SYNTHETIC INTERMEDIATE OF 1-(2-DEOXY-2-FLUORO-4-THIO-ß-D-ARABINOFURANOSYL)CYTOSINE, SYNTHETIC INTERMEDIATE OF THIONUCLEOSIDE, AND METHOD FOR PRODUCING THE SAME
US-2016362389-A1 · Dec 15, 2016 · US
Salt of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine
US9896471B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9896471-B2 |
| Application number | US-201414498334-A |
| Country | US |
| Kind code | B2 |
| Filing date | Sep 26, 2014 |
| Priority date | Mar 28, 2012 |
| Publication date | Feb 20, 2018 |
| Grant date | Feb 20, 2018 |
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- Title
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Abstract
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A superior antitumor agent is provided. A salt of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine shows at least one or more of such characteristics as (1) it has superior antitumor activity, (2) it shows superior crystallinity, (3) it shows high water solubility, (4) it does not show deliquescent property, (5) it shows superior flowability, (6) it shows superior tableting property, (7) it can be manufactured with less environmental load, and (8) it can be manufactured in a large scale, and therefore it is useful as a bulk drug for medicaments.
First claim
Opening claim text (preview).
The invention claimed is: 1. A crystal of methanesulfonate of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine showing characteristic peaks at diffraction angles (2θ) of 19.8, 21.8, 27.5, 28.4, and 29.9 degrees in powder X-ray diffractometry. 2. A pharmaceutical composition containing the crystal according to claim 1 and a pharmaceutically acceptable additive. 3. The pharmaceutical composition according to claim 2 , which is for use in a treatment of a tumor. 4. A method for preparing the crystal according to claim 1 , which comprises the step of converting 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine into the methanesulfonate thereof and crystallizing said salt. 5. A method for treating a tumor in a subject comprising the step of administering to a subject in need of such treatment the crystal according to claim 1 . 6. A crystal of hydrochloride of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine showing characteristic peaks at diffraction angles (2θ) of 9.2, 14.7, 15.7, 22.9, and 27.3 degrees in powder X-ray diffractometry. 7. A pharmaceutical composition containing the crystal according to claim 6 and a pharmaceutically acceptable additive. 8. The pharmaceutical composition according to claim 6 , which is for use in a treatment of a tumor. 9. A method for preparing the crystal according to claim 6 , which comprises the step of converting 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine into the hydrochloride thereof and crystallizing said salt. 10. A method for treating a tumor in a subject comprising the step of administering to a subject in need of such treatment the crystal according to claim 6 .
Assignees
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Classifications
Antineoplastic agents · CPC title
having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid · CPC title
with 2-deoxyribosyl as the saccharide radical · CPC title
- C07H19/06Primary
Pyrimidine radicals · CPC title
containing only one sulfo group · CPC title
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Frequently asked questions
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- What does patent US9896471B2 cover?
- A superior antitumor agent is provided. A salt of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine shows at least one or more of such characteristics as (1) it has superior antitumor activity, (2) it shows superior crystallinity, (3) it shows high water solubility, (4) it does not show deliquescent property, (5) it shows superior flowability, (6) it shows superior tableting property, (7…
- Who is the assignee on this patent?
- Fujifilm Corp
- What technology area does this patent fall under?
- Primary CPC classification C07H19/06. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Feb 20 2018 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 5 related publications on this page (citations in our corpus or others sharing the same primary CPC).