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    Heteroaromatic modulators of the retinoid-related orphan receptor gamma
    92.
    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.

    Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists
    94.
    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。

    Preparation of a crystalline antibiotic substance
    96.
    发明授权
    Preparation of a crystalline antibiotic substance 有权
    结晶抗生素物质的制备

    公开(公告)号：US08933063B2

    公开(公告)日：2015-01-13

    申请号：US12084231

    申请日：2006-10-30

    Applicant: Jan Jensen ,  Niels Rastrup Andersen

    Inventor： Jan Jensen ,  Niels Rastrup Andersen

    IPC: A61K31/575 ,  C07J13/00

    CPC classification number: C07J13/007

    Abstract: The present invention relates to processes for the crystallisation and for the preparation and isolation of a novel crystalline form of fusidic acid, to the use of said processes in the manufacture of pharmaceutical formulation or medicament, and to the use of said crystalline fusidic acid form for the treatment of bacterial infections.

    Abstract translation: 本发明涉及结晶和制备和分离夫西地酸的新结晶形式的方法，以及所述方法在制备药物制剂或药物中的用途，以及所述结晶夫西地酸形式用于 治疗细菌感染。

    Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases
    97.
    发明授权
    Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases 有权
    三唑并吡啶类作为治疗皮肤疾病的磷酸二酯酶抑制剂

    公开(公告)号：US08829190B2

    公开(公告)日：2014-09-09

    申请号：US12595922

    申请日：2008-04-16

    Applicant: Jakob Felding ,  Morten Dahl Sørensen

    Inventor： Jakob Felding ,  Morten Dahl Sørensen

    IPC: C07D471/04 ,  A61K31/437

    CPC classification number: C07D471/04 ,  A61K31/437

    Abstract: The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH2, CH2—CH2, CH2—NH, or NH; R1 is halogen, or R1 is alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkyl, alkoxycarbonyl, aryl, all of which are optionally substituted; R2 is hydrogen, or R2 is alkyl, cycloalkyl, alkoxy, heterocycloalkyl, aryl, heteroaryl, alkoxycarbonyl, aminocarbonyl, amino, all of which are optionally substituted; A is aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocycloalkyl or heterocycloalkenyl, all of which are optionally substituted; and pharmaceutically acceptable salts, hydrates, or solvates hereof. 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, in particular for the treatment of dermal diseases.

    Abstract translation: 本发明涉及式（I）化合物，其中X和Y为C和N或N和C; Z是CH 2，CH 2 -CH 2，CH 2 -NH或NH; R1是卤素，或R1是烷基，烯基，炔基，卤代烷基，烷氧基，环烷基，烷氧基羰基，芳基，它们都是任选被取代的; R2是氢，或R2是烷基，环烷基，烷氧基，杂环烷基，芳基，杂芳基，烷氧基羰基，氨基羰基，氨基，它们都是任选被取代的; A是芳基，环烷基，环烯基，杂芳基，杂环烷基或杂环烯基，它们都是任选被取代的; 和其药学上可接受的盐，水合物或溶剂合物。 本发明还涉及用于治疗的所述化合物，包含所述化合物的药物组合物，治疗疾病的方法，例如， 所述化合物的皮肤病，以及所述化合物在制备药物中的用途，特别是用于治疗真皮疾病。

    Substituted acetophenones useful as PDE4 inhibitors
    99.
    发明授权
    Substituted acetophenones useful as PDE4 inhibitors 有权
    用作PDE4抑制剂的取代苯乙酮

    公开(公告)号：US08497380B2

    公开(公告)日：2013-07-30

    申请号：US13546758

    申请日：2012-07-11

    Applicant: Jakob Felding ,  Simon Feldbæk Nielsen

    Inventor： Jakob Felding ,  Simon Feldbæk Nielsen

    IPC: A61K31/44 ,  C07D211/70

    CPC classification number: C07D213/61 ,  C07D413/12 ,  C07D417/12

    Abstract: The present invention relates to a compound according to formula: (1); wherein X1, X2, X3, X4 and X5 independently of each other represent —CH— or N; or X3, X4 and X5 independently of each other represent —CH— or N, and X1 and X2 independently of each other represent C and form part of an additional 6-membered aromatic ring; R1 represents hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, —CH2, —C(O)NR—R′, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, aikylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent —CH— or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to methods of treating dermal disease.

    Abstract translation: 本发明涉及式（1）化合物： 其中X1，X2，X3，X4和X5彼此独立地表示-CH-或N; 或X 3，X 4和X 5彼此独立地表示-CH-或N，并且X 1和X 2彼此独立地表示C并形成另外的6元芳环的一部分; R 1表示氢，烷基，烯基，炔基，卤代烷基，羟基烷基或烷基羰基，它们均为任选取代的; R2和R3独立地表示氢，-CH2，-C（O）NR-R'，烷基，环烷基，烯基，环烯基，炔基，卤代烷基，羟基烷基，杂环烯基，烷基芳基，烷基烷氧基羰基，烷基羰基氧基或烷氧基烷基， 取代 R 11表示氢，卤素，氰基，氨基，烷氧基或烷基氨基，X 1 -X 5表示-CH-或N，包括N-氧化物，对映体和非对映体; 及其药学上可接受的盐，水合物或溶剂化物。 本发明进一步涉及治疗真皮病的方法。

    POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND
    100.
    发明申请
    POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND 有权
    计算化合物的多晶形式

    公开(公告)号：US20130143846A1

    公开(公告)日：2013-06-06

    申请号：US13806391

    申请日：2011-06-24

    Applicant: Søren Ebdrup ,  Kim Troensegaard Nielsen ,  Tanja Maria Greve

    Inventor： Søren Ebdrup ,  Kim Troensegaard Nielsen ,  Tanja Maria Greve

    IPC: C07C217/74 ,  C07C213/10 ,  A61K31/196

    CPC classification number: C07C217/74 ,  A61K31/196 ,  C07C213/10 ,  C07C2601/08

    Abstract: The present invention relates to the crystalline, polymorphic Form X of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form X by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in a C1-C6 alkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C1-C6 alkyl ester of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.

    Abstract translation: 本发明涉及拟钙化合物{4 - [（1R，3S）-3 - （（R）-1-萘基-1-乙基氨基） - 环戊基] - 苯氧基} - 乙酸的晶体多晶型X 酸，其制备方法，通过单晶X射线晶体学（XRC），X射线粉末衍射，衰减全反射傅立叶变换红外（ATR-FTIR）光谱，固态NMR光谱和差示扫描的表征方法 量热法（DSC）及其用途。 本发明还涉及通过从饱和的{4 - [（1R，3S）-3 - （（R）-1-萘基-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸在C1-C6烷基醇中反应，或者通过碱解水解{4 - [（1R，3S）-3 - （（R） - 1-萘基-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸。

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