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1. 发明申请

US20050165242A1 Process for the preparation of amorphous atorvastatin calcium 审中-公开
标题翻译：制备无定形阿托伐他汀钙的方法
公开(公告)号：US20050165242A1
公开(公告)日：2005-07-28
申请号：US10771383
申请日：2004-02-05
申请人： Daqing Che , Aaron Kinsman , Bhaskar Guntoori , K.S. Murthy
发明人： Daqing Che , Aaron Kinsman , Bhaskar Guntoori , K.S. Murthy
IPC分类号： A61K31/40 , A61P3/06 , C07D207/34 , C07D405/06 , C07D27/333
CPC分类号： C07D207/34 , C07D405/06
摘要： A process for the preparation of amorphous atorvastatin calcium and hydrates thereof, which comprises: (a) hydrolysis of the precursor lactone using sodium hydroxide to form atorvastatin sodium salt solution; (b) addition of the atorvastatin sodium salt solution to a calcium chloride or calcium acetate solution in the absence or presence of seeds of amorphous atorvastatin calcium; and (c) isolation of the resultant amorphous atorvastatin calcium salt by filtration and drying.
摘要翻译：一种制备无定形阿托伐他汀钙及其水合物的方法，其包括：（a）使用氢氧化钠水解前体内酯以形成阿托伐他汀钠盐溶液; （b）在不存在或存在无定形阿托伐他汀钙的种子的情况下将阿托伐他汀钠盐溶液加入到氯化钙或乙酸钙溶液中; 和（c）通过过滤和干燥分离得到的无定形阿托伐他汀钙盐。

2. 发明申请

US20050119493A1 Process for the preparation of amorphous atorvastin calcium salt (2:1) 有权
标题翻译：无定形阿托伐他汀钙盐（2：1）制备方法
公开(公告)号：US20050119493A1
公开(公告)日：2005-06-02
申请号：US10488411
申请日：2001-08-31
申请人： Sanjay Suri , J. Singh , S. Sarin , R. Bansal
发明人： Sanjay Suri , J. Singh , S. Sarin , R. Bansal
IPC分类号： C07D207/34 , C07D207/40 , C07D207/416 , C07D409/06 , C07D27/333
CPC分类号： C07D207/416 , C07D207/34 , C07D405/06 , C07D409/06
摘要： Improved process for the preparation of amorphous atorvastatin calcium salt (2:1) comprises hydrolyzing the lactone form of atorvastatin of formula of FIG. 1 with aqueous alkali or alkaline earth metal base, extracting with organic solvent the reaction mixture and adding the same to an anti-solvent to precipitate the product and finally filtering the product to afford amorphous atorvastatin calcium (2:1). The process also comprises the preparation of amorphous atorvastatin calcium salt (2:1) from its crystalline form.
摘要翻译：用于制备无定形阿托伐他汀钙盐（2:1）的改进方法包括水解式（I）的阿托伐他汀的内酯形式。 1，用碱金属或碱土金属碱处理，用有机溶剂萃取反应混合物，并加入到反溶剂中沉淀产物，最后过滤产物，得到无定形阿托伐他汀钙（2:1）。该方法还包括从其结晶形式制备无定形阿托伐他汀钙盐（2:1）。

3. 发明申请

US20050101787A1 Process for preparing optically active nitro compounds and cyano compounds 失效
标题翻译：光学活性硝基化合物和氰基化合物的制备方法
公开(公告)号：US20050101787A1
公开(公告)日：2005-05-12
申请号：US10934338
申请日：2004-09-03
申请人： Masahito Watanabe , Kunihiko Murata , Takao Ikariya
发明人： Masahito Watanabe , Kunihiko Murata , Takao Ikariya
IPC分类号： C07D317/60 , C07B53/00 , C07B61/00 , C07C201/12 , C07C205/45 , C07C205/53 , C07C253/30 , C07C255/41 , C07D307/54 , C07D333/24 , C07D29/12 , C07D27/333
CPC分类号： B01J31/1805 , B01J31/2295 , B01J2231/348 , B01J2531/821 , B01J2540/34 , C07C253/30 , C07C255/22
摘要： A process for preparing optically active nitro compounds and cyano compounds represented by the chemical formula (C) using a metal complex, which is obtained by reaction of an optically active nitrogen-containing compound and a periodic table group VIII metal complex, in the asymmetric Michael reaction of a compound represented by the chemical formula (A) and a compound represented by the chemical formula (B) according to the claim 1.
摘要翻译：使用通过光学活性含氮化合物和周期表VIII族金属络合物的反应获得的金属络合物来制备由式（C）表示的光学活性硝基化合物和氰基化合物的方法，由化学式（A）表示的化合物与根据权利要求1的化学式（B）表示的化合物的反应。

4. 发明申请

US20030120086A1 New salts of HMG-CoA reductase inhibitors 有权
标题翻译： HMG-CoA还原酶抑制剂的新盐
公开(公告)号：US20030120086A1
公开(公告)日：2003-06-26
申请号：US10320285
申请日：2002-12-16
申请人： Lek Pharmaceuticals d.d.
发明人： Zlatko Pflaum
IPC分类号： C07D39/22 , C07C069/34 , C07C069/52 , C07D27/333
CPC分类号： C07C211/10 , C07C211/07 , C07C211/09 , C07C211/14 , C07C211/35 , C07C2601/14 , C07D309/30
摘要： Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis. The present invention relates to the new amine salts of HMG-CoA reductase inhibitors, the preparation thereof, the preparation of pure HMG-CoA reductase inhibitors via amine salts thereof, use of the amine salts of HMG-CoA reductase inhibitors in the process for semisynthetic preparation of HMG-CoA reductase inhibitors, use of the amine salts of HMG-CoA reductase inhibitors in the process for biotechnological modification of HMG-CoA reductase inhibitors as well as the conversion of the amine salts of HMG-CoA reductase inhibitors into the pharmaceutically acceptable salts of the HMG-CoA reductase inhibitors and the conversion of the amine salts of HMG-CoA reductase inhibitors into the HMG-CoA reductase inhibitors in the lactone form.
摘要翻译：洛伐他汀，普伐他汀，辛伐他汀，美伐他汀，阿托伐他汀及其衍生物和类似物被称为HMG-CoA还原酶抑制剂，并用作抗高胆固醇血症药。它们中的大多数是通过使用被鉴定为曲霉属，红曲霉，诺卡氏菌属，无性系，毛霉属或青霉属的物种的不同物种的微生物进行发酵的，一些是通过使用化学合成方法处理发酵产物而得到的，或者它们是产物的化学合成总量。本发明涉及HMG-CoA还原酶抑制剂的新的胺盐，其制备方法，通过其胺盐制备纯的HMG-CoA还原酶抑制剂，在半合成过程中使用HMG-CoA还原酶抑制剂的胺盐 HMG-CoA还原酶抑制剂的制备，HMG-CoA还原酶抑制剂的胺盐在HMG-CoA还原酶抑制剂的生物技术修饰方法中的用途以及将HMG-CoA还原酶抑制剂的胺盐转化为药学上可接受的 HMG-CoA还原酶抑制剂的盐和将HMG-CoA还原酶抑制剂的胺盐转化成内酯形式的HMG-CoA还原酶抑制剂。

5. 发明申请

US20030109569A1 Preparation of pharmaceutically acceptable atorvastatin salts in non-crystalline form 失效
标题翻译：以非结晶形式制备药学上可接受的阿托伐他汀盐
公开(公告)号：US20030109569A1
公开(公告)日：2003-06-12
申请号：US10323444
申请日：2002-12-18
发明人： Gorazd Sorsak
IPC分类号： A61K031/401 , C07D27/333
CPC分类号： C07D207/34 , Y02P20/55
摘要： Non-crystalline, in particular amorphous, pharmaceutically acceptable atorvastatin salts, especially the calcium salt, are prepared from atorvastatin lactone or from a compound of formula (I) 1 where A denotes a common protecting group or separate protecting groups for the two hydroxy groups, and B denotes a carboxylic acid protecting group, without the need of prior formation of atorvastatin lactone, the crystalline form of the atorvastatin salt, or a mixture of amorphous and crystalline forms of the atorvastatin salt. Pharmaceutical formulations are prepared from these salts.
摘要翻译：非结晶的，特别是无定形的药学上可接受的阿托伐他汀盐，特别是钙盐，由阿托伐他汀内酯或式（I）化合物制备，其中A表示常见保护基或两个羟基的单独保护基， B表示羧酸保护基团，而不需要先前形成阿托伐他汀内酯，阿托伐他汀盐的结晶形式或阿托伐他汀盐的无定形和结晶形式的混合物。药物制剂由这些盐制备。

6. 发明申请

US20030069432A1 NOVEL PROCESS FOR PREPARING 4-SUBSTITUTED-1H-PYRROLE-3-CARBOXYLIC ACID ESTER 失效
标题翻译：制备4-取代的1H-吡咯-3-羧酸酯的新方法
公开(公告)号：US20030069432A1
公开(公告)日：2003-04-10
申请号：US10204579
申请日：2002-08-22
发明人： Hyun Ik Shin , Sung Tak Oh , Jay Hyok Chang , Kyoo Woong Lee
IPC分类号： C07D27/333
CPC分类号： C07D207/34
摘要： The present invention relates to a novel process for preparing pyrrole ester compounds, which are key intermediates in the preparation of farnesyl transferase inhibitors, an anti-cancer agent. Horner-Emmons reaction of aldehyde compounds provides the corresponding null,null-unsaturated esters, which without any separation and/or purification steps, are treated with toluenesulfonylmethylisocyanate in the presence of base to give pyrrole esters in one-pot fashion.
摘要翻译：本发明涉及一种制备吡咯酯化合物的新方法，其是制备法呢基转移酶抑制剂，抗癌剂的关键中间体。醛化合物的霍纳 - 埃蒙斯反应提供了相应的α，β-不饱和酯，其在没有任何分离和/或纯化步骤的情况下，在甲苯存在下用甲苯磺酰基甲基异氰酸酯进行处理，以一锅形式提供吡咯酯。

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