IP Library Granted Patent US 9,682,054
Granted Patent B2
US 9,682,054 · App. 10/544,350 · Granted Jun 20, 2017

Medium-chain length fatty acids, glycerides and analogues as stimulators of erythropoiesis

Inventors: Christopher Penney (Quebec, CA); Lyne Gagnon (Quebec, CA); Pierre Laurin (Quebec, CA); Boulos Zacharie (Quebec, CA)
Assignee: PROMETIC PHARMA SMT LIMITED
A61K31/20A61K31/23A61K45/06A61K47/14
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Quick Facts
Patent No.
US 9,682,054
App. No.
10/544,350
Granted
Jun 20, 2017
Kind
B2
Abstract

Use of a composition comprising a compound of any of formulae I, II, Ila, III and Illa; or a combination thereof wherein each R 1 is independently C 7-11 alkyl; A and B are independently H or CO—R 1 ; R 2 is H or C 1-4 alkyl; M is a metal monocation (k=1) or dication (k=2); Y is 0 or NH; and Z is 0, NH, CH 2 O or a bond; for the manufacture of a medicament for stimulating erythropoiesis. Preferably, the composition further comprises human erythroporietin.

Claims (60)

1. A method for stimulating erythropoiesis wherein said method comprises administering, to a subject who is anemic, a composition comprising a compound of any of formulae I, II, and IIa, or a combination thereof;

R 1 —CO—OR 2   II

(R 1 —CO—O) k M  IIa

wherein each R 1 is independently C 7-11 alkyl;

A and B are independently H or CO—R 1 ;

R 2 is H or C 1-4 alkyl;

M is a metal monocation (k=1) or (k=2); and

Y is O;

wherein the administration of said composition is done by a route selected from sublingual, pulmonary, intramuscular, intradermal, subcutaneous and intravenous; wherein each dose of said composition that is administered comprises about 1 gram to about 10 grams of said compound(s); and wherein the administration of said compound(s) causes stimulation of erythropoiesis.

2. The method according to claim 1 , wherein the composition comprises a compound of formula II, wherein R 2 is hydrogen and which is a medium-chain fatty acid.

3. The method according to claim 1 , wherein the composition comprises a compound of formula IIa, and wherein M is a metallic counterion selected from the group consisting of calcium, magnesium, potassium, and sodium.

4. The method according to claim 1 , wherein the composition comprises caprylic acid or capric acid.

5. The method according to claim 1 , wherein the composition comprises sodium caprylate or sodium caprate.

6. The method according to claim 1 , wherein the composition comprises calcium caprylate or calcium caprate.

7. A method for stimulating erythropoiesis wherein said method comprises administering, to a subject who is anemic, a composition comprising a compound of any of formulae I, II, and IIa, or a combination thereof;

R 1 —CO—OR 2   II

(R 1 —CO—O) k M  IIa

wherein each R 1 is independently C 7-11 alkyl;

A and B are independently H or CO—R 1 ;

R 2 is H or C 1-4 alkyl;

M is a metal monocation (k=1) or (k=2); and

Y is O;

wherein the administration of said composition is done orally, and said oral administration is not accompanied with erythropoietin; wherein each dose of said composition that is administered comprises about 1 gram to about 10 grams of said compound(s); and wherein the administration of said compound(s) causes stimulation of erythropoiesis.

8. The method according to claim 7 , wherein the subject is receiving chemotherapy.

9. The method according to claim 7 , wherein the subject is receiving radiotherapy.

10. The method according to claim 7 , wherein the subject has chronic anemia.

11. The method according to claim 7 , wherein the subject has transient anemia.

12. The method according to claim 7 , wherein the subject has chronic renal failure.

13. The method according to claim 7 , wherein the subject has anemia arising from end-stage renal disease.

14. The method according to claim 1 , wherein the subject is receiving chemotherapy.

15. The method according to claim 1 , wherein the subject is receiving radiotherapy.

16. The method according to claim 1 , wherein the subject has chronic anemia.

17. The method according to claim 1 , wherein the subject is a human.

18. The method according to claim 7 , wherein the subject is a human.

19. A method for stimulating erythropoiesis wherein said method comprises administering, to a subject who is anemic, a composition comprising a compound of any of formulae I, II, and IIa, or a combination thereof;

R 1 —CO—OR 2   II

(R 1 —CO—O) k M  IIa

wherein each R 1 is independently C 7-11 alkyl;

A and B are independently H or CO—R 1 ;

R 2 is H or C 1-4 alkyl;

M is a metal monocation (k=1) or (k=2); and

Y is O,

wherein the administration of said composition is done orally, and said oral administration is not accompanied with erythropoietin; wherein the anemic condition of the subject does not result from iron-deficiency; and wherein the administration of said compound(s) causes stimulation of erythropoiesis.

20. The method according to claim 19 , wherein the subject is receiving chemotherapy.

21. The method according to claim 19 , wherein the subject is receiving radiotherapy.

22. The method according to claim 19 , wherein the subject has chronic anemia.

23. The method according to claim 19 , wherein the subject has transient anemia.

24. The method according to claim 19 , wherein the subject has chronic renal failure.

25. The method according to claim 19 , wherein the subject has anemia arising from end-stage renal disease.

26. The method according to claim 19 , wherein the subject is a human.

27. The method according to claim 7 , wherein the composition comprises a compound of formula II, wherein R 2 is hydrogen and which is a medium-chain fatty acid.

28. The method according to claim 7 , wherein the composition comprises a compound of formula IIa, and wherein M is a metallic counterion selected from the group consisting of calcium, magnesium, potassium, and sodium.

29. The method according to claim 7 , wherein the composition comprises caprylic acid or capric acid.

30. The method according to claim 7 , wherein the composition comprises sodium caprylate or sodium caprate.

31. The method according to claim 7 , wherein the composition comprises calcium caprylate or calcium caprate.

32. The method according to claim 19 , wherein the composition comprises a compound of formula II, wherein R 2 is hydrogen and which is a medium-chain fatty acid.

33. The method according to claim 19 , wherein the composition comprises a compound of formula IIa, and wherein M is a metallic counterion selected from the group consisting of calcium, magnesium, potassium, and sodium.

34. The method according to claim 19 , wherein the composition comprises caprylic acid or capric acid.

35. The method according to claim 19 , wherein the composition comprises sodium caprylate or sodium caprate.

36. The method according to claim 19 , wherein the composition comprises calcium caprylate or calcium caprate.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 28, 2016
From: PROMETIC BIOSCIENCES INC.
To: PROMETIC PHARMA SMT LIMITED
Reel/Frame 038114/0510 →
RELEASE OF SECURITY INTEREST Recorded Jul 18, 2013
From: VENTURE LENDING & LEASING IV, INC.
To: PROMETIC BIOSCIENCES INC.
Reel/Frame 030828/0109 →
SECURITY AGREEMENT Recorded May 15, 2007
From: PROMETIC BIOSCIENCES INC.
To: VENTURE LENDING & LEASING IV, INC.
Reel/Frame 019324/0585 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 16, 2005
From: PENNEY, CHRISTOPHER; GAGNON, LYNE; LAURIN, PIERRE; ZACHARIE, BOULOS
To: PROMETIC BIOSCIENCES INC.
Reel/Frame 016788/0600 →
Continuity (2)
Provisional Application 60445454 · Feb 7, 2003
Related Publication 20060128800A1 · Jun 15, 2006