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Last Updated: May 17, 2024

Claims for Patent: 9,604,948


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Summary for Patent: 9,604,948
Title:Process for preparing substituted 5-fluoro-1H-pyrazolopyridines
Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) ##STR00001## which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) ##STR00002## which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
Inventor(s): Fey; Peter (Wuppertal, DE), Grunenberg; Alfons (Wuppertal, DE), Bierer; Donald (Haan, DE)
Assignee: ADVERIO PHARMA GMBH (Schoenefeld, DE)
Application Number:14/796,703
Patent Claims: 1. A compound of formula (I) in crystalline form of polymorph I ##STR00085## wherein the x-ray diffractogram of the compound exhibits peak maxima of the 2 theta angle at 5.9, 6.9, 22.7.

2. The compound of claim 1, wherein the x-ray diffractogram of the compound exhibits peak maxima of the 2 theta angle at 5.9, 6.9, 16.2, 16.5, 24.1, 22.7, 24.7.

3. The compound of claim 1, wherein the IR spectrum of the compound exhibits band maxima at 1707, 1633, 1475 cm.sup.-1.

4. The compound of claim 3, wherein the IR spectrum of the compound exhibits band maxima at 1707, 1633, 1566, 1475, 1255, 1223 cm.sup.-1.

5. A process for preparing the compound of claim 1, comprising: stirring a solution of compounds of formula (I), wherein the compounds of formula (I) are present in one or more polymorphs or as a solvate in an inert solvent, at a temperature of 20.degree. C.-120.degree. C., and isolating the compound of formula (I) in the form of crystalline polymorph I from the solution.

6. A solid pharmaceutical composition comprising a compound of claim 1 and no greater proportion of any other form of the compound of the formula (I).

7. A solid pharmaceutical composition comprising a compound of claim 1 in more than 90 percent by weight based on the total amount any other form of the compound of the formula (I) present.

8. A method for treatment of cardiovascular disorders by administering an effective amount of the compound of claim 1 to a patient in need thereof.

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