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    ORGANIC COMPOUNDS
    1.
    发明申请
    ORGANIC COMPOUNDS 审中-公开
    有机化合物

    公开(公告)号：US20110015191A1

    公开(公告)日：2011-01-20

    申请号：US12528483

    申请日：2008-02-22

    申请人： Johannes Ludescher ,  Josef Wieser ,  Arthur Pichler ,  Ulrich Griesser ,  Doris Braun

    发明人： Johannes Ludescher ,  Josef Wieser ,  Arthur Pichler ,  Ulrich Griesser ,  Doris Braun

    IPC分类号： A61K31/5377 ,  C07D413/06 ,  A61P1/08

    CPC分类号： C07D413/06

    摘要： Novel polymorph form III of Aprepitant and a method for preparation of novel form III is disclosed. New processes for the preparation of Aprepitant form II are disclosed. The processes involve transformation of form III to form II by heating in decalin and the precipitation of form II from a solvent or solvent mixture by cooling and/or addition of addition of seed crystals or an anti solvent. Solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A process for the preparation of the solid dispersion by evaporation of a solution of Aprepitant and the carrier in a suitable solvent is disclosed. Stable Aprepitant form II is disclosed. Further pharmaceutical compositions containing Aprepitant form II, III or solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A methanol solvate of Aprepitant is disclosed.

    摘要翻译： 公开了Aprepitant的新型多晶型III和新型III的制备方法。 公开了制备Aprepitant II型的新方法。 所述方法包括通过在十氢化萘中加热和通过冷却和/或加入晶种或抗溶剂从溶剂或溶剂混合物中沉淀形式II而转化成形式II。 公开了在合适的载体中含有形式II的固体分散体。 公开了通过在适当溶剂中蒸发阿维地丁和载体溶液来制备固体分散体的方法。 公开了稳定的Aprepitant II型。 公开了另外的药物组合物，其中含有Aprepitant形式II，III或在合适的载体中含有Aprepitant II型的固体分散体。 公开了一种甲酸溶剂化物的Aprepitant。

    CRYSTALLINE FORM OF CINACALCET
    3.
    发明申请
    CRYSTALLINE FORM OF CINACALCET 审中-公开
    CINACALCET的结晶形式

    公开(公告)号：US20090197970A1

    公开(公告)日：2009-08-06

    申请号：US12303411

    申请日：2007-06-25

    申请人： Johannes Ludescher ,  Ulrich Griesser ,  Doris Braun ,  Josef Wieser

    发明人： Johannes Ludescher ,  Ulrich Griesser ,  Doris Braun ,  Josef Wieser

    IPC分类号： A61K31/137 ,  C07C211/52

    CPC分类号： C07C211/30

    摘要： The present invention relates to the polymorph form II of Cinacalcet hydrochloride, methods for the preparation of pure form II of Cinacalcet hydrochloride, and pharmaceutical compositions comprising the new polymorphic form in an pharmaceutically effective amount The present invention also provides novel solvates of Cinacalcet hydrochloride, methods for the preparation of these solvates, the use of these novel solvates for the preparation of pure Cinacalcet hydrochloride, the use of these novel solvates for the preparation of polymorphic form II of Cinacalcet hydrochloride and pharmaceutical compositions comprising the acetic acid solvate of Cinacalcet hydrochloride.

    摘要翻译： 本发明涉及盐酸西那卡塞的多晶型II，盐酸西那卡塞的纯形式II的制备方法和药物组合物，其含有药学有效量的新型多晶型本发明还提供盐酸西卡西塞的新型溶剂合物，方法 为了制备这些溶剂合物，使用这些新型溶剂合物制备纯的西那卡塞盐酸盐，这些新型溶剂合物用于制备盐酸西那卡塞的多晶型II和包含盐酸西卡西塞的乙酸溶剂化物的药物组合物的用途。

    CRYSTALLINE FORM OF AN ORGANIC COMPOUND
    9.
    发明申请
    CRYSTALLINE FORM OF AN ORGANIC COMPOUND 有权
    有机化合物的结晶形式

    公开(公告)号：US20110306764A1

    公开(公告)日：2011-12-15

    申请号：US13139863

    申请日：2009-12-18

    申请人： Johannes Ludescher ,  Josef Wieser ,  Gerhard Laus

    发明人： Johannes Ludescher ,  Josef Wieser ,  Gerhard Laus

    IPC分类号： C07D239/545

    CPC分类号： C07D401/04

    摘要： The present invention is directed to a crystalline form of 2-[6-[3(R)-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]-benzonitrile, a process for the preparation of said crystalline form and the use thereof in the manufacture of a pharmaceutical composition.

    摘要翻译： 本发明涉及2- [6- [3（R） - 氨基哌啶-1-基] -3-甲基-2,4-二氧代-1,2,3,4-四氢嘧啶-1-基 甲基] - 苄腈，制备所述结晶形式的方法及其在制备药物组合物中的用途。