氯甲酸-9-芴基甲酯,3-(1-萘基)-L-丙氨酸置于sodium Carbonate体系中,化学反应生成 Fmoc-3-(1-萘基)-L-丙氨酸 参考文献:Cyclic Peptides As Selective Tachykinin Antagonists 标题:Cyclic Peptides As Selective Tachykinin Antagonists 摘要:Twenty Homodetic Cyclic Peptides Based On The C-Terminal Sequence Of Substance P Were Prepared (Table I) By A Combination Of Solid-Phase Techniques And Cyclizations Using Azide Coupling Incorporation Of Dipeptide Mimics Based On Substituted Gamma-Lactams Were Used In Some Cases To Restrict Their Conformational Mobility. Five Of These Cyclic Peptides Were Shown To Have High Tachykinin Antagonist Activity (Pa2 > 6) At Nk-2 Receptors (Rat Vas Deferens). The Two Most Potent Of This Series,Xvii,Cyclo(Gln-Trp-Phe-Gly-Leu-Met) (Pa2 = 8.1),And I Cyclo(Gln-Trp-Phe-(R)Gly[anc-2]Leu-Met) (Pa2 = 6.7),Were Selective For Nk-2 Receptors Compared With The Other Tachykinin Receptors (Table Ii). DOI:10.1021/jm00053A001
专利号:US-8598089-B2 优先权日:2003-12-17 标题 :Methods for synthesis of encoded libraries 发明人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A 权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC 摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
专利号:US-8410028-B2 优先权日:2003-12-17 标 题:Methods for synthesis of encoded libraries 发明人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A 权利人:MORGAN BARRY; HALE STEPHEN; ARICO-MUENDEL CHRISTOPHER C; CLARK MATTHEW; WAGNER RICHARD; ISRAEL DAVID I; GEFTER MALCOLM L; BENJAMIN DENNIS; HANSEN NILS JAKOB VEST; KAVARANA MALCOLM J; CREASER STEFFAN PHILLIP; FRANKLIN GEORGE J; CENTRELLA PAOLO A; ACHARYA RAKSHA A; GLAXOSMITHKLINE LLC 摘要:The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
专利号:US-8933195-B2 优先权日:2011-11-17 标题:Histone deacetylase inhibitors and synthetic method thereof and use thereof in manufacture of medicaments 发明人:JIANG SHENG; LI SHANG; YAO ZHIYI; YAO YIWU; ZHANG FENG; CHAO YANG; YE HAI; CHEN MIN 权利人:JIANG SHENG; LI SHANG; YAO ZHIYI; YAO YIWU; ZHANG FENG; CHAO YANG; YE HAI; CHEN MIN; NANJING YOKO BIOMEDICAL R & D LTD; NANJING XINGANG MEDICAL CO LTD; NANJING YOKO PHARMACEUTICAL CO LTD 摘要:The invention provides histone deacetylase (HDAC) inhibitors shown as Formula I, where R 1 to R 8 are as defined in the specification. The invention also provides methods for synthesis of these compounds and applications of these compounds in preparing pharmaceuticals for preventing or treating mammal diseases related to the dysregulation of HDAC.
专利号:US-2007042401-A1 优先权日:2003-12-17 标题 :Methods for synthesis of encoded libraries
专利号:EP-3515880-B1 优先权日:2017-03-17 标题:Methods and compositions for synthesis of encoded libraries 发明人:LI JIN; MORGAN BARRY A; Wan jinqiao; DOU DENGFENG; LIU GUANSAI; CHANG YONG; CHEN QIUXIA; WANG XING; XU YANSHAN; HU DONGYAN; LIU JIAN; CHENG XUEMIN 权利人:HITGEN INC
专利号:US-2020149034-A1 优先权日:2017-03-17 标题:Methods and Compositions for Synthesis of Encoded Libraries
参考标题:Synthesis And Biological Activity Of Peptide α-Ketoamide Derivatives As Proteasome Inhibitors 作者:Salvatore Pacifico,Valeria Ferretti,Valentina Albanese,Anna Fantinati,Eleonora Gallerani,Francesco Nicoli,Riccardo Gavioli,Francesco Zamberlan,Delia Preti,Mauro Marastoni |发布日期:2019.7.11 摘要:Proteasome Activity Affects Cell Cycle Progression As Well As The Immune Response, And It Is Largely Recognized As An Attractive Pharmacological Target For Potential Therapies Against Several Diseases. Herein We Present The Synthesis Of A Series Of Pseudodi/tripeptides Bearing At The C-Terminal Position Different α-Ketoamide Moieties As Pharmacophoric Units For The Interaction With The Catalytic Threonine
合成参考文献
参考文献:10.1007/s10534-013-9638-y 摘要:Morris G, Robertson I, Tatko CD. Iron binding β-hairpin peptides. Biometals. 2013 Oct;26(5):667–75. doi: 10.1007/s10534-013-9638-y.