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    CRYSTALLINE FORMS OF SITAGLIPTIN PHOSPHATE
    3.
    发明申请
    CRYSTALLINE FORMS OF SITAGLIPTIN PHOSPHATE 审中-公开
    磷酸西他汀的结晶形式

    公开(公告)号：US20100041885A1

    公开(公告)日：2010-02-18

    申请号：US12410738

    申请日：2009-03-25

    Applicant: Nurit Perlman ,  Revital Ramaty ,  Mili Abramov ,  Nina Finkelstein ,  Eli Lancry ,  Shay Asis ,  Ariel Mittelman

    Inventor： Nurit Perlman ,  Revital Ramaty ,  Mili Abramov ,  Nina Finkelstein ,  Eli Lancry ,  Shay Asis ,  Ariel Mittelman

    IPC: C07D471/08

    CPC classification number: C07D487/04

    Abstract: A Sitagliptin phosphate characterized by data selected from the group consisting of: a powder XRD pattern with peaks at 4.7, 13.5, 17.7, 18.3, and 23.7±0.2 degrees two theta; a powder XRD pattern with peaks at about 4.7, 13.5, and 15.5±0.2 degrees two theta and at least another two peaks selected from the following list: 14.0, 14.4, 18.3, 19.2, 19.5 and 23.7±0.2 degrees two theta; and a powder XRD pattern with peaks at about 13.5, 19.2, and 19.5±0.2 degrees two theta and at least another two peaks selected from the following list: 4.7, 14.0, 15.1, 15.5, 18.3, and 18.7±0.2 degrees two theta; a powder XRD pattern with peaks at about 13.5, 15.5, 19.2, 23.7, and 24.4±0.2 degrees two theta; and a powder XRD pattern with peaks at about 4.65, 13.46, 17.63, 18.30, and 23.66±0.10 degrees two theta, processes for preparing said Sitagliptin crystalline form, and pharmaceutical compositions thereof, are provided.

    Abstract translation: 磷酸西他列汀，其特征在于选自以下的数据：粉末XRD图谱，其峰为4.7,13.5,17.7,18.3和23.7±0.2度2θ; 在约4.7,13.5和15.5±0.2度2θ处具有峰的粉末XRD图案和至少另外两个选自以下列表的峰：14.0,14.4,18.3,19.2,19.5和23.7±0.2度2θ; 和具有在约13.5,19.2和19.5±0.2度2θ处以及从下列列表中选择的至少另外两个峰的峰的粉末XRD图：4.7,14.0,15.1,15.5,18.3和18.7±0.2度2θ; 在约13.5,15.5,19.2,23.7和24.4±0.2度2θ处具有峰的粉末XRD图案; 并且提供了在约4.65,13.46,17.63,18.30和23.66±0.10度2θ处具有峰的粉末XRD图案，制备所述西格列汀结晶形式的方法及其药物组合物。

    Process for preparing telmisartan
    4.
    发明授权
    Process for preparing telmisartan 失效
    替米沙坦制备方法

    公开(公告)号：US07501448B2

    公开(公告)日：2009-03-10

    申请号：US11250267

    申请日：2005-10-13

    Applicant: Nurit Perlman ,  Eyal Gilboa

    Inventor： Nurit Perlman ,  Eyal Gilboa

    IPC: A61K31/4184 ,  C07D235/04

    CPC classification number: C07D235/14 ,  C07D235/18

    Abstract: Provided are processes for preparing telmisartan alkyl ester and telmisartan using environmentally friendly organic solvents that are easily removed from the reaction mixture, wherein a telmisartan alkyl ester is isolated and hydrolyzed to form telmisartan or the telmisartan is prepared using a synthesis in a single reaction vessel.

    Abstract translation: 提供了使用易于从反应混合物中除去的环境友好的有机溶剂来制备替米沙坦烷基酯和替米沙坦的方法，其中分离并水解替米沙坦烷基酯以形成替米沙坦，或者在单个反应容器中使用合成制备替米沙坦。

    Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe
    7.
    发明申请
    Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe 审中-公开
    制备（3R，4S）-4 - （（4-苄氧基）苯基）-1-（4-氟苯基）-3 - （（S）-3-（4-氟苯基）-3-羟丙基） - 2-氮杂环丁酮，合成依泽替米贝的中间体

    公开(公告)号：US20070259845A1

    公开(公告)日：2007-11-08

    申请号：US11517704

    申请日：2006-09-08

    Applicant: Vinod Kansal ,  Suhail Ahmad ,  Bhupendra Tyagi ,  Nitin Gupta ,  Nurit Perlman

    Inventor： Vinod Kansal ,  Suhail Ahmad ,  Bhupendra Tyagi ,  Nitin Gupta ,  Nurit Perlman

    IPC: A61K31/397 ,  A61P9/12 ,  C07D205/00

    CPC classification number: C07D205/08 ,  Y02P20/55

    Abstract: The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a) having an enantiomeric purity of at least about 97.5%. The invention also encompasses Compound 2a having a chemical purity of at least about 97%. The invention further encompasses processes for preparing Compound 2a from Compound 1 having the following formula: The invention also encompasses processes for preparing a compound having the following formula: from a compound having the following formula: wherein R is selected from the group consisting of: H or a hydroxyl protecting group. The invention also encompasses processes for preparing Compound 2a, preferably to form Compound 2a-Form 01. Also included are processes for preparing ezetimibe from Compound 2a-Form 01 or Compound 2a prepared according to the invention, compositions containing such ezetimibe, and methods for reducing cholesterol using such compositions.

    Abstract translation: 本发明包括（3R，4S）-4 - （（4-苄氧基）苯基）-1-（4-氟苯基）-3-（3-（4-氟苯基）-3-氧代丙基）-2-氮杂环丁酮（化合物2a ）具有至少约97.5％的对映体纯度。 本发明还包括具有至少约97％的化学纯度的化合物2a。 本发明还包括从具有下式的化合物1制备化合物2a的方法：本发明还包括由具有下式的化合物制备具有下式的化合物的方法：其中R选自：H 或羟基保护基。 本发明还包括制备化合物2a，优选形成化合物2a-形式01的方法。还包括用于制备根据本发明制备的化合物2a-形式01或化合物2a的依泽替米贝的方法，含有这种依泽替米贝的组合物，以及还原方法 使用这种组合物的胆固醇。

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