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    Methods for treating hypertension using optically pure S(-) felodipine
    42.
    发明授权
    Methods for treating hypertension using optically pure S(-) felodipine 失效
    使用光学纯的S（ - ）非洛地平治疗高血压的方法

    公开(公告)号：US5834496A

    公开(公告)日：1998-11-10

    申请号：US342669

    申请日：1994-11-21

    Applicant: James W. Young

    Inventor： James W. Young

    IPC: A61K31/4422 ,  A61K31/44

    CPC classification number: A61K31/4422

    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。

    In vitro method for predicting the evolutionary response of a protein to a drug targeted thereagainst
    44.
    发明授权
    In vitro method for predicting the evolutionary response of a protein to a drug targeted thereagainst 失效
    用于预测蛋白质对其靶向药物的进化反应的体外方法

    公开(公告)号：US5766842A

    公开(公告)日：1998-06-16

    申请号：US706178

    申请日：1996-08-30

    Applicant: Laurence M. Melnick ,  Donald L. Heefner

    Inventor： Laurence M. Melnick ,  Donald L. Heefner

    IPC: C12N9/50 ,  C12N15/10 ,  C12Q1/37 ,  C12Q1/68 ,  C12N15/48 ,  C12Q1/70

    CPC classification number: C12N15/1072 ,  C12N15/1048 ,  C12N9/506 ,  C12Q1/37 ,  C12Q1/6811 ,  G01N2333/16 ,  G01N2333/8142

    Abstract: A method for identifying, in vitro, distinct, drug-resistant, biologically-active mutants of a protein that may emerge in vivo in response to a drug targeted against the protein is disclosed. The method involves preparing, by heterologous expression of a library of nucleotide sequences, a complete library of mutant proteins accessible in a single generation. The mutant proteins from the library that are drug resistant are identified. When all the first generation mutants have been identified in the above manner, a combination of drugs can be identified that will block the development of resistance. The same technique allows evaluation of the ultimate clinical efficacy of a drug targeted against the protein by comparing the number of resistant first generation mutants. A preferred protein is an HIV protease.

    Abstract translation: 公开了一种用于鉴定体内可鉴定的针对蛋白质靶向药物可能在体内出现的蛋白质的体外，不同的耐药性，生物活性突变体的方法。 该方法包括通过异源表达核苷酸序列文库来制备在单代中可获得的突变蛋白的完整文库。 鉴定出抗药性的文库突变蛋白。 当所有第一代突变体都以上述方式鉴定时，可以鉴定出将阻止抗性发展的药物组合。 相同的技术允许通过比较抗性第一代突变体的数量来评估靶向蛋白质的药物的最终临床疗效。 优选的蛋白质是HIV蛋白酶。

    Taxol process and compounds
    45.
    发明授权
    Taxol process and compounds 失效
    紫杉醇工艺和化合物

    公开(公告)号：US5760251A

    公开(公告)日：1998-06-02

    申请号：US589142

    申请日：1996-01-19

    Applicant: Yun Gao ,  Charles M. Zepp

    Inventor： Yun Gao ,  Charles M. Zepp

    IPC: C07C271/22 ,  C07D305/14 ,  C07F7/18

    CPC classification number: C07F7/1856 ,  C07C271/22 ,  C07D305/14

    Abstract: A process for the preparation of taxol and derivatives of taxol ##STR1## is disclosed. The process involves reacting a .beta.-alkoxycarbonylamino-phenylpropionic acid with a 13-hydroxy taxane to produce an ester of the taxane at C-13; and then deprotecting the .beta.-alkoxycarbonylamino-phenylpropionic ester to produce a .beta.-amido-.alpha.-hydroxybenzenepropanoic ester of the taxane. Intermediates useful in the process are also disclosed.

    Abstract translation: 披露了紫杉醇和紫杉醇衍生物“IMAGE”的制备方法。 该方法包括使β-烷氧基羰基氨基 - 苯基丙酸与13-羟基紫杉烷反应以在C-13处产生紫杉烷的酯; 然后脱保护β-烷氧基羰基氨基 - 苯基丙酸酯以产生紫杉烷的β-氨基-α-羟基苯丙酸酯。 还公开了在该方法中有用的中间体。

    Compositions using optically pure R(+) ondansetron
    48.
    发明授权
    Compositions using optically pure R(+) ondansetron 失效
    使用光学纯的R（+）昂丹司琼的组合物

    公开(公告)号：US5712302A

    公开(公告)日：1998-01-27

    申请号：US513368

    申请日：1995-08-10

    Applicant: James W. Young

    Inventor： James W. Young

    IPC: A61K9/08 ,  A61K9/48 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/45

    CPC classification number: A61K31/4178 ,  A61K31/415 ,  Y10S514/872

    Abstract: Methods and compositions are disclosed utilizing the optically pure R(+) isomer of ondansetron. This compound is a potent drug for the treatment of nausea and vomiting associated with chemotherapy and radiation therapy, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. The R(+) isomer of ondansetron is also useful for the treatment of behavioral disorders such as mood anxiety and schizophrenia, and such other conditions as may be related to R(+) ondansetron's activity as a competitive antagonist of serotonin receptor subtype 5-HT.sub.3 such as disorders of gastrointestinal motility, depression, migraine, and as an aid for alcohol withdrawal, nicotine withdrawal, and drug (benzodiazepine et al.) withdrawal, without the concomitant liability of adverse effects associated with the racemic mixture of ondansetron. Furthermore, the R(+) isomer of ondansetron is also useful for the treatment of cognitive disorders such as dementia or age-associated memory impairment, while avoiding the concomitant liability of adverse effects associated with the racemic mixture of ondansetron.

    Abstract translation: 公开了使用昂丹司琼的光学纯的R（+）异构体的方法和组合物。 该化合物是用于治疗与化疗和放射治疗相关的恶心和呕吐的有效药物，同时避免与昂丹司琼外消旋混合物相关的副作用的伴随责任。 昂丹司琼的R（+）异构体也可用于治疗诸如情绪焦虑和精神分裂症等行为障碍，以及可能与R（+）昂丹司琼活性相关的其他条件，作为5-羟色胺受体亚型5-HT3的竞争性拮抗剂 例如消化道运动障碍，抑郁症，偏头痛，以及用于酒精戒断，尼古丁戒断和药物（苯并二氮杂类等）撤离的辅助，而不伴随昂丹司琼外消旋混合物的不良反应。 此外，昂丹司琼的R（+）异构体也可用于治疗诸如痴呆或年龄相关记忆障碍的认知障碍，同时避免与昂丹司琼的外消旋混合物相关的副作用的伴随责任。

    Methods for treating urticaria using optically pure (+) cetirizine
    50.
    发明授权
    Methods for treating urticaria using optically pure (+) cetirizine 失效
    使用光学纯（+）西替利嗪治疗荨麻疹的方法

    公开(公告)号：US5627183A

    公开(公告)日：1997-05-06

    申请号：US622617

    申请日：1996-03-26

    Applicant: Nancy M. Gray

    Inventor： Nancy M. Gray

    IPC: C07D241/04 ,  A61K31/495 ,  A61P11/00 ,  A61P37/08

    CPC classification number: A61K31/495

    Abstract: Methods are disclosed utilizing optically pure (+) cetirizine for the treatment of urticaria in humans while avoiding the concomitant liability of adverse effects associated with the racemic mixture of cetirizine.

    Abstract translation: 公开了利用光学纯（+）西替利嗪治疗人类荨麻疹的方法，同时避免与西替利嗪的外消旋混合物相关的副作用的伴随的责任。

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