US2013217708A1PendingUtilityA1
Meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide
Est. expirySep 30, 2030(~4.2 yrs left)· nominal 20-yr term from priority
A61P 31/12A61P 31/00A61P 31/16A61K 9/0019A61K 47/22C07D 241/24A61K 31/497A61K 9/19A61K 47/26A61K 47/183A61K 31/4965C07C 215/10A61K 9/08A61K 47/18
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Claims
Abstract
A preparation replete with a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide has superior solubility, and is useful as a preparation for injection.
Claims
exact text as granted — not AI-modified1 : A meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or a hydrate thereof.
2 : The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 1 , in a crystal form.
3 : The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 1 , in an amorphous form.
4 : An injectable preparation comprising the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 1 .
5 : The injectable preparation of claim 4 , wherein the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof is in a crystal form.
6 : The injectable preparation of claim 4 , wherein the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof is in an amorphous form.
7 : The injectable preparation of claim 4 , further comprising an amino acid and a saccharide, or an amino acid and a sugar alcohol.
8 : A lyophilized preparation comprising a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide.
9 : The lyophilized preparation of claim 8 , wherein the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide is in a crystal form.
10 : The lyophilized preparation of claim 8 , wherein the meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide is in an amorphous form.
11 : The lyophilized preparation of claim 8 , further comprising an amino acid and a saccharide, or an amino acid and a sugar alcohol.
12 : A process for producing a lyophilized preparation comprising a crystal of a meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide, the process comprising:
(1) cooling an aqueous solution comprising 6-fluoro-3-hydroxy-2-pyrazinecarboxamide and meglumine to produce a frozen product; (2) increasing the temperature of the frozen product; (3) cooling the frozen product again; and (4) carrying out lyophilization.
13 : The process according to claim 12 , wherein in (2) the temperature of the frozen product is increased to a temperature within the range of −20 of −5° C.
14 : The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 1 , which is the salt.
15 : The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 1 , which is the hydrate.
16 : The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 2 , which is the salt.
17 : The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 2 , which is the hydrate.
18 : The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 3 , which is the salt.
19 : The meglumine salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or the hydrate thereof of claim 3 , which is the hydrate.
20 : The injectable preparation of claim 5 , further comprising an amino acid and a saccharide, or an amino acid and a sugar alcohol.Join the waitlist — get patent alerts
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