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1. 发明申请

WO2002069970A1 SUBSTITUTED 8-ARYLQUINOLINE PHOSPHODIESTERASE-4 INHIBITORS 审中-公开
标题翻译：取代8-ARYLQUINOLINE磷酸二酯酶-4抑制剂
公开(公告)号：WO2002069970A1
公开(公告)日：2002-09-12
申请号：PCT/US2001/048674
申请日：2001-12-14
申请人： MERCK & CO., INC. , MERCK FROSST CANADA & CO. , VAILAYA, Anant , CONLON, David, A. , HO, Guo-Jie , MACDONALD, Dwight , PERRIER, Helene , THIBERT, Roch , KWONG, Elizabeth , CLAS, Sophie-Dorothee
发明人： VAILAYA, Anant , CONLON, David, A. , HO, Guo-Jie , MACDONALD, Dwight , PERRIER, Helene , THIBERT, Roch , KWONG, Elizabeth , CLAS, Sophie-Dorothee
IPC分类号： A61K31/47
CPC分类号： C07D401/10 , C07D215/12 , C07D215/14 , C07D413/10 , C07D417/10
摘要： Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.
摘要翻译：其中8位的芳基含有取代的取代的链烯基的取代的8-芳基喹啉的新型硫酸，甲磺酸，对甲苯磺酸，2-萘磺酸，盐酸或苯磺酸盐是PDE4抑制剂。

2. 发明申请

WO2010060199A1 TRANSDERMALLY ADMINISTERED ALISKIREN 审中-公开
标题翻译：变态管理ALISKIREN
公开(公告)号：WO2010060199A1
公开(公告)日：2010-06-03
申请号：PCT/CA2009/001694
申请日：2009-11-23
申请人： MERCK FROSST CANADA LTD. , TOULMOND, Sylvie , KWONG, Elizabeth , MACDONALD, Dwight
发明人： TOULMOND, Sylvie , KWONG, Elizabeth , MACDONALD, Dwight
IPC分类号： A61K31/165 , A61P9/12
CPC分类号： A61K31/165 , A61K9/0014 , A61K9/7061 , A61K47/40
摘要： Dosage form of aliskiren, comprising a device for transdermal administration of aliskiren and aliskiren (including salts, prodrugs and metabolites thereof), optionally together with pharmaceutically acceptable carrier(s) to a human being or an animal in order to achieve a desired therapeutic effect. Use of a compound comprising aliskiren, optionally encompassing salts, prodrugs and metabolites thereof, and optionally together with pharmaceutically acceptable carrier(s), for the manufacture of a composition to be administered transdermally for achieving a desired therapeutic effect. Method for achieving a desired therapeutic effect by transdermal administration of a compound comprising aliskiren, optionally encompassing salts, prodrugs and metabolites thereof, and optionally together with pharmaceutically acceptable carrier(s).
摘要翻译：阿利吉仑的剂量形式，包括用于透皮给药阿利吉仑和阿利吉仑（包括其盐，前药和代谢物）的装置，任选地与药学上可接受的载体一起给予人或动物，以达到所需的治疗效果。使用包含阿利吉仑，任选地包括其盐，前药和代谢物，以及任选与药学上可接受的载体一起的化合物，用于制备经皮给药以获得期望的治疗效果的组合物。通过透皮施用包含阿利吉仑，任选地包括其盐，前药和代谢物以及任选地与药学上可接受的载体的化合物来实现期望的治疗效果的方法。

3. 发明授权

EP1363635B1 SUBSTITUTED 8-ARYLQUINOLINE PHOSPHODIESTERASE-4 INHIBITORS 有权
标题翻译：取代的8- ARYLCHINOLINE ALS磷酸二酯酶-4-缝边
公开(公告)号：EP1363635B1
公开(公告)日：2009-04-15
申请号：EP01273908.2
申请日：2001-12-14
申请人： Merck & Co., Inc. , Merck Frosst Canada & Co.
发明人： VAILAYA, Anant , CONLON, David, A. , HO, Guo-Jie , MACDONALD, Dwight , PERRIER, Helene , THIBERT, Roch , KWONG, Elizabeth , CLAS, Sophie-Dorothee
IPC分类号： A61K31/47 , C07D215/12 , C07D215/14 , C07D401/10 , C07D413/10 , C07D417/10 , A61P11/00
CPC分类号： C07D401/10 , C07D215/12 , C07D215/14 , C07D413/10 , C07D417/10
摘要： Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

4. 发明公开

EP1363635A1 SUBSTITUTED 8-ARYLQUINOLINE PHOSPHODIESTERASE-4 INHIBITORS 有权
标题翻译：取代的8- ARYLCHINOLINE ALS磷酸二酯酶-4-缝边
公开(公告)号：EP1363635A1
公开(公告)日：2003-11-26
申请号：EP01273908.2
申请日：2001-12-14
申请人： Merck & Co., Inc. , MERCK FROSST CANADA & CO.
发明人： VAILAYA, Anant , CONLON, David, A. , HO, Guo-Jie , MACDONALD, Dwight , PERRIER, Helene , THIBERT, Roch , KWONG, Elizabeth , CLAS, Sophie-Dorothee
IPC分类号： A61K31/47 , C07D215/12 , C07D215/14 , C07D401/10 , C07D413/10 , C07D417/10 , A61P11/00
CPC分类号： C07D401/10 , C07D215/12 , C07D215/14 , C07D413/10 , C07D417/10
摘要： Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

5. 发明申请

WO2013066735A1 NANO-SUSPENSION PROCESS 审中-公开
标题翻译：纳米悬浮过程
公开(公告)号：WO2013066735A1
公开(公告)日：2013-05-10
申请号：PCT/US2012/062026
申请日：2012-10-26
申请人： MERCK SHARP & DOHME CORP. , LEUNG, Dennis , NELSON, Todd, D. , RHODES, Timothy, A. , KWONG, Elizabeth
发明人： LEUNG, Dennis , NELSON, Todd, D. , RHODES, Timothy, A. , KWONG, Elizabeth
IPC分类号： A61K9/00
CPC分类号： B02C19/18 , A61K9/10 , A61K9/145 , A61K9/1688 , A61K31/192 , A61K47/10 , A61K47/26 , A61K47/32 , A61K47/38
摘要： Described herein is a process for preparing nano-suspensions, wherein the process comprises: providing an admixture of at least one active pharmaceutical compound, an aqueous dispersion medium, and milling media and applying thereto acoustic energy having a frequency of from about 10 hertz to 1000 hertz and which supplies a linear acceleration of from about 10 G's to about 100 G's (where "G" is the force of gravity) for a period sufficient to supply a nano-suspension having a D 50 of less than about 1 micron, preferably less than about 500 nm. Described also are nano-suspensions having novel properties prepared via the inventive process.
摘要翻译：本文描述的是制备纳米悬浮液的方法，其中所述方法包括：提供至少一种活性药物化合物，水性分散介质和研磨介质的混合物，并向其施加具有约10赫兹至1000的频率的声能并且其提供从约10G至约100G的线性加速度（其中“G”是重力））足以提供具有小于约1微米，优选小于约1微米的D50的纳米悬浮液约500nm。还描述了通过本发明方法制备的具有新特性的纳米悬浮液。

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