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1. 发明授权

US09211340B2 Means and methods of enhancing delivery to biological systems 有权
标题翻译：增强对生物系统传播的手段和方法
公开(公告)号：US09211340B2
公开(公告)日：2015-12-15
申请号：US12443236
申请日：2007-09-26
申请人： Paolo Botti
发明人： Paolo Botti
IPC分类号： A61K47/48
CPC分类号： A61K47/48038 , A61K47/542 , A61K47/543 , A61K47/60 , C07K7/08
摘要： This invention relates to a peptide or polypeptide (a) which is esterified or thio-esterified (i) at the carboxylate of the C-terminus with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (ii) at a side-chain carboxylate of one or more Asp or GIu residues, if present, with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (iii) at a hydroxyl group of one or more Ser, Thr or Tyr residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; (iv) at a sulfhydryl group of one or more Cys residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; and/or (v) at the N-terminus with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group, wherein said N-terminus is previously amidated with an alpha- or beta-hydroxy acid, and wherein the ester is formed between the hydroxy group of said alpha- or beta-hydroxy acid and the carboxylic group of said guanidinium alkanoic acid or said PEG substituted with a guanidinium group and a carboxyl group; and/or (b) which contains one or more disulfides, the disulfide being formed between the sulfhydryl group of a Cys reside, if present, and a guanidinium alkanethiol or a PEG substituted with a guanidinium group and a sulfhydryl group.
摘要翻译：本发明涉及一种肽或多肽（a），其在C末端的羧酸酯上被酯化或硫酯化（i）与胍烷醇，胍链烷硫醇，被胍基取代并具有游离羟基的PEG 或被胍基和巯基取代的PEG; （ii）在一个或多个Asp或Glu残基的侧链羧酸酯上，如果存在的话，可以使用胍烷醇，胍烷硫醇，被胍基取代并具有游离羟基的PEG，或被胍基和巯基; （iii）在一个或多个Ser，Thr或Tyr残基的羟基（如果存在）与链烷酸胍或被胍基和羧基取代的PEG的羟基; （iv）在一个或多个Cys残基的巯基（如果存在）与链烷酸胍或被胍基和羧基取代的PEG的巯基; 和/或（v）在N末端具有胍基链烷酸或被胍基和羧基取代的PEG，其中所述N-末端预先用α-或β-羟基酸酰胺化，并且其中所述α-羟基酸或β-羟基酸的羟基与所述胍链烷酸的羧基或所述被胍基和羧基取代的PEG之间形成酯; 和/或（b）其中含有一个或多个二硫化物，在Cys的巯基之间形成的二硫键存在于烷基硫醇胍或被胍基和巯基取代的PEG之间。

2. 发明授权

US07884182B2 Chemical peptide ligation with three or more components 有权
标题翻译：化学肽与三个或更多成分结合
公开(公告)号：US07884182B2
公开(公告)日：2011-02-08
申请号：US10494928
申请日：2002-11-14
申请人： Paolo Botti , Hubert Gaertner , Sonia Manganiello , Matteo Villain
发明人： Paolo Botti , Hubert Gaertner , Sonia Manganiello , Matteo Villain
IPC分类号： A61K38/00
CPC分类号： C07K1/1077 , C07K1/026 , C07K1/04 , Y02P20/55
摘要： The invention provides a method of assembling oligopeptide intermediates in a native chemical ligation reaction that eliminates self-ligation of bi-functional intermediates. An important aspect of the invention is a bi-functional intermediate with an N-terminal heterocyclic protecting group which effectively prevents self-ligation in the chemical assembly process. The present invention is useful in methods for convergent synthesis of polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where three or more peptide fragments are used to assemble a polypeptide or protein product.
摘要翻译：本发明提供了在天然化学连接反应中组装寡肽中间体的方法，其消除双功能中间体的自连接。本发明的一个重要方面是具有N-末端杂环保护基的双功能中间体，其有效地防止化学组装过程中的自连接。本发明可用于多肽和蛋白质的收敛合成的方法，并提高天然化学连接反应的效率，特别是在使用三个或更多个肽片段来组装多肽或蛋白质产物的情况下。

3. 发明授权

US07030218B2 Pseudo native chemical ligation 失效
标题翻译：伪天然化学结扎
公开(公告)号：US07030218B2
公开(公告)日：2006-04-18
申请号：US10332386
申请日：2001-07-12
申请人： Christie L. Hunter , Paolo Botti , James A. Bradburne , Shiah-yun Chen , Sonya Cressman , Stephen B. H. Kent , Gerd G. Kochendoerfer , Donald W. Low
发明人： Christie L. Hunter , Paolo Botti , James A. Bradburne , Shiah-yun Chen , Sonya Cressman , Stephen B. H. Kent , Gerd G. Kochendoerfer , Donald W. Low
IPC分类号： C07K1/02 , C07K1/07
CPC分类号： C07K14/505 , A61K38/00
摘要： The present invention concerns methods and compositions for extending the technique of native chemical ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond (see FIG. 1). The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.
摘要翻译：本发明涉及通过酰胺键扩展更宽范围的肽，多肽，其它聚合物和其它分子的天然化学连接技术的方法和组合物（参见图1）。本发明还提供了这些蛋白质和衍生化蛋白质的方法和用途。本发明特别适用于合成任选的聚合物改性的合成生物活性蛋白质和含有这种蛋白质的药物组合物。

4. 发明授权

US09533048B2 Mucosal delivery of drugs 有权
标题翻译：粘膜递送药物
公开(公告)号：US09533048B2
公开(公告)日：2017-01-03
申请号：US14122182
申请日：2012-05-25
申请人： Paolo Botti , Sylvie Tchertchian
发明人： Paolo Botti , Sylvie Tchertchian
IPC分类号： A61K38/26 , A61P3/10 , A61P7/12 , C07K14/605 , A61K47/22 , A61K9/00 , A61K47/14 , A61K47/24 , A61K47/28 , A61K38/11 , A61K38/22 , A61K38/23 , A61K38/28 , A61K38/29
CPC分类号： A61K47/22 , A61K9/0014 , A61K38/11 , A61K38/2278 , A61K38/23 , A61K38/26 , A61K38/28 , A61K38/29 , A61K47/14 , A61K47/24 , A61K47/28
摘要： The present invention provides a composition comprising or consisting of components (a) (i) at least one mono-alkanoyl glycerol ester, wherein alkanoyl is selected from C4 to C21 alkanoyl, preferably from octanoyl and decanoyl; and (b) (i) at least one compound selected from cholesterol, phosphatidyl cholines and phosphatidyl glycerols, wherein the acyl moieties of the phosphatidyl moieties are independently selected from C6 to C21 alkanoyl and C6 to C21 alkenoyl.
摘要翻译：本发明提供一种组合物，其包含或由组分（a）（i）组成，至少一种单烷酰基甘油酯，其中烷酰基选自C 4至C 21烷酰基，优选为辛酰基和癸酰基; 和（b）（i）至少一种选自胆固醇，磷脂酰胆碱和磷脂酰甘油的化合物，其中磷脂酰基部分的酰基部分独立地选自C6至C21烷酰基和C6至C21链烯酰基。

5. 发明授权

US08729228B2 Method of producing a modified (poly) peptide 有权
标题翻译：生产修饰（多）肽的方法
公开(公告)号：US08729228B2
公开(公告)日：2014-05-20
申请号：US12088119
申请日：2006-09-28
申请人： Paolo Botti
发明人： Paolo Botti
IPC分类号： A61K38/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K1/1077 , C07K1/003
摘要： This invention relates to a method of producing a modified (poly)peptide, said method comprising the step of modifying in an organic solvent a crown ether-bound (poly)peptide at one or more carboxylic groups by esterification or thioesterification and/or at the amino group of the N-terminal amino acid by amidation or alkylation. Furthermore provided are (poly)peptides and antibodies obtainable with the method of the invention as well as medical uses thereof.
摘要翻译：本发明涉及生产修饰的（多）肽的方法，所述方法包括在有机溶剂中通过酯化或硫酯化在一个或多个羧基上改性冠醚结合（多）肽的步骤和/或在通过酰胺化或烷基化处理N-末端氨基酸的氨基。此外提供的是（多）肽和可用本发明的方法获得的抗体及其医疗用途。

6. 发明申请

US20090192300A1 Side-Chain Extended Ligation 审中-公开
标题翻译：侧链扩展连接
公开(公告)号：US20090192300A1
公开(公告)日：2009-07-30
申请号：US11917636
申请日：2006-06-16
申请人： Paolo Botti , Sylvie Tchertchian
发明人： Paolo Botti , Sylvie Tchertchian
IPC分类号： C07K1/10
CPC分类号： C07K1/04 , C07K1/026
摘要： The invention is directed to methods and compositions for chemical ligation of a first component that includes a carboxythioester and a second component that includes an amino-functionalized compound bearing a branched side chain that includes a removable thiol auxiliary, to give a ligation product having an amide bond at the ligation site. The reactants of the invention are chemoselective and the thiol moiety is removable from the ligation product. Removal of the thiol can be exploited to generate a native side chain at the ligation site. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate peptides, polypeptides and other amino acid containing polymers.
摘要翻译：本发明涉及用于化学连接第一组分的方法和组合物，所述第一组分包括羧基硫酯和第二组分，所述第二组分包括带有支链侧链的氨基官能化化合物，其包含可除去的硫醇辅助剂，得到具有酰胺的连接产物结扎部位的结合。本发明的反应物是化学选择性的，硫醇部分可从连接产物中除去。可以利用硫醇的去除在结合位点产生天然侧链。本发明的方法和组合物特别适用于肽和多肽的连接。本发明的连接系统可应用于各种各样的分子，因此可用于产生肽，多肽和其它含氨基酸的聚合物。

7. 发明授权

US07566697B2 Carboxy protection strategies for acidic C-terminal amino acids in chemical ligation of oligopeptides 失效
标题翻译：酸性C末端氨基酸在寡肽化学连接中的羧基保护策略
公开(公告)号：US07566697B2
公开(公告)日：2009-07-28
申请号：US10517392
申请日：2003-06-09
申请人： Paolo Botti , Matteo Villain , Sonia Manganiello , Hubert Gaertner
发明人： Paolo Botti , Matteo Villain , Sonia Manganiello , Hubert Gaertner
IPC分类号： A61K38/08
CPC分类号： C07K1/04 , C07K1/061 , C07K1/062 , C07K1/065 , C07K1/067 , C07K5/10 , C07K7/04 , C07K14/001 , C07K17/00
摘要： The present invention provides methods of assembling oligopeptides or polypeptides in a native chemical ligation reaction that eliminates the formation of unwanted side products resulting from the presence of an unprotected acidic C-terminal oligopeptide thioester. An important aspect of the present invention is providing side chain protected acidic C-terminal oligopeptide thioesters. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where aspartyl or glutamyl peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
摘要翻译：本发明提供了在天然化学连接反应中组装寡肽或多肽的方法，其消除由未保护的酸性C-末端寡肽硫酯的存在产生的不需要的副产物的形成。本发明的一个重要方面是提供侧链保护的酸性C末端寡肽硫酯。本发明可用于化学合成寡肽，多肽和蛋白质并提高天然化学连接反应的效率的方法，特别是当天冬氨酰基或谷氨酰肽片段用于组装寡肽，多肽或蛋白质产物时。

8. 发明申请

US20060149039A1 Pseudo-native chemical ligation 审中-公开
标题翻译：伪天然化学结扎
公开(公告)号：US20060149039A1
公开(公告)日：2006-07-06
申请号：US11340730
申请日：2006-01-27
申请人： Christie Hunter , Paolo Botti , James Bradburne , Shiah-yun Chen , Sonya Cressman , Stephen Kent , Gerd Kochendoerfer , Donald Low
发明人： Christie Hunter , Paolo Botti , James Bradburne , Shiah-yun Chen , Sonya Cressman , Stephen Kent , Gerd Kochendoerfer , Donald Low
IPC分类号： A61K38/19 , A61K38/18 , C07K14/53 , C07K14/51
CPC分类号： C07K14/505 , A61K38/00
摘要： The present invention concerns methods and compositions for extending the technique of native chemical ligation to permit the ligation of a wider range of peptides, polypeptides, other polymers and other molecules via an amide bond. The invention further provides methods and uses for such proteins and derivatized proteins. The invention is particularly suitable for use in the synthesis of optionally polymer-modified, synthetic bioactive proteins, and of pharmaceutical compositions that contain such proteins.
摘要翻译：本发明涉及用于延伸天然化学连接技术以允许通过酰胺键连接更宽范围的肽，多肽，其它聚合物和其它分子的方法和组合物。本发明还提供了这些蛋白质和衍生化蛋白质的方法和用途。本发明特别适用于合成任选的聚合物改性的合成生物活性蛋白质和含有这种蛋白质的药物组合物。

9. 发明申请

US20140187489A1 MUCOSAL DELIVERY OF DRUGS 有权
标题翻译：药物输送
公开(公告)号：US20140187489A1
公开(公告)日：2014-07-03
申请号：US14122182
申请日：2012-05-25
申请人： Paolo Botti , Sylvie Tchertchian
发明人： Paolo Botti , Sylvie Tchertchian
IPC分类号： A61K47/24 , A61K38/26 , A61K47/22 , A61K47/14
CPC分类号： A61K47/22 , A61K9/0014 , A61K38/11 , A61K38/2278 , A61K38/23 , A61K38/26 , A61K38/28 , A61K38/29 , A61K47/14 , A61K47/24 , A61K47/28
摘要： The present invention provides a composition comprising or consisting of components (a) (i) at least one mono-alkanoyl glycerol ester, wherein alkanoyl is selected from C4 to C21 alkanoyl, preferably from octanoyl and decanoyl; and (b) (i) at least one compound selected from cholesterol, phosphatidyl cholines and phosphatidyl glycerols, wherein the acyl moieties of the phosphatidyl moieties are independently selected from C6 to C21 alkanoyl and C6 to C21 alkenoyl.
摘要翻译：本发明提供一种组合物，其包含或由组分（a）（i）组成，至少一种单烷酰基甘油酯，其中烷酰基选自C 4至C 21烷酰基，优选为辛酰基和癸酰基; 和（b）（i）至少一种选自胆固醇，磷脂酰胆碱和磷脂酰甘油的化合物，其中磷脂酰基部分的酰基部分独立地选自C6至C21烷酰基和C6至C21链烯酰基。

10. 发明授权

US08624044B2 Orthoester derivatives of crown ethers as carriers for pharmaceutical and diagnostic compositions 失效
标题翻译：冠醚的异构体衍生物作为药物和诊断组合物的载体
公开(公告)号：US08624044B2
公开(公告)日：2014-01-07
申请号：US13511837
申请日：2010-11-25
申请人： Paolo Botti , Sylvie Tchertchian , Doriane Theurillat
发明人： Paolo Botti , Sylvie Tchertchian , Doriane Theurillat
IPC分类号： C07D323/00
CPC分类号： C07D323/00 , C07D493/10 , C07D493/20 , C07D495/10
摘要： This invention relates to A crown ether of formula (I) wherein m is 4, 5, 6, 7, or 8 and i is, independently for each occurrence, 1 or 2; each occurrence of R1 and R2 is independently selected from hydrogen; linear or branched and substituted or unsubstituted C1 to C10 alkyl, alkenyl and alkinyl; and substituted or unsubstituted aryl with up to 10 ring atoms; or R1 and R2 together form an oxo group; at least one occurrence in the crown ether of R1, R2 and the carbon to which R1 and R2 are attached, said carbon being bound directly to an ether oxygen of formula (I), form together a group of formula (II) wherein L is a linker which is absent or selected from a covalent bond and (CR5R6)n, each occurrence of R5 and R6 being independently selected from hydrogen; linear or branched and substituted or unsubstituted C1 to C10 alkyl, alkenyl and alkinyl; and substituted or unsubstituted aryl with up to 10 ring atoms, n being 1, 2 or 3; X and Y, independently from each other, are selected from O and S; Z, independently for each occurrence, is absent or an electron-withdrawing group; R3 and R4, independently for each occurrence, are selected from hydrogen; linear or branched and substituted or unsubstituted C1 to C10 alkyl, alkenyl and alkinyl; substituted or unsubstituted aryl with up to 10 ring atoms; H(OCH2CH2)k— and H(OCH2CH2)kO—, wherein k is an integer number from 1 to 10; wherein substituents, if present, are selected from OH, O—CH3 and halogens.
摘要翻译：本发明涉及式（I）的冠醚，其中m为4,5,6,7或8，i独立地为每次出现1或2; R 1和R 2各自独立地选自氢; 直链或支链和取代或未取代的C1至C10烷基，烯基和炔基; 和具有至多10个环原子的取代或未取代的芳基; 或R 1和R 2一起形成氧代基; 在R 1，R 2和R 1和R 2连接的碳的至少一个存在下，所述碳直接键合到式（I）的醚氧上，一起形成式（II）的基团，其中L是不存在或选自共价键的接头和（CR5R6）n，每个出现的R5和R6独立地选自氢; 直链或支链和取代或未取代的C1至C10烷基，烯基和炔基; 和具有至多10个环原子的取代或未取代的芳基，n为1,2或3; X和Y彼此独立地选自O和S; Z独立地为每次出现，不存在或吸电子基团; R3和R4各自独立地选自氢; 直链或支链和取代或未取代的C1至C10烷基，烯基和炔基; 具有至多10个环原子的取代或未取代的芳基; H（OCH 2 CH 2）k - 和H（OCH 2 CH 2）kO-，其中k是1至10的整数; 其中取代基（如果存在）选自OH，O-CH 3和卤素。

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