中文摘要：本发明公开了一种嘧啶化合物及其盐类；该化合物的组成为X、R1、R2、R3、R4、R5、R6、Y1、Y2、L和m；该化合物及其盐类可用作疫苗佐剂。
 
外文摘要：The present invention provides a compound represented by formula (1) (in the formula, X, R1, R2, R3, R4, R5, R6, Y1, Y2, L, and m are as defined in the description) and a pharmaceutically acceptable salt thereof, which are useful as a vaccine adjuvant.
NOVELTY - A pyrimidine compound (I) or (II) is new.
USE - New pyrimidine compound is used in pharmaceutical composition and in vaccine adjuvant to improve antigen-specific immunoreaction in mammal (all claimed).
主权项： A pyrimidine compound of formula (I) or (II) or its salt, is new.
A=group of formula (i);
X=methylene, O, S, SO, SO2 or NR7;
R7=H or 1-3C alkyl;
R1,R2=H or 1-6C alkyl optionally substituted by hydroxy, halo or 1-6C alkoxy;
R3=1-6C alkyl, a 1-6C alkoxy or 1-6C alkylthio;
R4=H, halo, hydroxy, 1-6C alkyl, 1-6C alkoxy or cyano;
Y1=single bond, -(CR9R10)p-, -CH=CH-(CR9R10)q-, -CC-(CR9CR10)q'- or -(CR9R10)r-O-(CR'9R'10)r'-;
R9,R10,R'9,R'10=H or 1-4C alkyl;
Y'2=single bond or -C(O)-;
L=2-6C linear alkylene or bivalent 4-8 membered cycloalkane (both optionally substituted by 1-4 1-5C alkyl, hydroxy, carbonyl or halo);
R5,R6=H or optionally substituted 1-6C alkyl;
R5+R6+L=4-8 membered! nitrogen-containing saturated heterocyclic ring;
m=0 or 1; p=1-6; q,q'=0-4; r=0-5; r'=1-5; r+r'=5 or less; andR8=H or amino.
(i) When the 1-6C alkyl is substituted by hydroxy or halo, the 4-8 membered nitrogen-containing saturated heterocyclic ring is optionally substituted by 1-4 substituents chosen from methyl, ethyl, propyl, hydroxymethyl, hydroxyethyl, carbonyl, hydroxy or halo; and (ii) When Y'2 is a single bond, r' is 2 or more, single bond or double bond. INDEPENDENT CLAIMS are included for the following:
(1) pharmaceutical composition, which contains the compound (I);
(2) vaccine adjuvant, which contains the compound (I);
(3) method to reinforce the antigen-specific immunoreaction in a mammal, which involves administering the compound (I) to the mammal; and
(4) method to improve the immune-response ability of the mammal, which involves administering the compound (I) to the mammal.
申请号：WO2016JP79756
公开/公告号：WO2017061532A1
申请日：2016-10-06
公开/公告日：2017-04-13
申请/专利权人：SUMITOMO DAINIPPON PHARMA CO LTD (SUMU-C)
发明/设计人：BAN, H;ISOBE, Y;KIMURA, H;WATANABE, H
分类号：A61K39/00; A61K39/39; C07D239/49
主分类号： A61K39/00; A61K39/39; A61P37/04; C07D239/49
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