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1. 发明申请

WO1996032413A1 PROCESS FOR THE PURIFICATION OF GLYCOPROTEINS LIKE ERYTHROPOIETIN 审中-公开
标题翻译：甘氨酸的纯化方法，如红细胞生成素
公开(公告)号：WO1996032413A1
公开(公告)日：1996-10-17
申请号：PCT/EP1996001509
申请日：1996-04-09
申请人： GRUPPO LEPETIT S.P.A. , ZANETTE, Dino , SARUBBI, Edoardo, Giacomo , SOFFIENTINI, Adolfo , RESTELLI, Ermenegildo , GRIGOLETTO, Armando
发明人： GRUPPO LEPETIT S.P.A.
IPC分类号： C07K14/505
CPC分类号： C07K1/22 , A61K38/00 , C07K14/505
摘要： The present invention is directed to a simple and efficient process for the recovery of a biologically active glycoprotein from a biological fluid containing it. It includes a phenyl boronate chromatography step and is particularly suitable for the purification of erythropoietin.
摘要翻译：本发明涉及从含有生物活性糖的生物流体中回收生物活性糖蛋白的简单有效的方法。它包括苯基硼酸盐层析步骤，特别适用于促红细胞生成素的纯化。

2. 发明申请

WO1997040067A1 IMPROVED CHEMICAL PROCESS FOR PREPARING AMIDE DERIVATIVES OF ANTIBIOTIC A 40926 审中-公开
标题翻译：用于制备抗生素A 40926的酰胺衍生物的改进化学方法
公开(公告)号：WO1997040067A1
公开(公告)日：1997-10-30
申请号：PCT/EP1997001874
申请日：1997-04-15
申请人： BIOSEARCH ITALIA S.P.A. , PANZONE, Gianbattista , MARAZZI, Alessandra, Maria , RESTELLI, Ermenegildo , GIANANTONIO, Anacleto
发明人： BIOSEARCH ITALIA S.P.A.
IPC分类号： C07K09/00
CPC分类号： C07K9/008
摘要： Improved chemical process for preparing the compounds of formula (I), wherein: R1 represents (C9-C12)alkyl; M represents hydrogen, alpha -D-mannopyranosyl or 6-O-acetyl- alpha -D-mannopyranosyl and Y represents an amino group of formula -NR2-alk1-(NR3-alk2)p-(NR4-alk3)q-W. One aspect of the invention refers to the preparation of the intermediate compound of formula (III) (which corresponds to the above compound of formula (I) wherein R1 and M are as above defined and Y is hydroxy), by reacting a compound of formula (II) (which corresponds to the above compound of formula (I) wherein R1 and M are as above defined and Y is hydroxymethyl), with a (C1-C4)alkanol in the presence of a concentrated mineral acid, using the same alkanol as the reaction solvent and submitting the obtained ester compound to a reductive process by adding an alkali metal borohydride into the same reaction mixture. A further aspect of the invention refers to the amidation reaction for obtaining the compound of formula (I), which is carried out by reacting a compound of formula (III) with a suitable amine of formula (IV): NHR3-alk1-(NR4-alk2)p-(NR5-alk3)q-W, wherein R3, R4, R5, alk1, alk2, alk3, p, q and W are as defined in formula (I), in an inert organic solvent, in the presence of a condensing agent and setting the initial pH of the mixture (measured after diluting a sample of the reaction mixture with 9 volumes of water) at a value of from 6.5 to 9.0. By combining the above improved steps into a single process, it is possible to set up a particularly convenient process for preparing the compounds of formula (I). In addition, a purification method involving the use of polyamide resins and aqueous eluents is provided.
摘要翻译：制备式（I）化合物的改进的化学方法，其中：R 1表示（C 9 -C 12）烷基; M代表氢，α-D-吡喃甘露糖基或6-O-乙酰基-β-D-吡喃甘露糖基，Y代表式-NR2-alk1-（NR3-alk2）p-（NR4-alk3）q-W的氨基。本发明的一个方面是指式（III）的中间体化合物（其对应于上述式（I）的化合物，其中R 1和M如上所定义且Y是羟基），通过使式（II）（其对应于上述式（I）化合物，其中R 1和M如上所定义，Y是羟甲基）与（C1-C4）烷醇在浓无机酸存在下，使用相同的链烷醇作为反应溶剂，并通过向相同的反应混合物中加入碱金属硼氢化物将所得的酯化合物进行还原反应。本发明的另一方面涉及获得式（I）化合物的酰胺化反应，其通过使式（III）的化合物与式（IV）的合适的胺反应来进行：NHR 3 - 烷基（NR 4 -alk2）p-（NR5-alk3）qW，其中R3，R4，R5，alk1，alk2，alk3，p，q和W如式（I）中所定义，在惰性有机溶剂中，缩合剂并设定混合物的初始pH（在用9体积水稀释反应混合物的样品后测量）的值为6.5至9.0。通过将上述改进的步骤组合成单一方法，可以建立一种特别方便的制备式（I）化合物的方法。此外，提供了涉及使用聚酰胺树脂和水性洗脱剂的纯化方法。

3. 发明申请

WO2008094182A3 APPARATUS FOR THE SEPARATION OF A RESIN FROM A REACTION MIXTURE 审中-公开
标题翻译：用于从反应混合物中分离树脂的装置
公开(公告)号：WO2008094182A3
公开(公告)日：2009-01-08
申请号：PCT/US2007015810
申请日：2007-07-10
申请人： SICOR INC , RESTELLI ERMENEGILDO , FORACE ESPEDITO , MESSINA ALFIO , FERRERI ANTONIO
发明人： RESTELLI ERMENEGILDO , FORACE ESPEDITO , MESSINA ALFIO , FERRERI ANTONIO
IPC分类号： B01D29/01
CPC分类号： B01D29/01 , B01D29/54 , B01D29/965
摘要： An apparatus is provided for the separation of a resin from a reaction mixture. The apparatus comprises a column fitted with a side port, two inlet/outlet ports, and two flanges. Each flange is fitted with a multilayer net screen supported by a support grid. The column itself is attached to a support structure. A process is provided for using this apparatus to remove a resin from a reaction mixture, wherein the reaction mixture is added to the apparatus and the resin is filtered off, remaining in the column as the waste leaves. The remaining resin is then washed and eluted to provide a purified product.
摘要翻译：提供了用于从反应混合物中分离树脂的装置。该装置包括一个装有侧面端口的列，两个入口/出口和两个凸缘。每个法兰都装有一个由支撑网格支撑的多层网屏。柱本身连接到支撑结构。提供了一种使用该装置从反应混合物中除去树脂的方法，其中将反应混合物加入到装置中，并且将树脂滤出，随着废物离开而残留在塔中。然后洗涤剩余的树脂并洗脱，得到纯化产物。

4. 发明申请

WO2008094182A2 APPARATUS FOR THE SEPARATION OF A RESIN FROM A REACTION MIXTURE 审中-公开
标题翻译：用于从反应混合物中分离树脂的装置
公开(公告)号：WO2008094182A2
公开(公告)日：2008-08-07
申请号：PCT/US2007/015810
申请日：2007-07-10
申请人： SICOR, INC. , RESTELLI, Ermenegildo , FORACE, Espedito , MESSINA, Alfio , FERRERI, Antonio
发明人： RESTELLI, Ermenegildo , FORACE, Espedito , MESSINA, Alfio , FERRERI, Antonio
IPC分类号： B01D29/01
CPC分类号： B01D29/01 , B01D29/54 , B01D29/965
摘要： An apparatus is provided for the separation of a resin from a reaction mixture. The apparatus comprises a column fitted with a side port, two inlet/outlet ports, and two flanges. Each flange is fitted with a multilayer net screen supported by a support grid. The column itself is attached to a support structure. A process is provided for using this apparatus to remove a resin from a reaction mixture, wherein the reaction mixture is added to the apparatus and the resin is filtered off, remaining in the column as the waste leaves. The remaining resin is then washed and eluted to provide a purified product.
摘要翻译：提供了用于从反应混合物中分离树脂的装置。该装置包括一个装有侧面端口的列，两个入口/出口和两个凸缘。每个法兰都装有一个由支撑网格支撑的多层网屏。柱本身连接到支撑结构。提供了一种使用该装置从反应混合物中除去树脂的方法，其中将反应混合物加入到装置中，并且将树脂滤出，随着废物离开而残留在塔中。然后洗涤剩余的树脂并洗脱，得到纯化产物。

5. 发明申请

WO1997030078A1 DERIVATIVES OF ANTIBIOTIC GE2270 FACTORS C2a, D2 AND E 审中-公开
标题翻译：抗生素GE2270因子C2a，D2和E的衍生物
公开(公告)号：WO1997030078A1
公开(公告)日：1997-08-21
申请号：PCT/EP1997000628
申请日：1997-02-12
申请人： BIOSEARCH ITALIA S.P.A. , LOCIURO, Sergio , TAVECCHIA, Paolo , CIABATTI, Romeo , RESTELLI, Ermenegildo
发明人： BIOSEARCH ITALIA S.P.A.
IPC分类号： C07K05/078
CPC分类号： C07K5/06139 , A61K38/00
摘要： Mono- or di-substituted derivatives of GE2270 factors C2a, D2 and E of general formula (I), wherein W represents a moiety of formula (a), (b) or (c), R and R representing a variety of substituents, X is methyl, X is a -CH2-W moiety and X is methylamino or amino, or X is a -CH2-W moiety, X is methoxymethylene and X is methylamino, with the proviso that when X is amino, then W must be 2-(aminocarbonyl)-pyrrolidinyl; with the further proviso that when W is 2-(aminocarbonyl)-pyrrolidinyl, then W cannot be hydroxy; and the pharmaceutically acceptable salts thereof. The mono- or di-substituted derivatives of antibiotic GE 2270 of formula (I) are antimicrobial agents mainly active against gram positive bacteria.
摘要翻译：通式（I）的GE2270因子C2a，D2和E的单取代或二取代衍生物，其中W表示式（a），（b）或（c）的部分，R 1和R 2，代表各种取代基，X 1是甲基，X 2是-CH 2 -W 1部分，X 3是甲基氨基或氨基，或X 1是-CH 2 -W 1 >部分，X 2是甲氧基亚甲基，X 3是甲基氨基，条件是当X 3是氨基时，则W必须是2-（氨基羰基） - 吡咯烷基; 另外条件是当W是2-（氨基羰基） - 吡咯烷基时，则W 1不能是羟基; 及其药学上可接受的盐。式（I）的抗生素GE2270的单取代或二取代衍生物是主要对革兰氏阳性细菌有活性的抗微生物剂。

6. 发明申请

WO1996024607A1 BASIC PROLINE-AMIDE DERIVATIVES OF GE 2270 AND GE 2270-LIKE ANTIBIOTICS 审中-公开
标题翻译： GE 2270和GE 2270抗生素的基本乳化剂衍生物
公开(公告)号：WO1996024607A1
公开(公告)日：1996-08-15
申请号：PCT/EP1996000407
申请日：1996-02-01
申请人： GRUPPO LEPETIT S.P.A. , LOCIURO, Sergio , SENECI, Pierfausto , RESTELLI, Ermenegildo , CIABATTI, Romeo
发明人： GRUPPO LEPETIT S.P.A.
IPC分类号： C07K05/06
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention refers to basic amides derivatives of GE 2270 and GE 2270-like antibiotics of general formula (I), wherein the group GE represents the antibiotic core molecule. The amide derivatives of antibiotic GE 2270 of formula (I) are antimicrobial agents mainly active against gram positive bacteria.
摘要翻译：本发明涉及GE 2270的碱性酰胺衍生物和通式（I）的GE2270样抗生素，其中GE代表抗生素核心分子。式（I）抗生素GE2270的酰胺衍生物是主要对革兰氏阳性细菌有活性的抗微生物剂。

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