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1. 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。

2. 发明申请

WO2003042235A3 EXTENDED NATIVE CHEMICAL LIGATION OF THREE OR MORE PEPTIDE FRAGMENTS 审中-公开
公开(公告)号：WO2003042235A3
公开(公告)日：2003-05-22
申请号：PCT/IB2002/005094
申请日：2002-11-14
申请人： GENEPROT, INC. , BOTTI, Paolo , GAERTNER, Hubert , MANGANIELLO, Sonia , VILLAIN, Matteo
发明人： BOTTI, Paolo , GAERTNER, Hubert , MANGANIELLO, Sonia , VILLAIN, Matteo
IPC分类号： C07K1/06
摘要： The invention provides a method of assembling oligopeptide intermediates in an extended 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 N-terminal heterocyclic protecting group of the intermediate is reacted with a nucleophilic agent under acidic conditions to form a N-terminal reactive peptide fragment with a free N-terminal cysteine or a secondary N-terminal amine having the auxiliary group -D-SH, wherein D is a linking moiety. 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 and intermediates with no N-terminal cysteine are involved.

3. 发明申请

WO2004007661A2 CARBOXY PROTECTION STRATEGIES FOR ACIDIC C-TERMINAL AMINO ACIDS IN CHEMICAL LIGATION OF OLIGOPEPTIDES 审中-公开
标题翻译：酸性化学氨基酸在低聚物化学结构中的保护性策略
公开(公告)号：WO2004007661A2
公开(公告)日：2004-01-22
申请号：PCT/IB2003/005473
申请日：2003-06-09
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： C07K1/04 , 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 unprotecte 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而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。

4. 发明申请

WO2003106615A3 POST-CLEAVAGE SULFUR DEPROTECTION FOR CONVERGENT PROTEIN SYNTHESIS BY CHEMICAL LIGATION 审中-公开
公开(公告)号：WO2003106615A3
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： C07K1/00
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.

5. 发明申请

WO2006133962A1 SIDE-CHAIN EXTENDED LIGATION 审中-公开
标题翻译：侧链延长码
公开(公告)号：WO2006133962A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005815
申请日：2006-06-16
申请人： GENEPROT INC. , BOTTI, Paolo , TCHERTCHIAN, Sylvie
发明人： BOTTI, Paolo , TCHERTCHIAN, Sylvie
IPC分类号： C07K1/04
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。

6. 发明申请

WO2002004015A1 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：WO2002004015A1
公开(公告)日：2002-01-17
申请号：PCT/US2001/021933
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： A61K38/19
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骨架。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。

7. 发明申请

WO2008037484A2 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：WO2008037484A2
公开(公告)日：2008-04-03
申请号：PCT/EP2007/008442
申请日：2007-09-27
申请人： BOTTI, Paolo
发明人： BOTTI, Paolo
IPC分类号： A61K31/365 , A61K47/14 , A61K47/22 , 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各自独立地为具有k个碳原子的烷烃-i，j-二基，i且独立地为小于或等于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; 和p（n + m）选自3至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，用于制备进一步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

WO2012160203A1 MUCOSAL DELIVERY OF DRUGS 审中-公开
标题翻译：药物输送
公开(公告)号：WO2012160203A1
公开(公告)日：2012-11-29
申请号：PCT/EP2012/059890
申请日：2012-05-25
申请人： ARISGEN SA , BOTTI, Paolo , TCHERTCHIAN, Sylvie
发明人： BOTTI, Paolo , TCHERTCHIAN, Sylvie
IPC分类号： A61K47/14 , A61K47/24 , A61K47/28 , A61K38/00 , A61K47/48 , A61K9/00
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 C 4 to C 21 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 C 6 to C 21 alkanoyi and C 6 to C 21 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，其中磷脂酰部分的酰基部分独立地选自C6至C21链烷酰基和C6至C21链烯酰基。

9. 发明申请

WO2011064316A2 MUCOSAL DELIVERY OF PEPTIDES 审中-公开
标题翻译：胶原蛋白交付
公开(公告)号：WO2011064316A2
公开(公告)日：2011-06-03
申请号：PCT/EP2010/068257
申请日：2010-11-25
申请人： BOTTI, Paolo , TCHERTCHIAN, Sylvie
发明人： BOTTI, Paolo , TCHERTCHIAN, Sylvie
CPC分类号： A61K9/006 , A61K9/12 , A61K38/02 , A61K38/26 , A61K47/22 , A61K47/545
摘要： Compositions and methods are provided for mucosal delivery of peptides. The compositions include a stably hydrated peptide active agent complexed with a crown compound and/or a counter ion solubilized in a nonaqueous hydrophobic vehicle at a pH different from the pI of the peptide active agent. The methods include administering to a subject an effective amount of a composition of the disclosure. Other aspects include methods for the manufacture of the compositions of the disclosure. Also provided are compositions and kits that find use in practicing embodiments of the disclosure. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.
摘要翻译：提供组合物和方法用于肽的粘膜递送。组合物包括与不同于肽活性剂的pI的pH的与非水性疏水载体溶解的冠状化合物和/或抗衡离子配合的稳定水合的肽活性剂。所述方法包括向受试者施用有效量的本发明的组合物。其它方面包括制造本公开的组合物的方法。还提供了在实践本公开的实施方案中使用的组合物和试剂盒。所述方法和组合物可用于各种应用，包括治疗各种不同疾病状况。

10. 发明申请

WO2011064300A1 ORTHOESTER DERIVATIVES OF CROWN ETHERS AS CARRIERS FOR PHARMACEUTICAL AND DIAGNOSTIC COMPOSITIONS 审中-公开
标题翻译：作为药物和诊断组合物的载体的其他药物的代谢物衍生物
公开(公告)号：WO2011064300A1
公开(公告)日：2011-06-03
申请号：PCT/EP2010/068224
申请日：2010-11-25
申请人： ARISGEN SA , BOTTI, Paolo , TCHERTCHIAN, Sylvie , THEURILLAT, Doriane
发明人： BOTTI, Paolo , TCHERTCHIAN, Sylvie , THEURILLAT, Doriane
IPC分类号： C07D323/00 , C07D493/10 , C07D493/20 , C07D495/10 , A61K31/365
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; at least one occurrence in the crown ether of R 1 , R 2 and the carbon to which R 1 and R 2 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 (CR 5 R 6 ) n , useful as carriers for pharmaceutical and diagnostic compositions.
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; 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用作药物和诊断组合物的载体的（CR5R6）n。

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