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    ENANTHIOSELECTIVE PREPARATION OF THIAZOLE DERIVATIVES
    2.
    发明申请
    ENANTHIOSELECTIVE PREPARATION OF THIAZOLE DERIVATIVES 审中-公开
    噻唑衍生物的选择性制备

    公开(公告)号：WO1995002585A1

    公开(公告)日：1995-01-26

    申请号：PCT/IB1994000062

    申请日：1994-04-06

    Applicant: PFIZER INC. ,  QUALLICH, George, Joseph

    Inventor： PFIZER INC.

    IPC: C07D277/24

    CPC classification number: C07D417/04 ,  C07D277/24 ,  C07F5/02

    Abstract: An enanthioselective process for preparing the compounds of formulas (I) and (II) from the prochiral ketone precursor of the alcohol of formula (I). The compounds of formulas (I) and (II) are thus obtained in substantially enantiomerically pure form by reducing the ketone with a borane reducing agent in the presence of a chiral oxazaborolidine catalyst.

    Abstract translation: 从式（I）的醇的前手性酮前体制备式（I）和（II）化合物的对映选择性方法。 因此，在手性恶唑硼烷催化剂存在下，通过用硼烷还原剂还原酮，从而以基本上对映体纯的形式获得式（I）和（II）化合物。

    PHARMACEUTICALLY ACCEPTABLE SALTS OF SERTRALINE AND PHARMACEUTICAL COMPOSITIONS THEREOF
    3.
    发明申请
    PHARMACEUTICALLY ACCEPTABLE SALTS OF SERTRALINE AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
    其药物和药物组合物的药学上可接受的盐

    公开(公告)号：WO2004065348A1

    公开(公告)日：2004-08-05

    申请号：PCT/IB2004/000116

    申请日：2004-01-14

    Applicant: PFIZER PRODUCTS INC. ,  QUALLICH, George, Joseph ,  WINT, Lewin, T.

    Inventor： QUALLICH, George, Joseph ,  WINT, Lewin, T.

    IPC: C07C211/42

    CPC classification number: C07C211/42 ,  C07C2602/10 ,  C07C2602/28

    Abstract: The present invention is directed to certain pharmaceutically acceptable salts of the therapeutically potent selective serotonin reuptake inhibitor, sertraline: Formula (I), and pharmaceutical compositions thereof, wherein said salts are selected from the group consisting of the p-toluenesulfonic acid salt, the fumaric acid salt, the benzenesulfonic acid salt, the benzoic acid salt, the L-tartaric acid salt and the (-)-camphor-10-sulfonic acid salt.

    Abstract translation: 本发明涉及治疗有效的选择性5-羟色胺再摄取抑制剂舍曲林的某些药学上可接受的盐，舍曲林：式（I）及其药物组合物，其中所述盐选自对甲苯磺酸盐，富马酸 苯磺酸盐，苯甲酸盐，L-酒石酸盐和（ - ） - 樟脑-10-磺酸盐。

    APO B-SECRETION/MTP INHIBITORY AMIDES
    5.
    发明申请
    APO B-SECRETION/MTP INHIBITORY AMIDES 审中-公开
    APO B分泌/ MTP抑制剂

    公开(公告)号：WO1998023593A1

    公开(公告)日：1998-06-04

    申请号：PCT/IB1997001368

    申请日：1997-11-03

    Applicant: PFIZER INC. ,  CHANG, George ,  QUALLICH, George, Joseph

    Inventor： PFIZER INC.

    IPC: C07D217/04

    CPC classification number: C07D401/04 ,  C07D217/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06

    Abstract: This invention is directed to compounds of formula (I) or the stereoisomers, pharmaceutically acceptable salts and hydrates thereof. The compounds are Apo B/MTP inhibitors and are useful in the treatment of various disorders and conditions such as atherosclerosis, pancreatitis, obesity, hypercholesteremia, hypertriglyceridemia, hyperlipidemia, and diabetes. The compounds of this invention are also useful in combination with other pharmaceutical agents including cholesterol biosynthesis inhibitors and cholesterol absorption inhibitors, especially HMG-CoA reductase inhibitors and HMG-CoA synthase inhibitors; HMG-CoA reductase gene expression inhibitors; CETP inhibitors; bile acid sequestrants; fibrates; cholesterol absorption inhibitors; ACAT inhibitors, squalene synthetase inhibitors, ion-exchange resins, anti-oxidants and niacin. This invention is also directed to intermediates and processes useful in the preparation of compounds of formula (I).

    Abstract translation: 本发明涉及式（I）化合物或其立体异构体，其药学上可接受的盐和水合物。 这些化合物是Apo B / MTP抑制剂，可用于治疗各种疾病和病症如动脉粥样硬化，胰腺炎，肥胖症，高胆固醇血症，高甘油三酯血症，高脂血症和糖尿病。 本发明的化合物还可与其它药剂组合使用，包括胆固醇生物合成抑制剂和胆固醇吸收抑制剂，特别是HMG-CoA还原酶抑制剂和HMG-CoA合成酶抑制剂; HMG-CoA还原酶基因表达抑制剂; CETP抑制剂; 胆汁酸螯合剂 贝特类药物; 胆固醇吸收抑制剂; ACAT抑制剂，角鲨烯合成酶抑制剂，离子交换树脂，抗氧化剂和烟酸。 本发明还涉及可用于制备式（I）化合物的中间体和方法。

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