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1. 发明申请

WO2020079184A2 UREA DERIVATIVES FOR TREATING AND/OR PREVENTING CANCER 审中-公开
公开(公告)号：WO2020079184A2
公开(公告)日：2020-04-23
申请号：PCT/EP2019/078274
申请日：2019-10-17
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE , UNIVERSITE PARIS DESCARTES , UNIVERSITE NICE SOPHIA ANTIPOLIS
发明人： BENHIDA, Rachid , PAGES, Gilles , DUFIES, Maeva , DEMANGE, Luc , RONCO, Cyril , GRYTSAI, Oleksandr
IPC分类号： A61K31/4184 , A61K31/428 , A61P35/00 , A61P27/00
摘要： The present invention relates to a compound or a pharmaceutically acceptable salt thereof of formulae (I) and (II), and a pharmaceutical composition comprising such compound for use for treating a cancer, particularly a cancer overexpressing CXCR1 and CXCR2 receptors, such as medulloblastoma, head and neck and kidney cancer. The invention further relates to such compounds for use for treating macular degeneration.

2. 发明申请

WO2019243431A1 COMPOSITIONS FOR TREATING MELANOMA 审中-公开
公开(公告)号：WO2019243431A1
公开(公告)日：2019-12-26
申请号：PCT/EP2019/066224
申请日：2019-06-19
申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , UNIVERSITE NICE SOPHIA ANTIPOLIS
发明人： TARTARE - DECKERT, Sophie , DECKERT, Marcel , BERESTJUK, Ilona
IPC分类号： A61K45/06 , A61K31/437 , A61K31/4523 , A61K31/506 , A61K31/519 , A61P35/00
摘要： Inventors have shown that targeting DDR1 and DDR2 collagen receptors by Imatinib resensitizes melanoma tumors to BRAFV600E to targeted therapy and normalizes the fibrotic stromal reaction. These findings provide the rationale to combine Imatinib (or other DDR inhibitors) and MAPK-targeting agents to disrupt the influence of the matrix microenvironment in order to delay or prevent the emergence of therapy-resistant cells. They have shown that inhibition of DDR1 and DDR2 kinase activities by Imatinib suppressed the protection of melanoma cells against Vemurafenib (BRAFi) and Trametinib (MEKi) co-drugging and led to cell cycle arrest and cell death. Similar biochemical cell cycle and apoptotic events were promoted in presence of Nilotinib. They validated this anti- tumor activity of Imatinib combined with Vemurafenib in a pre-clinical xenograft model of melanoma and showed that targeting DDR1/2 signaling delays tumor relapse. Accordingly, the present invention relates to a method for treating melanoma in a subject in need thereof comprising a step of administering said subject with a therapeutically effective amount of : i) an inhibitor of BRAF, ii) an inhibitor of MEK, and iii) an inhibitor of DDR1/2.

3. 发明申请

WO2019158689A1 METHODS AND COMPOSITIONS FOR TREATING LIVER DISEASES 审中-公开
公开(公告)号：WO2019158689A1
公开(公告)日：2019-08-22
申请号：PCT/EP2019/053807
申请日：2019-02-15
申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , CENTRE HOSPITALIER UNIVERSITAIRE DE NICE , UNIVERSITE NICE SOPHIA ANTIPOLIS
发明人： BAILLY-MAITRE RE, Beatrice , GUAL, Philippe , TRAN, Albert
IPC分类号： A61K31/00 , A61K31/381 , A61P1/16
摘要： The present invention relates to a method for treating a subject suffering from a liver disease comprising a step of administering said subject with a therapeutically effective amount of an inhibitor of the endoribonuclease activity of IRE1α. Inventors have shown that in livers of tunicamycin-treated BI-1-/- mice aIRE1α-dependent NLRP3 inflammasome activation, an hepatocyte death, a fibrosis and a dysregulated lipid homeostasis that led to liver failure within a week. To test whether the pharmacological inhibition of IRE1α endoribonuclease activity would block the transition to NASH, mice were injected with the small molecule STF-083010 twice a week for 2 weeks towards the end of a 3-month HFD. In BI-1-/- mice, STF-083010 treatment effectively counteracted IRE1α endoribonuclease activity, improving glucose tolerance and rescuing from NASH. The hepatocyte-specific role of IRE1α's RNase activity in mediating NLRP3 inflammasome activation and programmed cell death was confirmed in primary mouse hepatocytes through knockdown experiments and with STF-083010.

4. 发明申请

WO2019057820A1 TREATMENT OF ABNORMAL VISCERAL FAT DEPOSITION USING SOLUBLE FIBROBLAST GROWTH FACTOR RECEPTOR 3 (SFGFR3) POLYPEPTIDES 审中-公开
公开(公告)号：WO2019057820A1
公开(公告)日：2019-03-28
申请号：PCT/EP2018/075471
申请日：2018-09-20
申请人： THERACHON SAS , INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE) , UNIVERSITE NICE SOPHIA ANTIPOLIS , CENTRE NATIONAL RECHERCHE SCIENTIFIQUE
发明人： GOUZE, Elvire , GARCIA, Stéphanie
IPC分类号： A61K38/17 , A61K38/22 , A61P3/04 , A61P5/00
摘要： The invention features methods of using sFGFR3 polypeptides to treat abnormal visceral fat deposition and the conditions associated with abnormal visceral fat deposition.

5. 发明申请

WO2018178030A1 METHODS AND COMPOSITIONS FOR TREATING DEGENERATIVE MUSCULAR AND/OR NEUROLOGICAL CONDITIONS OR DISEASES 审中-公开
公开(公告)号：WO2018178030A1
公开(公告)日：2018-10-04
申请号：PCT/EP2018/057679
申请日：2018-03-26
申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE NICE SOPHIA ANTIPOLIS , RUIJIN HOSPITAL, SHANGHAI JIAOTONG UNIVERSITY SCHOOL OF MEDICINE , UNIVERSITÉ CLAUDE BERNARD LYON 1 , HOSPICES CIVILS DE LYON , CENTRE HOPITALIER UNIVERSITAIRE DE NICE
发明人： GILSON, Eric , ROBIN, Jérome , SACCONI, Sabrina , SCHAEFFER, Laurent , YE, Jing
IPC分类号： A61K31/7088 , A61K38/00 , A61K39/00 , A61P25/28 , A61P21/00
摘要： The present invention relates to a method for treating degenerative muscular and/or neurological conditions or diseases. The inventors found that TRF2 is decreased with age in human striated muscles which are post-mitotic cells. More particularly, in contrast to mitotic cells, downregulation of TRF2 in differentiated myotubes does not lead to telomere deprotection but triggers potent oxidative stress, along with increases in reactive oxygen species (ROS), mitochondrial dysfunction, FOXO3a activation, and autophagy. Thus, the invention relates to a method of treating diseases targeting post mitotic tissues such as muscle or neurodegenerative diseases in a subject in need thereof, comprising a step of administering said subject with a therapeutically effective amount of an activator, which activates the expression or activity of TRF2.

6. 发明申请

WO2018178029A1 METHODS AND COMPOSITIONS FOR TREATING DEGENERATIVE MUSCULAR AND/OR NEUROLOGICAL CONDITIONS OR DISEASES 审中-公开
公开(公告)号：WO2018178029A1
公开(公告)日：2018-10-04
申请号：PCT/EP2018/057677
申请日：2018-03-26
申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE NICE SOPHIA ANTIPOLIS , HOSPICES CIVILS DE LYON , UNIVERSITÉ CLAUDE BERNARD LYON 1 , CENTRE HOPITALIER UNIVERSITAIRE DE NICE , RUIJIN HOSPITAL, SHANGHAI JIAOTONG UNIVERSITY SCHOOL OF MEDICINE
发明人： GILSON, Eric , ROBIN, Jérome , SACCONI, Sabrina , SCHAEFFER, Laurent , YE, Jing
IPC分类号： A61K31/05 , A61K31/192 , A61K31/216 , A61K31/336 , A61K31/353 , A61K31/4439 , A61P25/28 , A61P21/00
摘要： The present invention relates to a method for treating degenerative muscular and/or neurological conditions or diseases. The inventors found that SIRT3 is decreased with age in human striated muscles which are post-mitotic cells. More particularly, in contrast to mitotic cells, downregulation of TRF2 in differentiated myotubes does not lead to telomere deprotection but triggers potent oxidative stress, along with increases in reactive oxygen species (ROS), mitochondrial dysfunction, FOXO3a activation, and autophagy. Thus, the invention relates to a method of treating muscle diseases or neurodegenerative diseases in a subject in need thereof, comprising a step of administering said subject with a therapeutically effective amount of an activator of the expression or activity of SIRT3.

7. 发明申请

WO2017202890A1 METHODS AND COMPOSITIONS FOR PREDICTING AND TREATING MYELOMA 审中-公开
标题翻译：预防和治疗骨髓瘤的方法和组合物
公开(公告)号：WO2017202890A1
公开(公告)日：2017-11-30
申请号：PCT/EP2017/062504
申请日：2017-05-24
申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , UNIVERSITE NICE SOPHIA ANTIPOLIS , CENTRE HOPITALIER UNIVERSITAIRE DE NICE
发明人： LUCIANO, Frédéric , HAMOUDA, Mohamed, Amine , ROBERT, Guillaume , AUBERGER, Patrick , CLUZEAU, Thomas
IPC分类号： G01N33/574
CPC分类号： G01N33/574 , G01N2800/50
摘要： The inventors have used the Εμ-bcl-b transgenic mouse model to study the effect of the Blc-B protein on the evolution of monoclonal gammopathy of undetermined significance (MGUS) to myeloma. They have performed the Bcl-B-positive plasma cell quantification by flow cytometry analysis of bone marrow cells from an MGUS and an multiple myeloma (MM) patient. They have showed that a subject having a high concentration of Bcl-B than a predetermined value is at risk of having myeloma. Accordingly, the invention relates to a method for predicting the risk of having myeloma in a subject suffering from MGUS comprising the steps of: i) measuring the concentration of Bcl-B in a biological sample obtained from said subject, ii) comparing the concentration obtained at step (i) to a predetermined value, and iii) concluding that the subject is at risk of having myeloma when the concentration of Bcl-B is higher than the predetermined value.
摘要翻译：本发明人已经使用了Eμ-bcl-b转基因小鼠模型来研究Blc-B蛋白对具有未定意义的单克隆丙种球蛋白病（MGUS）向骨髓瘤的进化的影响。他们通过对来自MGUS和多发性骨髓瘤（MM）患者的骨髓细胞进行流式细胞术分析来进行Bcl-B阳性浆细胞定量。他们已经表明，具有高于预定值的高浓度Bcl-B的受试者处于患有骨髓瘤的风险中。因此，本发明涉及用于预测患有MGUS的受试者中患有骨髓瘤的风险的方法，其包括以下步骤：i）测量从所述受试者获得的生物样品中Bcl-B的浓度，ii）比较获得的浓度在步骤（i）中达到预定值，以及iii）当Bcl-B的浓度高于预定值时，推断受试者有患骨髓瘤的风险。

8. 发明申请

WO2017129558A1 METHODS FOR PREDICTING OR TREATING MYELOPOIESIS-DRIVEN CARDIOMETABOLIC DISEASES AND SEPSIS 审中-公开
标题翻译：预测或治疗发育不良性心脏病和脓毒症的方法
公开(公告)号：WO2017129558A1
公开(公告)日：2017-08-03
申请号：PCT/EP2017/051418
申请日：2017-01-24
申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , UNIVERSITE NICE SOPHIA ANTIPOLIS
发明人： YVAN-CHARVET, Laurent , VIAUD, Manon , GUINAMARD, Rodolphe
IPC分类号： A61K31/197 , A61K39/00 , A61K45/00 , A61K31/235 , A61K31/166 , A61P9/10 , A61P31/00
CPC分类号： A61K31/235 , A61K31/165 , A61K31/195 , A61K31/197 , A61K31/353 , A61K31/7048 , A61K39/00
摘要： The present invention relates to a method of treating myelopoiesis-driven cardiometabolic diseases and sepsis in a subject in need thereof comprising the step of administering the subject with a therapeutically effective amount of an agent selected from the group consisting of GLUT1 inhibitors and GOTs inhibitors.
摘要翻译：本发明涉及在有需要的受试者中治疗骨髓生成 - 驱动的心脏代谢疾病和脓毒症的方法，包括给予受试者治疗有效量的选自以下的试剂的步骤：的GLUT1抑制剂和GOTs抑制剂。

9. 发明申请

WO2017102841A1 METHODS FOR DIAGNOSING OR PROGNOSING PROSTATE CANCER 审中-公开
标题翻译：诊断或预测前列腺癌的方法
公开(公告)号：WO2017102841A1
公开(公告)日：2017-06-22
申请号：PCT/EP2016/080998
申请日：2016-12-14
申请人： INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) , UNIVERSITE NICE SOPHIA ANTIPOLIS
发明人： BENAHMED, Mohamed
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , C12Q2600/158 , C12Q2600/178
摘要： The present invention relates to methods and kits for diagnosing or prognosing prostate cancer. More particularly, the invention relates to an in vitro method for predicting or diagnosing a prostate cancer in a subject, said method comprising the following steps of: i. measuring the expression levels of miR-101 and miR-195 in a biological sample obtained from said subject; ii. comparing said expression levels of miR-101 and miR-195 with their respective predetermined reference values; and iii. determining whether the subject has or is at risk of having a prostate cancer, wherein an expression level of miR-101 lower than the predetermined reference value and an expression level of miR-195 higher than the predetermined reference value is indicative that the subject has, or is at risk of having a prostate cancer.
摘要翻译：本发明涉及诊断或预后前列腺癌的方法和试剂盒。更具体地，本发明涉及用于预测或诊断受试者中的前列腺癌的体外方法，所述方法包括以下步骤：i。测量从所述受试者获得的生物样品中miR-101和miR-195的表达水平; II。比较miR-101和miR-195的所述表达水平与它们各自的预定参考值; 和iii。确定受试者是否患有前列腺癌或处于患有前列腺癌的风险中，其中低于预定参考值的miR-101的表达水平和高于预定参考值的miR-195的表达水平指示受试者具有，或有患前列腺癌的风险。

10. 发明申请

WO2016150824A1 CAPTEUR A FIBRE OPTIQUE DISTRIBUE D'ETAT DE CONTRAINTE 审中-公开
标题翻译：用于感应应力状态的分布式光纤传感器
公开(公告)号：WO2016150824A1
公开(公告)日：2016-09-29
申请号：PCT/EP2016/055866
申请日：2016-03-17
申请人： THALES , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , UNIVERSITE NICE SOPHIA-ANTIPOLIS
发明人： MOLIN, Stéphanie , DOISY, Martine , PEIGNE, Arnaud , RESIDORI, Stefania , BORTOLOZZO, Umberto , HUIGNARD, Jean-Pierre , BOUFFARON, Renaud , DOLFI, Daniel
IPC分类号： G01D5/353 , G01H9/00
CPC分类号： G01L1/242 , G01D5/353 , G01D5/35306 , G01H9/004
摘要： L'invention concerne un capteur à fibre optique distribué d'état de contrainte dynamique, comprenant : - un ensemble optique configuré pour générer une série d'impulsions optiques (l pi ); - une fibre optique (FO) de longueur optique L; - un système optique configuré pour : o injecter par ladite première extrémité (E x1 ) au moins ladite série d'impulsions optiques (l pi ); o recevoir au niveau de ladite extrémité (E x1 ) au moins une série d'impulsions optiques de sortie, issues desdites impulsions d'entrée après propagation et rétro-propagation dans la fibre; o générer au moins un faisceau de référence continu (Fr) ou des impulsions optiques de référence (l pri ) à partir dudit ensemble optique ou desdites impulsions optique de sortie (I psi ); o réaliser une série de zones d'interférences correspondant à l'interférence entre ledit faisceau de référence (Fr) ou une impulsion de référence (lpri) et une impulsion optique signal (l psiS ) issue d'une impulsion optique de sortie (l psi ); - un détecteur holographique (HD) comprenant : o une valve optique à cristal liquide (LCLV), ladite valve (LCLV) disposée de sorte qu'elle recouvre au moins partiellement lesdites zones d'interférence, et réalisant des hologrammes à partir desdites zones d'interférence; o au moins un détecteur optique (PD) configuré pour détecter des signaux optiques de sortie diffractés par lesdits hologrammes.
摘要翻译：本发明涉及用于感测动态应力状态的分布式光纤传感器，包括： - 被配置为产生一系列光脉冲（lpi）的光学组件; - 光学长度L的光纤（FO）; - 光学系统，被配置为：经由所述第一端（Ex1）注入至少所述一系列光脉冲（lpi）; 在所述端（Ex1）处接收来自光纤中传播和反向传播之后的所述输入脉冲的至少一系列输出光脉冲; o从所述光学组件或所述输出光脉冲（Ipsi）产生至少一个连续参考光束（Fr）或参考光脉冲（lpri）; o产生一系列相应于所述参考光束（Fr）或参考脉冲（lpri）与来自输出光脉冲（lpsi）的信号光脉冲（lpsiS）之间的干扰的干扰区域; - 全息检测器（HD），包括：液晶光阀（LCLV），所述阀（LCLV）以至少部分地覆盖所述干涉区域的方式布置，并且从所述干涉区域产生全息图; o至少一个光学检测器（PD），被配置为检测由所述全息图衍射的输出光信号。

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