CN111499612A - 一种作为irak抑制剂的化合物及其制备方法和用途 - Google Patents
一种作为irak抑制剂的化合物及其制备方法和用途 Download PDFInfo
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- CN111499612A CN111499612A CN202010049702.4A CN202010049702A CN111499612A CN 111499612 A CN111499612 A CN 111499612A CN 202010049702 A CN202010049702 A CN 202010049702A CN 111499612 A CN111499612 A CN 111499612A
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- alkyl
- compound
- cycloalkyl
- radical
- membered heterocyclyl
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- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 125000005493 quinolyl group Chemical group 0.000 description 1
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- 125000003107 substituted aryl group Chemical group 0.000 description 1
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- 238000004885 tandem mass spectrometry Methods 0.000 description 1
- FRACPXUHUTXLCX-BELIEFIBSA-N tert-butyl N-{1-[(1S)-1-{[(1R,2S)-1-(benzylcarbamoyl)-1-hydroxy-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl]carbamoyl}-2-cyclopropylethyl]-2-oxopyridin-3-yl}carbamate Chemical compound CC(C)(C)OC(=O)NC1=CC=CN(C1=O)[C@@H](CC2CC2)C(=O)N[C@@H](C[C@@H]3CCNC3=O)[C@H](C(=O)NCC4=CC=CC=C4)O FRACPXUHUTXLCX-BELIEFIBSA-N 0.000 description 1
- 108091008743 testicular receptors 4 Proteins 0.000 description 1
- FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 1
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Classifications
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C07D487/04—Ortho-condensed systems
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Abstract
Description
化合物编号 | IC<sub>50</sub>(nM) | 化合物编号 | IC<sub>50</sub>(nM) |
001 | 3.6 | 028 | 8.6 |
002 | 6.8 | 040 | 7.8 |
013 | 28 | 041 | 23 |
014 | 7.6 | 068 | 4.4 |
015 | 5.6 | 069 | 6.7 |
017 | 10 | 070 | 4.8 |
018 | 14 | 071 | 10 |
019 | 80 | 072 | 8.4 |
020 | 59 | 073 | 14 |
021 | 22 | 074 | 35 |
022 | 9.7 | 075 | 5.8 |
025 | 1.0 | 077 | 0.89 |
026 | 2.1 | 078 | 3.0 |
027 | 260 | 076 | 5.9 |
化合物编号 | TNF-α的抑制率% | 化合物编号 | TNF-α的抑制率% |
001 | 77% | 021 | 68% |
002 | 69% | 026 | 76% |
013 | 70% | 028 | 93% |
014 | 81% | 040 | 61% |
015 | 87% | 072 | 79% |
017 | 74% | 074 | 90% |
018 | 77% |
Claims (10)
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Cited By (4)
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WO2022194252A1 (zh) * | 2021-03-19 | 2022-09-22 | 上海美悦生物科技发展有限公司 | 一种化合物的多晶型及其制备方法和应用 |
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CN115252609A (zh) * | 2022-08-01 | 2022-11-01 | 上海美悦生物科技发展有限公司 | 一种irak4抑制剂的组合物及其制备方法、用途 |
CN117209489A (zh) * | 2023-05-30 | 2023-12-12 | 杭州邦顺制药有限公司 | Irak激酶抑制剂 |
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