for use as an agent for preventing, inhibiting or treating AIDS. The present invention further relates to compounds of formula (I) wherein X is CR 0 or N; R 0 , R 1 , R 2 , R 3 , R 4 , R 7 and R 8 independently represent a hydrogen atom, a halogen atom or a group chosen among a (C 1 -C 5 )alkyl group, a (C 3 -C 6 )cycloalkyl group, a (C 1 -C 5 )fluoroalkyl group, a (C 1 -C 5 )alkoxy group, a (C 1 -C 5 )fluoroalkoxy group, a -CN group, a -COOR a group, a -NO 2 group, a -NR a R b group, a -NR a- SO 2- NR a R b group, a -NR a- SO 2- R a group, a -NR a -C(=O)-R a group, a -NR a -C(=O)-NR a R b group, a -SO 2- NR a R b group, a -SO 3 H group, a -OH group, a -O-SO 2 -OR c group, a -O-P(=O)-(OR c )(OR d ) group, a -O-CH 2 -COOR c group and can further be a group chosen among:
R 5 represents a hydrogen atom, a (C 1 -C 5 )alkyl group or a (C 3 -C 6 )cycloalkyl group; R 10 is a hydrogen atom or a chlorine atom, and R 11 is a hydrogen atom or a (C 1 -C 4 )alkyl group or anyone of its pharmaceutically acceptable salts.
摘要翻译:本发明涉及用作预防,抑制或治疗AIDS的药剂的化合物(I)。 本发明还涉及其中X为CR 0或N的式(I)化合物; R 0,R 1,R 2,R 3,R 4,R 7和R 8独立地表示氢原子,卤素原子或选自(C 1 -C 5)烷基,(C 3〜 C 6)环烷基,(C 1 -C 5)氟代烷基,(C 1 -C 5)烷氧基,(C 1 -C 5)氟烷氧基,-CN基,-COOR a基, -NO 2基团,-NR a R b基团,-NR a -SO 2 NR a R b基团,-NR a -SO 2 R a基团,-NR a -C(= O) -R a基团,-NR a -C(= O)-NR a R b基团,-SO 2 NR a R b基团,-SO 3 H基团,-OH基团,-O-SO 2 -OR c基团,-OP(= O) - (OR c)(OR d)基团,-O-CH 2 -COOR c基团,可以进一步选自:R 5表示氢原子, (C 1 -C 5)烷基或(C 3 -C 6)环烷基; R 10为氢原子或氯原子,R 11为氢原子或(C 1〜C 4)烷基或其任何药学上可接受的盐。
摘要:
The present invention relates to a compound of formula (I):
wherein A and A' independently represent a phenylene group or a pyridylene group; R 2 is a hydrogen atom or a (C 1 -C 4 )alkyl group; R 3 is a 2-pyridyl group, 3-pyridyl group, a 4-pyridyl group, a 2-pyrimidinyl group, a 4-pyrimidinyl group or a 5-pyrimidinyl group; R 4 is a carbonyl group or a sulfonyl group; and R 5 is a - NH-(CH 2 ) a -NR 6 R 7 group or a 4-methylpiperazinyl group, with a being an integer from 1 to 4, R 6 and R 7 representing independently a (C 1 -C 4 )alkyl group, or R 6 and R 7 together with the nitrogen atom to which they are linked forming a heterocycle group which is chosen among a 4-methylpiperazinyl group, a morpholino group, a pyrrolidinyl group and a piperidino group; or any one of its pharmaceutically acceptable salt. The invention further relates to pharmaceutical compositions containing a compound of formula (I) or any one of its pharmaceutically acceptable salt and a preparation process for obtaining the same. Said compounds (I) are useful for treating cancer.
摘要翻译:本发明涉及式(I)化合物:其中A和A'独立地表示亚苯基或亚吡啶基; R 2是氢原子或(C 1 -C 4)烷基; R 3为2-吡啶基,3-吡啶基,4-吡啶基,2-嘧啶基,4-嘧啶基或5-嘧啶基; R 4是羰基或磺酰基; 和R 5是-NH - (CH 2)a -NR 6 R 7基或4-甲基哌嗪基,其中1至4的整数,R 6和R 7独立地表示(C 1 -C 4) )烷基,或R 6和R 7与它们所连接的氮原子一起形成选自4-甲基哌嗪基,吗啉代基,吡咯烷基和哌啶子基的杂环基; 或其药学上可接受的盐中的任何一种。 本发明还涉及含有式(I)化合物或其药学上可接受的盐中的任何一种的药物组合物及其制备方法。 所述化合物(I)可用于治疗癌症。
wherein R1 and R2 independently represent a hydrogen atom, a (C 1 -C 4 )alkoxy group, a fluoro(C 1 -C 4 )alkoxy group, a hydroxyl group, a benzyloxy group, a di(C 1 -C 4 )alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a -NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C 1 -C 4 )alkyl group, a CONHR6 group, a -CONR7R8 group, a -SO 2 NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a -(CH 2 ) n NR7R8 group or a hydroxy(C 1 -C 4 )alkyl group; R6 represents a hydrogen atom, a -(CHR9) m (CH 2 ) n NR7R8 group or a (C 1 -C 6 )alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use as an agent for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.
摘要:
A use of at least one miRNA, said at least one miRNA being miR-124, as a biomarker of a viral infection, or of an efficacy of a therapeutic treatment of said viral infection.
摘要:
The present invention relates to a method for screening a compound useful for treating or preventing a viral infection or a virus-related condition in an individual, comprising at least the steps of: a) determining the ability of a candidate compound to promote the interaction between CBP20 and CBP80 in a sample, and b) selecting the candidate compound that is determined to promote said interaction at step a). The present invention further relates to a method for screening a compound useful for treating or preventing a viral infection or virus-related condition in an individual, comprising at least the steps of: a) determining the ability of a candidate compound to interact with CBP20 or CBP80 in a sample, and b) selecting the candidate compound that is determined to interact with CBP20 or CBP80 at step a).
摘要:
The present invention relates to a quinoline derivative of formula (1)
or one of its pharmaceutically acceptable salts. The present invention further relates to said quinoline derivative for use as a medicament and for use in the treatment or prevention of a viral or retroviral infection and in particular AIDS or an AIDS-related condition or Human Immunodeficiency virus (HIV). The present invention also relates to a pharmaceutical composition comprising said quinoline derivative and to the process for preparing it as to a novel intermediate compound.
摘要:
The present invention relates to A quinoline derivative of formula (I)
or anyone of its pharmaceutically acceptable salt, or anyone of its metabolites, for use for treating or preventing a viral infection, in particular a HIV infection or a HIV-related condition in a patient; and then terminating said treatment when: the viral load is low or undetectable; and/or the level of CD4+ cell count is maintained or restored. The present invention further relates to a quinoline derivative of formula (I) as defined in claim 1, or anyone of its pharmaceutically acceptable salts and metabolites, for use for treating or preventing a viral infection, in particular a HIV infection or a HIV-related condition in a patient, for which an ineffectiveness or a decline in a prior anti-retroviral treatment effectiveness has been stated and to a quinoline derivative of formula (I) as defined above, or anyone of its pharmaceutically acceptable salts and metabolites, for use for treating or preventing a viral infection, in particular a HIV infection or a HIV-related condition in a patient, wherein the patient is infected by a drug-resistant viral strain, and more particularly by a drug-resistant HIV strain.
摘要:
The present invention relates to a compound of formula (I):
wherein:
means an aromatic ring wherein V is C or N and when V is N, V is in ortho, meta or para of Z, i.e. forms respectively a pyridazine, a pyrimidine or a pyrazine group, R independently represents a hydrogen atom, a halogen atom or a group chosen among a (C 1 -C 3 )alkyl group, a -CN group, a -COOH group, a (C 1 -C 3 )fluoroalkyl group, a (C 1 -C 3 )fluoroalkoxy group, a -NO 2 group, a -NR 1 R 2 group and a (C 1 -C 3 )alkoxy group, R 1 and R 2 are independently a hydrogen atom or a (C 1 -C 3 )alkyl group, n is 1 or 2, R' is a hydrogen atom or a group chosen among a (C 1 -C 3 )alkyl group, a halogen atom, a hydroxy group, a -COOH group and a -CN group, R" is a hydrogen atom or a (C 1 -C 4 )alkyl group, Z is N or C, Y is N or C, X is N or C, W is N or C,
and wherein at most two of the groups Z, Y, X and W are N, or anyone of its pharmaceutically acceptable salt, for use as an agent for preventing, inhibiting or treating pathological or nonpathological conditions linked with premature aging.