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公开(公告)号：US11084783B2
公开(公告)日：2021-08-10
申请号：US16700327
申请日：2019-12-02
申请人： INFLECTIS BIOSCIENCE
发明人： Philippe Guedat
IPC分类号： C07C281/18 , C07C317/18 , C07C323/12 , C07D213/61 , C07D295/108 , A61K31/155 , A61K31/44 , C07D295/088
摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, and its uses to treat a disorder associated with protein misfolding stress and in particular with an accumulation of misfolded proteins.
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公开(公告)号：US10954198B2
公开(公告)日：2021-03-23
申请号：US16694694
申请日：2019-11-25
发明人： Philippe Guedat , Anne Bertolotti
IPC分类号： C07D253/075 , A61K31/155 , A61K31/44 , A61K31/53 , C07C281/18 , C07D213/61 , A61K45/06 , A61K31/165 , A61K31/216 , C07C281/16
摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
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公开(公告)号：US10544093B2
公开(公告)日：2020-01-28
申请号：US15316797
申请日：2015-07-02
申请人： INFLECTIS BIOSCIENCE
发明人： Philippe Guedat
IPC分类号： C07C281/18 , C07C317/18 , C07C323/12 , C07D213/61 , C07D295/088
摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof Formula (I), and its uses to treat a disorder associated with protein misfolding stress and in particular with an accumulation of misfolded proteins.
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4.发明申请公开(公告)号：US20180354914A1
公开(公告)日：2018-12-13
申请号：US16119445
申请日：2018-08-31
发明人： Philippe Guedat , Anne Bertolotti
IPC分类号： C07D253/075 , C07C281/16 , A61K31/155 , A61K31/165 , A61K45/06 , A61K31/216 , A61K31/44 , A61K31/53 , C07C281/18 , C07D213/61
CPC分类号： C07D253/075 , A61K31/155 , A61K31/165 , A61K31/216 , A61K31/44 , A61K31/53 , A61K45/06 , C07C281/16 , C07C281/18 , C07D213/61 , A61K2300/00
摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein R1 is alkyl, Cl, F or Br, R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups R6 is selected from R7, OR7 and NR8R6; R7R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocycyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen. OH, CN NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy, X and Z are each independently CR11 and Y is selected from CR11 and N and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
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公开(公告)号：US10100020B2
公开(公告)日：2018-10-16
申请号：US15467613
申请日：2017-03-23
发明人： Philippe Guedat , Anne Bertolotti
IPC分类号： C07D253/075 , C07D213/61 , C07C281/16 , A61K31/44 , A61K31/53 , A61K31/155 , A61K31/165 , C07C281/18 , A61K45/06 , A61K31/216
摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
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公开(公告)号：US10709677B2
公开(公告)日：2020-07-14
申请号：US15316785
申请日：2015-07-02
申请人： InFlectis BioScience
发明人： Philippe Guedat
IPC分类号： A61K31/155 , A61K31/44 , A61K31/53
摘要： The present invention relates to novel uses of a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, in treating a disorder associated with the PPP1R15A pathway and associated with protein misfolding stress and in particular with accumulation of misfolded proteins selected in the group of tauopathies, synucleinopathies, polyglutamine and polyalanine diseases, leukodystrophies, cystic fibrosis, multiple sclerosis, lysosomal storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardio-vascular disorders, osteoporosis, nervous system trauma, ischemia.
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7.发明申请公开(公告)号：US20200095210A1
公开(公告)日：2020-03-26
申请号：US16694694
申请日：2019-11-25
发明人： Philippe Guedat , Anne Bertolotti
IPC分类号： C07D253/075 , A61K31/155 , A61K31/44 , A61K31/53 , C07C281/18 , C07D213/61 , A61K45/06 , A61K31/165 , A61K31/216 , C07C281/16
摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
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公开(公告)号：US10526297B2
公开(公告)日：2020-01-07
申请号：US16119445
申请日：2018-08-31
发明人： Philippe Guedat , Anne Bertolotti
IPC分类号： C07D253/075 , A61K31/155 , A61K31/44 , A61K31/53 , C07C281/18 , C07D213/61 , A61K45/06 , A61K31/165 , A61K31/216 , C07C281/16
摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein R1 is alkyl, Cl, F or Br, R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups R6 is selected from R7, OR7 and NR8R6; R7R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocycyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN NO1, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy, X and Z are each independently CR11 and Y is selected from CR11 and N and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
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公开(公告)号：US10675257B2
公开(公告)日：2020-06-09
申请号：US15749485
申请日：2016-07-26
申请人： InFlectis BioScience
发明人： Philippe Guedat , Pierre Miniou
IPC分类号： A61K31/44 , A61K31/155 , A61K31/519 , A61P35/00 , A61K31/4188
摘要： The present invention relates to a composition for use in treating a glioma or ameliorating the effects of a glioma, particularly glioblastoma, wherein said composition comprises a first active agent selected from the group consisting of a compound of formula (I), or a pharmaceutically acceptable salt thereof, (I) and a second active agent, which is temozolomide, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.
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10.发明申请公开(公告)号：US20170247344A1
公开(公告)日：2017-08-31
申请号：US15467613
申请日：2017-03-23
发明人： Philippe Guedat , Anne Bertolotti
IPC分类号： C07D253/075 , C07C281/16 , A61K31/53 , C07C281/18 , A61K45/06 , A61K31/155 , A61K31/44 , A61K31/216 , A61K31/165 , C07D213/61
CPC分类号： C07D253/075 , A61K31/155 , A61K31/165 , A61K31/216 , A61K31/44 , A61K31/53 , A61K45/06 , C07C281/16 , C07C281/18 , C07D213/61 , A61K2300/00
摘要： The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein: R1 is alkyl, Cl, F or Br; R2 is H or F; R3 is selected from H and alkyl; R4 is selected from H and C(O)R6; R5 is H; or R4 and R5 are linked to form a heterocyclic group which is optionally substituted with one or more R10 groups; R6 is selected from R7, OR7 and NR8R9; R7, R8 and R9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocyclyl and aryl, each of which is optionally substituted with one or more R10 groups; each R10 is independently selected from halogen, OH, CN, NO2, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy; X and Z are each independently CR11, and Y is selected from CR11 and N; and R11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.
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