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：WO2017125224A1

公开(公告)日：2017-07-27

申请号：PCT/EP2016/081688

申请日：2016-12-19

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

Inventor： PACZAL, Attila ,  SZLÁVIK, Zoltán ,  KOTSCHY, András ,  CHANRION, Maïa ,  MARAGNO, Ana Leticia ,  GENESTE, Olivier ,  DEMARLES, Didier ,  BÁLINT, Balázs ,  SIPOS, Szabolcs

IPC: C07F9/6561 ,  A61P35/00 ,  A61K31/661 ,  A61K31/519 ,  C07D495/04

CPC classification number: C07F9/6561 ,  C07D495/04

Abstract: Compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and Y are as defined in the description. Medicaments.

Abstract translation: 式（I）的化合物：其中R 1，R 2，R 3，R 3，R 4， 4，R 5，R 6和Y如说明书中所定义。 药物

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：WO2021018858A1

公开(公告)日：2021-02-04

申请号：PCT/EP2020/071181

申请日：2020-07-28

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

Inventor： NOVAK, Tibor ,  DAVIDSON, James Edward Paul ,  PACZAL, Attila ,  STARCK, Jérôme-Benoit ,  KOTSCHY, András ,  MURRAY, James Brooke ,  BEDFORD, Simon ,  CHANRION, Maïa ,  COLLAND, Frédéric ,  DODSWORTH, Mark Philip ,  HERNER, András ,  MARAGNO, Ana Leticia ,  SANDERS, Emma ,  TIMÁRI, Mátyás Pál ,  WEBB, Paul

IPC: C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4709 ,  A61K31/427 ,  A61K31/428 ,  A61K31/404 ,  A61K31/538 ,  A61K31/4439 ,  A61K31/437 ,  A61K31/5025 ,  A61K31/4155 ,  A61K31/55 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02

Abstract: The present invention discloses 6,7-dihydro-5H-pyrido[2,3- c]pyridazine, 1,2,3,4-tetrahydroquinoline, 1H-indole, 3,4- dihydro-2H-1,4-benzoxazine, 1H-pyrrolo[2,3-b]pyridin-1-yl, 7H- pyrrolo[2,3-c]pyridazine, 5H,6H,7H,8H,9H-pyridazino[3,4-b]azepine derivatives and related compounds of formula (I) as Bcl-xL protein inhibitors for use as pro-apoptotic agents for treating cancer, autoimmune diseases or immune system diseases. Formula (I). The description discloses the preparation of exemplary compounds (e.g. pages 113 to 354 examples 1 to 221) as well as pharmacological studies with relevant data (e.g. pages 355 to 367; examples A to E; tables 1 to 5). Exemplary compounds are e.g. 2-{6-[(1,3-benzothiazol-2-yl) amino]-1,2,3,4-tetrahydroquinolin-1-yl}-1,3-thiazole-4-carboxylic acid (example 1) or e.g. 3-{1-[(adamantan-1-yl)methyl]-5- methyl-1H-pyrazol-4-yl}-6-{3-[(1,3-benzothiazol-2-yl)amino]-4- methyl-5H,6H,7H,8H-pyrido[2,3-c]pyridazin-8-yl]pyridine-2-carboxylic acid (example 24).

公开(公告)号：WO2018015526A1

公开(公告)日：2018-01-25

申请号：PCT/EP2017/068453

申请日：2017-07-21

Applicant: LES LABORATOIRES SERVIER ,  NOVARTIS AG

Inventor： WEI, Andrew ,  MOUJALLED, Donia ,  POMILIO, Giovanna ,  MARAGNO, Ana Leticia ,  GENESTE, Olivier ,  CLAPERON, Audrey ,  MAACKE, Heiko ,  HALILOVIC, Ensar ,  PORTER, Dale ,  MORRIS, Erick ,  WANG, Youzhen ,  SANGHAVI, Sneha ,  MISTRY, Prakash

IPC: A61K31/436 ,  A61K31/407 ,  A61K31/4353 ,  A61K31/519 ,  A61K31/55 ,  A61K31/675 ,  A61P35/00

Abstract: A combination comprising a BCL-2 inhibitor and a MCL1 inhibitor, and compositions and uses thereof.

Abstract translation: 包含BCL-2抑制剂和MCL1抑制剂的组合及其组合物和用途。

公开(公告)号：WO2018127575A1

公开(公告)日：2018-07-12

申请号：PCT/EP2018/050298

申请日：2018-01-05

Applicant: LES LABORATOIRES SERVIER ,  NOVARTIS AG

Inventor： PORTER, Dale ,  HALILOVIC, Ensar ,  CHANRION, Maïa ,  MARAGNO, Ana Leticia ,  GENESTE, Olivier ,  MERINO, Delphine ,  WHITTLE, James ,  VAILLANT, François ,  VISVADER, Jane ,  LINDEMAN, Geoffrey ,  LESSENE, Guillaume ,  MARANGONI, Elisabetta

IPC: A61K31/337 ,  A61K31/519 ,  A61K45/06 ,  A61P35/00

Abstract: A combination comprising a MCL-1 inhibitor and a taxane compound, and compositions and uses thereof.