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1. 发明授权

EP0375058B1 New retro-inverso analogues of trymopentin, the method for their synthesis and their use in the preparation of pharmaceutical compositions 失效
标题翻译：逆反Thrymopentin类似物，它们的制备方法和它们的药物组合物的制备中的用途。
公开(公告)号：EP0375058B1
公开(公告)日：1994-03-16
申请号：EP89203230.1
申请日：1989-12-18
申请人： SCLAVO S.p.A.
发明人： Mariotti, Sabina , Sisto, Alessandro , Nencioni, Luciano , Villa, Luigi , Verdini, Antonio Silvio
IPC分类号： C07K5/02 , C07K7/02
CPC分类号： C07K5/0212 , A61K38/00 , C07K7/02

2. 发明授权

EP0282891B1 New thymopentin retro-inverso analogs and fragments thereof, a process of preparation of the new compounds and the intermediates obtained therein 失效
标题翻译：胸腺五肽逆反类似物和其片段，它们的制备方法和中间体如此获得。
公开(公告)号：EP0282891B1
公开(公告)日：1994-01-26
申请号：EP88103699.0
申请日：1988-03-09
申请人： ENIRICERCHE S.p.A. , SCLAVO S.p.A.
发明人： Sisto, Alessandro , Verdini, Antonio Silvio
IPC分类号： C07K5/02 , C07K7/02
CPC分类号： C07K5/0212

3. 发明公开

EP0253190A3 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：EP0253190A3
公开(公告)日：1989-10-04
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
摘要： New partially retro-inverted tuftsin analogues of general formula I
wherein
R represents the side-chain of the amino acids threonine, methionine or leucine
R¹ represents the side-chain of the amino acids lysine or arginine
R² is hydrogen or a metabolically labile acyl group,
all the asymmetric carbon atoms are either of the S- or R-configuration, or, alternatively, the first, third, and fourth asymmetric carbons, starting from the N-terminal residue, are of the S-configuration while the second one is of the R- or (R,S)-configuration, and the corresponding pharmacologically acceptable salts, esters and amides. The new compounds which share the same pharmacological properties of tuftsin, are much more stable toward the enzymatic degradation than the parent molecule.

4. 发明公开

EP0253190A2 Partially retro-inverted tuftsin analogues, method for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：部分地逆转化的它们的制备方法和含有它们的药物组合物的促吞噬肽类似物，方法。
公开(公告)号：EP0253190A2
公开(公告)日：1988-01-20
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
摘要： New partially retro-inverted tuftsin analogues of general formula I
wherein
R represents the side-chain of the amino acids threonine, methionine or leucine
R¹ represents the side-chain of the amino acids lysine or arginine
R² is hydrogen or a metabolically labile acyl group,
all the asymmetric carbon atoms are either of the S- or R-configuration, or, alternatively, the first, third, and fourth asymmetric carbons, starting from the N-terminal residue, are of the S-configuration while the second one is of the R- or (R,S)-configuration, and the corresponding pharmacologically acceptable salts, esters and amides.
The new compounds which share the same pharmacological properties of tuftsin, are much more stable toward the enzymatic degradation than the parent molecule.
摘要翻译：新的通式部分逆转化的促吞噬肽类似物I worinřdarstellt氨基酸苏氨酸，甲硫氨酸或亮氨酸的R侧链<1> darstellt氨基酸赖氨酸或精氨酸 - [R <2>的侧链是氢或代谢不稳定的酰基，所有的不对称碳原子的是无论是S-或R-构型，或，可选地，所述第一，第三和第四不对称碳原子，从N末端残基开始，是的 S-构型，而第二个是R或（R，S） - 构型，以及相应的药理学上可接受的盐，酯和酰胺的。共享促吞噬肽的相同的药理学性质的新的化合物，要稳定得多朝向比母体分子的酶促降解。

5. 发明公开

EP0375058A3 New retro-inverso analogues of trymopentin, the method for their synthesis and their use in the preparation of pharmaceutical compositions 失效
标题翻译：新戊酰胺的新型逆转录酶类似物，其合成方法及其在制备药物组合物中的应用
公开(公告)号：EP0375058A3
公开(公告)日：1991-06-12
申请号：EP89203230.1
申请日：1989-12-18
申请人： SCLAVO S.p.A.
发明人： Mariotti, Sabina , Sisto, Alessandro , Nencioni, Luciano , Villa, Luigi , Verdini, Antonio Silvio
IPC分类号： C07K5/02 , C07K7/02
CPC分类号： C07K5/0212 , A61K38/00 , C07K7/02
摘要： New analogues of thymopentin (TP5) and of its tetrapeptide fragment (TP5¹⁻⁴) containing two non-contiguous retro-inverted bonds in the peptide chain are described. The new compounds, of general formula (I)
where R is hydrogen or an acyl radical,
and R¹ is an -OR² group or an
group where R² is a hydrogen atom or a hydrocarbon radical, and R³ is a hydrogen atom or a hydroxyl group,
and the corresponding pharmaceutically acceptable salts of acid or basic addition, possess immunomodulating activity.

6. 发明公开

EP0375040A2 Process for the preparation of retro-inverso peptides and new intermediates thereof 失效
标题翻译： Verfahren zur Herstellung von Retro-Inverso-Peptiden und dessen Zwischenprodukte。
公开(公告)号：EP0375040A2
公开(公告)日：1990-06-27
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.
摘要翻译：一种合成部分逆转肽的方法，其包含至少一种式（III）-CO-H-CO-（III）的丙二酰残基，其中R表示α-氨基酸的侧链，其是其特征在于所述丙二酰残基通过将式（VI）的5-取代-2,2-二甲基-1,3-二恶烷-4,6-二酮缩合成CHEM，其中R min是侧链R，其中如果有的话，官能团被适当地保护，其中氨基酸，氨基酰胺，肽片段或假肽片段，其中如果存在末端羧基，并且可能的侧链官能团被适当地保护，并且反应性氨基是三烷基甲硅烷基化的。还描述和要求保护新的式（VI）化合物和涉及使用所述方法和所述中间体的部分逆转型绒毛蛋白类似物的制备方法。

7. 发明公开

EP0282891A3 New thymopentin retro-inverso analogs and fragments thereof, a process of preparation of the new compounds and the intermediates obtained therein 失效
标题翻译：新的三烯酚改性逆转录酶及其片段，新化合物的制备方法及其获得的中间体
公开(公告)号：EP0282891A3
公开(公告)日：1990-05-23
申请号：EP88103699.0
申请日：1988-03-09
申请人： ENIRICERCHE S.p.A. , SCLAVO S.p.A.
发明人： Sisto, Alessandro , Verdini, Antonio Silvio
IPC分类号： C07K5/02 , C07K7/02
CPC分类号： C07K5/0212
摘要： New retro-inverso analogs of thymopentin (TP5) and of its tripeptide fragment (TP5¹⁻³) of general formula (I)
are described wherein R is hydrogen or an acyl radical, and R¹ is -OR² or
wherein R² is hydrogen or a hydrocarbyl radical, and the corresponding pharmaceutically acceptable acid- or base-addition salts. The new compounds are enzyme-resistant immunomodulatory peptides.

8. 发明公开

EP0277561A1 New arginine derivative, process for the preparation thereof and its use in peptide synthesis 失效
标题翻译： Argininderivat，Verfahren zu seiner Herstellung und seine Verwendung in der Peptidsynthese。
公开(公告)号：EP0277561A1
公开(公告)日：1988-08-10
申请号：EP88100919.5
申请日：1988-01-22
申请人： ENIRICERCHE S.p.A. , SCLAVO S.p.A.
发明人： Caciagli, Valerio , Verdini, Antonio Silvio
IPC分类号： C07C279/04 , C07C279/18 , C07D249/18 , C07K1/06
CPC分类号： C07D249/18 , C07C2603/18 , C07K1/02
摘要： N α -fluorenylmethoxycarbonyl-N G -trityl-arginine, a new protected arginine derivative, and its use in peptide syntheses are described.
The new compound can be prepared by a three step process, via formation of N α -trityl-N G -trityl-arginine, selective mono-deprotection of said intermediate, and introduction of the fluorenylmethoxycarbonyl group on the amino function.
摘要翻译：描述了新的受保护的精氨酸衍生物及其在肽合成中的应用，其中N'-芴基甲氧羰基-N， - 三苯甲基 - 精氨酸。新化合物可以通过三步法制备，通过形成N， - 三苯甲基-N， - 三苯甲基 - 精氨酸，所述中间体的选择性单取代保护，并将氨基官能团上引入芴基甲氧基羰基。

9. 发明公开

EP0254080A2 Malonic acid derivatives and methods for their synthesis 失效
标题翻译： Malonsäurederivateund ihre Synthesemethoden。
公开(公告)号：EP0254080A2
公开(公告)日：1988-01-27
申请号：EP87109317.5
申请日：1987-06-29
申请人： ENIRICERCHE S.p.A. , SCLAVO S.p.A.
发明人： Di Trapani, Romano , Verdini, Antonio Silvio
IPC分类号： C07C69/34 , C07C69/734 , C07C67/343 , C07C323/57 , C07C319/18 , C07C271/10
CPC分类号： C07K5/0212 , C07C271/22 , C07C323/00 , Y02P20/55
摘要： The present invention refers to a new class of malonic acid derivatives of general formula I
wherein R¹ and R², each independently, represent hydrogen or a carboxyl protecting group, and the residue R corresponds to the side-chain of the amino acids lysine, ornithine, tyrosine, cysteine, aspartic acid and glutamic acid wherein the additional functionalities are suitably protected.
The new compounds of the present invention are useful for preparing analogues of biologically active peptides wherein the direction of some amide bonds in which the amino acids lysine, ornithine, tyrosine, cysteine, aspartic acid or glutamic acid are involved, has been reversed.
摘要翻译：本发明涉及一类新的通式I 的丙二酸衍生物，其中R 1和R 2各自独立地代表氢或羧基保护基，残基R对应于侧 - 氨基酸赖氨酸，鸟氨酸，酪氨酸，半胱氨酸，天冬氨酸和谷氨酸的链，其中额外的官能团被适当地保护。本发明的新化合物可用于制备生物活性肽的类似物，其中涉及氨基酸赖氨酸，鸟氨酸，酪氨酸，半胱氨酸，天冬氨酸或谷氨酸的一些酰胺键的方向已被逆转。

10. 发明公开

EP0190597A2 Retro-inverso analogs of the bradykinin potentiating peptide bpp 5a 失效
标题翻译： Retro-Inverso-Analoga von Peptid BPP5a mit Bradykinin-Wirkung。
公开(公告)号：EP0190597A2
公开(公告)日：1986-08-13
申请号：EP86100676.5
申请日：1986-01-20
申请人： SCLAVO S.p.A.
发明人： Sisto, Alessandro , Verdini, Antonio Silvio , Virdia, Antonino
IPC分类号： C07K5/00 , C07K5/06 , A61K37/02
CPC分类号： C07K5/0212
摘要： New partially retro-inverso peptides of the following
general formula wherein R' and R' are the same or different and represent, each independently, the side chain of the aminoacid residues present in the naturally occuring peptides, X is -S-Ph pr -O-CH 2 -Ph and Z is a hydroxy, alkoxy or amino group, ate described as well as a suitable method for their preparation. The new compounds are useful as antihypertensive agents.
摘要翻译：下列通式的新的部分逆转型肽其中R 1和R 2相同或不同，各自独立地表示存在于天然存在的肽中的氨基酸残基的侧链，X 是-S-Ph或-O-CH2-Ph，Z是羟基，烷氧基或氨基，以及它们制备的合适的方法。新化合物可用作抗高血压药。

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