Siga Technologies Inc.

Shanthakumar R Tyavanagimatt

Dennis E Hruby

William C Weimers

Melialani A C L S Anderson

N K Peter Samuel

Michael H O'Neill

Dylan Nelson

Gary Sweetapple

Kelley A McCloughan

Ying Tan

Tove′ C Bolken

Gopi Krishna Kasi

Tove C Bolken

Joseph Paz

N K Samuel

Matthew Reeves

Kris Holt

Melialani Acls Anderson

Melialani A C L Stone

Tove' C Bolken

Steven Priebe

Peter N K Samuel

Kelley A Mccloughan

Michael H O'neill

Melialani Acl Stone

Peter NK Samuel

Melialani ACL Stone

Michael H O'NEILL

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindo1-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

Polymorphic forms of ST-246 and methods of preparation

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

The present invention is directed to a dry suspension for reconstitution containing Tecovirimat (ST-246) powder and simethicone. The dry suspension is dispersed in water to provide an aqueous pharmaceutical suspension formulation for oral administration for treating orthopoxvirus infections and/or eczema vaccinatum. The suspension formulation exhibits excellent stability and good dissolution and has an improved taste and texture.

ST-246 (tecovirimat monohydrate) suspension formulations

The present invention provides for a novel liquid formulation for solubilizing poorly soluble ST-246 in cyclodextrins and a novel process of making the formulation.

ST-246 liquid formulations and methods

Disclosed are methods for hydration of ST-246 particles comprising exposing said particles to moisture by conveying volumes of air containing moisture.

Rehydration of micronized tecovirimat monohydrate

Rehydration of micronized tecovirmimat monohydrate

Disclosed are methods for the preparation of amorphous N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Also disclosed are methods for the preparation of amorphous solid dispersion of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide.

Amorphous Tecovirimat preparation

Disclosed are methods for the preparation of amorphous N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindo1-2(1H)-yl]-4-(trifluoromethyl)-benzamide for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Also disclosed are methods for the preparation of amorphous solid dispersion of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindo1-2(1H)-yl]-4-(trifluoromethyl)-benzamide.

Amorphous tecovirimat preparation

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Corvallis, OR, United States of America

Shanthakumar R Tyavanagimatt