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1.发明授权PROCESS FOR PREPARING TRIAZOLE SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES AND NOVEL SALT FORMS PRODUCED THEREIN 有权制备三唑取代的阿拉伯糖氧基哌嗪衍生物和其中产生的新盐形式的方法
公开(公告)号：EP1907389B1
公开(公告)日：2011-07-27
申请号：EP06785355.6
申请日：2006-06-21
发明人： SOUNDARARAJAN, Nachimuthu , QIU, Yuping , HU, Wenhao , KRONENTHAL, David, R. , SIRARD, Pierre , LAJEUNESSE, Jean , DROGHINI, Roberto , CHIDAMBARAM, Ramakrishnan , QIAN, Xinhua , NATALIE, JR., Kenneth, J. , PACK, Shawn, K. , REISING, Nathan , TANG, Erqing , FAKES, Michael, G. , GAO, Qi , QIAN, Feng , VAKKALAGADDA, Blisse, J. , LAI, Chiajen , KUANG, Shan-Ming
IPC分类号： C07D471/04 , A61K31/4745 , A61P31/12
CPC分类号： C07D471/04 , C07C311/49 , C07D213/26
摘要： A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and processes for producing such novel forms are also provided.
摘要翻译： 提供了制备三唑取代的氮杂吲哚氧乙酸哌嗪衍生物的方法。 还提供了在上述方法中制备的新型中间体，以及1,2,3-三唑取代的氮杂吲哚氧乙酸哌嗪衍生物的新型N-1和无定形形式以及制备这种新型形式的方法。
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公开(公告)号：EP1487450A1
公开(公告)日：2004-12-22
申请号：EP03721447.5
申请日：2003-03-25
IPC分类号： A61K31/496 , C07D487/04
CPC分类号： C07D471/04
摘要： Provided are processes and synthetic intermediates useful for the preparation of azaindole piperazine diamide derivatives of the formula [Insert chemical formula here] These azaindole piperazine diamide derivatives, among other things, are useful as therapeutic agents for the treatment of HIV and AIDS.
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3.发明公开PREPARATION OF (S)-2-AMINO-6,6-DIMETHOXYHEXANOIC ACID METHYL ESTER VIA NOVEL DIOXOLANES 审中-公开（S）-2-氨基-6,6-二甲氧基己酸甲酯通过新型二氧化硅的制备
公开(公告)号：EP1121351A2
公开(公告)日：2001-08-08
申请号：EP99932163.1
申请日：1999-07-01
发明人： GODFREY, Jollie, D., Jr. , KRONENTHAL, David, R. , SCHWINDEN, Mark, D. , SRIVASTAVA, Sushil, K. , RAMIG, Keith , VENIT, John, J. , JASS, Paul, A. , RACHA, Saibaba , DILLON, John, L., Jr. , SOUNDARARAJAN, Nachimuthu , POWERS, Gerald, L. , KOTNIS, Atul, S.
IPC分类号： C07D317/26 , C07D317/28
CPC分类号： C07C229/22 , C07D317/30
摘要： The invention relates to the synthesis of 2-amino-6, 6-dimethoxy hexanoic acid, methyl ester and novel dioxalane intermediates thereof, from the reaction of glycinamide of formula I with dioxolane of formula II.
摘要翻译： 本发明涉及由式I的甘氨酰胺与式II的二氧戊环反应合成2-氨基-6,6-二甲氧基己酸，甲酯和其新二氧杂环戊烷中间体。
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4.发明授权PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS 有权PRODRUGS VON ANTIVIRALEN MITTELN AUF BASIS VON PIPERAZIN UND SUBSTITUIERTEM PIPERIDIN
公开(公告)号：EP1725569B1
公开(公告)日：2008-01-23
申请号：EP05724510.2
申请日：2005-03-03
发明人： UEDA, Yasutsugu , CONNOLLY, Timothy, P. , KADOW, John, F. , MEANWELL, Nicholas, A. , WANG, Tao , CHEN, Chung-Pin, H. , YEUNG, Kap-Sun , ZHANG, Zhongxing , LEAHY, David Kenneth , PACK, Shawn, K. , SOUNDARARAJAN, Nachimuthu , SIRARD, Pierre , LEVESQUE, Kathia , THORAVAL, Dominique
IPC分类号： C07F9/09 , C07D471/04 , A61K31/437 , A61P31/18
CPC分类号： A61K31/675 , A61K31/497 , A61K45/06 , C07D471/04 , C07F9/062 , C07F9/5728 , C07F9/65515 , C07F9/65586 , C07F9/6561
摘要： This invention provides for prodrug Compounds (I), pharmaceutical compositions thereof, and their use in treating HIV infection. Also, this invention provides for intermediate Compounds (II) useful in making prodrug Compounds (I).
摘要翻译： 本发明提供前药化合物I，其药物组合物及其在治疗HIV感染中的用途。 其中：X为C或N，条件是当X为N时，R1不存在; W为C或N，条件是当W为N时，R2不存在; V是C; E是氢或其药学上可接受的盐; 并且Y选自由以下组成的组。另外，本发明提供可用于制备前药化合物I的中间体化合物II。其中：L和M独立地选自C1-C6烷基，苯基，苄基，三烷基甲硅烷基， 2,2,2-三氯乙氧基和2-三甲基甲硅烷基乙氧基。
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5.发明公开PROCESS FOR PREPARING NOVEL CRYSTALLINE FORMS OF (2S)-1-[[(7R)-7-(3,4-DICHLOROPHENYL)-4,7-DIHYDRO-5-METHYLPYRAZOLO[1,5]PYRIMIDINE-6-YL]CARBONYL]-2-(4-FLUOROPHENYL) PYRROLIDINE, NOVEL STABLE FORMS PRODUCED THEREIN AND FORMULATIONS 审中-公开过程用于产生（2S）新晶形-1 - [[（7R）-7-（3,4-二氯苯基）-4,7-二氢-5-甲基 - 吡唑并[1,5]嘧啶-6-基]羰基 基] -2-（4-氟苯基） - 吡咯烷及新IN它产生稳定形式和制剂
公开(公告)号：EP1814884A1
公开(公告)日：2007-08-08
申请号：EP05851950.5
申请日：2005-11-22
发明人： WANG, Xuebao , LAI, Chiajen , SOUNDARARAJAN, Nachimuthu , NGUYEN, Nina , YING, Weiming , BURTON, Lori, S. , GANDHI, Rajesh, Babulal , RAGHAVAN, Krishnaswamy Srinivas , WEST, Ronald, C. , ZHOU, Yuji, Simon , YAN, Lin , YIN, Xiaotian , DIMARCO, John, D. , GOUGOUTAS, Jack, Z.
IPC分类号： C07D487/04 , A61K31/519 , A61P9/06
CPC分类号： C07D487/04
摘要： A process is provided for preparing novel crystalline forms, namely selectively and consistently preparing the H2-1 dihydrate crystalline form, the H2-2 dihydrate crystalline form, the N-3 anhydrate crystalline form and the MTBE solvate crystalline form of the IKur compound (2S)-1-[[(7R)-7-(3,4-dichlorophenyl)-4,7-dihydro-5methylpyrazolo[1,5]pyrimidine-6-yl]carbonyl]-2-(4-fluorophenyl)pyrrolidine. The process includes preparation of the H2-1 and H2-2 forms which are used in preparing the N-3 anhydrate form which is particularly stable and has suitable flow properties and desired particle size. Novel H2-1 dihydrate and H2-2 dihydrate forms, the N-3 anhydrate form and the MTBE solvate form of the above IKur compound, pharmaceutical compositions containing such novel forms and a method for preventing or treating arrhythmias including atrial fibrillation and IKur related conditions employing such novel forms are also provided.
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6.发明公开PROCESS FOR PREPARING TRIAZOLE SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES AND NOVEL SALT FORMS PRODUCED THEREIN 有权用于生产TRIAZOLSUBSTITUIERTENAZAINDOLOXOESSIGSÄUREPIPERAZINDERIVATENWHILE产生了新的盐形式
公开(公告)号：EP1907389A2
公开(公告)日：2008-04-09
申请号：EP06785355.6
申请日：2006-06-21
发明人： SOUNDARARAJAN, Nachimuthu , QIU, Yuping , HU, Wenhao , KRONENTHAL, David, R. , SIRARD, Pierre , LAJEUNESSE, Jean , DROGHINI, Roberto , CHIDAMBARAM, Ramakrishnan , QIAN, Xinhua , NATALIE, JR., Kenneth, J. , PACK, Shawn, K. , REISING, Nathan , TANG, Erqing , FAKES, Michael, G. , GAO, Qi , QUIAN, Feng , VAKKALAGADDA, Blisse, J. , LAI, Chiajen , KUANG, Shan-Ming
IPC分类号： C07D471/04 , A61K31/4745 , A61P31/12
CPC分类号： C07D471/04 , C07C311/49 , C07D213/26
摘要： A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and processes for producing such novel forms are also provided.
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公开(公告)号：EP1725569A1
公开(公告)日：2006-11-29
申请号：EP05724510.2
申请日：2005-03-03
发明人： UEDA, Yasutsugu , CONNOLLY, Timothy, P. , KADOW, John, F. , MEANWELL, Nicholas, A. , WANG, Tao , CHEN, Chung-Pin, H. , YEUNG, Kap-Sun , ZHANG, Zhongxing , LEAHY, David Kenneth , PACK, Shawn, K. , SOUNDARARAJAN, Nachimuthu , SIRARD, Pierre , LEVESQUE, Kathia , THORAVAL, Dominique
IPC分类号： C07F9/09 , C07D471/04 , A61K31/437 , A61P31/18
CPC分类号： A61K31/675 , A61K31/497 , A61K45/06 , C07D471/04 , C07F9/062 , C07F9/5728 , C07F9/65515 , C07F9/65586 , C07F9/6561
摘要： This invention provides for prodrug Compounds (I), pharmaceutical compositions thereof, and their use in treating HIV infection. Also, this invention provides for intermediate Compounds (II) useful in making prodrug Compounds (I).
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公开(公告)号：EP1684754A1
公开(公告)日：2006-08-02
申请号：EP04811719.6
申请日：2004-11-19
发明人： O'CONNOR, Stephen P. , ROBL, Jeffrey , AHMAD, Saleem , BISAHA, Sharon , MURUGESAN, Natesan , NGU, Khehyong , SHI, Yan , STEIN, Philip D. , SOUNDARARAJAN, Nachimuthu , NATALIE, Kenneth J. Jr. , KOLLA, Laxma R. , SAUSKER, Justin , QUINLAN, Sandra L. , FAN, Junying , PETSCH, Dejah , GUO, Zhenrong
IPC分类号： A61K31/435 , A61K31/505 , C07D401/14 , C07D471/04
CPC分类号： C07D213/80 , C07D211/76 , C07D401/14 , C07D471/04 , C07D491/04 , C07D498/04 , C07D513/04
摘要： Compounds are provided having the following structure (I) and pharmaceutically acceptable salts thereof, A is (II) or (III); wherein R1, R2, R3, R4, U, V, W, Y, and n are as defined above, which compounds are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis and may be employed as hormone replacement therapy. A method for treating the above diseases employing the above compounds is also provided.
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