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    METHOD OF PREPARING OPTICALLY PURE PRECURSORS OF PAROXETINE
    82.
    发明申请
    METHOD OF PREPARING OPTICALLY PURE PRECURSORS OF PAROXETINE 审中-公开
    制备光学纯化前体的方法

    公开(公告)号：WO1994003428A1

    公开(公告)日：1994-02-17

    申请号：PCT/US1993007363

    申请日：1993-08-05

    Applicant: SEPRACOR, INC.

    Inventor： SEPRACOR, INC. ,  ZEPP, Charles, M. ,  GAO, Yun ,  HEEFNER, Donald, L.

    IPC: C07D211/22

    CPC classification number: C07D211/88 ,  C07D211/22 ,  C12P41/005

    Abstract: A biocatalytic method of preparing optically pure precursors of paroxetine and a method of preparing paroxetine therefrom are disclosed. A racemic trans ester precursor compound of paroxetine is first prepared. The racemic trans ester precursor compound comprises a mixture of (3S, 4R) and (3R, 4S) enantiomers. The (3R, 4S) enantiomer is hydrolyzed biocatalytically to the corresponding (3R, 4S)-trans carboxylic acid or alternatively, the (3S, 4R) enantiomer is biocatalytically hydrolyzed to the (3S, 4R)-trans carboxylic acid in a reaction catalyzed by an isolated enzyme or a microorganism. In the first instance, the unhydrolyzed (3S, 4R) enantiomer is separated from the (3R, 4S)-trans carboxylic acid, whereas in the second instance the (3S, 4R)-trans carboxylic acid is separated from the unhydrolyzed (3R, 4S) enantiomer. The (3S, 4R) enantiomer obtained following the selective hydrolysis is reduced to form a (-)-trans-(3S, 4R) primary alcohol precursor of paroxetine. Paroxetine is then formed from the (-)-trans-(3S, 4R) primary alcohol precursor.

    Abstract translation: 公开了制备帕罗西汀光学纯的前体的生物催化方法及其制备帕罗西汀的方法。 首先制备帕罗西汀的外消旋转酯前体化合物。 外消旋反式酯前体化合物包含（3S，4R）和（3R，4S）对映异构体的混合物。 将（3R，4S）对映异构体生物催化水解生成相应的（3R，4S） - 反式羧酸，或者（3S，4R）对映体在反应催化下生物催化水解成（3S，4R） - 反式羧酸 通过分离的酶或微生物。 在第一种情况下，从（3R，4R） - 反式羧酸分离出未水解的（3S，4R）对映异构体，而在第二种情况下，将（3S，4R） - 反式羧酸与未水解的（3R， 4S）对映异构体。 在选择性水解后获得的（3S，4R）对映异构体被还原形成帕罗西汀的（ - ） - 反 - （3S，4R）伯醇前体。 然后由（ - ） - 反 - （3S，4R）伯醇前体形成帕罗西汀。

    METHODS AND COMPOSITIONS FOR TREATING INFECTION USING OPTICALLY PURE (R)-LOMEFLOXACIN
    83.
    发明申请
    METHODS AND COMPOSITIONS FOR TREATING INFECTION USING OPTICALLY PURE (R)-LOMEFLOXACIN 审中-公开
    用光学纯化方法治疗感染的方法和组合物

    公开(公告)号：WO1993010786A1

    公开(公告)日：1993-06-10

    申请号：PCT/US1992010144

    申请日：1992-11-25

    Applicant: SEPRACOR, INC.

    Inventor： SEPRACOR, INC. ,  YOUNG, James, W.

    IPC: A61K31/495

    CPC classification number: A61K31/495

    Abstract: Methods and compositions are disclosed utilizing the optically pure (R)-isomer of lomefloxacin. This compound is a potent drug for the treatment of infection or other diseases requiring antibiotics while avoiding the concomitant liability of adverse effects that are associated with the racemic mixture of lomefloxacin.

    Abstract translation: 公开了使用洛美沙星的光学纯的（R） - 异构体的方法和组合物。 该化合物是治疗需要抗生素的感染或其他疾病的有效药物，同时避免与洛美沙星的外消旋混合物相关的副作用的伴随责任。

    METHODS AND COMPOSITIONS FOR TREATING HYPERTENSION, ANGINA, AND OTHER DISORDERS USING OPTICALLY PURE S(-) FELODIPINE
    84.
    发明申请
    METHODS AND COMPOSITIONS FOR TREATING HYPERTENSION, ANGINA, AND OTHER DISORDERS USING OPTICALLY PURE S(-) FELODIPINE 审中-公开
    使用光学纯S（ - ）FELODIPINE治疗高血压，血管紧张素和其他疾病的方法和组合物

    公开(公告)号：WO1993010781A1

    公开(公告)日：1993-06-10

    申请号：PCT/US1992010630

    申请日：1992-12-01

    Applicant: SEPRACOR, INC.

    Inventor： SEPRACOR, INC. ,  YOUNG, James, W.

    IPC: A61K31/44

    CPC classification number: A61K31/44

    Abstract: Methods and compositions are disclosed utilizing the optically pure S(-) isomer of felodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the racemic mixture of felodipine. The S(-) isomer of felodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of S(-) felodipine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the administration of the racemic mixture of felodipine.

    Abstract translation: 公开了使用非洛地平的光学纯的S（ - ）异构体的方法和组合物。 该化合物是治疗高血压的有效药物，同时避免与非洛地平的外消旋混合物相关的副作用的伴随责任。 非洛地平的S（ - ）异构体也可用于治疗心绞痛和其他可能与S（ - ）非洛地平作为钙通道拮抗剂如脑缺血，脑障碍，心律失常，心脏肥大的活性相关的其他病症 ，冠状动脉血管痉挛，心肌梗死，肾损伤和急性肾衰竭，而不伴随与非洛地平外消旋混合物的给药相关的不良反应。

    METHODS AND COMPOSITIONS FOR TREATING HYPERTENSION, ANGINA AND OTHER DISORDERS USING OPTICALLY PURE (-) AMLODIPINE
    85.
    发明申请
    METHODS AND COMPOSITIONS FOR TREATING HYPERTENSION, ANGINA AND OTHER DISORDERS USING OPTICALLY PURE (-) AMLODIPINE 审中-公开
    使用光学纯（ - ）AMLODIPINE治疗高血压，血管紧张素和其他疾病的方法和组合物

    公开(公告)号：WO1993010779A1

    公开(公告)日：1993-06-10

    申请号：PCT/US1992010145

    申请日：1992-11-25

    Applicant: SEPRACOR, INC.

    Inventor： SEPRACOR, INC. ,  YOUNG, James, W.

    IPC: A61K31/44

    CPC classification number: A61K31/44

    Abstract: Methods and compositions are disclosed utilizing the optically pure (-) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the racemic mixture of amlodipine. The (-) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of (-) amlodipine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.

    Abstract translation: 公开利用氨氯地平的光学纯（ - ）异构体的方法和组合物。 该化合物是治疗高血压的有效药物，同时避免与氨氯地平的外消旋混合物相关的副作用的伴随责任。 氨氯地平的（ - ）异构体也可用于治疗心绞痛和其他可能与（ - ）氨氯地平作为钙通道拮抗剂如脑缺血，脑障碍，心律失常，心脏肥大，冠状动脉 血管痉挛，心肌梗塞，肾功能衰竭和急性肾功能衰竭，无与氨氯地平外消旋混合物相关的副作用的伴随责任。

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