WO2023084313 - THERAPEUTIC COCRYSTALS OF 3-{[5-(AZETIDINE-1-YLCARBONYL)PYRAZIN-2-YL]OXY}-5-{[(1 S)-1 -METHYL-2- (METHYLOXY)ETHYL]OXY)-N-(5-METHYLPYRAZIN-2-YL)BENZAMIDE
National phase entry:
Publication Number
WO/2023/084313
Publication Date
19.05.2023
International Application No.
PCT/IB2022/000775
International Filing Date
12.10.2022
Title **
[English]
THERAPEUTIC COCRYSTALS OF 3-{[5-(AZETIDINE-1-YLCARBONYL)PYRAZIN-2-YL]OXY}-5-{[(1 S)-1 -METHYL-2- (METHYLOXY)ETHYL]OXY)-N-(5-METHYLPYRAZIN-2-YL)BENZAMIDE
[French]
CO-CRISTAUX DE BENZAMIDE THÉRAPEUTIQUES
Applicants **
CONDUIT UK MANAGEMENT LTD
110 Hillside Gardens Edgware
London HA8 8HD, GB
Inventors
EBERLIN, Alex
6 Scholars Walk
Cambridge CB4 1EJ, GB
FRAMPTON, Christopher
High Green House, 3 St. Andrews Mead
Mickfield
Stowmarket, Suffolk IP14 4NY, GB
HOLLAND, Joanne
20b Pages Close, Histon
Cambridge, Cambridgeshire CB24 9HF, GB
Priority Data
63/239,979
02.09.2021
US
Application details
| Total Number of Claims/PCT | * |
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| Number of Drawings | * |
| Pages for Publication | * |
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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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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing | 1637 | |
| EPO | Filing, Examination | 7988 | |
| Japan | Filing | 596 | |
| South Korea | Filing | 575 | |
| USA | Filing, Examination | 5710 |
Total: 16506 USD
The term for entry into the National Phase has expired. This quotation is for informational purposes only
Abstract[English]
Cocrystals of a benzamide compound, specifically 3-{[5-(azetidine-l-ylcarbonyl)pyrazin-2- yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, therapeutic uses of the benzamide cocrystals and pharmaceutical compositions containing them are disclosed. For purposes of this disclosure and for ease of understanding, "benzamide" or "benzamide compound" as well as "AZD1656" refer to 3-{[5-(azetidine-1-ylcarbonyl)pyrazin-2- yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide. The benzamide cocrystals of the invention include a 1:1 benzamide fumaric acid (Cocrystal 1), a 1:1 benzamide maleic acid (Cocrystal 2), a 1:1 benzamide malonic acid (Cocrystal 3), a 1:1 benzamide L-tartaric acid hydrate (Cocrystal 4), and a 1:1 benzamide gentisic acid (Cocrystal 5), which includes a 1:1 benzamide gentisic acid form 1 (Cocrystal 5A), a 1:1 benzamide gentisic acid form 2 (Cocrystal 5B), a 1:1 benzamide gentisic acid form 3 (Cocrystal 5C), and a 1:1 benzamide gentisic acid form 4 (Cocrystal 5D).[French]
Sont divulgués des co-cristaux d'un composé de benzamide, plus particulièrement de 3-{[5-(azétidine-l-ylcarbonyl)pyrazin-2- yl]oxy}-5-{[(1S)-1-méthyl-2-(méthyloxy)éthyl]oxy}-N-(5-méthylpyrazin-2-yl)benzamide, des utilisations thérapeutiques des co-cristaux de benzamide et des compositions pharmaceutiques les contenant. Aux fins de la présente divulgation et pour faciliter la compréhension, le « benzamide » ou le « composé de benzamide » ainsi que « AZD1656 » se réfèrent au 3-{[5-(azétidine-1-ylcarbonyl)pyrazin-2- yl]oxy}-5-{[(1S)-1-méthyl-2-(méthyloxy)éthyl]oxy}-N-(5-méthylpyrazin-2-yl)benzamide. Les co-cristaux de benzamide de l'invention comprennent un acide fumarique 1:1 benzamide (co-cristal 1), un acide maléique 1:1 benzamide (co-cristal 2), un acide malonique 1:1 benzamide (co-cristal 3), un hydrate d'acide L-tartrique 1:1 benzamide (co-cristal 4) et un acide gentisique 1:1 benzamide (co-cristal 5), qui comprend une forme 1 d'acide gentisique 1:1 benzamide (co-cristal 5A), une forme 2 d'acide gentisique 1:1 benzamide (co-cristal 5B), une forme 3 d'acide gentisique 1:1 benzamide (co-cristal 5C) et une forme 4 d'acide gentisique 1:1 benzamide (co-cristal 5D).