公开(公告)号：US20230092679A1

公开(公告)日：2023-03-23

申请号：US17613006

申请日：2020-05-19

Applicant: NOVARTIS AG ,  LES LABORATOIRES SERVIER

Inventor： Matthew T. Burger ,  Maia Chanrion ,  Frédéric Colland ,  Marton Csekei ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Jean-Michel Henlin ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  Eric McNeill ,  Mark G. Palermo ,  Francesca Rocchetti ,  Jérôme Starck ,  Bing Yu ,  Qiang Zhang ,  Ágnes Proszenyák ,  Szabolcs Sipos ,  Zhuoliang Chen ,  Katsumasa Nakajima ,  Joseph Anthony D'Alessio

IPC: A61K47/68 ,  A61K47/65 ,  A61K31/505 ,  A61P35/00

Abstract: Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20210371429A1

公开(公告)日：2021-12-02

申请号：US17182744

申请日：2021-02-23

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  John William Giraldes ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Martin Sendzik ,  Troy Douglas Smith ,  Bakary-Barry Toure ,  Sarah Williams

IPC: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

Abstract: The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20210309663A1

公开(公告)日：2021-10-07

申请号：US17191139

申请日：2021-03-03

Applicant: NOVARTIS AG

Inventor： Jeffrey T. Bagdanoff ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Patrick James Sarver ,  Michael Shultz ,  Troy Douglas Smith ,  Sarah Williams

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  A61K31/4523 ,  A61P35/00

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, Y4 R1, R2, R4a, R4b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20200369643A1

公开(公告)日：2020-11-26

申请号：US16987322

申请日：2020-08-06

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Denise Grunenfelder ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Travis Matthew Stams ,  Sarah Williams

IPC: C07D401/04 ,  C07D239/48 ,  C07D241/26 ,  C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US10287266B2

公开(公告)日：2019-05-14

申请号：US15736925

申请日：2016-06-15

Applicant: NOVARTIS AG

Inventor： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Andriana Jouk ,  Rajesh Karki ,  Matthew J. LaMarche ,  Gang Liu ,  Mark G. Palermo ,  Lawrence Blas Perez ,  Patrick James Sarver ,  Michael David Shultz ,  Martin Sendzik ,  Bakary-Barry Toure ,  Bing Yu

IPC: C07D401/14 ,  C07D401/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/10

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2, R4a, R4b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US11952386B2

公开(公告)日：2024-04-09

申请号：US17182756

申请日：2021-02-23

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  John William Giraldes ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Martin Sendzik ,  Troy Douglas Smith ,  Bakary-Barry Toure ,  Sarah Williams

IPC: C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07D498/10

CPC classification number: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07B2200/07

Abstract: The present invention relates to compounds of formula I:






in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20220396585A1

公开(公告)日：2022-12-15

申请号：US17182756

申请日：2021-02-23

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  John William Giraldes ,  Rajesh Karki ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Lawrence Blas Perez ,  Martin Sendzik ,  Troy Douglas Smith ,  Bakary-Barry Toure ,  Sarah Williams

IPC: C07D498/10 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10

Abstract: The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US09409871B2

公开(公告)日：2016-08-09

申请号：US13905686

申请日：2013-05-30

Applicant: NOVARTIS AG

Inventor： Feng He ,  Stefan Peukert ,  Karen Marie Miller-Moslin ,  Naeem Yusuff ,  Zhuoliang Chen ,  Bharat Lagu

IPC: C07D401/14 ,  C07D403/14 ,  C07D403/04 ,  C07D413/14 ,  A61K31/501 ,  A61K31/4523 ,  A61K31/4427 ,  C07D237/20 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D237/26 ,  A61P35/00

CPC classification number: C07D237/20 ,  A61K31/4427 ,  A61K31/4523 ,  A61K31/501 ,  C07D237/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04

Abstract: The present invention relates to compounds of formula I: in which L, W, X, Y, Z, m, p, R1, R2, R3, R4 and R7 are defined in the Summary of the Invention; capable of inhibiting the Hedgehog and Smo signaling pathway. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the diagnosis and treatment of pathologies relating to the Hedgehog and Smo signaling pathway, for example, tumor formation, cancer, neoplasia and non-malignant hyperproliferative disorders.

Abstract translation: 本发明涉及式I化合物：其中L，W，X，Y，Z，m，p，R 1，R 2，R 3，R 4和R 7在发明概述中定义; 能够抑制Hedgehog和Smo信号通路。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物诊断和治疗与Hedgehog和Smo信号传导途径有关的病理学的方法，例如肿瘤形成， 癌症，瘤形成和非恶性过度增生性疾病。

公开(公告)号：US20240269304A1

公开(公告)日：2024-08-15

申请号：US18038435

申请日：2021-11-23

Applicant: Novartis AG ,  Les Laboratoires Servier

Inventor： Matthew T. Burger ,  Zhuoliang Chen ,  Joseph Anthony D'Alessio ,  Eric McNeill ,  Katsumasa Nakajima ,  Richard Vaughan Newcombe ,  Mark G. Palermo ,  Bing Yu ,  Qiang Zhang ,  Frédéric Colland ,  James Edward Paul Davidson ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  James Brooke Murray ,  Tibor Novak ,  Jérôme Benoit Starck

IPC: A61K47/68 ,  A61P35/00

CPC classification number: A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  A61P35/00

Abstract: Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure farther relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20220089597A1

公开(公告)日：2022-03-24

申请号：US17191082

申请日：2021-03-03

Applicant: NOVARTIS AG

Inventor： Jeffrey T. Bagdanoff ,  Zhuoliang Chen ,  Michael Dore ,  Jorge Garcia Fortanet ,  Mitsunori Kato ,  Matthew J. LaMarche ,  Patrick James Sarver ,  Michael Shultz ,  Troy Douglas Smith ,  Sarah Williams

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  A61K31/4523 ,  A61P35/00

Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, Y4 R1, R2, R4a, R4b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.