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    • 3. 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。
    • 5. 发明申请
    • PURINE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS FOR PREVENTION OR TREATMENT OF BACTERIAL INFECTIONS
    • 嘌呤衍生物及其作为预防或治疗细菌感染的药物
    • WO2012172043A1
    • 2012-12-20
    • PCT/EP2012/061428
    • 2012-06-15
    • LABORATOIRE BIODIMATAMANYUK, DmytroDENIS, AlexisGERUSZ, VincentLEDOUSSAL, BenoîtBONVIN, YannickDESROY, NicolasGOLD, JohanMOREAU, FrançoisOXOBY, Mayalen
    • ATAMANYUK, DmytroDENIS, AlexisGERUSZ, VincentLEDOUSSAL, BenoîtBONVIN, YannickDESROY, NicolasGOLD, JohanMOREAU, FrançoisOXOBY, Mayalen
    • C07D473/32A61K31/52A61P31/04
    • C07D473/32
    • The invention relates to the compounds of general formula (I) and their addition salts thereof with acids and bases: wherein A is phenyl, naphthyl and 5-10 membered monocyclic or bicyclic unsaturated heterocycle, optionally substituted by a group R1 which is as defined in the application and is itself optionally substitutes by a group R2 which is as defined in the application and is itself optionally substituted by a group R3 which is defined in the application, Y and W, identical or different, are H, (C 1 -C 6 ) alkyl, (C 2 -C 6 ) alkenyl, (C 2 -C 6 ) alkynyl, phenyl or 4-10 monocyclic or bicyclic saturated or unsaturated heterocycle, optionally substituted by R1, or Y and/or W form a 4-10 membered cycle with R1, or Y and W form with N a saturated or unsaturated nitrogenous 4-10 membered mono, bi or tricyclic system, fused, bridged or spiro system, said system being optionally substituted by R1, said system being different from morpholine, with the proviso that when Y and A are phenyl or heterocycle, W is not H, a process and intermediates for 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, and pharmaceutical compositions and associations containing them.
    • 本发明涉及通式(I)的化合物及其与酸和碱的加成盐:其中A是苯基,萘基和5-10元单环或双环不饱和杂环,任选地被如下定义的基团R 1所取代: 本申请本身可以任选地被如申请中定义的基团R2取代,并且本身任选被在应用中定义的基团R 3取代,Y和W相同或不同,为H,(C 1 -C 6) 烷基,(C 2 -C 6)烯基,(C 2 -C 6)炔基,苯基或4-10单环或双环饱和或不饱和杂环,任选被R 1取代,或Y和/或W与R 1形成4-10元环, 或Y和W与N形成饱和或不饱和的含氮4-10元单,双或三环系统,稠合,桥连或螺环系统,所述系统任选被R 1取代,所述系统不同于吗啉,条件是当 Y和A是苯基或杂环 W不是H,它们的制备方法和中间体以及它们在抗菌预防和治疗中的用途,其单独使用或与抗菌剂,抗毒素剂或增强宿主先天免疫力的药物联合使用,以及含有它们的药物组合物和组合物。