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1. 发明申请

WO2006027789A1 PROCESS FOR PRODUCING 11-[4-[2-(2-HYDROXYETHOXY)ETHYL]-1-PIPERAZINYL]DIBENZO[b,f][1,4]THIAZEPINE AND A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
标题翻译：制备11- [4- [2-（2-羟基乙氧基）乙基] -1-哌嗪基]二苯并[b，f] [1,4]噻吩及其药物可接受的盐的方法
公开(公告)号：WO2006027789A1
公开(公告)日：2006-03-16
申请号：PCT/IN2004/000281
申请日：2004-09-08
申请人： JUBILANT ORGANOSYS LIMITED , PATHAK, Shailendra , SHARMA, Jitendra , KAUSHIK, Geetesh , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
发明人： PATHAK, Shailendra , SHARMA, Jitendra , KAUSHIK, Geetesh , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
IPC分类号： C07D281/02
CPC分类号： C07D281/16
摘要： A process for producing 11-[4-[2-(2-hydroxyethoxy)ethyl]-l-piperazinyl]dibenzo [b,f][1,4]thiazepine [I] and a pharmaceutically suitable acid addition salt is disclosed. Accordingly, thiosalicylic acid [XVI] is reacted with o-halonitrobenzene [XVII] using a phase transfer catalyst to obtain 2-nitro-2'-carboxydiphenylsulphide [XI]. It is hydrogenated in the presence of a noble metal catalyst to obtain 2-amino-2' carboxydiphenyl sulphide [X]. The 2-amino-2'-carboxydiphenylsulphide [X] is reacted with halide or oxyhalide of the phosphorous to obtain in situ iminohalide [VI], which further reacts as such with 1-hydroxyethoxyethylpiperazine or condenses with piperazine to obtain 11-piperazinyldi.benzo[b,f][1,4]thiazepine [XIX] which further reacts with 2- chloroethoxyethanol or reacts with 1-(2-hydroxyethyl)piperazine to give 11-[4-(2-hydroxyethyl)piperazine-1-yl]dibenzo[b,f][ 1,4]thiazepine [XXXI] which further converts to an intermediate 11-[4-(2-substitutedethyl)piperazin-1- yl)dibenzo[b,f][1,4]thiazepine wherein the substituent at the 2-position is selected from mesyloxy or tosyloxy or halo group [XXXII] followed by reaction with ethylene glycol to give quetiapine [1].
摘要翻译：公开了制备11- [4- [2-（2-羟基乙氧基）乙基] -1-哌嗪基]二苯并[b，f] [1,4]硫氮杂] [I]和药学上合适的酸加成盐的方法。因此，使用相转移催化剂将硫代水杨酸[XVI]与邻硝基苯[XVII]反应，得到2-硝基-2'-羧基二苯基硫化物[XI]。在贵金属催化剂存在下氢化得到2-氨基-2'-羧基二苯基硫醚[X]。将2-氨基-2'-羧基二苯基硫化物[X]与磷的卤化物或卤氧化物反应，得到原位亚氨基卤[VI]，其进一步与1-羟基乙氧基乙基哌嗪反应或与哌嗪缩合，得到11-哌嗪基二苯并 [b，f] [1,4]硫氮杂[XIX]，其进一步与2-氯乙氧基乙醇反应或与1-（2-羟乙基）哌嗪反应，得到11- [4-（2-羟乙基）哌嗪-1-基] 二苯并[b，f] [1,4]硫氮杂[XXXI]，其进一步转化为中间体11- [4-（2-取代乙基）哌嗪-1-基）二苯并[b，f] [1,4] 2位上的取代基选自甲磺酰氧基或甲苯磺酰氧基或卤代基[ⅩⅩⅫ]，随后与乙二醇反应得到喹硫平[1]。

2. 发明申请

WO2006067795A2 NOVEL POLYMORPHIC FORMS OF ATORVASTATIN LACTONE AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：异烟肼的新型多形态及其制备方法
公开(公告)号：WO2006067795A2
公开(公告)日：2006-06-29
申请号：PCT/IN2004/000401
申请日：2004-12-23
申请人： JUBILANT ORGANOSYS LIMITED , BHATRAJU, Sreenivas, Rao , DUA, Annu , KAUSHIK, Geetesh , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
发明人： BHATRAJU, Sreenivas, Rao , DUA, Annu , KAUSHIK, Geetesh , THAPER, Rajesh, Kumar , DUBEY, Sushil, Kumar
IPC分类号： A61K31/401
CPC分类号： C07D405/06
摘要： The present invention provides novel crystalline polymorphic Forms and amorphous Form of atorvastatin lactone, characterized by powder X-ray diffraction pattern and Infrared absorption spectrum. The novel processes for their preparation are also disclosed.
摘要翻译：本发明提供了阿托伐他汀内酯的新型结晶多晶型和无定形形式，其特征在于粉末X射线衍射图和红外吸收光谱。还公开了其制备的新方法。

3. 发明申请

WO2007105225A1 PROCESS FOR PRODUCING PURE AND STABLE FORM 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-噻吩并[2,3-b] [1,5]苯并咪唑的纯度和稳定形式的方法
公开(公告)号：WO2007105225A1
公开(公告)日：2007-09-20
申请号：PCT/IN2006/000091
申请日：2006-03-14
申请人： JUBILANT ORGANOSYS LIMITED , PANCHASARA, Dinesh , GUPTA, Poorvi , KAUSHIK, Geetesh , DUBEY, Sushil, Kumar
发明人： PANCHASARA, Dinesh , GUPTA, Poorvi , KAUSHIK, Geetesh , DUBEY, Sushil, Kumar
IPC分类号： C07D243/00
CPC分类号： C07D495/04
摘要： Disclosed is an improved process for producing pure and thermally color stable crystalline Form I of 2-methyl-4-(4-methyl-l-piperazinyl)-10H-thieno[2,3-b][l,5] benzodiazepine and product thereof. The process comprises of reacting 2-(2- aminoanilino)-5-methylthiophene-3-carbonitrile with N-methyl piperazine in conjunction with N-methylpiperazine acid salt, to produce 2-methyl-4-(4-methyl-l- piperazinyl)-10H-thieno[2,3-b][l,5] benzodiazepine. Also disclosed is a process for obtaining the Polymorphic Form I of 2-methyl-4-(4-methyl-l-piperazinyl)-10H- thieno[2,3-b][l ,5J benzodiazepine by crystallizing the crude 2-methyl-4-(4-methyl-l- piperazinyl)-10H-thieno [2,3-b][l ,5] benzodiazepine in a mixture of solvents. Further the invention also provides a new polymorph of Olanzapine, dihydrate Form Ji and process for its preparation and a new hydrate Form J 2 of Olanzapine having moisture content 1 -3% and process for its preparation.
摘要翻译：公开了一种改进的2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和产物的纯色和热色稳定晶型I的方法它们。该方法包括使2-（2-氨基苯胺基）-5-甲基噻吩-3-腈与N-甲基哌嗪与N-甲基哌嗪酸盐一起反应，得到2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂卓。还公开了通过将粗2-甲基-4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂的粗品2- -4-（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂在溶剂混合物中。此外，本发明还提供了奥氮平，二水合物形式及其制备方法的新型多晶型物，以及水分含量为1-3％的奥氮平的新型水合物形式2＆lt; 2＆gt;及其制备方法。

4. 发明公开

EP1994013A1 PROCESS FOR PRODUCING PURE AND STABLE FORM OF 2-METHYL-4-(4- METHYL- 1 -PIPERAZINYL)-10H-THIENO[2,3-b] [1,5]BENZODIAZEPINE 审中-公开
标题翻译：方法生产2-甲基-4-（4-甲基-1-哌嗪基）的纯和稳定的形式-10H-噻吩并[2,3-B] [1,5]苯并二氮杂
公开(公告)号：EP1994013A1
公开(公告)日：2008-11-26
申请号：EP06728410.9
申请日：2006-03-14
申请人： Jubilant Organosys Limited
发明人： PANCHASARA, Dinesh , GUPTA, Poorvi , KAUSHIK, Geetesh , DUBEY, Sushil Kumar
IPC分类号： C07D243/00
CPC分类号： C07D495/04
摘要： Disclosed is an improved process for producing pure and thermally color stable crystalline Form I of 2-methyl-4-(4-methyl-l-piperazinyl)-10H-thieno[2,3-b][l,5] benzodiazepine and product thereof. The process comprises of reacting 2-(2- aminoanilino)-5-methylthiophene-3-carbonitrile with N-methyl piperazine in conjunction with N-methylpiperazine acid salt, to produce 2-methyl-4-(4-methyl-l- piperazinyl)-10H-thieno[2,3-b][l,5] benzodiazepine. Also disclosed is a process for obtaining the Polymorphic Form I of 2-methyl-4-(4-methyl-l-piperazinyl)-10H- thieno[2,3-b][l ,5J benzodiazepine by crystallizing the crude 2-methyl-4-(4-methyl-l- piperazinyl)-10H-thieno [2,3-b][l ,5] benzodiazepine in a mixture of solvents. Further the invention also provides a new polymorph of Olanzapine, dihydrate Form Ji and process for its preparation and a new hydrate Form J2 of Olanzapine having moisture content 1 -3% and process for its preparation.

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