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：US20180021345A1

公开(公告)日：2018-01-25

申请号：US15673155

申请日：2017-08-09

Applicant: Novartis AG

Inventor： David BEATTIE ,  Urs BAETTIG ,  Darren Mark LE GRAND ,  Andrew Stuart LISTER ,  Jeffrey MCKENNA ,  David William PEARCE ,  David Andrew SANDHAM ,  Oliver Ross STEWARD ,  Christopher THOMSON

IPC: A61K31/551 ,  C07D401/12 ,  A61K31/445 ,  C07D413/12 ,  A61K31/5513 ,  A61K45/06 ,  A61K31/504 ,  C07D401/10 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/439 ,  C07D405/12 ,  C07D417/10 ,  C07D417/14 ,  A61K31/4545 ,  C07D403/10 ,  C07D413/14 ,  A61K31/4245 ,  C07D471/08 ,  C07D403/12 ,  A61K31/427 ,  C07D413/10 ,  C07D401/14 ,  A61K31/506 ,  C07D407/12 ,  C07D257/04 ,  C07D403/14 ,  A61K31/45 ,  A61K31/496 ,  A61K31/41

CPC classification number: A61K31/551 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/439 ,  A61K31/445 ,  A61K31/45 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/504 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5513 ,  A61K45/06 ,  C07D257/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D407/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/08 ,  A61K2300/00

Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.

公开(公告)号：US20210228554A1

公开(公告)日：2021-07-29

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: A61K31/44 ,  A61K31/4418 ,  C07D213/81 ,  C07D401/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  C07D213/38 ,  C07D401/12 ,  C07D403/12 ,  A61K31/4412 ,  A61K45/06 ,  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：US20130172349A1

公开(公告)日：2013-07-04

申请号：US13774305

申请日：2013-02-22

Applicant: Novartis AG

Inventor： Ian BRUCE ,  Bernard CUENOUD ,  Thomas Hugo KELLER ,  Gaynor Elizabeth WOODWARD ,  Nicola PRESS ,  Darren Mark LE GRAND ,  Cathy RITCHIE ,  Barbara VALADE ,  Judy Fox HAYLER ,  Emma BUDD

IPC: A61K31/5377 ,  A61K31/497 ,  A61K45/06 ,  C07D417/14

CPC classification number: A61K31/5377 ,  A61K31/497 ,  A61K45/06 ,  C07D417/04 ,  C07D417/14

Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase.Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract translation: 游离或盐形式的式I化合物，其中R 1，R 2，R 3和R 4具有说明书中所示的含义，可用于治疗由磷脂酰肌醇3-激酶介导的病症。 还描述了含有化合物的药物组合物和制备该化合物的方法。