C13-substituted estra-1,3,5,(10)-trien-3-yl sulfamates, methods of preparing same, and pharmaceutical compositions containing these compounds

US6583130B1 · kind B1 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Sigfrid Schwarz · Jena, DE
• Gerd Muller · Jena, DE
• Dirk Kosemund · Berlin, DE
• Margit Richter · Jena, DE
• Olaf Peters · Bad Tabarz, DE
• Ina Scherlitz-Hofmann · Falkensee, DE
• Thomas Michel · Leipzig, DE
• Walter Elger · Berlin, DE
• Gudrun Reddersen · Jena, DE
• Birgitt Schneider · Jena, DE

Key dates

• Filing date: Sep 6, 2000
• Grant date: Jun 24, 2003
• Expiry date: Sep 6, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J1/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to new C13-substituted estra-1,3,5(10)-trien-3-yl sulfamates of general formula I, wherein R1 represents an acyl residue, oxycarbonyl residue, aminocarbonyl residue, sulfonyl residue, or aminosulfonyl residue, and R15 represents ethyl, methods of preparing same, and pharmaceutical compositions containing these compounds.The compounds of the invention of general formula I inhibit the activity of steroid sulfatase (EC 3.1.6.2) and do not exhibit any estrogenic effect.