[EN] NOVEL TETRAGALNAC AND PEPTIDE CONTAINING CONJUGATES AND METHODS FOR DELIVERY OF OLIGONUCLEOTIDES<br/>[FR] NOUVEAUX CONJUGUÉS CONTENANT TÉTRAGALNAC ET PEPTIDE ET PROCÉDÉS POUR L'ADMINISTRATION D'OLIGONUCLÉOTIDES
申请人:MERCK SHARP & DOHME
公开号:WO2013166155A1
公开(公告)日:2013-11-07
Disclosed herein is a modular composition comprising 1) an oligonucleotide; 2) one or more tetraGalNAc ligands of Formula (I), which may be the same or different; optionally, 3) one or more linkers, which may be the same or different; 4) one or more peptides independently selected from Table 3, which may be the same or different; and optionally, 5) one or more targeting ligands, solubilizing agents, pharmacokinetics enhancing agents, lipids, and/or masking agents.
The present invention relates to a method for producing amphiphilic functionalized highly branched melamine-polyamine polymers by condensing melamine and optionally a melamine derivate having at least one different amine having at least two primary amino groups and optionally also with urea and/or at least one urea derivative and/or with at least one at least difunctional diisocyanate or polyisocyanate and/or at least one carbolic acid having at least two carboxyl groups or at least one derivative thereof, optionally quaternizing a portion of the amino groups of the polymer thereby obtained, reacting the polymer thus obtained with at least one compound capable of undergoing a condensation or addition reaction with amino groups, and optionally quaternizing at least part of the amino groups of the polymer obtained in the first step. The invention further relates to the amphiphilic functionalized highly branched melamine-polyamine polymers that can be obtained by the method according to the invention, and to the use thereof as surface active agents.
bis-porphyrin molecularclip with a glycoluril backbone has been synthesized. The clip provides an adaptable molecular cavity for binding of diamines. Binding constants for diamines of 104–107 M−1 are orders of magnitude higher than those for monoamines of 103 M−1, indicating a preference to bidentate binding. NMR studies confirmed that binding of bidentate guests occurs inside the clip. Short- and medium-size
已经合成了具有甘脲骨架的半刚性双卟啉分子夹。该夹子为二胺的结合提供了适应性的分子腔。10 4 –10 7 M -1的二胺的结合常数比10 3 M -1的单胺的结合常数高几个数量级。,表示优先选择双齿绑定。NMR研究证实,在片段内部发生了双齿宾客的结合。短和中等大小的无环分子客体被锁定为一个单一的延伸构象,并且具有更长的柔性链的客体显示的构象迁移性比溶液中游离时小得多。如模型研究和配合物的自扩散常数所表明的,空腔的尺寸与客体的尺寸相适应。
Conjugates of hydroxyalkyl starch and an active substance, prepared by chemical ligation via thiazolidine
申请人:Fresenius Kabi Deutschland GmbH
公开号:EP1762250A1
公开(公告)日:2007-03-14
The present invention relates to a method for preparing conjugates of an active substance and hydroxyalkyl starch and to conjugates of an active substance and hydroxyalkyl starch, preferably hydroxyethyl starch, wherein the conjugates are prepared by covalently linking the hydroxyalkyl starch and the active substance by a chemical residue having a structure according to formula (I)
or formula (I')
or formula (I")
wherein R1, R2, R2', R3, R3' and R4 are independently selected from the group consisting of hydrogen, an optionally suitably substituted, linear, cyclic and/or branched alkyl, aryl, heteroaryl, aralkyl, and heteroaralkyl group, preferably hydrogen.