公开(公告)号：US09714221B1

公开(公告)日：2017-07-25

申请号：US15432470

申请日：2017-02-14

申请人： Sanofi

发明人： Monsif Bouaboula ,  Maurice Brollo ,  Victor Certal ,  Youssef El-Ahmad ,  Bruno Filoche-Romme ,  Frank Halley ,  Gary McCort ,  Laurent Schio ,  Michel Tabart ,  Corinne Terrier ,  Fabienne Thompson

IPC分类号： C07D207/12 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  A61K31/4025 ,  A61K31/341 ,  A61K31/351 ,  C07D471/04 ,  C07D413/12 ,  C07F7/08 ,  C07D417/12

CPC分类号： C07D207/12 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07F7/0812

摘要： Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.

公开(公告)号：US11214541B2

公开(公告)日：2022-01-04

申请号：US17124852

申请日：2020-12-17

申请人： SANOFI

发明人： Monsif Bouaboula ,  Maurice Brollo ,  Victor Certal ,  Youssef El-Ahmad ,  Bruno Filoche-Romme ,  Frank Halley ,  Gary Mccort ,  Laurent Schio ,  Michel Tabart ,  Corinne Terrier ,  Fabienne Thompson

IPC分类号： C07D207/12 ,  C07D403/12 ,  C07D401/12 ,  C07D471/04 ,  C07D405/12 ,  C07D413/12 ,  C07F7/08 ,  C07D417/12 ,  C07F5/02

摘要： Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.

公开(公告)号：US11149031B2

公开(公告)日：2021-10-19

申请号：US16414558

申请日：2019-05-16

申请人： SANOFI

发明人： Monsif Bouaboula ,  Maurice Brollo ,  Victor Certal ,  Youssef El-Ahmad ,  Bruno Filoche-Romme ,  Frank Halley ,  Gary McCort ,  Laurent Schio ,  Michel Tabart ,  Corinne Terrier ,  Fabienne Thompson

IPC分类号： A61P15/00 ,  A61P19/10 ,  A61P35/00 ,  C07D207/12 ,  C07D409/12 ,  C07D405/12

摘要： The present disclosure relates to novel substituted N-(3-fluoropropyl)-pyrrolidine compounds of formula (I-A), wherein R1 and R2 represent independently a hydrogen atom or a deuterium atom; A represents an oxygen or nitrogen atom; and SERM-F represents a selective estrogen receptor modulator fragment comprising an aryl or heteroaryl group linked to the adjacent “A” group. The disclosure also relates to the preparation and to the therapeutic uses of the compounds of formula (I-A) as inhibitors and degraders of estrogen receptors.

公开(公告)号：US10570090B2

公开(公告)日：2020-02-25

申请号：US15613689

申请日：2017-06-05

申请人： SANOFI

发明人： Monsif Bouaboula ,  Maurice Brollo ,  Victor Certal ,  Youssef El-Ahmad ,  Bruno Filoche-Romme ,  Frank Halley ,  Gary McCort ,  Laurent Schio ,  Michel Tabart ,  Corinne Terrier ,  Fabienne Thompson

IPC分类号： A61K31/40 ,  A61K31/025 ,  C07C13/32 ,  C07C22/08 ,  C07D207/12 ,  C07D403/12 ,  C07D401/12 ,  C07D471/04 ,  C07D405/12 ,  C07D413/12 ,  C07F7/08 ,  C07D417/12 ,  C07F5/02

摘要： Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.

公开(公告)号：US08993565B2

公开(公告)日：2015-03-31

申请号：US14312124

申请日：2014-06-23

申请人： Sanofi

发明人： Jean-Christophe Carry ,  Victor Certal ,  Frank Halley ,  Karl Andreas Karlsson ,  Laurent Schio ,  Fabienne Thompson

IPC分类号： A61K31/5377 ,  A61K31/538 ,  C07D239/22 ,  C07D239/47 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04

CPC分类号： C07D239/22 ,  C07D239/47 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04

摘要： The invention relates to the novel materials of formula (I), wherein each of the substituents R, R1, R2, R3, R4 and R5 is as defined herein. The materials are useful as inhibitors of AKT(PKB) phosphorylation.

摘要翻译： 本发明涉及式（I）的新型材料，其中取代基R 1，R 2，R 3，R 4和R 5中的每一个如本文所定义。 该物质可用作AKT（PKB）磷酸化抑制剂。