公开(公告)号：EP2505198A1

公开(公告)日：2012-10-03

申请号：EP11305385.4

申请日：2011-04-01

申请人： Société Splicos ,  Centre National de la Recherche Scientifique ,  Institut Curie ,  Université de Montpellier 2

发明人： Roux, Pierre ,  Mahuteau, Florence ,  Najman, Romain ,  Tazi, Jamal ,  Scherrer, Didier

IPC分类号： A61K31/4164 ,  A61K31/4192 ,  A61K31/44 ,  C07D213/74 ,  C07D233/54 ,  C07D249/06 ,  C07D401/12 ,  A61P35/00 ,  A61P29/00 ,  A61P25/00 ,  A61P21/00 ,  A61P9/00 ,  A61P1/16

CPC分类号： C07C237/30 ,  A61K31/166 ,  A61K31/167 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4192 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  C07D213/36 ,  C07D213/38 ,  C07D233/61 ,  C07D233/64 ,  C07D249/06 ,  C07D401/12

摘要： The present invention relates to compound (I)

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.

摘要翻译： 本发明涉及化合物（I）其中R1和R2独立地表示氢原子，（C 1 -C 4）烷氧基，氟代（C 1 -C 4）烷氧基，羟基，苄氧基， 二（C 1 -C 4）烷基氨基，吡啶基乙烯基，嘧啶基乙烯基，苯乙烯基，或基团-NHCOphenyl; R3，R4和R5独立地表示氢原子，（C 1 -C 4）烷基，CONHR6基，-CONR 7 R 8基，-SO 2 NHR 6基团，或者被卤素原子任选取代的杂芳基，一个 - （CH 2）n的NR7R8基团或羟基（C 1 -C 4）烷基; R 6表示氢原子， - （CHR 9）M（CH 2）n的NR7R8基团或（C 1 -C 6）烷基，其任选由substituiertem羟基; 或其药学上可接受的盐中的任何一个，其用作用于预防，治疗的疾病抑制在一个或患者患有它们，所述疾病涉及失调的p53基因的试剂。 某些所述化合物是新的，因此构成本发明的一部分。

公开(公告)号：EP2465502A1

公开(公告)日：2012-06-20

申请号：EP10306417.6

申请日：2010-12-15

申请人： Société Splicos ,  Centre National de la Recherche Scientifique CNRS ,  Institut Curie ,  Université Montpellier II

发明人： Tazi, Jamal ,  Mahuteau, Florence ,  Najman, Romain

IPC分类号： A61K31/47 ,  A61P31/18

CPC分类号： C07D215/38 ,  C07D295/135 ,  C07D401/12

摘要： The present invention relates to compound (I)

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。

公开(公告)号：EP2712862A1

公开(公告)日：2014-04-02

申请号：EP12186684.2

申请日：2012-09-28

申请人： Splicos ,  Centre National de la Recherche Scientifique ,  Institut Curie ,  Université Montpellier II

发明人： Roux, Pierre ,  Mahuteau, Florence ,  Najman, Romain ,  Gadea, Gilles ,  Tazi, Jamal ,  Scherrer, Didier ,  Brock, Carsten ,  Cahuzac, Nathalie, M.

IPC分类号： C07D213/75 ,  C07D239/42 ,  C07D401/12 ,  A61K31/44 ,  A61P35/00

CPC分类号： C07D401/14 ,  C07D213/75 ,  C07D239/42 ,  C07D401/12

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。

公开(公告)号：EP3059591A1

公开(公告)日：2016-08-24

申请号：EP15305276.6

申请日：2015-02-23

申请人： ABIVAX ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  Institut Curie ,  Université Montpellier

发明人： Scherrer, Didier ,  Garcel, Aude ,  Campos, Noelie ,  Vautrin, Audrey ,  Mahuteau-Betzer, Florence ,  Najman, Romain ,  Fornarelli, Pauline ,  Tazi, Jamal

IPC分类号： G01N33/569

CPC分类号： G01N33/56983 ,  G01N2333/16 ,  G01N2469/10 ,  G01N2500/02 ,  G01N2500/10

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).

摘要翻译： 本发明涉及一种用于筛选用于治疗或预防病毒感染或在个体的病毒相关病症有用的化合物的方法，包括至少以下步骤：a）确定的采矿的候选化合物，以促进之间的相互作用的能力 CBP20和CBP80的样品中，和b）选择所述候选化合物确实是确定性的开采，以促进在步骤a）中所述相互作用。 本发明还涉及一种方法，用于筛选用于治疗或预防病毒感染或在单独的病毒相关病症有用的化合物，其至少包括以下步骤：a）确定的采矿的候选化合物的能力与CBP20或交互 CBP80的样品中，和b）选择所述候选化合物确实是确定性的开采在步骤a）中与CBP20或CBP80进行交互。

公开(公告)号：EP2266972A1

公开(公告)日：2010-12-29

申请号：EP09305540.8

申请日：2009-06-12

申请人： Splicos ,  Université Montpellier 2 Sciences et Techniques ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) ,  Institut Curie

发明人： Mahuteau Betezer, Florence ,  Tazi, Jamal

IPC分类号： C07D401/12 ,  A61K31/444

CPC分类号： C07D401/12

摘要： The present invention relates to a compound of the formula I; a pharmaceutical composition comprising at least one such compound; and the use of such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.

摘要翻译： 本发明涉及式I的化合物; 一种药物组合物，其包括测试至少一种化合物; 和在制备药物以治疗，在受试者中使用测试化合物的，遗传性疾病由至少一种剪接异常所致。

公开(公告)号：EP3058940A1

公开(公告)日：2016-08-24

申请号：EP15305277.4

申请日：2015-02-23

申请人： ABIVAX ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  Institut Curie ,  Université Montpellier

发明人： Scherrer, Didier ,  Garcel, Aude ,  Campos, Noelie ,  Tazi, Jamal ,  Vautrin, Audrey ,  Mahuteau-Betzer, Florence ,  Najman, Romain ,  Fornarelli, Pauline

IPC分类号： A61K31/4709 ,  A61P31/18

CPC分类号： A61K31/47 ,  A61K31/4709 ,  A61K31/706 ,  A61K2300/00

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.

摘要翻译： 本发明涉及式（I）的喹啉衍生物或其任何其药学上可接受的盐或其任何代谢物，用于治疗或预防病毒感染，特别是HIV感染或HIV相关病症 患者; 然后在以下情况下终止所述治疗：病毒载量低或不可检测; 和/或维持或恢复CD4 +细胞计数的水平。 本发明还涉及如权利要求1所定义的式（I）喹啉衍生物或其任何药学上可接受的盐和代谢物，用于治疗或预防病毒感染，特别是HIV感染或HIV相关 已经陈述了先前的抗逆转录病毒治疗有效性的无效性或下降的患者以及上述式（I）的喹啉衍生物或其药学上可接受的盐和代谢物中的任何一种，用于 治疗或预防患者的病毒感染，特别是HIV感染或HIV相关病症，其中患者被抗药性病毒株感染，特别是耐药性HIV毒株。

公开(公告)号：EP2261214A1

公开(公告)日：2010-12-15

申请号：EP09162630.9

申请日：2009-06-12

申请人： Splicos Sas ,  CNRS (Centre National de La Recherche Scientifique) ,  Institut Curie ,  Université Montpellier 2

发明人： Mahuteau, Florence ,  Tazi, Jamal ,  Najman, Romain

IPC分类号： C07D215/38 ,  C07D401/12 ,  A61K31/33 ,  A61P43/00

CPC分类号： C07D401/12 ,  C07D215/38

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.

摘要翻译： 本发明涉及式（I）的化合物：worin：芳环worinⅤ的手段是C或N，并且当V是N，V是在邻位，间位或Z的对位，即 分别形成哒嗪，嘧啶或吡嗪基，R独立地darstellt氢原子，卤原子或（C 1 -C 3）烷基，-CN基，-COOH基，一个中选择的基团（ C 1 -C 3）氟烷基，（C 1 -C 3）氟烷基，-NO 2基，-NR 1 R 2基团和（C 1 -C 3）烷氧基，R 1和R 2 独立地为氢原子或（C 1 -C 3）烷基基团，n是1或2，R“为氢原子或（C 1 -C 3）中选择的烷基基团，一个卤素原子，一个基团 羟基基团，-COOH基团和-CN基团，R“是氢原子或（C 1 -C 4）烷基基团，Z为N或C，Y是N或C，X为N或C，W 是N或C，以及worin至多两个基团Z，Y，X和W的为N，或其药学上可接受的盐中的任何一个，其用作用于预防，抑制性或治疗与过早老化联的病理或nonpathological条件的试剂 ，

公开(公告)号：EP3059236A1

公开(公告)日：2016-08-24

申请号：EP15305274.1

申请日：2015-02-23

申请人： ABIVAX ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  Institut Curie ,  UNIVERSITE DE MONTPELLIER

发明人： Scherrer, Didier ,  Garcel, Aude ,  Campos, Noelie ,  Tazi, Jamal ,  Vautrin, Audrey ,  Mahuteau, Florence ,  Najman, Romain ,  Fornarelli, Pauline

IPC分类号： C07D405/12

CPC分类号： C07H17/02 ,  C07D405/12

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.

摘要翻译： 本发明涉及式（1）的喹啉衍生物或其药学上可接受的盐之一。 本发明还涉及用作药物并用于治疗或预防病毒或逆转录病毒感染，特别是AIDS或AIDS相关病症或人类免疫缺陷病毒（HIV）的喹啉衍生物。 本发明还涉及包含所述喹啉衍生物的药物组合物及其制备新型中间体化合物的方法。

公开(公告)号：EP2757161A1

公开(公告)日：2014-07-23

申请号：EP13305053.4

申请日：2013-01-17

申请人： Splicos ,  Centre National de la Recherche Scientifique ,  Université Montpellier II

发明人： Tazi, Jamal ,  Scherrer, Didier ,  Garcel, Aude ,  Campos, Noëlie ,  Najman, Romain ,  Mahuteau-Beyzer, Florence

IPC分类号： C12Q1/70

CPC分类号： C12Q1/6876 ,  C12Q1/70 ,  C12Q2600/106 ,  C12Q2600/112 ,  C12Q2600/136 ,  C12Q2600/158 ,  C12Q2600/178

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.

摘要翻译： 使用至少一种miRNA，所述至少一种miRNA是miR-124，作为病毒感染的生物标志物或治疗性治疗所述病毒感染的功效。