5-(4-FLUOROPHENYL)-2,3-DIHYDRO-1H-IMIDAZO[1,2-A]IMIDAZOLE DERIVATIVES AS ALK INHIBITORS FOR THE TREATMENT OF FIBROSIS
The present invention relates to 5-(4-fluorophenyl)-2,3-dihydro-1H- imidazo[1,2-a]imidazole derivatives of formula (I) as ALK5 inhibitors (transforming growth factor 3 (TGF3) type 1 receptor) for the treatment of fibrosis, such as e.g. pulmonary fibrosis, idiopathic pulmonary fibrosis (IPF), hepatic fibrosis, renal fibrosis, ocular fibrosis, cardiac fibrosis, arterial fibrosis and systemic sclerosis. An example with good activity is e.g. example 5: 2-(dimethylamino) -N-(2-fluoro-5-(6-(6-methylpyridin-2-yl)-2,3-dihydro-1H imidazo[1,2- a]imidazol-5-yl)phenyl)acetamide (Formula IA). Pharmacological data is provided: (Table 3).
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Patent| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Europäisches Patentamt - (2023) vom: 28. Dez. Zur Gesamtaufnahme - year:2023 |
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| Sprache: |
Englisch |
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| Beteiligte Personen: |
PALA DANIELE [VerfasserIn] |
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| Links: |
Volltext [kostenfrei] |
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| Anmerkungen: |
Source: www.epo.org (no modifications made), First posted: 2023-12-28, Last update posted on www.tib.eu: 2024-01-24, Last updated: 2024-02-02 |
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| Patentnummer: |
WO2023247592 |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
EPA018986900 |
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| 245 | 1 | 0 | |a 5-(4-FLUOROPHENYL)-2,3-DIHYDRO-1H-IMIDAZO[1,2-A]IMIDAZOLE DERIVATIVES AS ALK INHIBITORS FOR THE TREATMENT OF FIBROSIS |
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| 520 | |a The present invention relates to 5-(4-fluorophenyl)-2,3-dihydro-1H- imidazo[1,2-a]imidazole derivatives of formula (I) as ALK5 inhibitors (transforming growth factor 3 (TGF3) type 1 receptor) for the treatment of fibrosis, such as e.g. pulmonary fibrosis, idiopathic pulmonary fibrosis (IPF), hepatic fibrosis, renal fibrosis, ocular fibrosis, cardiac fibrosis, arterial fibrosis and systemic sclerosis. An example with good activity is e.g. example 5: 2-(dimethylamino) -N-(2-fluoro-5-(6-(6-methylpyridin-2-yl)-2,3-dihydro-1H imidazo[1,2- a]imidazol-5-yl)phenyl)acetamide (Formula IA). Pharmacological data is provided: (Table 3) | ||
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