中文摘要：本发明提供了一种新型胞壁酰二肽衍生化合物，合成过程、成分及其应用。该化合物具有较好的药理作用，尤其是一种可作为疫苗佐剂的免疫调控作用。该化合物能作为抗菌、抗病毒或哺乳动物其它抗原疫苗的佐剂进行应用。
外文摘要：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. R = alkyl (both linear and branched), aryl, substituted aryl, alkoxy alkyl 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.
NOVELTY - A muramyl dipeptide derivative (I), is new.
USE - The muramyl dipeptide derivative of formula (I) is useful as adjuvant in vaccine formulation chosen from bacterial vaccine, viral vaccine or any potential infectious pathogens against mammals (all claimed).
ADVANTAGE - The muramyl dipeptide derivative of formula (I) has reduced pyrogenicity, while maintaining a considerable functionality as vaccine adjuvants, and cytotoxicity.
 
主权项：A muramyl dipeptide derivative of formula (I), is new.
R=both alkyl linear and branched, aryl, substituted aryl or alkoxy alkyl.
INDEPENDENT CLAIMS are included for the following:
(1) method for preparing muramyl dipeptide derivative;
(2) mannopyranoside compound of formula (V);
(3) carbamate compound of formula (VI);
(4) propanoic acid compound of formula (VII);
(5) use of muramyl dipeptide derivative as an adjuvant in vaccine formulation with antigen chosen  from live attenuated vaccine antigen, inactivated vaccine antigen, subunit vaccine antigen, a conjugate vaccine antigen and recombinant vaccine antigen or their combinations; and
(6) vaccine formulation comprising muramyl dipeptide derivative of formula (I), preferably (4R)-5-amino-4-((2S)-2-((2R)-2-(((3R,4R,5S,6R)-3-((ethoxycarbonyl)amino)-2,5- dihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-4-yl)oxy)propanamido)propanamido)-5-oxopentanoic acid (MDP-ET) as an adjuvant.
申请号：WO2016IN50436
公开/公告号：WO2017098529A1
申请日：2016-12-06
公开/公告日：2017-06-15
申请/专利权人：BHARAT BIOTECH INT LTD (BHAR-N); COUNCIL SCI & IND RES INDIA (COUI-C)
发明/设计人：ELLA, K M;BRUNDA, G;KUMAR, H M S;SREEKANTH, M
分类号：A61K38/14; C07K9/00; C07K9/005
主分类号：A61K38/14; C07K9/00
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