IP Library Granted Patent US 9,301,949
Granted Patent B2
US 9,301,949 · App. 13/203,351 · Granted Apr 5, 2016

Thienopyridine derivatives for the treatment and prevention of dengue virus infections

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Quick Facts
Patent No.
US 9,301,949
App. No.
13/203,351
Granted
Apr 5, 2016
Kind
B2
Abstract

Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.

Claims (15)

1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound selected from the group consisting of: 3-amino-6,7,8,9-tetrahydro-5H-1-thia-10-aza-cyclohepta[f]indene-2-carboxylic acid (5-phenyl-[1,3,4]thiadiazol-2-yl)-amide; 1-amino-5-methyl-6,7,8,9-tetrahydro-thieno[2,3-c]isoquinoline-2-carboxylic acid (4-methyl-thiazol-2-yl)-amide; 3,6-diamino-5-cyano-4-furan-2-yl-thieno[2,3-b]pyridine-2-carboxylic acid (4-bromo-phenyl)-amide; 3-amino-6-ethyl-5,6,7,8-tetrahydro-thieno[2,3-b][1,6]naphthyridine-2-carboxylic acid (4-trifluoromethyl-phenyl)-amide; 4-[(3-amino-6-isopropyl-5,6,7,8-tetrahydro-thieno[2,3-b][1,6]naphthyridine-2-carbonyl)-amino]-benzoic acid ethyl ester; 3-amino-6-methyl-5,6,7,8-tetrahydro-thieno[2,3-b][1,6]naphthyridine-2-carboxylic acid (4-trifluoromethoxy-phenyl)-amide and 3-amino-6-thiophen-2-yl-thieno[2,3-b]pyridine-2-carboxylic acid (3-trifluoromethyl-phenyl)-amide.

2. The composition of claim 1 , wherein the compound of Formula I is 3-amino-6,7,8,9-tetrahydro-5H-1-thia-10-aza-cyclohepta[f]indene-2-carboxylic acid (5-phenyl-[1,3,4]thiadiazol-2-yl)-amide.

3. A method for the treatment or of a Dengue virus, comprising administering in a therapeutically effective amount to a mammal in need thereof, a compound selected from the group consisting of: 3-amino-6,7,8,9-tetrahydro-5H-1-thia-10-aza-cyclohepta[f]indene-2-carboxylic acid (5-phenyl-[1,3,4]thiadiazol-2-yl)-amide; 1-amino-5-methyl-6,7,8,9-tetrahydro-thieno[2,3-c]isoquinoline-2-carboxylic acid (4-methyl-thiazol-2-yl)-amide; 3,6-diamino-5-cyano-4-furan-2-yl-thieno[2,3-b]pyridine-2-carboxylic acid (4-bromo-phenyl)-amide; 3-amino-6-ethyl-5,6,7,8-tetrahydro-thieno[2,3-b][1,6]naphthyridine-2-carboxylic acid (4-trifluoromethyl-phenyl)-amide; 4-[(3-amino-6-isopropyl-5,6,7,8-tetrahydro-thieno[2,3-b][1,6]naphthyridine-2-carbonyl)-amino]-benzoic acid ethyl ester; 3-amino-6-methyl-5,6,7,8-tetrahydro-thieno[2,3-b][1,6]naphthyridine-2-carboxylic acid (4-trifluoromethoxy-phenyl)-amide and 3-amino-6-thiophen-2-yl-thieno[2,3-b]pyridine-2-carboxylic acid (3-trifluoromethyl-phenyl)-amide or a pharmaceutically acceptable salt thereof.

4. The method of claim 3 , wherein the compound of Formula I is 3-amino-6,7,8,9-tetrahydro-5H-1-thia-10-aza-cyclohepta[f]indene-2-carboxylic acid (5-phenyl-[1,3,4]thiadiazol-2-yl)-amide.

5. The method of claim 3 , wherein the mammal is a human.

6. The method of claim 3 , wherein said Dengue virus is selected from the group consisting of DEN-I, DEN-2, DEN-3, and DEN-4.

7. The method of claim 3 , wherein said Dengue virus is associated with Dengue fever.

8. The method of claim 7 , wherein said Dengue fever is selected from the group consisting of classical dengue fever, dengue hemorrhagic fever syndrome, and dengue shock syndrome.

9. The method of claim 3 , which further comprises coadministration of at least one agent selected from the group consisting of antiviral agent, vaccine, and interferon.

10. The method of claim 9 , wherein said interferon is pegylated.

11. The pharmaceutical composition according to claim 1 , wherein said pharmaceutical composition is suitable for administration in a human or animal, wherein said administration is selected from the group consisting of: oral administration, rectal administration, parenteral administration, intravaginal administration, intraperitoneal administration and administration by inhalation.

12. The pharmaceutical composition of claim 1 , wherein said pharmaceutically acceptable carrier is selected form the group consisting of solvents, diluents, dispersion aids, suspension aids, surface active agents, isotonic agents, thickening agents, emulsifying agents, preservatives, solid binders and lubricants.

13. The pharmaceutical composition of claim 1 , wherein said pharmaceutically acceptable carrier is solid.

14. The pharmaceutical composition of claim 1 , wherein said pharmaceutically acceptable carrier is liquid.

15. The pharmaceutical composition of claim 11 , wherein said parenteral administration is selected from the group consisting of: intramuscular injection, subcutaneous injection and intravenous infusion.

Assignments (6)
RELEASE OF SECURITY INTEREST IN INTELLECTUAL PROPERTY AT REEL/FRAME NO. 40349/0219 Recorded Mar 13, 2020
From: CORTLAND CAPITAL MARKET SERVICES LLC
To: SIGA TECHNOLOGIES, INC.
Reel/Frame 052163/0014 →
SECURITY INTEREST Recorded Nov 16, 2016
From: SIGA TECHNOLOGIES, INC.
To: CORTLAND CAPITAL MARKET SERVICES, LLC
Reel/Frame 040349/0219 →
RELEASE OF SECURITY INTEREST Recorded Apr 2, 2015
From: GENERAL ELECTRIC CAPITAL CORPORATION, AS AGENT
To: SIGA TECHNOLOGIES, INC.
Reel/Frame 035319/0001 →
SECURITY AGREEMENT Recorded Dec 31, 2012
From: SIGA TECHNOLOGIES, INC.
To: GE CAPITAL EQUITY INVESTMENTS, INC. C/O GE HEALTHCARE FINANCIAL SERVICES, INC.
Reel/Frame 029557/0771 →
CONFIRMATORY LICENSE Recorded Dec 22, 2011
From: SIGA TECHNOLOGIES, INC.
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 027437/0878 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 13, 2011
From: BYRD, CHELSEA M.; DAI, DONGCHENG; JORDAN, ROBERT; HRUBY, DENNIS E.
To: SIGA TECHNOLOGIES, INC.
Reel/Frame 027057/0128 →