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1. 发明申请

WO2017103275A1 PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES 审中-公开
标题翻译：制造DEGARELIX及其中间体的方法
公开(公告)号：WO2017103275A1
公开(公告)日：2017-06-22
申请号：PCT/EP2016/081784
申请日：2016-12-19
申请人： FRESENIUS KABI ANTI-INFECTIVES S.R.L
发明人： GURYANOV, Ivan , ORLANDIN, Andrea , BIONDI, Barbara , FORMAGGIO, Fernando , VISENTINI, Dario
IPC分类号： C07K7/23
CPC分类号： C07K7/23
摘要： The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and Converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.
摘要翻译：本发明提供了通过在氨基酸序列中优选在逐步固相合成过程中掺入对硝基 - 苯丙氨酸制备肽，优选十肽，如地加瑞克的制备方法，并且将这些转化成所需氨基酸Aph（Hor）和/或D-Aph（Cbm），优选同时附着于固相。本发明进一步提供了用于制造过程的中间体。

2. 发明申请

WO2015188774A1 加尼瑞克前体以及由其制备醋酸加尼瑞克的方法审中-公开
公开(公告)号：WO2015188774A1
公开(公告)日：2015-12-17
申请号：PCT/CN2015/081311
申请日：2015-06-12
申请人：深圳翰宇药业股份有限公司
发明人：陈友金 , 刘建 , 马亚平 , 袁建成
IPC分类号： C07K7/23 , C07K1/06 , C07K7/06 , C07K1/04 , C07K1/107
CPC分类号： C07K7/23 , C07K1/04 , C07K1/06 , C07K1/107 , C07K7/06
摘要：一种制备醋酸加尼瑞克的方法，其采用Fmoc-Lys(Boc)-OH和Fmoc-D-Lys(Boc)-OH或Fmoc-Lys(Alloc)-OH和Fmoc-D-Lys(Alloc)-OH分别替代Fmoc-HArg(Et) 2 -OH和Fmoc-D-HArg(Et) 2 -OH，预先合成加尼瑞克前体I或加尼瑞克前体II-肽树脂，再分别对前体I或前体II-肽树脂中Lys和D-Lys的侧链氨基进行修饰、处理即可获得醋酸加尼瑞克。由此合成的醋酸加尼瑞克纯度高，杂质少，且成本相对较低，适合规模化生产。

3. 发明申请

WO2015143581A1 靶特异性双突变体融合蛋白质及其制备工艺审中-公开
公开(公告)号：WO2015143581A1
公开(公告)日：2015-10-01
申请号：PCT/CN2014/000353
申请日：2014-03-31
申请人：北京博翱泰生物技术有限公司
发明人：张俊英 , 侯晓允
IPC分类号： C07K19/00 , C12N15/62 , C12N15/70 , A61K38/16 , A61P35/00
CPC分类号： C12N9/1077 , A61K38/00 , A61K38/164 , C07K7/23 , C07K14/21 , C07K2319/55 , C12Y204/02036
摘要：公开了人促性腺激素释放激素突变体（mGnRH）与绿脓杆菌外毒素A突变体（PE38m4a）的融合蛋白及其制备方法，所述融合蛋白可用于制备抗肿瘤药物。

4. 发明申请

WO2015040635A3 PURIFICATION OF ORGANIC COMPOUNDS BY SURFACTANT MEDIATED PREPARATIVE HPLC 审中-公开
标题翻译：通过表面活性剂介导的制备型HPLC纯化有机化合物
公开(公告)号：WO2015040635A3
公开(公告)日：2015-06-04
申请号：PCT/IN2014000607
申请日：2014-09-18
申请人： DAVULURI RAMAMOHAN RAO
发明人： ANWER MOHAMMED KHALID
IPC分类号： B01D15/08 , B01D15/32 , G01N1/18
CPC分类号： C07K1/20 , B01D15/325 , B01D15/42 , C07K7/23
摘要： There are only two ways to increase the amount of sample that can be purified by preparative reversed phase high performance liquid chromatography (Prep-RP-HPLC) in a single run in spite of recent advances in the production of reversed phase derivatized silica stationary supports: (1) The traditional approach is to use a bigger column (greater amount of stationary phase); and (2) Use displacement chromatography which (while labor intensive to develop) uses the stationary phase more effectively. This invention describes a unique Prep-RP-HPLC technique that uses a C-18/ C-8 derivatized silica coated with a surfactant such as Triton X-100 to result in 7 to 10 fold increase in sample loading (of the crude mixture of organic compounds including synthetic crude peptides) in contrast to the conventional Prep-RP-HPLC technique. This increase in sample loading capacity and output is due to the additional surrogate stationary phase characteristic of the C-18/ C8 adsorbed (bound) surfactant. The surfactant is bound to the C-18/ C-8 chains of the stationary phase via Van der Waals forces (hydrophobic interactions) and ionic interactions with the residual silanols of the stationary phase.
摘要翻译：尽管反相衍生的二氧化硅固定支架的生产最近有进展，但是在单次运行中，只有两种途径可以通过制备型反相高效液相色谱法（Prep-RP-HPLC）来提高样品的量。（1）传统的方法是使用较大的色谱柱（更大量的固定相）; 和（2）使用置换色谱法（尽管劳动密集型开发）更有效地使用固定相。本发明描述了独特的Prep-RP-HPLC技术，其使用涂覆有表面活性剂如Triton X-100的C-18 / C-8衍生的二氧化硅，导致样品负载量增加7至10倍有机化合物，包括合成粗肽）与传统的Prep-RP-HPLC技术相反。样品负载能力和产量的增加是由于C-18 / C8吸附（结合）表面活性剂的附加替代固定相特征。表面活性剂通过范德华力（疏水相互作用）和与固定相的残余硅烷醇的离子相互作用与固定相的C-18 / C-8链结合。

5. 发明申请

WO2012055903A1 PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES 审中-公开
标题翻译：制造方法及其中间体
公开(公告)号：WO2012055903A1
公开(公告)日：2012-05-03
申请号：PCT/EP2011/068733
申请日：2011-10-26
申请人： FERRING B.V. , KALITA, Dipak , LAYEK, Mohosin , RAO, Atmakuri Venkata Dhanunjaya , POTULA, Venkat Aravinda , GAJARE, Vikas , BALAKUMARAN, Kesavan , NILSSON, Anders , JIANG, Guangcheng
发明人： KALITA, Dipak , LAYEK, Mohosin , RAO, Atmakuri Venkata Dhanunjaya , POTULA, Venkat Aravinda , GAJARE, Vikas , BALAKUMARAN, Kesavan , NILSSON, Anders , JIANG, Guangcheng
IPC分类号： C07K1/02 , C07K5/08 , C07K7/06
CPC分类号： C07K7/06 , A61K38/00 , A61K38/04 , A61K38/08 , A61K38/09 , C07K1/02 , C07K1/026 , C07K1/06 , C07K1/10 , C07K5/08 , C07K7/00 , C07K7/04 , C07K7/23 , Y02P20/55
摘要： The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degareiix, its amino-protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degareiix itself. The manufacturing process comprises the step of cleaving the ε-amino protecting group Ρε from a Degareiix precursor according to formula {P 4 )(Pε)Ac-AA 1 -AA 10 -NH 2 in an organic solvent comprising the precursor and a cleaving agent dissolved therein: wherein P 4 is a hydroxyl-protecting group or hydrogen, preferably hydrogen.
摘要翻译：本发明涉及用于制备十肽Degareiix，其氨基保护的前体和其它有用的中间体的液体（或溶液）相制备方法。本发明还涉及可用于溶液相制备方法中的多肽和Degareiix本身的纯化。制备方法包括在包含前体的有机溶剂和溶解在其中的裂解剂的情况下，从式（P4）（Pe）Ac-AA1-AA10-NH2的Degareiix前体裂解e-氨基保护基的步骤：其中P4是羟基保护基或氢，优选氢。

6. 发明申请

WO2010033580A2 CURCUMIN CONJUGATES FOR TREATING AND PREVENTING CANCERS 审中-公开
标题翻译： CURCUMIN共轭物治疗和预防癌症
公开(公告)号：WO2010033580A2
公开(公告)日：2010-03-25
申请号：PCT/US2009/057141
申请日：2009-09-16
申请人： BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITY AND AGRICULTURAL AND MECHANICAL COLLEGE , HANSEL, William , AGGARWAL, Sita , HAMMER, Robert, P.
发明人： HANSEL, William , AGGARWAL, Sita , HAMMER, Robert, P.
IPC分类号： C12N15/16 , C12N15/63 , A61K48/00 , A61P35/00
CPC分类号： A61K47/64 , A61K38/00 , A61K38/24 , A61K47/54 , C07K7/23
摘要： Conjugating LHRH to curcumin (LHRH-Curcumin) substantially enhances the bioavailability of curcumin, targets it to cells expressing LHRH receptors, facilitates intravenous administration, and increases the anti-cancer efficacy of curcumin. The conjugate may be used against cancer cells that express the LHRH receptor: pancreas, prostate, breast, testicular, uterine, ovarian, melanoma. LH-Curcumin conjugates may be used against cancer cells that express the LH receptor: prostate, breast, ovary, testis, uterus, pancreas, and melanoma.
摘要翻译：结合LHRH与姜黄素（LHRH-姜黄素）显着增强姜黄素的生物利用度，将其靶向表达LHRH受体的细胞，促进静脉内施用，并增加姜黄素的抗癌功效。该缀合物可用于表达LHRH受体的癌细胞：胰腺，前列腺，乳房，睾丸，子宫，卵巢，黑素瘤。 LH-姜黄素缀合物可用于表达LH受体的癌细胞：前列腺，乳房，卵巢，睾丸，子宫，胰腺和黑素瘤。

7. 发明申请

WO2010022639A1 靶特异性双突变体融合蛋白质审中-公开
公开(公告)号：WO2010022639A1
公开(公告)日：2010-03-04
申请号：PCT/CN2009/073441
申请日：2009-08-24
申请人：北京博翱泰生物技术有限公司 , 张俊英
发明人：张俊英
IPC分类号： C07K19/00 , C12N15/62 , C12N15/70 , A61K38/16 , A61P35/00
CPC分类号： C07K7/23 , C07K2319/02

8. 发明申请

WO2008028934A8 CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF 审中-公开
标题翻译：异恶唑及其衍生物与细胞结合分子的偶联，新型二唑衍生物，生产过程及其用途
公开(公告)号：WO2008028934A8
公开(公告)日：2008-05-02
申请号：PCT/EP2007059310
申请日：2007-09-06
申请人： AETERNA ZENTARIS GMBH
发明人： GUENTHER ECKHARD , SCHAEFER OLAF , TEIFEL MICHAEL , PAULINI KLAUS
IPC分类号： C07D498/22 , A61K31/424 , A61P35/00 , C07D498/18 , C07K14/59 , C07K14/655
CPC分类号： C12P17/188 , C07D498/18 , C07D498/22 , C07K7/23 , C07K14/6555
摘要： The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and anti-bodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
摘要翻译：本发明提供了异唑类及其衍生物与细胞结合分子如肽，蛋白质，激素，血液蛋白质和抗体的缀合物。本发明进一步提供了新的迪索拉唑衍生物和制备这种偶联物和二唑杂衍生物的方法。这些化合物可以用作治疗哺乳动物生理和/或病理生理状况的药物，特别是用于治疗各种肿瘤。

9. 发明申请

WO2008044890A1 A METHOD FOR PREPARING PEPTIDES USING BY SOLID PHASE SYNTHESIS 审中-公开
标题翻译：一种通过固相合成制备肽的方法
公开(公告)号：WO2008044890A1
公开(公告)日：2008-04-17
申请号：PCT/KR2007/004989
申请日：2007-10-12
申请人： DONG KOOK PHARM. CO., LTD , KIM, Kyoung Min , RYOO, Sun Jong , CHA, Kyung Hoi , LIM, Dae Sung , LEE, Han Won
发明人： KIM, Kyoung Min , RYOO, Sun Jong , CHA, Kyung Hoi , LIM, Dae Sung , LEE, Han Won
IPC分类号： C07K7/06
CPC分类号： C07K7/23
摘要： The present invention relates to the preparation method of goserelin, buserelin and leuprolide having various pharmacological activities, in particular, novel method for preparing the peptides comprising the steps; coupling the amino acids on high molecular solid support step-by-step, and finally releasing the amino acids from the supports to obtain the peptides with high yield and high purity.
摘要翻译：本发明涉及具有各种药理活性的戈舍瑞林，布舍瑞林和亮丙瑞林的制备方法，特别涉及制备包含以下步骤的肽的新方法：在高分子固体支持物上逐步偶联氨基酸，最后从载体中释放出氨基酸，以获得高产率和高纯度的肽。

10. 发明申请

WO2008028934A1 CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF 审中-公开
标题翻译：异恶唑及其衍生物与细胞结合分子的结合，新型异唑衍生物，制造方法及其用途
公开(公告)号：WO2008028934A1
公开(公告)日：2008-03-13
申请号：PCT/EP2007/059310
申请日：2007-09-06
申请人： AETERMA ZENTARIS GMBH
发明人： GÜNTHER, Eckhard , SCHAEFER, Olaf , TEIFEL, Michael , PAULINI, Klaus
IPC分类号： C07D498/22 , C07D498/18 , C07K14/59 , C07K14/655 , A61K31/424 , A61P35/00
CPC分类号： C12P17/188 , C07D498/18 , C07D498/22 , C07K7/23 , C07K14/6555
摘要： The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and anti-bodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
摘要翻译：本发明提供了disorazole及其衍生物与细胞结合分子如肽，蛋白质，激素，血液蛋白和抗体的缀合物。本发明还提供了新的二唑衍生物和制备这种缀合物和二唑衍生物的方法。这些化合物可以用作治疗哺乳动物的生理和/或病理生理状况的药物，特别是用于治疗各种肿瘤。

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