中文摘要：本发明公开了一种胞壁酰二肽（MDP）衍生物、结构及其合成过程，该衍生物结构为Formula-VIII。在Formula-VIII结构中，R1和R2均为氢结构，或者R1为氢结构、R2为烃基或芳基，或R1为烃基或芳基、R2为氢基，或者R1\R2均为烃基或芳基；烃基集团由C1-C6烃基组成或更高碳原子数烃基组成，可以包含也可以不包含杂原子；芳基基团由苯基、芳香基、芳基、多环芳香烃组成。这些化合物具有优秀的药理学特征，能够作为疫苗佐剂起到特殊的免疫调控作用。
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; (Formula VIII) wherein R1 and R2 both are hydrogen; or R1 is hydrogen and R2 is alkyl or aryl; or R1 is alkyl or aryl and R2 is hydrogen; or R1 and R2 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.
NOVELTY - A muramyl dipeptide derivative compound (VIII) is new.
USE - The muramyl dipeptide derivative compound is used as adjuvant in vaccine formulation with antigen e.g. live attenuated vaccine antigen, inactivated vaccine antigen, subunit vaccine antigen, conjugate vaccine antigen and recombinant vaccine antigen. The vaccine formulation is chosen from bacterial vaccine, viral vaccine, and potential infectious pathogens against mammals (all claimed). The muramyl dipeptide derivative compound is used for providing immunomodulating activity, and treating chronic infections, autoimmune diseases, cancer and infectious diseases e.g. tuberculosis, ophthalmic herpetic infection, psoriasis, ulcer and inflammation.
ADVANTAGE - The muramyl dipeptide derivative has excellent pharmacological activity, preferably adjuvant activity for vaccine formulations.
主权项：DETAILED DESCRIPTION - A muramyl dipeptide derivative compound of formula (VIII) is new.
R1=H;
R2=alkyl or aryl;
or R1=alkyl or aryl;
R2=H; and
or R1,R2=alkyl or aryl, where linear and branched 1-6C alkyl or higher with or without heteroatoms, and aryl is optionally substituted phenyl, heteraryl, arylalkyl or polynuclear aryl.
INDEPENDENT CLAIMS are included for the following:
(1) preparation of compound (VIII);
(2) hydroxyl group-containing amide compound of formula (V);
(3) carboxylic acid group-containing amide compound of formula (VI);
(4) peptide compound of formula (VII); and
(5) vaccine formulation, which comprises compound (VIII) as an adjuvant.
申请号：WO2016IN50440
公开/公告号：WO2017103944A1
申请日：2016-12-10
公开/公告日：2017-06-22
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