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1. 发明申请

WO0050465A3 STYRENE/DIVINYLBENZENE COPOLYMERS FUNCTIONALIZED WITH A HIGH DEGREE OF AMINOMETHYL GROUPS 审中-公开
标题翻译：具有高度氨基甲酸基官能团的苯乙烯/二苯乙烯共聚物
公开(公告)号：WO0050465A3
公开(公告)日：2000-11-30
申请号：PCT/BR0000023
申请日：2000-02-23
申请人： CONSELHO NACIONAL CNPQ , RYUICHI NAKAIE CLOVIS , CILLI EDUARDO MAFFUD , JABILUT GUITA NICOLAEWSKI , HADDAD CARVALHO REGINA SIQUEIR
发明人： RYUICHI NAKAIE CLOVIS , CILLI EDUARDO MAFFUD , JABILUT GUITA NICOLAEWSKI , HADDAD CARVALHO REGINA SIQUEIR
IPC分类号： B01J41/12 , C08F20060101 , C08F8/30 , C08F8/32
CPC分类号： B01J41/12 , C08F8/30 , C08F8/32
摘要： Resins containing apolar styrene-divinylbenzenc-type matrices may solvate in aqueous medium, depending on the amount of positively charged ammonium groups incorporated in its structure. Experiments with a resin containing 4.9 mmol/g aminomethyl groups and denominated aminomethyl-resin (hereafter referred as to EPM-1) showed that this resin presents a good solvation in polar organic solvents and even in water. Based on a special strategy already developed for estimation of pKa of ionizable groups of the resin, it was found a value around 5,5 for the EPM-1 amine group. As model of anionic solutes for chromatographic assays with EPM-1, differently negatively charged peptide fragments were synthesized and tested in chromatographic purification thus demonstrating that EPM-1 can be considered an alternative anion exchange resin also for other anionic solutes. Besides, for containing easily reactive primary amine groups in its structure, this resin can be also precursor for other resins with different chromatographic potentialities. In the same trend, chemical variation involving the divinylbenzene degree of crosslinking of this copolymer may affect its solvation characteristics, porosity, etc., hence modifying the use of this polymeric material.
摘要翻译：含有非极性苯乙烯 - 二乙烯基苯类型基质的树脂可以在水性介质中溶解，这取决于结合在其结构中的带正电荷的铵基团的量。含有4.9 mmol / g氨基甲基和氨基甲基树脂（以下称为EPM-1）的树脂的实验表明，该树脂在极性有机溶剂中甚至在水中具有良好的溶剂化性。基于已经开发用于估计树脂可离子化基团的pKa的特殊策略，EPM-1胺基的值约为5,5。作为使用EPM-1进行色谱分析的阴离子溶质模型，合成了不同的带负电荷的肽片段，并在色谱纯化中进行了测试，证明了EPM-1也可以被认为是其他阴离子溶质的替代阴离子交换树脂。此外，为了在其结构中含有容易反应的伯胺基，该树脂也可以是具有不同色谱势的其它树脂的前体。在同样的趋势中，涉及该共聚物的二乙烯基苯交联度的化学变化可能影响其溶剂化特性，孔隙率等，因此改变了该聚合物材料的用途。

2. 发明申请

WO0049867A3 SYNTHESIS OF THE FIRST PARAMAGNETIC AND ACTIVE ANALOGUE (EPM-2) OF THE MELANOCYTE STIMULATING HORMONE 审中-公开
标题翻译： MELANOCYTE刺激激素的第一参与和活性成像（EPM-2）的合成
公开(公告)号：WO0049867A3
公开(公告)日：2000-12-21
申请号：PCT/BR0000025
申请日：2000-02-23
申请人： CONSELHO NACIONAL CNPQ , RYUICHI NAKAIE CLOVIS , CILLI EDUARDO MAFFUD , LAMY FREUND MARIA TEREZA , BARBOSA SIMONE DOS REIS
发明人： RYUICHI NAKAIE CLOVIS , CILLI EDUARDO MAFFUD , LAMY-FREUND MARIA TEREZA , BARBOSA SIMONE DOS REIS
IPC分类号： C07K14/685 , G01N33/532
CPC分类号： C07K14/685 , G01N33/532 , Y10T436/24 , Y10T436/25
摘要： The present invention refers to the chemical synthesis and potentiality for application in several biochemical assays, of a new alpha -melanocyte stimulating hormone ( alpha -MSH) analogue, labeled with an amino acid-type paramagnetic spin probe (Toac, or 2, 2, 6, 6-tetramethylpiperidine-1-oxyl-4-amino-4-carboxylic acid). The referred analogue of the present invention, acetyl-Toac - alpha -MSH or briefly EPM-2 are the first publish in the scientific literature which although containing a non-natural compound in its structure, maintained entirely the alpha -MSH activity. Its integral activity associated with the presence of the Toac residue which allow its conformational study through the electron paramagnetic resonance (RPE) spectroscopy associated with the fact that it contains a natural fluorescence (due to the Trp residue of its sequence) give to this labeled analogue a unique potential for a great variety of studies regarding relevant physiological roles already known of this neuroimmunomodulator.
摘要翻译：本发明涉及在几种生物化学测定中应用于用氨基酸型顺磁性自旋探针（Toac，或2，2，2）标记的新的α-黑素细胞刺激激素（α-MSH）类似物的化学合成和潜力， 6,6-四甲基哌啶-1-氧基-4-氨基-4-羧酸）。本发明的引用的类似物，乙酰基-acac-α-MSH或简称EPM-2是科学文献中的第一个出版物，尽管其结构中含有非天然化合物，但完全保持α-MSH活性。其与Toac残基的存在相关的整体活性允许其通过与包含天然荧光（由于其序列的Trp残基）相关的电子顺磁共振（RPE）光谱的构象研究而得到该标记的类似物对于这种神经免疫调节剂已知的相关生理学作用，有着广泛的研究的独特潜力。

3. 发明申请

WO02053578A9 NOVEL APPLICATIONS FOR AN ANION EXCHANGE RESIN (EPM-8) 审中-公开
标题翻译： ANION交换树脂的新应用（EPM-8）
公开(公告)号：WO02053578A9
公开(公告)日：2012-04-19
申请号：PCT/BR0100161
申请日：2001-12-26
申请人： CONSELHO NACIONAL CNPQ , NAKAIE CLOVIS RYUICHI , IANZER DANIELLE ALVES , CILLI EDUARDO MAFFUD , MALAVOLTA LUCIANA , RODRIGUES MAURICIO MARTINS
发明人： NAKAIE CLOVIS RYUICHI , IANZER DANIELLE ALVES , CILLI EDUARDO MAFFUD , MALAVOLTA LUCIANA , RODRIGUES MAURICIO MARTINS
IPC分类号： C07K1/04 , C07K1/18
CPC分类号： C07K1/18 , C07K1/042

4. 发明申请

WO0146216A3 USE OF AN ANION EXCHANGE RESIN (EPM-7) AS SOLID SUPPORT FOR PEPTIDE SYNTHESIS AND AFFINITY CHROMATOGRAPHY 审中-公开
标题翻译：使用ANION交换树脂（EPM-7）作为固体支持用于肽合成和亲和色谱
公开(公告)号：WO0146216A3
公开(公告)日：2002-01-17
申请号：PCT/BR0000160
申请日：2000-12-20
申请人： CONSELHO NACIONAL CNPQ , NAKAIE CLOVIS RYUICHI , IANZER DANIELLE ALVEZ , CILLI EDUARDO MAFFUD , RODRIGUES MAURICIO MARTINS
发明人： NAKAIE CLOVIS RYUICHI , IANZER DANIELLE ALVEZ , CILLI EDUARDO MAFFUD , RODRIGUES MAURICIO MARTINS
IPC分类号： C07K1/04 , C07K1/22 , C07K17/00 , C07K1/00 , G01N33/00
CPC分类号： C07K1/042 , C07K1/22
摘要： The present invention refers to the discovery that the anion exchange resin DEAE-Sephadex A50 might be also used alternatively as polymeric support for peptide synthesis and affinity chromatography. It was possible to synthesize a model octapeptide (angiotensin II) in this resin using the Fmoc-chemistry and when appropriate "linker groups" are used, free peptide cleaved from the resin can be obtained containing C-terminal extremity in carboxylate or carboxamide forms. By considering the feasibility of synthesizing peptide sequence throughout its structure, the repetitive (NANP)3 sequence found in the antigenic epitope of the sporozoite form of Plasmodium falciparum involved in the malaria transmission was assembled in the DEAE-Sephadex A50 resin. Column with the synthesized (NANP)3-containing DEAE-Sephadex A50 resin retained quantitatively antibody for (NANP)3 sequence which was further removed through usual washing process, thus demonstrating the feasibility of using this anion.
摘要翻译：本发明涉及阴离子交换树脂DEAE-Sephadex A50 TM也可以替代地用作肽合成和亲和层析的聚合物载体的发现。可以使用Fmoc化学在该树脂中合成模型八肽（血管紧张素II），并且当使用适当的“连接基团”时，可以获得在羧酸盐或羧酰胺形式中含有C末端末端的从树脂切割的游离肽。通过考虑在其整个结构中合成肽序列的可行性，在疟疾传播中参与疟原虫传播的子孢子形式的子孢子形式的抗原表位中发现的重复（NANP）3序列在DEAE-Sephadex A50树脂。含有合成（NANP）3的DEAE-Sephadex A50树脂的柱保留了（NANP）3序列的定量抗体，通过通常的洗涤过程进一步除去，从而证明了使用该阴离子的可行性。

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