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1. 发明申请

WO2003055438A2 CRYSTALLINE FORM I OF 2-METHYL-4-(4-METHYL-1-PIPERAZINYL) 10H THIENO [2,3-B][1,5]BENZODIAZEPINE 审中-公开
标题翻译： 2-甲基-4-（4-甲基-1-哌嗪基）10H三苯并[2,3-B] [1,5]苯并咪唑的晶体形式
公开(公告)号：WO2003055438A2
公开(公告)日：2003-07-10
申请号：PCT/IN2002/000241
申请日：2002-12-23
申请人： SUN PHARMACEUTICAL INDUSTRIES LIMITED , CHHABADA, Vijay, Chhangamal , RAJEEV, Rehani, Budhdev , THENNATI, Rajamannar
发明人： CHHABADA, Vijay, Chhangamal , RAJEEV, Rehani, Budhdev , THENNATI, Rajamannar
IPC分类号： A61K
CPC分类号： C07D495/04
摘要： Crystalline Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine characterised by x-ray powder diffraction peaks at approximately 9.94, 8.53, 8.19, 6.86, 6.35, 5.47, 4.83, 4.71, 4.53, 4.22, 4.08, 3.82, 3.75, 3.69, 3.50, 3.34, 3.11, 2.94, 2.82, 2.76, 2.59, 2.34, 2.03, 1.92 d (interplanar spacing) values; infrared absorbance bands at approximately 1456, 1365, 905, 757, 662 & 604 cm-1 and having stable colour at ambient conditions of storage; and the process of its preparation comprising at least two repetitive steps of crystallization from one or more organic solvent by dissolving 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine in said solvent and allowing crystallization to occur; wherein in at least one step the solution is purified by treating with a solid adsorbent material and filtering; and wherein in the last step the crystalline material is subjected to drying.
摘要翻译： 2-甲基-4-（4-甲基-1-哌嗪基）-10,11-噻吩并[2,3-b] [1,5]苯并二氮杂的结晶形式I，其特征在于X-射线粉末衍射峰在约9.94,8.53， 8.19,6.86,6.35,5.47,4.83,4.71,4.53,4.22,2.08,3.82,3.75,3.89,3.75,3.43,3.96,3.50,3.43,3.92,3.09,3.28,2.36,2.59,2.48,2.03,1.92d（晶面间距）值; 在大约... 1456,1365,905,757,662和604cm-1处的红外吸收带，并且在环境储存条件下具有稳定的颜色; 并且其制备方法包括通过将2-甲基-4-（4-甲基-1-哌嗪基）-1H-噻吩并[2,3-b] [1（R））溶解在至少两个重复步骤中从一种或多种有机溶剂中结晶出来，5]苯并二氮杂在所述溶剂中并允许结晶发生; 其中在至少一个步骤中，所述溶液通过用固体吸附剂材料处理和过滤进行纯化; 并且其中在最后步骤中使晶体材料干燥。

2. 发明申请

US20050070593A1 Novel process for the preparation of trans-3-ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl cyclohexyl) amino]carbonyl] amino]sulfonyl] phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide 失效
标题翻译：制备反式-3-乙基-2,5-二氢-4-甲基-N- [2- [4 - [[[[（4-甲基环己基）氨基]羰基]氨基]磺酰基]苯基] 乙基] -2-氧代-1H-吡咯-1-甲酰胺
公开(公告)号：US20050070593A1
公开(公告)日：2005-03-31
申请号：US10501743
申请日：2003-01-06
申请人： Rohit Soni , Thennati Rajamannar , Rajeev Rehani
发明人： Rohit Soni , Thennati Rajamannar , Rajeev Rehani
IPC分类号： C07D207/38 , A61K31/4015 , C07D207/28
CPC分类号： C07D207/38
摘要： The present invention provides a novel process for preparation of trans-3-ethyl 2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide via the novel intermediate compounds of formula 3.
摘要翻译：本发明提供了制备反式-3-乙基2,5-二氢-4-甲基-N- [2- [4 - [[[（4-甲基环己基）氨基]羰基]氨基]磺酰基的新方法。 ]苯基]乙基] -2-氧代-1H-吡咯-1-甲酰胺，通过式3的新型中间体化合物。

3. 发明申请

US20070191616A1 Process for preparation of an antidepressant compound 失效
标题翻译：制备抗抑郁药的方法
公开(公告)号：US20070191616A1
公开(公告)日：2007-08-16
申请号：US11659230
申请日：2005-08-05
申请人： Kartik Patel , Nischal Patel , Rajeev Rehani , Rajamannar Thennati
发明人： Kartik Patel , Nischal Patel , Rajeev Rehani , Rajamannar Thennati
IPC分类号： C07D333/22
CPC分类号： C07D333/20
摘要： The present invention provides optically pure (S)-(+)-N-methyl-3-(1-naphthaleneoxy)-3-(2-thienyl)propanamine, a compound of formula (I), and optically pure (S)-isomer of compound of formula 4, wherein R1 and R2 both are methyl or R1 is methyl and R2 is benzyl or substituted benzyl group and process for preparation thereof. Formula (I) and (IV). In another aspect the present invention provides a process for preparation of an acid addition salt of compound of formula (I).
摘要翻译：本发明提供光学纯的（S） - （+） - N-甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺，式（I）的化合物和光学纯的（S） - 式4化合物的异构体，其中R 1和R 2两者都是甲基或R 1是甲基，R 2是氢， SUP>是苄基或取代的苄基及其制备方法。式（I）和（IV）。另一方面，本发明提供了制备式（I）化合物的酸加成盐的方法。

4. 发明申请

US20060270858A1 A PROCESS FOR PREPARATION OF 1-[9H-CARBAZOL-4-YLOXY]-3-[{2-(2-(METHOXY)PHENOXY)-ETHYL}-AMINO]-PROPAN-2-OL 失效
标题翻译：制备1- [9H-环己基-4-甲氧基] -3 - [{2-（2-（甲氧基）苯氧基） - 乙基} - 氨基]丙-2-醇的方法
公开(公告)号：US20060270858A1
公开(公告)日：2006-11-30
申请号：US10553957
申请日：2004-03-04
申请人： Vijay Chhabada , Rajeev Rehani , Rajamannar Thennati
发明人： Vijay Chhabada , Rajeev Rehani , Rajamannar Thennati
IPC分类号： C07D209/82
CPC分类号： C07D405/12 , C07D209/88
摘要： The present invention provides a process for preparation of 1-[9H-carbazol-4-yloxy]-3-[{2-(2-(methoxy)phenoxy)-ethyl}-amino]-propan-2-ol, a compound of formula 1 in racemic form or in the form of optically active R or S enantiomer or its pharmaceutically acceptable salt, comprising, reacting 4-(oxiranylmethoxy)-9H-carbazole, a compound of formula (2) or the R or S enantiomer thereof with a compound of formula (5), wherein R1 is benzyl or substituted benzyl group, in an aprotic organic solvent in presence of a catalyst to obtain a compound of formula (6), or the R or S enantiomer thereof, wherein R1 is as defined above. The resultant compound of formula (6) is subjected to debenzylation reaction by catalytic hydrogenation to obtain the compound of formula (1), if desired converting the resultant compound of formula (1) to a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了制备1- [9H-咔唑-4-基氧基] -3 - [{2-（2-（甲氧基）苯氧基） - 乙基} - 氨基] - 丙-2-醇的方法，包括使4-（环氧乙烷基甲氧基）-9H-咔唑，式（2）的化合物或其R或S对映异构体与式（2）的化合物反应，或者以旋光形式的R或S对映体或其药学上可接受的盐的形式，与式（5）化合物反应，其中R 1是苄基或取代的苄基，在非质子有机溶剂中，在催化剂存在下，得到式（6）的化合物，或R或 S对映异构体，其中R 1'如上所定义。所得到的式（6）化合物通过催化氢化进行脱苄基化反应，得到式（1）化合物，如果需要将所得式（1）化合物转化为其药学上可接受的盐。

5. 发明申请

WO03055438A3 CRYSTALLINE FORM I OF 2-METHYL-4-(4-METHYL-1-PIPERAZINYL) 10H THIENO [2,3-B][1,5]BENZODIAZEPINE 审中-公开
标题翻译： 2-甲基-4-（4-甲基-1-哌嗪基）10H三苯并[2,3-B] [1,5]苯并咪唑的晶体形式
公开(公告)号：WO03055438A3
公开(公告)日：2003-08-14
申请号：PCT/IN0200241
申请日：2002-12-23
申请人： SUN PHARMACEUTICAL IND LTD , CHHABADA VIJAY CHHANGAMAL , RAJEEV REHANI BUDHDEV , THENNATI RAJAMANNAR
发明人： CHHABADA VIJAY CHHANGAMAL , RAJEEV REHANI BUDHDEV , THENNATI RAJAMANNAR
IPC分类号： A61K31/551 , A61P25/18 , C07D495/04 , A61K31/55
CPC分类号： C07D495/04
摘要： A novel crystalline form of a known substance cannot be characterized in a sufficient clear and concise manner - distinguishing it form prior art compounds - by a vague property ("having a stable colour upon storage at ambient conditions") or by the giving of infrared absorbance bands alone. Only the characterisation by certain x-ray powder diffraction peaks seems to be sufficient (and a combination of such peaks with IR absorbance bands). For this reason, claims 1 and 3 (and claims 22-23 as far as they refer to claim 1 or 3) are not searchable. Further, the characterization of a novel product by its preparation process (see product-by-process claims 4-21) is not allowable, because such a characterization is only allowable in cases where no other possibility of characterizing a product is possible (which is not the case for the new compound of the present application).
摘要翻译：已知物质的新型结晶形式不能以足够清楚和简明的方式表征 - 通过模糊性质（“在环境条件下储存时具有稳定的颜色”）或通过提供红外吸光度来区分其形成现有技术化合物乐队单独。只有某些X射线粉末衍射峰的表征似乎是足够的（以及这些峰与IR吸收带的组合）。因此，权利要求1和3（和权利要求22-23至于它们涉及权利要求1或3）是不可搜索的。此外，通过其制备方法（参见产品方法权利要求4-21）对新产品的表征是不允许的，因为只有在没有其他可能性表征产品的情况下才允许这样的表征（其是不是本申请的新化合物的情况）。

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