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1. 发明申请

WO2008079266A3 SYNTHESIS OF PYRROLIDINE COMPOUNDS 审中-公开
公开(公告)号：WO2008079266A3
公开(公告)日：2008-07-03
申请号：PCT/US2007/026002
申请日：2007-12-20
申请人： WYETH , ALIMARDANOV, Asaf Ragim , KRISHNAN, Lalitha , ZHOU, Maotang , WANG, Ting-zhong , REN, Jianxin , CONSIDINE, John Leo , WU, Charles C. , BRAZZILLO, Jason , RAVEENDRANATH, Panolil , SUTHERLAND, Karen Wiggins , MIRMEHRABI, Mahmoud , DESHMUKH, Subodh S.
发明人： ALIMARDANOV, Asaf Ragim , KRISHNAN, Lalitha , ZHOU, Maotang , WANG, Ting-zhong , REN, Jianxin , CONSIDINE, John Leo , WU, Charles C. , BRAZZILLO, Jason , RAVEENDRANATH, Panolil , SUTHERLAND, Karen Wiggins , MIRMEHRABI, Mahmoud , DESHMUKH, Subodh S.
IPC分类号： C07D207/16 , A61K31/40
摘要： Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S, 4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.

2. 发明申请

WO2005026105A3 PROCESS FOR THE SYNTHESIS OF 3-(3-FLUORO-4-HYDROXYPHENYL)-7-HYDROXYNAPHTHONITRILE 审中-公开
公开(公告)号：WO2005026105A3
公开(公告)日：2005-03-24
申请号：PCT/US2004/028645
申请日：2004-09-02
申请人： WYETH , WU, Yanzhong , REN, Jianxin , GHOSH, Mousumi , LEVENT, Mahmut , SUTHERLAND, Karen, Wiggins , RAVEENDRANATH, Panolil
发明人： WU, Yanzhong , REN, Jianxin , GHOSH, Mousumi , LEVENT, Mahmut , SUTHERLAND, Karen, Wiggins , RAVEENDRANATH, Panolil
IPC分类号： C07C41/30
摘要： A process for making a compound of formula I wherein R 1 , is CN, F or CI; R 2 is H or Br; and R 3 and R 4 are each independently H or F. These compounds are useful in the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.

3. 发明申请

WO2008024492A2 PROCESS FOR PREPARING INDOLINONE PHENYLAMINOPROPANOL DERIVATIVES 审中-公开
标题翻译：制备吲哚啉酮苯基丙氨酸衍生物的方法
公开(公告)号：WO2008024492A2
公开(公告)日：2008-02-28
申请号：PCT/US2007/018782
申请日：2007-08-22
申请人： WYETH , 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 , C07D405/06 , A61K31/4045 , A61P25/00
CPC分类号： C07D209/34
摘要： Processes are disclosed for preparing indolinone phenylaminopropanol derivatives, particularly chiral indolinone phenylaminopropanol derivatives of the general formula (I). The processes disclosed may be used to prepare, inter alia , 7-fluoro-1 - [(1 S, 2R)-1-(3-fluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one and 7-fluoro-1 -[( 1S, 2/R )-1-(3,5-difluorophenyl)-2-hydroxy-3-(methylamino) propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one. Intermediates of the processes are also disclosed.
摘要翻译：公开了制备吲哚啉酮苯基氨基丙醇衍生物，特别是通式（I）的手性吲哚啉酮苯基氨基丙醇衍生物的方法。所公开的方法可以用于制备7-氟-1 - [（1S，2R）-1-（3-氟苯基）-2-羟基-3-（甲基氨基）丙基] 二甲基-1,3-二氢-2H-吲哚-2-酮和7-氟-1 - [（1S，2 / R）-1-（3,5-二氟苯基）-2-羟基-3-（甲基氨基）丙基] -3,3-二甲基-1,3-二氢-2H-吲哚-2-酮。还公开了该方法的中间体。

4. 发明申请

WO2007098030A1 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：WO2007098030A1
公开(公告)日：2007-08-30
申请号：PCT/US2007/004091
申请日：2007-02-15
申请人： WYETH , CHAN, Anita, Wai-Yin , JIANXIN, Ren , GHOSH, Mousumi , RAVEENDRANATH, Panolil
发明人： CHAN, Anita, Wai-Yin , JIANXIN, Ren , 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）。

5. 发明申请

WO2007098029A1 METHODS FOR PREPARING SULFONAMIDE SUBSTITUTED ALCOHOLS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备磺酰胺取代的醇及其中间体的方法
公开(公告)号：WO2007098029A1
公开(公告)日：2007-08-30
申请号：PCT/US2007/004090
申请日：2007-02-15
申请人： WYETH , CHAN, Anita, Wai-Yin , JIANXIN, Ren , GHOSH, Mousumi , RUBEZHOV, Arkadiy , RAVEENDRANATH, Panolil , ZELDIS, Joseph
发明人： CHAN, Anita, Wai-Yin , JIANXIN, Ren , GHOSH, Mousumi , RUBEZHOV, Arkadiy , RAVEENDRANATH, Panolil , ZELDIS, Joseph
IPC分类号： C07C213/00 , C07C215/08 , C07D333/34
CPC分类号： C07C213/00 , C07B2200/07 , C07D333/34 , C07C215/08
摘要： Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.
摘要翻译：提供了制备氨基醇或其盐和磺酰胺取代的醇化合物的方法。理想地，磺酰胺取代的醇化合物是杂环磺酰胺三氟烷基取代的醇化合物或苯基磺酰胺三氟烷基取代的醇化合物。

6. 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。

7. 发明申请

WO2007059421A2 POLYMORPHS OF 5-CYCLOPROPYL-2-(4-FLUOROPHENYL)-6-[(2-HYDROXYETHYL)(METHYLSULFONYL) AMINO]-N-METHYL-1-BENZOFURAN-3-CARBOXAMIDE AND METHODS OF MAKING THE SAME 审中-公开
标题翻译： 5-环丙基-2-（4-氟代苯基）-6 - [（2-羟基乙基）（甲基磺酰基）氨基] -N-甲基-1-苯并呋喃-3-羧酸酰胺的聚合物及其制备方法
公开(公告)号：WO2007059421A2
公开(公告)日：2007-05-24
申请号：PCT/US2006/060750
申请日：2006-11-09
申请人： WYETH , VIROPHARMA INCORPORATED , LIU, Weiguo , WANG, Qiuxia , TONG, Wei , RAVEENDRANATH, Panolil , IERA, Silvio
发明人： LIU, Weiguo , WANG, Qiuxia , TONG, Wei , RAVEENDRANATH, Panolil , IERA, Silvio
IPC分类号： C07D307/84 , A61K31/34 , A61P31/12
CPC分类号： C07D307/84
摘要： Substantially pure polymorphic forms of 5-cycloproρyl-2-(4- fluorophenyl)-6-[(2-hydroxyethyl)(methylsulfonyl)amino]-N-methyl-l- benzofuran-3-carboxamide are produced by recrystallization in an organic solvent.
摘要翻译： 5-环戊基-2-（4-氟苯基）-6 - [（2-羟基乙基）（甲基磺酰基）氨基] -N-甲基-1-苯并呋喃-3-甲酰胺的基本上纯的多晶型物是通过在有机溶剂。

8. 发明申请

WO2006119104A2 PROCESS FOR PREPARING ISATINS WITH CONTROL OF SIDE-PRODUCT FORMATION 审中-公开
标题翻译：控制边产品形成的方法
公开(公告)号：WO2006119104A2
公开(公告)日：2006-11-09
申请号：PCT/US2006/016436
申请日：2006-04-27
申请人： WYETH , WILK, Bogdan, Kazimierz , RAVEENDRANATH, Panolil , DING, Zhixian , WEHRENBERG, Peter
发明人： WILK, Bogdan, Kazimierz , RAVEENDRANATH, Panolil , DING, Zhixian , WEHRENBERG, Peter
IPC分类号： C07D209/38
CPC分类号： C07D209/38 , C07D403/04
摘要： Methods and kits for preventing or minimizing the formation of isatin oximes during formation of an isatin from an isonitrosoacetanilide are provided. Also provided are methods and kits for preventing or minimizing the formation of isatin oxime impurities after formation of an isatin from an isonitrosoacetanilide by using a decoy agent in the quenching and/or extraction steps. The isatins can be prepared using a decoy agent and desirably a strong acid. Further provided are methods for preparing isatin oximes.
摘要翻译：提供了用于防止或最小化来自异硝基乙酰替苯胺的靛红形成期间靛红肟形成的方法和试剂盒。还提供了用于在骤冷和/或萃取步骤中通过使用诱饵剂从异亚氨基乙酰替苯胺形成靛红后，防止或最小化靛红肟杂质形成的方法和试剂盒。异丁锭可以使用诱饵剂和期望的强酸来制备。还提供了制备靛红肟的方法。

9. 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。

10. 发明申请

WO2005058820A1 A SYNTHETIC METHODOLOGY FOR THE REDUCTIVE ALKYLATION AT THE C-3 POSITION OF INDOLES 审中-公开
标题翻译：在C-3位置上减少烷基化的合成方法
公开(公告)号：WO2005058820A1
公开(公告)日：2005-06-30
申请号：PCT/US2004/041989
申请日：2004-12-15
申请人： WYETH , MICHALAK, Ronald, S. , RAVEENDRANATH, Panolil
发明人： MICHALAK, Ronald, S. , RAVEENDRANATH, Panolil
IPC分类号： C07D209/18
CPC分类号： C07D209/22
摘要： A process for the reductive alkylation at the C-3 position of an indole compound in which the indole is treated with an aldehyde in the presence of a Lewis acid and a silicon hydride reducing agent. The process is useful for alkylating the C-3 position of indoles that contain acid-sensitive substituents at the N-1 position.
摘要翻译：在路易斯酸和氢化硅还原剂存在下，用吲哚处理吲哚的吲哚化合物的C-3位还原烷基化方法。该方法可用于在N-1位置烷基化含有酸敏感性取代基的吲哚的C-3位。

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