D-谷氨酸置于trifluoroborane Diethyl Ether,三乙胺体系中,用 四氢呋喃,苯甲醇 用作溶剂,化学反应生成D-谷氨酸-5-苄酯 参考文献:Chemical Synthesis And Anti-Tumor And Anti-Metastatic Effects Of Dual Functional Conjugate 标题:Chemical Synthesis And Anti-Tumor And Anti-Metastatic Effects Of Dual Functional Conjugate 摘要:本发明披露了一种双重功能的共轭物的化学合成,抗肿瘤和抗转移作用,如公式i所示.具体来说,紫杉醇或多西他赛与杆菌二肽衍生物结合形成共轭物,从而通过化疗和免疫疗法的结合实现双重抗肿瘤和抗转移作用.本发明还披露了紫杉醇或多西他赛和杆菌二肽衍生物共轭物的合成是通过固相和溶液相合成的组合实现的,并且所述共轭物可以用于制造抗肿瘤药物,这已经通过可靠的生物测定证明.
专利号:US-8212002-B2 优先权日:2008-08-07 标 题:Synthesis of glatiramer acetate 发明人:HSIAO TSUNG-YU; HO MENG-FEN 权利人:HSIAO TSUNG-YU; HO MENG-FEN; SCINOPHARM TAIWAN LTD 摘要:A process of making a polylpeptide or a pharmaceutically acceptable salt thereof comprises reacting a L-lysine protected polypeptide, which comprises L-alanine, L-tyrosine, L-glutamate, and L-lysine that is protected with a protecting group, with a tetraalkylammonium hydroxide in water to remove the protecting group.
专利号:US-10927147-B2 优先权日:2015-12-10 标 题:Muramyl peptide derivative compound, synthesis and uses thereof 发明人:ELLA KRISHNA MURTHY; BRUNDA GANNERU; KUMAR HALMATHUR MAHABALARAO SAMPATH; SREEKANTH MIRYALA 权利人:BHARAT BIOTECH INT LTD; COUNCIL SCIENT IND RES 摘要:The invention relates to novel Muramyl Dipeptide (MDP) derivative compound of structural Formula-VIII, a process for synthesis, intermediates used in the synthesis and use thereof. n n n n n n n n n n Wherein, R can be both linear and branched alkyl, aryl, substituted aryl and alkoxy alkyl. These compounds possess excellent pharmacological properties, in particular immunomodulating properties for use as adjuvant in vaccine formulations. These compounds are, particularly useful as adjuvants in vaccines.
专利号:US-9085605-B2 优先权日:2010-05-27 标 题:Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate 发明人:LIU GANG; ZHAO NAN; MA YAO 权利人:LIU GANG; ZHAO NAN; MA YAO; SHENZHEN SALUBRIS PHARM CO LTD 摘要:The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.
专利号:US-10576147-B2 优先权日:2015-12-15 标题:Muramyl peptide derivative compound, synthesis and uses thereof 发明人:ELLA KRISHNA MURTHY; BRUNDA GANNERU; KUMAR HALMATHUR MAHABALARAO SAMPATH; SREEKANTH MIRYALA 权利人:BHARAT BIOTECH INT LTD; COUNCIL SCIENT IND RES 摘要:The invention relates to novel Muramyl Dipeptide (MDP) derivative compound of structural Formula-VIII, a process for synthesis, intermediates used in the synthesis and use thereof; n nwherein R 1 and R 2 both are hydrogen; or R 1 is hydrogen and R 2 is alkyl or aryl; or R 1 is alkyl or aryl and R 2 is hydrogen; or R 1 and R 2 both are alkyl or aryl (same or different groups); wherein alkyl group constitute C1-C6 alkyl or higher (both linear and branched) with or without heteroatoms; and aryl group constitute phenyl, substituted phenyl, heteraryl, arylalkyl and polynuclear aromatics. These compounds possess excellent pharmacological properties, in particular immunomodulating properties for use as adjuvant in vaccine formulations. These compounds are, particularly useful as adjuvants in vaccines.
专利号:JP-2011530523-A 优先权日:2008-08-07 标题:Synthesis of glatiramer acetate
专利号:EP-2326657-B1 优先权日:2008-08-07 标 题 :Synthesis of glatiramer acetate
参考标题:Proximity-Induced Cooperative Polymerization In "Hinged" Helical Polypeptides 作者:Chongyi Chen,Hailin Fu,Ryan Baumgartner,Ziyuan Song,Yao Lin,Jianjun Cheng |发布日期:2019.6.5 摘要:N-Carboxyanhydrides (Ncas) With Initiators Structurally As Simple As Linear Aliphatic Diamines For The Synthesis Of Polypeptides. The Polymerization Initiated By Diamines Proceeds Via The Formation Of "Hinged" Polypeptides, Which Are Two Blocks Of Helical Chains Connected Head-To-Head By The Diamine Molecules In The Polymerization Solution. The Reactions Follow A Two-Stage, Cooperative Polymerization