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：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.

公开(公告)号：US20170065618A1

公开(公告)日：2017-03-09

申请号：US15297984

申请日：2016-10-19

Applicant: LEO PHARMA A/S

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

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

CPC classification number: A61K31/593 ,  A61K9/0014 ,  A61K9/122 ,  A61K9/124 ,  A61K31/573 ,  A61K31/58 ,  A61K31/59 ,  A61K47/06 ,  A61K47/08 ,  A61K47/14 ,  A61K47/22 ,  A61M11/00 ,  A61M35/003 ,  A61M2210/04 ,  B65D83/207 ,  B65D83/752 ,  A61K2300/00

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.

Abstract translation: 本发明涉及包含生物活性维生素D衍生物或类似物和皮质类固醇的局部喷雾组合物，及其用于治疗真皮疾病和病症。

公开(公告)号：US09586961B2

公开(公告)日：2017-03-07

申请号：US13809059

申请日：2011-07-08

Applicant: Simon Felbdæk Nielsen ,  Daniel R. Greve ,  Gunnar Grue-Sørensen ,  Carsten Ryttersgaard ,  Søren Christian Schou ,  Anette Graven Sams

Inventor： Simon Felbdæk Nielsen ,  Daniel R. Greve ,  Gunnar Grue-Sørensen ,  Carsten Ryttersgaard ,  Søren Christian Schou ,  Anette Graven Sams

IPC: A01N43/62 ,  A61K31/55 ,  C07D223/14 ,  C07D487/00 ,  C07D491/00 ,  C07D513/00 ,  C07D487/04 ,  A61K31/5513 ,  A61K45/00

CPC classification number: C07D487/04 ,  A61K31/5513 ,  A61K45/00

Abstract: The invention relates to compounds of general formula (I) wherein R1, R2, R3, R4, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immuno-suppression would be desirable for example in organ transplantation.

Abstract translation: 本发明涉及通式（I）的化合物，其中R 1，R 2，R 3，R 4，m和n如本文所定义，及其药学上可接受的盐，水合物或溶剂合物，其单独使用或与 更多其他药物活性化合物 - 在治疗中，作为用于预防，治疗或改善疾病及其并发症的JAK激酶和蛋白酪氨酸激酶抑制剂，包括例如牛皮癣，特应性皮炎，酒渣鼻，狼疮，多发性硬化，类风湿性关节炎，I型 糖尿病，哮喘，癌症，自身免疫性甲状腺疾病，溃疡性结肠炎，克罗恩病，阿尔茨海默氏病，白血病，眼睛疾病如糖尿病性视网膜病变和黄斑变性以及其他自身免疫性疾病以及免疫抑制在器官移植中是理想的适应症 。