IP Library Granted Patent US 10,633,356
Granted Patent B2
US 10,633,356 · App. 16/278,778 · Granted Apr 28, 2020

Hydrates of substituted 5-fluoro-1H-pyrazolopyridines

Inventors: Peter Fey (Wuppertal, DE); Alfons Grunenberg (Wuppertal, DE); Donald Bierer (Haan, DE)
Assignee: ADVERIO PHARMA GMBH
C07D295/104A61P9/00C07C303/28C07C309/04C07C317/04C07D265/30C07D295/067C07D471/04C07B2200/13
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,633,356
App. No.
16/278,778
Granted
Apr 28, 2020
Kind
B2
Abstract

The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) 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) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

Claims (13)

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

wherein the hydrate is a monohydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 9.6, 18.2, and 25.7 or a dihydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 7.9, 24.9, and 25.5.

2. The hydrate according to claim 1 , wherein the hydrate is a monohydrate containing about 4.1% water or a dihydrate containing about 7.8% water.

3. The hydrate according to claim 1 , wherein the hydrate is a monohydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 8.5, 9.6, 18.2, 20.2, and 25.7 or a dihydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 7.9, 19.8, 24.9, 25.5, and 27.8.

4. The hydrate according to claim 1 , wherein the hydrate is a monohydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 8.5, 9.6, 18.2, 20.2, 23.5, 25.7, and 29.4 or a dihydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 5.9, 7.9, 9.0, 19.8, 24.9, 25.5, and 27.8.

5. The hydrate according to claim 1 , wherein the hydrate is a monohydrate containing about 4.1% water.

6. The hydrate according to claim 1 , wherein the hydrate is a monohydrate with the x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 9.6, 18.2, and 25.7.

7. The hydrate according to claim 1 , wherein the hydrate is a monohydrate with the x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 8.5, 9.6, 18.2, 20.2, and 25.7.

8. The hydrate according to claim 1 , wherein the hydrate is a monohydrate with the x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 8.5, 9.6, 18.2, 20.2, 23.5, 25.7, and 29.4.

9. The hydrate according to claim 1 , wherein the hydrate is a dihydrate containing about 7.8% water.

10. The hydrate according to claim 1 , wherein the hydrate is a dihydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 7.9, 24.9, and 25.5.

11. The hydrate according to claim 1 , wherein the hydrate is a dihydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 7.9, 19.8, 24.9, 25.5, and 27.8.

12. The hydrate according to claim 1 , wherein the hydrate is a dihydrate with an x-ray diffractogram exhibiting peak maxima of the 2 theta angle at 5.9, 7.9, 9.0, 19.8, 24.9, 25.5, and 27.8.

Assignments (1)
CHANGE OF PATENTEE ADDRESS Recorded Feb 8, 2021
From: ADVERIO PHARMA GMBH
To: ADVERIO PHARMA GMBH
Reel/Frame 056907/0570 →
Priority Claims (2)
EP 11190789 · Nov 25, 2011 · regional
EP 11192301 · Dec 7, 2011 · regional
Continuity (6)
Continuation 15812534 · Nov 14, 2017
Division 15435964 · Feb 17, 2017
Division 14796703 · Jul 10, 2015
Division 14320875 · Jul 1, 2014
Division 13684670 · Nov 26, 2012
Related Publication 20190177287A1 · Jun 13, 2019