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1. 发明申请

WO2009138985A3 COUPLING AGENTS FOR THE SYNTHESIS OF POLYPEPTIDES AND POLYNUCLEOTIDES 审中-公开
标题翻译：用于合成聚氨酯和多核苷酸的联合剂
公开(公告)号：WO2009138985A3
公开(公告)日：2010-03-18
申请号：PCT/IL2009000486
申请日：2009-05-14
申请人： LUXEMBOURG BIO TECHNOLOGIES LT , ALBERICIO FERNANDO , EL-FAHAM AYMAN , LUXEMBOURG YOAV , EWENSON ARIEL
发明人： ALBERICIO FERNANDO , EL-FAHAM AYMAN , LUXEMBOURG YOAV , EWENSON ARIEL
IPC分类号： C07H21/00 , C07K1/10
CPC分类号： C07K1/04 , C07D213/89 , C07D235/22 , C07D239/90
摘要： Novel coupling agents containing a unique leaving group moiety, which can be used beneficially and safely as coupling agents in various chemical polypeptide and/or polynucleotide syntheses, and are particularly useful as yield enhancing and racemization suppressing coupling agents for use in peptide syntheses, are disclosed. Also disclosed are processes of preparing such coupling agents and their use in the preparation of polypeptides and/or polynucleotides.
摘要翻译：公开了包含独特的离去基团部分的新型偶联剂，其可以有益地和安全地用作各种化学多肽和/或多核苷酸合成中的偶联剂，并且特别可用作用于肽合成中的产率增加和外消旋化抑制偶联剂。。还公开了制备这种偶联剂及其在制备多肽和/或多核苷酸中的用途的方法。

2. 发明申请

WO2008139481A3 PROTON ACCEPTOR IMINIUM/CARBOCATION-TYPE COUPLING AGENTS 审中-公开
标题翻译： PROTON ACCEPTOR IMINIUM / CARBOCATION-TYPE COUPLING AGENTS
公开(公告)号：WO2008139481A3
公开(公告)日：2009-02-12
申请号：PCT/IL2008000674
申请日：2008-05-15
申请人： LUXEMBOURG BIOTECHNOLOGIES LTD , ALBERICIO FERNANDO , EL-FAHAM AYMAN , LUXEMBOURG YOAV , EWENSON ARIEL
发明人： ALBERICIO FERNANDO , EL-FAHAM AYMAN , LUXEMBOURG YOAV , EWENSON ARIEL
IPC分类号： C07D207/46 , C07D213/89 , C07D249/18 , C07D295/13 , C07D417/06 , C07D471/04
CPC分类号： C07D295/13 , C07D207/46 , C07D209/34 , C07D213/57 , C07D213/89 , C07D235/18 , C07D239/92 , C07D249/18 , C07D295/205 , C07D403/06 , C07D471/04
摘要： Novel iminium-type coupling agents of formula I oder II containing proton acceptors in their iminium moiety, which can be used beneficially as coupling agents in various chemical polypeptide and/or polynucleotide syntheses, and are particularly useful as yield enhancing and racemization suppressing coupling agents for use in peptide syntheses, are disclosed. Further disclosed are a process of preparing such iminium-type coupling agents and their use in the preparation of polypeptides and/or polynucleotides.
摘要翻译：具有在其亚胺部分中含有质子受体的式I的新型亚胺鎓型偶联剂，其可有利地用于各种化学多肽和/或多核苷酸合成中的偶联剂，并且特别可用作产率增强和外消旋化抑制偶联剂用于肽合成。进一步公开的是制备这种亚胺型偶联剂的方法及其在制备多肽和/或多核苷酸中的用途。

3. 发明申请

WO2006061140A3 COMPOSITION OF SSAO SUBSTRATES AND METAL COMPOUNDS OF THE VLA AND VLB GROUPS OF THE PERIODIC TABLE 审中-公开
标题翻译： VLA和VLB组织的SSAO基材和金属化合物的组成
公开(公告)号：WO2006061140A3
公开(公告)日：2007-01-18
申请号：PCT/EP2005012848
申请日：2005-12-01
申请人： GENMEDICA THERAPEUTICS , ALBERICIO FERNANDO , ZORZANO ANTONIO , MARTI LUC , ROYO MIRIAM , YRAOLA FRANCESC
发明人： ALBERICIO FERNANDO , ZORZANO ANTONIO , MARTI LUC , ROYO MIRIAM , YRAOLA FRANCESC
IPC分类号： A61K33/04 , A61K31/137 , A61K33/24 , A61P3/10
CPC分类号： A61K33/04 , A61K31/137 , A61K33/24 , A61K2300/00
摘要： This invention relates to (pharmaceutical) compositions comprising a combination of SSAO substrates and pharmaceutically acceptable compounds of the Vla and Vlb group of the periodic table, i.e. selenium (VI)-, molybdenum (VI)- and tungsten (V)/(VI) compounds, etc. and to their use as insulin mimetic, i.e., to treat illness Diabetes mellitus, Obesity, or their symptoms. A here discovered synergism between the compounds of the Vla and Vlb groups of the periodic table, i.e. selenium (VI)-, molybdenum (VI)- and tungsten (V)/(VI) compounds, etc. and the SSAO substrates makes the effective concentration of the compounds of the Via and Vlb groups of the periodic table in the (pharmaceutical) composition one order of magnitude lower than the corresponding compound of the Vla and Vlb groups alone. Consequently the inventive (pharmaceutical) composition has much lower toxicity than the known compounds or compositions in the art alone, what is a crucial advantage of the former for its use in the treatment and/or prevention of Diabetes mellitus, particularly of Diabetes type 2, or Obesity.
摘要翻译：本发明涉及包含SSAO底物和周期表Vla和Vlb基团的药学上可接受的化合物（即硒（VI） - ，钼（VI） - 和钨（V）/（VI））的组合的（药物）化合物等，并将其用作胰岛素模拟物，即治疗疾病糖尿病，肥胖或其症状。这里发现周期表的Vla和Vlb基团的化合物（即硒（VI） - ，钼（VI） - 和钨（V）/（VI））化合物等的协同作用，并且SSAO底物使得有效（药物）组合物中的元素周期表的Via和Vlb基团的化合物的浓度比单独的Vla和Vlb基团的相应化合物低一个数量级。因此，本发明（药物）组合物的毒性比本领域已知的化合物或组合物低得多，前者用于治疗和/或预防糖尿病，特别是2型糖尿病的关键优势是什么，或肥胖。

4. 发明申请

WO2011006644A3 PROCESS FOR THE PRODUCTION OF EXENATIDE AND OF AN EXENATIDE ANALOGUE 审中-公开
标题翻译：用于生产放线菌和放线菌类似物的方法
公开(公告)号：WO2011006644A3
公开(公告)日：2011-03-24
申请号：PCT/EP2010004280
申请日：2010-07-14
申请人： LONZA AG , LONZA BRAINE SA , BRICHARD MARIE-HELENE , CAUVIN JEANNE-MARIE , DEVIJVER CHRISTINE , DROZ ANNE-SOPHIE , GILLES PASCAL , GIRAUD MATTHIEU , LATASSA DANIEL , REKAI EL DJOUHAR , VARRAY STEPHANE , ALBERICIO FERNANDO , PARADIS BAS MARTA
发明人： BRICHARD MARIE-HELENE , CAUVIN JEANNE-MARIE , DEVIJVER CHRISTINE , DROZ ANNE-SOPHIE , GILLES PASCAL , GIRAUD MATTHIEU , LATASSA DANIEL , REKAI EL DJOUHAR , VARRAY STEPHANE , ALBERICIO FERNANDO , PARADIS BAS MARTA
IPC分类号： C07K1/02 , C07K14/575
CPC分类号： C07K14/605 , C07K14/57563
摘要： Exenatide, a polypeptide having the 39 amino acid sequence H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu- -Ala-Val-20Arg-Leu-Phe-lle-Glu-25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala- -Pro-Pro-Pro-Ser-NH2, respectively its 44-mer analogue H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu- -Ala-Val-20Arg-Leu-Phe-lle-Glu-25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala- -Pro-Pro-Ser-Lys-40Lys-Lys-Lys-Lys-Lys-NH2 is prepared via a convergent four-fragment synthesis strategy from the fragments comprising the amino acid positions 1-10, 11-21, 22-29 and 30-39, respectively 30-44.
摘要翻译：艾塞那肽，具有39个氨基酸序列H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu-Ala-Val -20Arg-Leu-Phe-Ile-Glu-25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala-Pro- Pro-Pro-Ser-NH 2， H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15 Glu- Glu- Glu- -Ala- Val- 20Arg- Leu- Phe- -25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala- -Pro-Pro-Ser-Lys-40Lys-Lys- 片段合成策略从分别包含氨基酸位置1-10,11-21,22-29和30-39，分别为30-44的片段获得。

5. 发明申请

WO2011006644A2 PROCESS FOR THE PRODUCTION OF EXENATIDE AND OF AN EXENATIDE ANALOGUE 审中-公开
标题翻译：生产异构体和异构体类似物的方法
公开(公告)号：WO2011006644A2
公开(公告)日：2011-01-20
申请号：PCT/EP2010004280
申请日：2010-07-14
申请人： LONZA AG , LONZA BRAINE SA , BRICHARD MARIE-HELENE , CAUVIN JEANNE-MARIE , DEVIJVER CHRISTINE , DROZ ANNE-SOPHIE , GILLES PASCAL , GIRAUD MATTHIEU , LATASSA DANIEL , REKAI EL DJOUHAR , VARRAY STEPHANE , ALBERICIO FERNANDO , PARADIS BAS MARTA
发明人： BRICHARD MARIE-HELENE , CAUVIN JEANNE-MARIE , DEVIJVER CHRISTINE , DROZ ANNE-SOPHIE , GILLES PASCAL , GIRAUD MATTHIEU , LATASSA DANIEL , REKAI EL DJOUHAR , VARRAY STEPHANE , ALBERICIO FERNANDO , PARADIS BAS MARTA
IPC分类号： C07K1/02
CPC分类号： C07K14/605 , C07K14/57563
摘要： Exenatide, a polypeptide having the 39 amino acid sequence H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu- -Ala-Val-20Arg-Leu-Phe-lle-Glu-25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala- -Pro-Pro-Pro-Ser-NH2, respectively its 44-mer analogue H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu- -Ala-Val-20Arg-Leu-Phe-lle-Glu-25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala- -Pro-Pro-Ser-Lys-40Lys-Lys-Lys-Lys-Lys-NH2 is prepared via a convergent four-fragment synthesis strategy from the fragments comprising the amino acid positions 1-10, 11-21, 22-29 and 30-39, respectively 30-44.
摘要翻译：艾塞那肽，具有39个氨基酸序列H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu-Ala-Val -20Arg-Leu-Phe-Ile-Glu-25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala-Pro Pro-Pro-Ser-NH2分别为其44聚体 H-1His-Gly-Glu-Gly-5Thr-Phe-Thr-Ser-Asp-10Leu-Ser-Lys-Gln-Met-15Glu-Glu-Glu--Ala-Val-20Arg-Leu-Phe-Lys- -25Trp-Leu-Lys-Asn-Gly-30Gly-Pro-Ser-Ser-Gly-35Ala-Pro-Pro-Ser-Lys-40Lys-Lys-Lys-Lys-Lys-NH2通过收敛的四 - 来自包含氨基酸位置1-10,11-21,22-29和30-39的片段的片段合成策略分别为30-44。

6. 发明申请

WO2004073598A3 SOLID PHASE SYNTHESIS OF ANTITUMORAL COMPOUNDS 审中-公开
标题翻译：抗菌化合物的固相合成
公开(公告)号：WO2004073598A3
公开(公告)日：2004-11-11
申请号：PCT/GB2004000683
申请日：2004-02-20
申请人： PHARMA MAR SAU , ALVAREZ MERCEDES , ALBERICIO FERNANDO , CIRONI PABLO , CUEVAS CARMEN , FRANCESCH ANDRES , MARFIL MARTA , RUFFLES GRAHAM KEITH
发明人： ALVAREZ MERCEDES , ALBERICIO FERNANDO , CIRONI PABLO , CUEVAS CARMEN , FRANCESCH ANDRES , MARFIL MARTA
IPC分类号： C07D207/34 , C07D491/14
CPC分类号： C07D491/14 , C07D207/34 , Y02P20/55
摘要： Lamellarins are prepared using a solid phase synthesis. In a first aspect, the process includes a step as follows: Formula (I) where R1 to R15 are as defined, and X is halogen, provided that one of R2, R3 or R4 is immobilised to a resin. In a second aspect, the process includes a step as follows: Formula (II) where R1' to R5', R11' and R13' are as defined, X1 and X2 are halogen, M is a metal function and PG is an amino protecting group, provided that one of that R2', R3' or R4' is immobilised to a resin.
摘要翻译：使用固相合成制备层状分子。在第一方面，该方法包括如下步骤：其中R 1至R 15如所定义，式（I）其中X为卤素，条件是R2，R3或R4中的一个被固定在树脂上。在第二方面，该方法包括如下步骤：其中R 1'至R 5'，R 11'和R 13'如上所定义的式（II），X 1和X 2为卤素，M为金属官能团，PG为氨基保护基其中R2'，R3'或R4'中的一个被固定在树脂上。

7. 发明申请

WO0158934A3 KAHALALIDE F AND RELATED COMPOUNDS 审中-公开
标题翻译： KAHALALIDE F及相关化合物
公开(公告)号：WO0158934A3
公开(公告)日：2002-03-21
申请号：PCT/GB0100576
申请日：2001-02-09
申请人： PHARMA MAR SA , RUFFLES GRAHAM KEITH , ALBERICIO FERNANDO , GIRALT ERNEST , JIMENEZ JOSE CARLOS , LOPEZ ANGEL , MANZANARES IGNACIO , RODRIGUES IGNACIO , ROYO MIRIAM
发明人： ALBERICIO FERNANDO , GIRALT ERNEST , JIMENEZ JOSE CARLOS , LOPEZ ANGEL , MANZANARES IGNACIO , RODRIGUES IGNACIO , ROYO MIRIAM
IPC分类号： A61K38/00 , A61P35/00 , C07K7/06 , C07K7/08 , C07K11/00 , A61K38/10
CPC分类号： C07K7/06 , A61K38/00 , C07K7/08
摘要： A process is provided for preparing kahalalide F and which leads to other kahalalide mimic compounds having useful biological activity.
摘要翻译：提供了制备辣椒碱F的方法，并且其导致具有有用生物活性的其它卡哈拉宾模拟化合物。

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