941685-27-4Relevant articles and documents
Pyrrole/imidazo six-membered hetero-aromatic ring compound as well as preparation method and medical application thereof
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, (2020/07/13)
The invention relates to a pyrrole/imidazo six-membered hetero-aromatic ring compound as well as a preparation method and medical application thereof. Particularly, the invention relates to a compoundas shown by general formula (I), a preparation method t
Simple synthetic method of 7-protecting group-4-(1-hydrogen-pyrazole-4-yl)pyrrole[2,3-d]pyrimidine
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Paragraph 0075; 0076; 0079; 0080, (2019/04/30)
The invention discloses a simple synthetic method of 7-protecting group-4-(1-hydrogen-pyrazole-4-yl)pyrrole[2,3-d]pyrimidine. The method comprises the following steps: preparing compound (IV) by a dehydrohalogenation reaction between cyanoacetoacetate and haloacetaldehyde glycol, and then preparing a compound (V) by condensation between the compound (V) and formamidine hydrochloride and alkali; preparing a compound (VIII) by amino group protection through a protecting group reagent, methylation of DMFDMA and hydrazine hydrate condensation; preparing a compound (IX) by reacting with a chlorination reagent; and carrying out catalytic hydrodechlorination to obtain 7-protecting group-4-(1-hydrogen-pyrazole-4-yl)pyrrole[2,3-d]pyrimidine. The raw materials used in the invention are cheap and easily available; by using the ''one-pot method'' operation twice, the environmental protection property is high, and the process route is simple; the reaction operation is convenient, and the reaction selectivity is high; the obtained product has high purity, high yield and low cost; and the method is beneficial to green industrial production.
AZETIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
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, (2018/08/29)
The present invention relates to an azetidine derivative for use as a Janus kinase (JAK) inhibitor, a drug composition comprising same, a preparation method therefor, and a use thereof in the treatment of JAK-related diseases comprising, for example, infl
Pyrrole pyrimidine five-membered nitrogen-heterocyclic derivative and application thereof
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, (2017/07/21)
The invention relates to a novel JAK (Janus kinase) inhibitor, namely a pyrrole pyrimidine five-membered nitrogen-heterocyclic derivative, and application of the pyrrole pyrimidine five-membered nitrogen-heterocyclic derivative in preparation of a medicine for preventing and/or treating JAK function-related adaptation diseases. The pyrrole pyrimidine five-membered nitrogen-heterocyclic derivative disclosed by the invention is an ideal efficient JAK inhibitor, and can be used for treating or preventing diseases such as rheumatoid arthritis, polycythemia vera, psoriasis, primary thrombocythemia and myelofibrosis.
Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat
Yao, Lianbin,Mustafa, Nurulhuda,Tan, Eng Chong,Poulsen, Anders,Singh, Prachi,Duong-Thi, Minh-Dao,Lee, Jeannie X. T.,Ramanujulu, Pondy Murugappan,Chng, Wee Joo,Yen, Jeffrey J. Y.,Ohlson, Sten,Dymock, Brian W.
, p. 8336 - 8357 (2017/11/03)
Concomitant inhibition of multiple oncogenic pathways is a desirable goal in cancer therapy. To achieve such an outcome with a single molecule would simplify treatment regimes. Herein the core features of ruxolitinib (1), a marketed JAK1/2 inhibitor, have been merged with the HDAC inhibitor vorinostat (2), leading to new molecules that are bispecific targeted JAK/HDAC inhibitors. A preferred pyrazole substituted pyrrolopyrimidine, 24, inhibits JAK1 and HDACs 1, 2, 3, 6, and 10 with IC50 values of less than 20 nM, is 100 nM potent against JAK2 and HDAC11, and is selective for the JAK family against a panel of 97 kinases. Broad cellular antiproliferative potency of 24 is supported by demonstration of JAK-STAT and HDAC pathway blockade in hematological cell lines. Methyl analogue 45 has an even more selective profile. This study provides new leads for assessment of JAK and HDAC pathway dual inhibiton achieved with a single molecule.
PROCESSES FOR THE PREPARATION OF RUXOLITINIB PHOSPHATE
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Page/Page column 27; 28, (2016/03/19)
The present invention relates to processes for the preparation of ruxolitinib and ruxolitinib phosphate. The present invention also provides a compound of Formula IV, processes for its preparation, and its use for the preparation of ruxolitinib and ruxolitinib phosphate. The present invention provides ruxolitinib phosphate having a chiral purity of 99.96% and the compound of Formula IV having a chiral purity of 99.95%.
JAK1 INHIBITORS FOR THE TREATMENT OF MYELODYSPLASTIC SYNDROMES
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, (2015/10/05)
This invention relates to JAK1 selective inhibitors, particularly pyrrolo[2,3-d]pyrimidine and pyrrolo[2,3-b]pyridine derivatives, and their use in treating myelodysplastic syndromes (MDS).
PROCESSES AND INTERMEDIATES FOR MAKING A JAK INHIBITOR
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, (2013/03/26)
This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.
PIPERIDIN-4-YL AZETIDINE DERIVATIVES AS JAK1 INHIBITORS
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, (2011/10/04)
The present invention provides piperidin-4-yl azetidine derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase 1 (JAK1) and are useful in the treatment of diseases related to the activity of JAK1 including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS
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Page/Page column 84-85, (2010/08/07)
The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.