中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

21 records (took 0.027 seconds)

    IN VITRO METHOD FOR PREDICTING THE EVOLUTIONARY RESPONSE OF HIV PROTEASE TO A DRUG TARGETED THEREAGAINST
    11.
    发明申请
    IN VITRO METHOD FOR PREDICTING THE EVOLUTIONARY RESPONSE OF HIV PROTEASE TO A DRUG TARGETED THEREAGAINST 审中-公开
    用于预测艾滋病病毒蛋白酶对药物靶向药物的演变反应的体外方法

    公开(公告)号：WO1996008580A1

    公开(公告)日：1996-03-21

    申请号：PCT/US1995011860

    申请日：1995-09-18

    Applicant: SEPRACOR INC. ,  MELNICK, Laurence, M. ,  HEEFNER, Donald, L.

    Inventor： SEPRACOR INC.

    IPC: C12Q01/37

    CPC classification number: C12N9/506 ,  C12N15/1048 ,  C12Q1/37 ,  C12Q1/6811 ,  G01N2333/16 ,  G01N2333/8142 ,  Y10S435/974 ,  Y10S435/975

    Abstract: An in vitro method for identifying distinct, first generation, drug-resistant, biologically active, HIV protease mutants that may emerge in vivo in response to a drug targeted thereagainst comprising: (a) preparing, in the presence of the drug, a library of all first-generation mutants of the protease differing therefrom by one to three amino acid substitutions, each of the protease mutants being generated as part of a polyprotein with reverse transcriptase; (b) isolating drug-resistant, biologically-active mutant proteases by assaying for activity of the reverse transcriptase; and (c) identifying the distinct amino acid changes leading to the drug-resistance of the active, mutant proteases so isolated. An in vitro method for evaluating the efficacy of a drug against a biologically active mutant or wild-type form of HIV protease comprising combining the drug and a mutant polyprotein, comprising an inactive HIV protease, HIV reverse transcriptase, and one or more protease cleavage sites, adding biologically-active mutant or wild-type protease, assaying for release of active reverse transcriptase, whereby reverse transcriptase activity indicates that the drug is not efficacious against the mutant or wild-type form of HIV protease tested.

    Abstract translation: 一种体外方法，其用于鉴定可能在其靶向靶向药物的体内可能出现的不同的第一代，耐药性，生物活性的HIV蛋白酶突变体，其包括：（a）在所述药物存在下，制备 所有蛋白酶突变体的所有第一代突变体通过一至三个氨基酸取代基与之不同，每个蛋白酶突变体作为具有逆转录酶的多聚蛋白的一部分产生; （b）通过测定逆转录酶的活性来分离耐药性，生物活性的突变型蛋白酶; 和（c）鉴定导致如此分离的活性突变蛋白酶的耐药性的不同氨基酸变化。 一种用于评估药物对生物活性突变体或野生型形式的HIV蛋白酶的功效的体外方法，包括将药物和突变体多蛋白（包括无活性的HIV蛋白酶，HIV逆转录酶和一个或多个蛋白酶切割位点） ，添加生物活性突变体或野生型蛋白酶，测定活性逆转录酶的释放，由此逆转录酶活性表明该药物对于所测试的HIV蛋白的突变体或野生型形式是无效的。

    ANTIPYRETIC AND ANALGESIC METHODS AND COMPOSITIONS CONTAINING OPTICALLY PURE R-KETOROLAC
    12.
    发明申请
    ANTIPYRETIC AND ANALGESIC METHODS AND COMPOSITIONS CONTAINING OPTICALLY PURE R-KETOROLAC 审中-公开
    含有光学纯度的R-KETOROLAC的抗菌和分解方法及组合物

    公开(公告)号：WO1994013283A1

    公开(公告)日：1994-06-23

    申请号：PCT/US1993012299

    申请日：1993-12-17

    Applicant: SEPRACOR INC.

    Inventor： SEPRACOR INC. ,  BARBERICH, Timothy, J. ,  MATSON, Stephen, L.

    IPC: A61K31/40

    CPC classification number: A61K31/40

    Abstract: A pharmaceutical composition comprising R-ketorolac, substantially free of the S stereoisomer, for use in an analgesic or antipyretic treatment which does not induce significant adverse side effects associated with the administration of racemic ketorolac, comprising administering a therapeutically effective amount of R-ketorolac to a human patient.

    Abstract translation: 一种药物组合物，其包含基本上不含S立体异构体的R-酮咯酸，用于镇痛或解热治疗，其不引起与外消旋酮咯酸相关的显着不良副作用，包括给予治疗有效量的R-酮咯酸 一个人的病人。

    OPTICALLY PURE R(-) ALBUTEROL FOR TREATING ASTHMA
    14.
    发明申请
    OPTICALLY PURE R(-) ALBUTEROL FOR TREATING ASTHMA 审中-公开
    光学纯度R（ - ）阿尔伯特尔治疗哮喘

    公开(公告)号：WO1991009596A1

    公开(公告)日：1991-07-11

    申请号：PCT/US1991000088

    申请日：1991-01-04

    Applicant: SEPRACOR INC.

    Inventor： SEPRACOR INC. ,  BARBERICH, Timothy, J. ,  YOUNG, James, W.

    IPC: A61K31/135

    CPC classification number: A61K31/135

    Abstract: The optically pure R(-) isomer of albuterol, which is substantially free of the S(+) isomer, is a potent bronchodilator for relieving the symptoms associated with asthma in individuals. A method is disclosed utilizing the optically pure R(-) isomer of albuterol for treating asthma while minimizing the side effects associated with albuterol.

    Abstract translation: 基本上不含S（+）异构体的沙丁胺醇的光学纯的R（ - ）异构体是用于缓解个体哮喘相关症状的有效支气管扩张剂。 公开了利用沙丁胺醇的光学纯的R（ - ）异构体治疗哮喘，同时最小化与沙丁胺醇相关的副作用的方法。

    USE OF CIS-HYDROXYITRACONAZOLE IN ORDER TO AVOID SIDE-EFFECTS OF ITRACONAZOLE AND HYDROXYINTRACONAZOLE
    15.
    发明申请
    USE OF CIS-HYDROXYITRACONAZOLE IN ORDER TO AVOID SIDE-EFFECTS OF ITRACONAZOLE AND HYDROXYINTRACONAZOLE 审中-公开
    使用CIS-羟基噻唑酮避免亚硝酸和羟基吡咯并唑的副作用

    公开(公告)号：WO1998020876A1

    公开(公告)日：1998-05-22

    申请号：PCT/US1997020290

    申请日：1997-11-11

    Applicant: SEPRACOR INC.

    Inventor： SEPRACOR INC. ,  MCCULLOUGH, John, R. ,  KOCH, Patrick

    IPC: A61K31/495

    CPC classification number: A61K31/496

    Abstract: The invention involves prophylactic methods and methods of treatment using cis-hydroxyitraconazole, a metabolic derivative of cis-itraconazole, for the treatment or prevention of microbial, particularly fungal infection and other disorders, while avoiding the concomitant liability of adverse side effects associated with the administration of cis-itraconazole. Methods of treating or preventing such infections in the brain and other areas of CNS are also disclosed.

    Abstract translation: 本发明涉及使用顺式 - 羟基特他康唑（顺式伊曲康唑的代谢衍生物）治疗或预防微生物，特别是真菌感染和其他疾病的预防方法和治疗方法，同时避免与给药相关的副作用的伴随的责任 的顺式伊曲康唑。 还公开了在CNS的大脑和其他区域中治疗或预防这种感染的方法。

    METHODS FOR TREATING EMESIS AND CENTRAL NERVOUS SYSTEM DISORDERS USING OPTICALLY PURE (+) NORCISAPRIDE
    16.
    发明申请
    METHODS FOR TREATING EMESIS AND CENTRAL NERVOUS SYSTEM DISORDERS USING OPTICALLY PURE (+) NORCISAPRIDE 审中-公开
    使用光学纯净（+）NORCISAPRIDE治疗EMESIS和中枢神经系统疾病的方法

    公开(公告)号：WO1998003173A1

    公开(公告)日：1998-01-29

    申请号：PCT/US1997011629

    申请日：1997-07-02

    Applicant: SEPRACOR INC.

    Inventor： SEPRACOR INC. ,  McCULLOUGH, John, R. ,  JERUSSI, Thomas, P.

    IPC: A61K31/445

    CPC classification number: A61K31/4468 ,  A61K31/495 ,  A61K31/445 ,  A61K2300/00

    Abstract: Compositions employing and methods utilizing the optically pure (+) isomer of norcisapride are disclosed. This compound has surprisingly been found to be a potent drug for the treatment of disorders of the central nervous system. The compound, (+) norcisapride, has also been found to be a potent antiemetic agent. Finally, the (+) isomer of norcisapride also avoids certain adverse side effects and certain adverse drug interactions.

    Abstract translation: 公开了使用和使用旋光纯（+）异构体的诺西沙必利的方法的组合物。 令人惊讶地发现，该化合物是用于治疗中枢神经系统疾病的有效药物。 化合物（+）诺西沙必利还被发现是一种有效的止吐剂。 最后，诺西沙必利的（+）异构体也避免了某些不良副作用和某些不良药物相互作用。

    METHODS OF USING (+) CISAPRIDE FOR THE TREATMENT OF GASTRO-ESOPHAGEAL REFLUX DISEASE AND OTHER DISORDERS
    18.
    发明申请
    METHODS OF USING (+) CISAPRIDE FOR THE TREATMENT OF GASTRO-ESOPHAGEAL REFLUX DISEASE AND OTHER DISORDERS 审中-公开
    使用（+）CISAPRIDE治疗胃食管反流病和其他疾病的方法

    公开(公告)号：WO1994001111A1

    公开(公告)日：1994-01-20

    申请号：PCT/US1993006378

    申请日：1993-07-06

    Applicant: SEPRACOR INC.

    Inventor： SEPRACOR INC. ,  GRAY, Nancy, M. ,  YOUNG, James, W.

    IPC: A61K31/445

    CPC classification number: A61K31/445 ,  A61K31/4468

    Abstract: Methods are disclosed utilizing the optically pure (+) isomer of cisapride. This compound is a potent drug for the treatment of gastro-esophageal reflux disease while avoiding the concomitant liability of adverse effects associated with the racemic mixture of cisapride. This compound is also useful in treating or preventing emesis while avoiding the adverse effects associated with racemic cisapride. The optically pure (+) isomer of cisapride is also useful for the treatment of dyspepsia and such other conditions as may be related to the activity of (+) cisapride as a prokinetic agent such as gastroparesis, constipation, post-operative ileus, and intestinal pseudo-obstruction without the concomitant liability of adverse effects associated with the racemic mixture of cisapride. The (+) isomer of cisapride has been found to exhibit higher bioavailability over the racemic cisapride.

    Abstract translation: 公开利用西沙必利的光学纯（+）异构体的方法。 该化合物是用于治疗胃食管反流疾病的有效药物，同时避免与西沙必利的外消旋混合物相关的副作用的伴随的责任。 该化合物也可用于治疗或预防呕吐，同时避免与外消旋西沙必利有关的不良反应。 西沙必利的光学纯（+）异构体也可用于治疗消化不良和其他可能与（+）西沙必利作为促动力剂如胃轻瘫，便秘，手术后肠梗阻和肠道的活性相关的其他病症 假性梗阻与西沙必利的外消旋混合物相关的副作用没有伴随的责任。 已经发现西沙必利的（+）异构体在外消旋西沙必利素上表现出较高的生物利用度。

    PASSIVATED AND STABILIZED POROUS SUPPORTS AND METHODS FOR THE PREPARATION AND USE OF SAME
    19.
    发明申请
    PASSIVATED AND STABILIZED POROUS SUPPORTS AND METHODS FOR THE PREPARATION AND USE OF SAME 审中-公开
    经过钝化和稳定的多孔支持物及其制备和使用方法

    公开(公告)号：WO1994000214A1

    公开(公告)日：1994-01-06

    申请号：PCT/US1993005793

    申请日：1993-06-18

    Applicant: SEPRACOR INC.

    Inventor： SEPRACOR INC. ,  GIROT, Pierre ,  BOSCHETTI, Egisto

    IPC: B01D15/08

    CPC classification number: B01D15/20 ,  B01D15/3804 ,  B01J20/103 ,  B01J20/28004 ,  B01J20/28057 ,  B01J20/28069 ,  B01J20/28078 ,  B01J20/288 ,  B01J20/3204 ,  B01J20/321 ,  B01J20/327 ,  B01J20/3289 ,  B01J39/17 ,  B01J39/26 ,  B01J41/20 ,  B01J2220/54 ,  B01J2220/58

    Abstract: This invention relates generally to modified porous solid supports and processes for the preparation and use of same. In particular, passivated porous mineral oxide, polymeric, or polymer-coated mineral oxide supports are disclosed which are characterized by a reversible high sorptive capacity substantially unaccompanied by non-specific adsorption of or interaction with biomolecules. Passivation is achieved by use of a passivation mixture comprising a main monomer, a passivating monomer and a crosslinking agent, which mixture upon polymerization results in the substantial elimination of the undesirable non-specific interaction with biomolecules.

    Abstract translation: 本发明一般涉及改性的多孔固体载体及其制备和使用方法。 特别地，公开了钝化的多孔矿物氧化物，聚合物或聚合物涂覆的矿物氧化物载体，其特征在于基本上不伴随生物分子的非特异性吸附或相互作用的可逆的高吸附能力。 通过使用包含主单体，钝化单体和交联剂的钝化混合物实现钝化，该聚合物上的该混合物导致基本上消除了与生物分子的不期望的非特异性相互作用。

Patent Agency Ranking