公开(公告)号：US10662181B2

公开(公告)日：2020-05-26

申请号：US16317655

申请日：2017-07-11

Applicant: LEO PHARMA A/S

Inventor： Alan Stuart Jessiman ,  Patrick Stephen Johnson ,  Kristoffer Maansson ,  Morten Dahl Sørensen

IPC: C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D241/04

Abstract: The present invention relates to a compound according to general formula (I) wherein X represents N or CH; R1 is —CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C3-C7)cycloalkyl(C1-C4)alkyl, (3-7 membered)heterocycloalkyl-(C1-C4)alkyl or (5-6 membered)heteroaryl-(C1-C4)alkyl; R2 is halogen, cyano, (C1-C4)alkyl or (C3-C7)cycloalkyl; R3 is halogen, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl or (C3-C7)cycloalkyl; R4 is (C1-C4)alkyl or (C1-C4)haloalkyl; R5 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or —ORa. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds.

公开(公告)号：US11377425B1

公开(公告)日：2022-07-05

申请号：US16765143

申请日：2019-12-19

Applicant: LEO Pharma A/S

Inventor： Kevin Neil Dack ,  Xifu Liang ,  Mogens Larsen ,  Mark Andrews ,  Alan Stuart Jessiman ,  Mia Nørreskov Burhardt ,  Patrick Stephen Johnson ,  Peter Andersen ,  Lars Jørgensen

IPC: C07D231/12 ,  C07D403/12 ,  C07D249/06 ,  C07D271/10 ,  C07D263/32 ,  C07D413/12 ,  C07D233/64 ,  C07D231/14 ,  C07D233/68 ,  C07D233/70 ,  C07D261/08

Abstract: The present invention relates to a compound according to formula I and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.

公开(公告)号：US10934282B2

公开(公告)日：2021-03-02

申请号：US16874961

申请日：2020-05-15

Applicant: LEO PHARMA A/S

Inventor： Alan Stuart Jessiman ,  Patrick Stephen Johnson ,  Kristoffer Maansson ,  Morten Dahl Sørensen

IPC: C07D413/14 ,  C07D413/12 ,  C07D417/14 ,  C07D241/04

Abstract: The present invention relates to a compound according to general formula (I) wherein X represents N or CH; R1 is —CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C3-C7)cycloalkyl(C1-C4)alkyl, (3-7 membered)heterocycloalkyl-(C1-C4)alkyl or (5-6 membered)heteroaryl-(C1-C4)alkyl; R2 is halogen, cyano, (C1-C4)alkyl or (C3-C7)cycloalkyl; R3 is halogen, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl or (C3-C7)cycloalkyl; R4 is (C1-C4)alkyl or (C1-C4)haloalkyl; R5 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or —ORa. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds.