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    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
    11.
    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。

    Process for preparing telmisartan
    14.
    发明申请
    Process for preparing telmisartan 审中-公开
    替米沙坦制备方法

    公开(公告)号：US20090124814A1

    公开(公告)日：2009-05-14

    申请号：US12319834

    申请日：2009-01-12

    Applicant: Nurit Perlman ,  Eyal Gilboa

    Inventor： Nurit Perlman ,  Eyal Gilboa

    IPC: C07D403/02

    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，或者使用单个反应容器中的合成制备替米沙坦 。

    Processes for the preparation of a linezolid intermediate, linezolid hydroxide
    15.
    发明申请
    Processes for the preparation of a linezolid intermediate, linezolid hydroxide 审中-公开
    制备利奈唑胺中间体，利奈唑烷氢氧化物的方法

    公开(公告)号：US20090093631A1

    公开(公告)日：2009-04-09

    申请号：US12231769

    申请日：2008-09-05

    Applicant: Ben-Zion Dolitzky ,  Nurit Perlman ,  Marina Kalujny

    Inventor： Ben-Zion Dolitzky ,  Nurit Perlman ,  Marina Kalujny

    IPC: C07D413/10

    CPC classification number: C07D263/24 ,  C07D263/26

    Abstract: Provided are methods for the enantiomeric purification of Linezolid hydroxide, comprising providing a solution or a slurry of Linezolid hydroxide and a solvent selected from alcohols and ketones and crystallizing Linezolid hydroxide from the solution or slurry to obtain Linezolid hydroxide with a low content of S isomer.

    Abstract translation: 本发明提供了利奈唑烷氢氧化物的对映异构体纯化方法，包括从溶液或浆液中提供选自醇和酮的溶剂或溶剂和选自醇和酮的溶剂和结晶的利奈唑烷，以获得具有低含量的S异构体的生产线型利唑烷。

    Amorphous and polymorphic forms of telmisartan sodium
    17.
    发明申请
    Amorphous and polymorphic forms of telmisartan sodium 审中-公开
    替米沙坦钠的无定形和多晶型

    公开(公告)号：US20060293377A1

    公开(公告)日：2006-12-28

    申请号：US11267520

    申请日：2005-11-03

    Applicant: Shlomit Wizel ,  Nurit Perlman ,  Sharon Avhar-Maydan ,  Eyal Gilboa

    Inventor： Shlomit Wizel ,  Nurit Perlman ,  Sharon Avhar-Maydan ,  Eyal Gilboa

    IPC: A61K31/4184 ,  C07D403/02

    CPC classification number: C07D235/20

    Abstract: Provided is the amorphous form of telmisartan sodium and the preparation thereof. Also provided are the telmisartan sodium polymorph crystal Forms 0 to XIII and XV to XX and preparations thereof. Also provided are pharmaceutical composition of amorphous and polymorphic forms of telmisartan sodium or mixtures thereof, and methods of treatment of a mammal in need thereof.

    Abstract translation: 提供替米沙坦钠的无定形形式及其制备方法。 还提供了替米沙坦钠多晶型晶型0至XIII和XV至XX及其制剂。 还提供了替米沙坦钠或其混合物的无定形和多晶型形式的药物组合物，以及治疗有需要的哺乳动物的方法。

    Crystalline form of sitagliptin
    19.
    发明申请
    Crystalline form of sitagliptin 审中-公开
    西他列汀的结晶形式

    公开(公告)号：US20090221595A1

    公开(公告)日：2009-09-03

    申请号：US12313975

    申请日：2008-11-25

    Applicant: Nurit Perlman ,  Revital Ramaty ,  Eli Lancry ,  Marina Kalujny

    Inventor： Nurit Perlman ,  Revital Ramaty ,  Eli Lancry ,  Marina Kalujny

    IPC: A61K31/4985 ,  C07D471/04 ,  A61P3/10

    CPC classification number: C07D487/04

    Abstract: A Sitagliptin crystalline form characterized by PXRD pattern having any 5 peaks selected from the group consisting of 7.4, 11.5, 16.7, 17.7, 18.9, 24.1, 24.5, 27.0, 28.5 and 28.8±0.2 degrees 2-theta, wherein any combination of peaks selected includes the peak at 7.4±0.2 degrees two theta, processes for preparing said Sitagliptin crystalline form, and pharmaceutical compositions thereof, are provided.

    Abstract translation: 西他列汀结晶形式，其特征在于具有选自7.4,11.5,16.7,17.7,18.9,24.1,24.5,27.0,28.5和28.8±0.2度2-θ的任何5个峰的PXRD图，其中所选择的峰的任意组合 包括峰值在7.4±0.2度2θ，制备所述西格列汀结晶形式的方法及其药物组合物。

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