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1. 发明申请

WO2007016029A2 DIAZEPINOQUINOLINES, SYNTHESIS THEREOF, AND INTERMEDIATES THERETO 审中-公开
标题翻译：二氮杂环丁烷，其合成及其中间体
公开(公告)号：WO2007016029A2
公开(公告)日：2007-02-08
申请号：PCT/US2006028655
申请日：2006-07-24
申请人： WYETH CORP , MEGATI SREENIVASULU , CHAN ANITA WAI-YIN , FEIGELSON GREGG B
发明人： MEGATI SREENIVASULU , CHAN ANITA WAI-YIN , FEIGELSON GREGG B
IPC分类号： C07D471/06 , C07D221/16
CPC分类号： C07D221/16 , C07D471/06
摘要： The present invention relates to methods for synthesizing compounds useful as 5HT2c agonists or partial agonists, derivatives thereof, and to intermediates thereto.
摘要翻译：本发明涉及合成可用作5HT2c激动剂或部分激动剂，其衍生物及其中间体的化合物的方法。

2. 发明申请

WO2009039362A2 CHIRAL SYNTHESIS OF DIAZEPINOQUINOLINES 审中-公开
标题翻译： DIAZEPINOQUINOLINES的CHIRAL SYNTHESIS
公开(公告)号：WO2009039362A2
公开(公告)日：2009-03-26
申请号：PCT/US2008077003
申请日：2008-09-19
申请人： WYETH CORP , MEGATI SREENIVASULU , BHANSALI SHILPA , DEHNHARDT CHRISTOPH , DESHMUKH SUBODH , FUNG PETER , MACEWAN MICHAEL , TINDER ROBERT J
发明人： MEGATI SREENIVASULU , BHANSALI SHILPA , DEHNHARDT CHRISTOPH , DESHMUKH SUBODH , FUNG PETER , MACEWAN MICHAEL , TINDER ROBERT J
IPC分类号： C07D471/06 , A61K31/5517 , A61P25/18
CPC分类号： C07D471/06
摘要： The present invention relates to improved methods of resolution and recrystallization for synthesizing compounds useful as 5HT2c agonists or partial agonists, including intermediates thereto.
摘要翻译：本发明涉及用于合成可用作5HT 2C激动剂或部分激动剂（包括其中间体）的化合物的分辨和重结晶的改进方法。

3. 发明申请

WO2006052768A3 PROCESS FOR PREPARING QUINOLINE COMPOUNDS AND PRODUCTS OBTAINED THEREFROM 审中-公开
标题翻译：制备喹啉化合物的方法及其获得的产品
公开(公告)号：WO2006052768A3
公开(公告)日：2006-08-17
申请号：PCT/US2005040062
申请日：2005-11-04
申请人： WYETH CORP , DEHNHARDT CHRISTOPH , MEGATI SREENIVASULU , SUN JERRY
发明人： DEHNHARDT CHRISTOPH , MEGATI SREENIVASULU , SUN JERRY
IPC分类号： C07D471/06 , A61K31/5513 , A61P3/04 , A61P25/18
CPC分类号： C07D471/06 , Y10T428/2982
摘要： Methods for synthesizing tetrahydroquinoline-containing compounds of formula (II) are provided, along with synthetic intermediates and products associated with such methods.
摘要翻译：提供了合成含有四氢喹啉的式（II）化合物的方法以及与这些方法相关的合成中间体和产物。

4. 发明申请

WO2008100769A3 PROCESS FOR SELECTIVE SULFATION OF AROMATIC HYDROXYL GROUPS 审中-公开
标题翻译：芳香羟基选择性硫化方法
公开(公告)号：WO2008100769A3
公开(公告)日：2009-01-29
申请号：PCT/US2008053276
申请日：2008-02-07
申请人： WYETH CORP , MEGATI SREENIVASULU , RAVEENDRANATH PANOLIL
发明人： MEGATI SREENIVASULU , RAVEENDRANATH PANOLIL
IPC分类号： C07J31/00 , A61K31/565 , A61P5/30
CPC分类号： C07J31/006
摘要： The present invention relates to processes for selective sulfation of an aromatic hydroxyl group over an aliphatic hydroxyl group where both are present in the same molecule. This invention also relates to processes for selective sulfation of the aromatic hydroxyl group of equilin, equilenin, estradiol, estra(1,3,5-triene)- 3,16,17-triol, dihydroequilenin or dihydroequilin. This invention further relates to alkali metal salts of dihydroequilenin sulfates, dihydroequilin sulfates, estradiol sulfates, and estriol sulfates, processes for making thereof, stable compositions comprising thereof, and the use thereof.
摘要翻译：本发明涉及在脂肪族羟基上选择性硫酸化芳族羟基的方法，其中两者都存在于同一分子中。本发明还涉及选择性硫酸化平衡，平衡，雌二醇，雌二醇（1,3,5-三烯）-3,16,17-三醇，二氢马来西林或二氢马雌二醇的芳族羟基的方法。本发明还涉及硫酸二氢马来酰氯，二氢巯基硫酸盐，雌二醇硫酸盐和雌三醇硫酸盐的碱金属盐，其制备方法，包含它们的稳定组合物及其用途。

5. 发明申请

WO2004026814A3 PROCESS FOR THE SYNTHESIS OF INTERMEDIATES USEFUL FOR THE SYNTHESIS OF TUBULIN INHIBITORS 审中-公开
标题翻译：合成中间体的方法用于合成微管蛋白抑制剂
公开(公告)号：WO2004026814A3
公开(公告)日：2004-08-12
申请号：PCT/US0328661
申请日：2003-09-12
申请人： WYETH CORP , WU YANZHONG , MEGATI SREENIVASULU , GLETSOS CONSTANTINE , KENDALL JOHN THOMAS , WILK BOGDAN KAZIMIERZ , PADMANATHAN THURAIRAJAH , RAVEENDRANATH PANOLIL
发明人： WU YANZHONG , MEGATI SREENIVASULU , GLETSOS CONSTANTINE , KENDALL JOHN THOMAS , WILK BOGDAN KAZIMIERZ , PADMANATHAN THURAIRAJAH , RAVEENDRANATH PANOLIL
IPC分类号： A61K38/00 , C07C45/44 , C07C45/58 , C07C231/18 , C07C237/22 , C07C269/08 , C07C271/22 , C07C313/06 , C07K5/02 , C07B57/00 , C07K5/06 , C07K5/065
CPC分类号： C07K5/0205 , A61K38/00 , C07B2200/07 , C07C45/44 , C07C45/58 , C07C231/18 , C07C237/22 , C07C269/08 , C07C271/22 , C07C313/06 , C07C47/228
摘要： The invention is a process for the preparation of compounds of the Formula (I): where R1, R2, R3, R4 and R5 are defined in the specification, which are intermediates useful for the preparation of tubulin inhibitors useful in the treatment of cancer.
摘要翻译：本发明是制备式（I）化合物的方法：其中R 1，R 2，R 3，R 4和R 5在说明书中定义，它们是可用于制备用于治疗癌症的微管蛋白抑制剂的中间体。

6. 发明申请

WO2010039851A9 PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF 审中-公开
标题翻译：外周血糖受体拮抗剂及其用途
公开(公告)号：WO2010039851A9
公开(公告)日：2010-06-24
申请号：PCT/US2009059058
申请日：2009-09-30
申请人： WYETH LLC , BAZHINA NATALIYA , DONATO GEORGE JOSEPH , FABIAN STEVEN R , LOKHNAUTH JOHN , MEGATI SREENIVASULU , MELUCCI CHARLES , OFSLAGER CHRISTIAN , PATEL NIKETA , RADEBAUGH GALEN , SHAH SYED M , SZELIGA JAN , ZHANG HUYI , ZHU TIANMIN
发明人： BAZHINA NATALIYA , DONATO GEORGE JOSEPH , FABIAN STEVEN R , LOKHNAUTH JOHN , MEGATI SREENIVASULU , MELUCCI CHARLES , OFSLAGER CHRISTIAN , PATEL NIKETA , RADEBAUGH GALEN , SHAH SYED M , SZELIGA JAN , ZHANG HUYI , ZHU TIANMIN
IPC分类号： C07D471/08 , A61K31/485 , A61P1/10 , C07D489/08
CPC分类号： A61K31/485 , A61J1/05 , A61K9/0019 , A61K9/0053 , A61K9/08 , A61K9/20 , A61M5/178 , C07D471/08 , C07D489/08 , Y10T436/145555
摘要： The present invention provides a compound of formula I wherein X", R1, and R2 are as defined herein, and compositions thereof. The compounds include and are based on an impurity of methylnaltrexone, a peripheral opioid antagonist.
摘要翻译：本发明提供了其中X“，R 1和R 2如本文所定义的式I化合物及其组合物。该化合物包括并基于甲基纳曲酮，外周阿片样物质拮抗剂的杂质。

7. 发明申请

WO0242304A3 CYCLOPENTA[B][1,4] DIAZEPINO[6,7,1-HI]INDOLES AS 5HT2C ANTAGONISTS 审中-公开
标题翻译：环己基[B] [1,4] DIAZEPINO [6,7,1-HI]作为5HT2C拮抗剂
公开(公告)号：WO0242304A3
公开(公告)日：2002-08-29
申请号：PCT/US0145792
申请日：2001-11-01
申请人： WYETH CORP
发明人： SABB ANNMARIE LOUISE , VOGEL ROBERT LEWIS , NELSON JAMES ALBERT , ROSENZWEIG-LIPSON SHARON JOY , WELMAKER GREGORY SCOTT , SABALSKI JOAN EILEEN , SMITH MICHAEL DAVID , CHAN ANITA WAI-YIN , ANTANE MADELENE MIYOKO , RAVEENDRANATH PANOLIL , MEGATI SREENIVASULU
IPC分类号： C07D209/94 , C07D487/00 , C07D487/06 , A61K31/551 , A61P3/10
CPC分类号： C07D487/06 , C07D209/94
摘要： This invention provides compounds of the formulae: (I) or (II), wherein: R1 is hydrogen, alkyl of 1-6 carbon atoms, atoms, acyl of 2-7 carbon atoms, aryl, heteroaryl, or -C(O)R' wherein R' is alkyl of from 1 to 6 carbon atoms, aryl, or heteoaryl; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-7 carbon atoms, alkoxy of 1-6 carbon atoms, -CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, -CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing these compounds and methods for their use, including treatment of obsessive-compulsive disorder, panic disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.
摘要翻译：本发明提供式（I）或（II）化合物，其中：R 1是氢，1-6个碳原子的烷基，2-7个碳原子的酰基，芳基，杂芳基或-C（O） R'其中R'是1至6个碳原子的烷基，芳基或杂芳基; R2和R3各自独立地为氢，1-6个碳原子的烷基，3-7个碳原子的环烷基，1-6个碳原子的烷氧基，-CH2OH，氟代烷基，1-6个碳原子的烷基磺酰胺，烷基酰胺 1-6个碳原子的氨基，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基，R4和R5各自独立地为氢，1-6个碳原子的烷基，1- 6个碳原子，卤素，氟烷基，-CN，1-6个碳原子的烷基磺酰胺，1-6个碳原子的烷基酰胺，1-6个碳原子的烷基氨基，每个烷基部分1-6个碳原子的二烷基氨基， 1-6个碳原子的氟烷氧基，2-7个碳原子的酰基，或芳酰基; R6和R7各自独立地为氢，C1-C6烷基或环烷基; 或其药学上可接受的盐，以及含有这些化合物的药物组合物及其使用方法，包括治疗强迫症，恐慌症，抑郁症，焦虑症，广泛性焦虑症，精神分裂症，偏头痛，睡眠障碍，进食障碍，肥胖，癫痫和脊髓损伤。

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