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参考文献:使用多销方法固相合成穆拉基二肽(mdp)衍生物.
标题:使用多销方法固相合成穆拉基二肽(mdp)衍生物.
摘要:报道了固相合成穆拉基二肽衍生物的方法.基于此药物筛选方法,可以通过酰化,还原烷基化,磺酰胺形成,尿素形成,N-烷基化,胺加成或组分ugi反应潜在地合成多样的穆拉基二肽文库.
DOI:10.1016/s0960-894X(00)00241-9
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专利信息
专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
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:US-12134664-B2
优先权日:2015-12-10
标 题:Muramyl peptide derivatives
发明人:ELLA KRISHNA MURTHY; BRUNDA GANNERU; KUMAR HALMUTHUR MAHABALARAO SAMPATH; REDDY PATURU RAMA SUBBA
权利人:BHARAT BIOTECH INT LTD; COUNCIL SCIENT IND RES; BHARAT BIOTECH INT LTD
摘要:The invention is directed to Muramyl Dipeptide (MDP) derivative compounds of structural Formula-VIII, a process for synthesis, intermediates used in the synthesis and use thereof: n nwherein, R can be a linear or branched alkyl, an aryl, a substituted aryl, or an 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:EP-3239139-B1
优先权日:2010-05-27
标题 :Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate