825619-02-1Relevant articles and documents
Pyrazole spleen tyrosine kinase inhibitor as well as preparation method and application thereof
-
Paragraph 0402-0409, (2020/12/29)
The invention discloses a pyrazole spleen tyrosine kinase inhibitor, a preparation method thereof, a pharmaceutical composition containing the same, and application of the pyrazole spleen tyrosine kinase inhibitor and the pharmaceutical composition in the preparation of drugs for treating Syk-mediated diseases including cancers, inflammatory diseases and the like.
Pyrazole derivatives and use thereof
-
, (2019/04/04)
The invention relates to a substituted pyrazole derivative for inhibiting over-expression of protein kinase, and a stereoisomer, a geometrical isomer, a tautomer, an oxynitride, a solvate, a hydrate, a metabolite, an ester, a pharmaceutically acceptable s
As Aurora kinase inhibitor derivatives
-
, (2019/06/27)
The present invention relates to a substituted pyrazole derivative used for inhibiting Aurora kinase and represented by formula (I) or formula (Ia), or stereo isomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, esters, pharmaceutically acceptable salts or prodrugs thereof, a medicinal composition containing the above compounds as active ingredients, and a use of the compounds and the medicinal composition in preparation of medicines for protecting, processing, treating or mitigating proliferative diseases of patients.
Fragment-based design, synthesis, biological evaluation, and SAR of 1H-benzo[d]imidazol-2-yl)-1H-indazol derivatives as potent PDK1 inhibitors
Chen, Ting,Sorna, Venkataswamy,Choi, Susie,Call, Lee,Bearss, Jared,Carpenter, Kent,Warner, Steven L.,Sharma, Sunil,Bearss, David J.,Vankayalapati, Hariprasad
, p. 5473 - 5480 (2017/11/27)
In this work, we describe the use of the rule of 3 fragment-based strategies from biochemical screening data of 1100 in-house, small, low molecular weight fragments. The sequential combination of in silico fragment hopping and fragment linking based on S1
PYRAZOLYLBENZO[D]IMIDAZOLE DERIVATIVES
-
, (2014/09/29)
A compound represented by the general Formula (I), whereinhydrogen atoms shown as attached to pyrazole and benzimidazole rings are attached to one of nitrogen atoms of the pyrazole or benzimidazole ring, respectively; R1 represents -X-Q-P, wherein X is absent or represents –CH2-, –C(O)-, or –C(O)NH-(CH2)k-, wherein k is 0, 1 or 2; Q is selected from the group consisting of Q1, Q2, Q3, Q4 and Q5; P is absent or represents straight-or branched-chain C1-C3 alkyl, –(CH2)l-NR2R3, or–(CH2)m-C(O)-NR2R3, wherein l and m independently of each other represent 0, 1 or 2, with the proviso that when B in Q1 represents oxygen atom, then P is absent;and R2and R3 independently represent C1 or C2 alkyl, or R2 and R3 together with nitrogen atom to which they are both attached form a 6- membered saturated heterocyclicring, wherein one of carbon atoms can be replaced with oxygen, -NH-or –N(C1-C2)alkyl-; and acid addition salts thereof. The compound can be useful in the treatment of cancer diseases. (I)
Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors
Zheng, Youguang,Zheng, Ming,Ling, Xin,Liu, Yi,Xue, Yunsheng,An, Lin,Gu, Ning,Jin, Min
, p. 3523 - 3530 (2013/07/11)
Novel pyrazole-benzimidazole derivatives have been designed and synthesized. The entire target compounds were determined against cancer cell lines U937, K562, A549, LoVo and HT29 and were screened for Aurora A/B kinase inhibitory activity in vitro. The compounds 7a, 7b, 7i, 7k and 7l demonstrated significant cancer cell lines and Aurora A/B kinase inhibitory activities. Molecular modeling studies suggested the derivatives have bound in the active site of Aurora A kinase through the formation of four hydrogen bonds. Quantum chemical studies were carried out on these compounds to understand the structural features essential for activity. The cellular activity of 7k was also tested by immunofluorescence.
PHARMACEUTICAL COMBINATIONS OF 1-CYCLOPROPYL-3- [3-(5-M0RPHOOLIN-4-YL-METHYL-1H-BENZOIMIDAZOL-2-YL)- LH-1-PYRAZOL-4-YL]- UREA
-
, (2010/04/23)
The invention provides combinations of an ancillary compound and a compound which is a salt of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea selected from the lactate and citrate salts and mixtures thereof. Also p
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity
Howard, Steven,Berdini, Valerio,Boulstridge, John A.,Carr, Maria G.,Cross, David M.,Curry, Jayne,Devine, Lindsay A.,Early, Theresa R.,Fazal, Lynsey,Gill, Adrian L.,Heathcote, Michelle,Maman, Sarita,Matthews, Julia E.,McMenamin, Rachel L.,Navarro, Eva F.,O'Brien, Michael A.,O'Reilly, Marc,Rees, David C.,Reule, Matthias,Tisi, Dominic,Williams, Glyn,Vinkovi?, Mladen,Wyatt, Paul G.
experimental part, p. 379 - 388 (2009/09/29)
Here, we describe the identification of a clinical candidate via structure-based optimization of a ligand efficient pyrazole-benzimidazole fragment. Aurora kinases play a key role in the regulation of mitosis and in recent years have become attractive tar
PHARMACEUTICAL COMBINATIONS
-
Page/Page column 290-291; 296-297, (2008/06/13)
The invention provides combinations of an ancillary compound of the formula (0): and a compound of the formula (I'): Also provided are crystalline forms of the constituent compounds, methods for making them and their uses in treating cancers.
PHARMACEUTICAL COMPOUNDS
-
Page/Page column 236-237; 242-243, (2010/11/28)
The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDKl , Chk (e.g. Cbkl or Chk2),