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：US20180125849A1

公开(公告)日：2018-05-10

申请号：US15867425

申请日：2018-01-10

Applicant: Novartis AG

Inventor： Graham Charles Bloomfield ,  Ian Bruce ,  Brian Cox ,  Lee Edwards ,  Judy Fox Hayler ,  Catherine Howsham

IPC: A61K31/519 ,  A61K31/5377 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5377 ,  C07D487/04

Abstract: The present invention concerns a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, where R1-R3 and Y are defined in the description, and its use in the treatment of disorders in which pi3 kinase is implicated.

公开(公告)号：US08901134B2

公开(公告)日：2014-12-02

申请号：US14261890

申请日：2014-04-25

Applicant: Novartis AG

Inventor： Graham Charles Bloomfield ,  Ian Bruce ,  Brian Cox ,  Lee Edwards ,  Judy Fox Hayler ,  Catherine Howsham

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5377 ,  C07D487/04

Abstract: The present invention concerns a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, where R1-R3 and Y are defined in the description, and its use in the treatment of disorders in which pi3 kinase is implicated.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐或溶剂合物，其中R1-R3和Y在说明书中定义，及其用于治疗其中涉及pi3激酶的病症。

公开(公告)号：USRE46757E1

公开(公告)日：2018-03-20

申请号：US14755691

申请日：2015-06-30

Applicant: Novartis AG

Inventor： Urs Baettig ,  Kamlesh Jagdis Bala ,  Emma Budd ,  Lee Edwards ,  Catherine Howsham ,  Glyn Alan Hughes ,  Darren Mark Legrand ,  Katrin Spiegel

IPC: A61K31/5355 ,  C07D213/26 ,  A61K31/4965 ,  A61K31/4453 ,  C07D241/16 ,  C07D213/04 ,  C07D213/61 ,  C07D413/12 ,  C07D211/06 ,  A61K31/497 ,  C07D213/22 ,  A61K31/445 ,  A61K31/444 ,  A61K31/443 ,  A61K31/454 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/4418 ,  A61K31/4545 ,  A61K31/4412 ,  A61K31/5377 ,  A61K45/06 ,  C07D213/81 ,  C07D241/28 ,  C07D241/26 ,  C07D213/38 ,  C07D401/12 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04

CPC classification number: A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61K45/06 ,  C07D213/38 ,  C07D213/81 ,  C07D241/26 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12

Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

公开(公告)号：US11911371B2

公开(公告)日：2024-02-27

申请号：US17221555

申请日：2021-04-02

Applicant: Novartis AG

Inventor： Urs Baettig ,  Kamlesh Jagdis Bala ,  Emma Budd ,  Lee Edwards ,  Catherine Howsham ,  Glyn Alan Hughes ,  Darren Mark Le Grand ,  Katrin Spiegel

IPC: A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/44 ,  A61K31/4418 ,  C07D241/28 ,  C07D213/81 ,  C07D401/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/497 ,  C07D213/38 ,  C07D401/12 ,  C07D403/12 ,  A61K31/4412 ,  C07D405/04 ,  C07D241/26

CPC classification number: A61K31/44 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/4965 ,  A61K31/5377 ,  A61K45/06 ,  C07D213/38 ,  C07D213/81 ,  C07D241/26 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12

Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

公开(公告)号：US20190262324A1

公开(公告)日：2019-08-29

申请号：US16143202

申请日：2018-09-26

Applicant: NOVARTIS AG

Inventor： Urs BAETTIG ,  Kamlesh Jagdis Bala ,  Emma Budd ,  Lee Edwards ,  Catherine Howsham ,  Glyn Alan Hughes ,  Darren Mark LE GRAND ,  Katrin Spiegel

IPC: A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  C07D401/12 ,  C07D213/38 ,  C07D403/12 ,  C07D241/26 ,  C07D405/04 ,  C07D413/12 ,  C07D413/04 ,  C07D405/12 ,  C07D401/04 ,  C07D241/28 ,  C07D213/81 ,  A61K45/06

Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

公开(公告)号：US10117858B2

公开(公告)日：2018-11-06

申请号：US15156528

申请日：2016-05-17

Applicant: Novartis AG

Inventor： Urs Baettig ,  Kamlesh Bala ,  Emma Budd ,  Lee Edwards ,  Catherine Howsham ,  Glyn Alan Hughes ,  Darren Mark LeGrand ,  Katrin Spiegel

IPC: A61K31/44 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4412 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/4418 ,  C07D213/81 ,  C07D241/28 ,  C07D401/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D213/38 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D241/26

Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

公开(公告)号：US09365552B2

公开(公告)日：2016-06-14

申请号：US14521843

申请日：2014-10-23

Applicant: Novartis AG

Inventor： Urs Baettig ,  Kamlesh Bala ,  Emma Budd ,  Lee Edwards ,  Catherine Howsham ,  Glyn Alan Hughes ,  Darren Mark Legrand ,  Katrin Spiegel

IPC: A61K31/44 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/4418 ,  A61K45/06 ,  C07D405/04 ,  C07D213/81 ,  C07D241/28 ,  C07D401/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D213/38 ,  C07D401/12 ,  C07D403/12 ,  A61K31/4412

CPC classification number: A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61K45/06 ,  C07D213/38 ,  C07D213/81 ,  C07D241/26 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12

Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.

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。