IP Library › Granted Patent US 10,112,933
Granted Patent B2
US 10,112,933 · App. 14/335,804 · Granted Oct 30, 2018

Methods and compositions for treatment of fibrosis

Inventors: David J. Tweardy (Houston, TX); Moses M. Kasembeli (Houston, TX); Marvin X. Xu (Shanghai, CN); Sandeep K. Agarwal (Houston, TX); Mesias Pedroza (Houston, TX)
Assignee: BAYLOR COLLEGE OF MEDICINE
C07D417/12A61K31/18A61K31/343A61K31/39A61K31/4196A61K45/06C07C317/28C07C317/30C07C317/32C07D213/71C07D215/06C07D231/18C07D239/60C07D261/10C07D333/34C07D409/12C07D413/12
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 10,112,933
App. No.
14/335,804
Granted
Oct 30, 2018
Kind
B2
Abstract

Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.

Claims (23)

1. A method of treating an individual that has fibrosis, comprising the step of providing to the individual an effective amount of one or more compositions selected from the group consisting of N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide, N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide, N-(3,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(4,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(5,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(6,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(7,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(8,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, 4-Bromo-N-(1,6′-dihydroxy-[2,2′]binaphthalenyl-4-yl)-benzenesulfonamide, 4-Bromo-N-[4-hydroxy-3-(1H-[1,2,4]triazol-3-ylsulfanyl)-naphthalen-1-yl]-benzenesulfonamide, and a functional derivative thereof, wherein the fibrosis is not pulmonary fibrosis or myelofibrosis.

2. The method of claim 1 , wherein the fibrosis is of the skin, heart, intestine, pancreas, joint, liver, or retroperionteum.

3. The method of claim 1 , wherein the individual is provided the composition in multiple doses.

4. The method of claim 3 , wherein the multiple doses are separated by hours, days, or weeks.

5. The method of claim 1 , wherein the individual is provided with an additional therapy for the fibrosis.

6. The method of claim 1 , wherein the composition is selected from the group consisting of N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide, N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide, N-(3,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(4,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(5,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(6,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(7,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(8,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, 4-Bromo-N-(1,6′-dihydroxy-[2,2′]binaphthalenyl-4-yl)-benzenesulfonamide, 4-Bromo-N-[4-hydroxy-3-(1H-[1,2,4]triazol-3-ylsulfanyl)-naphthalen-1-yl]-benzenesulfonamide, a functionally active derivative thereof, and a mixture thereof.

7. The method of claim 1 , wherein the composition inhibits Stat3, Stat1, or both.

8. The method of claim 1 , further comprising the step of diagnosing the fibrosis.

9. The method of claim 1 , wherein the composition is provided intravenously, intradermally, intraarterially, intraperitoneally, intralesionally, intracranially, intraarticularly, intraprostaticaly, intrapleurally, intratracheally, intranasally, intravitreally, intravaginally, intrarectally, topically, intratumorally, intramuscularly, intraperitoneally, subcutaneously, subconjunctival, intravesicularlly, mucosally, intrapericardially, intraumbilically, intraocularally, orally, topically, locally, injection, infusion, continuous infusion, localized perfusion, via a catheter, via a lavage, in lipid compositions, in liposome compositions, or as an aerosol.

10. The method of claim 1 , wherein the composition is provided by injection.

11. The method of claim 1 , wherein the composition is provided topically.

12. The method of claim 1 , wherein the composition is provided subcutaneously.

13. The method of claim 1 , wherein the composition is provided systemically.

14. The method of claim 1 , wherein the composition is provided locally.

15. The method of claim 1 , wherein the individual does not have cancer.

16. The method of claim 1 , wherein the individual is not suspected of having cancer.

17. The method of claim 1 , wherein the fibrosis is scleroderma.

18. The method of claim 1 , wherein the composition comprises N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide.

19. A method of treating an individual, comprising the step of providing to the individual an effective amount of one or more compositions selected from the group consisting of N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide, N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide, N-(3,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(4,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(5,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(6,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(7,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(8,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, 4-Bromo-N-(1,6′-dihydroxy-[2,2′]binaphthalenyl-4-yl)-benzenesulfonamide, 4-Bromo-N-[4-hydroxy-3-(1H-[1,2,4]triazol-3-ylsulfanyl)-naphthalen-1-yl]-benzenesulfonamide, and a functional derivative thereof, wherein the fibrosis is not pulmonary fibrosis or myelofibrosis, and wherein the fibrosis is of the heart, pancreas, joint, liver, or retroperionteum.

20. The method of claim 19 , wherein the composition is selected from the group consisting of N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide, N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide, N-(3,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(4,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(5,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(6,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(7,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, N-(8,1′-Dihydroxy-[1,2′]binaphthalenyl-4′-yl)-4-methoxy-benzenesulfonamide, 4-Bromo-N-(1,6′-dihydroxy-[2,2′]binaphthalenyl-4-yl)-benzenesulfonamide, 4-Bromo-N-[4-hydroxy-3-(1H-[1,2,4]triazol-3-ylsulfanyl)-naphthalen-1-yl]-benzenesulfonamide, a functionally active derivative thereof, and a mixture thereof.

21. The method of claim 19 , wherein the composition is provided intravenously, intradermally, intraarterially, intraperitoneally, intralesionally, intracranially, intraarticularly, intraprostaticaly, intrapleurally, intratracheally, intranasally, intravitreally, intravaginally, intrarectally, topically, intratumorally, intramuscularly, intraperitoneally, subcutaneously, subconjunctival, intravesicularlly, mucosally, intrapericardially, intraumbilically, intraocularally, orally, topically, locally, injection, infusion, continuous infusion, localized perfusion, via a catheter, via a lavage, in lipid compositions, in liposome compositions, or as an aerosol.

22. The method of claim 19 , wherein the fibrosis is scleroderma.

23. The method of claim 19 , wherein the composition comprises N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 28, 2016
From: TWEARDY, DAVID J.; KASEMBELI, MOSES M.; XU, MARVIN X.; AGARWAL, SANDEEP K.; PEDROZA, MESIAS
To: BAYLOR COLLEGE OF MEDICINE
Reel/Frame 039280/0324 →
Continuity (2)
Provisional Application 61847744 · Jul 18, 2013
Related Publication 20150051233A1 · Feb 19, 2015
Cited By (6)
US 12,365,729 US 12,497,452 US 12,617,810 US 12,655,210 US 12,715,916 US 12,715,917