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1. 发明申请

WO2012131656A3 COMPOUNDS FOR USE AS THERAPEUTIC AGENTS AFFECTING P53 EXPRESSION AND/OR ACTIVITY 审中-公开
标题翻译：用作影响P53表达和/或活性的治疗剂的化合物
公开(公告)号：WO2012131656A3
公开(公告)日：2012-11-22
申请号：PCT/IB2012051603
申请日：2012-04-02
申请人： SPLICOS SOC , CENTRE NAT RECH SCIENT , INST CURIE , UNIV MONTPELLIER 2 , SCHERRER DIDIER , TAZI JAMAL , NAJMAN ROMAIN , MAHUTEAU FLORENCE , ROUX PIERRE
发明人： SCHERRER DIDIER , TAZI JAMAL , NAJMAN ROMAIN , MAHUTEAU FLORENCE , ROUX PIERRE
IPC分类号： A61K31/4164 , A61K31/4192 , A61K31/44 , A61P1/16 , A61P9/00 , A61P21/00 , A61P25/00 , A61P29/00 , A61P35/00 , C07D213/74 , C07D233/54 , C07D249/06 , C07D401/12
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 (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)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 (C1-C4)alkyl group, a CONHR6 group, a -CONR7R8 group, a -SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a -(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a -(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method 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：本发明涉及其中R 1和R 2独立地表示氢原子，（C 1 -C 4）烷氧基，氟（C 1 -C 4）烷氧基，羟基，苄氧基，二（C 1 -C 4） -C4）烷基氨基，吡啶基 - 乙烯基，嘧啶基 - 乙烯基，苯乙烯基或-NHCO苯基; R3，R4和R5独立地表示氢原子，（C1-C4）烷基，CONHR6基，-CONR7R8基，-SO2NHR6基或任选被卤素原子取代的杂芳基， - （CH2） nR 7 R 8基团或羟基（C 1 -C 4）烷基; R6表示氢原子， - （CHR9）m（CH2）nNR7R8基团或任选被羟基取代的（C1-C6）烷基; 或其任何药学上可接受的盐，用于在患有其的患者中预防，抑制或治疗疾病的方法中，所述疾病涉及失调的p53。一些所述化合物是新的并且也构成本发明的一部分。

2. 发明申请

WO2010143168A3 COMPOUNDS USEFUL FOR TREATING CANCER 审中-公开
标题翻译：化合物可用于治疗癌症
公开(公告)号：WO2010143168A3
公开(公告)日：2011-06-09
申请号：PCT/IB2010052650
申请日：2010-06-14
申请人： SPLICOS SOC , CENTRE NAT RECH SCIENT , INST CURIE , UNIV MONTPELLIER 2 , ROUX PIERRE , MAHUTEAU FLORENCE , NAJMAN ROMAIN , TAZI JAMAL , GADEA GILLES
发明人： ROUX PIERRE , MAHUTEAU FLORENCE , NAJMAN ROMAIN , TAZI JAMAL , GADEA GILLES
IPC分类号： A61K31/444 , A61P43/00 , C07D213/74 , C07D215/38 , C07D241/44 , C07D401/12 , C07D403/12
CPC分类号： C07D403/12 , A61K31/4709 , A61K31/4985 , C07D213/74 , C07D215/38 , C07D215/42 , C07D215/46 , C07D241/44 , C07D401/12
摘要： The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a NO2 group, a NR1R2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n is 1 or 2, R is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group,, a hydroxyl group, a COOR1 group, a NO2 group, a NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating cancer. 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：表示哒嗪，嘧啶或吡嗪基，R独立地表示氢原子，卤原子或选自CN基，羟基，COOR1基，（C1-C3）氟代烷基，（C1-C3）氟烷氧基，NO2基，NR1R2基，（C1-C4）烷氧基，苯氧基和（C1-C3）烷基）任选被羟基单取代，n为1,2或3，n为1或2，R为氢原子，卤素原子或选自（C1-C3）烷基，羟基中的基团，COOR1基团，NO2基团，NR1R2基团，吗啉基或吗啉基，N-甲基哌嗪基，（C1-C3）氟烷基，（C1-C4）烷氧基和CN基，Z为 N或C，Y是N或C，X是N或C，W是N或C，T是N或C，U是N或C，用作预防，抑制或治疗癌症的药剂。一些所述化合物是新的并且也构成本发明的一部分。

3. 发明申请

WO2010143170A3 COMPOUNDS USEFUL FOR TREATING PREMATURE AGING AND IN PARTICULAR PROGERIA 审中-公开
标题翻译：用于治疗预防老化和特殊原因的化合物
公开(公告)号：WO2010143170A3
公开(公告)日：2011-08-11
申请号：PCT/IB2010052652
申请日：2010-06-14
申请人： SPLICOS SOC , CENTRE NAT RECH SCIENT , INST CURIE , UNIV MONTPELLIER 2 , TAZI JAMAL , MAHUTEAU FLORENCE , NAJMAN ROMAIN
发明人： TAZI JAMAL , MAHUTEAU FLORENCE , NAJMAN ROMAIN
IPC分类号： C07D401/12 , A61K31/444 , A61P43/00 , C07D213/74 , C07D215/38 , C07D241/44 , C07D403/12
CPC分类号： C07D403/12 , A61K31/4709 , A61K31/4985 , C07D213/74 , C07D215/38 , C07D215/42 , C07D215/46 , C07D241/44 , C07D401/12
摘要： The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a -CN group, a hydroxyl group, a -COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a -NO2 group, a -NRiR2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n' is 1 or 2, R' is a hydrogen atom, a halogen atom or a group chosen among a (Ci-C3)alkyl group,, a hydroxyl group, a -COOR1 group, a -NO2 group, a -NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (Ci-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a -CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating pathological or nonpathological conditions linked with premature aging. 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：表示哒嗪，嘧啶或吡嗪基，R独立地表示氢原子，卤素原子或选自-CN基，羟基，-COOR1基团，（C1-C3）氟代烷基，（C1-C3）氟烷氧基，-NO2基，-NR1R2基，（C1-C4）烷氧基，苯氧基和（C1-C3）烷基所述烷基任选被羟基单取代，n为1,2或3，n'为1或2，R'为氢原子，卤原子或选自（C 1 -C 3）烷基基团，羟基，-COOR 1基团，-NO 2基团，-NR 1 R 2基团，吗啉基或吗啉基，N-甲基哌嗪基，（C 1 -C 3）氟代烷基，（C 1 -C 4）烷氧基和-CN基，Z是N或C，Y是N或C，X是N或C，W是N或C，T是N或C，U是N或C，用作预防，抑制或治疗与过早老化相关的病理或非病理状况。一些所述化合物是新的并且也构成本发明的一部分。

4. 发明申请

WO2010143169A2 COMPOUNDS USEFUL FOR TREATING AIDS 审中-公开
标题翻译：用于治疗艾滋病的化合物
公开(公告)号：WO2010143169A2
公开(公告)日：2010-12-16
申请号：PCT/IB2010052651
申请日：2010-06-14
申请人： SPLICOS SOC , CENTRE NAT RECH SCIENT , INST CURIE , UNIV MONTPELLIER 2 , TAZI JAMAL , MAHUTEAU FLORENCE , NAJMAN ROMAIN
发明人： TAZI JAMAL , MAHUTEAU FLORENCE , NAJMAN ROMAIN
IPC分类号： C07D215/38 , A61K31/33 , A61K31/444 , A61P43/00 , C07D401/12
CPC分类号： C07D403/12 , A61K31/4709 , A61K31/4985 , C07D213/74 , C07D215/38 , C07D215/42 , C07D215/46 , C07D241/44 , C07D401/12
摘要： The present invention relates to compound Formula (I) wherein: Formula (II) means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a NO2 group, a NR1R2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n is 1 or 2, R is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group,, a hydroxyl group, a COOR1 group, a NO2 group, a NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating AIDS. Some of said compounds are new and also form part of the invention.
摘要翻译：本发明涉及化合物式（I），其中：式（II）表示哒嗪，嘧啶或吡嗪基，R独立地表示氢原子，卤素原子或选自CN基，羟基，（C1-C3）氟代烷基，（C1-C3）氟烷氧基，NO2基，NR1R2基，（C1-C4）烷氧基，苯氧基和（C1-C3）烷基所述烷基任选被羟基单取代，n为1,2或3，n为1或2，R为氢原子，卤原子或选自（C1-C3）烷基中的基团，羟基，COOR1基，NO2基，NR1R2基，吗啉基或吗啉基，N-甲基哌嗪基，（C1-C3）氟代烷基，（C1-C4）烷氧基和 CN组，Z为N或C，Y为N或C，X为N或C，W为N或C，T为N或C，U为N或C，用作预防，抑制或处理剂艾滋病。一些所述化合物是新的并且也构成本发明的一部分。

5. 发明申请

WO2009087238A3 CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES 审中-公开
标题翻译：化学分子，禁止用于治疗由分离异常引起的疾病的机制
公开(公告)号：WO2009087238A3
公开(公告)日：2010-09-16
申请号：PCT/EP2009050280
申请日：2009-01-12
申请人： CENTRE NAT RECH SCIENT , INST CURIE , UNIV MONTPELLIER 2 SCIENCES ET , TAZI JAMAL , GRIERSON DAVID , MAHUTEAU-BETZER FLORENCE , ROUX PIERRE
发明人： TAZI JAMAL , GRIERSON DAVID , MAHUTEAU-BETZER FLORENCE , ROUX PIERRE
IPC分类号： C07D401/12 , A61K31/444 , C07D213/74 , C07D401/14
CPC分类号： A61K31/166 , A61K31/417 , A61K31/4192 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/4725 , C07C237/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/82 , C07D233/61 , C07D233/64 , C07D249/06 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one 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至XXI之一的化合物; 包含至少一种这样的化合物的药物组合物; 以及至少一种这样的化合物在制备药物中的用途，以在受试者中治疗由至少一个拼接异常引起的遗传疾病。

6. 发明申请

WO2009087238A9 CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES 审中-公开
标题翻译：化学分子抑制切断机制治疗因摔打异常引起的疾病
公开(公告)号：WO2009087238A9
公开(公告)日：2010-02-25
申请号：PCT/EP2009050280
申请日：2009-01-12
申请人： CENTRE NAT RECH SCIENT , INST CURIE , UNIV MONTPELLIER 2 SCIENCES ET , TAZI JAMAL , GRIERSON DAVID , MAHUTEAU-BETZER FLORENCE , ROUX PIERRE
发明人： TAZI JAMAL , GRIERSON DAVID , MAHUTEAU-BETZER FLORENCE , ROUX PIERRE
IPC分类号： C07D401/12 , A61K31/444 , C07D213/74 , C07D401/14
CPC分类号： A61K31/166 , A61K31/417 , A61K31/4192 , A61K31/4406 , A61K31/4409 , A61K31/4439 , A61K31/4725 , C07C237/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/82 , C07D233/61 , C07D233/64 , C07D249/06 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one 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至XXI之一的化合物; 包含至少一种这样的化合物的药物组合物; 以及至少一种所述化合物在制备药物中的用途，所述药物用于治疗受试者由至少一种剪接异常引起的遗传疾病。

7. 发明申请

WO2005023255A3 USE OF INDOLE-DERIVED COMPOUNDS FOR THE PREPARATION OF A MEDICAMENT THAT CAN BE USED TO TREAT DISEASES RELATED TO THE SPLICING PROCESS 审中-公开
标题翻译：用于制备可用于治疗与分离过程相关的疾病的药物的吲哚衍生化合物的使用
公开(公告)号：WO2005023255A3
公开(公告)日：2006-04-20
申请号：PCT/FR2004002261
申请日：2004-09-06
申请人： CENTRE NAT RECH SCIENT , UNIV MONTPELLIER II , INST CURIE , TAZI JAMAL , SORET JOHANN , JEANTEUR PHILIPPE , GRIERSON DAVID
发明人： TAZI JAMAL , SORET JOHANN , JEANTEUR PHILIPPE , GRIERSON DAVID
IPC分类号： A61K31/4745 , A61K31/403 , A61K31/437 , A61K31/4375 , A61K31/475 , A61K31/496 , A61K31/5377 , A61P11/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P35/00 , A61P43/00 , C07D209/80 , C07D471/04 , C07D471/14 , C07D519/00
CPC分类号： A61K31/4375 , A61K31/403 , A61K31/437 , A61K31/4745 , A61K31/496 , A61K31/5377 , C07D209/80 , C07D471/04 , C07D471/14
摘要： The invention relates to indole-derived compounds and to the use of said compounds for the preparation of a medicament that can be used to treat diseases related to the process of splicing pre-messenger RNAs in the cell, such as Frasier syndrome, frontotemporal dementia linked to chromosome 17 (a form of Parkinson's disease), Leigh syndrome (a type of encephalopathy), atypical cystic fibrosis, certain neuropathologies including Alzheimer's disease linked to a mutation in the Tau protein, muscle atrophy which affects the SMN (Survival of Motor Neuron) gene, depression linked to a serotonin splicing impairment, and certain cancers in which the global splicing process is affected (e.g. breast cancer, colon cancer and certain lymphomas), as well as viral diseases such as AIDS.
摘要翻译：本发明涉及吲哚衍生的化合物和所述化合物用于制备药物的用途，所述药物可用于治疗与剪接细胞中的前信使RNA的过程相关的疾病，例如Frasier综合征，额颞额痴呆到17号染色体（帕金森病的一种形式），Leigh综合征（一种脑病），非典型囊性纤维化，某些神经病理学包括与Tau蛋白突变有关的阿尔茨海默氏病，影响SMN的肌肉萎缩（运动神经元的存活）基因，与血清素剪接损伤相关的抑郁症，以及影响全球剪接过程的某些癌症（例如乳腺癌，结肠癌和某些淋巴瘤）以及病毒性疾病如艾滋病。

8. 发明申请

WO2008101935A3 NEW INDOLE DERIVATIVE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译：新型衍生化合物和含有其的药物组合物
公开(公告)号：WO2008101935A3
公开(公告)日：2009-01-22
申请号：PCT/EP2008052025
申请日：2008-02-19
申请人： CENTRE NAT RECH SCIENT , INST CURIE , LEJEUNE FABRICE , TAZI JAMAL , GRIERSON DAVID , RIVALLE CHRISTIAN , MAHUTEAU-BETZER FLORENCE
发明人： LEJEUNE FABRICE , TAZI JAMAL , GRIERSON DAVID , RIVALLE CHRISTIAN , MAHUTEAU-BETZER FLORENCE
IPC分类号： C07D471/04 , C07D401/12
CPC分类号： C07D471/14 , C07D401/12 , C07D471/04
摘要： The invention relates to an indole derivative compound of the formula (II) in which: X is N, CR8 or N+ R8, wherein R8 is a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted by a phenyl group; R2, R3 and R4 are independently a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 is a hydrogen atom or an optionally substituted alkyl, amine, benzyl group; R6 is an optionally substituted C1-C3 alkyl group; R7 is a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the cycle A is at the b position, A representing a cycle; R9 and R10 form together a carbon bond or independently represent a R11, OR11, SR11 group, wherein R11 is hydrogen or a saturated or unsaturated optionally substituted C1-C3 alkyl group that may contain one or more sulphur, oxygen or nitrogen atoms. The invention also relates to the pharmaceutically acceptable salts of said compounds, their isomers and/or a mixture thereof, to a pharmaceutical composition containing such compound, and to the use of said compound in the preparation of a drug for treating a genetic disease resulting from at least one mutation inducing the occurrence of an early termination codon.
摘要翻译：本发明涉及式（II）的吲哚衍生物化合物，其中：X为N，CR8或N + R8，其中R8为氢原子，羟基或任选被苯基取代的烷基或甲氧基; R2，R3和R4独立地是氢原子或卤素原子或任选取代的烷基，胺，烯烃，酯，磺酰胺，醚或苄基; R5是氢原子或任选取代的烷基，胺，苄基; R6是任选取代的C 1 -C 3烷基; 当环A位于b位置时，R 7为氢原子或任选取代的C 1 -C 3烷基且R 7不存在，A代表一个周期; R 9和R 10一起形成碳键或独立地表示R 11，OR 11，SR 11基团，其中R 11是氢或可以含有一个或多个硫，氧或氮原子的饱和或不饱和的任选取代的C 1 -C 3烷基。本发明还涉及所述化合物的药学上可接受的盐，它们的异构体和/或其混合物，其含有该化合物的药物组合物，以及所述化合物在制备用于治疗由至少一个突变引起早期终止密码子的发生。

9. 发明申请

WO2016009065A3 QUINOLINE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：喹啉衍生物治疗炎性疾病
公开(公告)号：WO2016009065A3
公开(公告)日：2016-03-24
申请号：PCT/EP2015066458
申请日：2015-07-17
申请人： ABIVAX , CENTRE NAT RECH SCIENT , INST CURIE , UNIV MONTPELLIER
发明人： TAZI JAMAL , NAJMAN ROMAIN , MAHUTEAU FLORENCE , SCHERRER DIDIER
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/497 , A61K31/5377 , A61P1/00 , A61P19/02 , A61P25/00 , A61P29/00 , C07D215/38 , C12Q1/68 , G01N33/50
CPC分类号： C07D215/38 , A61K31/47 , A61K31/4709 , A61K31/497 , A61K31/5377 , C07D401/12 , C12Q1/6883 , C12Q2600/136 , C12Q2600/158 , C12Q2600/178 , G01N33/5023 , G01N33/5055
摘要： The present invention relates to a compound of formula (I) wherein: Formula (II) means an aromatic ring wherein V is C or N and when V is N; Q is N or O, provided that R" does not exist when Q is O; R' independently represent a hydrogen atom or a group chosen among a (C1-C3)alkyl group, a halogen atom, a hydroxy! group, a - COOR1 group, a -NO2 group, a -NR1R2 group, a morpholinyl or a morpholino group, a N- methylpiperazinyl group, a (Ci-C3)fluoroalkyl group, a -O-P(=O)-(OR3XOR4) group, a (C1-C4)alkoxy group and a -CN group, and can further be a group chosen among:(IIa), (IIIa) or anyone of its pharmaceutically acceptable salt, for use in the treatment and/or prevention of an inflammatory disease.
摘要翻译：本发明涉及式（I）化合物，其中：式（II）是指其中V是C或N并且当V是N时的芳环; Q是N或O，条件是当Q是O时R“不存在; R'独立地表示氢原子或选自（C1-C3）烷基，卤素原子，羟基， COOR 1基团，-NO 2基团，-NR 1 R 2基团，吗啉基或吗啉基，N-甲基哌嗪基，（C 1 -C 3）氟烷基，-OP（= O） - （OR 3 XOR 4） C1-C4）烷氧基和-CN基团，并且可以进一步为选自：（IIa），（IIIa）或其任何可药用盐的基团，用于治疗和/或预防炎性疾病。

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