公开(公告)号：US20150210709A1

公开(公告)日：2015-07-30

申请号：US14154170

申请日：2012-07-13

Applicant: Novartis AG

Inventor： Atwood Kim Cheung ,  Donovan Noel Chin ,  Jianmei Fan ,  Michael David Shultz ,  Ronald Charles Tomlinson

IPC: C07D491/052

CPC classification number: C07D491/052 ,  A61K31/519

Abstract: The present invention provides for compounds of formula (I) wherein R1 and R2 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.

Abstract translation: 本发明提供式（I）化合物，其中R 1和R 2在本文中定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。

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：US10112931B2

公开(公告)日：2018-10-30

申请号：US15499824

申请日：2017-04-27

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 Clifford Sutton ,  Yaping Wang ,  Qian Zhao

IPC: C07D413/14 ,  C07D413/04 ,  C07D417/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

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.

公开(公告)号：US09688672B2

公开(公告)日：2017-06-27

申请号：US15209731

申请日：2016-07-13

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 Clifford Sutton ,  Yaping Wang ,  Qian Zhao

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

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.

公开(公告)号：US11485742B2

公开(公告)日：2022-11-01

申请号：US17065367

申请日：2020-10-07

Applicant: NOVARTIS AG

Inventor： Amy Calhoun ,  Xin Chen ,  Kevin Matthew Gardinier ,  Edward Charles Hall ,  Keith Jendza ,  Nancy Labbe-Giguere ,  James Neef ,  Daniel Steven Palacios ,  Ming Qian ,  Michael David Shultz ,  Christopher G. Thomson ,  Kate Yaping Wang ,  Fan Yang

IPC: C07D491/107 ,  A61P25/18 ,  A61K45/06

Abstract: Provided herein are compounds according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.

公开(公告)号：US09822092B2

公开(公告)日：2017-11-21

申请号：US14508285

申请日：2014-10-07

Applicant: Novartis AG

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

IPC: A61K31/402 ,  C07D207/30 ,  C07D333/22 ,  A61K31/381 ,  C07D213/50 ,  A61K31/4409 ,  C07D231/56 ,  A61K31/416 ,  A61K45/06

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.

公开(公告)号：US11820778B2

公开(公告)日：2023-11-21

申请号：US17818321

申请日：2022-08-08

Applicant: NOVARTIS AG

Inventor： Amy Calhoun ,  Xin Chen ,  Kevin Matthew Gardinier ,  Edward Charles Hall ,  Keith Jendza ,  Nancy Labbe-Giguere ,  James Neef ,  Daniel Steven Palacios ,  Ming Qian ,  Michael David Shultz ,  Christopher G. Thomson ,  Kate Yaping Wang ,  Fan Yang

IPC: C07D491/107 ,  A61P25/18 ,  A61K45/06

CPC classification number: C07D491/107 ,  A61K45/06 ,  A61P25/18

Abstract: Provided herein are compounds according to Formula (I)




or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.

公开(公告)号：US08975439B2

公开(公告)日：2015-03-10

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

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。

公开(公告)号：US12122761B2

公开(公告)日：2024-10-22

申请号：US18062356

申请日：2022-12-06

Applicant: NOVARTIS AG

Inventor： Amy Calhoun ,  Xin Chen ,  Kevin Matthew Gardinier ,  Edward Charles Hall ,  Keith Jendza ,  Nancy Labbe-Giguere ,  James Neef ,  Daniel Steven Palacios ,  Ming Qian ,  Michael David Shultz ,  Christopher G. Thomson ,  Kate Yaping Wang ,  Fan Yang

IPC: C07D401/04 ,  A61K45/06

CPC classification number: C07D401/04 ,  A61K45/06

Abstract: Provided herein are compounds according to Formula (I)




or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.

公开(公告)号：US11548865B2

公开(公告)日：2023-01-10

申请号：US17065360

申请日：2020-10-07

Applicant: NOVARTIS AG

Inventor： Amy Calhoun ,  Xin Chen ,  Kevin Matthew Gardinier ,  Edward Charles Hall ,  Keith Jendza ,  Nancy Labbe-Giguere ,  James Neef ,  Daniel Steven Palacios ,  Ming Qian ,  Michael David Shultz ,  Christopher G. Thomson ,  Kate Yaping Wang ,  Fan Yang

IPC: C07D401/04 ,  A61K45/06

Abstract: Provided herein are compounds according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.