4-dinitrobenzene undergoes nucleophilic substitution with sodium phenoxide and several hindered 2,6-disubstituted phenoxides to afford diphenyl ethers.
- Sammes, P. G.,Thetford, D.,Voyle, M.
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p. 1373 - 1374
(2007/10/02)
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