WO2023247592 - 5-(4-FLUOROPHENYL)-2,3-DIHYDRO-1H-IMIDAZO[1,2-A]IMIDAZOLE DERIVATIVES AS ALK INHIBITORS FOR THE TREATMENT OF FIBROSIS
National phase entry:
Publication Number
WO/2023/247592
Publication Date
28.12.2023
International Application No.
PCT/EP2023/066728
International Filing Date
21.06.2023
Title **
[English]
5-(4-FLUOROPHENYL)-2,3-DIHYDRO-1H-IMIDAZO[1,2-A]IMIDAZOLE DERIVATIVES AS ALK INHIBITORS FOR THE TREATMENT OF FIBROSIS
[French]
DÉRIVÉS DE 5-(4-FLUOROPHÉNYL)-2,3-DIHYDRO-1H-IMIDAZO[1,2-A]IMIDAZOLE UTILISÉS EN TANT QU'INHIBITEURS D'ALK POUR TRAITER LA FIBROSE
Applicants **
CHIESI FARMACEUTICI S.P.A.
Via Palermo 26/A
43122 Parma, IT
Inventors
PALA, Daniele
c/o Chiesi Farmaceutici S.p.a.
Via Palermo 26/A
43122 Parma, IT
PIZZIRANI, Daniela
c/o Chiesi Farmaceutici S.p.a.
Via Palermo 26/A
43122 Parma, IT
GUARIENTO, Sara
c/o Chiesi Farmaceutici S.p.a.
Via Palermo 26/A
43122 Parma, IT
RONCHI, Paolo
c/o Chiesi Farmaceutici S.p.a.
Via Palermo 26/A
43122 Parma, IT
Priority Data
22180542.7
22.06.2022
EP
Application details
| Total Number of Claims/PCT | * |
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| Number of Drawings | * |
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International Searching Authority |
EPO
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| Applicant's Legal Status |
Legal Entity
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| Entry into National Phase under |
Chapter I
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| Translation |
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Recalculate
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing | 1165 | |
| EPO | Filing, Examination | 4964 | |
| Japan | Filing | 597 | |
| South Korea | Filing | 575 | |
| USA | Filing, Examination | 3310 |
Total: 10611 USD
The term for entry into the National Phase has expired. This quotation is for informational purposes only
Abstract[English]
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)[French]
La présente invention concerne des dérivés de 5-(4-fluorophényl)-2,3-dihydro-1H-imidazo[1,2-a]imidazole de formule (I) utilisés en tant qu'inhibiteurs d'ALK5 (facteur de croissance transformant 3 (TGF3) de type 1) pour le traitement de la fibrose, telle que, par exemple, la fibrose pulmonaire, la fibrose pulmonaire idiopathique (IPF), la fibrose hépatique, la fibrose rénale, la fibrose oculaire, la fibrose cardiaque, la fibrose artérielle et la sclérose systémique. Un exemple ayant une bonne activité est, par exemple, 5 : 2-(diméthylamino)-N-(2-fluoro-5-(6-(6-méthylpyridin-2-yl)-2,3-dihydro-1H imidazo[1,2-a]imidazol-5-yl)phényl)acétamide (formule IA). Des données pharmacologiques sont fournies : (TABLEAU 3)