公开(公告)号：US20230404909A1

公开(公告)日：2023-12-21

申请号：US18154566

申请日：2023-01-13

Applicant: LEO Pharma A/S

Inventor： Karsten PETERSSON ,  Karen Margrethe ENGELL ,  Jorgen JANSSON ,  Kim Troensegaard NIELSEN ,  Andre Huss ERIKSSON ,  Anne MOORE ,  Sonja VUCEN ,  Caroline O'SULLIVAN ,  Abina CREAN

IPC: A61K9/00 ,  A61K31/573 ,  A61K31/593 ,  A61K31/59 ,  A61K47/32 ,  A61K47/34 ,  A61M37/00

CPC classification number: A61K9/0021 ,  A61K31/573 ,  A61K31/593 ,  A61K31/59 ,  A61K47/32 ,  A61K47/34 ,  A61M37/0015 ,  A61M2037/0053 ,  A61M2037/0046 ,  A61M2037/0023 ,  A61M2037/0061

Abstract: The present invention relates to a microneedle patch composition comprising one or more microneedles each comprising: (a) a tapered tip portion containing a therapeutically active ingredient dispersed in a matrix of a biodegradable polymer capable of providing sustained release of the therapeutically active ingredient over a period of at least two days after insertion of the microneedle or microneedles into the skin, and (b) a fast dissolving microneedle backing layer portion containing a water-soluble polymer overlayering the tip portion, said microneedle or microneedles being attached to and extending from an adhesive surface of a removable substrate.

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：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：US20210269447A1

公开(公告)日：2021-09-02

申请号：US17257905

申请日：2019-06-27

Applicant: LEO Pharma A/S

Inventor： Jens C. Højland LARSEN ,  Mogens LARSEN ,  Andreas RITZEN

IPC: C07D487/04 ,  A61K31/52

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：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.

公开(公告)号：US20200291010A1

公开(公告)日：2020-09-17

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: C07D413/12 ,  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：US20200009160A1

公开(公告)日：2020-01-09

申请号：US16554603

申请日：2019-08-28

Applicant: LEO Pharma A/S

Inventor： Marianne LIND ,  Gritt RASMUSSEN ,  Mette Rydahl SONNE ,  Jens HANSEN ,  Karsten PETERSSON

IPC: A61K31/593 ,  A61K31/59 ,  A61K47/06 ,  A61K47/08 ,  A61M11/00 ,  A61K9/00 ,  A61K9/12 ,  A61K31/573 ,  A61K31/58 ,  A61M35/00 ,  A61K47/14 ,  A61K47/22

Abstract: A Pharmaceutical Spray Composition Comprising a Vitamin D Analogue and a CorticosteroidThe present invention relates to a topical spray composition comprising a biologically active vitamin D derivative or analogue and a corticosteroid, and its use in the treatment of dermal 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：US20180258080A1

公开(公告)日：2018-09-13

申请号：US15759622

申请日：2016-09-13

Applicant: LEO Pharma A/S

Inventor： Patrick Stephen JOHNSON ,  Kevin Neil DACK ,  Krister HENRIKSSON

IPC: C07D405/06 ,  C07D405/14 ,  A61K31/4545 ,  C07D417/14 ,  C07D413/14 ,  A61K31/4525 ,  A61K31/454

CPC classification number: C07D405/06 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to a compound according to formula (I) wherein R1 is selected from the group consisting of 5- and 6-membered heteroaryl, (C1-C6)alkyl, (C3-C6)cycloalkyl, (4-6)-membered heterocycloalkyl and phenyl; R2 is selected from (C1-C3)alkyl and halo(C1-C3)alkyl; R3 is selected from phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R4 is selected from hydrogen, halogen, (C1-C4)alkyl and halo(C1-C4)alkyl; X1 is selected from CH, C(Rb) and N, X2 is selected from CH and N; Y is selected from —NH— and —O—; m is 0 or 1; n is 0 or 1; L represents a bond, —O—, —NH— or —N(Rc)—; or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

公开(公告)号：US20180078498A1

公开(公告)日：2018-03-22

申请号：US15562278

申请日：2016-03-16

Applicant: LEO Pharma A/S

Inventor： Karsten Petersson ,  Karen Margrethe Engell ,  Jorgen Jansson ,  Kim Troensegaard Nielsen ,  Andre Huss Eriksson ,  Anne Moore ,  Sonja Vucen ,  Caroline O'Sullivan ,  Abina Crean

IPC: A61K9/00 ,  A61K31/573 ,  A61K31/59 ,  A61K47/34 ,  A61K47/32 ,  A61M37/00

CPC classification number: A61K9/0021 ,  A61K31/573 ,  A61K31/59 ,  A61K31/593 ,  A61K47/32 ,  A61K47/34 ,  A61M37/0015 ,  A61M2037/0023 ,  A61M2037/0046 ,  A61M2037/0053 ,  A61M2037/0061 ,  A61K2300/00

Abstract: The present invention relates to a microneedle patch composition comprising one or more microneedles each comprising: (a) a tapered tip portion containing a therapeutically active ingredient dispersed in a matrix of a biodegradable polymer capable of providing sustained release of the therapeutically active ingredient over a period of at least two days after insertion of the microneedle or microneedles into the skin, and (b) a fast dissolving microneedle backing layer portion containing a water-soluble polymer overlayering the tip portion, said microneedle or microneedles being attached to and extending from an adhesive surface of a removable substrate.