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1. 发明申请

WO2005100366A1 PROLINE CCI-779 (PROLINE-RAPAMYCIN 42-ESTER WITH 2,2-BIS (HYDROXYMETHYL) PROPIONIC ACID) AND TWO-STEP ENZYMATIC SYNTHESIS OF PROLINE CCI-779 AND CCI-779 USING MICROBIAL LIPASE 审中-公开
标题翻译： PROLINE CCI-779（具有2,2-BIS（羟基甲基）丙酸的PROLINE-RAPAMYCIN 42-ESTER）和使用微生物脂蛋白的丙烯酸CCI-779和CCI-779的两步酶合成
公开(公告)号：WO2005100366A1
公开(公告)日：2005-10-27
申请号：PCT/US2005/012030
申请日：2005-04-12
申请人： WYETH , GU, Jianxin , RUPPEN, Mark, E. , RAVEENDRANATH, Panolil , CHEW, Warren , SHAW, Chia-Cheng
发明人： GU, Jianxin , RUPPEN, Mark, E. , RAVEENDRANATH, Panolil , CHEW, Warren , SHAW, Chia-Cheng
IPC分类号： C07D498/18
CPC分类号： C07D498/08
摘要： Disclosed are proline-rapamycin 42-ester with 2,2-bis(hydroxymethyl)propionic acid (proline-CCI-779) as well as a method for the regiospecific preparation of a rapamycin 42-ester or proline-rapamycin 42-ester with 2,2-bis(hydroxymethyl)propionic acid (CCI-779 and proline-CCI-779) comprising the steps of: (a) reacting rapamycin or proline-rapamycin with an activated ester derivative of 2,2-bis(hydroxymethyl)propionic acid having the structure (A) wherein R 1 and R 2 are hydrogen, or taken together to form a ketal with the structure (B) wherein R 3 and R 4 are each, independently, hydrogen, C 1-6 alkyl, either linear or branched, or taken together form C 5-7 cycloalkyl or taken together form cyclic boronate with the structure (C), wherein R 5 is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl and phenyl; in a suitable organic solvent in the presence of an effective amount of microbial lipase; and (b) deprotecting the intermediate resulting from step (a) to provide CCI-779 or proline-CCI-779.
摘要翻译：公开的是具有2,2-双（羟甲基）丙酸（脯氨酸-CII-779）的脯氨酸 - 雷帕霉素42-酯以及用于区域特异性制备雷帕霉素42-酯或脯氨酸 - 雷帕霉素42-酯的方法，其具有2 包括以下步骤：（a）将雷帕霉素或脯氨酸 - 雷帕霉素与2,2-双（羟甲基）丙酸的活化酯衍生物反应，得到2-双（羟甲基）丙酸（CCI-779和脯氨酸-CII-779）具有结构（A），其中R 1和R 2是氢，或者一起形成具有结构（B）的缩酮，其中R 3和R 4各自独立地是氢，直链或支链的C 1-6烷基或一起形成C 5-7环烷基或一起形成具有结构（C）的环状硼酸酯，其中R 5选自甲基，乙基，正丙基，异丙基，正丁基，异丁基和苯基; 在合适的有机溶剂中，在有效量的微生物脂肪酶存在下，和（b）将步骤（a）得到的中间体脱保护，得到CCI-779或脯氨酸-CII-779。

2. 发明申请

WO2005016935A3 REGIOSELECTIVE SYNTHESIS OF CCI-779 审中-公开
公开(公告)号：WO2005016935A3
公开(公告)日：2005-02-24
申请号：PCT/US2004/022860
申请日：2004-07-15
申请人： WYETH , CHEW, Warren , SHAW, Chia-Cheng
发明人： CHEW, Warren , SHAW, Chia-Cheng
IPC分类号： C07D498/22
摘要： A method for regioselective synthesis of CCI-779 based on boronate chemistry is provided. Also provided are novel intermediates useful in this method.

3. 发明申请

WO2007123941A2 CHROMANE AND CHROMENE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： CHROMANE和CHROMENE DORIVATIVES及其用途
公开(公告)号：WO2007123941A2
公开(公告)日：2007-11-01
申请号：PCT/US2007/009463
申请日：2007-04-18
申请人： WYETH , GONTCHAROV, Alexander, V. , NIKITENKO, Antonia, A. , RAVEENDRANATH, Panolil , SHAW, Chia-Cheng , WILK, Bogdan, K. , ZHOU, Dahui
发明人： GONTCHAROV, Alexander, V. , NIKITENKO, Antonia, A. , RAVEENDRANATH, Panolil , SHAW, Chia-Cheng , WILK, Bogdan, K. , ZHOU, Dahui
IPC分类号： C07D311/58
CPC分类号： C07D311/58
摘要： Methods of preparing compounds of formula (I) or pharmaceutically acceptable salts thereof are provided wherein each of R 1 , R 2 , R 3 , R 4 , x, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
摘要翻译：提供制备式（I）化合物或其药学上可接受的盐的方法，其中R 1，R 2，R 3，R 3， x，m，n和Ar定义如下，并且在本文的类别和亚类中描述，其是脑5-羟色胺受体的2C亚型的激动剂或部分激动剂。化合物和含有这些化合物的组合物可用于治疗各种中枢神经系统疾病如精神分裂症。

4. 发明申请

WO2006047228A1 ASYMMETRIC SYNTHESIS OF SUBSTITUTED DIHYDROBENZOFURANS 审中-公开
标题翻译：替代二氢苯并呋喃的不对称合成
公开(公告)号：WO2006047228A1
公开(公告)日：2006-05-04
申请号：PCT/US2005/037772
申请日：2005-10-21
申请人： WYETH , GONTCHAROV, Alexander, V. , KHAFIZOVA, Gulnaz , POTOSKI, John, R. , YU, Qing , SHAW, Chia-Cheng , STACK, Gary Paul , ZHOU, Dahui
发明人： GONTCHAROV, Alexander, V. , KHAFIZOVA, Gulnaz , POTOSKI, John, R. , YU, Qing , SHAW, Chia-Cheng , STACK, Gary Paul , ZHOU, Dahui
IPC分类号： C07D303/22 , C07D307/81 , A61K31/343 , A61P25/18
CPC分类号： C07D209/48 , C07D303/22 , C07D307/79 , C07D307/81 , C07D405/04
摘要： The present invention concerns production of a compound of the formula (I) or a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula (II) where Ar, Y, R 1 , R Y , R 2 , and m are as defined herein.
摘要翻译：本发明涉及通过利用式（II）的化合物环化的方法制备式（I）化合物或其药学上可接受的盐，其中Ar，Y，R 1， R 2，R 2和R 2如本文所定义。

5. 发明申请

WO2007139797A2 METHOD OF PREPARING 4-HALOGENATED QUINOLINE INTERMEDIATES 审中-公开
标题翻译：制备4-羟基喹啉中间体的方法
公开(公告)号：WO2007139797A2
公开(公告)日：2007-12-06
申请号：PCT/US2007/012211
申请日：2007-05-23
申请人： WYETH , BERNIER, Caroline , SHAW, Chia-Cheng
发明人： BERNIER, Caroline , SHAW, Chia-Cheng
IPC分类号： C07D215/56 , C07D401/12
CPC分类号： C07D215/56 , C07D401/12
摘要： This invention is directed to methods of preparing compounds of formula (I): comprising the step of reacting a compound of formula (II): with a reagent of formula POX 3 and silica gel at a temperature greater than about 75°C, and wherein substitutions at X, PG, A, G, R 1 and R 4 are set forth in the specification.
摘要翻译：本发明涉及制备式（I）化合物的方法：包括使式（II）化合物与式POX 3 3的试剂和硅胶在大于约75℃，并且其中X，PG，A，G，R 1和R 4上的取代在说明书中阐述。

6. 发明申请

WO2006002125A1 INDOLYLALKYLAMINE METABOLITES AS 5-HYDROXYTRYTAMINE-6 LIGANDS 审中-公开
标题翻译：作为5-羟基鸟氨酸-6配体的间苯二酚代谢物
公开(公告)号：WO2006002125A1
公开(公告)日：2006-01-05
申请号：PCT/US2005/021852
申请日：2005-06-21
申请人： WYETH , WANG, Youchu , SHAW, Chia-Cheng , BERNOTAS, Ronald Charles , WANG, Chung-Chiee Paul , CAI, Ping , WANG, Zhi
发明人： WANG, Youchu , SHAW, Chia-Cheng , BERNOTAS, Ronald Charles , WANG, Chung-Chiee Paul , CAI, Ping , WANG, Zhi
IPC分类号： C07D417/12
CPC分类号： C07D513/04 , C07H7/033 , C07H15/26
摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与5-HT 6受体有关或受其影响的病症的用途。

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