公开(公告)号：US20220119408A1

公开(公告)日：2022-04-21

申请号：US17603533

申请日：2020-04-09

申请人： Indena S.P.A.

发明人： Gabriele Fontana ,  Ruggero Beretta ,  Maurizio Taddei ,  Salvatore Princiotto

IPC分类号： C07D498/12

摘要： The invention discloses a process for the preparation of maytansinoid esters of formula (I) comprising a thiol or disulphide group wherein R1, R4 and R5 and the asterisk are as defined in the description, by reacting maytansinol with an enantiopure alpha-azido acid, followed by reduction of the azido group and reacting the obtained amino-ester with a compound of formula (IX) (IX) R3—S—S—X—COOH wherein X and R3 are as defined in the description, or with a reactive derivative thereof and optionally reducing the obtained disulfide-containing maytansinoid ester to give a maytansinoid ester wherein R1 is a —X—SH group.

公开(公告)号：US20160115111A1

公开(公告)日：2016-04-28

申请号：US14892153

申请日：2014-06-17

申请人： INDENA S.P.A.

发明人： Paolo Morazzoni ,  Antonella Riva ,  Gabriele Fontana

IPC分类号： C07C49/757

CPC分类号： C07C49/757 ,  C07C45/673 ,  C07C2602/46

摘要： Disclosed is a compound having the formula a) or b); a: R=CH3; b: R=CH2CH3, and its use in the prevention and/or treatment of Alzheimer's disease.

摘要翻译： 公开了具有式a）或b）的化合物; a：R = CH3; b：R = CH2CH3，以及其在预防和/或治疗阿尔茨海默病中的用途。

公开(公告)号：US11420981B2

公开(公告)日：2022-08-23

申请号：US17603533

申请日：2020-04-09

申请人： Indena S.P.A.

发明人： Gabriele Fontana ,  Ruggero Beretta ,  Maurizio Taddei ,  Salvatore Princiotto

IPC分类号： C07D498/18 ,  C07D498/12

摘要： The invention discloses a process for the preparation of maytansinoid esters of formula (I) comprising a thiol or disulphide group wherein R1, R4 and R5 and the asterisk are as defined in the description, by reacting maytansinol with an enantiopure alpha-azido acid, followed by reduction of the azido group and reacting the obtained amino-ester with a compound of formula (IX) (IX) R3—S—S—X—COOH wherein X and R3 are as defined in the description, or with a reactive derivative thereof and optionally reducing the obtained disulfide-containing maytansinoid ester to give a maytansinoid ester wherein R1 is a —X—SH group.

公开(公告)号：US09556099B2

公开(公告)日：2017-01-31

申请号：US14892153

申请日：2014-06-17

申请人： INDENA S.P.A.

发明人： Paolo Morazzoni ,  Antonella Riva ,  Gabriele Fontana

IPC分类号： C07C49/757 ,  C07C45/67

CPC分类号： C07C49/757 ,  C07C45/673 ,  C07C2602/46

摘要： Disclosed is a compound having the formula a) or b); a: R=CH3; b: R=CH2CH3, and its use in the prevention and/or treatment of Alzheimer's disease.

摘要翻译： 公开了具有式a）或b）的化合物; a：R = CH3; b：R = CH2CH3，以及其在预防和/或治疗阿尔茨海默病中的用途。