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    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
    31.
    发明申请
    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS 审中-公开
    作为磷酸二酯酶抑制剂的苯二酚或苯并二氧杂环己烷化合物

    公开(公告)号：US20150111915A1

    公开(公告)日：2015-04-23

    申请号：US14586681

    申请日：2014-12-30

    Applicant: LEO PHARMA A/S

    Inventor： Simon Feldbaek NIELSEN

    IPC: C07D495/10 ,  C07D493/10

    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。

    DISPENSING SYSTEMS
    32.
    发明申请
    DISPENSING SYSTEMS 审中-公开
    分配系统

    公开(公告)号：US20140371690A1

    公开(公告)日：2014-12-18

    申请号：US14352471

    申请日：2012-10-18

    Applicant: Leo Pharma A/S

    Inventor： Peter Sprada ,  Graeme Howard Davies ,  Nicholas Henry Reddall ,  Graham Keith Lacy ,  Steven William McLellan ,  Georgina Rogers ,  Alun Wilcox

    IPC: A61M35/00

    CPC classification number: A61M35/003 ,  B05B1/14 ,  B05B11/00416 ,  B05B11/0054 ,  B05B11/3011 ,  B05B11/303 ,  B05B11/3033 ,  B05B11/3035 ,  B05B11/3043 ,  B05B11/3059 ,  B05B11/3061 ,  B05B11/3069 ,  B05B11/3084

    Abstract: A hand-held applicator (10) for self-administration of a semi-solid medicament comprises an applicator head (14) with one or more elongate dispensing nozzles (40) and an applicator body (12) for housing a medicament reservoir, such as a cartridge (20). The applicator has a pump assembly and an actuator (30) for pumping the medicament from the one or more of the dispensing nozzles. The applicator head and applicator body are fixed relative to each other in use such that movement of the nozzle or nozzles away from the scalp or other body area during actuation may be avoided. The applicator may further include an application face for spreading medicament over a body area thereby enabling dual functionality as a scalp and body applicator. A dispensing system in the form of a dispensing head and cartridge therefor is also described and characterised by venting features for improving priming of the dispenser. Such priming means are suitable for use in the applicators of the application.

    Abstract translation: 用于自行管理半固体药物的手持式施用器（10）包括具有一个或多个细长分配喷嘴（40）的施用器头（14）和用于容纳药物储存器的施用器主体（12），例如 盒（20）。 施用器具有泵组件和用于从一个或多个分配喷嘴泵送药物的致动器（30）。 施用器头和施用器主体在使用中相对于彼此固定，使得可以避免在致动期间喷嘴或喷嘴远离头皮或其他身体区域的运动。 施用器还可以包括用于将药物铺展在身体区域上的使用面，从而实现作为头皮和身体涂抹器的双重功能。 还描述了其分配头和盒的形式的分配系统，其特征在于排气特征以改善分配器的启动。 这种起动装置适用于本申请的施加器。

    SMALL MOLECULE MODULATORS OF IL-17
    34.
    发明公开
    SMALL MOLECULE MODULATORS OF IL-17 审中-公开

    公开(公告)号：US20240208938A1

    公开(公告)日：2024-06-27

    申请号：US18526149

    申请日：2023-12-01

    Applicant: LEO Pharma A/S

    Inventor： Mark ANDREWS ,  Mogens LARSEN ,  Alan JESSIMAN ,  Patrick JOHNSON ,  Kevin Neil DACK

    IPC: C07D401/14

    CPC classification number: C07D401/14

    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.

    TREATMENT OF HAND ECZEMA
    36.
    发明申请
    TREATMENT OF HAND ECZEMA 有权

    公开(公告)号：US20230138114A1

    公开(公告)日：2023-05-04

    申请号：US17811347

    申请日：2022-07-08

    Applicant: LEO Pharma A/S

    Inventor： Tero WENNBERG ,  Anders Per SØRENSEN

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

    Abstract: The present disclosure relates to the treatment of hand eczema. The problem to be solved by the disclosure 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 hand eczema, 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.

    Bicyclic amines as novel JAK kinase inhibitors
    40.
    发明授权
    Bicyclic amines as novel JAK kinase inhibitors 有权

    公开(公告)号：US10851116B2

    公开(公告)日：2020-12-01

    申请号：US16479375

    申请日：2018-01-19

    Applicant: LEO Pharma A/S

    Inventor： Daniel Rodriguez Greve ,  Tue Heesgaard Jepsen ,  Mogens Larsen ,  Andreas Ritzen

    IPC: C07D519/00 ,  A61K31/519

    Abstract: The present invention relates to a compound according to formula I wherein R1 is alkyl; n is 1 or 2; R2 is selected from the group consisting of hydrogen, cyano, —SO2Ra, —SO2NRbRc, —C(O)Rb, phenyl and 5- and 6-membered heteroaryl or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to pharmaceutical compositions comprising said compounds, and to methods of treating proliferative or inflammatory skin disorders with said compounds.

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