专利号:US-6143722-A 优先权日:1996-11-26 标 题 :Heptapeptide oxytocin analogues 发明人:MELIN PER; NILSSON ANDERS; TROJNAR JERZY; AURELL CARL-JOHAN; RIVIERE PIERRE; HAIGH ROBERT 权利人:FERRING BV 摘要:PCT No. PCT/SE97/01968 Sec. 371 Date Aug. 2, 1999 Sec. 102(e) Date Aug. 2, 1999 PCT Filed Nov. 21, 1997 PCT Pub. No. WO98/23636 PCT Pub. Date Jun. 4, 1998Heptapeptide analogues or pharmaceutically acceptable salts thereof consist of a hexapeptide moiety S and a C-terminal beta -aminoalcohol residue Z bound to the moiety S by an amide bond, wherein the beta -aminoalcohol Z is -NR-CH(Q)-CH2OH, Q is (CH2)n-NH-A is H or -C(=NH)NH2, and R is CH3 or C2H5, and the moiety S wherein H is a D-aromatic alpha -aminoacid and Y is an aliphatic alpha -aminoacid and have oxytocin antagonist activity. Also disclosed is: a method of their synthesis; pharmaceutical compositions containing these analogues; the synthesis of such compositions; a method of control of uterine contractions.
专利号:US-5859190-A 优先权日:1997-02-04 标题 :Combinatorial libraries of hydantoin and thiohydantoin derivatives, methods of making the libraries and compounds therein 发明人:MEYER JEAN-PHILIPPE; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of hydantoin and thiohydantoin compounds. The present invention further provides the compounds made by the combinatorial synthesis.
专利号:US-11279734-B2 优先权日:2017-12-01 标 题:Solution-phase affinity selection of inhibitors from combinatorial peptide libraries 发明人:PENTELUTE BRADLEY L; TOUTI FAYCAL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., K D of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly). These inventive peptides were rapidly generated and identified using novel methods described herein comprising combinatorial peptide synthesis and/or solution affinity selection.
专利号:US-8338565-B2 优先权日:2008-08-20 标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha 发明人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P 权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP 摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.
专利号:CN-116535459-A 优先权日:2023-04-12 标题 :A kind of phenolic acid compound and its synthesis method and application
参考标题:Design And Synthesis Of Novel Prodrugs Of 2′-Deoxy-2′-Methylidenecytidine Activated By Membrane Dipeptidase Overexpressed In Tumor Tissues 作者:Yasunori Kohchi,Kazuo Hattori,Nobuhiro Oikawa,Eisaku Mizuguchi,Yoshiaki Isshiki,Kohsuke Aso,Kiyoshi Yoshinari,Haruyoshi Shirai,Masanori Miwa,Yukiko Inagaki,Masako Ura,Kotaroh Ogawa,Hisafumi Okabe,Hideo Ishitsuka,Nobuo Shimma |发布日期:2007.4 摘要:Dna Microarray Analysis Comparing Human Tumor Tissues With Normal Tissues Including Hematopoietic Progenitor Cells Resulted In Identification Of Membrane Dipeptidase As A Prodrug Activation Enzyme. Novel Prodrugs Of 2'-Deoxy-2'-Methylidenecytidine (Dmdc) Including Compound 23 That Are Activated By Membrane Dipeptidase (Mdp) Preferentially In Tumor Tissue Were Designed And Synthesized To Generate The
合成参考文献
参考文献:10.1007/978-1-0716-0227-0_14 摘要:Hamada Y, Ziora ZM. Peptidomimetic Synthesis: Drug Discovery for Alzheimer's Disease. Methods Mol Biol. 2020;2103():215–23. doi: 10.1007/978-1-0716-0227-0_14.