公开(公告)号：US09403810B2

公开(公告)日：2016-08-02

申请号：US14711684

申请日：2015-05-13

Applicant: Novartis AG

Inventor： Kamlesh Jagdis Bala ,  Andrew Brearley ,  James Dale ,  Anne-Marie Edwards ,  Mahbub Ahmed ,  David Porter ,  Robert Alexander Pulz ,  Lisa Ann Rooney ,  David Andrew Sandham ,  Duncan Shaw ,  Nichola Smith ,  Jessica Louise Taylor ,  Roger John Taylor ,  Thomas Josef Troxler ,  Joe Wrigglesworth

IPC: C07D413/12 ,  C07D413/14 ,  A61K31/4155 ,  A61K31/422

CPC classification number: A61K31/422 ,  A61K31/4155 ,  C07D413/12 ,  C07D413/14 ,  A61K2300/00

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐; 制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。

公开(公告)号：US11208399B2

公开(公告)日：2021-12-28

申请号：US16874862

申请日：2020-05-15

Applicant: Novartis AG

Inventor： Christopher Farady ,  Nina Gommermann ,  Philipp Janser ,  Angela Mackay ,  Henri Mattes ,  Nichola Smith ,  Catherine Fooks Solovay ,  Nikolaus Johannes Stiefl ,  Eric Vangrevelinghe ,  Juraj Velcicky ,  Anette von Matt

IPC: C07D401/12 ,  C07D237/14 ,  C07D237/20 ,  C07D403/12 ,  C07D413/12 ,  C07D451/04

Abstract: The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R1, R2, R3, R4, R5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

公开(公告)号：US11672782B2

公开(公告)日：2023-06-13

申请号：US17089064

申请日：2020-11-04

Applicant: Novartis AG

Inventor： Kamlesh Jagdis Bala ,  Andrew Brearley ,  James Dale ,  Anne-Marie Edwards ,  Mahbub Ahmed ,  David Porter ,  Robert Alexander Pulz ,  Lisa Ann Rooney ,  David Andrew Sandham ,  Duncan Shaw ,  Nichola Smith ,  Jessica Louise Taylor ,  Roger John Taylor ,  Thomas Josef Troxler ,  Joe Wrigglesworth

IPC: A61K31/422 ,  A61K31/4155 ,  C07D413/12 ,  C07D413/14

CPC classification number: A61K31/422 ,  A61K31/4155 ,  C07D413/12 ,  C07D413/14 ,  A61K31/422 ,  A61K2300/00

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof;




a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US09522149B2

公开(公告)日：2016-12-20

申请号：US14690513

申请日：2015-04-20

Applicant: NOVARTIS AG

Inventor： Gurdip Bhalay ,  Lee Edwards ,  Catherine Howsham ,  Peter Hunt ,  Nichola Smith

IPC: A61K31/497 ,  C07D471/10

CPC classification number: A61K31/497 ,  C07D471/10

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

公开(公告)号：US11254653B2

公开(公告)日：2022-02-22

申请号：US16874905

申请日：2020-05-15

Applicant: Novartis AG

Inventor： Christopher Farady ,  Nina Gommermann ,  Philipp Janser ,  Angela Mackay ,  Henri Mattes ,  Nichola Smith ,  Catherine Fooks Solovay ,  Nikolaus Johannes Stiefl ,  Eric Vangrevelinghe ,  Juraj Velcicky ,  Anette von Matt

IPC: C07D401/12 ,  C07D237/14 ,  C07D237/20 ,  C07D403/12 ,  C07D413/12 ,  C07D451/04

Abstract: The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R1, R2, R3, R4, R5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

公开(公告)号：US10195181B2

公开(公告)日：2019-02-05

申请号：US15184730

申请日：2016-06-16

Applicant: Novartis AG

Inventor： Kamlesh Jagdis Bala ,  Andrew Brearley ,  James Dale ,  Anne-Marie Edwards ,  Mahbub Ahmed ,  David Porter ,  Robert Alexander Pulz ,  Lisa Ann Rooney ,  David Andrew Sandham ,  Duncan Shaw ,  Nichola Smith ,  Jessica Louise Taylor ,  Roger John Taylor ,  Thomas Josef Troxler ,  Joe Wrigglesworth

IPC: A61K31/422 ,  C07D413/14 ,  A61K31/4155 ,  C07D413/12

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US12139471B2

公开(公告)日：2024-11-12

申请号：US17574820

申请日：2022-01-13

Applicant: Novartis AG

Inventor： Christopher Farady ,  Nina Gommermann ,  Philipp Janser ,  Angela Mackay ,  Henri Mattes ,  Nichola Smith ,  Catherine Fooks Solovay ,  Nikolaus Johannes Stiefl ,  Eric Vangrevelinghe ,  Juraj Velcicky ,  Anette von Matt

IPC: C07D401/12 ,  C07D237/14 ,  C07D237/20 ,  C07D403/12 ,  C07D413/12 ,  C07D451/04

Abstract: The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R1, R2, R3, R4, R5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

公开(公告)号：US11530213B2

公开(公告)日：2022-12-20

申请号：US17071311

申请日：2020-10-15

Applicant: NOVARTIS AG

Inventor： Guillaume Barbe ,  Gregory Raymond Bebernitz ,  Sicong Geng ,  Hatice Belgin Gulgeze Efthymiou ,  Lv Liao ,  Fupeng Ma ,  Ruowei Mo ,  David Thomas Parker ,  Yunshan Peng ,  Stefan Peukert ,  Nichola Smith ,  Ken Yamada ,  Kayo Yasoshima

IPC: A61P9/00 ,  A61P9/06 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/675 ,  A61K45/06 ,  C07F9/6561

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; Wherein R1, R3-R6, X2 and X3 are as defined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US20210284635A1

公开(公告)日：2021-09-16

申请号：US17071311

申请日：2020-10-15

Applicant: NOVARTIS AG

Inventor： Guillaume BARBE ,  Gregory Raymond BEBERNITZ ,  Sicong GENG ,  Hatice Belgin GULGEZE EFTHYMIOU ,  Lv LIAO ,  Fupeng MA ,  Ruowei MO ,  David Thomas PARKER ,  Yunshan PENG ,  Stefan PEUKERT ,  Nichola Smith ,  Ken YAMADA ,  Kayo YASOSHIMA

IPC: C07D471/04 ,  A61P9/06 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/675 ,  A61K45/06 ,  C07F9/6561

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; Wherein R1, R3-R6, X2 and X3 are as defined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US09050339B2

公开(公告)日：2015-06-09

申请号：US13657001

申请日：2012-10-22

Applicant: NOVARTIS AG

Inventor： Gurdip Bhalay ,  Lee Edwards ,  Catherine Howsham ,  Peter Hunt ,  Nichola Smith

IPC: A61K31/497 ,  C07D241/10 ,  C07D471/10

CPC classification number: A61K31/497 ,  C07D471/10

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract translation: 式I化合物及其药学上可接受的盐和溶剂合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9和R10具有说明书中所示的含义，可用于治疗由 阻断上皮钠通道。 还描述了含有化合物的药物组合物和用于制备化合物的方法。