L-苯甘氨酸置于platinum(Iv) Oxide 氢气,三乙胺体系中,用 1,4-二氧六环,乙醇,水,溶剂黄146 用作溶剂,45.0 °C,344.73 Kpa 条件下,反应 24.0H,反应生成Boc-L-环己基甘氨酸 参考文献:Cck-B Agonist Or Antagonist Activities Of Structurally Hindered And Peptidase-Resistant Boc-Cck4 Derivatives 标题:Cck-B Agonist Or Antagonist Activities Of Structurally Hindered And Peptidase-Resistant Boc-Cck4 Derivatives 摘要:Replacement Of Met31 By (N-Me)Nle In Cck8 Or Cck4 Has Been Shown To Improve The Affinity And Selectivity For Cck-B Receptors. In Order To Obtain Molecules With Enhanced Bioavailability,Two Novel Series Of Protected Tetrapeptides Of The General Formula Boc-Trp30-X-Asp-Y33 Have Been Developed. Introduction Of (N-Me)Nle And The Bulky,Aromatic Naphthylalaninamide (Nal-Nh2) In Positions X And Y,Respectively,Does Not Greatly Modify The Affinity For Guinea Pig Brain Cck-B Receptors. In Contrast,Incorporation Of Hindering N-Methyl Amino Acids Such As (N-Me)Phe,(N-Me)Phg,Or (N-Me)Chg,But Not Their Non-Methylated Counterparts,In Position X Induced A Large Decrease In Affinity For The Cck-B Binding Sites. Among The Various Peptides Synthesized,Boc-[(N-Me)Nle31,1Nal-Nh233]Cck4 (2) (K(I) = 2.8 Nm),Boc-[phg31,1Nal-Nh233]Cck4 (15) (K(I) = 14 Nm),And Boc-[phg31,1Nal-N(Ch3)233]Cck4 (17) (K(I) = 39 Nm) Displayed Good Affinities For Brain Cck-B Receptors And Had Good Selectivity Ratios. These Pseudopeptides,In Which The Presence Of Unnatural And Hydrophobic Residues Is Expected To Improve Their Penetration Of The Central Nervous System,Were Shown To Be Very Resistant To Brain Peptidases. Interestingly,Whereas Compounds 2 And 15 Proved To Be Full Agonists For Rat Hippocampal Cck-B Receptors When Measured In An Electrophysiological Assay,Compound 17 Behaved As A Potent Antagonist In The Same Test And Displayed A Good Affinity In Rat Brain K(I)(Cck-B) = 51 Nm As Compared To The Merck Antagonist L365,260,K(I)(Cck-B) = 12 Nm. This Illustrates A Simple Means To Obtain Cck-B Antagonists And Suggests That The Free,Conh2 Group Plays A Critical Role In The Recognition Of The Agonist Date Of Brain Cck-B Receptors. Doi:10.1021/jm00053A022
专利信息
专利号:US-6552166-B1 优先权日:1999-10-19 标 题:Process for the preparation of conjugates useful in the treatment of prostate cancer 发明人:LYNCH JOSEPH E; ROBBINS MICHAEL A; SHI YAO-JUN; LIEBERMAN DAVID R 权利人:MERCK & CO INC 摘要:The present invention is directed to the improved synthesis of compounds of formula I:which may be useful in the treatment of prostate cancer. Such compounds are synthesized in the presence of a carboxyl activating agent, an additive and a base for the preparation of a PSA conjugate which comprises an anthracycline antibiotic and an oligopeptide.
专利号:US-7262169-B1 优先权日:1999-10-19 标 题 :Process for preparing peptide intermediates 发明人:ASHWOOD MICHAEL STEWART; BISHOP BRIAN CHRISTOPHER; COTTRELL IAN FRANK; EMERSON KHATEETA MONEEK; HANDS DAVID; HO GUO JIE; LYNCH JOSEPH EDWARD; SHI YAO JUN; WILSON ROBERT DARRIN 权利人:MERCK SHARP & DOHME 摘要:The present invention is directed to the improved synthesis of compounds of formula (I) an intermediate compound which is useful in the synthesis of the anticancer agents known as PSA conjugates.
专利号:US-10906033-B2 优先权日:2016-03-28 标题 :Synthesis and application of chiral substituted polyvinylpyrrolidinones 发明人:HUA DUY H 权利人:UNIV KANSAS STATE 摘要:Chiral polyvinylpyrrolidinone (CSPVP), complexes of CSPVP with a core species, such as a metallic nanocluster catalyst, and enantioselective oxidation reactions utilizing such complexes are disclosed. The CSPVP complexes can be used in asymmetric oxidation of diols, enantioselective oxidation of alkenes, and carbon-carbon bond forming reactions, for example. The CSPVP can also be complexed with biomolecules such as proteins, DNA, and RNA, and used as nanocarriers for siRNA or dsRNA delivery.
专利号:WO-2025008732-A1 优先权日:2023-07-03 标 题 :Novel compounds as modulators of il17 发明人:DESAI RANJIT; DESAI JIGAR 权利人:ZYDUS LIFESCIENCES LTD 摘要:The present invention relates to novel compounds of general formula (1), their suitable pharmaceutically acceptable salts, their solvates, their hydrates, their stereoisomers, their polymorphs, their racemic mixtures, their optically active forms and their use in the treatment of inflammatory conditions such as psoriasis, asthma, psoriatic arthritis or rheumatoid arthritis. Further, the present invention relates to processes of preparing such compounds, novel intermediates involved in their synthesis.
专利号:JP-2001503782-A 优先权日:1996-11-22 标题 :Method and compound for inhibiting release of beta-amyloid peptide and / or its synthesis
专利号:US-2020306737-A1 优先权日:2016-03-28 标 题:Synthesis and application of chiral substituted polyvinylpyrrolidinones