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.
Inventors
PALA, Daniele
PIZZIRANI, Daniela
GUARIENTO, Sara
RONCHI, Paolo
Priority Data
22180542.7
22.06.2022
EP
Application details
| Total Number of Claims/PCT | * |
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International Searching Authority |
EPO
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| Recordal of a Change of the Applicant's Name/Address |
Change of Applicant's Name and Address
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| Type of Assignment |
The Standard Agent's Assignment
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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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| Patent Delivery |
Send the Letters Patent by Courier
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| Translation |
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 2093 | |
| EPO | Filing, Examination, Granting | 8524 | |
| Japan | Filing, Examination, Granting | 2141 | |
| South Korea | Filing, Examination, Granting | 1995 | |
| USA | Filing, Examination, Granting | 5340 |
Total:
20,093
The term for entry into the National Phase has expired. This quotation is for informational purposes only
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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)