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    METHODS FOR PREPARING SYNTHETIC BILE ACIDS AND COMPOSITIONS COMPRISING THE SAME
    26.
    发明申请
    METHODS FOR PREPARING SYNTHETIC BILE ACIDS AND COMPOSITIONS COMPRISING THE SAME 审中-公开
    制备合成胆酸的方法及其组合物

    公开(公告)号：WO2012047495A3

    公开(公告)日：2012-08-09

    申请号：PCT/US2011052204

    申请日：2011-09-19

    Applicant: KYTHERA BIOPHARMACEUTICALS INC ,  MORIARTY ROBERT M ,  RAO PHOTON

    Inventor： MORIARTY ROBERT M ,  RAO PHOTON

    IPC: C07J21/00 ,  A61K31/56 ,  A61P3/04 ,  C07J9/00 ,  C07J41/00 ,  C07J75/00

    CPC classification number: C07J41/0061 ,  A61K31/56 ,  A61K45/06 ,  C07J1/0011 ,  C07J5/0053 ,  C07J9/005 ,  C07J13/005 ,  C07J13/007 ,  C07J21/006 ,  C07J43/003 ,  A61K2300/00

    Abstract: This invention relates generally to methods for preparing certain bile acids from non-mammalian sourced starting materials as well as to synthetic bile acids and compositions comprising such acids wherein the acids are characterized by a different C14 population than naturally occurring bile acids as well as being free from any mammalian pathogens. This invention is also directed to the synthesis of intermediates useful in the synthesis of such bile acids. Accordingly, the C ring of the steroidal scaffold is oxidized to provide a synthetic route and intermediates to DCA. This invention also provides synthetic methods for preparing deoxycholic acid or a salt thereof starting from aromatic steroids such as estrogen, equilenin, and derivatives thereof. This invention is also directed to intermediates such as 12-oxo or delta-9,11-ene steroids as well as novel processes for their preparation. In preferred embodiments, bile acids are provided herein which have substituents on the B-ring and/or D-ring side chain and optionally on the hydroxy group of the A-ring.

    Abstract translation: 本发明一般涉及从非哺乳动物源起始原料以及合成胆汁酸制备某些胆汁酸的方法以及包含这些酸的组合物，其中酸的特征在于与天然存在的胆汁酸不同的C14种群以及游离的 来自任何哺乳动物病原体。 本发明还涉及可用于合成这种胆汁酸的中间体的合成。 因此，甾体支架的C环被氧化以提供DCA的合成途径和中间体。 本发明还提供从芳族类固醇如雌激素，平衡物及其衍生物制备脱氧胆酸或其盐的合成方法。 本发明还涉及中间体，例如12-氧代或δ-9,11-烯类固醇，以及它们制备的新方法。 在优选的实施方案中，本文提供了在B-环和/或D-环侧链和任选地在A环的羟基上具有取代基的胆汁酸。

    METHODS FOR PREPARING SYNTHETIC BILE ACIDS AND COMPOSITIONS COMPRISING THE SAME
    27.
    发明申请
    METHODS FOR PREPARING SYNTHETIC BILE ACIDS AND COMPOSITIONS COMPRISING THE SAME 审中-公开
    制备合成胆汁酸的方法和包含其的组合物

    公开(公告)号：WO2012047495A2

    公开(公告)日：2012-04-12

    申请号：PCT/US2011/052204

    申请日：2011-09-19

    Applicant: KYTHERA BIOPHARMACEUTICALS, INC. ,  MORIARTY, Robert M. ,  RAO, Photon

    Inventor： MORIARTY, Robert M. ,  RAO, Photon

    IPC: C07J21/00 ,  C07J75/00 ,  C07J9/00 ,  C07J41/00 ,  A61K31/56 ,  A61P3/04

    CPC classification number: C07J41/0061 ,  A61K31/56 ,  A61K45/06 ,  C07J1/0011 ,  C07J5/0053 ,  C07J9/005 ,  C07J13/005 ,  C07J13/007 ,  C07J21/006 ,  C07J43/003 ,  A61K2300/00

    Abstract: This invention relates generally to methods for preparing certain bile acids from non-mammalian sourced starting materials as well as to synthetic bile acids and compositions comprising such acids wherein the acids are characterized by a different C 14 population than naturally occurring bile acids as well as being free from any mammalian pathogens. This invention is also directed to the synthesis of intermediates useful in the synthesis of such bile acids. Accordingly, the C ring of the steroidal scaffold is oxidized to provide a synthetic route and intermediates to DCA. This invention also provides synthetic methods for preparing deoxycholic acid or a salt thereof starting from aromatic steroids such as estrogen, equilenin, and derivatives thereof. This invention is also directed to intermediates such as 12-oxo or delta-9,11-ene steroids as well as novel processes for their preparation. In preferred embodiments, bile acids are provided herein which have substituents on the B-ring and/or D-ring side chain and optionally on the hydroxy group of the A-ring.

    Abstract translation: 本发明一般涉及从非哺乳动物来源的起始材料以及合成胆汁酸和包含这些酸的组合物制备某些胆汁酸的方法，其中所述酸的特征在于不同的C 14群体比天然存在的胆汁酸以及没有任何哺乳动物病原体。 本发明还涉及用于合成这种胆汁酸的中间体的合成。 因此，类固醇支架的C环被氧化以提供合成途径和DCA的中间体。 本发明还提供从芳香族类固醇如雌激素，equilenin及其衍生物开始制备脱氧胆酸或其盐的合成方法。 本发明还涉及中间体如12-氧代或δ-9,11-烯类固醇以及其制备新方法。 在优选的实施方案中，本文提供了在B-环和/或D-环侧链上以及任选地在A-环的羟基上具有取代基的胆汁酸。

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