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Nitrogen-containing fused ring compounds as well as preparation method and application thereof

A compound and heterocycloalkyl technology, applied in the field of nitrogen-containing fused-ring compounds and their preparation, can solve the problems of low target inhibition activity, easy generation of drug resistance, poor pharmacokinetic properties of compounds, etc.

Active Publication Date: 2019-05-07
RUDONG RINGENE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to overcome the ubiquity of existing FGFR inhibitor compounds in the prior art or poor target selectivity, or low target inhibitory activity, or poor pharmacokinetic properties of compounds, or prone to resistance Therefore, a class of nitrogen-containing fused ring compounds and their preparation methods and uses are provided. The nitrogen-containing fused ring compounds of the present invention are novel specific irreversible inhibitors of FGFR kinases and can be used to treat abnormalities in FGFR kinases. related diseases such as tumor

Method used

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  • Nitrogen-containing fused ring compounds as well as preparation method and application thereof
  • Nitrogen-containing fused ring compounds as well as preparation method and application thereof
  • Nitrogen-containing fused ring compounds as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0236] Example 1: N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)imidazol[1',2':1,6]pyridin[2,3- d] pyrimidin-2-yl) amino) phenyl) -2-fluoroacrylamide

[0237] LC-MS:ESI[M+H] +=553.2 / 555.2; 1H-NMR (400MHz, CD3OD) δ9.83(s, 1H), 9.50(s, 1H), 9.14(s, 1H), 8.16(s, 1H), 7.87(d, J=7.6 Hz,1H),7.69(d,J=6.8Hz,1H),7.52(s,1H),7.50(s,1H),7.21-7.31(m,2H),7.06(s,1H),6.24(dd , J=2.0, 17.2Hz, 1H), 5.72(dd, J=2.0, 10.4Hz, 1H), 3.99(s, 6H).

Embodiment 2

[0238] Example 2: N-(2-((4-(2,6-dichloro-3,5-dimethoxyphenyl)imidazo[1,2-a][1,6]naphthyridine-8- Base) amino) phenyl) -2-fluoroacrylamide

[0239] LC-MS:ESI[M+H] + =552.4 / 554.4; 1H-NMR (400MHz, CD3OD) δ9.88(s, 1H), 8.83(s, 1H), 8.74(s, 1H), 8.33(s, 1H), 7.70(d, J=7.6 Hz,1H),7.63(d,J=7.6Hz,1H),7.50(s,1H),7.46(s,1H),7.15-7.28(m,3H),7.06(s,1H),6.24(dd , J=2.0, 16.8Hz, 1H), 5.72(dd, J=2.0, 10.4Hz, 1H), 4.00(s, 6H).

Embodiment 3

[0240] Example 3: N-(3-((6-(2,6-dichloro-3,5-dimethoxybenzene)imidazol[1',2':1,6]pyridine[2,3-d ]pyrimidin-2-yl)amino)-1-methyl-1H-pyrazol-4-yl)-2-fluoroacrylamide

[0241] LC-MS:ESI[M+H] + =557.2559.2; 1H-NMR (400MHz, CD3OD) δ10.91(s, 1H), 10.07(s, 1H), 9.14(s, 1H), 8.64(s, 1H), 8.47(s, 1H), 7.51-7.60(m,2H),7.07(s,1H),6.37(dd,J=1.6,8.8Hz,1H),5.84(d,J=10.4Hz,1H),3.99(s,6H),3.93 (s,1H).

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Abstract

The invention discloses nitrogen-containing fused ring compounds as well as a preparation method and application thereof. The nitrogen-containing fused ring compounds have a structure represented by aformula (I) shown in the description, wherein each group is defined in the description. The nitrogen-containing fused ring compounds provided by the invention belong to novel irreversible inhibitorsof specific fibroblast growth factor receptor (FGFR) kinase, and can be used for treating related diseases such as tumors caused by abnormal FGFR kinase.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and specifically relates to a class of nitrogen-containing condensed ring compounds and a preparation method and application thereof. Background technique [0002] Abnormal expression and activation of receptor tyrosine kinases or gene mutations play a key role in the occurrence, development, invasion, metastasis, and drug resistance of tumors, making them important targets for anticancer drug development. Among them, fibroblast growth factor receptor (FGFR) is an important member of the tyrosine kinase family, mainly including four subtypes of FGFR1, FGFR2, FGFR3 and FGFR4. Due to gene amplification, mutation, fusion or ligand induction, the members of FGFR are continuously activated, which induces tumor cell proliferation and invasion, promotes angiogenesis and tumor progression. FGFRs are highly expressed and abnormally activated in a variety of tumors, and are closely related to the poor p...

Claims

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Application Information

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IPC IPC(8): C07D471/14C07D519/00A61K31/519A61K31/496A61K31/4375A61K31/4545A61K31/4995A61P35/00A61P35/02
CPCA61K31/4375A61K31/4545A61K31/496A61K31/4995A61K31/519A61P35/00A61P35/02C07D471/14C07D487/14C07D519/00
Inventor 王慧
Owner RUDONG RINGENE PHARMA CO LTD
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