IP Library Granted Patent US 10,501,437
Granted Patent B2
US 10,501,437 · App. 16/097,506 · Granted Dec 10, 2019

Crystalline forms of N-[2-(3-Hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2H-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide

Inventors: Tobias Thaler (Köln, DE); Johannes Platzek (Berlin, DE); Nicolas Guimond (Wuppertal, DE)
Assignee: Bayer Pharma Aktiengesellschaft
C07D401/12A61K9/2095C07B2200/13
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Quick Facts
Patent No.
US 10,501,437
App. No.
16/097,506
Granted
Dec 10, 2019
Kind
B2
Abstract

The present invention relates to crystalline forms of N-[2-(3-Hydroxy-3-methylbutyl)-6-(2-hydroxypropan-2-yl)-2H-indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide, to processes for their preparation, to pharmaceutical compositions comprising them and to their use in the control of disorders.

Claims (13)

1. A hydrate of the compound of formula (I)

wherein the hydrate has a X-ray powder diffraction diagram at 25° C. and with Cu-K alpha 1 as radiation source displaying at least the following reflections, quoted as 2Theta value ±0.2°: 9.4, 10.8, and 15.0.

2. The hydrate of the compound of formula (I) of claim 1 , wherein the hydrate has a X-ray powder diffraction diagram at 25° C. and with Cu-K alpha 1 as radiation source displaying at least the following reflections, quoted as 2Theta value ±0.2°: 9.4, 10.8, 15.0, 16.0, and 17.0.

3. The hydrate of the compound of formula (I) of claim 1 , wherein the hydrate has a X-ray powder diffraction diagram at 25° C. and with Cu-K alpha 1 as radiation source displaying at least the following reflections, quoted as 2Theta value ±0.2°: 9.4, 10.8, 15.0, 16.0, 17.0, 20.1, and 22.9.

4. The hydrate of the compound of formula (I) of claim 1 , wherein the hydrate has a X-ray powder diffraction diagram at 25° C. and with Cu-K alpha 1 as radiation source displaying at least the following reflections, quoted as 2Theta value ±0.2°: 9.4, 10.8, 15.0, 16.0, 17.0, 20.1, 22.9, 24.3, 26.6, and 29.8.

5. A pharmaceutical composition comprising only a hydrate of the compound of formula (I) according to claim 1 mainly and no significant fractions of another form of the compound of formula (I).

6. A pharmaceutical composition comprising a hydrate of the compound of formula (I) according to claim 1 and pharmaceutically acceptable excipients.

7. The pharmaceutical composition of claim 6 , comprising only the hydrate of the compound of formula (I) mainly and no significant fractions of another form of the compound of formula (I).

8. The pharmaceutical composition of claim 6 , comprising the hydrate of the compound of formula (I) in more than 85 percent by weight related to the total amount of all forms of the compound of the formula (I) present in the composition.

9. The pharmaceutical composition of claim 8 , comprising the hydrate of the compound of formula (I) in more than 90 percent by weight related to the total amount of all forms of the compound of formula (I) present in the composition.

10. A method for treatment of rheumatoid arthritis in a human in need thereof, comprising administering to the human an effective amount of a hydrate of the compound of formula (I) according to claim 1 .

11. A method for treatment of rheumatoid arthritis in a human in need thereof, comprising administering to the human an effective amount of a pharmaceutical composition according to claim 5 .

12. A method for treatment of rheumatoid arthritis in a human in need thereof, comprising administering to the human an effective amount of a pharmaceutical composition according to claim 6 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 2, 2019
From: THALER, TOBIAS; PLATZEK, JOHANNES; GUIMOND, NICOLAS
To: BAYER PHARMA AKTIENGESELLSCHAFT
Reel/Frame 049658/0344 →
Priority Claims (2)
EP 16167649 · Apr 29, 2016 · regional
EP 16167650 · Apr 29, 2016 · regional
Continuity (1)
Related Publication 20190152944A1 · May 23, 2019
Cited By (2)
US 12,459,916 US 12,559,473