公开(公告)号：WO2021018857A1

公开(公告)日：2021-02-04

申请号：PCT/EP2020/071179

申请日：2020-07-28

Applicant: LES LABORATOIRES SERVIER ,  VERNALIS (R&D) LIMITED

Inventor： DAVIDSON, James Edward Paul ,  NOVÁK, Tibor ,  PACZAL, Attila ,  KOTSCHY, András ,  STARCK, Jérôme-Benoît ,  MURRAY, James Brooke ,  BEDFORD, Simon ,  CHANRION, Maïa ,  COLLAND, Frédéric ,  DESOS, Patrice ,  DODSWORTH, Mark Philip ,  DUNKEL, Petra ,  HERNER, András ,  MADARÁSZ, Zoltán ,  MARAGNO, Ana Leticia ,  MOLNÁR, Márk ,  NYERGES, Miklós ,  PARSONS, Rachel Jane ,  RUDASOVÁ, Monika ,  STROFEK, Ágnes ,  SZIGETI, Marianna ,  TIMÁRI, Mátyás Pál ,  WEBB, Paul

IPC: C07D417/12 ,  A61P35/00 ,  C07D417/14 ,  A61K31/428

Abstract: Compounds of formula (I) wherein Het 1 , Het 2 , R 1 , R 2 and R 3 are as defined in the description. Medicaments.

公开(公告)号：WO2022152705A1

公开(公告)日：2022-07-21

申请号：PCT/EP2022/050460

申请日：2022-01-11

Applicant: LES LABORATOIRES SERVIER ,  VERNALIS (R&D) LIMITED

Inventor： STOKES, Stephen ,  BEDFORD, Simon ,  CHEN, I-Jen ,  DAVIDSON, James Edward Paul ,  DAVIES, Nicholas ,  GRAHAM, Christopher John ,  MCKENNA, Sean Martin ,  MEISSNER, Johannes W.G. ,  MURRAY, James ,  PARSONS, Rachel Jane ,  RAY, Stuart ,  SANDERS, Emma ,  WALMSLEY, Claire Louise ,  BROUGH, Paul Andrew ,  KOTSCHY, András ,  PROSZENYÁK, Ágnes ,  SINAI, Ádám ,  BÁLINT, Balázs ,  CSÉKEI, Márton ,  ZWILLINGER, Márton ,  GARAMVÖLGYI, Rita ,  SIPOS, Szabolcs ,  KUN, Vilibald ,  SZABÓ, Zoltán ,  CHANRION, Maïa ,  ROCCHETTI, Francesca ,  COLLAND, Frédéric ,  MARAGNO, Ana Leticia ,  BRESSON, Laura

IPC: C07D205/04 ,  C07C71/00 ,  C07D213/72 ,  C07D215/233 ,  C07D221/20 ,  C07D401/12 ,  C07D405/12 ,  C07D491/056 ,  C07D495/04 ,  A61K31/404 ,  A61P35/00 ,  C07C49/697 ,  C07C233/52 ,  C07C229/50 ,  C07C323/61

Abstract: Compounds of Formula (I) wherein R1, R3, R11, R12, X, Y1, Y2, Y3, Y4 and formula (II) are as defined in the description. Medicaments.

公开(公告)号：WO2015040425A1

公开(公告)日：2015-03-26

申请号：PCT/GB2014/052876

申请日：2014-09-22

Applicant: VERNALIS (R&D) LIMITED

Inventor： BROUGH, Paul Andrew ,  MACIAS, Alba ,  ROUGHLEY, Stephen David ,  WANG, Yikang ,  PARSONS, Rachel Jane ,  NORTHFIELD, Christopher John

IPC: C07C235/64 ,  A61K31/16 ,  A61P35/00 ,  C07C255/60 ,  C07C275/40 ,  C07D209/02 ,  C07D211/06 ,  C07D213/04 ,  C07D215/02 ,  C07D231/00 ,  C07D233/64 ,  C07D235/04 ,  C07D237/00 ,  C07D239/02 ,  C07D241/12

CPC classification number: C07C255/60 ,  C07C235/64 ,  C07C237/42 ,  C07C275/40 ,  C07C2601/02 ,  C07C2601/08 ,  C07D209/02 ,  C07D209/42 ,  C07D211/26 ,  C07D211/46 ,  C07D211/58 ,  C07D213/40 ,  C07D213/61 ,  C07D213/62 ,  C07D213/71 ,  C07D213/73 ,  C07D215/12 ,  C07D215/18 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D235/14 ,  C07D235/26 ,  C07D237/08 ,  C07D237/12 ,  C07D237/20 ,  C07D237/30 ,  C07D239/26 ,  C07D239/28 ,  C07D239/30 ,  C07D239/34 ,  C07D239/42 ,  C07D239/74 ,  C07D239/78 ,  C07D241/12 ,  C07D241/42 ,  C07D261/08 ,  C07D261/18 ,  C07D295/13 ,  C07D333/20 ,  C07D333/58 ,  C07D333/60 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D498/04

Abstract: A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: Y is –CONR 1 - or optionally substituted arylene or optionally substituted heteroarylene; R 1 is H, Cl, F, CH 3 or CF 3 ; 10 each R4 is independently H, CH 3 or F; R 5 is H or CH 3 ; and each R 2 and R 6 is independently (Alk) n -R n -(Alk) n -Rn-(Alk) n -X; The compounds of the invention are useful as resorcinol N-aryl amide (NAA) compounds, which are suitable for use as PDK inhibitors, for example for 15 inhibition of cancer cell proliferation.

Abstract translation: 式I的化合物或其药学上可接受的盐，其中：Y是-CONR1-或任选取代的亚芳基或任选取代的亚杂芳基; R1是H，Cl，F，CH3或CF3; 10个，每个R 4独立地为H，CH 3或F; R5是H或CH3; 并且每个R 2和R 6独立地为（Alk）n-Rn-（Alk）n-Rn-（Alk）n-X; 本发明的化合物可用作间苯二酚N-芳酰胺（NAA）化合物，其适合用作PDK抑制剂，例如用于抑制癌细胞增殖的15种。