公开(公告)号：US08362238B2

公开(公告)日：2013-01-29

申请号：US12921820

申请日：2009-02-25

申请人： Byoung-Taek Choi ,  Yun-Beom Ham ,  Seong-Seon Yu ,  Kyung-Il Jeong ,  Byung-Sik Kim

发明人： Byoung-Taek Choi ,  Yun-Beom Ham ,  Seong-Seon Yu ,  Kyung-Il Jeong ,  Byung-Sik Kim

IPC分类号： C07D413/00

CPC分类号： C07D498/18

摘要： The present invention relates to a process of preparing a highly pure tacrolimus, which comprising a pre-purification process carried out by means of crystallization, and particularly to a process of preparing a highly pure tacrolimus, which comprises a pre-purification process comprising the steps of (a) extracting mycelia cake collected by filtering a tacrolimus-containing oily compound with an organic solvent, (b) concentrating the extract under reduced pressure and (c) crystallizing the concentrate. In addition, a highly pure tacrolimus can be obtained by dissolving the pre-purified crystals in an organic solvent, passing through the solution in an adsorption resin and concentrating the eluate under reduced pressure, followed by crystallization. According to a process of the present invention, Tacrolimus as pure as appropriate for a pharmaceutical purpose can be prepared by a simple process and at a relatively low cost.

摘要翻译： 本发明涉及一种制备高纯度他克莫司的方法，其包括通过结晶进行的预纯化方法，特别涉及一种制备高纯度他克莫司的方法，其包括预纯化方法，其包括步骤 （a）通过用有机溶剂过滤含有他克莫司的油性化合物而收集的菌丝体饼，（b）在减压下浓缩提取物和（c）使浓缩物结晶。 此外，通过将预纯化的晶体溶解在有机溶剂中，通过溶液吸附树脂并减压浓缩洗脱液，然后结晶，可以获得高纯度他克莫司。 根据本发明的方法，可以通过简单的方法并以相对较低的成本制备适合于药物目的的纯粹的他克莫司。

公开(公告)号：US20100298560A1

公开(公告)日：2010-11-25

申请号：US12863569

申请日：2009-01-08

申请人： Byoung Taek Choi ,  Yun Bum Ham ,  Yong Kyu Park ,  Sung Hun Bang ,  Jin Woong Kim ,  Seung Uk Lee ,  Hyun Jun Jung

发明人： Byoung Taek Choi ,  Yun Bum Ham ,  Yong Kyu Park ,  Sung Hun Bang ,  Jin Woong Kim ,  Seung Uk Lee ,  Hyun Jun Jung

IPC分类号： C07D413/12 ,  C07D307/88

CPC分类号： C07D307/88

摘要： The present invention relates to an improved method of manufacturing mycophenolate mofetil. More particularly, the present invention relates to a method of manufacturing mycophenolate mofetil with high purity comprising : a) converting mycophenolate to an amine salt by reacting with an amine base; and b) reacting the resultant with a halogenating agent and 2-morpholinoethanol continuously.

摘要翻译： 本发明涉及一种制造霉酚酸酯的改进方法。 更具体地说，本发明涉及一种制备高纯度霉酚酸酯的方法，包括：a）通过与胺基反应将霉酚酸酯转化成胺盐; 和b）将所得物与卤化剂和2-吗啉代乙醇连续反应。

公开(公告)号：US06426202B1

公开(公告)日：2002-07-30

申请号：US09869440

申请日：2001-06-26

申请人： Chung-II Hong ,  Kyung-Hwan Kim ,  Byoung-Taek Choi ,  Jang Woo Park ,  Nak Kyu Sung ,  Byoung Kook Kim

发明人： Chung-II Hong ,  Kyung-Hwan Kim ,  Byoung-Taek Choi ,  Jang Woo Park ,  Nak Kyu Sung ,  Byoung Kook Kim

IPC分类号： C12P742

CPC分类号： C12R1/66 ,  C12N1/14 ,  C12P7/42 ,  Y10S435/913

摘要： A nystatin-resistant mutant microorganism belonging to Aspegillus genus is provided for preparing triol heptanoic acid, a precursor of 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor. A mutant Aspergillus terreus CLS247-13, KCTC 0673 BP is prepared by treating Aspergillus terreus CLS216-7, KCTC 0359 BP with ultraviolet ray or chemical mutagens. The mutant provides high productivity (at least 11.5 g/L, 95/6% of the total product) of triol heptanoic acid, while reducing (less than 0.53 g/L, 4.4% of total product) productivity of triol heptanoic acid analogues. Since the nystatin-resistant mutant strain CLS347-13 has a capability of producing triol heptanioc acid with a high yield in a short period of culture time compared with known triol heptanoic acid producing strains, it can be widely used in industrial applications.

摘要翻译： 提供了属于Aspegillus属的制霉菌素抗性突变体微生物，用于制备3-羟基-3-甲基戊二酰辅酶A还原酶抑制剂的前体三醇庚酸。 通过用紫外线或化学诱变剂处理土曲霉CLS216-7，KCTC 0359 BP制备突变体土曲霉CLS247-13，KCTC 0673 BP。 该突变体提供三醇庚酸的高生产率（至少11.5g / L，总产物的95/6％），同时减少（小于0.53g / L，总产物的4.4％）三醇庚酸类似物的生产率。 由于与已知的三醇庚酸生产菌株相比，制霉菌素抗性突变株CLS347-13具有在短的培养时间内以高产率生产三醇庚酸的能力，因此可广泛用于工业应用中。

公开(公告)号：US20120065393A1

公开(公告)日：2012-03-15

申请号：US12921820

申请日：2009-02-25

申请人： Byoung-Taek Choi ,  Yun-Beom Ham ,  Seong-Seon Yu ,  Kyung-II Jeong ,  Byung-Sik Kim

发明人： Byoung-Taek Choi ,  Yun-Beom Ham ,  Seong-Seon Yu ,  Kyung-II Jeong ,  Byung-Sik Kim

IPC分类号： C07D498/12

CPC分类号： C07D498/18

摘要： The present invention relates to a process of preparing a highly pure tacrolimus, which comprising a pre-purification process carried out by means of crystallization, and particularly to a process of preparing a highly pure tacrolimus, which comprises a pre-purification process comprising the steps of (a) extracting mycelia cake collected by filtering a tacrolimus-containing oily compound with an organic solvent, (b) concentrating the extract under reduced pressure and (c) crystallizing the concentrate. In addition, a highly pure tacrolimus can be obtained by dissolving the pre-purified crystals in an organic solvent, passing through the solution in an adsorption resin and concentrating the eluate under reduced pressure, followed by crystallization. According to a process of the present invention, Tacrolimus as pure as appropriate for a pharmaceutical purpose can be prepared by a simple process and at a relatively low cost.

摘要翻译： 本发明涉及一种制备高纯度他克莫司的方法，其包括通过结晶进行的预纯化方法，特别涉及一种制备高纯度他克莫司的方法，其包括预纯化方法，其包括步骤 （a）通过用有机溶剂过滤含有他克莫司的油性化合物而收集的菌丝体饼，（b）在减压下浓缩提取物和（c）使浓缩物结晶。 此外，通过将预纯化的晶体溶解在有机溶剂中，通过溶液吸附树脂并减压浓缩洗脱液，然后结晶，可以获得高纯度他克莫司。 根据本发明的方法，可以通过简单的方法并以相对较低的成本制备适合于药物目的的纯粹的他克莫司。

公开(公告)号：US07405267B2

公开(公告)日：2008-07-29

申请号：US10621353

申请日：2003-07-18

申请人： Tae-Won Kang ,  Byoung-Taek Choi ,  Gang-Sun Choi ,  Yong-Rack Choi ,  Sung-Ho Hwang

发明人： Tae-Won Kang ,  Byoung-Taek Choi ,  Gang-Sun Choi ,  Yong-Rack Choi ,  Sung-Ho Hwang

IPC分类号： C07K1/14 ,  C07K1/18 ,  C07K1/20 ,  C07K1/22 ,  C12P19/28 ,  C07K5/12 ,  C07K5/02

CPC分类号： C07K9/008

摘要： Disclosed is a method for purifying teicoplanin A2 comprising: (i) a primary pre-purification step of purifying a filtrate of fermentation broth of a strain using a synthetic adsorbent; (ii) a secondary pre-purification step of purifying the primary pre-purification solution using a cation exchange resin having a high cross-linkage, a catalytic resin or a chelate resin; (iii) a final purification step of purifying the secondary pre-purification solution using a reversed phase resin; and (iv) a powder-forming step. According to the present invention, it is possible to obtain teicoplanin A2 with a higher purity through a relatively simple process without using an excessive amount of an organic solvent.

摘要翻译： 公开了一种纯化泰可菌素A 2 O 2的方法，其包括：（i）使用合成吸附剂纯化菌株发酵液的滤液的初级预纯化步骤; （ii）使用具有高交联键的阳离子交换树脂，催化树脂或螯合树脂来纯化所述初级预纯化溶液的二次预纯化步骤; （iii）使用反相树脂纯化二次预纯化溶液的最终纯化步骤; 和（iv）粉末形成步骤。 根据本发明，可以通过相对简单的方法获得具有较高纯度的替考拉宁A 2 N 2，而不使用过量的有机溶剂。