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1. 发明公开

EP0357137A2 New silylating agent for the preparation of chromatographic supports 失效
标题翻译： Silylierungsmittel zur Herstellung von色谱仪Trägern。
公开(公告)号：EP0357137A2
公开(公告)日：1990-03-07
申请号：EP89202171.8
申请日：1989-08-28
申请人： ENIRICERCHE S.p.A. , SCLAVO S.p.A.
发明人： Cardinali, Franco , Longobardi, Maria Grazia , Viscomi, Giuseppe Claudio , Ziggiotti, Alessandra
IPC分类号： C07F7/18 , B01J20/32
CPC分类号： C07F7/1896 , B01J20/103 , B01J20/28004 , B01J20/286 , B01J20/3071 , B01J20/3078 , B01J20/3085 , B01J20/3092 , B01J20/3204 , B01J20/3246 , B01J2220/54 , B01J2220/58
摘要： A new mono-silylating agent of general formula (I)
(R₁,R₂,R₃)Si-NH-CO-O-Si(R₁,R₂,R₃) (I)
is described as well as its use in the preparation of chromatographic supports based on silica with functional groups covalently bonded thereto, the so-called "bonded stationary phases".
The new compounds are easy and safe to prepare from the corresponding mono-halosilanes with ammonium carbamate, and their use as silylating agents leads to stationary phases with a higher degree of surface coating than that attainable with the corresponding chlorosilanes.
摘要翻译：描述了通式（I）（R1，R2，R3）Si-NH-CO-O-Si（R1，R2，R3）（Ⅰ）的新单甲硅烷基化剂及其在色谱法制备中的应用基于与其共价键合的官能团的二氧化硅的载体，即所谓的“键合固定相”。新化合物由相应的单卤硅烷与氨基甲酸铵制备容易和安全，并且它们作为甲硅烷基化剂的用途导致具有比相应的氯硅烷可获得的更高程度的表面涂层的固定相。

2. 发明公开

EP0357137A3 New silylating agent for the preparation of chromatographic supports 失效
标题翻译：用于制备色谱支持剂的新硅胶剂
公开(公告)号：EP0357137A3
公开(公告)日：1991-01-16
申请号：EP89202171.8
申请日：1989-08-28
申请人： ENIRICERCHE S.p.A. , SCLAVO S.p.A.
发明人： Cardinali, Franco , Longobardi, Maria Grazia , Viscomi, Giuseppe Claudio , Ziggiotti, Alessandra
IPC分类号： C07F7/18 , B01J20/32
CPC分类号： C07F7/1896 , B01J20/103 , B01J20/28004 , B01J20/286 , B01J20/3071 , B01J20/3078 , B01J20/3085 , B01J20/3092 , B01J20/3204 , B01J20/3246 , B01J2220/54 , B01J2220/58
摘要： A new mono-silylating agent of general formula (I)
(R₁,R₂,R₃)Si-NH-CO-O-Si(R₁,R₂,R₃) (I)
is described as well as its use in the preparation of chromatographic supports based on silica with functional groups covalently bonded thereto, the so-called "bonded stationary phases". The new compounds are easy and safe to prepare from the corresponding mono-halosilanes with ammonium carbamate, and their use as silylating agents leads to stationary phases with a higher degree of surface coating than that attainable with the corresponding chlorosilanes.

3. 发明授权

EP0416416B1 Method for purifying low molecular weight compounds of peptide or pseudo-peptide structure 失效
标题翻译：一种用于在具有低分子量和肽或肽样结构纯化化合物过程。
公开(公告)号：EP0416416B1
公开(公告)日：1993-12-01
申请号：EP90116366.7
申请日：1990-08-27
申请人： SCLAVO S.p.A.
发明人： Viscomi, Giuseppe Claudio , Cardinali, Franco , Longobardi, Maria Grazia
IPC分类号： C07K1/14 , C07K5/02
CPC分类号： C07K1/18 , B01D15/422 , C07K5/0212 , G01N30/02

4. 发明公开

EP0551535A1 Process for the purification of recombinant human beta interferon, beta interferon thus purified, and pharmaceutical compositions which contain them 失效
标题翻译：一种用于纯化重组人干扰素-β，干扰素β，并由此进行纯化，含有它们的药物组合物的过程。
公开(公告)号：EP0551535A1
公开(公告)日：1993-07-21
申请号：EP92100404.0
申请日：1992-01-13
申请人： SCLAVO S.p.A.
发明人： Viscomi, Giuseppe Claudio , Rappuoli, Paolo
IPC分类号： C12N15/22 , C12P21/02 , C07K3/20 , C07K3/28 , A61K37/66 , C07K13/00
CPC分类号： C07K14/565 , A61K38/00
摘要： A process is described for the purification of recombinant human beta interferon which comprises the use of three chromatographic stages carried out in series, utilizing as stationary phases: glass particles of controlled porosity, cation exchange polymer resins and polymer resins able to complex heavy metals.
摘要翻译：方法描述为重组人干扰素β的纯化，其包括使用串联进行了三次色谱阶段，利用作为固定相：可控孔隙率的玻璃颗粒，阳离子交换聚合物树脂和能够复重金属聚合物树脂。

5. 发明公开

EP0416416A1 Method for purifying low molecular weight compounds of peptide or pseudo-peptide structure 失效
标题翻译：一种用于在具有低分子量和肽或肽样结构纯化化合物过程。
公开(公告)号：EP0416416A1
公开(公告)日：1991-03-13
申请号：EP90116366.7
申请日：1990-08-27
申请人： SCLAVO S.p.A.
发明人： Viscomi, Giuseppe Claudio , Cardinali, Franco , Longobardi, Maria Grazia
IPC分类号： C07K1/14 , C07K5/02
CPC分类号： C07K1/18 , B01D15/422 , C07K5/0212 , G01N30/02
摘要： This invention firstly provides a method for purifying particular compounds of peptide or pseudo-peptide structure in which the number of protonable basic functions is greater than the number of acid functions and which have a molecular weight of less than 1000 daltons, by ion exchange displacement chromatography. In the method of the present invention the stationary phase used is a cationic exchange resin or a cross-linked polymer matrix activated with acid groups; the transporter solvent used is water if the compound to be purified already possesses at least one net positive charge, or aqueous dilute solutions of inorganic or strong organic acids which protonate the basic groups of the peptide or pseudo-peptide to be separated without modifying the structure of the peptide compound, such as acetic acid, trifluoroacetic acid, formic acid, hydrochloric acid or sulphuric acid; the displacer compound used is a triethylenetetraammonium salt.
摘要翻译：本发明首先提供了一种用于纯化的肽或拟肽结构的具体化合物，其中的质子能够基本功能数比的酸官能团的数量更大，并且其中具有小于1,000道尔顿的分子量，通过离子交换置换色谱，在本发明的方法中使用的固定相为阳离子交换树脂或与酸基团活化的交联的聚合物基体; 所使用的转运溶剂是水，如果要被已经纯化化合物具有至少一个净正电荷，或wässrige稀的哪质子化肽或类肽的碱性基团，而无需修改结构被分离的无机或强有机酸溶液所述肽化合物，颜色：如乙酸，三氟乙酸，甲酸，盐酸或硫酸; 所使用的排代剂化合物为triethylenetetraammonium盐。

6. 发明公开

EP0224088A3 Process for the solid-phase synthesis of retro-inverso peptides 失效
标题翻译：逆转录酶的固相合成方法
公开(公告)号：EP0224088A3
公开(公告)日：1989-07-05
申请号：EP86115386.4
申请日：1986-11-06
申请人： ENIRICERCHE S.p.A.
发明人： Pessi, Antonello , Verdini, Antonio Silvio , Viscomi, Giuseppe Claudio
IPC分类号： C07K1/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0212 , Y02P20/55
摘要： A process for the solid-phase synthesis of a peptide containing at least one retro-inverso amide bond characterized in that :
a) the C-terminal partial peptide sequence up to the bond which has to be retro-inverted is synthesized by stepwise condensation of the amino acids suitably protected at the amino group as well as at the side chain functional groups, on a solid support which is insoluble in the reaction medium, b) the dipeptide derivative of general formula (I) :
wherein
Fmoc is N-9-fluorenylmethoxycarbonyl, and
R and R₁, each independently, represent the side-chain residues of natural amino acids wherein the functional groups, if any, are suitably protected,
is coupled to the amino terminus of the partial peptide sequence covalently bound to the solid insoluble support, c) the Fmoc amino-protecting group is cleaved from the peptide bound to the solid insoluble support, d) the whole sequence of the desired retro-inverso peptide is then stepwise built up by conventional procedures e) the thus obtained retro-inverso peptide is detached from the solid insoluble support and purified.

7. 发明公开

EP0224088A2 Process for the solid-phase synthesis of retro-inverso peptides 失效
标题翻译：弗雷泽伦zur Herstellung在fester阶段von Retro-Inverso-Peptiden。
公开(公告)号：EP0224088A2
公开(公告)日：1987-06-03
申请号：EP86115386.4
申请日：1986-11-06
申请人： ENIRICERCHE S.p.A.
发明人： Pessi, Antonello , Verdini, Antonio Silvio , Viscomi, Giuseppe Claudio
IPC分类号： C07K1/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0212 , Y02P20/55
摘要： A process for the solid-phase synthesis of a peptide containing at least one retro-inverso amide bond characterized in that :

a) the C-terminal partial peptide sequence up to the bond which has to be retro-inverted is synthesized by stepwise condensation of the amino acids suitably protected at the amino group as well as at the side chain functional groups, on a solid support which is insoluble in the reaction medium,
b) the dipeptide derivative of general formula (I) :
wherein
Fmoc is N-9-fluorenylmethoxycarbonyl, and
R and R₁, each independently, represent the side-chain residues of natural amino acids wherein the functional groups, if any, are suitably protected,
is coupled to the amino terminus of the partial peptide sequence covalently bound to the solid insoluble support,
c) the Fmoc amino-protecting group is cleaved from the peptide bound to the solid insoluble support,
d) the whole sequence of the desired retro-inverso peptide is then stepwise built up by conventional procedures
e) the thus obtained retro-inverso peptide is detached from the solid insoluble support and purified.
摘要翻译：一种用于固相合成含有至少一个逆转酰胺键的肽的方法，其特征在于：a）直至结合反转的键的C末端部分肽序列通过逐步缩合在不溶于反应介质的固体支持物上氨基酸和侧链官能团适当保护的氨基酸，b）通式（I）的二肽衍生物：其中Fmoc为N -9-芴基甲氧基羰基，R和R 1各自独立地表示天然氨基酸的侧链残基，其中官能团（如果有的话）被适当地保护）与共价结合到部分肽序列的氨基末端偶联固体不溶性载体，c）Fmoc氨基保护基团从与固体不溶性载体结合的肽切割，d）然后，按常规方法逐步建立所需的逆转换肽序列过量e）将由此获得的逆转肽与固体不溶性支持物分离并纯化。 Ë

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