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1. 发明申请

WO2007089669A3 PROCESSES FOR THE PREPARATION OF COMPOUNDS WHICH MODULATE CELL PROLIFERATION 审中-公开
标题翻译：制备调节细胞增殖化合物的方法
公开(公告)号：WO2007089669A3
公开(公告)日：2007-11-22
申请号：PCT/US2007002323
申请日：2007-01-25
申请人： WYETH CORP , KRISHNAN LALITHA , BLUM DAVID M , DILLEY ANJA SUSANNE , PAN SHERRY , POTOSKI JOHN R , SHAH URESH S , SHARMA ARCHANA , STRONG HENRY LEE , WU YANZHONG , ZHANG MEI-YI
发明人： KRISHNAN LALITHA , BLUM DAVID M , DILLEY ANJA SUSANNE , PAN SHERRY , POTOSKI JOHN R , SHAH URESH S , SHARMA ARCHANA , STRONG HENRY LEE , WU YANZHONG , ZHANG MEI-YI
IPC分类号： C07D213/61 , C07C271/24 , C07D333/70 , C07D409/12 , C07F5/02
CPC分类号： C07D409/12 , C07D213/61 , C07D333/70
摘要： The present invention provides improved synthetic methods for the preparation of compounds (I) that modulate proliferation or differentiation in a cell or tissue.
摘要翻译：本发明提供用于制备调节细胞或组织中的增殖或分化的化合物（I）的改进的合成方法。

2. 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。

3. 发明申请

WO2007146072A3 PROCESS FOR SYNTHESIZING PIPERAZINE-PIPERIDINE COMPOUNDS 审中-公开
公开(公告)号：WO2007146072A3
公开(公告)日：2007-12-21
申请号：PCT/US2007/013433
申请日：2007-06-07
申请人： WYETH , LIU, Weiguo , DRAGAN, Vladimir , STRONG, Henry Lee , WU, Yanzhong , WEN, Zhixin , LIANG, Jessica Kangping , DURUTLIC, Haris , SUTHERLAND, Karen Wiggins , PILCHER, Anthony Scott
发明人： LIU, Weiguo , DRAGAN, Vladimir , STRONG, Henry Lee , WU, Yanzhong , WEN, Zhixin , LIANG, Jessica Kangping , DURUTLIC, Haris , SUTHERLAND, Karen Wiggins , PILCHER, Anthony Scott
IPC分类号： C07D215/40 , C07D401/14 , C07D405/14
摘要： The present invention relates to processes for synthesizing piperazine-piperidine compounds, and compounds useful as 5-HT 1A binding agents, particularly as 5-HT 1A receptor antagonists and agonists. The processes also allow for safer and environmentally tolerant production of these useful compounds.

4. 发明申请

WO2007089669A2 PROCESSES FOR THE PREPARATION OF COMPOUNDS 审中-公开
标题翻译：化合物的制备方法
公开(公告)号：WO2007089669A2
公开(公告)日：2007-08-09
申请号：PCT/US2007/002323
申请日：2007-01-25
申请人： WYETH , KRISHNAN, Lalitha , BLUM, David, M. , DILLEY, Anja, Susanne , PAN, Sherry , POTOSKI, John, R. , SHAH, Uresh, S. , SHARMA, Archana , STRONG, Henry, Lee , WU, Yanzhong , ZHANG, Mei-Yi
发明人： KRISHNAN, Lalitha , BLUM, David, M. , DILLEY, Anja, Susanne , PAN, Sherry , POTOSKI, John, R. , SHAH, Uresh, S. , SHARMA, Archana , STRONG, Henry, Lee , WU, Yanzhong , ZHANG, Mei-Yi
IPC分类号： C07D213/61 , C07D333/70 , C07D409/12 , C07C271/24 , C07F5/02
CPC分类号： C07D409/12 , C07D213/61 , C07D333/70
摘要： The present invention provides improved synthetic methods for the preparation of compounds that modulate proliferation or differentiation in a cell or tissue.
摘要翻译：本发明提供了用于制备调节细胞或组织中的增殖或分化的化合物的改进的合成方法。

5. 发明申请

WO2005019201A3 PROCESS FOR THE PREPARATION OF 4-AMINO-3-QUINOLINECARBONITRILES 审中-公开
标题翻译：制备4-氨基-3-喹啉酮的方法
公开(公告)号：WO2005019201A3
公开(公告)日：2005-08-04
申请号：PCT/US2004026329
申请日：2004-08-13
申请人： WYETH CORP , WIGGINS SUTHERLAND KAREN , FEIGELSON GREGG BRIAN , BOSCHELLI DIANE HARRIS , BLUM DAVID MICHAEL , STRONG HENRY LEE
发明人： WIGGINS SUTHERLAND KAREN , FEIGELSON GREGG BRIAN , BOSCHELLI DIANE HARRIS , BLUM DAVID MICHAEL , STRONG HENRY LEE
IPC分类号： C07D215/54 , C07D405/04 , C07D495/04
CPC分类号： C07D405/04 , C07D215/54 , C07D495/04
摘要： This invention discloses a process for the preparation of a 4-amino-3quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up-to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield an 2-amino-2-cyanoacrylamide; combining the 3-amino2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine6-carbonitrile comprising combining a 3-amino thiophene with a cyanoacetamide and trial kylorthoformate in an alcoholic solvent to obtain a 3-amino2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4 amino-3-quinolinecarbonitrile comprising: combining an amine compound with cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension; to yield cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline with an alcoholic solvent to yield a 4-amino-3-quinolinecarbonitrile, and the invention discloses a process for obtaining a cyanoacetamide.
摘要翻译：本发明公开了一种制备4-氨基-3-喹啉腈的方法，包括将胺化合物与氰基乙酸和酸催化剂混合以产生氰基乙酰胺; 将氰基乙酰胺与醇溶剂和原甲酸三烷基酯中的任选的上述四取代的苯胺缩合，得到2-氨基-2-氰基丙烯酰胺; 将3-氨基-2-氰基丙烯酰胺与磷酰氯在乙腈，丁腈，甲苯或二甲苯中，任选在催化剂存在下合并，得到4-氨基-3-喹啉腈，并公开了制备7-氨基 - 噻吩并[ 3,2-b]吡啶-6-甲腈，其包括将3-氨基噻吩与氰基乙酰胺组合并在醇溶剂中试验草酸甲酯，得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯和乙腈，丁腈，甲苯或二甲苯组合，任选在催化剂存在下，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈和还公开了一种制备4氨基-3-喹啉腈的方法，包括：将胺化合物与氰基乙酸和肽偶联剂混合以获得悬浮液; 过滤悬浮液; 得到氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺与醇溶剂缩合，得到4-氨基-3-喹啉腈，本发明公开了一种获得氰基乙酰胺的方法。

6. 发明申请

WO2005019201A2 PROCESS FOR THE PREPARATION OF 4-AMINO-3-QUINOLINECARBONITRILES 审中-公开
标题翻译：制备4-氨基-3-喹啉碳纳米管的方法
公开(公告)号：WO2005019201A2
公开(公告)日：2005-03-03
申请号：PCT/US2004/026329
申请日：2004-08-13
申请人： WYETH HOLDINGS CORPORATION , WIGGINS SUTHERLAND, Karen , FEIGELSON, Gregg, Brian , BOSCHELLI, Diane, Harris , BLUM, David, Michael , STRONG, Henry, Lee
发明人： WIGGINS SUTHERLAND, Karen , FEIGELSON, Gregg, Brian , BOSCHELLI, Diane, Harris , BLUM, David, Michael , STRONG, Henry, Lee
IPC分类号： C07D401/00
CPC分类号： C07D405/04 , C07D215/54 , C07D495/04
摘要： This invention discloses a process for the preparation of a 4-amino-3quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up-to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield an 2-amino-2-cyanoacrylamide; combining the 3-amino2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine6-carbonitrile comprising combining a 3-amino thiophene with a cyanoacetamide and trial kylorthoformate in an alcoholic solvent to obtain a 3-amino2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4 amino-3-quinolinecarbonitrile comprising: combining an amine compound with cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension; to yield cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline with an alcoholic solvent to yield a 4-amino-3-quinolinecarbonitrile, and the invention discloses a process for obtaining a cyanoacetamide.
摘要翻译：本发明公开了一种制备4-氨基-3-喹啉甲腈的方法，该方法包括将胺化合物与氰基乙酸和酸催化剂合并以得到氰基乙酰胺; 使氰基乙酰胺与任选地最多四取代的苯胺在醇溶剂和原甲酸三烷基酯中缩合，得到2-氨基-2-氰基丙烯酰胺; 将3-氨基-2-氰基丙烯酰胺与三氯氧磷在乙腈，丁腈，甲苯或二甲苯中合并，任选在催化剂存在下反应生成4-氨基-3-喹啉甲腈，并且还公开了制备7-氨基 - 噻吩并[ 包括将3-氨基噻吩与氰基乙酰胺和试验原甲酸酯在醇溶剂中混合以获得3-氨基-2-氰基丙烯酰胺; 并任选在催化剂存在下将3-氨基-2-氰基丙烯酰胺与三氯氧化磷和乙腈，丁腈，甲苯或二甲苯合并，得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈，和还公开了一种制备4-氨基-3-喹啉腈的方法，包括：将胺化合物与氰基乙酸和肽偶联剂组合以获得悬浮液; 过滤悬浮液; 生成氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺与醇溶剂缩合，得到4-氨基-3-喹啉腈，本发明公开了一种获得氰基乙酰胺的方法。

7. 发明申请

WO2004104006A2 PROCESS FOR SYNTHESIZING β-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：WO2004104006A2
公开(公告)日：2004-12-02
申请号：PCT/US2004/014834
申请日：2004-05-12
申请人： WYETH HOLDINGS CORPORATION , WINKLEY, Michael, William , CHAN, Anita Wai-Yin , JIRKOVSKY, Ivo, L. , KREMER, Kenneth, Alfred, Martin , ZELDIS, Joseph , NIKITENKO, Antonina, Aristotelevna , 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, Aristotelevna , STRONG, Henry, Lee , MANSOUR, Tarek, Suhayl , KHAFIZOVA, Gulnaz , VENKATESAN, Aranapakam, Mudumbai
IPC分类号： C07D487/00
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 β-lactamase inhibitors.
摘要翻译：提供了制备具有结构式I的双环杂芳基羧醛的方法，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。

8. 发明申请

WO2007146072A2 PROCESS FOR SYNTHESIZING PIPERAZINE-PIPERIDINE COMPOUNDS 审中-公开
标题翻译：合成哌嗪 - 哌啶化合物的方法
公开(公告)号：WO2007146072A2
公开(公告)日：2007-12-21
申请号：PCT/US2007013433
申请日：2007-06-07
申请人： WYETH CORP , LIU WEIGUO , DRAGAN VLADIMIR , STRONG HENRY LEE , WU YANZHONG , WEN ZHIXIN , LIANG JESSICA KANGPING , DURUTLIC HARIS , SUTHERLAND KAREN WIGGINS , PILCHER ANTHONY SCOTT
发明人： LIU WEIGUO , DRAGAN VLADIMIR , STRONG HENRY LEE , WU YANZHONG , WEN ZHIXIN , LIANG JESSICA KANGPING , DURUTLIC HARIS , SUTHERLAND KAREN WIGGINS , PILCHER ANTHONY SCOTT
IPC分类号： C07D215/40 , C07D401/14 , C07D405/14
CPC分类号： C07D401/14 , C07D215/40
摘要： The present invention relates to processes for synthesizing piperazine-piperidine compounds, and compounds useful as 5-HT 1A binding agents, particularly as 5-HT 1A receptor antagonists and agonists. The processes also allow for safer and environmentally tolerant production of these useful compounds.
摘要翻译：本发明涉及用于合成哌嗪 - 哌啶化合物的方法和用作5-HT 1A结合剂的化合物，特别是作为5-HT 1A受体拮抗剂和激动剂。这些方法还允许这些有用化合物的更安全和环境耐受的生产。

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