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    NEW POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND
    131.
    发明申请
    NEW POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND 有权
    一种计算化合物的新型多晶型

    公开(公告)号：US20130131023A1

    公开(公告)日：2013-05-23

    申请号：US13806690

    申请日：2011-06-24

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

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

    IPC: C07C217/74 ,  C07C213/10 ,  A61K31/593 ,  A61K31/196 ,  A61K31/592

    CPC classification number: C07C217/74 ,  A61K31/196 ,  A61K31/592 ,  A61K31/593 ,  C07C213/10 ,  C07C2601/08

    Abstract: The present invention relates to the crystalline, polymorphic Form C 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 C by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in the presence of crystallization seeds of Form C, or alternatively by conversion of an amorphous starting material into the different crystalline polymorphic Form X by crystallization of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, followed by a solid solution transformation thereof into the desired polymorphic Form C.

    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} - 乙酸的结晶多晶型C 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} - 乙酸在形式C的结晶晶种存在下，或者通过{4 - [（1R，3S）-3 - （（R）-1）的结晶将无定形原料转化成不同结晶多晶型X 萘-1-基 - 乙基氨基） - 环戊基] - 苯氧基} - 乙酸，然后将其固溶转化为所需的多晶型C.

    Substituted acetophenones useful as PDE4 inhibitors
    134.
    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：US08324394B2

    公开(公告)日：2012-12-04

    申请号：US13406932

    申请日：2012-02-28

    Applicant: Jakob Felding ,  Simon Feldbæk Nielsen

    Inventor： Jakob Felding ,  Simon Feldbæk Nielsen

    IPC: C07D213/46 ,  A61K31/44

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

    Abstract: The present invention relates to a compound according to formula: (I); 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, hydroxyallyl, 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, alkylcarbonyloxy, 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 processes for the preparation of said compounds, 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.

    Abstract translation: 本发明涉及式（I）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; R1代表氢，烷基，烯基，炔基，卤代烷基，羟基烯基或烷基羰基，它们都是任选取代的; 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，杂链烯基，烷基芳基，烷基烷氧基羰基，烷基羰氧基或烷氧基烷基， ; 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。 本发明进一步涉及制备所述化合物，所述化合物用于治疗的方法，包含所述化合物的药物组合物，治疗疾病的方法。 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。

    Topical Composition Comprising an Antibacterial Substance
    139.
    发明申请
    Topical Composition Comprising an Antibacterial Substance 审中-公开
    包含抗菌物质的局部组合物

    公开(公告)号：US20090054389A1

    公开(公告)日：2009-02-26

    申请号：US12087743

    申请日：2007-02-01

    Applicant: Mette Rydahl Sonne

    Inventor： Mette Rydahl Sonne

    IPC: A61K31/575 ,  A61P17/00 ,  A61P31/04

    CPC classification number: A61K9/0014 ,  A61K31/23 ,  A61K31/575 ,  A61K47/14

    Abstract: A pharmaceutical composition for topical application comprises a fusidic acid derivative of general formula I as disclosed herein and one or more monoglycerides of a fatty acid. The composition may be used in the treatment of a disease or condition of the skin or mucosa, in particular skin infections.

    Abstract translation: 用于局部施用的药物组合物包含本文公开的通式I的夫西地酸衍生物和一种或多种脂肪酸的单甘油酯。 该组合物可用于治疗皮肤或粘膜的疾病或病症，特别是皮肤感染。

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