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    Heteroaromatic modulators of the retinoid-related orphan receptor gamma
    45.
    发明授权
    Heteroaromatic modulators of the retinoid-related orphan receptor gamma 有权

    公开(公告)号：US10662181B2

    公开(公告)日：2020-05-26

    申请号：US16317655

    申请日：2017-07-11

    Applicant: LEO PHARMA A/S

    Inventor： Alan Stuart Jessiman ,  Patrick Stephen Johnson ,  Kristoffer Maansson ,  Morten Dahl Sørensen

    IPC: C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D241/04

    Abstract: The present invention relates to a compound according to general formula (I) wherein X represents N or CH; R1 is —CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C3-C7)cycloalkyl(C1-C4)alkyl, (3-7 membered)heterocycloalkyl-(C1-C4)alkyl or (5-6 membered)heteroaryl-(C1-C4)alkyl; R2 is halogen, cyano, (C1-C4)alkyl or (C3-C7)cycloalkyl; R3 is halogen, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl or (C3-C7)cycloalkyl; R4 is (C1-C4)alkyl or (C1-C4)haloalkyl; R5 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or —ORa. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds.

    BICYCLIC AMINES AS NOVEL JAK KINASE INHIBITORS
    46.
    发明申请
    BICYCLIC AMINES AS NOVEL JAK KINASE INHIBITORS 审中-公开

    公开(公告)号：US20190382418A1

    公开(公告)日：2019-12-19

    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 represents 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, 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.

    Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists
    48.
    发明授权
    Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists 有权
    取代的吡咯并[1,2-a]哌嗪和吡咯并[1,2-a] [1,4]二氮杂卓作为神经激肽1受体拮抗剂

    公开(公告)号：US09181259B2

    公开(公告)日：2015-11-10

    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: A61K31/4985 ,  A61K31/551 ,  C07D241/38 ,  C07D243/10 ,  C07D487/04 ,  A61K31/5377 ,  C07D471/20 ,  C07D491/20

    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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