CN107531633B - 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 - Google Patents
5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 Download PDFInfo
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- CN107531633B CN107531633B CN201680021804.7A CN201680021804A CN107531633B CN 107531633 B CN107531633 B CN 107531633B CN 201680021804 A CN201680021804 A CN 201680021804A CN 107531633 B CN107531633 B CN 107531633B
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/56—Amides
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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Abstract
Description
编号 | mGluR5 IC<sub>50</sub> | mGluR1 IC<sub>50</sub> | mGluR5/mGluR1 |
ZD001 | 13.9nM | >100μM | >7194 |
ZD004 | 11nM | >100μM | >9091 |
ZD012 | 14.4nM | >100μM | >6944 |
ZD013 | 14.2nM | >100μM | >7042 |
ZD014 | 14.8nM | >100μM | >6757 |
ZD016 | 29.2nM | >100μM | >3425 |
ZD036 | 20.29nM | >100μM | >4929 |
ZD037 | 7.312nM | >100μM | >13676 |
ZD042 | 19.4nM | >100μM | >5155 |
ZD043 | 5.601nM | >100μM | >17854 |
ZD046 | 15.15nM | >100μM | >6601 |
ZD047 | 6.647nM | >100μM | >15044 |
ZD049 | 37.99nM | >100μM | >2632 |
JNJ16259685 | —— | 91.23nM | —— |
Claims (10)
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EA202091787A1 (ru) * | 2018-01-26 | 2020-11-06 | Рекордати Индустрия Кимика Э Фармасеутика С.П.А | ТРИАЗОЛ-, ИМИДАЗОЛ- И ПИРРОЛ-КОНДЕНСИРОВАННЫЕ ПИПЕРАЗИНОВЫЕ ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ mGLu5 РЕЦЕПТОРОВ |
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WO2023122212A2 (en) * | 2021-12-21 | 2023-06-29 | Southern Research Institute | Substituted phenyl ethynyl pyridine carboxamides as potent inhibitors of sars virus |
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