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：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。

公开(公告)号：US20140357641A1

公开(公告)日：2014-12-04

申请号：US14371575

申请日：2013-01-11

Applicant: NOVARTIS AG

Inventor： Gurdip Bhalay ,  Steven Carl Chatlton ,  Mark Patrick Healy ,  Catherine Leblanc ,  Stephen Carl McKeown

IPC: C07D471/04 ,  A61K31/4985

CPC classification number: C07D471/04 ,  A61K31/4985

Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Formula (I):

Abstract translation: 本发明提供活化IP受体的杂环衍生物，制备它们的方法，包含所述衍生物的药物组合物及其用途。 激活IP受体信号通路可用于治疗多种形式的PAH，肺纤维化，并在动物模型和患者的各种器官的纤维化病症中发挥有益作用。 式（I）：