公开(公告)号：EP1558559A1

公开(公告)日：2005-08-03

申请号：EP03797782.4

申请日：2003-09-18

Applicant: NicOx S.A.

Inventor： ANDERSSON, Johan ,  BELLI, Aldo ,  CANNATA, Vincenzo ,  HEDBERG, Martin ,  PALMGREN, Andreas ,  SCHULDEI, Sigrid ,  STRÖM, Marika ,  VILLA, Marco

IPC: C07C201/00 ,  C07C309/63 ,  A61K31/216 ,  A61P29/00 ,  C07C211/55

CPC classification number: C07C303/28 ,  A61K31/216 ,  C07C67/08 ,  C07C201/02 ,  C07C203/04 ,  C07C227/16 ,  C07C227/20 ,  C07C229/42 ,  C07C309/66 ,  C07C69/738

Abstract: The present invention relates to a new process for the preparation of NO-donating compounds using a sulfonated intermediate. The invention relates to new intermediates prepared therein suitable for large scale manufacturing of NO-donating compounds. The invention further relates to the use of the new intermediates for the manufacturing of pharmaceutically active NO-donating compounds.The invention further relates to a substantially crystalline form of NO-donating NSAIDs, especially 2-[2-(nitrooxy)ethoxy]ethyl {2-[(2,6-dichlorophenyl)amino]phenyl}acetate, the preparation thereof and to pharmaceutical formulations containing said crystalline form and to the use of said crystalline form in the preparation of a medicament.

Abstract translation: 本发明涉及使用磺化中间体制备NO供体化合物的新方法。 本发明涉及适用于大规模生产NO供体化合物的新中间体。 本发明进一步涉及该新中间体在制备药学活性NO供体化合物中的用途。本发明还涉及NO供体非甾体抗炎药的基本结晶形式，尤其是2- [2-（硝基氧基）乙氧基]乙基{ 2 - [（2,6-二氯苯基）氨基]苯基}乙酸乙酯，其制备方法和含有所述结晶形式的药物制剂以及所述结晶形式在制备药物中的用途。