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    COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING HEARING IMPAIRMENT
    1.
    发明申请
    COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING HEARING IMPAIRMENT 审中-公开
    用于治疗或预防听觉障碍的组合物和方法

    公开(公告)号：WO2004043447A2

    公开(公告)日：2004-05-27

    申请号：PCT/US2003/036269

    申请日：2003-11-13

    Applicant: SEPRACOR, INC. ,  CURRIE, Mark, G. ,  HEEFNER, Donald, L. ,  RUBIN, Paul ,  ZEPP, Charles, M.

    Inventor： CURRIE, Mark, G. ,  HEEFNER, Donald, L. ,  RUBIN, Paul ,  ZEPP, Charles, M.

    IPC: A61K31/17

    CPC classification number: A61K31/17 ,  A61K31/495

    Abstract: Ototoxic side-effects have either limited the application of an important group of antibiotics, aminoglycoside antibiotics, or have added further burden to those who have to resort to platinum-containing antineoplastic agents to treat life-threatening tumors. The present invention discloses pharmaceutical compositions that prevent or treat the ototoxic side-effects of aminoglycoside antibiotics and platinum-containing antineoplastic agents. The otoprotective compositions disclosed herein can also be used to treat noise induced hearing loss.

    Abstract translation: 耳毒性副作用限制了一组重要的抗生素，氨基糖苷类抗生素的应用，或者为那些不得不使用含铂抗肿瘤剂治疗危及生命的肿瘤的人增加了进一步的负担。 本发明公开了预防或治疗氨基糖苷类抗生素和含铂抗肿瘤剂的耳毒性副作用的药物组合物。 本文公开的保护性组合物也可用于治疗噪声引起的听力损失。

    METHODS FOR TREATING DEPRESSION AND OTHER CNS DISORDERS USING ENANTIOMERICALLY ENRICHED DESMETHYL- AND DIDESMETHYL-METABOLITES OF CITALOPRAM
    4.
    发明申请
    METHODS FOR TREATING DEPRESSION AND OTHER CNS DISORDERS USING ENANTIOMERICALLY ENRICHED DESMETHYL- AND DIDESMETHYL-METABOLITES OF CITALOPRAM 审中-公开
    使用全面加强的对苯二甲酸二甲酯和代谢物代谢物治疗呕吐和其他中枢神经系统疾病的方法

    公开(公告)号：WO2003040121A1

    公开(公告)日：2003-05-15

    申请号：PCT/US2002/035408

    申请日：2002-11-05

    Applicant: SEPRACOR, INC. ,  BUSH, Larry, R. ,  CURRIE, Mark, G. ,  SENANAYAKE, Chris, H. ,  FANG, Kevin, Q.

    Inventor： BUSH, Larry, R. ,  CURRIE, Mark, G. ,  SENANAYAKE, Chris, H. ,  FANG, Kevin, Q.

    IPC: C07D307/87

    CPC classification number: C07D307/87 ,  C07D317/20

    Abstract: This invention relates to novel compositions of matter containing enantiomerically enriched (-)-desmethylcitalopram, (+)-didesmethylcitalopram, or (-)-didesmethylcitalopram or mixtures thereof in optimal ratios. Contrary to prior teachings, the enantiomerically enriched citalopram metabolites disclosed herein possess potent serotonin reuptake inhibitory activity, with minimal inhibitory effects on the reuptake of other known monoamines, e.g., norepinephrine (NE) or dopamine (DA). The present invention also discloses methods for treating disorders, dysfunctions and diseases for which inhibition of serotonin reuptake is therapeutically beneficial. In particular, the present invention discloses a method for treating various forms of depression with pharmaceutical compositions described herein.

    Abstract translation: 本发明涉及以最佳比例含有对映体富集（ - ） - 去甲基西酞普兰，（+） - 二甲基西酞普兰或（ - ） - 二甲基西酞普兰或其混合物的物质的新型组合物。 与现有技术相反，本文公开的对映异构体富集的西酞普兰代谢物具有有效的5-羟色胺再摄取抑制活性，对其他已知的单胺例如去甲肾上腺素（NE）或多巴胺（DA）的再摄取具有最小的抑制作用。 本发明还公开了治疗疾病，功能障碍和5-羟色胺再摄取抑制治疗有益的疾病的方法。 特别地，本发明公开了一种用本文所述的药物组合物治疗各种形式的抑郁症的方法。

    D-AMINO ACID OXIDASE INHIBITORS FOR LEARNING AND MEMORY
    5.
    发明申请
    D-AMINO ACID OXIDASE INHIBITORS FOR LEARNING AND MEMORY 审中-公开
    用于学习和记忆的D-氨基酸氧化酶抑制剂

    公开(公告)号：WO2003039540A2

    公开(公告)日：2003-05-15

    申请号：PCT/US2002/036051

    申请日：2002-11-12

    Applicant: SEPRACOR INC. ,  HEEFNER, Donald, L. ,  CURRIE, Mark, G. ,  ROSSI, JR., Richard, Filip ,  ZEPP, Charles, M.

    Inventor： HEEFNER, Donald, L. ,  CURRIE, Mark, G. ,  ROSSI, JR., Richard, Filip ,  ZEPP, Charles, M.

    IPC: A61K31/405

    CPC classification number: A61K31/34 ,  A61K31/401 ,  A61K31/404 ,  A61K31/405 ,  A61K31/473

    Abstract: Methods and pharmaceutical compositions which inhibit the activity of D-amino acid oxidase (DAO) are disclosed. Inhibition of DAO improves memory, learning and cognition in individuals suffering from neurodegenerative diseases such as Alzheimer's, Huntington's or Parkinson's diseases; the methods and pharmaceutical compositions which inhibit the activity of DAO also improve cognitive dysfunctions associated with aging and improve catatonic schizophrenia. Several genera of heterocycle-2-carboxylic acids are disclosed as DAO inhibitors.

    Abstract translation: 公开了抑制D-氨基酸氧化酶（DAO）活性的方法和药物组合物。 DAO的抑制改善了患有神经退行性疾病如阿尔茨海默病，亨廷顿舞蹈病或帕金森病的个体的记忆，学习和认知; 抑制DAO活性的方法和药物组合物也改善与衰老相关的认知功能障碍并改善紧张性精神分裂症。 作为DAO抑制剂公开了几个杂环-2-羧酸的属。

    METHODS OF PREPARING AND USING 2-HYDROXY DERIVATIVES OF SIBUTRAMINE AND ITS METABOLITES
    6.
    发明申请
    METHODS OF PREPARING AND USING 2-HYDROXY DERIVATIVES OF SIBUTRAMINE AND ITS METABOLITES 审中-公开
    制备和使用西布曲明及其代谢物的2-羟基衍生物的方法

    公开(公告)号：WO2003022259A1

    公开(公告)日：2003-03-20

    申请号：PCT/US2002/029014

    申请日：2002-09-12

    Applicant: SEPRACOR INC.

    Inventor： SENANAYAKE, Chris, H. ,  JERUSSI, Thomas, P. ,  CURRIE, Mark, G. ,  FANG, Qun, K. ,  HSU, Bob

    IPC: A61K31/135

    CPC classification number: C07C215/28 ,  A61K31/135 ,  C07C2601/04

    Abstract: The invention is directed, in part, to racemic and stereomerically pure 2-hydroxy derivatives of sibutramine and its metabolites, and 2-hydroxy derivatives of desmethylsibutramine and didesmethylsibutramine in particular. The invention is further directed to novel methods of preparing these derivatives are also disclosed. The invention is also directed to pharmaceutical compositions and dosage forms that comprise therapeutically or prophylactically effective amounts of the compounds, optionally in combination with an additional pharmacologically active compound. These pharmaceutical compositions and dosage forms can be used in the methods of the invention, which provide for the treatment or prevention of a variety of diseases and disorders.

    Abstract translation: 本发明部分地涉及西布曲明及其代谢物的外消旋和立体异构纯的2-羟基衍生物，特别是脱甲基西布曲明和二甲基西布曲明的2-羟基衍生物。 本发明还涉及新的制备这些衍生物的方法。 本发明还涉及药物组合物和剂型，其包含治疗或预防有效量的化合物，任选与另外的药理活性化合物组合。 这些药物组合物和剂型可用于本发明的方法，其提供治疗或预防各种疾病和病症。

    AMINO ACID AND PEPTIDE-MODIFIED FORMS OF GLUCOCORTICOIDS
    10.
    发明申请
    AMINO ACID AND PEPTIDE-MODIFIED FORMS OF GLUCOCORTICOIDS 审中-公开
    氨基酸和肽修饰形式的葡萄糖苷

    公开(公告)号：WO2003070194A2

    公开(公告)日：2003-08-28

    申请号：PCT/US2003/005204

    申请日：2003-02-20

    Applicant: SEPRACOR INC. ,  CURRIE, Mark, G. ,  GROVER, Paul ,  JONES, Steve ,  SENANAYAKE, Chris, H. ,  NIE, Xiaoyi

    Inventor： CURRIE, Mark, G. ,  GROVER, Paul ,  JONES, Steve ,  SENANAYAKE, Chris, H. ,  NIE, Xiaoyi

    IPC: A61K

    CPC classification number: C07J71/0031 ,  A61K9/0073 ,  C07J41/005 ,  C07J43/003

    Abstract: Amino acid corticosteroid esters which may function as pro-drugs, and formulations of the amino acid corticosteroid esters with a second active ingredient such as formoterol are disclosed. Composition of the invention include amino acid corticosteroid esters of Formula (I) that are used to make solution-stable pharmaceutical compositions or stable co-dispersions of pharmaceutical compositions in an aerosol formulation, or in a manual pump spray formulation containing one or more active ingredients. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

    Abstract translation: 公开了可用作前药的氨基酸皮质类固醇酯，以及具有第二活性成分如福莫特罗的氨基酸皮质类固醇酯的制剂。 本发明的组合物包括式（I）的氨基酸皮质类固醇酯，其用于制备溶液稳定的药物组合物或药物组合物在气溶胶制剂中的稳定共分散体，或在含有一种或多种活性成分的手动泵喷雾制剂中 。 该化合物可用于治疗鼻炎和哮喘，特别是通过吸入治疗和治疗炎症，特别是通过局部或局部给药治疗炎症。

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