CN107207531B - 作为TGF-β抑制剂的稠合的咪唑衍生物 - Google Patents
作为TGF-β抑制剂的稠合的咪唑衍生物 Download PDFInfo
- Publication number
- CN107207531B CN107207531B CN201580074061.5A CN201580074061A CN107207531B CN 107207531 B CN107207531 B CN 107207531B CN 201580074061 A CN201580074061 A CN 201580074061A CN 107207531 B CN107207531 B CN 107207531B
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- Prior art keywords
- imidazol
- dihydro
- pyrrolo
- pyridine
- methylphenyl
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- A61K31/4164—1,3-Diazoles
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462082959P | 2014-11-21 | 2014-11-21 | |
| US62/082,959 | 2014-11-21 | ||
| US201562141509P | 2015-04-01 | 2015-04-01 | |
| US62/141,509 | 2015-04-01 | ||
| PCT/US2015/060872 WO2016081364A1 (en) | 2014-11-21 | 2015-11-16 | Fused imidazole derivatives as tgf-beta inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107207531A CN107207531A (zh) | 2017-09-26 |
| CN107207531B true CN107207531B (zh) | 2021-05-25 |
Family
ID=54704137
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580074061.5A Expired - Fee Related CN107207531B (zh) | 2014-11-21 | 2015-11-16 | 作为TGF-β抑制剂的稠合的咪唑衍生物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10696693B2 (https=) |
| EP (1) | EP3221318B1 (https=) |
| JP (1) | JP6789941B2 (https=) |
| CN (1) | CN107207531B (https=) |
| ES (1) | ES2895626T3 (https=) |
| WO (1) | WO2016081364A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2928773T3 (es) | 2017-01-17 | 2022-11-22 | Heparegenix Gmbh | Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos |
| US11124509B2 (en) | 2017-03-23 | 2021-09-21 | Clavius Pharmaceuticals, LLC. | Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment |
| US12077548B2 (en) * | 2018-08-22 | 2024-09-03 | Clavius Pharmaceuticals, LLC. | Substituted imidazoles for the inhibition of TGF-β and methods of treatment |
| SG11202104331YA (en) | 2018-12-11 | 2021-05-28 | Theravance Biopharma R&D Ip Llc | Naphthyridine and quinoline derivatives useful as alk5 inhibitors |
| CN114728941A (zh) | 2019-11-22 | 2022-07-08 | 施万生物制药研发Ip有限责任公司 | 作为alk5抑制剂的经取代的1,5-萘啶或喹啉 |
| KR102801205B1 (ko) | 2019-12-04 | 2025-04-29 | 허난 즈웨이 바이오메디슨 씨오., 엘티디. | 브루톤 티로신 키나제 억제제인 이미다졸 카복사마이드 유도체 |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| US20250270215A1 (en) | 2022-04-27 | 2025-08-28 | Chiesi Farmaceutici S.P.A. | Imidazole derivatives as alk5 inhibitors |
| US20250368650A1 (en) | 2022-06-22 | 2025-12-04 | Chiesi Farmaceutici S.P.A. | 5-(4-fluorophenyl)-2,3-dihydro-1h-imidazo[1,2-a]imidazole derivatives as alk inhibitors for the treatment of fibrosis |
| EP4556478A4 (en) * | 2022-08-08 | 2025-10-22 | Medinno Pharmaceutical Tech Zhuhai Co Ltd | TGF-BETA INHIBITOR COMPOUND AND USE THEREOF |
| PL248267B1 (pl) * | 2023-04-13 | 2025-11-17 | Univ Medyczny W Lublinie | 1-arylo-6-hydroksyimino-5(1H)okso-2,3-dihydroimidazo[1,2-a] imidazole oraz sposób ich wytwarzania oraz ich zastosowanie |
Family Cites Families (13)
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| AU772694B2 (en) | 1999-01-21 | 2004-05-06 | Metamorphix International, Inc. | Growth differentiation factor inhibitors and uses therefor |
| DE60018037T2 (de) * | 1999-11-10 | 2006-01-12 | Ortho-Mcneil Pharmaceutical, Inc. | Substituierte 2-aryl-3-(heteroaryl)-imidazo[1,2-alpha]pyrimidine und ihren verwandten arzneimittel und verfahren |
| US7320789B2 (en) | 2001-09-26 | 2008-01-22 | Wyeth | Antibody inhibitors of GDF-8 and uses thereof |
| WO2004014900A1 (en) | 2002-08-09 | 2004-02-19 | Eli Lilly And Company | Benzimidazoles and benzothiazoles as inhibitors of map kinase |
| AU2003290734A1 (en) * | 2002-11-27 | 2004-06-23 | Eli Lilly And Company | Novel compounds as pharmaceutical agents |
| PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
| EP1973914A2 (en) * | 2005-12-22 | 2008-10-01 | Biogen Idec MA Inc. | Transforming growth factor modulators |
| WO2008063287A2 (en) | 2006-10-06 | 2008-05-29 | Abbott Laboratories | Novel imidazothiazoles and imidazoxazoles |
| WO2009005675A1 (en) * | 2007-06-28 | 2009-01-08 | Abbott Laboratories | Novel triazolopyridazines |
| DK2731949T3 (en) * | 2011-07-13 | 2018-06-14 | Tiumbio Co Ltd | 2-PYRIDYL-SUBSTITUTED IMIDAZOLS AS ALK5 AND / OR ALK4 INHIBITORS |
| JP6267231B2 (ja) * | 2012-12-21 | 2018-01-24 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | カゼインキナーゼ1δ/ε阻害剤としての新規な置換イミダゾール |
| US20150159134A1 (en) * | 2013-12-11 | 2015-06-11 | Pfizer Limited | Method for producing retinal pigment epithelial cells |
| CA2933083A1 (en) * | 2013-12-11 | 2015-06-18 | Pfizer Limited | Method for producing retinal pigment epithelial cells |
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- 2015-11-16 WO PCT/US2015/060872 patent/WO2016081364A1/en not_active Ceased
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- 2015-11-16 US US15/527,908 patent/US10696693B2/en active Active
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| US20180346487A1 (en) | 2018-12-06 |
| CN107207531A (zh) | 2017-09-26 |
| EP3221318B1 (en) | 2021-08-25 |
| JP6789941B2 (ja) | 2020-11-25 |
| US10696693B2 (en) | 2020-06-30 |
| ES2895626T3 (es) | 2022-02-22 |
| JP2018501209A (ja) | 2018-01-18 |
| EP3221318A1 (en) | 2017-09-27 |
| WO2016081364A1 (en) | 2016-05-26 |
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