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1. 发明公开

EP2561891A2 Means and methods of enhancing delivery to biological systems 审中-公开
标题翻译： Mittel und Verfahren zur Verbesserung der Verabreichung a biologische Systeme
公开(公告)号：EP2561891A2
公开(公告)日：2013-02-27
申请号：EP12188878.8
申请日：2007-09-26
申请人： Botti, Paolo
发明人： Botti, Paolo
IPC分类号： A61K47/22 , A61K47/14 , A61K31/365 , C07D323/00
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 Glu 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，胍烷基硫醇胍，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（如果存在的话）的侧链羧酸酯上与胍烷醇，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（如果存在）的羟基上，与胍基链烷酸或被胍基和羧基取代的PEG; （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被胍基和羧基取代的所述PEG之间形成酯; 和/或（b）含有一个或多个二硫化物，在Cys的巯基之间形成的二硫化物存在于烷基硫醇胍或巯基胍取代的胍基中。

2. 发明授权

EP2068936B1 MEANS AND METHODS OF ENHANCING DELIVERY TO BIOLOGICAL SYSTEMS 有权转让
标题翻译：手段与方法用于改善生物系统CHARGE
公开(公告)号：EP2068936B1
公开(公告)日：2016-06-22
申请号：EP07818479.3
申请日：2007-09-26
申请人： Botti, Paolo
发明人： Botti, Paolo
IPC分类号： A61K47/48
CPC分类号： A61K47/48038 , A61K47/542 , A61K47/543 , A61K47/60 , C07K7/08

3. 发明公开

EP2068936A2 MEANS AND METHODS OF ENHANCING DELIVERY TO BIOLOGICAL SYSTEMS 有权转让
标题翻译：手段与方法用于改善生物系统CHARGE
公开(公告)号：EP2068936A2
公开(公告)日：2009-06-17
申请号：EP07818479.3
申请日：2007-09-26
申请人： Botti, Paolo
发明人： Botti, Paolo
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.

4. 发明授权

EP2068934B1 FORMULATIONS COMPRISING CYCLIC COMPOUNDS 有权转让
公开(公告)号：EP2068934B1
公开(公告)日：2018-07-18
申请号：EP07818525.3
申请日：2007-09-27
申请人： Botti, Paolo
发明人： Botti, Paolo
IPC分类号： A61K47/22 , A61K47/14 , A61K31/365 , C07D323/00
CPC分类号： C07D323/00 , A61K47/22 , A61K47/6949 , B82Y5/00
摘要： This invention relates to the use of a cyclic compound of formula (I) wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p-(n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p-(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition further comprising a pharmaceutically or diagnostically active agent, said active agent comprising one or more protonated primary and/or protonated secondary amino groups and/or a protonated guanidinium groups, wherein (a) transmembrane and/or transmucosal delivery; (b) solubility in non-aqueous solvents; and/or (c) stability of said active agent are improved.

5. 发明公开

EP2561891A3 Means and methods of enhancing delivery to biological systems 审中-公开
标题翻译：装置和改善给予生物系统的方法
公开(公告)号：EP2561891A3
公开(公告)日：2013-03-06
申请号：EP12188878.8
申请日：2007-09-26
申请人： Botti, Paolo
发明人： Botti, Paolo
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 Glu 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.

6. 发明公开

EP2068934A2 FORMULATIONS COMPRISING CYCLIC COMPOUNDS 有权转让
标题翻译： FORMULIERUNGEN MIT CYCLISCHEN VERBINDUNGEN
公开(公告)号：EP2068934A2
公开(公告)日：2009-06-17
申请号：EP07818525.3
申请日：2007-09-27
申请人： Botti, Paolo
发明人： Botti, Paolo
IPC分类号： A61K47/22 , A61K47/14 , A61K31/365 , C07D323/00
CPC分类号： C07D323/00 , A61K47/22 , A61K47/6949 , B82Y5/00
摘要： This invention relates to the use of a cyclic compound of formula (I) wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p-(n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p-(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition further comprising a pharmaceutically or diagnostically active agent, said active agent comprising one or more protonated primary and/or protonated secondary amino groups and/or a protonated guanidinium groups, wherein (a) transmembrane and/or transmucosal delivery; (b) solubility in non-aqueous solvents; and/or (c) stability of said active agent are improved.
摘要翻译：本发明涉及式（I）的环状化合物的用途，其中A，B在每次出现时均独立地为具有k个碳原子的烷烃-i，j-二基，i且独立地j小于或等于k且k被选定 1至10，其中所述烷烃i，j-二基（i）可以包含一个或多个双键; （ii）任选被取代; 和/或（iii）包括循环，其中所述化合物中环状糖的总循环数为0至4，小于p（n + m）; X，Y各自独立地为包含至少一个氧原子或两个硫原子的生物相容性官能团; n，m彼此独立地选自0至20; p选自1至10; n + m等于或大于1; 并且p（n + m）选自3-30; 其中所述化合物能够与质子化的伯和/或质子化仲氨基和/或质子化胍基形成络合物，用于制备药物或诊断组合物，其进一步包含药学或诊断活性剂，所述活性剂包含一种或更多质子化的伯和/或质子化仲氨基和/或质子化胍基，其中（a）跨膜和/或经粘膜递送; （b）在非水溶剂中的溶解度; 和/或（c）所述活性剂的稳定性得到改善。

7. 发明公开

EP1905454A1 Formulations comprising cyclic compounds 审中-公开
标题翻译： Formulierungen welche zyklische Verbindungen enthalten
公开(公告)号：EP1905454A1
公开(公告)日：2008-04-02
申请号：EP06020286.8
申请日：2006-09-27
申请人： Botti, Paolo
发明人： Botti, Paolo
IPC分类号： A61K47/22 , A61K47/14 , A61K31/365 , C07D323/00
CPC分类号： C07D323/00 , A61K47/22 , A61K47/6949 , B82Y5/00
摘要： This invention relates to the use of a cyclic compound of formula (I)

wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p-(n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p-(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition further comprising a pharmaceutically or diagnostically active agent, said active agent comprising one or more protonated primary and/or protonated secondary amino groups and/or a protonated guanidinium groups, wherein (a) transmembrane and/or transmucosal delivery; (b) solubility in non-aqueous solvents; and/or (c) stability of said active agent are improved.
摘要翻译：本发明涉及式（I）的环状化合物的用途，其中A，B在每次出现时均独立地为具有k个碳原子的烷烃-i，j-二基，i且独立地j小于或等于k且k被选定 1至10，其中所述烷烃i，j-二基（i）可以包含一个或多个双键; （ii）任选被取代; 和/或（iii）包括循环，其中所述化合物中环状糖的总循环数为0至4，小于p（n + m）; X，Y各自独立地为包含至少一个氧原子或两个硫原子的生物相容性官能团; n，m彼此独立地选自0至20; p选自1至10; n + m等于或大于1; 并且p（n + m）选自3-30; 其中所述化合物能够与质子化的伯和/或质子化仲氨基和/或质子化胍基形成络合物，用于制备药物或诊断组合物，其进一步包含药学或诊断活性剂，所述活性剂包含一种或更多质子化的伯和/或质子化仲氨基和/或质子化胍基，其中（a）跨膜和/或经粘膜递送; （b）在非水溶剂中的溶解度; 和/或（c）所述活性剂的稳定性得到改善。

8. 发明申请

WO0204015A9 POLYMER-MODIFIED BIOACTIVE SYNTHETIC CHEMOKINES, AND METHODS FOR THEIR MANUFACTURE AND USE 审中-公开
标题翻译：聚合物改性的生物合成化学品及其制造和使用方法
公开(公告)号：WO0204015A9
公开(公告)日：2003-08-07
申请号：PCT/US0121933
申请日：2001-07-12
申请人： GRYPHON THERAPEUTICS INC , KOCHENDOERFER GERD , BOTTI PAOLO , BRADBURNE JAMES A , CHEN SHIAH-YUN , CRESSMAN SONYA
发明人： KOCHENDOERFER GERD , BOTTI PAOLO , BRADBURNE JAMES A , CHEN SHIAH-YUN , CRESSMAN SONYA
IPC分类号： A61K47/30 , A61K38/00 , A61K38/19 , A61K45/00 , A61K47/34 , A61K47/48 , A61P9/10 , A61P11/06 , A61P17/00 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/08 , C07H21/04 , C07K14/47 , C07K14/52 , C07K14/715 , C07K19/00 , C12P21/02
CPC分类号： C07K14/7158 , A61K38/00 , A61K47/60 , A61K47/62
摘要： The invention relates to polymer-modified bioactive synthetic chemokines and to methods for their production and use. The bioactive synthetic chemokines of the invention comprises a polymer modified polypeptide chemokine backbone. The compounds and methods or the invention are useful for the treatment of disorders involving naturally occurring chemokines, such as for the treatment of HIV and AIDS related disorders and for the treatment of asthma, allergic rhinitis, atopic dermatitis, atheroma/atherosclerosis, organ transplant rejection, and rheumatoid arthritis.
摘要翻译：本发明涉及聚合物改性的生物活性合成趋化因子及其生产和使用方法。本发明的生物活性合成趋化因子包含聚合物修饰的多肽趋化因子主链。化合物和方法或本发明可用于治疗涉及天然存在的趋化因子的疾病，例如用于治疗HIV和AIDS相关疾病以及治疗哮喘，过敏性鼻炎，特应性皮炎，动脉粥样硬化/动脉粥样硬化，器官移植排斥和类风湿性关节炎。

9. 发明申请

WO2008037484A3 FORMULATIONS COMPRISING CYCLIC COMPOUNDS 审中-公开
标题翻译：包含环化合物的制剂
公开(公告)号：WO2008037484A3
公开(公告)日：2008-12-18
申请号：PCT/EP2007008442
申请日：2007-09-27
申请人： BOTTI PAOLO
发明人： BOTTI PAOLO
IPC分类号： A61K47/22 , A61K31/365 , A61K47/14 , C07D323/00
CPC分类号： C07D323/00 , A61K47/22 , A61K47/6949 , B82Y5/00
摘要： This invention relates to the use of a cyclic compound of formula (I), wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p (n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p.(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition further comprising a pharmaceutically or diagnostically active agent, said active agent comprising one or more protonated primary and/or protonated secondary amino groups and/or a protonated guanidinium groups, wherein (a) transmembrane and/or transmucosal delivery; (b) solubility in non-aqueous solvents; and/or (c) stability of said active agent are improved.
摘要翻译：本发明涉及式（I）环状化合物的用途，其中A，B在每种情况下独立地为具有k个碳原子的链烷-ε，j-二基，i和独立地j小于或等于k且k为选自1至10，其中所述烷烃-i，j-二基（i）可以包含一个或多个双键; （ii）任选被取代; 和/或（iii）包括一个循环，其中所述化合物中循环糖的总循环次数选自0至4且小于p（n + m）;和/或（iii）包含循环。 X，Y在每种情况下独立地为包含至少一个氧原子或两个硫原子的生物相容性官能团; n，m彼此独立地选自0至20; p选自1至10; n + m等于或大于1; 并且p（n + m）选自3至30; 其中所述化合物能够与质子化的伯氨基和/或质子化的仲氨基和/或质子化的胍基形成复合物用于制备还包含药学或诊断活性剂的药物或诊断组合物，所述活性剂包含一种或质子化的主要和/或质子化的仲氨基和/或质子化的胍基，其中（a）跨膜和/或透粘膜递送; （b）在非水溶剂中的溶解度; 和/或（c）所述活性剂的稳定性得到改善。

10. 发明申请

WO2003106615A2 POST-CLEAVAGE SULFUR DEPROTECTION FOR CONVERGENT PROTEIN SYNTHESIS BY CHEMICAL LIGATION 审中-公开
标题翻译：通过化学发光法合成蛋白质的后消融硫化物
公开(公告)号：WO2003106615A2
公开(公告)日：2003-12-24
申请号：PCT/IB2003/005087
申请日：2003-06-10
申请人： GENEPROT, INC. , BOTTI, Paolo , VILLAIN, Matteo , MANGANIELLO, Sonia , GAERTNER, Hubert
发明人： BOTTI, Paolo , VILLAIN, Matteo , MANGANIELLO, Sonia , GAERTNER, Hubert
IPC分类号： C12N
CPC分类号： C07K1/1077 , C07K1/026 , C07K1/04 , C07K7/06 , C07K14/47
摘要： The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. 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 four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
摘要翻译：本发明提供了一种通过在化学连接反应中汇聚多对寡肽来合成寡肽或多肽的方法和组合物。本发明的一个重要方面是具有C末端二硫键保护的羧基硫代酯基团的寡肽，其可被去保护以自发产生游离C末端硫酯部分。这允许单个前体参与连续的化学连接反应，从而使收敛的合成方法成为可能。本发明可用于化学合成寡肽，多肽和蛋白质的方法，并且可提高天然化学连接反应的效率，特别是四种或多种肽片段用于组装寡肽，多肽或蛋白质产物时。

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