IP Library Granted Patent US 7,956,197
Granted Patent B2
US 7,956,197 · App. 12/752,462 · Granted Jun 7, 2011

Compounds, compositions and methods for treatment and prevention of orthopoxvirus infections and associated diseases

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Quick Facts
Patent No.
US 7,956,197
App. No.
12/752,462
Granted
Jun 7, 2011
Kind
B2
Abstract

Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.

Claims (17)

1. A method of making 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide, said method comprising:

a) reacting 4-trifloromethylbenzhydrazide with a compound of formula

 in a solvent to form a reaction product; and

b) collecting 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide.

2. The method of claim 1 , wherein the ratio of compound 1(a) to 4-trifloromethylbenzhydrazide is 0.89 to 1.

3. The method of claim 1 wherein the solvent is ethanol.

4. The method of claim 1 wherein the reaction occurs at above room temperature.

5. The method of claim 1 wherein the reaction occurs under argon.

6. The method of claim 1 wherein the solvent is removed by evaporation.

7. The method of claim 1 wherein 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide is further purified by chromatography.

8. A method of making 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide, said method comprising:

a) reacting cycloheptatriene and maleic anhydride in a first solvent to form compound 1(a);

b) collecting compound 1(a);

c) reacting 4-trifloromethylbenzhydrazide with said compound 1(a) in a second solvent to form 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide; and

d) collecting 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide.

9. The method of claim 8 , wherein said first solvent comprises xylenes.

10. The method of claim 8 , wherein said second solvent is ethanol.

Assignments (3)
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 →
CONFIRMATORY LICENSE Recorded Dec 12, 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 027365/0765 →