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1.发明申请Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases 有权亚苄基胍衍生物和治疗用于治疗蛋白质错折叠疾病的治疗用途公开(公告)号：US20160046589A1
公开(公告)日：2016-02-18
申请号：US14760350
申请日：2014-01-10
发明人： Philippe Guedat , Anne Bertolotti
IPC分类号： C07D253/075 , C07C281/16 , A61K31/165 , A61K31/216 , A61K31/44 , C07D213/61 , A61K31/155 , A61K31/53
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.
摘要翻译： 本发明涉及式（I）化合物或其互变异构体和/或其药学上可接受的盐，其中：R 1是烷基，Cl，F或Br; R2为H或F; R3选自H和烷基; R 4选自H和C（O）R 6; R5是H; 或R 4和R 5连接形成任选被一个或多个R 10基取代的杂环基; R6选自R7，OR7和NR8R9; R 7，R 8和R 9各自独立地选自烷基，环烷基，芳烷基，环烯基，杂环基和芳基，其各自任选被一个或多个R 10基团取代; 每个R 10独立地选自卤素，OH，CN，NO 2，COO-烷基，芳烷基，SO 2 - 烷基，SO 2 - 芳基，COOH，CO-烷基，CO-芳基，NH 2，NH-烷基，N（烷基） CF 3，烷基和烷氧基; X和Z各自独立地为CR11，Y选自CR11和N; R11为H或F; 用于治疗与蛋白质错误折叠应激相关的病症，特别是与错误折叠的蛋白质的积累相关。
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公开(公告)号：US11337941B2
公开(公告)日：2022-05-24
申请号：US16804353
申请日：2020-02-28
发明人： Anne Bertolotti , Indrajit Das , Agnieszka Krzyzosiak , Adrien Rousseau , Kim Schneider , Anna Gudny Sigurdardottir
IPC分类号： A61K31/155 , C07C281/18 , A61P25/28 , A61P25/14 , A61P21/00 , C12Q1/42 , C07D239/30 , C07D213/61 , G01N33/573 , C12N11/14 , G01N21/31 , G01N33/53
摘要： The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R1a, R3a, R5a, Xa and Ya are as defined herein.
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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：US11331286B2
公开(公告)日：2022-05-17
申请号：US16804402
申请日：2020-02-28
发明人： Anne Bertolotti , Indrajit Das , Agnieszka Krzyzosiak , Adrien Rousseau , Kim Schneider , Anna Gudny Sigurdardottir
IPC分类号： A61K31/155 , C07C281/18 , A61P25/28 , A61P25/14 , A61P21/00 , C12Q1/42 , C07D239/30 , C07D213/61 , G01N33/573 , C12N11/14 , G01N21/31 , G01N33/53
摘要： The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R1a, R3a, R5a, Xa and Ya are as defined herein.
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公开(公告)号：US11154519B2
公开(公告)日：2021-10-26
申请号：US15564834
申请日：2016-04-08
发明人： Anne Bertolotti , Indrajit Das , Agnieszka Krzyzosiak , Adrien Rousseau , Kim Schneider , Anna Gudny Sigurdardottir
IPC分类号： C07C281/18 , A61K31/155 , C12Q1/42 , C07D239/30 , C07D213/61 , A61P25/28 , G01N33/573 , A61P25/14 , A61P21/00 , C12N11/14 , G01N21/31 , G01N33/53
摘要： The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R1a, R3a, R5a, Xa and Ya are as defined herein.
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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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公开(公告)号：US11364211B2
公开(公告)日：2022-06-21
申请号：US15564863
申请日：2016-04-08
发明人： Anne Bertolotti , Indrajit Das , Agnieszka Krzyzosiak , Adrien Rousseau , Kim Schneider , Anna Gudny Sigurdardottir
IPC分类号： A61K31/155 , C07C281/18 , C07D213/61 , A61P21/00 , A61P25/14 , C12Q1/42 , C07D239/30 , A61P25/28 , G01N33/573 , C12N11/14 , G01N21/31 , G01N33/53
摘要： The present invention discloses a method to discover selective inhibitors of phosphatases. Thus the invention provides a method for screening a test compound to determine whether the compound binds a holophosphatase selectively or non-selectively comprising: i) providing a first holophosphatase wherein said holophosphatase is captured/immobilised; ii) testing a test compound for its ability to bind to the first holophosphatase; iii) providing a second holophosphatase wherein said second holophosphatase is captured/immobilised; iv) testing the same test compound for its ability to bind to the second holophosphatase; v) comparing the binding of the test compound to said first holophosphatase with the binding to said second phosphatase wherein a compound that binds a holophosphatase selectively will bind to said first holophosphatase but not said second holophosphatase; or will bind to said second holophosphatase but not said first; or wherein a compound that binds a holophosphatase non-selectively will bind to both said first holophosphatase and said second holophosphatase.
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