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    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
    62.
    发明申请
    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS 审中-公开

    公开(公告)号：US20160022657A1

    公开(公告)日：2016-01-28

    申请号：US14872487

    申请日：2015-10-01

    Applicant: LEO PHARMA A/S

    Inventor： Simon Feldbaek NIELSEN

    IPC: A61K31/4436 ,  A61K31/4433 ,  A61K9/00 ,  A61K31/443

    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.

    A METHOD OF INHIBITING THE EXPRESSION OF IL-22 IN ACTIVATED T-CELLS
    63.
    发明申请
    A METHOD OF INHIBITING THE EXPRESSION OF IL-22 IN ACTIVATED T-CELLS 有权
    抑制活化T细胞中IL-22表达的方法

    公开(公告)号：US20150297616A1

    公开(公告)日：2015-10-22

    申请号：US14648480

    申请日：2013-11-28

    Applicant: LEO PHARMA A/S

    Inventor： Paola LOVATO

    IPC: A61K31/59 ,  A61K31/44 ,  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 3) sufficient to inhibit the upregulation of IL-22 expression.

    Abstract translation: 本发明涉及抑制活化和分化的人T细胞中促炎细胞因子白细胞介素-22（IL-22）表达上调的方法，所述上调是通过施用治疗有效量的磷酸二酯酶4 （PDE4）抑制剂。 该方法包括向PDE4抑制剂的依次施用或同时施用足以抑制IL-22表达上调的量3）的维生素D受体激动剂。

    NOVEL NEUROKININ 1 RECEPTOR ANTAGONIST COMPOUNDS
    67.
    发明申请
    NOVEL NEUROKININ 1 RECEPTOR ANTAGONIST COMPOUNDS 有权
    新型神经营养因子1受体拮抗剂化合物

    公开(公告)号：US20150018345A1

    公开(公告)日：2015-01-15

    申请号：US14380078

    申请日：2013-02-20

    Applicant: LEO PHARMA A/S

    Inventor： Morten Dahl Sørensen ,  Romano Di Fabio ,  Alfonso Pozzan ,  Maria Pia Catalani ,  Haakon Bladh ,  Jakob Felding

    IPC: C07D487/04 ,  C07D491/20 ,  A61K31/5377 ,  C07D471/20 ,  A61K31/4985 ,  A61K31/551

    CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/551 ,  C07D471/20 ,  C07D491/20

    Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(═O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(═O)R7, C(═O)OR7, C(═O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(═O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ═CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further 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 or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments.

    Abstract translation: 本发明涉及式（A）化合物，其中n为1或2; R1和R2独立地是氢，C1-4烷基，C1-4卤代烷基，C1-4烷氧基，CD3或卤素; R 3是氢，C（= O）OR 7或任选被羟基或NR 8 R 9取代的C 1-4烷基; R4是氢或氧代; R 5和R 6独立地是氢，羟基，NR 8 R 9，C（= O）R 7，C（= O）OR 7，C（= O）NR 8 R 9，C 1-4烷基，其中所述C 1-4烷基任选被羟基，NR 8 R 9 或5-或6-元杂环，其中所述5-或6-元杂环任选被C 1-4烷基或C（= O）R 7取代; 或R 5和R 6与它们所连接的碳原子一起形成= CH 2或5或6元杂环烷基，其中所述杂环烷基任选被C 1-4烷基取代; R7是氢或C1-4烷基; R8和R9独立地为氢或C1-4烷基，或R8和R9与它们所连接的氮原子一起形成5-或6-元杂环，或其药学上可接受的盐或溶剂化物。 本发明进一步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，治疗或改善瘙痒性皮肤疾病或所述化合物的病症的方法，以及所述化合物的用途 在制药中。

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