IP Library Granted Patent US 10,029,956
Granted Patent B2
US 10,029,956 · App. 12/922,449 · Granted Jul 24, 2018

Therapies for cancer using isotopically substituted lysine

Inventor: Mikhail S. Shchepinov (Kingston upon Thames, GB)
Assignee: Retrotope, Inc.
C07B59/001A61K31/195C07C229/26C07B2200/05
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Quick Facts
Patent No.
US 10,029,956
App. No.
12/922,449
Granted
Jul 24, 2018
Kind
B2
Abstract

Methods of treatment and substances for treatment of cancer may use or cause the creation of isotopically modified lysine at levels that do not occur naturally.

Claims (30)

1. A method, comprising:

selecting a human patient in need of treatment for a condition associated with degradation of lysine-containing moieties, wherein the condition is breast cancer or fibrosis;

repeatedly delivering to the patient an effective lysine-oxidation-inhibiting material consisting essentially of a compound

of Formula (I), Formula (II), or Formula (III);

wherein D is deuterium;

wherein a carbon in Formula (I), (II), or (III) is optionally carbon-13; and

wherein the carbon-13, deuterium or both are enriched at least 20% more individually or collectively in comparison to naturally occurring carbon-13, deuterium or both at the same positions in the compound; and

thereby treating the condition by affecting an alteration of the isotopic composition of lysine-containing moieties in the body of the patient to effectively reduce the extent of degradation of lysine-containing moieties in vivo in the patient.

2. The method of claim 1 , wherein the method reduces oxidation of the delivered compound of formula I, II, or III, or the lysine-containing moieties, by a lysyl oxidase.

3. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is administered to the patient as a foodstuff or supplement.

4. The method of claim 2 , wherein the lysine-oxidation-inhibiting material reduces tumor growth in the patient.

5. The method of claim 2 , wherein the lysine-oxidation-inhibiting material reduces angiogenesis in the patient.

6. The method of claim 2 , wherein reducing degradation of lysine containing moieties via non-naturally occurring levels of heavy isotope reduces fibrosis in the patient.

7. The method of claim 4 , wherein said tumor is a primary tumor or a metastatic tumor.

8. The method of claim 7 , wherein metastatic tumor burden of the patient is stabilized.

9. The method of claim 1 , wherein the fibrosis is a liver fibrosis, a lung fibrosis, a kidney fibrosis, a cardiac fibrosis or schleroderma.

10. The method of claim 9 , wherein said kidney fibrosis is diabetic nephropathy, glomerulosclerosis, diabetic nephropathy, vesicoureteral reflux, tubulointerstitial renal fibrosis or glomerulonephritis.

11. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is the compound of formula (I).

12. The method of claim 11 , wherein the lysine-oxidation-inhibiting material is the compound of formula (I) wherein both D 1 and D 2 are deuterium ( 2 H).

13. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is the compound of formula (II).

14. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is the compound of formula (III).

15. The method of claim 1 , wherein the activity of a LOX enzyme is reduced.

16. The method of claim 15 , wherein the activity of the LOX enzyme is not completely blocked.

17. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is administered to the patient as part of the patient's diet.

18. The method of claim 17 , wherein the oxidation of collagen or an elastin is reduced.

19. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is incorporated into the patient's body.

20. The method of claim 1 , wherein at least one carbon in the lysine-oxidation-inhibiting material is carbon-13.

21. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is stabilized against a chemical oxidation of a lysyl oxidase.

22. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is stabilized against an enzymatic oxidation of a lysyl oxidase.

23. The method of claim 1 , wherein the lysine-oxidation-inhibiting material is administered to the patient orally, intravenously, or topically.

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded Sep 9, 2022
From: RTMFP ENTERPRISES INC.
To: RETROTOPE, INC.
Reel/Frame 061403/0670 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 9, 2022
From: RETROTOPE, INC.
To: RTMFP ENTERPRISES INC.
Reel/Frame 061403/0835 →
CHANGE OF NAME Recorded Sep 9, 2022
From: RTMFP ENTERPRISES INC.
To: BIOJIVA LLC
Reel/Frame 061405/0819 →
SECURITY INTEREST Recorded Mar 30, 2022
From: RETROTOPE, INC.
To: RTMFP ENTERPRISES, INC.
Reel/Frame 059442/0414 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 22, 2011
From: SHCHEPINOV, MIKHAIL S.
To: RETROTOPE, INC.
Reel/Frame 025998/0682 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 9, 2010
From: SHCHEPINOV, MIKHAIL S.
To: RETROTOPE, INC.
Reel/Frame 025584/0611 →
Continuity (2)
Provisional Application 61036841 · Mar 14, 2008
Related Publication 20110082208A1 · Apr 7, 2011