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1. 发明申请

WO2012077853A1 PROCESS FOR PREPARING CASPOFUNGIN AND NOVEL INTERMEDIATES THEREOF 审中-公开
标题翻译：制备CASPOFUNGIN及其新型中间体的方法
公开(公告)号：WO2012077853A1
公开(公告)日：2012-06-14
申请号：PCT/KR2011/000196
申请日：2011-01-12
申请人： CKD BIO CORP. , KANG, Heui-Il , HAM, Yun-Beom , KYONG, Su-Hyun , KANG, Heung-Mo , HAN, Tae-Hee , KANG, Doo-Jin
发明人： KANG, Heui-Il , HAM, Yun-Beom , KYONG, Su-Hyun , KANG, Heung-Mo , HAN, Tae-Hee , KANG, Doo-Jin
IPC分类号： C07D487/14 , C07C211/10
CPC分类号： C07K7/56 , C07D487/14
摘要： The present invention relates to a novel process for preparing the aza cyclohexapeptide compound 1-[(4R,5S)-5-[(2-aminoethyl)amino]-N 2 -(10,12-dimethyl-1-oxotetradecyl)-4-hydroxy-L-ornithine]-5-[(3R)-3-hydroxy-L-ornithine]-pneumocandin B 0 (caspofungin), which can improve the problem due to a pungent odor and toxicity during the process and can prepare caspofungin as a final product at high yield compared to conventional processes, and to novel intermediates which are used in the preparation process.
摘要翻译：本发明涉及一种制备氮杂环己肽化合物1 - [（4R，5S）-5 - [（2-氨基乙基）氨基] -N2-（10,12-二甲基-1-氧代十四烷基）-4- 羟基-L-鸟氨酸] -5 - [（3R）-3-羟基-L-鸟氨酸]肺炎球菌素B0（卡泊芬净），其可以改善由于在该过程中刺激性气味和毒性引起的问题，并且可以制备卡泊芬净最终产品与常规方法相比具有高产率，以及用于制备过程中的新型中间体。

2. 发明申请

WO2009116729A2 METHOD FOR REFINING OF HIGH PURITY OF TACROLIMUS 审中-公开
标题翻译：用于精制TACROLIMUS高纯度的方法
公开(公告)号：WO2009116729A2
公开(公告)日：2009-09-24
申请号：PCT/KR2009/000905
申请日：2009-02-25
申请人： CHONGKUNDANG BIO CORPORATION , CHOI, Byoung-Taek , HAM, Yun-Beom , YU, Seong-Seon , JEONG, Kyung-Il , KIM, Byung-Sik
发明人： CHOI, Byoung-Taek , HAM, Yun-Beom , YU, Seong-Seon , JEONG, Kyung-Il , KIM, Byung-Sik
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。

3. 发明申请

WO1996012031A1 PROCESS FOR PREPARING CYCLOSPORIN A 审中-公开
标题翻译：制备环磷酰胺A的方法
公开(公告)号：WO1996012031A1
公开(公告)日：1996-04-25
申请号：PCT/KR1995000095
申请日：1995-07-31
申请人： CHONG KUN DANG CORP. , KIM, Jung, Woo , CHOI, Nam, Hee , LEE, Sang, Chul , CHOI, Gang, Sun , HAM, Yun, Beom , LEE, Don, Wha , MIN, Kyeong, Bok
发明人： CHONG KUN DANG CORP.
IPC分类号： C12P21/04
CPC分类号： C07K7/645
摘要： According to the present invention, a process for the preparation of cyclosporin A comprising the steps of adding lower alkanol solvent to a culture fluid of a mutant of Tolypocladium inflatum and extracting the mixture; transferring the extract to a halogenated lower hydrocarbon solvent; if required, the resultant solution being treated with activated charcoal; and the solution being column chromatographed on silica gel is provided. The process of the present invention is advantageous from the aspect of process economics and environmental protection because the culture fluid is directly extracted without filtration, drying procedure is omitted and the chromatography process is simplified to a single process using silica gel.
摘要翻译：根据本发明，一种制备环孢菌素A的方法，包括以下步骤：将低级链烷醇溶剂加入到嗜淋巴球菌突变体的培养液中并提取混合物; 将提取物转移到卤代低级烃溶剂中; 如果需要，所得溶液用活性炭处理; 并提供在硅胶上进行柱色谱分离的溶液。本发明的方法从工艺经济性和环保性方面是有利的，因为培养液直接在不过滤的情况下被提取，干燥过程被省略，并且色谱法简化为使用硅胶的单一方法。

4. 发明申请

WO2009116729A4 METHOD FOR REFINING OF HIGH PURITY OF TACROLIMUS 审中-公开
标题翻译：用于精制TACROLIMUS高纯度的方法
公开(公告)号：WO2009116729A4
公开(公告)日：2010-01-14
申请号：PCT/KR2009000905
申请日：2009-02-25
申请人： CHONGKUNDANG BIO CORP , CHOI BYOUNG-TAEK , HAM YUN-BEOM , YU SEONG-SEON , JEONG KYUNG-IL , KIM BYUNG-SIK
发明人： CHOI BYOUNG-TAEK , HAM YUN-BEOM , YU SEONG-SEON , JEONG KYUNG-IL , KIM BYUNG-SIK
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。

5. 发明申请

WO2009116729A3 METHOD FOR REFINING OF HIGH PURITY OF TACROLIMUS 审中-公开
标题翻译：精制牙龈卟啉单胞菌的方法
公开(公告)号：WO2009116729A3
公开(公告)日：2009-11-26
申请号：PCT/KR2009000905
申请日：2009-02-25
申请人： CHONGKUNDANG BIO CORP , CHOI BYOUNG-TAEK , HAM YUN-BEOM , YU SEONG-SEON , JEONG KYUNG-IL , KIM BYUNG-SIK
发明人： CHOI BYOUNG-TAEK , HAM YUN-BEOM , YU SEONG-SEON , JEONG KYUNG-IL , KIM BYUNG-SIK
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，并且特别涉及制备高纯度他克莫司的方法，其包括预纯化方法，所述方法包括步骤（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，通过吸附树脂中的溶液并在减压下浓缩洗脱液，然后结晶，可以获得高纯度的他克莫司。根据本发明的方法，可以通过简单的方法并以相对低的成本制备适合于药物目的的纯的他克莫司。

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