公开(公告)号：US20170137438A1

公开(公告)日：2017-05-18

申请号：US15320227

申请日：2015-06-22

Applicant: Leo Pharma A/S

Inventor： Bjorn Metzler ,  Andre Faldt

IPC: C07D495/10

CPC classification number: C07D495/10

Abstract: The present invention relates to novel methods for the preparation of 1,3-benzodioxole heterocyclic compounds and intermediates for the same. The compounds are useful as PDE4 inhibitors.

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：US20160207930A1

公开(公告)日：2016-07-21

申请号：US14913647

申请日：2014-08-15

Applicant: LEO PHARMA A/S

Inventor： Haakan BLADH ,  Jakob FELDING ,  Ding ZHOU ,  Zhen-wei CAI ,  Morten Dahl SØRENSEN

IPC: C07D487/04 ,  A61K9/00 ,  A61K31/4985

CPC classification number: C07D487/04 ,  A61K9/0014 ,  A61K31/4985

Abstract: The invention relates novel NK1 receptor antagonists represented in formula A, wherein R1 and R2 independently are selected from the group consisting of (C1-4)alkyl, (C1-4)haloalkyl, (C1-4)alkoxy, CD3 or halogen; R3 is selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4)haloalkyl and (C1-4)hydroxyalkyl; R4 is selected from the group consisting of phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R5 and R6 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, (C1-4) hydroxyalkyl and (C1-4)haloalkyl and X and Y are independently selected from the group consisting of CH and N. The invention furthermore relates to intermediates for the preparation of said compounds, to their use in therapy, and to pharmaceutical compositions comprising said compounds.

Abstract translation: 本发明涉及式A中所示的新型NK1受体拮抗剂，其中R1和R2独立地选自（C1-4）烷基，（C1-4）卤代烷基，（C1-4）烷氧基，CD3或卤素; R3选自氢，（C1-4）烷基，（C1-4）卤代烷基和（C1-4）羟基烷基; R4选自苯基，5元杂芳基和6元杂芳基; R 5和R 6独立地选自氢，（C 1-4）烷基，（C 1-4）羟基烷基和（C 1-4）卤代烷基，X和Y独立地选自CH和N。 本发明还涉及制备所述化合物的中间体，其在治疗中的用途以及包含所述化合物的药物组合物。

公开(公告)号：US20160009751A1

公开(公告)日：2016-01-14

申请号：US14330808

申请日：2014-07-14

Applicant: LEO Pharma A/S

Inventor： Michael L. SIERRA ,  Jakob FELDING ,  Qianghui ZHOU ,  Hans RENATA ,  Philippe S. BARAN

IPC: C07J7/00 ,  C07J21/00 ,  A61K31/573

CPC classification number: C07J7/0085 ,  A61K31/573 ,  A61K45/06 ,  C07J21/006

Abstract: The present invention relates to a compound according to formula I wherein R1 is selected from the group consisting of hydrogen and fluoro and R2 is selected from C1-C4 alkyl and hydrates or solvates thereof. The invention further relates 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.

Abstract translation: 本发明涉及式Ⅰ化合物，其中R 1选自氢和氟，R 2选自C 1 -C 4烷基及其水合物或溶剂合物。 本发明还涉及用于制备所述化合物的中间体，用于治疗的所述化合物，包含所述化合物的药物组合物，用所述化合物治疗疾病的方法，以及所述化合物在制备药物中的用途。

公开(公告)号：US20150196646A1

公开(公告)日：2015-07-16

申请号：US14410489

申请日：2013-07-05

Applicant: LEO PHARMA A/S

Inventor： Karsten Petersson ,  Kit Frederiksen ,  Diana Omkvist ,  Jörgen Jansson

IPC: A61K47/32 ,  A61K47/22 ,  A61K47/10 ,  A61K31/573 ,  A61K47/14

CPC classification number: A61K31/573 ,  A61K9/0014 ,  A61K9/124 ,  A61K9/7015 ,  A61K47/06 ,  A61K47/08 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38 ,  A61K47/44 ,  B65D83/752

Abstract: A film-forming pharmaceutical composition for dermal application comprises at least one therapeutically active ingredient dissolved in a volatile solvent, the composition further comprising a film-forming polymer, a plasticizer and an oily release-enhancing agent. The composition is capable of forming, after application on skin and evaporation of the solvent, a continuous phase comprising the film-forming polymer and the plasticizer and a dispersed phase comprising droplets of the oily release-enhancing agent.

Abstract translation: 用于真皮施用的成膜药物组合物包含溶解在挥发性溶剂中的至少一种治疗活性成分，所述组合物还包含成膜聚合物，增塑剂和油性释放增强剂。 组合物能够在皮肤上施用和蒸发溶剂后形成包含成膜聚合物和增塑剂的连续相和包含油性释放增强剂的液滴的分散相。

公开(公告)号：USD725470S1

公开(公告)日：2015-03-31

申请号：US29434939

申请日：2012-10-18

Applicant: LEO Pharma A/S

Designer： Alun Wilcox ,  Peter Sprada ,  Graeme Howard Davies ,  Nicholas Henry Reddall ,  Joshua Thomas Richards

公开(公告)号：US20140322331A1

公开(公告)日：2014-10-30

申请号：US14220843

申请日：2014-03-20

Applicant: LEO PHARMA A/S

Inventor： Karsten PETERSSON

IPC: A61K31/592 ,  A61K45/06 ,  A61K9/06 ,  C07C35/21

CPC classification number: A61K31/592 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/146 ,  A61K31/593 ,  A61K45/06 ,  C07C35/21 ,  Y10T428/2982

Abstract: Calcipotriol monohydrate nanocrystals prepared by the process disclosed herein may be incorporated in a pharmaceutical composition for use in the prevention or treatment of dermal diseases and conditions.

Abstract translation: 通过本文公开的方法制备的卡泊三醇一水合物纳米晶体可以掺入用于预防或治疗皮肤疾病和病症的药物组合物中。

公开(公告)号：USD709374S1

公开(公告)日：2014-07-22

申请号：US29434963

申请日：2012-10-18

Applicant: LEO Pharma A/S

Designer： Alun Wilcox ,  Peter Sprada ,  Graeme Howard Davies ,  Nicholas Henry Reddall ,  Joshua Thomas Richards