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1. 发明申请

WO2009005801A1 PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 1,2-SUBSTITUTED 3,4-DIOXO-1-CYCLOBUTENE COMPOUNDS 审中-公开
标题翻译：合成1,2-取代的3,4-二氧代-1-环己基化合物的方法和中间体
公开(公告)号：WO2009005801A1
公开(公告)日：2009-01-08
申请号：PCT/US2008/008187
申请日：2008-07-01
申请人： SCHERING CORPORATION , FU, Xiaoyong , GUENTER, Frank, Bruno , KIM-MEADE, Agnes, S. , MATTHEWS, Kenneth, Stanley , MAUST, Mathew, Thomas , MCALLISTER, Timothy, L. , WERNE, Gerald , WINTERS, Jason, L. , YIN, Jianguo , ZHANG, Shuyi
发明人： FU, Xiaoyong , GUENTER, Frank, Bruno , KIM-MEADE, Agnes, S. , MATTHEWS, Kenneth, Stanley , MAUST, Mathew, Thomas , MCALLISTER, Timothy, L. , WERNE, Gerald , WINTERS, Jason, L. , YIN, Jianguo , ZHANG, Shuyi
IPC分类号： C07C233/65 , C07D307/52
CPC分类号： C07D307/52 , C07C231/12 , C07C237/44
摘要： This application discloses a novel process for the preparation of 1.2 - substituted 3, 4 - dioxo - 1 - cyclobutene compounds of formula (A), which have utility, for example, in the treatment of CXC chemokine -mediated diseases, and intermediates useful in the synthesis thereof.
摘要翻译：本申请公开了一种制备式（A）的1.2-取代的3,4-二氧代-1-环丁烯化合物的新方法，其可用于例如治疗CXC趋化因子介导的疾病，以及可用于其合成。

2. 发明申请

WO2010028232A1 PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 8-[{1-(3,5-BIS-(TRIFLUOROMETHYL)PHENYL)-ETHOXY}-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE COMPOUNDS 审中-公开
标题翻译：合成8 - [{1-（3,5-双 - （三氟甲基）苯基） - 乙基} - 甲基] -8-苯基-1,7-二氮杂螺[4.5]癸-2-醇的方法和中间体一个化合物
公开(公告)号：WO2010028232A1
公开(公告)日：2010-03-11
申请号：PCT/US2009/056020
申请日：2009-09-04
申请人： SCHERING CORPORATION , WU, George, G. , WERNE, Gerald , FU, Xiaoyong , ORR, Robert, K. , CHEN, Frank, Xing , CUI, Jian , SPRAGUE, Victoria, M. , ZHANG, Fucheng , XIE, Ji , ZENG, Liansheng , CASTELLANOS, Louis, Peter , CHEN, Yuyin , POIRIER, Marc , MERGELSBERG, Ingrid
发明人： WU, George, G. , WERNE, Gerald , FU, Xiaoyong , ORR, Robert, K. , CHEN, Frank, Xing , CUI, Jian , SPRAGUE, Victoria, M. , ZHANG, Fucheng , XIE, Ji , ZENG, Liansheng , CASTELLANOS, Louis, Peter , CHEN, Yuyin , POIRIER, Marc , MERGELSBERG, Ingrid
IPC分类号： C07D207/26 , C07D471/10 , C07D498/04
CPC分类号： C07D471/10 , C07C217/46 , C07C217/48 , C07D207/26 , C07D207/267 , C07D207/28 , C07D498/04
摘要： This application discloses a novel process to synthesize 8-[{1-(3,5-Bis- (trifluoromethyl)phenyl)-ethoxy}-nnethyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes. IM=102123
摘要翻译：该申请公开了合成8 - [{1-（3,5-双 - （三氟甲基）苯基） - 乙氧基} - 乙基] -8-苯基-1,7-二氮杂 - 螺[4.5]癸烷-2 一种可用于例如可用于所述方法的药物制剂中间体中的NK-1抑制剂化合物的化合物，以及制备所述中间体的方法; 还公开了从N-杂环卡宾金属络合物中除去金属的方法。 IM = 102123

3. 发明申请

WO2006031788A2 PROCESS FOR PREPARING SUBSTITUTED 8-AZABICYCLO[3.2.1] OCTAN-3-OLS 审中-公开
标题翻译：制备替代的8-亚氨基半胱氨酸[3.2.1] OCT-3-OLS的方法
公开(公告)号：WO2006031788A2
公开(公告)日：2006-03-23
申请号：PCT/US2005/032512
申请日：2005-09-13
申请人： SCHERING-PLOUGH LTD. , MERGELSBERG, Ingrid , WERNE, Gerald
发明人： MERGELSBERG, Ingrid , WERNE, Gerald
CPC分类号： C07D451/06
摘要： The present invention relates to a process for preparing substituted 8-azabicyclo[3.2.1]octan-3-ols having the structural formula I (Chemical formula should be inserted here as it appears on abstract in paper form) I or a pharmaceutically acceptable salt or solvate thereof, wherein R is benzyl, R5 -benzyl, allyl, -C(O)R 6 , -C(O)OR 8 or -CH(R 7 )2; R 1 is optionally substituted aryl or optionally substituted heteroaryl; and R 5 , R 6 , R 7 and R 8 are as defined in the specification; comprising a) reacting an amine of formula II R-NH 2 II with 2,5-dimethoxytetrahydrofuran or HC(O)(CH 2 ) 2 C(O)H, and C(O)(CH 2 C(O)OR 4 ) 2 , wherein R 4 is H or alkyl, to obtain a compound of formula III (Chemical formula should be inserted here as it appears on abstract in paper form) III b) reacting a compound of formula III with I-R 1 , alkyl lithium, and optionally a lithium salt, to obtain a compound of formula I; and c) optionally converting a compound of formula I wherein R is benzyl, R 5 -benzyl, allyl, -C(O)R 6 or -C(O)OR 8 to a compound of formula I wherein R is -CH(R 7 ) 2 . Intermediates in the process are also claimed.
摘要翻译：本发明涉及一种制备具有结构式I的取代的8-氮杂双环[3.2.1]辛-3-醇的方法（化学式应该插在这里，如其以纸的形式出现）I或其药学上可接受的盐或其溶剂合物，其中R是苄基，

4. 发明公开

EP2178826A1 PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 1,2-SUBSTITUTED 3,4-DIOXO-1-CYCLOBUTENE COMPOUNDS 有权
标题翻译：处理和用于合成中间体的1,2-取代的3,4-二氧代-1- CYCLOBUTENVERBINDUNGEN
公开(公告)号：EP2178826A1
公开(公告)日：2010-04-28
申请号：EP08779918.5
申请日：2008-07-01
申请人： Schering Corporation
发明人： FU, Xiaoyong , GUENTER, Frank, Bruno , KIM-MEADE, Agnes, S. , MATTHEWS, Kenneth, Stanley , MAUST, Mathew, Thomas , MCALLISTER, Timothy, L. , WERNE, Gerald , WINTERS, Jason, L. , YIN, Jianguo , ZHANG, Shuyi
IPC分类号： C07C233/65 , C07D307/52
CPC分类号： C07D307/52 , C07C231/12 , C07C237/44
摘要： This application discloses a novel process for the preparation of 1.2 - substituted 3, 4 - dioxo - 1 - cyclobutene compounds of formula (A), which have utility, for example, in the treatment of CXC chemokine -mediated diseases, and intermediates useful in the synthesis thereof.

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