Process of making isomers of norelgestromin and methods using the same

US7576226B2 · kind B2 · utility

Assignee

• Richter Gedeon Vegyeszeti Gyar RT · HU

Inventors

• Zoltan Tuba · Budapest, HU
• Sándor Mahó · Budapest, HU
• Gyorgy Keseru · Budapest, HU
• József Kozma · Budapest, HU
• Janos Horvath · Bad Blankenburg, DE
• Gabor Balogh · Debrecen, HU

Key dates

• Filing date: Jun 30, 2004
• Grant date: Aug 18, 2009
• Expiry date: Dec 12, 2026

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P15/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention is directed to a process of preparing substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3E- and -3Z-oxime isomers, as well as a process for the synthesis of the mixture of isomers and the pure isomers. The invention also relates to substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime and substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer. Further aspects of the invention include a composition comprising substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime or substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer, and methods of treatment using said compositions.