公开(公告)号：KR20180041222A

公开(公告)日：2018-04-23

申请号：KR20187007810

申请日：2016-08-25

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： WU TONGFEI ,  BREHMER DIRK ,  BEKE LIJS ,  BOECKX AN ,  DIELS GASTON STANISLAS MARCELLA ,  GILISSEN RONALDUS ARNODUS HENDRIKA JOSEPH ,  LAWSON EDWARD CHARLES ,  PANDE VINEET ,  PARADE MARCUS CORNELIS BERNARDUS CATHARINA ,  SCHEPENS WIM BERT GRIET ,  THURING JOHANNES WILHELMUS JOHN F ,  VIELLEVOYE MARCEL ,  SUN WEIMEI ,  MEERPOEL LIEVEN

IPC: C07D487/04 ,  A61K31/34 ,  A61K31/357 ,  A61K31/519 ,  A61P3/00 ,  A61P7/00 ,  A61P25/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: 본발명은하기화학식 I: [화학식 I](여기서, 변수들은청구범위에정의된의미를가짐)의신규한 6-6 이환식방향족고리치환뉴클레오시드유사체에관한것이다. 본발명에따른화합물은 PRMT5 저해제로서유용하다. 추가로본 발명은활성성분으로서상기화합물을포함하는제약조성물과, 약제로서의상기화합물의용도에관한것이다.

公开(公告)号：EP3126365B1

公开(公告)日：2018-01-10

申请号：EP15713523

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： DIELS GASTON STANISLAS MARCELLA ,  SCHOENTJES BRUNO ,  VERSELE MATTHIAS LUC AIMÉ ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WILLEMS MARC ,  VIELLEVOYE MARCEL ,  SOMMEN FRANÇOIS MARIA ,  WROBLOWSKI BERTHOLD ,  MEERPOEL LIEVEN

IPC: C07D471/22 ,  A61K31/505 ,  A61P35/00 ,  C07D498/22

CPC classification number: C07D471/22 ,  C07D491/22 ,  C07D498/22 ,  C07D513/22 ,  Y02P20/582

Abstract: wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：AU2020309745A1

公开(公告)日：2022-03-03

申请号：AU2020309745

申请日：2020-07-07

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ROMBOUTS FREDERIK JAN RITA ,  DIELS GASTON STANISLAS MARCELLA ,  JERHAOUI SOUFYAN ,  SURKYN MICHEL ,  VAN ROOSBROECK YVES EMIEL MARIA ,  JOUFFROY MATTHIEU DOMINIQUE

IPC: C07D513/22 ,  A61K31/553 ,  A61P35/00 ,  C07D513/20

Abstract: The present invention relates to pharmaceutical agents of formula (I) useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

公开(公告)号：CA3104055A1

公开(公告)日：2019-12-26

申请号：CA3104055

申请日：2019-06-13

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： LU TIANBAO ,  CONNOLLY PETER J ,  CUMMINGS MAXWELL DAVID ,  DIELS GASTON STANISLAS MARCELLA ,  THURING JAN WILLEM ,  PHILIPPAR ULRIKE ,  EDWARDS JAMES PATRICK ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WU TONGFEI

IPC: C07D471/04 ,  A61K31/4439 ,  A61P35/00

Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, R6, R7, G1 and G2, are defined herein.

公开(公告)号：AU2015239098B2

公开(公告)日：2019-08-01

申请号：AU2015239098

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEERPOEL LIEVEN ,  DIELS GASTON STANISLAS MARCELLA ,  SCHOENTJES BRUNO ,  VERSELE MATTHIAS LUC AIME ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WILLEMS MARC ,  VIELLEVOYE MARCEL ,  EMBRECHTS WERNER CONSTANT JOHAN ,  WROBLOWSKI BERTHOLD

IPC: C07D471/22 ,  A61K31/505 ,  A61P35/00 ,  C07D498/22

Abstract: The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：AU2015239100B2

公开(公告)日：2019-06-27

申请号：AU2015239100

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： DIELS GASTON STANISLAS MARCELLA ,  SCHOENTJES BRUNO ,  VERSELE MATTHIAS LUC AIME ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WILLEMS MARC ,  VIELLEVOYE MARCEL ,  SOMMEN FRANCOIS MARIA ,  WROBLOWSKI BERTHOLD ,  MEERPOEL LIEVEN

IPC: C07D471/22 ,  A61K31/505 ,  A61P35/00 ,  C07D498/22

Abstract: The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：PE20181894A1

公开(公告)日：2018-12-11

申请号：PE2018001785

申请日：2017-02-24

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BERTHELOT DIDIER JEAN-CLAUDE ,  BREHMER DIRK ,  BEKE LIJS ,  BOECKX AN ,  DIELS GASTON STANISLAS MARCELLA ,  GILISSEN RONALDUS ARNODUS HENDRIKA JOSEPH ,  LAWSON EDWARD CHARLES ,  PANDE VINEET ,  PARADE MARCUS CORNELIS BERNARDUS CATHARINA ,  SCHEPENS WIM BERT GRIET ,  SHOOK BRIAN CHRISTOPHER ,  THURING JOHANNES WILHELMUS JOHN F ,  VIELLEVOYE MARCEL ,  SUN WEIME ,  WU TONGFEI ,  MEERPOEL LIEVEN

IPC: C07D519/00 ,  A61K31/519 ,  A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D473/34 ,  C07D487/04 ,  C07H19/06 ,  C07H19/16

Abstract: Referido a analogos de nucleosidos sustituidos de formula (I); en donde R1 es H o CH3; R2 es H; Ra y Rb son, independientemente, H o -C(=0)-alquiloC1-4; Y es -O-, -CH2- o -CF2-; R7a es H; R7b es H, o alquilo C1-4 opcionalmente sustituido con uno o mas atomos halo; X1 es un enlace covalente o -O-; X2 es un enlace covalente, -CH2-, -CF2-, entre otros; X3 es N o CH; R8 y R10 se selecciona independientemente entre H, halo, y alquiloC1-6 opcionalmente sustituido; R9 y R11 se selecciona independientemente entre halo, -NH2, entre otros; Z es -CH2-, -C(=O)-, entre otros; y Het es un sistema anular heterociclico aromatico biciclico seleccionado entre (a-1), (a-2), (a-3) y (a-4). Dichos compuestos son inhibidores de PRMT5 (proteina arginina metil transferasa 5). Tambien se refiere a composiciones farmaceuticas que comprenden dichos compuestos, asi como su uso en el tratamiento o prevencion de enfermedades como trastorno metabolico, trastorno autoinmunitario, cancer, entre otros.

公开(公告)号：PE20180929A1

公开(公告)日：2018-06-08

申请号：PE2018000306

申请日：2016-08-25

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： WU TONGFEI ,  BREHMER DIRK ,  BEKE LIJS ,  BOECKX AN ,  DIELS GASTON STANISLAS MARCELLA ,  GILISSEN RONALDUS ARNODUS HENDRIKA JOSEPH ,  LAWSON EDWARD CHARLES ,  PANDE VINEET ,  PARADE MARCUS CORNELIS BERNARDUS CATHARINA ,  SCHEPENS WIM BERT GRIET ,  THURING JOHANNES WILHELMUS JOHN F ,  VIELLEVOYE MARCEL ,  SUN WEIME ,  MEERPOEL LIEVEN

IPC: C07D471/04 ,  A61K31/519 ,  A61K31/53

Abstract: SE REFIERE A COMPUESTOS ANALOGOS DE NUCLEOSIDOS SUSTITUIDOS EN EL ANILLO AROMATICO BICICLICO 6-6 DE FORMULA (I) DONDE R1 Y R2 SON CADA UNO H O -C-(=O)-(ALQUILO C1-C4); Y ES -O-, -CH2- O -CF2-; Z ES -CH2-, ETINILO, ENTRE OTROS; Ar ES UN SISTEMA ANULAR AROMATICO BICICLICO DE 10 MIEMBROS CONSTITUIDO POR DOS ANILLOS DE 6 MIEMBROS CONDENSADOS; Het ES UN SISTEMA ANULAR HETEROCICLICO AROMATICO BICICLICO. SON COMPUESTOS PREFERIDOS LOS DE FORMULA (i), (ii), ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA METILTRANSFERASA PRMT5 SIENDO UTILES EN EL TRATAMIENTO DE TRASTORNOS AUTOINMUNITARIOS, CANCER, ENFERMEDAD NEURODEGENERATIVA

公开(公告)号：EA029758B1

公开(公告)日：2018-05-31

申请号：EA201692000

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： DIELS GASTON STANISLAS MARCELLA ,  SCHOENTJES BRUNO ,  VERSELE MATTHIAS LUC AIME ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WILLEMS MARC ,  VIELLEVOYE MARCEL ,  SOMMEN FRANCOIS MARIA ,  WROBLOWSKI BERTHOLD ,  MEERPOEL LIEVEN

IPC: C07D471/22 ,  A61K31/505 ,  A61P35/00 ,  C07D498/22

Abstract: Изобретениеотноситсяк замещенныммакроциклическимпроизводнымпиримидинаформулы (I)гдепеременныеимеютзначения, определенныев формулеизобретения. Соединенияв соответствиис изобретениемобладают EF2K-ингибирующейактивностьюи необязательнотакже Vps34-ингибирующейактивностью. Изобретение, крометого, относитсяк способамполучениятакихновыхсоединений, кфармацевтическимкомпозициям, содержащимуказанныесоединенияв качествеактивногоингредиента, атакжек применениюуказанныхсоединенийв качествелекарственногопрепарата.

公开(公告)号：CA3016096A1

公开(公告)日：2017-09-14

申请号：CA3016096

申请日：2017-02-24

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BERTHELOT DIDIER JEAN-CLAUDE ,  BREHMER DIRK ,  BEKE LIJS ,  BOECKX AN ,  DIELS GASTON STANISLAS MARCELLA ,  GILISSEN RONALDUS ARNODUS HENDRIKA JOSEPH ,  LAWSON EDWARD CHARLES ,  PANDE VINEET ,  PARADE MARCUS CORNELIS BERNARDUS CATHARINA ,  SCHEPENS WIM BERT GRIET ,  SHOOK BRIAN CHRISTOPHER ,  THURING JOHANNES WILHELMUS JOHN F ,  VIELLEVOYE MARCEL ,  SUN WEIMEI ,  WU TONGFEI ,  MEERPOEL LIEVEN

IPC: C07D519/00 ,  A61K31/519 ,  A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D473/34 ,  C07D487/04 ,  C07H19/06 ,  C07H19/16

Abstract: The present invention relates novel substituted nucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.