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1.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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3.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：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：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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6.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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公开(公告)号：US09682943B2
公开(公告)日：2017-06-20
申请号：US14760350
申请日：2014-01-10
发明人： Philippe Guedat , Anne Bertolotti
IPC分类号： C07D213/61 , C07C281/18 , A61K31/155 , A61K31/44 , C07D253/075 , A61K31/53 , A61K45/06 , A61K31/165 , A61K31/216 , C07C281/16
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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