公开(公告)号：US10676479B2

公开(公告)日：2020-06-09

申请号：US16311575

申请日：2017-06-09

Applicant: Novartis AG

Inventor： Ho Man Chan ,  Xingnian Fu ,  Xiang-Ju Justin Gu ,  Ying Huang ,  Ling Li ,  Yuan Mi ,  Wei Qi ,  Martin Sendzik ,  Yongfeng Sun ,  Long Wang ,  Zhengtian Yu ,  Hailong Zhang ,  Ji Yue Zhang ,  Man Zhang ,  Qiong Zhang ,  Kehao Zhao

IPC: C07D487/04 ,  A61P35/00

Abstract: A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R3, R4, R6, and R7 are as defined herein.

公开(公告)号：US12209098B2

公开(公告)日：2025-01-28

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: A61K31/497 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D471/10 ,  C07D491/107 ,  C07D495/10 ,  C07D498/10

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：US20240216513A1

公开(公告)日：2024-07-04

申请号：US18281732

申请日：2022-03-10

Applicant: Novartis AG

Inventor： Claire Adcock ,  Valerie Broennimann ,  Jiashun Cheng ,  Rohit Kumar Duvadie ,  Tanzina Fazal ,  Jinhai Gao ,  Fengfeng Guo ,  Robert Martin Grotzfeld ,  Christina Hebach ,  Gregory John Hollingworth ,  Darryl Brynley Jones ,  Alexei Karpov ,  Jialiang Li ,  Julien Lorber ,  Chester A. Metcalf, III ,  Walter Michael ,  Mark Gabriel Palermo ,  Scott Vaughan Plummer ,  James Harold Roache ,  Martin Sendzik ,  Ranny Mathew Thomas ,  Aimee Richardson Usera ,  Anna Vulpetti ,  Frederic Zecri ,  Liang Zhao ,  Thomas Zoller

IPC: A61K47/54 ,  A61K31/395 ,  A61K47/10 ,  A61P35/00

CPC classification number: A61K47/542 ,  A61K31/395 ,  A61K47/10 ,  A61P35/00

Abstract: Described herein are fatty acid-bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.

公开(公告)号：US20200181168A1

公开(公告)日：2020-06-11

申请号：US16418978

申请日：2019-05-21

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：US10167279B2

公开(公告)日：2019-01-01

申请号：US15510609

申请日：2015-09-11

Applicant: NOVARTIS AG

Inventor： Robert John Aversa ,  Matthew T. Burger ,  Michael Patrick Dillon ,  Thomas A. Dineen, Jr. ,  Yan Lou ,  Gisele A. Nishiguchi ,  Savithri Ramurthy ,  Alice C. Rico ,  Vivek Rauniyar ,  Martin Sendzik ,  Sharadha Subramanian ,  Lina Quattrocchio Setti ,  Benjamin R. Taft ,  Huw Rowland Tanner ,  Lifeng Wan

IPC: C07D405/14 ,  C07D405/12 ,  C07D305/06 ,  A61P35/00 ,  C07D413/14

Abstract: The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.

公开(公告)号：US20180201623A1

公开(公告)日：2018-07-19

申请号：US15899821

申请日：2018-02-20

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

CPC classification number: C07D498/10 ,  C07B2200/07 ,  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：US20150152093A1

公开(公告)日：2015-06-04

申请号：US14408418

申请日：2014-03-12

Applicant: NOVARTIS AG

Inventor： Thomas Raymond Caferro ,  Zhuoliang Chen ,  Young Shin Cho ,  Abran Q. Costales ,  Julian Roy Levell ,  Gang Liu ,  James R. Manning ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  James Sutton ,  Yaping Wang ,  Qian Zhao

IPC: C07D413/14 ,  C07D413/04 ,  A61K31/5377 ,  A61K31/506 ,  C07D417/14

CPC classification number: C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14

Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

Abstract translation: 本发明涉及式（I）：或其药学上可接受的盐，其中R1，R2a，R2b和R3-R7为本文。 本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。 本发明还涉及式（I）化合物在治疗与这种突变体IDH蛋白相关的疾病或病症中的用途，包括但不限于细胞增殖病症如癌症。

公开(公告)号：US08778951B2

公开(公告)日：2014-07-15

申请号：US13773052

申请日：2013-02-21

Applicant: Novartis AG

Inventor： Paul A. Barsanti ,  Cheng Hu ,  Jeff Jin ,  Robert Keyes ,  Robert Kucejko ,  Xiaodong Lin ,  Yue Pan ,  Keith B. Pfister ,  Martin Sendzik ,  James Sutton ,  Lifeng Wan

IPC: A61K31/50 ,  A61K31/501 ,  A61K31/497 ,  C07D241/20

CPC classification number: A61K31/497 ,  C07D213/74 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，对映体，立体异构体，旋转异构体，互变异构体，非对映体或其外消旋物。 还提供了治疗由CDK9介导的疾病或病症的方法。

公开(公告)号：US11905283B2

公开(公告)日：2024-02-20

申请号：US17130374

申请日：2020-12-22

Applicant: Novartis AG

Inventor： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Rajesh Karki ,  Matthew J. Lamarche ,  Dyuti Majumdar ,  Lawrence Blas Perez ,  Martin Sendzik ,  Troy Douglas Smith ,  Fan Yang ,  Bing Yu

IPC: C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D455/02 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D455/02 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

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






in which Y1, Y2, R1, R2 and R3 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：US11207325B2

公开(公告)日：2021-12-28

申请号：US16863631

申请日：2020-04-30

Applicant: Novartis AG

Inventor： Ho Man Chan ,  Xiang-Ju Justin Gu ,  Ying Huang ,  Ling Li ,  Yuan Mi ,  Wei Qi ,  Martin Sendzik ,  Yongfeng Sun ,  Long Wang ,  Zhengtian Yu ,  Hailong Zhang ,  Ji Yue (Jeff) Zhang ,  Man Zhang ,  Qiong Zhang ,  Kehao Zhao

IPC: A61K31/539 ,  A61K31/343 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D487/04 ,  A61K31/519 ,  A61K45/06

Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.