KR20230041680A - 안구 질환 치료제로서의 trpv4 억제제 - Google Patents
안구 질환 치료제로서의 trpv4 억제제 Download PDFInfo
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- KR20230041680A KR20230041680A KR1020237000435A KR20237000435A KR20230041680A KR 20230041680 A KR20230041680 A KR 20230041680A KR 1020237000435 A KR1020237000435 A KR 1020237000435A KR 20237000435 A KR20237000435 A KR 20237000435A KR 20230041680 A KR20230041680 A KR 20230041680A
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- Prior art keywords
- cyclopropyl
- pyrimido
- azepin
- phenyl
- hexahydro
- Prior art date
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- -1 nitro, hydroxyl Chemical group 0.000 claims description 177
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 151
- 125000000217 alkyl group Chemical group 0.000 claims description 127
- GLZXFITXXAMCRJ-UHFFFAOYSA-N azepin-4-one Chemical compound O=C1C=CC=NC=C1 GLZXFITXXAMCRJ-UHFFFAOYSA-N 0.000 claims description 112
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 92
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- 125000001424 substituent group Chemical group 0.000 claims description 41
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- 125000003118 aryl group Chemical group 0.000 claims description 39
- 239000001257 hydrogen Substances 0.000 claims description 39
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 34
- 125000000623 heterocyclic group Chemical group 0.000 claims description 34
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 32
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- NCZYSQOTAYFTNM-UHFFFAOYSA-N 2-methyl-1-(3-morpholin-4-ylpropyl)-5-phenyl-n-[3-(trifluoromethyl)phenyl]pyrrole-3-carboxamide Chemical compound C1COCCN1CCCN1C(C)=C(C(=O)NC=2C=C(C=CC=2)C(F)(F)F)C=C1C1=CC=CC=C1 NCZYSQOTAYFTNM-UHFFFAOYSA-N 0.000 claims description 17
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- 125000004321 azepin-2-yl group Chemical group [H]N1C([H])=C([H])C([H])=C([H])C([H])=C1* 0.000 claims description 12
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- NQCQLXARDFPQDK-OAQYLSRUSA-N 6-[(2R)-2-hydroxy-2-[3-(trifluoromethyl)phenyl]acetyl]-2-[1-(4-propan-2-ylthiophen-2-yl)cyclopropyl]-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-one Chemical compound CC(C)C1=CSC(C2(CC2)C(N2)=NC(CCN(C3)C([C@@H](C4=CC(C(F)(F)F)=CC=C4)O)=O)=C3C2=O)=C1 NQCQLXARDFPQDK-OAQYLSRUSA-N 0.000 claims description 9
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- VLHCWBMCBLUFBN-HXUWFJFHSA-N 6-[(2R)-2-(3-chlorophenyl)-2-hydroxyacetyl]-2-(1-phenylcyclopropyl)-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-one Chemical compound O[C@@H](C(N(CC1)CC2=C1N=C(C1(CC1)C1=CC=CC=C1)NC2=O)=O)C1=CC(Cl)=CC=C1 VLHCWBMCBLUFBN-HXUWFJFHSA-N 0.000 claims description 8
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| WO2024217446A1 (zh) * | 2023-04-18 | 2024-10-24 | 河北乌图药业有限公司 | 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用 |
| WO2024217439A1 (zh) * | 2023-04-18 | 2024-10-24 | 河北乌图药业有限公司 | 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用 |
| CN116726013A (zh) * | 2023-04-25 | 2023-09-12 | 中国科学院大学深圳医院(光明) | Gsk2193874在防治痛性糖尿病周围神经病变中的应用 |
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| MX2017011166A (es) | 2017-08-31 | 2019-03-07 | Univ Mexico Nac Autonoma | Uso de los farmacos antagonistas del canal ionico transient receptor potential vaniloid 4 (trpv4) para el tratamiento del edema macular. |
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| JP2009527495A (ja) | 2006-02-17 | 2009-07-30 | スミスクライン・ビーチャム・コーポレイション | 新規化合物 |
| JP5294601B2 (ja) | 2007-09-28 | 2013-09-18 | 小林製薬株式会社 | Trpv4受容体抑制剤 |
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- 2021-07-16 JP JP2022536464A patent/JPWO2022014707A1/ja active Pending
- 2021-07-16 TW TW110126328A patent/TW202216143A/zh unknown
- 2021-07-16 KR KR1020237000435A patent/KR20230041680A/ko active Pending
- 2021-07-16 CA CA3189206A patent/CA3189206A1/en active Pending
- 2021-07-16 BR BR112022024553A patent/BR112022024553A2/pt unknown
- 2021-07-16 MX MX2023000610A patent/MX2023000610A/es unknown
- 2021-07-16 WO PCT/JP2021/026829 patent/WO2022014707A1/ja not_active Ceased
- 2021-07-16 EP EP21842049.5A patent/EP4183415A4/en active Pending
- 2021-07-16 CN CN202180045312.2A patent/CN115776890A/zh active Pending
- 2021-07-16 US US18/014,367 patent/US20230255965A1/en active Pending
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Also Published As
| Publication number | Publication date |
|---|---|
| BR112022024553A2 (pt) | 2023-01-24 |
| TW202216143A (zh) | 2022-05-01 |
| WO2022014707A1 (ja) | 2022-01-20 |
| US20230255965A1 (en) | 2023-08-17 |
| JPWO2022014707A1 (https=) | 2022-01-20 |
| EP4183415A4 (en) | 2024-07-17 |
| MX2023000610A (es) | 2023-02-13 |
| EP4183415A1 (en) | 2023-05-24 |
| CN115776890A (zh) | 2023-03-10 |
| CA3189206A1 (en) | 2022-01-20 |
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