Prodrug acid esters of [2-(4-benzyl-3-hydroxy-piperidin-1-yl)-ethansulfonyl]phenol

US6407235B1 · kind B1 · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Alexander Alanine · Basel, CH
• Bernd Buettelmann · Palo Alto, US
• Holger Fischer · Karlsruhe, DE
• Marie-Paule Heitz Neidhart · Rixheim, FR
• Joerg Huwyler · Bürg, CH
• Georg Jaeschke · Basel, CH
• Emmanuel Pinard · Rixheim, FR
• Rene Wyler · Zürich, CH

Key dates

• Filing date: Aug 16, 2001
• Grant date: Jun 18, 2002
• Expiry date: Aug 16, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/59
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention is a compound of the formula whereinR isa) —C(O)(CH2)nC(O)OH,b)  wherein R1 is —N(R2)(R3), or is a five or six member aromatic or non-aromatic heterocyclic ring having one or more heteroatoms selected from nitrogen, oxygen or sulfur, unsubstituted or substituted by lower alkyl,c) —P(O)(OH)2, or isd) —C(O)(CH2)nNHC(O)(CH2)nN(R2)(R3); andR2/R3 are hydrogen or lower alkyl;n is 1, 2, 3 or 4;or a pharmaceutically acceptable acid addition salt thereof