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    • 5. 发明申请
    • NEW ANTIBACTERIAL COMPOUNDS AND BIOLOGICAL APPLICATIONS THEREOF
    • 新抗菌化合物及其生物应用
    • WO2014067904A1
    • 2014-05-08
    • PCT/EP2013/072526
    • 2013-10-28
    • LABORATOIRE BIODIM
    • ATAMANYUK, DmytroGERUSZ, VincentMOREAU, FrançoisHENRYON, VivienMONBRUN, JérômeAIRIAU, Etienne
    • C07F9/09A61K31/661A61P31/04
    • C07F9/09A61K31/661A61K45/06C07F9/091C07F9/38Y02A50/473Y02A50/475Y02A50/481A61K2300/00
    • The invention relates to compounds of formulae (Ia), (Ib) or (Ic) wherein, - A 1 and A 2 , identical or different, are H, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) fluoroalkyl, (C 2 -C 6 ) alkenyl, (C 2 -C 6 ) alkynyl, (C 1 -C 6 ) alkyl-OR a , (C 1 -C 6 ) alkyl-SR a , (C 1 -C 6 ) alkyl-NR a R b , OR a , SR a , NR a R b , or COR a ; - A 3 is H, OH or form a carbonyl with A 4 ; - A 4 is H, OH or form a carbonyl with A 3 ; - A 5 is H, CR a R b OH, F, OH or forms a double bond with X in the case where X is CH; - A 6 is H or F; - X is CH 2 , CHF, CF 2 , CHOH, O, S, NR a or a simple bond, or X is CH in the case where A 5 forms with X a double bond; - Y is P(O) (OR a ) (OR b ) or P (O) (OR a ) (NR a R b ); - V is O or S; - A 7 is H, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) fluoroalkyl, (C 2 -C 6 ) alkenyl, (C 2 -C 6 ) alkynyl or (C 1 -C 6 ) alkyl-OR a ; - A 8 is OH or H, - R a and R b , identical or different, are H, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) fluoroalkyl, (C 1 -C 6 ) alkyl-OH or (C 1 -C 6 ) alkyl-O- (C 1 - C 6 ) alkyl; and their addition salts thereof with acids and bases, their preparation and their use in the antibacterial prevention and therapy, used alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity.
    • 本发明涉及式(Ia),(Ib)或(Ic)化合物,其中-A1和A2相同或不同,为H,(C1-C6)烷基,(C1-C6)氟烷基,(C2-C6 ),(C 1 -C 6)烷基-OR a,(C 1 -C 6)烷基-SRa,(C 1 -C 6)烷基-NR a R b,OR a,SR a,NR a R b或COR 3; - A3是H,OH或与A4形成羰基; - A4是H,OH或与A3形成羰基; 在X为CH的情况下,A5为H,CRaRbOH,F,OH或与X形成双键; - A6是H或F; - X为CH 2,CHF,CF 2,CHOH,O,S,NR a或简单键,或者X为CH时,X为双键; - Y是P(O)(OR a)(OR b)或P(O)(OR a)(NR a R b); - V是O或S; A7为H,(C1-C6)烷基,(C1-C6)氟代烷基,(C2-C6)烯基,(C2-C6)炔基或(C1-C6)烷基-ORa; - A8是OH或H,-Ra和Rb相同或不同,是H,(C1-C6)烷基,(C1-C6)氟代烷基,(C1-C6)烷基-OH或(C1-C6)烷基-O - (C 1 -C 6)烷基; 以及它们与酸和碱的加成盐,它们的制备及其在抗菌预防和治疗中的用途,其单独使用或与抗菌素,抗毒性药物或增强宿主先天免疫力的药物联合使用。