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：USRE46942E1

公开(公告)日：2018-07-10

申请号：US15786125

申请日：2017-10-17

Applicant: NOVARTIS AG

Inventor： Christine Hiu-Tung Chen ,  Donovan Noel Chin ,  Lucien V. DiPietro ,  Jianmei Fan ,  Mark G. Palermo ,  Michael David Shultz ,  Bakary-Barry Toure

IPC: C07D491/052 ,  C07D493/04 ,  C07D401/12 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/052 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

公开(公告)号：US20130096105A1

公开(公告)日：2013-04-18

申请号：US13690274

申请日：2012-11-30

Applicant: NOVARTIS AG

Inventor： Ruben Alberto Tommasi ,  Michael David Shultz ,  Leslie Wighton McQuire ,  Pascal Rigollier ,  Olivier Rogel ,  Claus Ehrhardt

IPC: A61K31/5375 ,  A61K31/18 ,  C07D213/40 ,  A61K31/4402 ,  C07D211/06 ,  A61K31/451 ,  C07D241/04 ,  A61K31/495 ,  C07D471/04 ,  A61K31/437 ,  C07D265/30 ,  C07D223/04 ,  A61K31/55 ,  A61K45/06 ,  C07C311/29

CPC classification number: C07D333/22 ,  A61K31/18 ,  A61K31/381 ,  A61K31/402 ,  A61K31/416 ,  A61K31/437 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/451 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/55 ,  A61K45/06 ,  C07C311/16 ,  C07C311/29 ,  C07C311/39 ,  C07C311/46 ,  C07C317/24 ,  C07C323/67 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D207/20 ,  C07D207/30 ,  C07D207/333 ,  C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D209/14 ,  C07D209/80 ,  C07D209/82 ,  C07D211/06 ,  C07D211/14 ,  C07D211/24 ,  C07D213/40 ,  C07D213/50 ,  C07D213/61 ,  C07D221/16 ,  C07D223/04 ,  C07D231/56 ,  C07D235/06 ,  C07D235/08 ,  C07D241/04 ,  C07D265/30 ,  C07D295/112 ,  C07D295/116 ,  C07D295/192 ,  C07D333/18 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Abstract translation: 本发明提供式（I）化合物：所述化合物是MMP-2和/或MMP-8和/或MMP-9和/或MMP-12和/或MMP-13的抑制剂，因此 可以用于治疗以MMP-2，/或MMP-8和/或MMP-9，和/或MMP-12和/或MMP-13异常活性为特征的疾病或疾病。 因此，式（I）化合物可用于治疗由MMP-2和/或MMP-8和/或MMP-9和/或MMP-12和/或MMP- 13。 最后，本发明还提供药物组合物。