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1. 发明申请

US20060111438A1 Asymmetric synthesis of substituted dihydrobenzofurans 审中-公开
标题翻译：取代的二氢苯并呋喃的不对称合成
公开(公告)号：US20060111438A1
公开(公告)日：2006-05-25
申请号：US11255645
申请日：2005-10-21
申请人： Alexander Gontcharov , Gulnaz Khafizova , John Potoski , Qing Yu , Chia-Cheng Shaw , Gary Stack , Dahui Zhou
发明人： Alexander Gontcharov , Gulnaz Khafizova , John Potoski , Qing Yu , Chia-Cheng Shaw , Gary Stack , Dahui Zhou
IPC分类号： A61K31/343 , C07D307/87 , C07F3/02
CPC分类号： C07D209/48 , C07D303/22 , C07D307/79 , C07D307/81 , C07D405/04
摘要： The present invention concerns production of a compound of the formula or a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula: where Ar, Y, R1, Ry, R2, and m are as defined herein.
摘要翻译：本发明涉及通过使下式化合物环化的方法生产下式化合物或其药学上可接受的盐：其中Ar，Y，R 1，R 2， y，R 2，和m如本文所定义。

2. 发明申请

US20080039639A1 Chromane and chromene derivatives and uses thereof 审中-公开
标题翻译：色原和色烯衍生物及其用途
公开(公告)号：US20080039639A1
公开(公告)日：2008-02-14
申请号：US11787860
申请日：2007-04-18
申请人： Alexander Gontcharov , Antonia Nikitenko , Panolil Raveendranath , Chia-Cheng Shaw , Bogdan Wilk , Dahui Zhou
发明人： Alexander Gontcharov , Antonia Nikitenko , Panolil Raveendranath , Chia-Cheng Shaw , Bogdan Wilk , Dahui Zhou
IPC分类号： C07D311/04
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 R1, R2, R3, R4, 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， SUP，4，x，m，n和Ar如上所定义，并且在本文的类别和亚类中描述，它们是脑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。

3. 发明授权

US07384953B2 Purification of rapamycin 失效
标题翻译：雷帕霉素的纯化
公开(公告)号：US07384953B2
公开(公告)日：2008-06-10
申请号：US11359294
申请日：2006-02-22
申请人： Chia-Cheng Shaw , Warren Chew , Bogdan Kazimierz Wilk
发明人： Chia-Cheng Shaw , Warren Chew , Bogdan Kazimierz Wilk
IPC分类号： C07D498/18 , A61K31/435
CPC分类号： C07D498/18
摘要： Purified rapamycin and a chemical process for obtaining the purified rapamycin are described.
摘要翻译：描述了纯化的雷帕霉素和用于获得纯化的雷帕霉素的化学方法。

4. 发明申请

US20060199253A1 Recovery of CCI-779 from mother liquors 失效
标题翻译：从母液中回收CCI-779
公开(公告)号：US20060199253A1
公开(公告)日：2006-09-07
申请号：US11359842
申请日：2006-02-22
申请人： Chia-Cheng Shaw , Warren Chew , Bogdan Wilk , Genevieve Fortier
发明人： Chia-Cheng Shaw , Warren Chew , Bogdan Wilk , Genevieve Fortier
IPC分类号： C07D491/14 , C12P17/00
CPC分类号： C07D498/18 , C12P17/188
摘要： The invention provides a process for recovering CCI-779 from mother liquors.
摘要翻译：本发明提供了从母液中回收CCI-779的方法。

5. 发明授权

US06277983B1 Regioselective synthesis of rapamycin derivatives 失效
公开(公告)号：US06277983B1
公开(公告)日：2001-08-21
申请号：US09670358
申请日：2000-09-27
申请人： Chia-Cheng Shaw , John Sellstedt , Razzak Noureldin , Gloria K. Cheal , Genevieve Fortier
发明人： Chia-Cheng Shaw , John Sellstedt , Razzak Noureldin , Gloria K. Cheal , Genevieve Fortier
IPC分类号： C07D49114
CPC分类号： C07F7/1892
摘要： This invention provides a regioselective process for preparing a 42-ester or ether of rapamycin, and 31-silyl ether intermediates.

6. 发明申请

US20050234086A1 Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779 失效
标题翻译：脯氨酸CCI-779，其生产和用途，以及脯氨酸CCI-779和CCI-779的两步酶合成
公开(公告)号：US20050234086A1
公开(公告)日：2005-10-20
申请号：US11103779
申请日：2005-04-12
申请人： Jianxin Gu , Mark Ruppen , Panolil Raveendranath , Warren Chew , Chia-Cheng Shaw
发明人： Jianxin Gu , Mark Ruppen , Panolil Raveendranath , Warren Chew , Chia-Cheng Shaw
IPC分类号： A61K31/4745 , C07D281/18 , C07D491/04 , C07D498/08 , C07D498/18 , C07F7/18
CPC分类号： C07D498/08
摘要： Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.
摘要翻译：描述了合成CCI-779和脯氨酸-CCI-779的方法，包括在有机溶剂中使用2,2-双（羟甲基）丙酸的乙烯基酯将雷帕霉素的42-羟基脂肪酶催化的乙酰化的方法然后脱保护。还提供含有脯氨酸CCI-779的产品及其用途。

7. 发明授权

US4172078A Thiazolineazetidinone derivatives 失效
标题翻译：噻唑啉氮杂环丁酮衍生物
公开(公告)号：US4172078A
公开(公告)日：1979-10-23
申请号：US860857
申请日：1977-12-15
申请人： Ronald G. Micetich , Chia-Cheng Shaw , Peter K. Wolfert
发明人： Ronald G. Micetich , Chia-Cheng Shaw , Peter K. Wolfert
IPC分类号： C07D513/04 , C07D277/08
CPC分类号： C07D513/04 , Y02P20/55
摘要： Thiazolineazetidinone derivatives of the formulae 1,2, and 3. ##STR1## wherein R is derived from the commonly known carboxamido groups present in penicillins, R.sup.1 is a carboxy protecting group commonly used in penicillin chemistry, and R.sup.2 is Cl, Br, I, CN, lower alkoxy, lower acyloxy, SCN, SCH.sub.3, S-phenyl, S-heteroaryl such as 5-mercaptotetrazole or 2-mercapto-5-methyl-1,3,4-thiadiazole, NO.sub.3, N.sub.3, NH-phenyl, and N(CH.sub.3).sub.2 with the proviso that R.sup.2 in the compounds of formula 1 is limited to Cl, Br, I, and lower acyloxy, and a process for preparing said compounds from 2-(substituted methyl) penicillin sulfoxides followed by treatment with a base.The compounds of formulae 1,2, and 3 are useful as intermediates in the synthesis of cephalosporins.
摘要翻译：式1,2和3的噻唑啉氮杂环丁酮衍生物。其中R衍生自青霉素中常见的羧酰胺基，R1是青霉素化学通常使用的羧基保护基，R2是Cl，Br ，I，CN，低级烷氧基，低级酰氧基，SCN，SCH3，S-苯基，S-杂芳基如5-巯基四唑或2-巯基-5-甲基-1,3,4-噻二唑，NO 3，N 3，NH- 苯基和N（CH 3）2，条件是式1化合物中的R 2限于Cl，Br，I和低级酰氧基，以及由2-（取代的甲基）青霉素亚砜制备所述化合物的方法，用基地治疗。

8. 发明授权

US07498327B2 Indolylalkylamine metabolites as 5-hydroxytryptamine-6 ligands 失效
标题翻译：吲哚烷基胺代谢物作为5-羟色胺-6配体
公开(公告)号：US07498327B2
公开(公告)日：2009-03-03
申请号：US11158702
申请日：2005-06-22
申请人： Youchu Wang , Chia-Cheng Shaw , Ronald Charles Bernotas , Chung-Chiee Paul Wang , Ping Cai , Zhi Wang
发明人： Youchu Wang , Chia-Cheng Shaw , Ronald Charles Bernotas , Chung-Chiee Paul Wang , Ping Cai , Zhi Wang
IPC分类号： C07D513/04 , C07D209/08 , C07D471/04 , A61K31/4162 , A61P25/18
CPC分类号： C07D513/04 , C07H7/033 , C07H15/26
摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
摘要翻译：本发明提供式I化合物及其用于治疗与5-HT 6受体有关或受其影响的病症的用途。

9. 发明申请

US20070281932A1 Method of preparing 4-halogenated quinoline intermediates 审中-公开
标题翻译：制备4-卤代喹啉中间体的方法
公开(公告)号：US20070281932A1
公开(公告)日：2007-12-06
申请号：US11802430
申请日：2007-05-23
申请人： Caroline Bernier , Chia-Cheng Shaw
发明人： Caroline Bernier , Chia-Cheng Shaw
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/47 , C07D413/02 , C07D403/02
CPC分类号： C07D215/56 , C07D401/12
摘要： This invention is directed to methods of preparing compounds of formula (I): comprising the step of reacting a compound of formula (II): with a reagent of formula POX3 and silica gel at a temperature greater than about 75° C., and wherein substitutions at X, PG, A, G, R1 and R4 are set forth in the specification.
摘要翻译：本发明涉及制备式（I）化合物的方法：包括使式（II）化合物与式POX 3 3的试剂和硅胶在大于约75℃，并且其中X，PG，A，G，R 1和R 4上的取代在说明书中阐述。

10. 发明授权

US4391975A Process for 1-oxacephem derivatives 失效
标题翻译： 1-羟基乙酸酯衍生物的方法
公开(公告)号：US4391975A
公开(公告)日：1983-07-05
申请号：US356236
申请日：1982-03-08
申请人： Saul Wolfe , Chia-Cheng Shaw
发明人： Saul Wolfe , Chia-Cheng Shaw
IPC分类号： C07D205/085 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/14 , C07D505/00 , C07F7/18 , C07D498/04
CPC分类号： C07D403/04 , C07D205/085 , C07D403/12 , C07D405/04 , C07D405/14 , C07D505/00 , C07F7/186 , Y02P20/55
摘要： A process for preparing compounds of the formula ##STR1## in which R is hydrogen or methoxy,R.sub.1 is a hydroxyl group,R.sub.2 is chlorine, bromine, OAc or SHET,R.sub.3 is hydrogen or a cleavable carboxy-protecting group preferably selected from loweralkyl, benzyl, benzhydryl, loweralkoxyloweralkyl, loweralkoxybenzyl, phenacyl, trimethylsilyl, 2,2,2-trichloroethyl or pivaloloxy,R.sub.4 is hydrogen or a cleavable amino-protecting acyl group, or R.sub.4 NH represents phthalimido, andHET is a five or six membered aromatic heterocycle containing 1-4 heteroatoms and optionally substituted with loweralkyl,and from which the corresponding 1-oxacephem derivatives can be prepared is described. The novel intermediate compounds of the formula 1 are produced from a penicillin derivative of formula 1 wherein R, R.sub.3 and R.sub.4 are as above described and R.sub.1 and R.sub.2 are both the same halogen, by treatment with a formylating agent in a halogenated hydrocarbon solvent to obtain the corresponding compound in which R.sub.1 and R.sub.2 are both OCHO which is then treated with less than one molar equivalent of a boron halide to obtain a 2:1 to 4:1 mixture of the corresponding compounds of formula 1 in which R.sub.1 is OCHO and R.sub.2 is the corresponding halogen or R.sub.1 is halogen and R.sub.2 is OCHO, and in which the former compound predominates. This mixture is separated and the compound in which R.sub.1 is OCHO and R.sub.2 is halogen is isolated. This last compound is hydrolyzed and the desired intermediate compound in which R.sub.1 is OH and R.sub.2 is a halogen is isolated. Alternatively, the compound of formula 1 in which R.sub.1 is OCHO and R.sub.2 is halogen is subjected to displacement by .sup.- OAc or HSHET prior to the hydrolysis.
摘要翻译：其中R为氢或甲氧基，R1为羟基，R2为氯，溴，OAc或SHET，R3为氢或可裂解的羧基保护基，优选选自低级烷基，苄基，二苯甲基，低级烷氧基低级烷基，低级烷氧基苄基，苯甲酰甲基，三甲基甲硅烷基，2,2,2-三氯乙基或新戊酰氧基，R4为氢或可裂解氨基保护酰基，或R4NH为苯二酰亚氨基，HET为五或六元芳族杂环含有1-4个杂原子并且任选被低级烷基取代，并且可以从其中制备相应的1-羟基乙酸酯衍生物。式1的新型中间体化合物由式1的青霉素衍生物制备，其中R，R 3和R 4如上所述，并且R 1和R 2都是相同的卤素，通过在卤代烃溶剂中用甲酰化剂处理得到其中R1和R2都是OCHO的相应化合物，然后用少于1摩尔当量的卤化硼处理，得到相应的式1化合物的2:1至4:1的混合物，其中R 1是OCHO和R 2 是相应的卤素，或者R1是卤素，R2是OCHO，其中前者是主要的。分离该混合物，分离其中R 1为OCHO且R 2为卤素的化合物。将最后一种化合物水解，并且分离出其中R 1为OH且R 2为卤素的所需中间体化合物。或者，其中R 1为OCHO且R 2为卤素的式1化合物在水解之前通过-OAc或HSHET置换。

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