公开(公告)号：US09150540B2

公开(公告)日：2015-10-06

申请号：US14513814

申请日：2014-10-14

Applicant: Janssen Pharmaceutica, NV

Inventor： Patrick Rene Angibaud ,  Laurence Anne Mevellec ,  Bruno Roux ,  Pierre-Henri Storck ,  Christophe Meyer ,  Jorge Eduardo Vialard

IPC: C07D401/06 ,  C07D221/12 ,  A61K31/4353

CPC classification number: C07D401/06 ,  A61K31/4353 ,  C07D221/12

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.

Abstract translation: 本发明提供式（I）化合物，其作为微管蛋白聚合抑制剂及其作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R1，R2，R3，R4，R5，R6， R7和Y定义含义。

公开(公告)号：US10894793B2

公开(公告)日：2021-01-19

申请号：US16309999

申请日：2017-06-15

Applicant: Janssen Pharmaceutica NV

Inventor： Didier Jean-Claude Berthelot ,  Laurence Anne Mevellec ,  Patrick Rene Angibaud ,  Sophie Coupa ,  Christophe Gabriel Marcel Demestre ,  Lieven Meerpoel ,  Guillaume Jean Maurice Mercey ,  Christophe Meyer ,  Elisabeth Therese Jeanne Pasquter ,  Isabelle Noelle Constance Pilatte ,  Virginie Sophie Poncelet ,  Olivier Alexis Georges Querolle

IPC: C07D471/04 ,  C07D487/04 ,  A61P35/00

Abstract: The present invention relates to bicyclic pyridine, pyrazine, and pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ 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.

公开(公告)号：US10526316B2

公开(公告)日：2020-01-07

申请号：US15766887

申请日：2016-10-07

Applicant: Janssen Pharmaceutica NV

Inventor： Patrick Rene Angibaud ,  Olivier Alexis Georges Querolle ,  Didier Jean-Claude Berthelot ,  Christophe Meyer ,  Matthieu Philippe Victor Willot ,  Lieven Meerpoel ,  Thierry Francois Alain Jean Jousseaume

IPC: C07D403/10 ,  C07D487/04 ,  C07D495/10 ,  C07D498/10 ,  C07D471/04 ,  C07D241/42 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04 ,  C07D413/06 ,  C07D241/14 ,  C07D417/04 ,  C07D487/02 ,  C07D491/10 ,  C07D513/10

Abstract: The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ 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.

公开(公告)号：US20180057496A1

公开(公告)日：2018-03-01

申请号：US15537619

申请日：2015-12-18

Applicant: Janssen Pharmaceutica NV

Inventor： Laurence Anne Mevellec ,  Lieven Meerpoel ,  Sophie Coupa ,  Virginie Sophie Poncelet ,  Isabelle Noelle Constance Pilatte ,  Elisabeth Therese Jeanne Pasquier ,  Didier Jean-Claude Berthelot ,  Olivier Alexis Georges Querolle ,  Christophe Meyer ,  Patrick Rene Angibaud ,  Christophe Gabriel Marcel Demestre ,  Guillaume Jean Maurice Mercey

IPC: C07D487/04 ,  C07D519/00 ,  C07B59/00

CPC classification number: C07D487/04 ,  A61K31/5377 ,  C07B59/002 ,  C07B2200/05 ,  C07D405/10 ,  C07D519/00

Abstract: The present invention relates to heterocyclyl linked imidazopyridazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PI3Kβ inhibitors. 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：US09598396B2

公开(公告)日：2017-03-21

申请号：US14829493

申请日：2015-08-18

Applicant: Janssen Pharmaceutica NV

Inventor： Patrick Rene Angibaud ,  Laurence Anne Mevellec ,  Bruno Roux ,  Pierre-Henri Storck ,  Christophe Meyer ,  Jorge Eduardo Vialard

IPC: C07D221/12 ,  C07D401/06 ,  A61K31/4353

CPC classification number: C07D401/06 ,  A61K31/4353 ,  C07D221/12

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.

公开(公告)号：US11267804B2

公开(公告)日：2022-03-08

申请号：US16680605

申请日：2019-11-12

Applicant: Janssen Pharmaceutica NV

Inventor： Patrick Rene Angibaud ,  Olivier Alexis Georges Querolle ,  Didier Jean-Claude Berthelot ,  Christophe Meyer ,  Matthieu Philippe Victor Willot ,  Lieven Meerpoel ,  Thierry Francois Alain Jean Jousseaume

IPC: C07D241/44 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D498/10 ,  C07D487/02 ,  C07D241/14 ,  C07D403/06 ,  C07D417/04 ,  C07D403/04 ,  C07D413/04 ,  C07D401/06 ,  C07D513/10 ,  C07D491/10 ,  C07D413/06 ,  C07D401/04 ,  C07D413/14 ,  C07D495/04 ,  C07D241/42 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07D495/10

Abstract: The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ 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.

公开(公告)号：US20150353526A1

公开(公告)日：2015-12-10

申请号：US14829493

申请日：2015-08-18

Applicant: Janssen Pharmaceutica NV

Inventor： Patrick Rene Angibaud ,  Laurence Anne Mevellec ,  Bruno Roux ,  Pierre-Henri Storck ,  Christophe Meyer ,  Jorge Eduardo Vialard

IPC: C07D401/06 ,  C07D221/12

CPC classification number: C07D401/06 ,  A61K31/4353 ,  C07D221/12

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.

公开(公告)号：US20190263804A1

公开(公告)日：2019-08-29

申请号：US16310413

申请日：2017-06-15

Applicant: Janssen Pharmaceutica NV

Inventor： Isabelle Noelle Constance Pilatte ,  Laurence Anne Mevellec ,  Patrick Rene Angibaud ,  Sophie Coupa ,  Christophe Gabriel Marcel Demestre ,  Lieven Meerpoel ,  Guillaume Jean Maurice Mercey ,  Christophe Meyer ,  Elisabeth Therese Jeanne Pasquier ,  Olivier Alexis Georges Querolle ,  Virginie Sophie Poncelet ,  Didier Jean-Claude Berthelot

IPC: C07D471/04 ,  A61P35/00

Abstract: The present invention relates to azabenzimidazole derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ 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.

公开(公告)号：US10202387B2

公开(公告)日：2019-02-12

申请号：US15537619

申请日：2015-12-18

Applicant: Janssen Pharmaceutica NV

Inventor： Laurence Anne Mevellec ,  Lieven Meerpoel ,  Sophie Coupa ,  Virginie Sophie Poncelet ,  Isabelle Noelle Constance Pilatte ,  Elisabeth Therese Jeanne Pasquier ,  Didier Jean-Claude Berthelot ,  Olivier Alexis Georges Querolle ,  Christophe Meyer ,  Patrick Rene Angibaud ,  Christophe Gabriel Marcel Demestre ,  Guillaume Jean Maurice Mercey

IPC: A61K31/5377 ,  C07D487/04 ,  C07D405/10 ,  C07B59/00 ,  C07D519/00

Abstract: The present invention relates to heterocyclyl linked imidazopyridazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PI3Kβ inhibitors. 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：US20180327401A1

公开(公告)日：2018-11-15

申请号：US16040004

申请日：2018-07-19

Applicant: Janssen Pharmaceutica NV

Inventor： Peter J. Connolly ,  Gilles C. Bignan ,  Tianbao Lu ,  Michael H. Parker ,  Donald W. Ludovici ,  Christophe Meyer ,  Lieven Meerpoel ,  Karine Smans ,  Christian Rocaboy

IPC: C07D417/14 ,  C07D498/04 ,  C07D491/107 ,  C07D487/10 ,  C07D471/10 ,  C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D403/06 ,  C07D401/06 ,  C07D413/14 ,  C07D405/14 ,  C07D409/14

CPC classification number: C07D417/14 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10 ,  C07D491/107 ,  C07D498/04

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.