ES2586231T3 - Inhibidores de glutaminil ciclasa - Google Patents
Inhibidores de glutaminil ciclasa Download PDFInfo
- Publication number
- ES2586231T3 ES2586231T3 ES11707395.7T ES11707395T ES2586231T3 ES 2586231 T3 ES2586231 T3 ES 2586231T3 ES 11707395 T ES11707395 T ES 11707395T ES 2586231 T3 ES2586231 T3 ES 2586231T3
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- ES
- Spain
- Prior art keywords
- benzo
- imidazole
- thiadiazol
- phenyl
- compound
- Prior art date
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- GEDBSTPYAKXKIP-UHFFFAOYSA-N 2-(3h-benzimidazol-5-yl)-5-[(3,4-dimethoxyphenyl)sulfonylmethyl]-1,3,4-thiadiazole Chemical compound C1=C(OC)C(OC)=CC=C1S(=O)(=O)CC1=NN=C(C=2C=C3N=CNC3=CC=2)S1 GEDBSTPYAKXKIP-UHFFFAOYSA-N 0.000 claims description 3
- ODURKURUHXWNHZ-UHFFFAOYSA-N 2-(3h-benzimidazol-5-yl)-5-[2-[4-(trifluoromethyl)phenyl]ethyl]-1,3,4-thiadiazole Chemical compound C1=CC(C(F)(F)F)=CC=C1CCC1=NN=C(C=2C=C3N=CNC3=CC=2)S1 ODURKURUHXWNHZ-UHFFFAOYSA-N 0.000 claims description 3
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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| ES2660249T3 (es) | 2012-12-20 | 2018-03-21 | Inception 2, Inc. | Compuestos de tipo triazolona y sus usos |
| US9040712B2 (en) | 2013-01-23 | 2015-05-26 | Novartis Ag | Thiadiazole analogs thereof and methods for treating SMN-deficiency-related-conditions |
| KR102318727B1 (ko) | 2013-07-31 | 2021-10-28 | 노파르티스 아게 | 1,4-이치환된 피리다진 유사체 및 smn-결핍-관련 상태를 치료하기 위한 그의 용도 |
| JP2016529311A (ja) | 2013-09-06 | 2016-09-23 | インセプション 2、 インコーポレイテッド | トリアゾロン化合物類及びそれらの使用 |
| US20170363645A1 (en) | 2014-12-19 | 2017-12-21 | Probiodrug Ag | Novel Method for the Detection of pGlu-Abeta Peptides |
| DE102015011780A1 (de) | 2015-09-16 | 2017-03-16 | Hochschule Anhalt | Neue Glutaminylcyclase-lnhibitoren |
| CN108250196B (zh) * | 2016-12-29 | 2022-12-30 | 上海汇伦医药股份有限公司 | (哌嗪-1-基)-1氢-咪唑并杂芳环化合物的制备方法 |
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| WO2018213377A1 (en) | 2017-05-17 | 2018-11-22 | Arcus Biosciences, Inc. | Quinazoline-pyrazole derivatives for the treatment of cancer-related disorders |
| PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
| EP3521308B1 (en) | 2018-01-31 | 2024-03-13 | Vivoryon Therapeutics N.V. | Humanized and de-immunized antibodies |
| JP2024506858A (ja) | 2021-02-02 | 2024-02-15 | リミナル・バイオサイエンシーズ・リミテッド | Gpr84アンタゴニストおよびその使用 |
| KR20230153387A (ko) | 2021-02-02 | 2023-11-06 | 리미널 바이오사이언시스 리미티드 | Gpr84 길항제 및 이의 용도 |
| KR102750722B1 (ko) * | 2022-03-16 | 2025-01-09 | 재단법인 대구경북첨단의료산업진흥재단 | 싸이아다이아졸 화합물 및 이를 포함하는 염증성 질환의 예방 또는 치료용 약학적 조성물 |
| CN116102440B (zh) * | 2023-02-06 | 2026-04-03 | 上海琼燕医药科技有限公司 | 1-(3,4-二氨基苯基)乙酮的制备方法 |
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-
2011
- 2011-03-03 JP JP2012555421A patent/JP6026284B2/ja active Active
- 2011-03-03 ES ES11707395.7T patent/ES2586231T3/es active Active
- 2011-03-03 US US13/040,159 patent/US9181233B2/en active Active
- 2011-03-03 WO PCT/EP2011/053154 patent/WO2011107530A2/en not_active Ceased
- 2011-03-03 EP EP11707395.7A patent/EP2542549B1/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011107530A3 (en) | 2011-11-10 |
| EP2542549A2 (en) | 2013-01-09 |
| US20110224259A1 (en) | 2011-09-15 |
| JP2013521260A (ja) | 2013-06-10 |
| JP6026284B2 (ja) | 2016-11-16 |
| EP2542549B1 (en) | 2016-05-11 |
| US9181233B2 (en) | 2015-11-10 |
| WO2011107530A2 (en) | 2011-09-09 |
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