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1. 发明申请

WO2007056175A3 41-METHOXY ISOTOPE LABELED RAPAMYCIN 42-ESTER 审中-公开
标题翻译： 41-甲氧基异黄酮标记的RAPAMYCIN 42-ESTER
公开(公告)号：WO2007056175A3
公开(公告)日：2007-06-28
申请号：PCT/US2006043016
申请日：2006-11-03
申请人： WYETH CORP , GU JIANXIN , RUPPEN MARK
发明人： GU JIANXIN , RUPPEN MARK
IPC分类号： C07D498/18 , C07F7/18
CPC分类号： C07D498/18 , C07F7/1856
摘要： 41-methoxy-labeled rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2- methylpropionic acid (CCI-779) compounds are provided, along with methods for the synthesis and use thereof.
摘要翻译：提供具有3-羟基-2-（羟甲基）-2-甲基丙酸（CCI-779）化合物的41-甲氧基标记的雷帕霉素42-酯及其合成和使用方法。

2. 发明申请

WO2004093918A2 WATER SOLUBLE WORTMANNIN DERIVATIVES 审中-公开
标题翻译：水溶性沃尔曼宁衍生物
公开(公告)号：WO2004093918A2
公开(公告)日：2004-11-04
申请号：PCT/US2004/012158
申请日：2004-04-20
申请人： WYETH HOLDINGS CORPORATION , ZHU, Tianmin , YU, Ker , LUCAS, Judy , GU, Jianxin , ZASK, Arie
发明人： ZHU, Tianmin , YU, Ker , LUCAS, Judy , GU, Jianxin , ZASK, Arie
IPC分类号： A61K47/48
CPC分类号： A61K31/765
摘要： This invention relates to soluble derivatives of wortmannin that utilizes water-soluble polymers as carriers for a drug and includes compounds having the structures as described within the specification.
摘要翻译：本发明涉及使用水溶性聚合物作为药物载体的渥曼青霉素的可溶性衍生物，包括具有本说明书所述结构的化合物。

3. 发明申请

WO2007103348A3 PROCESS FOR PREPARING WATER-SOLUBLE POLYETHYLENE GLYCOL CONJUGATES OF MACROLIDE IMMUNOSUPPRESSANTS 审中-公开
标题翻译：制备高分子量免疫球蛋白的水溶性聚乙烯甘油的方法
公开(公告)号：WO2007103348A3
公开(公告)日：2008-05-08
申请号：PCT/US2007005646
申请日：2007-03-05
申请人： WYETH CORP , GU JIANXIN , RUPPEN MARK , ZHU TIANMIN , FAWZI MAHDI
发明人： GU JIANXIN , RUPPEN MARK , ZHU TIANMIN , FAWZI MAHDI
IPC分类号： A61K47/48 , A61P37/06
CPC分类号： C07D498/18 , A61K47/60
摘要： Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.
摘要翻译：描述了制备42-聚乙二醇化雷帕霉素的方法，包括在脂肪酶存在下使雷帕霉素与酰化剂反应形成酰化雷帕霉素，并在碱的存在下使酰化雷帕霉素与甲氧基聚（乙二醇）衍生物反应。还描述了使用这些步骤制备32-聚乙二醇化他克莫司和/或小霉素的方法。

4. 发明申请

WO2007103348A2 PROCESS FOR PREPARING WATER-SOLUBLE POLYETHYLENE GLYCOL CONJUGATES OF MACROLIDE IMMUNOSUPPRESSANTS 审中-公开
标题翻译：制备高分子量免疫球蛋白的水溶性聚乙烯甘油的方法
公开(公告)号：WO2007103348A2
公开(公告)日：2007-09-13
申请号：PCT/US2007/005646
申请日：2007-03-05
申请人： Wyeth , GU, Jianxin , RUPPEN, Mark , ZHU, Tianmin , FAWZI, Mahdi
发明人： GU, Jianxin , RUPPEN, Mark , ZHU, Tianmin , FAWZI, Mahdi
IPC分类号： A61K47/48 , A61P37/06
CPC分类号： C07D498/18 , A61K47/60
摘要： Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol) derivative in the presence of a base. Also described are processes for preparing 32-pegylated tacrolimus and/or ascomycin using these steps.
摘要翻译：描述了制备42-聚乙二醇化雷帕霉素的方法，包括在脂肪酶存在下使雷帕霉素与酰化剂反应形成酰化雷帕霉素，并在碱的存在下使酰化雷帕霉素与甲氧基聚（乙二醇）衍生物反应。还描述了使用这些步骤制备32-聚乙二醇化他克莫司和/或小霉素的方法。

5. 发明申请

WO2008124026A1 WORTMANNIN-RAPAMYCIN CONJUGATE AND USES THEREOF 审中-公开
标题翻译： WORTMANNIN-RAPAMYCIN结合物及其用途
公开(公告)号：WO2008124026A1
公开(公告)日：2008-10-16
申请号：PCT/US2008/004331
申请日：2008-04-03
申请人： WYETH , GU, Jianxin , YU, Ker , LUCAS, Judy , RUPPEN, Mark , ZASK, Arie , AYRAL-KALOUSTIAN, Semiramis
发明人： GU, Jianxin , YU, Ker , LUCAS, Judy , RUPPEN, Mark , ZASK, Arie , AYRAL-KALOUSTIAN, Semiramis
IPC分类号： C07D519/00 , A61K31/395 , A61P35/00
CPC分类号： C07D519/00 , A61K47/55
摘要： A rapamycin - wortmannin conjugate is described, in which the conjugate is formed by linking the rapamycin and wortmannin together in such a manner that the rapamycin and the wortmannin are separated following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.
摘要翻译：描述了雷帕霉素 - 渥曼青霉素缀合物，其中通过将雷帕霉素和渥曼青霉素连接在一起，使得雷帕霉素和渥曼青霉素在给予受试者后分离形成缀合物。描述了在抗肿瘤方案中使用这种缀合物。

6. 发明申请

WO2008124020A1 WORTMANNIN-RAPALOG CONJUGATE AND USES THEREOF 审中-公开
标题翻译： WORTMANNIN-RAPALOG合并及其用途
公开(公告)号：WO2008124020A1
公开(公告)日：2008-10-16
申请号：PCT/US2008/004323
申请日：2008-04-03
申请人： WYETH , GU, Jianxin , YU, Ker , LUCAS, Judy , RUPPEN, Mark , ZASK, Arie , AYRAL-KALOUSTIAN, Semiramis
发明人： GU, Jianxin , YU, Ker , LUCAS, Judy , RUPPEN, Mark , ZASK, Arie , AYRAL-KALOUSTIAN, Semiramis
IPC分类号： C07D519/00 , A61K31/395 , A61P35/00
CPC分类号： C07D519/00 , A61K31/395 , A61K31/407 , A61K31/436
摘要： An anti-neoplastic wortmannin conjugate is described formed by a linking a rapalog and wortmannin. Such a linkage is removable following administration to a subject. Use of such a conjugate in an antineoplastic regimen is described.
摘要翻译：描述了通过连接rapalog和渥曼青霉素形成的抗肿瘤性渥曼青霉素缀合物。这样的连接在给予受试者之后是可移除的。描述了在抗肿瘤方案中使用这种缀合物。

7. 发明申请

WO2007098124A3 PROCESSES FOR THE CONVERGENT SYNTHESIS OF CALICHEAMICIN DERIVATIVES 审中-公开
公开(公告)号：WO2007098124A3
公开(公告)日：2007-08-30
申请号：PCT/US2007/004301
申请日：2007-02-16
申请人： WYETH , MORAN, Justin, Keith , GU, Jianxin
发明人： MORAN, Justin, Keith , GU, Jianxin
IPC分类号： C07H15/203
摘要： This invention describes processes for the convergent synthesis of calicheamicin derivatives of Formula (I)1 and similar analogs using bifunctional and trifunctional linker intermediates.

8. 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。

9. 发明申请

WO2004093918A3 PEG-WORTMANNIN CONJUGATES 审中-公开
标题翻译： PEG-WORTMANNIN结合物
公开(公告)号：WO2004093918A3
公开(公告)日：2005-03-24
申请号：PCT/US2004012158
申请日：2004-04-20
申请人： WYETH CORP , ZHU TIANMIN , YU KER , LUCAS JUDY , GU JIANXIN , ZASK ARIE
发明人： ZHU TIANMIN , YU KER , LUCAS JUDY , GU JIANXIN , ZASK ARIE
IPC分类号： A61K31/765 , A61K47/48
CPC分类号： A61K31/765
摘要： This invention relates to soluble derivatives of wortmannin that utilizes water-soluble polymers as carriers for a drug and includes compounds having the structures as described within the specification.
摘要翻译：本发明涉及使用水溶性聚合物作为药物载体的渥曼青霉素的可溶性衍生物，包括具有本说明书所述结构的化合物。

10. 发明申请

WO2004031394A3 PROCESS FOR PREPARING MONOPROTECTED DIOLS FROM SYMMETRIC DIOLS 审中-公开
公开(公告)号：WO2004031394A3
公开(公告)日：2004-04-15
申请号：PCT/US2003/030920
申请日：2003-09-26
申请人： WYETH HOLDINGS CORPORATION , GU, Jianxin , RUPPEN, Mark, Edward
发明人： GU, Jianxin , RUPPEN, Mark, Edward
IPC分类号： C12P7/62
摘要： This invention provides a two-step enzymatic process for the synthesis of monoprotected diols from symmetric diols.

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