IP Library Granted Patent US 12,358,940
Granted Patent B2
US 12,358,940 · App. 18/963,281 · Granted Jul 15, 2025

Method of making nicotinamide ribofuranoside salts, nicotinamide ribofuranoside salts as such, and uses thereof

Inventors: Günter Schabert (Goldach, CH); Urs Spitz (St. Gallen, CH); Aysel Soydemir (Rorschach, CH); Iris Zimmermann (Bregenz, AT)
Assignee: Biosynth AG
C07H19/048C07H1/06
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Quick Facts
Patent No.
US 12,358,940
App. No.
18/963,281
Filed
Nov 27, 2024
Granted
Jul 15, 2025
Kind
B2
Art Unit
1693
USPC
536/28.1
Abstract

The present invention relates to a method of making nicotinamide ribofuranosie salts, in particular pharmaceutically acceptable nicotinamide ribofuranoside salts. The invention further relates to the nicotinamide ribofuranoside salts as such, in particular carboxylic acid salts in crystalline form, and their use in nutritional supplements and pharmaceutical compositions.

Claims (27)

1. A crystalline form of nicotinamide-β-D-ribofuranoside hydrogen tartrate.

2. The crystalline form of claim 1 , wherein the crystalline form is a crystalline form of nicotinamide-β-D-ribofuranoside hydrogen L-tartrate.

3. The crystalline form of claim 2 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having one or more peaks as provided in Table 5, ±0.2 degrees two theta.

4. The crystalline form of claim 2 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 17.0±0.2, 22.7±0.2, and 23.6±0.2 degrees two theta.

5. The crystalline form of claim 2 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 17.0±0.2, 22.7±0.2, 23.6±0.2, and 27.5±0.2 degrees two theta.

6. The crystalline form of claim 1 , wherein the crystalline form is a crystalline form of nicotinamide-β-D-ribofuranoside hydrogen D-tartrate.

7. The crystalline form of claim 6 , wherein the crystalline form is a crystalline form of nicotinamide-β-D-ribofuranoside hydrogen D-tartrate monohydrate or anhydrous nicotinamide-β-D-ribofuranoside hydrogen D-tartrate.

8. The crystalline form of claim 7 , wherein the crystalline form is a crystalline form of nicotinamide-β-D-ribofuranoside hydrogen D-tartrate monohydrate, wherein the crystalline form is characterized by a powder X-ray diffraction pattern having one or more peaks as provided in Table 4, ±0.2 degrees two theta.

9. The crystalline form of claim 8 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 16.4±0.2, 21.7±0.2 and 24.0±0.2 degrees two theta.

10. The crystalline form of claim 8 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 16.4±0.2, 21.7±0.2, 23.2±0.2, 24.0±0.2, 26.3±0.2, and 29.8±0.2 degrees two theta.

11. The crystalline form of claim 7 , wherein the crystalline form is a crystalline form of anhydrous nicotinamide-β-D-ribofuranoside hydrogen D-tartrate, wherein the crystalline form is characterized by a powder X-ray diffraction pattern having one or more peaks as provided in Table 9, ±0.2 degrees two theta.

12. The crystalline form of claim 11 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 12.9±0.2, 17.5±0.2 and 21.4±0.2 degrees two theta.

13. The crystalline form of claim 11 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 12.9±0.2, 16.4±0.2, 17.5±0.2, 21.4±0.2, 22.2±0.2, and 26.1±0.2 degrees two theta.

14. The crystalline form of claim 1 , wherein the crystalline form is a crystalline form of nicotinamide-β-D-ribofuranoside hydrogen DL-tartrate.

15. The crystalline form of claim 14 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having one or more peaks as provided in Table 6, ±0.2 degrees two theta.

16. The crystalline form of claim 14 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 17.0±0.2, 22.8±0.2 and 24.5±0.2 degrees two theta.

17. The crystalline form of claim 14 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 12.6±0.2, 21.6±0.2 and 27.8±0.2 degrees two theta.

18. The crystalline form of claim 14 , wherein the crystalline form is characterized by a powder X-ray diffraction pattern having the following peaks 12.6=0.2, 17.0±0.2, 21.6±0.2, 22.8±0.2, 24.5±0.2, and 27.8±0.2 degrees two theta.

19. A nutritional supplement comprising a crystalline form of claim 1 .

20. A pharmaceutical composition comprising a crystalline form of claim 1 .

21. A crystalline nicotinamide-β-D-ribofuranoside salt or crystalline nicotinamide-2,3,5-O-triacetyl-β-D-ribofuranoside salt selected from the group consisting of:

(a) crystalline nicotinamide-β-D-ribofuranoside hydrogen D-tartrate monohydrate characterized by a powder X-ray diffraction pattern as defined in FIG. 4 ;

(b) crystalline nicotinamide-β-D-ribofuranoside hydrogen L-tartrate characterized by a powder X-ray diffraction pattern as defined in FIG. 5 ;

(c) crystalline nicotinamide-β-D-ribofuranoside hydrogen DL-tartrate characterized by a powder X-ray diffraction pattern as defined in FIG. 6 ;

(d) crystalline nicotinamide-2,3,5-O-triacetyl-β-D-ribofuranoside hydrogen L-tartrate characterized by a powder X-ray diffraction pattern as defined in FIG. 7 ;

(e) crystalline nicotinamide-2,3,5-O-triacetyl-β-D-ribofuranoside hydrogen D-tartrate characterized by a powder X-ray diffraction pattern as defined in FIG. 8 ; and

(f) crystalline anhydrous nicotinamide-β-D-ribofuranoside hydrogen D-tartrate characterized by a powder X-ray diffraction pattern as defined in FIG. 9 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 24, 2025
From: SCHABERT, GUNTER; SPITZ, URS; SOYDEMIR, AYSEL; ZIMMERMANN, IRIS
To: BIOSYNTH AG
Reel/Frame 071034/0386 →
Priority Claims (2)
EP 19187314 · Jul 19, 2019 · regional
EP 19206542 · Oct 31, 2019 · regional
Continuity (3)
Continuation 17576699 · Jan 14, 2022
Continuation PCTEP2020070451 · Jul 20, 2020
Related Publication 20250092079A1 · Mar 20, 2025
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