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1.发明公开SUBSTITUTED $g(g)-PHENYL-$g(D)-LACTONES AND ANALOGS THEREOF AND USES RELATED THERETO 有权取代GAMMA苯基-δ-内酯及其模拟和用途
公开(公告)号：EP1112262A1
公开(公告)日：2001-07-04
申请号：EP99941351.1
申请日：1999-09-09
发明人： SHEN, Yaping , BURGOYNE, David, L. , LAUENER, Ronald, W. , ZHOU, Yuanlin , REBSTEIN, Patrick, J. , ABRAHAM, Samuel, D., M.
IPC分类号： C07D309/30 , C07F5/02 , C07D405/10 , C07F9/40 , C07D211/76 , A61K31/35
CPC分类号： C07F5/025 , A61K31/366 , C07D211/76 , C07D309/30 , C07F9/6552
摘要： η-Phenyl-substituted Δ-lactones and analogs thereof, including lactams, are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.
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2.发明授权SUBSTITUTED GAMMA-PHENYL-DELTA-LACTONES AND ANALOGS THEREOF AND USES RELATED THERETO 有权取代GAMMA苯基-δ-内酯及其模拟和用途
公开(公告)号：EP1112262B1
公开(公告)日：2004-08-04
申请号：EP99941351.1
申请日：1999-09-09
发明人： SHEN, Yaping , BURGOYNE, David, L. , LAUENER, Ronald, W. , ZHOU, Yuanlin , REBSTEIN, Patrick, J. , ABRAHAM, Samuel, D., M.
IPC分类号： C07D309/30 , C07F5/02 , C07D405/10 , C07F9/40 , C07D211/76 , A61K31/35
CPC分类号： C07F5/025 , A61K31/366 , C07D211/76 , C07D309/30 , C07F9/6552
摘要： η-Phenyl-substituted Δ-lactones and analogs thereof, including lactams, are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.
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公开(公告)号：EP1615866A1
公开(公告)日：2006-01-18
申请号：EP04727484.0
申请日：2004-04-15
发明人： RAYMOND, Jeffery, R. , HAN, Kang , ZHOU, Yuanlin , HE, Yuehua , NOREN, Bradley , YEE, James, Gee, Ken
IPC分类号： C07C35/21 , C07C35/32 , C07C35/52 , C07C69/03 , C07C215/42 , C07C233/18 , C07C279/08 , C07C311/04 , C07D213/30 , C07D233/56 , A61K31/047 , A61K31/133 , A61K31/155 , A61K31/164 , A61K31/18
CPC分类号： C07C35/32 , C07C35/14 , C07C35/21 , C07C51/083 , C07C51/347 , C07C62/34 , C07C69/013 , C07C213/00 , C07C213/08 , C07C215/42 , C07C233/18 , C07C233/21 , C07C233/72 , C07C247/14 , C07C279/08 , C07C311/04 , C07C315/00 , C07C2601/14 , C07C2602/08 , C07C2602/24 , C07D207/335 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/74 , C07D233/54 , C07D233/64 , C07D295/096 , C07D307/66 , C07D317/66 , C07D317/70 , Y10S514/825 , Y10S514/826 , Y10S514/863
摘要： Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
摘要翻译： 式（Ia）化合物：其中R1，R2，R3，R4a，R4b，R5和R6如本文所定义，以及其它茚衍生物在本文中公开。 还公开了含有化合物的药物组合物和使用该化合物的方法。
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4.发明公开PROCESS FOR THE PRODUCTION OF 6,7-DIHYDROXY STEROID COMPOUNDS BY ALLYLIC OXIDATION OF STEROID-5-ENE COMPOUNDS TO STEROID-5-ENE-7-ONE COMPOUNDS FOLLOWED BY HYDROBORATION AND OXIDATION AND INTERMEDIATES OF THIS PROCESS 审中-公开用于生产6,7-二羟基类固醇化合物BY烯丙基氧化类固醇-5- EN链接，相关类固醇5-CN-7-ON连接和HYDRO BORA TION氧化等的中间产品的PROCEDURE
公开(公告)号：EP1404700A2
公开(公告)日：2004-04-07
申请号：EP02727121.2
申请日：2002-05-22
发明人： BURGOYNE, David, L. , SHEN, Yaping , JI, Gueijun , ZHOU, Yuanlin , RAMACHANDRAN, Kishore , PASCHALIDES, Nicholas, D. , KELLEHER, Eugene, W.
IPC分类号： C07J21/00
CPC分类号： C07J53/00 , C07J1/0011 , C07J21/008 , C07J41/0038 , Y02P20/55
摘要： Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding α, β-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the α, β-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.
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5.发明公开
公开(公告)号：EP1551805A1
公开(公告)日：2005-07-13
申请号：EP03753187.8
申请日：2003-09-30
发明人： SHEN, Yaping , BURGOYNE, David, L. , LAUENER, Ronald, W. , ZHOU, Yuanlin , REBSTEIN, Patrick , ABRAHAM, Samuel, D., M.
IPC分类号： C07D211/76 , C07D405/06 , A61K31/45 , A61K31/4525 , A61P29/00
CPC分类号： A61K31/366 , A61K31/45 , A61K31/4525 , C07D211/76 , C07D309/30 , C07F5/025 , C07F9/6552
摘要： Ϝ-Phenyl-substituted Δ-lactams are disclosed. They may be formulated into pharmaceutical compositions, and/or used in the treatment or prevention of inflammation or other conditions or disease states.
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公开(公告)号：EP1265861A2
公开(公告)日：2002-12-18
申请号：EP01914888.1
申请日：2001-03-16
发明人： LAUENER, Ronald, W. , BURGOYNE, David, L. , REBSTEIN, Patrick, J. , MACKENZIE, Lloyd, F. , ZHOU, Yuanlin , SHEN, Yaping
IPC分类号： C07D207/26 , C07D233/32 , C07D239/10 , C07D473/04 , C07D473/06 , C07D213/75 , C07C271/60 , C07C255/46 , A61K31/4015 , A61K31/4166 , A61K31/513 , A61K31/52 , A61K31/44 , A61K31/325 , A61K31/277
CPC分类号： C07D207/26 , C07C255/46 , C07C271/60 , C07D213/75 , C07D233/32 , C07D239/10 , C07D473/04 , C07D473/06
摘要： The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g. benzyl bromide or a derivative thereof.
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