公开(公告)号：US10688108B2

公开(公告)日：2020-06-23

申请号：US16554539

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: 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：US10660908B2

公开(公告)日：2020-05-26

申请号：US16135366

申请日：2018-09-19

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: 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：US20190015430A1

公开(公告)日：2019-01-17

申请号：US16135366

申请日：2018-09-19

Applicant: LEO Pharma A/S

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

IPC: A61K31/593 ,  A61K47/08 ,  A61K9/12 ,  A61M35/00 ,  A61M11/00 ,  A61K47/22 ,  A61K47/14 ,  A61K9/00 ,  A61K47/06 ,  A61K31/59 ,  A61K31/58 ,  A61K31/573 ,  B65D83/20 ,  B65D83/14

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：US10130640B2

公开(公告)日：2018-11-20

申请号：US14707733

申请日：2015-05-08

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: The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative or analog and a corticosteroid, and its use in the treatment of dermal diseases and conditions.

公开(公告)号：US20160324875A1

公开(公告)日：2016-11-10

申请号：US15214216

申请日：2016-07-19

Applicant: LEO PHARMA A/S

Inventor： Karsten PETERSSON

IPC: A61K31/592 ,  A61K47/18 ,  A61K47/06 ,  A61K9/00 ,  A61K47/44 ,  A61K47/14

CPC classification number: A61K31/592 ,  A61K9/0014 ,  A61K9/1075 ,  A61K31/593 ,  A61K47/06 ,  A61K47/14 ,  A61K47/18 ,  A61K47/44

Abstract: A pharmaceutical composition comprising a vitamin D derivative or analogue as the active ingredient dissolved in a three-component surfactant-solvent mixture is useful in the treatment of dermal disorders or conditions.

Abstract translation: 包含溶解在三组分表面活性剂 - 溶剂混合物中的作为活性成分的维生素D衍生物或类似物的药物组合物可用于治疗真皮病症或病症。

公开(公告)号：US20160206629A1

公开(公告)日：2016-07-21

申请号：US15084210

申请日：2016-03-29

Applicant: LEO Pharma A/S

Inventor： Karsten PETERSSON ,  Kit FREDERIKSEN ,  Diana OMKVIST ,  Jörgen JANSSON

IPC: A61K31/573 ,  A61K47/14 ,  A61K9/70 ,  A61K47/26 ,  A61K9/00 ,  A61K47/32 ,  A61K47/10

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.

公开(公告)号：US09345774B2

公开(公告)日：2016-05-24

申请号：US14412978

申请日：2013-07-05

Applicant: LEO PHARMA A/S

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

IPC: A61K9/00 ,  A61K47/32 ,  A61K9/70 ,  A61K9/12 ,  A61K31/573 ,  A61K47/06 ,  A61K47/08 ,  A61K47/10 ,  A61K47/14 ,  A61K47/38 ,  A61K47/44 ,  B65D83/14 ,  A61K47/22

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 sprayable film-forming pharmaceutical composition for dermal application comprises at least one therapeutically active ingredient dissolved in a pharmaceutically acceptable propellant selected from the group consisting of dimethyl ether, diethyl ether and methylethylether, and a mixture of dimethyl ether, diethylether and methylethyl ether, and a second propellant selected from C3-5 alkanes, hydrofluoroalkanes, hydrochloroalkanes, fluoroalkanes and chlorofluoroalkanes, the propellant being present in an amount of 50-99.5% w/w of the composition, the composition further comprising a film-forming polymer, a plasticizer and an oily release-enhancing agent.

Abstract translation: 用于真皮施用的可喷雾成膜药物组合物包含溶解在选自二甲醚，二乙醚和甲基乙醚的药学上可接受的推进剂中的至少一种治疗活性成分，以及二甲醚，二乙醚和甲基乙基醚的混合物，以及 选自C3-5烷烃，氢氟烷烃，氢氯烃，氟代烷烃和氯氟烷烃的第二推进剂，推进剂的含量为组合物的50-99.5％w / w，组合物还包含成膜聚合物，增塑剂和 油性释放增强剂。

公开(公告)号：US09273064B2

公开(公告)日：2016-03-01

申请号：US14586681

申请日：2014-12-30

Applicant: LEO PHARMA A/S

Inventor： Simon Feldbaek Nielsen

IPC: C07D495/10 ,  C07D493/10 ,  A61K31/4427 ,  A61K31/4433

CPC classification number: C07D495/10 ,  A61K9/0053 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  C07D493/10

Abstract: Compounds of the general formula I wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.

Abstract translation: 通式I的化合物，其中m和n各自独立地为0或1; R1和R2与它们连接的碳原子一起形成包含一个或两个选自氧，硫，-S（O） - 和-S（O）2 - 的杂原子的杂环; R3是-CHF2，-CF3，-OCHF2，-OCF3，-SCHF2或-SCF3; X是键，-CH 2 - 或-NH-; A是任选被一个或多个相同或不同的选自R4的取代基取代的芳基，环烷基，环烯基，芳基烷基，杂芳基，杂芳基烷基，杂环烷基或杂环烯基。 R 4是氢，氨基，硫代，烷基，卤代烷基，羟基烷基，烷氧基，卤代烷氧基，卤素，氧代，硫杂或羟基; 已发现其药学上可接受的盐，水合物或溶剂化物表现出PDE4抑制活性，因此可用于治疗炎性疾病和病症。

公开(公告)号：US09238056B2

公开(公告)日：2016-01-19

申请号：US14000811

申请日：2012-02-21

Applicant: Nina Østergaard Knudsen ,  Thorsten Thormann

Inventor： Nina Østergaard Knudsen ,  Thorsten Thormann

IPC: A61K38/04 ,  A61K31/593 ,  A61K8/64 ,  A61K38/12 ,  A61K47/48 ,  C07K7/06 ,  C07K7/64 ,  A61K9/127 ,  A61K31/047 ,  A61K38/00

CPC classification number: A61K38/12 ,  A61K8/64 ,  A61K9/1271 ,  A61K31/047 ,  A61K38/00 ,  A61K47/48246 ,  A61K47/48815 ,  A61K47/64 ,  A61K47/6911 ,  A61Q19/008 ,  C07K7/06 ,  C07K7/64

Abstract: A cyclic peptide capable of binding specifically to the α2 I domain of a collagen binding integrin receptor may be conjugated to a drug containing particle via a linker moiety. The conjugate may be used to target a therapeutic drug to a cell expressing a collagen binding integrin receptor on its surface.

Abstract translation: 能够特异性结合胶原结合整联蛋白受体的α2I结构域的环肽可通过接头部分与含药物的颗粒结合。 缀合物可用于将治疗药物靶向表面上表达胶原结合整联蛋白受体的细胞。

公开(公告)号：US09181248B2

公开(公告)日：2015-11-10

申请号：US14572218

申请日：2014-12-16

Applicant: LEO Pharma A/S

Inventor： Simon Feldbaek Nielsen ,  Jens Christian Hojland Larsen

IPC: A61K31/437 ,  C07D471/04

CPC classification number: C07D471/04 ,  A61K31/437

Abstract: The present invention relates to novel [1,2,4]triazolopyridine compounds with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

Abstract translation: 本发明涉及具有磷酸二酯酶抑制活性的新型[1,2,4]三唑并吡啶化合物，以及它们在治疗炎性疾病和病症中作为治疗剂的用途。