88805-76-9Relevant articles and documents
Identification of pyrazolopyridine derivatives as novel spleen tyrosine kinase inhibitors
Huang, Yahui,Li, Yu,Dong, Guoqiang,Zhang, Wannian,Liu, Na,Sheng, Chunquan
, (2018/08/21)
Inhibition of spleen tyrosine kinase (Syk) is a promising strategy for the treatment of various allergic and autoimmune disorders such as asthma, rheumatoid arthritis, and allergic rhinitis. Previously, a Syk inhibitor with novel indazole scaffold was discovered by structure-based virtual screening. Herein, the structure–activity relationship of the indazole Syk inhibitors was investigated. Several new inhibitors demonstrated potent activity against Syk. In particular, compound 18c showed good Syk inhibitory activity (IC50 = 1.2 μM), representing a good lead compound for further optimization.
Aminoindazole derivatives
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, (2008/06/13)
A compound of the formula (I): STR1 wherein W1 and W2 each independently is a hydrogen atom or a STR2 group wherein Y is a n-C1-6 alkylene group or a n-C1-6 alkylene group having a C1-6 alkyl group substituent; and R1 and R2 each independently is a hydrogen atom or a C1-6 alkyl group, and STR3 group in STR4 group may form a saturated heterocyclic ring selected from the group consisting of morpholino, pyrrolidino, piperidino, homopiperidino and piperazino groups, and the saturated heterocyclic ring except the morpholino group may have at least one C1-4 alkyl group, hydroxyl group or halogen atom as a substituent; Z1 is a hydrogen atom, a chlorine atom, a bromine atom, an iodine atom, a hydroxyl group, an amino group, a C1-3 alkyl group or a methoxy group; Z2 is a hydrogen atom or an amino group; when W1 and W2 are both hydrogen atoms, Z1 is a hydroxyl group or an iodine atom and Z2 is hydrogen atom, or Z1 and Z2 are both amino groups; when Z1 and Z2 are both hydrogen atoms, the STR5 group in either W1 or W2 is a morpholino group; when Z1 is a chlorine atom, a hydroxyl group, an iodine atom, a methyl group or a methoxy group, Z2 is a hydrogen atom; when Z1 is an amino group, Z2 is a hydrogen atom or an amino group; when Z1 is a methyl group, a methoxy group or an amino group, Z1 is in the 5-position; when Z1 is an iodine atom, Z1 is in the 5- or 7-position; and when Z1 and Z2 are both amino groups, Z1 and Z2 are in the 5- and 7-positions; and the physiologically acceptable acid addition salt thereof which compounds have pharmaceutical utility, e.g.: treating inflammation.
