公开(公告)号：US20110003863A1

公开(公告)日：2011-01-06

申请号：US12792387

申请日：2010-06-02

申请人： Sabine M. Pyles ,  Michael Cyr ,  Ramachandran Radhakrishnan

发明人： Sabine M. Pyles ,  Michael Cyr ,  Ramachandran Radhakrishnan

IPC分类号： A61K31/4418 ,  C07D213/64 ,  A61P11/00

CPC分类号： C07D213/64 ,  A61K31/4412

摘要： A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenzene is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.

摘要翻译： 公开了一种从具有小于约0.15重量％二溴苯的溴苯合成吡非尼酮的方法。 还公开了在不使用乙酸乙酯或正丁醇的情况下合成吡非尼酮的方法，以及具有受控含量的乙酸乙酯，正丁醇，二（5-甲基-2-吡啶酮）苯和具有特定保留时间的其它杂质的吡非尼酮。 还公开了包括所公开的吡非尼酮的配制剂型。

公开(公告)号：US08519140B2

公开(公告)日：2013-08-27

申请号：US13244786

申请日：2011-09-26

申请人： Ramachandran Radhakrishnan ,  Michael Cyr ,  Sabine M. Pyles

发明人： Ramachandran Radhakrishnan ,  Michael Cyr ,  Sabine M. Pyles

IPC分类号： A61K31/44 ,  C07D211/72

CPC分类号： C07D213/64 ,  A61K31/4412

摘要： A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenze is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.

摘要翻译： 公开了一种从小于约0.15％（重量）二溴苯的溴苯合成吡非尼酮的方法。 还公开了在不使用乙酸乙酯或正丁醇的情况下合成吡非尼酮的方法，以及具有受控含量的乙酸乙酯，正丁醇，二（5-甲基-2-吡啶酮）苯和具有特定保留时间的其它杂质的吡非尼酮。 还公开了包括所公开的吡非尼酮的配制剂型。

公开(公告)号：US20120016133A1

公开(公告)日：2012-01-19

申请号：US13244786

申请日：2011-09-26

申请人： Sabine M. Pyles ,  Michael Cyr ,  Ramachandran Radhakrishnan

发明人： Sabine M. Pyles ,  Michael Cyr ,  Ramachandran Radhakrishnan

IPC分类号： C07D213/64

CPC分类号： C07D213/64 ,  A61K31/4412

摘要： A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenze is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.

摘要翻译： 公开了一种从小于约0.15％（重量）二溴苯的溴苯合成吡非尼酮的方法。 还公开了在不使用乙酸乙酯或正丁醇的情况下合成吡非尼酮的方法，以及具有受控含量的乙酸乙酯，正丁醇，二（5-甲基-2-吡啶酮）苯和具有特定保留时间的其它杂质的吡非尼酮。 还公开了包括所公开的吡非尼酮的配制剂型。