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1. 发明公开

EP1807084A2 UTILISATION DE DERIVES DE PYRROLO-PYRAZINES POUR LE TRAITEMENT DE LA MUCOVISCIDOSE 有权
标题翻译：吡咯并吡嗪，用于治疗囊性纤维化的用途
公开(公告)号：EP1807084A2
公开(公告)日：2007-07-18
申请号：EP05804722.6
申请日：2005-10-14
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE DE POITIERS
发明人： BECQ, Frédéric , MEIJER, Laurent , METTEY, Yvette
IPC分类号： A61K31/4985 , A61P11/00 , A61P1/00
CPC分类号： A61K31/4985
摘要： The invention relates to the use of pyrrolopyrazine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of formula (I): where R2 and R3 independently = H, C1-C6 straight or branched chain optionally-substituted alkyl, R6 = an aromatic ring Ar or cycloalkyl, optionally substituted, said cycloalkyl optionally substituted by an aryl group which may equally be substituted, R7 = H, C1-C6 alkyl, (alk.)n-Hal, CH2-CH = CH2, CH2-cycloalkyl, CH2-Ar and Z = H or CH3.

2. 发明授权

EP1807084B1 UTILISATION DE DERIVES DE PYRROLO-PYRAZINES POUR LE TRAITEMENT DE LA MUCOVISCIDOSE 有权
标题翻译：吡咯并吡嗪，用于治疗囊性纤维化的用途
公开(公告)号：EP1807084B1
公开(公告)日：2010-12-15
申请号：EP05804722.6
申请日：2005-10-14
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE DE POITIERS
发明人： BECQ, Frédéric , MEIJER, Laurent , METTEY, Yvette
IPC分类号： A61K31/4985 , A61P11/00 , A61P1/00
CPC分类号： A61K31/4985
摘要： The invention relates to the use of pyrrolopyrazine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of formula (I): where R2 and R3 independently = H, C1-C6 straight or branched chain optionally-substituted alkyl, R6 = an aromatic ring Ar or cycloalkyl, optionally substituted, said cycloalkyl optionally substituted by an aryl group which may equally be substituted, R7 = H, C1-C6 alkyl, (alk.)n-Hal, CH2-CH = CH2, CH2-cycloalkyl, CH2-Ar and Z = H or CH3.

3. 发明公开

EP1802310A1 UTILISATION DE DERIVES DE PURINES POUR LA FABRICATION DE MEDICAMENTS POUR LE TRAITEMENT DE LA MUCOVISCIDOSE ET DE MALADIES LIEES A UN DEFAUT D'ADRESSAGE DES PROTEINES DANS LES CELLULES 有权
标题翻译：嘌呤衍生物的药品学报囊性纤维化和疾病相关的与PROTEINADRESSIERFEHLERN细胞中的治疗制剂中使用
公开(公告)号：EP1802310A1
公开(公告)日：2007-07-04
申请号：EP05804720.0
申请日：2005-10-14
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE DE POITIERS
发明人： BECQ, Frédéric , MEIJER, Laurent
IPC分类号： A61K31/52 , A61P11/00
CPC分类号： A61K31/52
摘要： The invention relates to the use of purine derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of formula (I): where R2, R6 and R9, independently = halogen, a R-NH-, R-NH-NH-, NH2-R'-NH- or R-NH-R'-NH- group, where R = straight or branched chain saturated or unsaturated alkyl, aryl, cycloalkyl, or heterocyclyl group, R' = straight or branched chain, saturated or unsaturated alkylene, arylene or cycloalkylene, R and R' each include 1 to 8 carbon atoms optionally substituted with one or more -OH, halogen, amino or alkyl groups, R2 furthermore may be a heterocycle optionally with a straight or branched chain saturated or unsaturated alkyl, aryl or cycloaryl or a heterocycle optionally substituted by one or more -OH, halogen, amino or alkyl groups, R9 furthermore may be a straight or branched chain saturated or unsaturated alkyl, aryl or cycloalkyl and R2 and R9 furthermore may be hydrogen with the exception of 2-(2-hydroxyethylamino)-6-benzylamino-9-methylpurine.

4. 发明授权

EP1799225B1 UTILISATION DE DERIVES DE PAULLONES POUR LA FABRICATION DE MEDICAMENTS POUR LE TRAITEMENT DE LA MUCOVISCIDOSE ET DE MALADIES LIEES A DEFAUT D'ADRESSAGE DES PROTEINES DANS LES CELLULES 有权
标题翻译： PAULLON衍生物用于药物的囊肿性纤维化和疾病的治疗制剂中由于蛋白质在寻址错误细胞
公开(公告)号：EP1799225B1
公开(公告)日：2011-12-07
申请号：EP05809765.0
申请日：2005-10-14
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE DE POITIERS
发明人： BECQ, Frédéric , MEIJER, Laurent , KUNICK, Conrad
IPC分类号： A61K31/55 , A61P11/12
CPC分类号： A61K31/55
摘要： The invention relates to paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of general formula (I): where X = C=O, C-S-CH3, C-S,-C-NHOH, Z = C or N, Y = with the adjacent ring, a phenyl or thiazolyl group, the ring(s) of said derivatives being optionally substituted with one or more halogen atoms, hydroxy, alkylenehydroxy, alkynealkylenehydroxy, alkynehydroxycyclohexyl, alkyl, alkoxy, alkylenealkoxy, or alkylenecyano groups where the alkylene group is either saturated or unsaturated, the groups having a straight or branched chain with C1 to C18, said chain being optionally substituted with one or more hydroxy or amino groups, or one or more trifluoromethyl, -COM, -COOM, or -CH2COOM groups (where M = H, C1 to C18 straight or branched chain alkyl, optionally substituted with one or more hydroxy and/or amino groups), nitroso, or cyano, R5 = H, or C1 to C5 alkyl and R12 = H, or -C-CO2-(CH3)3 and the physiologically-acceptable salts and derivatives thereof.

5. 发明公开

EP1799225A1 UTILISATION DE DERIVES DE PAULLONES POUR LA FABRICATION DE MEDICAMENTS POUR LE TRAITEMENT DE LA MUCOVISCIDOSE ET DE MALADIES LIEES A DEFAUT D'ADRESSAGE DES PROTEINES DANS LES CELLULES 有权
标题翻译： PAULLON衍生物用于药物的囊肿性纤维化和疾病的治疗制剂中由于蛋白质在寻址错误细胞
公开(公告)号：EP1799225A1
公开(公告)日：2007-06-27
申请号：EP05809765.0
申请日：2005-10-14
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE DE POITIERS
发明人： BECQ, Frédéric , MEIJER, Laurent , KUNICK, Conrad
IPC分类号： A61K31/55 , A61P11/12
CPC分类号： A61K31/55
摘要： The invention relates to paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of general formula (I): where X = C=O, C-S-CH3, C-S,-C-NHOH, Z = C or N, Y = with the adjacent ring, a phenyl or thiazolyl group, the ring(s) of said derivatives being optionally substituted with one or more halogen atoms, hydroxy, alkylenehydroxy, alkynealkylenehydroxy, alkynehydroxycyclohexyl, alkyl, alkoxy, alkylenealkoxy, or alkylenecyano groups where the alkylene group is either saturated or unsaturated, the groups having a straight or branched chain with C1 to C18, said chain being optionally substituted with one or more hydroxy or amino groups, or one or more trifluoromethyl, -COM, -COOM, or -CH2COOM groups (where M = H, C1 to C18 straight or branched chain alkyl, optionally substituted with one or more hydroxy and/or amino groups), nitroso, or cyano, R5 = H, or C1 to C5 alkyl and R12 = H, or -C-CO2-(CH3)3 and the physiologically-acceptable salts and derivatives thereof.

6. 发明公开

EP2185547A2 DERIVES D'IMIDAZOLONES, PROCEDE DE PREPARATION ET APPLICATIONS BIOLOGIQUES 有权转让
标题翻译：咪达洛丹德，VERFAHREN ZU IHRER HERSTELLUNG UND BIISCHE ANWENDUNG DAVON
公开(公告)号：EP2185547A2
公开(公告)日：2010-05-19
申请号：EP08838929.1
申请日：2008-08-01
申请人： Universite Rennes 1 , Centre National de la Recherche Scientifique- CNRS
发明人： CARREAUX, François , BAZUREAU, Jean-Pierre , RENAULT, Stéven , MEIJER, Laurent , LOZACH, Olivier
IPC分类号： C07D405/06 , C07D405/14 , C07D233/96 , A61K31/4166 , A61K31/4178
CPC分类号： C07D405/06 , C07D233/96 , C07D405/14
摘要： The invention relates to imidazolone derivatives and the use thereof as drugs, having formula (I), wherein: R1 = H, alkyl at C1 to C5, aryl, or a heterocyclic group with 5 or 6 elements; Ar1 = aryl, optionally substituted, or an aromatic heterocycle; R = R2-S-, R3-HN-, R4COHN or Ar2, with - R2 = an alkyl radical at C1-C5, vinyl or alkyl-vinyl at C1-C5, nitrile or alkyl-nitrile at C1-C5, aryl, benzyl, which are optionally substituted; - R3 = as defined above; and - Ar2 = substituted or non-substituted aryl.
摘要翻译：可用作药物的咪唑啉酮衍生物（I）是新的。可用作药物的式（I）咪唑啉酮衍生物是新的。 R 1，C 1 -C 5烷基（任选取代的），芳基或5或6杂环基（其中芳基和杂环基团任选地包含一个或多个占据任何位置的取代基）; Ar 1芳基（任选地包含一个或多个取代基和两个相邻的取代基，其形成5或6元环（任选取代的））或具有任选一个或多个取代基的芳族杂环和/或与5或6元芳族环或N的杂原子稠合， S或O; R：R 2 -S-，R 3-HN-，R 4COHN或Ar 2; R 2线性，支化或环状的1-5C烷基，乙烯基或1-5C乙烯基 - 烷基，腈或1-5C-腈 - 烷基，芳基或苄基（全部任意取代，在一个或多个碳原子上，被一个或多个占据形成5或6元环（任选取代）的任何位置和两个相邻取代基）; R 3R 2或H; R 43-5C烷基; 和Ar 2取代的芳基或形成5或6元环（任选取代的）的两个相邻取代基。活动：神经保护; 精神药物; 脑保护。作用机制：双特异性酪氨酸磷酸化调节激酶（DYRK）1A抑制剂。测试（I）抑制双特异性酪氨酸磷酸化调节激酶的能力。结果表明，（I）显示的IC 50值小于5〜mM，优选小于1〜mM。

7. 发明授权

EP1585523B1 USE OF PURINE DERIVATIVES FOR INDUCING DIFFERENTIATION OF SUPERNUMERARY HAIR CELLS AND DEITERS' CELLS IN THE DEVELOPING ORGAN OF CORTI FOR TREATING DEAFNESS 有权
标题翻译：嘌呤衍生物用于分化诱导盈余毛细胞和细胞Deiter在开发CORTI机关性耳聋的治疗
公开(公告)号：EP1585523B1
公开(公告)日：2008-10-01
申请号：EP03812071.3
申请日：2003-12-17
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
发明人： MEIJER, Laurent , KNOCKAERT, Marie , MALGRANGE, Brigitte
IPC分类号： A61K31/52 , A61P27/16
CPC分类号： A61K31/522 , A61K31/404 , A61K31/519
摘要： Use of at least one kinase inhibitor for making drugs for inducing differentiation of supernumerary hair cells and Deiters' cells in the developing organ of Corti.

8. 发明授权

EP2328866B1 3',6-SUBSTITUTED INDIRUBINS AND THEIR BIOLOGICAL APPLICATIONS 有权
标题翻译： 3”，6-取代的炮弹树碱及其生物应用
公开(公告)号：EP2328866B1
公开(公告)日：2012-02-29
申请号：EP09802595.0
申请日：2009-07-21
申请人： Centre National de la Recherche Scientifique (CNRS)
发明人： MEIJER, Laurent , SKALTSOUNIS, Leandros , MIKROS, Emmanuel , MAGIATIS, Prokopios , JOHNSON, Carl
IPC分类号： C07D209/40 , A61K31/404 , A61P35/00 , A61P25/00
CPC分类号： C07D209/40
摘要： Indirubin derivatives of formula (I) wherein R represents - (A)
n - R
1 or -CO-N(R
2 ,R
3 ) with • A being C1-C5 alkylene group, optionally substituted by one or several A
1 radical, A
1 being an halogen Br, OH, OR
4 or NH
2 , R
4 being C1-C5 alkyl; - R
1 being halogen, OH, N(R
2 , R
3 ); R
2 and R
3 , identical or different, being C 1 -C5 alkyl, optionally substituted by A
1 such as above defined, or R
2 and R
3 are part of a cycle with 5 or 6 elements optionally comprising another heteroatom such as O or N; • n = 1-5. It also relates to the biological application thereof.

9. 发明公开

EP2328866A1 3',6-SUBSTITUTED INDIRUBINS AND THEIR BIOLOGICAL APPLICATIONS 有权
标题翻译： 3”，6-取代的炮弹树碱及其生物应用
公开(公告)号：EP2328866A1
公开(公告)日：2011-06-08
申请号：EP09802595.0
申请日：2009-07-21
申请人： Centre National de la Recherche Scientifique (CNRS)
发明人： MEIJER, Laurent , SKALTSOUNIS, Leandros , MIKROS, Emmanuel , MAGIATIS, Prokopios , JOHNSON, Carl
IPC分类号： C07D209/40 , A61K31/404 , A61P35/00 , A61P25/00
CPC分类号： C07D209/40
摘要： Indirubin derivatives of formula (I) wherein R represents - (A)
n - R
1 or -CO-N(R
2 ,R
3 ) with • A being C1-C5 alkylene group, optionally substituted by one or several A
1 radical, A
1 being an halogen Br, OH, OR
4 or NH
2 , R
4 being C1-C5 alkyl; - R
1 being halogen, OH, N(R
2 , R
3 ); R
2 and R
3 , identical or different, being C 1 -C5 alkyl, optionally substituted by A
1 such as above defined, or R
2 and R
3 are part of a cycle with 5 or 6 elements optionally comprising another heteroatom such as O or N; • n = 1-5. It also relates to the biological application thereof.

10. 发明公开

EP1686988A1 INDIRUBIN-TYPE COMPOUNDS, COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译：连接来源于靛类型和组合物的方法
公开(公告)号：EP1686988A1
公开(公告)日：2006-08-09
申请号：EP04817477.5
申请日：2004-10-28
申请人： THE ROCKEFELLER UNIVERSITY , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
发明人： MEIJER, Laurent , GREENGARD, Paul , KNOCKAERT, Marie , SKALTOUNIS, Alexios-Leandros
IPC分类号： A61K31/404 , C07D403/04
CPC分类号： C07D209/34 , A61K31/404 , Y02A50/411
摘要： Compounds and compositions including 6-bromo-indirubin, 5-amino-indirubin and N-methyl-indirubins and related indirubin derivatives are provided that are useful as selective modulators of glycogen synthase kinase-3, cyclin-dependent protein kinases or aryl hydrocarbon receptors. Methods of inhibiting or modulating cell growth or cell cycling are provided using the compounds of the invention. In other aspects, compounds and methods for the treatment of protozoan-mediated diseases, Alzheimer's disease and diabetes are provided.

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