公开(公告)号：US20220088020A1

公开(公告)日：2022-03-24

申请号：US17228831

申请日：2021-04-13

Applicant: LEO PHARMA A/S ,  Japan Tobacco Inc.

Inventor： Michael SIERRA ,  Tord LABUDA ,  Atsuo TANIMOTO ,  Yuichi SHINOZAKI

IPC: A61K31/519 ,  A61K9/00 ,  A61K47/06 ,  A61K9/06 ,  A61P17/14

Abstract: The present invention provides a novel treatment of alopecia areate. The problem to be solved by the invention is to provide a new pharmaceutical use of 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile. A therapeutic or preventive agent for alopecia areata, containing 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile as an active ingredient.

公开(公告)号：US11065257B2

公开(公告)日：2021-07-20

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: C07D491/20 ,  A61K31/55

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：US20210128588A1

公开(公告)日：2021-05-06

申请号：US16903730

申请日：2020-06-17

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: The 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：US20210079012A1

公开(公告)日：2021-03-18

申请号：US16772615

申请日：2018-12-14

Applicant: LEO Pharma A/S

Inventor： Mark ANDREWS ,  Daniel Rodriguez GREVE ,  Bjarne NØRREMARK

IPC: C07D495/04

Abstract: The present invention relates to novel substituted azetidine dihydrothienopyridines 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：US10906915B2

公开(公告)日：2021-02-02

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：US10799507B2

公开(公告)日：2020-10-13

申请号：US16483079

申请日：2018-02-01

Applicant: LEO Pharma A/S

Inventor： Mogens Larsen ,  Andreas Ritzen ,  Bjarne Nørremark ,  Daniel Rodriguez Greve

IPC: C07D487/04 ,  A61K31/519

Abstract: The present invention relates to a compound according to formula (I) wherein X represents NH or O; n is an integer selected from 1-3; Y represents a bond, —C(O)O—*, —C(O)OR3—* or —C(O)NHR3—*; W is selected from the group consisting of phenyl, pyridyl, (C3-C7)cycloalkyl and 4-6 membered heterocycloalkyl; or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further 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：US10682364B2

公开(公告)日：2020-06-16

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 ,  B65D83/20 ,  B65D83/14

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：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.

公开(公告)号：US09855285B2

公开(公告)日：2018-01-02

申请号：US14648480

申请日：2013-11-28

Applicant: LEO PHARMA A/S

Inventor： Paola Lovato

IPC: A61K31/59 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/593 ,  A61K45/06

CPC classification number: A61K31/59 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/593 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to a method of inhibiting the upregulation of the expression of the proinflammatory cytokine interleukin-22 (IL-22) in activated and differentiated human T-cells, said upregulation being induced by administration of a therapeutically effective amount of a phosphodiesterase 4 (PDE4) inhibitor. The method comprises administering, either sequentially to or simultaneously with the administration of the PDE4 inhibitor, a vitamin D receptor agonist in an amount sufficient to inhibit the upregulation of IL-22 expression.