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1. 发明申请

WO2009012201A2 PROCESS FOR THE PREPARATION OF TRIFLUOROALKYL-PHENYL AND HETEROCYCLIC SULFONAMIDES 审中-公开
标题翻译：制备三氟烷基苯基和杂环磺酰胺的方法
公开(公告)号：WO2009012201A2
公开(公告)日：2009-01-22
申请号：PCT/US2008069934
申请日：2008-07-14
申请人： WYETH CORP , CONNOLLY TERRENCE JOSEPH , CHAN ANITA WAI-YIN , DING ZHIXIAN , GHOSH MOUSUMI R , SHI XINXU , REN JIANXIN , HANSEN ERIC , FARR ROGER , MACEWAN MICHAEL , ALIMARDANOV ASAF , NIKITENKO ANTONIA , POTOSKI JOHN
发明人： CONNOLLY TERRENCE JOSEPH , CHAN ANITA WAI-YIN , DING ZHIXIAN , GHOSH MOUSUMI R , SHI XINXU , REN JIANXIN , HANSEN ERIC , FARR ROGER , MACEWAN MICHAEL , ALIMARDANOV ASAF , NIKITENKO ANTONIA , POTOSKI JOHN
IPC分类号： C07D295/185 , C07D263/26 , C07D333/34
CPC分类号： C07D295/108 , C07D263/26 , C07D333/34
摘要： A novel trifluoroacetylating agent, i.e., N-trifluoroacetylmorpholine, is described. This reagent is useful in the preparation of phenyl and heterocyclic sulfonamide compounds. Methods are therefore described for preparing sulfonamide compounds of the following structure, wherein R1 and R2 are defined herein, using N- trifluoroacetylmorpholine. The sulfonamide compounds that may be prepared as described herein include 5-chloro-thiophene-2-sulfonic acid [(1S,2R)-2-(3,5-difluoro- phenyl)-3,3,3-trifluoro-1-hydroxymethyl-propyl]-amide using N- trifluoroacetylmorpholine.Formula (I).
摘要翻译：描述了一种新型的三氟乙酰化剂，即N-三氟乙酰吗啉。该试剂可用于制备苯基和杂环磺酰胺化合物。因此描述了使用N-三氟乙酰基吗啉制备具有以下结构的磺酰胺化合物的方法，其中R1和R2如本文所定义。可以如本文所述制备的磺酰胺化合物包括5-氯 - 噻吩-2-磺酸[（1S，2R）-2-（3,5-二氟 - 苯基）-3,3,3-三氟-1- 使用N-三氟乙酰基吗啉制备标题化合物（I）。

2. 发明申请

WO2008024492A3 INDOLINONE PHENYLAMINOPROPANOL DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF 审中-公开
标题翻译：吲哚啉酮苯基丙烯酸衍生物及其制备方法
公开(公告)号：WO2008024492A3
公开(公告)日：2008-05-15
申请号：PCT/US2007018782
申请日：2007-08-22
申请人： WYETH CORP , CHAN ANITA WAI-YIN , DING ZHIXIAN , GHOSH MOUSUMI , LEVENT MAHMUT , RAVEENDRANATH PANOLIL , REN JIANXIN , ZHOU MAOTANG , ALIMARDANOV ASAF , GONTCHAROV ALEXANDER V , NIKITENKO ANTONIA A , POTOSKI JOHN R
发明人： CHAN ANITA WAI-YIN , DING ZHIXIAN , GHOSH MOUSUMI , LEVENT MAHMUT , RAVEENDRANATH PANOLIL , REN JIANXIN , ZHOU MAOTANG , ALIMARDANOV ASAF , GONTCHAROV ALEXANDER V , NIKITENKO ANTONIA A , POTOSKI JOHN R
IPC分类号： C07D209/34 , A61K31/4045 , A61P25/00 , C07D405/06
CPC分类号： C07D209/34
摘要： Indolinone phenylaminopropanol derivatives of the general formula (I) : Processes for preparing them, intermediates useful in said processes and use thereof for treating conditions ameliorated by monoamine reuptake.
摘要翻译：通式（I）的吲哚啉酮苯基氨基丙醇衍生物：其制备方法，可用于所述方法的中间体及其用于处理通过单胺再摄取改善的条件。

3. 发明申请

WO2006089053A3 CYCLOALKYLFUSED INDOLE, BENZOTHIOPHENE, BENZOFURAN AND INDENE DERIVATIVES 审中-公开
标题翻译：环烷基吲哚，苯并苯，苯并呋喃和茚衍生物
公开(公告)号：WO2006089053A3
公开(公告)日：2007-01-11
申请号：PCT/US2006005521
申请日：2006-02-16
申请人： WYETH CORP , SABB ANNMARIE LOUISE , VOGEL ROBERT LEWIS , STACK GARY PAUL , EVRARD DEBORAH ANN , FAILLI AMEDEO ARTURO , KRISHNAN LALITHA , CHAN ANITA WAI-YIN , REN JIANXIN , GUINOSSO CHARLES , BAUDY REINHARDT BERNAHRD , SZE JEAN YI-CHING , LI YANFANG , STANTON CHARLES JOHN III , NIKITENKO ANTONIA
发明人： SABB ANNMARIE LOUISE , VOGEL ROBERT LEWIS , STACK GARY PAUL , EVRARD DEBORAH ANN , FAILLI AMEDEO ARTURO , KRISHNAN LALITHA , CHAN ANITA WAI-YIN , REN JIANXIN , GUINOSSO CHARLES , BAUDY REINHARDT BERNAHRD , SZE JEAN YI-CHING , LI YANFANG , STANTON CHARLES JOHN III , NIKITENKO ANTONIA
IPC分类号： C07D493/04 , A61K31/381 , A61K31/407 , A61K31/4741 , A61P25/24 , C07D209/88 , C07D233/76
CPC分类号： C07D209/88 , C07D233/76 , C07D491/04 , C07D493/04
摘要： The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HT1A receptors and modulating serotonin levels.
摘要翻译：本发明提供环烷基稠合吲哚，苯并噻吩，苯并呋喃和茚衍生物，以及使用它们例如通过拮抗5-HT 1A受体和调节5-羟色胺水平来治疗，预防和/或改善中枢神经系统疾病的方法。

4. 发明申请

WO2009006267A3 N'-(2-HALOBENZYLIDENE)SULFONYLHYDRAZIDES AS INTERMEDIATES IN THE MANUFACTURE OF ARYLSULFONYLINDAZOLES 审中-公开
标题翻译： N' - （2-卤代苯亚甲基）磺酰基肼在芳基磺酰基吲哚生产中的中间体
公开(公告)号：WO2009006267A3
公开(公告)日：2009-04-16
申请号：PCT/US2008068509
申请日：2008-06-27
申请人： WYETH CORP , RAVEENDRANATH SANJAY , RAVEENDRANATH VIJAY , RAVEENDRANATH GIRIJA , CHAN ANITA WAI-YIN , LEVENT MAHMUT , PLACE DAVID , SHI XINXU , WU CHARLES
发明人： CHAN ANITA WAI-YIN , LEVENT MAHMUT , PLACE DAVID , SHI XINXU , WU CHARLES , RAVEENDRANATH PANOLIL
IPC分类号： C07D231/56 , C07C303/40 , C07C311/49 , C07D295/12 , C07D295/20
CPC分类号： C07C311/49 , C07C303/40 , C07D231/56 , C07D295/135 , C07D295/205
摘要： The present invention provides N'-(2-halobenzylidene)sulfonylhydrazides of formula (I). Compounds of formula (I) are useful for the manufacture of 1-arylsulfonylindazole 5-HT6 ligands.
摘要翻译：本发明提供了式（I）的N' - （2-卤代亚苄基）磺酰肼。式（I）化合物可用于制备1-芳基磺酰基吲唑5-HT 6配体。

5. 发明申请

WO2007098030A8 SELECTIVE N-SULFONYLATION OF 2-AMINO TRIFLUOROALKYL SUBSTITUTED ALCOHOLS 审中-公开
标题翻译： 2-氨基三氟甲磺酸取代的醇的选择性N-磺酰化
公开(公告)号：WO2007098030A8
公开(公告)日：2007-10-25
申请号：PCT/US2007004091
申请日：2007-02-15
申请人： WYETH CORP , CHAN ANITA WAI-YIN , REN JIANXIN , GHOSH MOUSUMI , RAVEENDRANATH PANOLIL
发明人： CHAN ANITA WAI-YIN , REN JIANXIN , GHOSH MOUSUMI , RAVEENDRANATH PANOLIL
IPC分类号： C07D333/34 , C07C303/38 , C07C311/17
CPC分类号： C07C303/38 , C07B2200/07 , C07D333/34 , C07D333/38 , C07C311/17
摘要： Processes for the preparation of trifluoroalkyl substituted N-(2-hydroxyalkyl) heteroarene- and benzenesulphonamide derivatives of formula (I) or formula (II) (wherein the variables are as defined in the claims) are provided which comprises reacting a trifluoroalkyl substituted amino alcohol, a sulphonyl chloride and a base/solvent system selected from the group consisting of (a) 4-methylmorpholine/isopropyl acetate, (b) Hünig's base/tetrahydrofuran, (c) 4-methylmorpholine/acetonitrile, (d) 4-methylmorpholine/propionitrile and (e) 4-methylmorpholin/ftoluene. Formulae (I) and (II).
摘要翻译：制备式（I）或式（II）的三氟烷基取代的N-（2-羟基烷基）杂芳烃和苯磺酰胺衍生物的方法（其中变量如权利要求中所定义）包括使三氟烷基取代的氨基醇（a）4-甲基吗啉/乙酸异丙酯，（b）Hünig碱/四氢呋喃，（c）4-甲基吗啉/乙腈，（d）4-甲基吗啉/ 丙腈和（e）4-甲基吗啉/甲苯。式（I）和（II）。

6. 发明申请

WO2004104006A3 PROCESS FOR SYNTHESIZING beta-LACTAMASE INHIBITOR IN INTERMEDIATES 审中-公开
标题翻译：在中间体中合成β-LACTAMASE抑制剂的方法
公开(公告)号：WO2004104006A3
公开(公告)日：2005-01-27
申请号：PCT/US2004014834
申请日：2004-05-12
申请人： WYETH CORP , WINKLEY MICHAEL WILLIAM , CHAN ANITA WAI-YIN , JIRKOVSKY IVO L , KREMER KENNETH ALFRED MARTIN , ZELDIS JOSEPH , NIKITENKO ANTONINA ARISTOTELEV , STRONG HENRY LEE , MANSOUR TAREK SUHAYL , KHAFIZOVA GULNAZ , VENKATESAN ARANAPAKAM MUDUMBAI
发明人： WINKLEY MICHAEL WILLIAM , CHAN ANITA WAI-YIN , JIRKOVSKY IVO L , KREMER KENNETH ALFRED MARTIN , ZELDIS JOSEPH , NIKITENKO ANTONINA ARISTOTELEV , STRONG HENRY LEE , MANSOUR TAREK SUHAYL , KHAFIZOVA GULNAZ , VENKATESAN ARANAPAKAM MUDUMBAI
IPC分类号： C07D487/04 , C07D513/12 , C07D519/00
CPC分类号： C07D498/04 , C07D487/04
摘要： There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula (I) where X and Y are defined in the specification. The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of beta-lactamase inhibitors.
摘要翻译：提供了具有结构式（I）的双环杂芳基羧醛的制备方法，其中X和Y在说明书中定义。双环杂芳基羧醛可用作制备β-内酰胺酶抑制剂的中间体。

7. 发明申请

WO03078396A8 PREPARATION OF N1-(2'-PYRIDYL)-1,2-PROPANEDIAMINE SULFAMIC ACID AND ITS USE IN THE SYNTHESIS OF BIOLOGICALLY ACTIVE PIPERAZINES 审中-公开
标题翻译： N1-（2'-吡啶基）-1,2-丙二胺磺酸的制备及其在生物活性哌嗪的合成中的应用
公开(公告)号：WO03078396A8
公开(公告)日：2004-01-29
申请号：PCT/US0307228
申请日：2003-03-10
申请人： WYETH CORP , CHAN ANITA WAI-YIN , FEIGELSON GREGG BRIAN , ZELDIS JOSEPH , JIRKOVSKY IVO
发明人： CHAN ANITA WAI-YIN , FEIGELSON GREGG BRIAN , ZELDIS JOSEPH , JIRKOVSKY IVO
IPC分类号： A61P25/00 , C07D213/74 , C07D213/75 , C07D213/76 , C07D405/12 , A61K31/44
CPC分类号： C07D213/74 , C07D213/75 , C07D213/76 , C07D405/12
摘要： A process for making an N1-(2'-pyridyl)-1,2-alkanediamine sulfamic acid of formula (II) by reacting a compound of formula (I) with NH2R', wherein R and R' are as defined in the specification. The invention also includes the compound of formula (II), and optical isomers thereof. The compound of formula (II) is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT1A receptor.
摘要翻译：通过使式（I）化合物与NH 2 R'反应制备式（II）的N1-（2'-吡啶基）-1,2-链烷二胺氨基磺酸的方法，其中R和R'如说明书中所定义。本发明还包括式（II）化合物及其旋光异构体。式（II）化合物是可用于制备在5-HT 1A受体上具有活性的手性哌嗪衍生物的中间体。

8. 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。

9. 发明申请

WO02092602A3 PROCESSES FOR THE SYNTHESIS OF DERIVATIVES OF 2,3-DIHYDRO-1,4-DIOXINO-[2,3-f] QUINOLINE 审中-公开
标题翻译：合成2,3-二氢-1,4-二氧杂 - [2,3-f]喹啉的衍生物的方法
公开(公告)号：WO02092602A3
公开(公告)日：2003-02-27
申请号：PCT/US0215097
申请日：2002-05-14
申请人： WYETH CORP
发明人： CHAN ANITA WAI-YIN , CURRAN TIMOTHY THOMAS , IERA SILVIO , CHEW WARREN , SELLSTEDT JOHN HAMILTON , VID GALINA , FEIGELSON GREGG , DING ZHIXIAN
IPC分类号： C07D215/20 , A61P25/00 , C07D401/04 , C07D491/04 , C07D491/056 , C07D519/00 , A61K31/436
CPC分类号： C07D491/04
摘要： Methods of preparing compounds of Formula (I) are provided.
摘要翻译：提供制备式（I）化合物的方法。

10. 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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