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1. 发明授权

EP0667786B1 RETRO-, INVERSO-, AND RETRO-INVERSO SYNTHETIC PEPTIDE ANALOGUES 失效
标题翻译：复古，逆反，和逆反合成肽类似物
公开(公告)号：EP0667786B1
公开(公告)日：2004-01-21
申请号：EP93918788.6
申请日：1993-08-27
申请人： DEAKIN RESEARCH LIMITED
发明人： COMIS, Alfio , FISCHER, Peter , TYLER, Margaret Isabel
IPC分类号： C07K7/08 , A61K39/00 , G01N33/68
CPC分类号： C07K14/005 , A61K39/00 , C07K5/0212 , C07K7/02 , C07K14/34 , C07K14/43518 , C07K14/445 , C07K16/082 , C07K16/1063 , C07K16/109 , C07K16/12 , C07K16/18 , C07K16/205 , C12N2740/16122 , C12N2770/24222 , G01N33/56905 , G01N33/576 , G01N33/68 , Y02A50/412 , Y10S530/806 , Y10S530/825 , Y10S530/826
摘要： Synthetic peptide antigen analogues of native peptide antigens with partial or complete retro, inverso or retro-inverso modifications are provided. When administered as an immunogen to an immunocompetent host the synthetic peptide antigen analogues induce the production of antibodies which recognize the native peptide antigen. Uses of these analogues, vaccines and methods of preparing vaccines comprising these antigen analogues, and antibodies generated using these antigen analogues are also provided.

2. 发明授权

EP0636140B1 PARTIALLY MODIFIED AND RETRO-INVERTED TETRAPEPTIDES ANALOGUES OF C-REACTIVE PROTEIN FRAGMENTS 失效
标题翻译：纤维蛋白修饰抗逆转录病毒蛋白模拟蛋白
公开(公告)号：EP0636140B1
公开(公告)日：1997-09-10
申请号：EP93908898.5
申请日：1993-04-02
申请人： ITALFARMACO S.p.A.
发明人： VERDINI, Antonio, Silvio , PINORI, Massimo , CAPPELLETTI, Silvana , GAZERRO, Laura , LEONI, Flavio
IPC分类号： C07K5/02 , A61K38/07
CPC分类号： C07K5/0212
摘要： Retro-inverted tetrapeptides analogues of C-reactive protein fragments endowed with immuno-modulating activity.
摘要翻译： PCT No.PCT / EP93 / 00825 Sec。 371日期：1994年9月27日 102（e）日期1994年9月27日PCT提交1993年4月2日PCT公布。出版物WO93 / 21208 日期：1993年10月28日。式I的四取代四肽，即苏氨酸的侧链; R1是精氨酸，亮氨酸或谷氨酰胺的侧链; R2是氢原子或代谢易腐的酰基; 条件是当R1是精氨酸的侧链时，R不能是苏氨酸的侧链; 非对映异构体形式及其药理学上可接受的盐，酯和酰胺。这些化合物可用作免疫刺激剂。

3. 发明公开

EP0667786A1 RETRO-, INVERSO-, AND RETRO-INVERSO SYNTHETIC PEPTIDE ANALOGUES 失效
标题翻译：复古，逆反，和逆反合成肽模拟。
公开(公告)号：EP0667786A1
公开(公告)日：1995-08-23
申请号：EP93918788.0
申请日：1993-08-27
申请人： DEAKIN RESEARCH LIMITED
发明人： COMIS, Alfio , FISCHER, Peter , TYLER, Margaret Isabel
IPC分类号： G01N33 , A61K39 , C07K5 , C07K7 , C07K14 , C07K16
CPC分类号： C07K14/005 , A61K39/00 , C07K5/0212 , C07K7/02 , C07K14/34 , C07K14/43518 , C07K14/445 , C07K16/082 , C07K16/1063 , C07K16/109 , C07K16/12 , C07K16/18 , C07K16/205 , C12N2740/16122 , C12N2770/24222 , G01N33/56905 , G01N33/576 , G01N33/68 , Y02A50/412 , Y10S530/806 , Y10S530/825 , Y10S530/826
摘要： Synthetic peptide antigen analogues of native peptide antigens with partial or complete retro, inverso or retro-inverso modifications are provided. When administered as an immunogen to an immunocompetent host the synthetic peptide antigen analogues induce the production of antibodies which recognize the native peptide antigen. Uses of these analogues, vaccines and methods of preparing vaccines comprising these antigen analogues, and antibodies generated using these antigen analogues are also provided.

4. 发明授权

EP0375040B1 Process for the preparation of retro-inverso peptides and new intermediates thereof 失效
标题翻译：一种制备逆反肽，及其中间产物的过程。
公开(公告)号：EP0375040B1
公开(公告)日：1994-03-16
申请号：EP89203194.9
申请日：1989-12-14
申请人： SCLAVO S.p.A.
发明人： Pinori, Massimo , Centini, Felice , Verdini, Antonio Silvio
IPC分类号： C07K1/02 , C07K1/12 , C07K5/02 , C07D319/06
CPC分类号： C07K1/02 , C07D319/06 , C07K5/0212

5. 发明授权

EP0253190B1 Partially retro-inverted tuftsin analogues, method for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：部分逆转TUFTSIN类似物，其制备方法和含有它们的药物组合物
公开(公告)号：EP0253190B1
公开(公告)日：1992-12-30
申请号：EP87109318.3
申请日：1987-06-29
申请人： ENIRICERCHE S.p.A. , SCLAVO S.p.A.
发明人： Verdini, Antonio Silvio , Bonelli, Fabio , Pessi, Antonello , Cardinali, Franco , Boraschi, Diana , Censini, Stefano , Di Trapani, Romano
IPC分类号： C07K5/02 , C07K1/00 , A61K37/02
CPC分类号： C07K5/0212 , C07C271/22 , C07C323/00

6. 发明公开

EP0347802A3 Neurokinin A antagonists 失效
标题翻译：神经刺激素
公开(公告)号：EP0347802A3
公开(公告)日：1991-07-17
申请号：EP89111108.0
申请日：1989-06-19
申请人： MERRELL DOW PHARMACEUTICALS INC.
发明人： Buck, Stephen H. , Krstenansky, John L. , McCarthy, James R. , Harbeson, Scott L. ,
IPC分类号： C07K7/02 , C07K1/00 , A61K37/02
CPC分类号： C07K5/0207 , A61K38/00 , C07K5/0212 , C07K7/22
摘要： Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.

7. 发明公开

EP0375040A3 Process for the preparation of retro-inverso peptides and new intermediates thereof 失效
标题翻译：制备逆转录酶的方法及其新的中间体
公开(公告)号：EP0375040A3
公开(公告)日：1991-07-03
申请号：EP89203194.9
申请日：1989-12-14
申请人： SCLAVO S.p.A.
发明人： Pinori, Massimo , Centini, Felice , Verdini, Antonio Silvio
IPC分类号： C07K1/02 , C07K1/12 , C07K5/02 , C07D319/06
CPC分类号： C07K1/02 , C07D319/06 , C07K5/0212
摘要： A method of synthesis of a partially retro-inverso peptide incorporating at least one malonyl residue of formula (III)
-CO- H-CO- (III)
wherein R represents the side chain of an α-amino acid, is described which is characterized in that said malonyl residue is incorporated by condensing a 5-substituted-2,2-dimethyl-1,3-dioxane-4,6-dione of formula (VI)
wherein R′ is the side-chain R wherein the functional groups, if any, are suitably protected, with an amino acid, amino acid amide, peptide fragment, or pseudo-peptide fragment wherein the terminal carboxyl group, if present, and the possible side-chain functionalities are suitably protected and the reactive amino group is tri-alkyl-silylated. The new compounds of formula (VI) and a process for the preparation of a partially retro-inverso tuftsin analog which involves use of said method and said intermediate are also described and claimed.

8. 发明公开

EP0384523A3 New gem-diamino derivatives and their use in the synthesis of retro-inverso peptides 失效
标题翻译：新型GEM-DIAMINO衍生物及其在逆转录酶合成中的应用
公开(公告)号：EP0384523A3
公开(公告)日：1991-05-15
申请号：EP90200352.4
申请日：1990-02-16
申请人： ENIRICERCHE S.p.A. , SCLAVO S.p.A.
发明人： Gazerro, Laura , Pinori, Massimo , Verdini, Antonio Silvio
IPC分类号： C07C235/10 , C07C235/78 , C07K1/06 , C07K5/02
CPC分类号： C07K1/063 , C07C235/20 , C07C235/34 , C07C237/20 , C07C237/22 , C07C271/22 , C07K5/0212
摘要： This invention relates to new gem-diamino derivatives of general formula (I)
where
R is the side chain of an amino acid, of which any functional groups are suitably protected, and X is an acyl group chosen from the group consisting of 2-nitro-benzoyl, 4-chloro-butyryl, acetoacetyl, 4-bromo-butyryl, (2-nitro-phenoxy)-acetyl and 2-methyl-2-(2'-nitro-phenoxy)propionyl, of use in introducing gem-diamino residues into retro-inverso peptides. The invention further relates to a method for the synthesis of retro-inverso peptides in which the gem-diamino residue or residues are introduced using the new compound (I).

9. 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。

10. 发明公开

EP0393786A1 New retro-inverse, one- or more bond bearing analogues of thymopentin, a method for synthesizing the same and their employment for the preparation of pharmaceutical 失效
标题翻译：逆反肽，Thymopenthin的类似物携带一个或多个键，它们的制备方法以及它们用于制备药物的用途。
公开(公告)号：EP0393786A1
公开(公告)日：1990-10-24
申请号：EP90200954.7
申请日：1990-04-18
申请人： SCLAVO S.p.A.
发明人： Mariotti, Sabina , Sisto, Alessandro , Nencioni, Luciano , Villa, Luigi , Verdini, Antonio Silvio , Pessi, Antonello
IPC分类号： C07K5/02 , A61K38/00 , A61K31/215
CPC分类号： C07K7/02 , A61K38/00 , C07K5/0212
摘要： New thymopentin (TP5) analogues are disclosed which contain in their peptide chain one or more retro-inverse bonds.
The new compounds have one of the following general formulas (I), (II) and (III)
wherein R is hydrogen or an acyl radical, and
R¹ is a group of the formula -OR² wherein R² is a hydrogen atom or a hydrocarbon radical,
and the corresponding acid or basic addition salts pharmaceutically acceptable.
Such new compounds have immunostimulating activity.
摘要翻译：新胸腺五肽（TP5）类似物游离缺失光盘包含哪些在其肽链的一个或多个逆 - 反键。新化合物具有下列通式（I）中的一个，（II）和（III） worin R是氢或基团的酰基，且R <1>是下式基团-OR <的 2> worinř<2>是氢原子或烃基，和相应的酸或碱加成盐可药用的。搜索新化合物具有免疫刺激活性。

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