公开(公告)号：US20230219898A1

公开(公告)日：2023-07-13

申请号：US18010642

申请日：2021-06-16

申请人： President and Fellows of Harvard College

发明人： Junying Yuan ,  Heng Zhao ,  Daichao Xu ,  Mingzhi Jin ,  Hong Zhu ,  Gregory D. Cuny

IPC分类号： C07D233/42 ,  C07D233/26 ,  C07C335/32 ,  C07D401/12 ,  C07D295/195 ,  C07D207/08 ,  A61K31/4178 ,  A61K31/4184

CPC分类号： C07D233/42 ,  C07D233/26 ,  C07C335/32 ,  C07D401/12 ,  C07D295/195 ,  C07D207/08 ,  A61K31/4178 ,  A61K31/4184

摘要： Disclosed herein are small molecules that inhibit apoptosis and promote autophagy through the TRADD pathway, and their use for treatment of neurodegenerative diseases. Methods of preparing these small molecules and medicinal efficacy are described.

公开(公告)号：US20190135718A1

公开(公告)日：2019-05-09

申请号：US16055898

申请日：2018-08-06

申请人： President and Fellows of Harvard College

发明人： Junying Yuan ,  Emily P. Hsu

IPC分类号： C07C35/37 ,  C07C33/38 ,  C07D233/02 ,  C07D211/78 ,  C07D498/08 ,  C07D495/04 ,  C07D417/12 ,  C07D405/06 ,  C07D403/12 ,  C07D403/06 ,  C07D333/20 ,  C07D307/52 ,  C07D277/46 ,  C07D231/56 ,  C07D231/12 ,  C07D231/06 ,  C07D215/08 ,  C07D211/90 ,  C07D209/08 ,  C07D277/18

摘要： The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

公开(公告)号：US20170305824A1

公开(公告)日：2017-10-26

申请号：US15427699

申请日：2017-02-08

申请人： President and Fellows of Harvard College

发明人： Junying Yuan ,  Emily P. Hsu

IPC分类号： C07C35/37 ,  C07C33/38 ,  C07D417/12 ,  C07D405/06 ,  C07D403/12 ,  C07D403/06 ,  C07D333/20 ,  C07D307/52 ,  C07D277/46 ,  C07D277/18 ,  C07D233/02 ,  C07D231/56 ,  C07D231/12 ,  C07D231/06 ,  C07D215/08 ,  C07D211/90 ,  C07D211/78 ,  C07D209/08 ,  C07D495/04 ,  C07D498/08

CPC分类号： C07C35/37 ,  C07C33/38 ,  C07D209/08 ,  C07D211/78 ,  C07D211/90 ,  C07D215/08 ,  C07D231/06 ,  C07D231/12 ,  C07D231/56 ,  C07D233/02 ,  C07D277/18 ,  C07D277/46 ,  C07D307/52 ,  C07D333/20 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D417/12 ,  C07D495/04 ,  C07D498/08

摘要： The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.