公开(公告)号：US20200323869A1

公开(公告)日：2020-10-15

申请号：US16468444

申请日：2017-12-12

Applicant: LEO PHARMA A/S

Inventor： Xifu LIANG ,  Jens LARSEN ,  Simon Feldbaek NIELSEN ,  Peter ANDERSEN

IPC: A61K31/55 ,  C07D491/20

Abstract: The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

公开(公告)号：US20210070769A1

公开(公告)日：2021-03-11

申请号：US16772428

申请日：2018-12-14

Applicant: LEO Pharma A/S

Inventor： Mark ANDREWS ,  Daniel Rodriguez GREVE ,  Jens LARSEN

IPC: C07D495/04

Abstract: The present invention relates to novel substituted azetidine dihydrothienopyrimidines with phosphodiesterase inhibitory activity, and to their use in therapy, and to pharmaceutical compositions comprising the compounds and to methods of treating diseases with the compounds (I).

公开(公告)号：US20200239493A1

公开(公告)日：2020-07-30

申请号：US16648263

申请日：2018-09-20

Applicant: LEO Pharma A/S

Inventor： Jens LARSEN

IPC: C07D495/04

Abstract: The present invention relates to novel substituted dihydrothienopyrimidines with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

公开(公告)号：US20220362259A1

公开(公告)日：2022-11-17

申请号：US17303955

申请日：2021-06-10

Applicant: LEO Pharma A/S

Inventor： Xifu LIANG ,  Jens LARSEN ,  Simon Feldbaek NIELSEN ,  Peter ANDERSEN

IPC: A61K31/55 ,  C07D491/20

Abstract: The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

公开(公告)号：US20190367512A1

公开(公告)日：2019-12-05

申请号：US16477249

申请日：2018-01-10

Applicant: LEO Pharma A/S

Inventor： Jens LARSEN ,  Mogens LARSEN ,  Lars Kyhn RASMUSSEN ,  Andreas RITZEN ,  Tine Marianne DUUS

IPC: C07D471/04

Abstract: The present invention relates to a compound according to formula (I) or pharmaceutically acceptable salts, hydrates, or solvates thereof; wherein R1 is C1-alkyl, R2 is C1-alkyl, R3 is C2-alkyl, R4 is hydrogen, R5 is hydrogen. The invention relates further to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to said compounds for use in the treatment autoimmune diseases and to intermediates for the preparation of said compounds.

公开(公告)号：US20200010477A1

公开(公告)日：2020-01-09

申请号：US16468420

申请日：2016-12-12

Applicant: LEO Pharma A/S

Inventor： Xifu LIANG ,  Jens LARSEN ,  Simon Feldbaek NIELSEN ,  Peter ANDERSEN

IPC: C07D491/20

Abstract: The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

公开(公告)号：US20190330223A1

公开(公告)日：2019-10-31

申请号：US16468429

申请日：2016-12-12

Applicant: LEO Pharma A/S

Inventor： Xifu LIANG ,  Jens LARSEN

IPC: C07D491/20

Abstract: The present invention relates to novel pyrazoloazepin-8-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.