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1. 发明授权

US5763653A Key intermediates in the manufacture of simvastatin 失效
标题翻译：辛伐他汀制造中的关键中间体
公开(公告)号：US5763653A
公开(公告)日：1998-06-09
申请号：US816574
申请日：1997-03-13
申请人： Jag Mohan Khanna , Yatendra Kumar , Rajesh Kumar Thaper , Satyananda Misra , S. M. Dileep Kumar
发明人： Jag Mohan Khanna , Yatendra Kumar , Rajesh Kumar Thaper , Satyananda Misra , S. M. Dileep Kumar
IPC分类号： C07C231/00 , C07C235/30 , C07D309/30 , C07C67/02
CPC分类号： C07C235/30 , C07D309/30 , C07C2101/02 , C07C2102/28
摘要： A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.
摘要翻译：以盐形式从洛伐他汀或甲维林酸制备辛伐他汀的方法包括用环丙基或丁胺处理起始原料，当洛伐他汀为原料时，吡喃酮环由此开放，向2-甲基丁酸酯侧链加入甲基，然后关闭开放的吡喃酮环以产生辛伐他汀。在不保护和去保护开放式吡喃酮环的两个羟基的情况下进行该方法。在优选的实施方案中，用环丙胺处理起始物质，其通过新的中间体洛伐他汀环丙基酰胺产生辛伐他汀。

2. 发明授权

US06528660B1 Process for the production of amorphous atorvastatin calcium 有权
公开(公告)号：US06528660B1
公开(公告)日：2003-03-04
申请号：US09979475
申请日：2002-02-12
申请人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar
发明人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar
IPC分类号： C07D207327
CPC分类号： C07D207/34
摘要： A process for the preparation of amorphous atorvastatin calcium and hydrates thereof which comprises: (a) dissolving crystalline atorvastatin calcium in a non-hydroxylic solvent; (b) adding a non-polar hydrocarbon anti-solvent or adding the dissolved atorvastatin to the non-polar anti-solvent to precipitate out atorvastatin calcium; and (c) removing the solvent by filtration to afford amorphous atorvastatin calcium.

3. 发明授权

US5917058A Process of lactonization in the preparation of statins 失效
标题翻译：内酯化制备他汀类药物的过程
公开(公告)号：US5917058A
公开(公告)日：1999-06-29
申请号：US64285
申请日：1998-04-22
申请人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
发明人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： An improved process of lactonization in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises treating the open ring hydroxy acid form of the statins with an excess of acetic acid and in the absence of a strong acid catalyst under mild heating conditions (e.g., ambient to 55.degree. C.), and adding an anti-solvent to the reaction mixture, thereby causing the statins in lactone form to crystalize from the reaction mixture. The acetic acid serves as both a solvent and a catalyst for the lactonization reaction.
摘要翻译：在制备他汀类药物（例如，HMG-CoA还原酶抑制剂洛伐他汀和辛伐他汀）中改进的内酯化方法采用非常温和的反应条件。改进的方法包括用温和的加热条件（例如，环境温度至55℃）用过量的乙酸处理开环羟基酸形式的他汀类和不存在强酸催化剂的情况下，加入抗溶剂反应混合物，从而使内酯形式的他汀类从反应混合物中结晶。乙酸既用作内酯化反应的溶剂和催化剂。

4. 发明授权

US5939564A Process of lactonization in the preparation of statins 失效
标题翻译：内酯化制备他汀类药物的过程
公开(公告)号：US5939564A
公开(公告)日：1999-08-17
申请号：US055572
申请日：1998-04-06
申请人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
发明人： Yatendra Kumar , Rajesh Kumar Thaper , S. M. Dileep Kumar , Jag Mohan Khanna
IPC分类号： C07D309/30
CPC分类号： C07D309/30
摘要： A novel process of lactonizaton in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises dissolving the open ring hydroxy acid form of the statins in an organic solvent by heating at a temperature, which ranges from ambient to reflux of the solvent, under anhydrous conditions to produce a solution, treating the solution with a mild catalyst at a temperature from about ambient to 50.degree. C., and adding water to the solution to cause the statins in lactone form to crystalize from the reaction mixture. The mild catalyst used in the reaction is a salt of an organic base with an organic or inorganic acid, such as pyridine hydrobromide, pyridine hydrochloride, or pyridinium, p-toluene sulfonate. The organic solvent comprises a lower alkanol, a non-alcoholic polar solvent, or a mixture of the two.
摘要翻译：在制备他汀类药物（例如，HMG-CoA还原酶抑制剂洛伐他汀和辛伐他汀）中的新方法使用非常温和的反应条件。改进的方法包括通过在无水条件下从环境温度至溶剂回流的温度加热，将开环羟基酸形式的他汀类药物溶解在有机溶剂中，以产生溶液，用温和的催化剂处理溶液温度为约环境温度至50℃，并向溶液中加入水，使得内酯形式的他汀类从反应混合物中结晶。反应中使用的温和催化剂是有机碱与有机或无机酸的盐，例如吡啶氢溴酸盐，吡啶盐酸盐或吡啶鎓对甲苯磺酸盐。有机溶剂包括低级链烷醇，非醇极性溶剂或两者的混合物。

5. 发明授权

US5763646A Process for manufacturing simvastatin from lovastatin or mevinolinic acid 失效
标题翻译：从洛伐他汀或甲维林酸生产辛伐他汀的方法
公开(公告)号：US5763646A
公开(公告)日：1998-06-09
申请号：US816573
申请日：1997-03-13
申请人： Yatendra Kumar , Rajesh Kumar Thaper , Satyananda Misra , S. M. Dileep Kumar , Jag Mohan Khanna
发明人： Yatendra Kumar , Rajesh Kumar Thaper , Satyananda Misra , S. M. Dileep Kumar , Jag Mohan Khanna
IPC分类号： C07D309/30 , C07C67/02
CPC分类号： C07D309/30
摘要： A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.
摘要翻译：以盐形式从洛伐他汀或甲维林酸制备辛伐他汀的方法包括用环丙基或丁胺处理起始原料，当洛伐他汀为原料时，吡喃酮环由此开放，向2-甲基丁酸酯侧链加入甲基，然后关闭开放的吡喃酮环以产生辛伐他汀。在不保护和去保护开放式吡喃酮环的两个羟基的情况下进行该方法。在优选的实施方案中，用环丙胺处理起始物质，其通过新的中间体洛伐他汀环丙基酰胺产生辛伐他汀。

6. 发明授权

US06541511B1 Methyl analogs of simvastatin as novel HMG-CoA reductase inhibitors 失效
标题翻译：辛伐他汀的甲基类似物作为新的HMG-CoA还原酶抑制剂
公开(公告)号：US06541511B1
公开(公告)日：2003-04-01
申请号：US10166468
申请日：2002-06-10
申请人： Rajesh Kumar Thaper , Saridi Madhava Dileep Kumar , Yatendra Kumar
发明人： Rajesh Kumar Thaper , Saridi Madhava Dileep Kumar , Yatendra Kumar
IPC分类号： A61K3135
CPC分类号： C07C69/30 , C07C2602/28 , C07D309/30
摘要： The present invention relates to a novel methyl analog of simvastatin, which has the ability to inhibit the synthesis of cholesterol. The compound of the present invention holds promise for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders. The invention also relates to a process for making the novel compound.
摘要翻译：本发明涉及辛伐他汀的新型甲基类似物，其具有抑制胆固醇合成的能力。本发明的化合物具有治疗和预防高胆固醇血症和各种心脏病的希望。本发明还涉及制备该新化合物的方法。

7. 发明授权

US09085556B2 Salts of dexlansoprazole and their preparation 有权
标题翻译：右兰索拉盐及其制备
公开(公告)号：US09085556B2
公开(公告)日：2015-07-21
申请号：US13638310
申请日：2011-03-29
申请人： Anu Mittal , Anmol Kumar Ray , Mahavir Singh Khanna , Rajesh Kumar Thaper , Mohan Prasad
发明人： Anu Mittal , Anmol Kumar Ray , Mahavir Singh Khanna , Rajesh Kumar Thaper , Mohan Prasad
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to the salts of dexlansoprazole in amorphous form. The present invention further relates to processes for the preparation of salts of dexlansoprazole.
摘要翻译：本发明涉及无定形形式的右兰索拉唑盐。本发明还涉及右兰索拉唑盐的制备方法。

8. 发明授权

US08853411B2 Process for the preparation of dexlansoprazole 有权
标题翻译：制备右兰索拉唑的方法
公开(公告)号：US08853411B2
公开(公告)日：2014-10-07
申请号：US13638399
申请日：2011-03-29
申请人： Anu Mittal , Anmol Kumar Ray , Mahavir Singh Khanna , Rajesh Kumar Thaper , Mohan Prasad
发明人： Anu Mittal , Anmol Kumar Ray , Mahavir Singh Khanna , Rajesh Kumar Thaper , Mohan Prasad
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to a process for the preparation of crystalline dexlansoprazole.
摘要翻译：本发明涉及一种制备结晶右兰索拉唑的方法。

9. 发明申请

US20130210865A1 SORAFENIB DIMETHYL SULPHOXIDE SOLVATE 有权
标题翻译： SORAFENIB二甲基硫醚溶剂
公开(公告)号：US20130210865A1
公开(公告)日：2013-08-15
申请号：US13575057
申请日：2011-01-28
申请人： Jagdev Singh Jaryal , Swargam Sathyanarayana , Rajesh Kumar Thaper , Mohan Prasad , Sachin Deorao Zade , Ajay Shankar Sinch
发明人： Jagdev Singh Jaryal , Swargam Sathyanarayana , Rajesh Kumar Thaper , Mohan Prasad , Sachin Deorao Zade , Ajay Shankar Sinch
IPC分类号： C07D213/81 , G01N30/02
CPC分类号： C07D213/81 , G01N30/02
摘要： The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-N2-methylpyridine-2-carboxamide, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of cancer. The present invention also provides a novel HPLC method for the identification, quantification and isolation of related substances of sorafenib.
摘要翻译：本发明提供4-（4- {3- [4-氯-3-（三氟甲基）苯基]脲基}苯氧基）-N2-甲基吡啶-2-甲酰胺的二甲基亚砜溶剂合物，其制备方法，包含它的药物组合物并用于治疗癌症。本发明还提供了用于鉴定，定量和分离索拉非尼相关物质的新型HPLC方法。

10. 发明申请

US20130197232A1 PROCESS FOR THE PREPARATION OF CRYSTALLINE FORMS OF DEXLANSOPRAZOLE 审中-公开
标题翻译：制备DEXLANSOPRAZOLE的晶体形式的方法
公开(公告)号：US20130197232A1
公开(公告)日：2013-08-01
申请号：US13574849
申请日：2011-01-28
申请人： Anmol Kumar Ray , Mahavir Singh Khanna , Rajesh Kumar Thaper , Mohan Prasad
发明人： Anmol Kumar Ray , Mahavir Singh Khanna , Rajesh Kumar Thaper , Mohan Prasad
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to crystalline forms of dexlansoprazole designated as forms A and B, and their preparation. The present invention further relates to processes for the preparation of anhydrous dexlansoprazole and dexlansoprazole sesquihydrate using crystalline Forms A and B of dexlansoprazole.
摘要翻译：本发明涉及称为形式A和B的右兰索拉唑的结晶形式及其制备方法。本发明还涉及使用右兰索拉唑的晶型A和B制备无水右兰索拉唑和右兰索拉唑倍半水合物的方法。

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