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41. 发明公开

EP0387309A1 NEUE RENINHEMMER, VERFAHREN ZU DEREN HERSTELLUNG UND DEREN VERWENDUNG 失效
标题翻译：新的肾素抑制剂，工艺用于生产和用途。
公开(公告)号：EP0387309A1
公开(公告)日：1990-09-19
申请号：EP89906087.0
申请日：1989-05-09
申请人： SANDOZ AG , SANDOZ-PATENT-GMBH
发明人： WEIDMANN, Beat
IPC分类号： A61K31 , A61P9 , A61P31 , A61P43 , C07C237 , C07C271 , C07C275 , C07C327 , C07C333 , C07C335 , C07D213 , C07D295 , C07D521 , C07F7 , C07K5
CPC分类号： C07D295/088 , C07C237/22 , C07C271/22 , C07C327/42 , C07C327/44 , C07C333/04 , C07D213/30 , C07D213/82 , C07F7/0818 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/0212 , C07K5/0227
摘要： Composé de formule (I), où R1, W, R2, Z, A et B ont la notation donnée dans la revendication 1, procédé pour le fabriquer, et son emploi comme inhibiteur de la rénine dans le traitement de l'hypertension et de l'insuffisance cardiaque chronique ainsi que des maladies d'origine rétrovirale.

42. 发明公开

EP0384523A2 New gem-diamino derivatives and their use in the synthesis of retro-inverso peptides 失效
标题翻译： Gem-diamino-Derivate und ihre Verwendung bei der Herstellung von Retro-Inverso-Peptiden。
公开(公告)号：EP0384523A2
公开(公告)日：1990-08-29
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).
摘要翻译：本发明涉及通式（I）X-NH-H-NH 2（I）的新的偕二氨基衍生物，其中R是氨基酸的侧链，其中任何官能团都被适当地保护，X是选自2-硝基 - 苯甲酰基，4-氯 - 丁酰基，乙酰乙酰基，4-溴 - 丁酰基，（2-硝基 - 苯氧基） - 乙酰基和2-甲基-2-（2min - 苯氧基）丙酰基，用于将偕二氨基残基引入逆转肽。本发明还涉及一种用于合成其中使用新化合物（I）引入偕二氨基残基或残基的逆转肽的方法。

43. 发明公开

EP0347802A2 Neurokinin A antagonists 有权转让
标题翻译：神经激肽A-Antagonisten。
公开(公告)号：EP0347802A2
公开(公告)日：1989-12-27
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.
摘要翻译：描述了其中连接羧基末端上的两个氨基酸的酰胺键被修饰的天然存在的神经激肽A的衍生物的神经激肽A的拮抗剂。使用常规的竞争性结合和生物化学测定法以及常规生理测试证实了拮抗作用，并且还描述了在涉及神经激肽A的各种情况下使用这些衍生物。

44. 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.

45. 发明公开

EP0215410A3 Retro-inverso hexapeptide neurotensin analogs, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：逆转逆转录酶神经元模拟物，其制备方法和含有它们的药物组合物
公开(公告)号：EP0215410A3
公开(公告)日：1989-07-05
申请号：EP86112387.5
申请日：1986-09-08
申请人： ENIRICERCHE S.p.A.
发明人： Bonelli, Fabio , Pessi, Antonello , Verdini, Antonio Silvio
IPC分类号： C07K5/00 , C07K1/04 , C07K5/02 , A61K37/02
CPC分类号： C07K5/0212 , C07K1/06
摘要： Hexapeptides with vasodilating and hypotensive activity are described corresponding to the formula:
wherein :
X is a hydrogen atom or an acyl radical R₃-CO- wherein R₃ is a straight or branched (C₁-C₇) alkyl group,
R₁ and R₂, each independently, represent the side-chain residue of the amino acid glycine (-H), alanine (-CH₃),
Arg is the abbreviated designation for arginine,
Pro is the abbreviated designation for proline,
Tyr is the abbreviated designation for tyrosine,
and the pharmaceutically acceptable salts, lower alkyl esters and amides thereof, a process for their preparation and the pharmaceutical compositions containing them.

46. 发明公开

EP0254080A3 Malonic acid derivatives and methods for their synthesis 失效
标题翻译：马来酸衍生物及其合成方法
公开(公告)号：EP0254080A3
公开(公告)日：1989-05-31
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.

47. 发明公开

EP0185433A3 Retro-inverted peptides analogues of bradykinin potentiator BPP 5a 失效
标题翻译： BRADYKININ潜在剂BPP 5A的逆转肽类似物
公开(公告)号：EP0185433A3
公开(公告)日：1988-11-09
申请号：EP85202099
申请日：1985-12-18
申请人： ENICHEM S.p.A. , ENIRICERCHE S.p.A.
发明人： Sisto, Alessandro , Verdini, Antonio Silvio , Virdia, Antonino
IPC分类号： C07K05/00 , C07K05/02 , A61K37/02
CPC分类号： C07K5/0212
摘要： Retro-inverted peptides, analogues of Bradykinin Poten- (I) tiator Pentapeptide (BPP 5a ), definable by the general formula
useful as antihypertensives and diagnostics.

48. 发明授权

EP0097994B1 Method for the solid-phase synthesis of retro-inverso polypeptides 失效
标题翻译：用于反相多元醇固相合成的方法
公开(公告)号：EP0097994B1
公开(公告)日：1987-09-30
申请号：EP83200889.0
申请日：1983-06-17
申请人： ENICHEM S.p.A.
发明人： Pessi, Antonello , Pinori, Massimo , Verdini, Antonio Silvio , Viscomi, Giuseppe Claudio
IPC分类号： C07K1/04
CPC分类号： C07K1/042 , C07K5/0212

49. 发明授权

EP0127234B1 A retro-inverso analogue of the (5-14) decapeptide of equine angiotensinogen, as a specific renin inhibitor with high resistance to enzymatic hydrolysis 失效
标题翻译：作为具有高酶能水解功能的特异性RENIN抑制剂的（5-14）EQUINE ANGIOTENSINOGEN DECADEPTIDDE的逆转录反应
公开(公告)号：EP0127234B1
公开(公告)日：1987-09-23
申请号：EP84200710.6
申请日：1984-05-17
申请人： ENI-Ente Nazionale Idrocarburi
发明人： Pinori, Massimo , Verdini, Antonio Silvio
IPC分类号： C07K7/02 , C07K1/04 , C07K1/06
CPC分类号： C07K7/02 , A61K38/00 , C07K5/0212 , Y10S530/86 , Y10S930/32

50. 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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