-
公开(公告)号：US07799907B2
公开(公告)日：2010-09-21
申请号：US11573869
申请日：2005-12-29
申请人： Jaeheon Lee , Gha Seung Park , Moonsub Lee , Hyo-Jeong Bang , Jae Chul Lee , Cheol Kyong Kim , Chang-Ju Choi , Han Kyong Kim , Hoe Chul Lee , Young-Kil Chang , Gwan Sun Lee
发明人： Jaeheon Lee , Gha Seung Park , Moonsub Lee , Hyo-Jeong Bang , Jae Chul Lee , Cheol Kyong Kim , Chang-Ju Choi , Han Kyong Kim , Hoe Chul Lee , Young-Kil Chang , Gwan Sun Lee
IPC分类号： C07H19/073
摘要： Provided is an improved method for stereoselectively preparing 2′-deoxy-2′,2′-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formula (IV) in a solvent to obtain a nucleo side of formula (II) with removal of a silyl halide ((alkyl)3SiX (X=halide)); and deprotecting the nucleoside of formula (II) to obtain 2′-deoxy-2′,2′-difluorocytidine of formula (I). 2′-Deoxy-2′,2′-difluorocytidine of formula (I) is effective for treating various cancers such as non-small cell lung (NSCLC), pancreatic, bladder, breast or ovarian cancers.
摘要翻译： 提供了一种用于立体选择性制备式（I）的2'-脱氧-2'，2'-二氟胞苷的改进方法，其包括使1-卤代呋喃核糖化合物与式（IV）的核碱基在溶剂中反应以获得核 除去甲硅烷基卤化物（（烷基）3 SiX（X =卤化物））的式（II）侧。 并使式（II）的核苷脱保护，得到式（I）的2'-脱氧-2'，2'-二氟胞苷。 式（I）的2'-脱氧-2'，2'-二氟胞苷对于治疗各种癌症如非小细胞肺（NSCLC），胰腺，膀胱，乳腺或卵巢癌是有效的。
-
公开(公告)号：US20070249818A1
公开(公告)日：2007-10-25
申请号：US11573869
申请日：2003-12-29
申请人： Jaeheon Lee , Gha Seung Park , Moonsub Lee , Hyo-Jeong Bang , Jae Lee , Cheol Kim , Chang-Ju Choi , Han Kyong Kim , Hoe Chul Lee , Young-Kil Chang , Gwan Lee
发明人： Jaeheon Lee , Gha Seung Park , Moonsub Lee , Hyo-Jeong Bang , Jae Lee , Cheol Kim , Chang-Ju Choi , Han Kyong Kim , Hoe Chul Lee , Young-Kil Chang , Gwan Lee
IPC分类号： C07H19/00
摘要： This invention relates to an improved method for stereoselectively preparing 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I).
摘要翻译： 本发明涉及一种用于立体选择性制备式（I）的2'-二脱氧-2¢¥，2¢-二氟胞苷的改进方法，其包括以下步骤：使式（III）的1-卤代呋喃核糖化合物与 （IV）的核碱基在溶剂中得到式（II）的核苷，同时除去反应中产生的式（Ⅴ）的甲硅烷基卤化物; 并使式（II）的核苷脱保护，得到式（I）的2¢¥脱氧-2¢¥，2¢¥ - 二氟胞苷。
-
3.发明授权1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivatives and process for the preparation thereof 失效1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物及其制备方法公开(公告)号：US07858761B2
公开(公告)日：2010-12-28
申请号：US11572790
申请日：2005-06-21
申请人： Jaeheon Lee , Gha-Seung Park , Moonsub Lee , Han Kyong Kim , Hyo-Jeong Bang , Young-Kil Chang , Gwan Sun Lee
发明人： Jaeheon Lee , Gha-Seung Park , Moonsub Lee , Han Kyong Kim , Hyo-Jeong Bang , Young-Kil Chang , Gwan Sun Lee
CPC分类号： C07H3/08
摘要： 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.
摘要翻译： 具有用联苯基羰基保护的3-羟基的式（I）的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物是可以通过简单的方法容易地纯化的固体，例如 重结晶，因此可以有利地用作大量制备吉西他滨的中间体。 此外，式（I）的1-α-卤代-2,2-二氟-2-脱氧-D-呋喃核糖衍生物可以使用式（V）化合物作为中间体以高立体选择性制备。
-
4.发明授权Method for the preparation of D-erythro-2,2-difluoro-2-deoxy-1-oxoribose derivative 失效D-赤式-2,2-二氟-2-脱氧-1-氧代糖配合物的制备方法公开(公告)号：US07638642B2
公开(公告)日：2009-12-29
申请号：US11572404
申请日：2005-06-23
申请人： Jaeheon Lee , Gha-Seung Park , Moonsub Lee , Cheol-Kyong Kim , Jae-Chul Lee , Young-Kil Chang , Gwan-Sun Lee
发明人： Jaeheon Lee , Gha-Seung Park , Moonsub Lee , Cheol-Kyong Kim , Jae-Chul Lee , Young-Kil Chang , Gwan-Sun Lee
IPC分类号： C07D307/02
CPC分类号： C07H3/08
摘要： 3R-carboxylate enantiomer derivative of formula (III) can be prepared easily and selectively by the method of the present invention, and a highly pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose derivative can be prepared efficiently from the compound of formula (III) as an intermediate.
摘要翻译： 可以通过本发明的方法容易地和选择性地制备式（III）的3R-羧酸酯对映异构体衍生物，并且可以有效地制备高纯度的D-赤式-2,2-二氟-2-脱氧-1-氧代果糖衍生物 由作为中间体的式（III）化合物制备。
-
5.发明申请Method for the Preparation of D-Erythro-2,2-Difluoro-2-Deoxy-1-Oxoribose Derivative 失效D-赤型-2,2-二氟-2-脱氧-1-氧代糖衍生物的制备方法公开(公告)号：US20080058509A1
公开(公告)日：2008-03-06
申请号：US11572404
申请日：2005-06-23
申请人： Jaeheon Lee , Gha-Seung Park , Moonsub Lee , Cheol-Kyong Kim , Jae-Chul Lee , Young-Kil Chang , Gwan-Sun Lee
发明人： Jaeheon Lee , Gha-Seung Park , Moonsub Lee , Cheol-Kyong Kim , Jae-Chul Lee , Young-Kil Chang , Gwan-Sun Lee
IPC分类号： C07H19/00 , C07D317/14
CPC分类号： C07H3/08
摘要： 3R-carboxylate enantiomer derivative of formula (III) can be prepared easily and selectively by the method of the present invention, and a highly pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose derivative can be prepared efficiently from the compound of formula (III) as an intermediate.
摘要翻译： 可以通过本发明的方法容易地和选择性地制备式（III）的3R-羧酸酯对映异构体衍生物，并且可以有效地制备高纯度的D-赤式-2,2-二氟-2-脱氧-1-氧代果糖衍生物 由作为中间体的式（III）化合物制备。
-
6.发明申请(S)-(-)-Amlodipine Camsylate or Hydrate Thereof And Pharmaceutical Composition Comprising Same 审中-公开（S） - （ - ） - 氨氯地平卡姆磺酸盐或其水合物及其组成的药物组合物公开(公告)号：US20090326234A1
公开(公告)日：2009-12-31
申请号：US12374087
申请日：2007-07-16
申请人： Jaeheon Lee , Moon Sub Lee , Weon Ki Yang , Jaeho Yoo , Jae-Chul Lee , Chang-Ju Choi , Han Kyong Kim , Young-Kil Chang , Gwansun Lee
发明人： Jaeheon Lee , Moon Sub Lee , Weon Ki Yang , Jaeho Yoo , Jae-Chul Lee , Chang-Ju Choi , Han Kyong Kim , Young-Kil Chang , Gwansun Lee
IPC分类号： C07D213/80
CPC分类号： C07D211/90
摘要： Disclosed is (S)-(−)-amlodipine camsylate or a hydrate thereof having good photostability and high solubility, and a pharmaceutical composition comprising same, which can be efficiently used in treating cardiovascular diseases.
摘要翻译： 公开了具有良好的光稳定性和高溶解度的（S） - （ - ） - 氨磺酸樟脑磺酸盐或其水合物，以及包含该组合物的药物组合物，其可有效地用于治疗心血管疾病。
-
7.发明授权Pharmaceutical composition comprising crystalline sibutramine methanesulfonate hemihydrate 失效包含结晶西布曲明甲磺酸盐半水合物的药物组合物公开(公告)号：US06900245B2
公开(公告)日：2005-05-31
申请号：US10678325
申请日：2003-10-03
申请人： Jae-Heon Lee , Gha-Seung Park , Jae-Cheol Lee , Han-Kyong Kim , Young-Kil Chang , Gwan-Sun Lee
发明人： Jae-Heon Lee , Gha-Seung Park , Jae-Cheol Lee , Han-Kyong Kim , Young-Kil Chang , Gwan-Sun Lee
IPC分类号： A61K31/13 , A61K31/205
CPC分类号： A61K31/205 , C30B7/00
摘要： The present invention relates to a pharmaceutical composition for treating or preventing obesity, comprising novel crystalline sibutramine methanesulfonate hemihydrate of formula (I). The crystalline sibutramine methanesulfonate hemihydrate according to the present invention has a much higher solubility in water, and enhanced stability under a high humidity/temperature condition, as compared with sibutramine hydrochloride monohydrate
摘要翻译： 本发明涉及用于治疗或预防肥胖症的药物组合物，其包含式（I）的新型结晶西布曲明甲磺酸盐半水合物。 与西布曲明盐酸盐一水合物相比，本发明的结晶西布曲明甲磺酸盐半水合物在水中的溶解度高，并且在高湿度/温度条件下提高了稳定性
-
公开(公告)号：US08569490B2
公开(公告)日：2013-10-29
申请号：US13140640
申请日：2009-12-24
申请人： Jaeheon Lee , Gha-Seung Park , Jin Hee Kim , Ji Eun Lee , Chul Hyun Park , Tae Jin Choi , Eun-Ju Park , Cheol Kyung Kim , Eun Jung Lim , Young-Kil Chang , Gwan Sun Lee
发明人： Jaeheon Lee , Gha-Seung Park , Jin Hee Kim , Ji Eun Lee , Chul Hyun Park , Tae Jin Choi , Eun-Ju Park , Cheol Kyung Kim , Eun Jung Lim , Young-Kil Chang , Gwan Sun Lee
IPC分类号： C07D473/18 , C07F7/08 , C07C49/517
CPC分类号： C07D473/18
摘要： The present invention relates to a novel, high-yield and low-cost method for preparing entecavir, [1-S-(1α,3α,4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one, an antiviral agent, and novel intermediates used therein.
摘要翻译： 本发明涉及一种制备恩替卡韦[1-S-（1α，3α，4α）] -2-氨基-1,9-二氢-9- [4-羟基 -3-（羟甲基）-2-亚甲基环戊基] -6H-嘌呤-6-酮，抗病毒剂及其中使用的新型中间体。
-
9.发明申请公开(公告)号：US20110251387A1
公开(公告)日：2011-10-13
申请号：US13140640
申请日：2009-12-24
申请人： Jaeheon Lee , Gha-Seung Park , Jin Hee Kim , Ji Eun Lee , Chul Hyun Park , Tae Jin Choi , Eun-Ju Park , Cheol Kyung Kim , Eun Jung Lim , Young-Kil Chang , Gwan Sun Lee
发明人： Jaeheon Lee , Gha-Seung Park , Jin Hee Kim , Ji Eun Lee , Chul Hyun Park , Tae Jin Choi , Eun-Ju Park , Cheol Kyung Kim , Eun Jung Lim , Young-Kil Chang , Gwan Sun Lee
IPC分类号： C07D473/18 , C07F7/08 , C07C49/517
CPC分类号： C07D473/18
摘要： The present invention relates to a novel, high-yield and low-cost method for preparing entecavir, [1-S-(1α,3α,4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one, an antiviral agent, and novel intermediates used therein.
摘要翻译： 本发明涉及一种制备恩替卡韦[1-S-（1α，3α，4α] b] -2-氨基-1,9-二氢-9- [4- 羟基-3-（羟甲基）-2-亚甲基环戊基] -6H-嘌呤-6-酮，抗病毒剂及其中使用的新型中间体。
-
10.发明授权Methods for preparing capecitabine and beta-anomer-rich trialkyl carbonate compound used therein 失效制备用于其中的卡培他滨和β-异头物富含三烷基碳酸酯化合物的方法公开(公告)号：US08097706B2
公开(公告)日：2012-01-17
申请号：US12742367
申请日：2008-11-07
申请人： Jaeheon Lee , Gha-Seung Park , Weon Ki Yang , Jin Hee Kim , Cheol Hyun Park , Yong-Hoon An , Yoon Ju Lee , Young-Kil Chang , Gwan Sun Lee
发明人： Jaeheon Lee , Gha-Seung Park , Weon Ki Yang , Jin Hee Kim , Cheol Hyun Park , Yong-Hoon An , Yoon Ju Lee , Young-Kil Chang , Gwan Sun Lee
CPC分类号： C07D405/04 , C07H1/00 , C07H19/06 , Y02P20/55
摘要： The present invention relates to a method for preparing capecitabine and a method for preparing a β-anomer-rich trialkyl carbonate compound used therein, and a highly pure capecitabine can be efficiently prepared with a high yield by the method of the present invention using the β-anomer-rich trialkyl carbonate compound as an intermediate.
摘要翻译： 本发明涉及一种制备卡培他滨的方法和一种制备其中使用的富含甘油的三烷基碳酸酯化合物的方法，可以通过本发明的方法以高产率有效地制备高纯度的卡培他滨 富马酸三烷基碳酸酯化合物作为中间体。
-
-
-
-
-
-
-
-
-
搜索结果
34 条记录 (耗时 0.052 秒)
