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262 条记录 (耗时 0.054 秒)

    Method of treatment or prophylaxis
    91.
    发明申请
    Method of treatment or prophylaxis 审中-公开
    治疗或预防的方法

    公开(公告)号：US20010029262A1

    公开(公告)日：2001-10-11

    申请号：US09879462

    申请日：2001-06-12

    发明人： Kapil Dev Sethi

    IPC分类号： A61K031/404

    CPC分类号： A61K31/4045

    摘要： The present invention provides a method of treating Restless Legs Syndrome in human or animal patient, which method comprises administering to said patient an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof. Preferably, a dose of ropinirole or a pharmaceutically acceptable salt or solvate thereof is administered to the patient 1 to 3 hours before the patient goes to bed. A typical dose comprises 0.1 mg-5 mg of ropinirole. The invention also provides a pharmaceutical composition for use in the treatment of Restless Legs Syndrome which comprises an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier.

    摘要翻译： 本发明提供了一种在人或动物患者中治疗不宁腿综合征的方法，该方法包括向所述患者施用有效量的罗匹尼罗或其药学上可接受的盐或溶剂合物。 优选地，在患者睡觉前1-3小时向患者施用罗匹尼罗或其药学上可接受的盐或溶剂化物的剂量。 典型剂量包含0.1mg-5mg罗匹尼罗。 本发明还提供了一种用于治疗不宁腿综合征的药物组合物，其包含有效量的罗匹尼罗或其药学上可接受的盐或溶剂化物和药学上可接受的载体。

    Structural carotenoid analogs for the inhibition and amelioration of disease
    93.
    发明申请
    Structural carotenoid analogs for the inhibition and amelioration of disease 有权
    结构类胡萝卜素类似物用于抑制和改善疾病

    公开(公告)号：US20040162329A1

    公开(公告)日：2004-08-19

    申请号：US10629538

    申请日：2003-07-29

    发明人： Samuel Fournier Lockwood ,  Sean O'Malley ,  David G. Watumull ,  Laura M. Hix ,  Henry Jackson ,  Geoff Nadolski

    IPC分类号： A61K031/66 ,  A61K031/4172 ,  A61K031/404 ,  A61K031/401 ,  A61K031/325

    CPC分类号： C07C403/24 ,  C07D207/16 ,  C07D265/30 ,  C07D307/58 ,  C07F9/117 ,  C07H13/04

    摘要： A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid structural analog, either alone or in combination with another carotenoid analog, or co-antioxidant formulation. The analog or analog combination is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of ischemia-reperfusion injury. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of liver disease. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of cancer. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of cardiac arrhythmia and/or sudden cardiac death. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of any disease that involves production of reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals. In one embodiment, a water-soluble and/or water-dispersible astaxanthin analog is particularly effective. This invention further includes pharmaceutical compositions comprising structural carotenoid analogs either alone or in combination.

    摘要翻译： 用于抑制和/或改善与受试者相关的疾病的发生的方法，其中受试者单独或与另一种类胡萝卜素组合施用类胡萝卜素结构类似物，受试者中的活性氧，活性氮物质，自由基和/或非自由基 类似物或辅助抗氧化剂制剂。 给予类似物或模拟组合，使得受试者可能因此减少与活性氧，活性氮物质，自由基和/或非自由基相关的疾病的风险。 模拟或模拟组合可以施用于受试者以抑制和/或改善缺血再灌注损伤。 可以将受试者的类似物或类似物组合施用于肝脏疾病的抑制和/或改善。 类似物或类似物组合可以施用于受试者以抑制和/或改善癌症。 模拟或模拟组合可以施用于受试者以抑制和/或改善心律失常和/或心脏猝死。 类似物或模拟组合可以施用于受试者以抑制和/或改善涉及产生活性氧，活性氮物质，自由基和/或非自由基的任何疾病。 在一个实施方案中，水溶性和/或水分散性虾青素类似物是特别有效的。 本发明还包括单独或组合包含结构类胡萝卜素类似物的药物组合物。

    Indolone derivatives having vascular damaging activity
    95.
    发明申请
    Indolone derivatives having vascular damaging activity 失效
    吲哚酮衍生物具有血管损伤活性

    公开(公告)号：US20040147589A1

    公开(公告)日：2004-07-29

    申请号：US10469834

    申请日：2004-01-16

    发明人： Jean-Claude Arnould

    IPC分类号： A61K031/404

    CPC分类号： C07D209/34 ,  A61K31/404

    摘要： This invention relates to the use of compounds of Formula (I) as vascular damaging agents: wherein X is selected from: nullOnull, nullSnull, nullS(O)null, nullS(O2)null, nullN(R5)null, nullC(O)null, nullC(O)N(R5)null, nullN(R5)C(O)null, nullS(O2)N(R5)null, or nullN(R5)S(O2)null; R1 is independently selected from: amino, halo, hydroxy, nullOPO3H2, C1-4alkyl, or C1-4alkoxy, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified; R2 is selected from: hydrogen or C1-4alkyl; R3 is selected from: hydrogen, halo, hydroxy, hydroxyC1-4alkyl, cyano, cyanoC1-4alkyl, carboxy, carboxyC1-4alkyl, C1-4alkanoyl, C1-4alkanoylC1-4alkyl, carbamoyl, carbamoylC1-4alkyl, C1-4alkoxy, C1-4alkoxycarbonyl, C1-4alkoxycarbonylC1-4alkyl, C1-4alkoxycarbonylamino, amino, N-C1-4alkylamino, NN-diC1-4alkylamino, aminoC1-4alkyl, N-C1-4alkylaminoC1-4alkyl, NN-diC1-4alkylaminoC1-4alkyl, ureido, or C1-4alkylureyleno; R4 is independently selected from: C1-4alkyl, C1-4alkoxy or halo; R5 is selected from: hydrogen or C1-4alkyl; n is 0 or 1; p is 0, 1, 2 or 3; and q is 0, 1 or 2; or a salt, pro-drug or solvate thereof. The invention also relates to novel compounds of Formula (I) and to processes for the preparation of compounds of Formula (I). 1

    摘要翻译： 本发明涉及式（I）化合物作为血管损伤剂的用途：其中X选自：-O - ， - S - ， - S（O） - ， - S（O 2） - ， - N（R 5 ） - ， - C（O） - ， - C（O）N（R5） - ， - N（R5）C（O） - ， - S（O2）N（R5） - 或-N （O 2） - ; R 1独立地选自：氨基，卤素，羟基，-OPO 3 H 2，C 1-4烷基或C 1-4烷氧基，其中氨基任选被氨基酸残基取代，羟基任选被酯化; R2选自：氢或C 1-4烷基; R 3选自：氢，卤素，羟基，羟基C 1-4烷基，氰基，氰基C 1-4烷基，羧基，羧基C 1-4烷基，C 1-4烷酰基，C 1-4烷酰基C 1-4烷基，氨基甲酰基，氨基甲酰基C 1-4烷基，C 1-4烷氧基，C 1-4烷氧基羰基 ，C 1-4烷氧基羰基C 1-4烷基，C 1-4烷氧基羰基氨基，氨基，N-C 1-4烷基氨基，NN-二C 1-4烷基氨基，氨基C 1-4烷基，N-C 1-4烷基氨基C 1-4烷基，NN-二C 1-4烷基氨基C 1-4烷基， 4-烷基脲基 R 4独立地选自：C 1-4烷基，C 1-4烷氧基或卤素; R5选自：氢或C 1-4烷基; n为0或1; p为0,1,2或3; q为0,1或2; 或其盐，前药或溶剂化物。 本发明还涉及新的式（I）化合物和制备式（I）化合物的方法。

    Indolinone derivatives as protein kinase/phosphatase inhibitors
    96.
    发明申请
    Indolinone derivatives as protein kinase/phosphatase inhibitors 失效
    吲哚啉酮衍生物作为蛋白激酶/磷酸酶抑制剂

    公开(公告)号：US20040147586A1

    公开(公告)日：2004-07-29

    申请号：US10725277

    申请日：2003-12-02

    申请人： Sugen, Inc.

    发明人： Peng Cho Tang ,  G. Davis Harris ,  Xiaoyuan Li

    IPC分类号： A61K031/404 ,  C07D43/02

    CPC分类号： C07D401/14 ,  C07D209/34 ,  C07D403/14

    摘要： The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (nullPKsnull) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

    Methods of treating age associated memory impairment (AAMI), mild cognitive impairment (MCI), and dementias with cell cycle inhibitors
    97.
    发明申请
    Methods of treating age associated memory impairment (AAMI), mild cognitive impairment (MCI), and dementias with cell cycle inhibitors 审中-公开
    治疗年龄相关记忆障碍（AAMI），轻度认知障碍（MCI）和痴呆与细胞周期抑制剂的方法

    公开(公告)号：US20040127471A1

    公开(公告)日：2004-07-01

    申请号：US10664817

    申请日：2003-09-17

    发明人： Barry Reisberg

    IPC分类号： A61K031/65 ,  A61K031/60 ,  A61K031/404 ,  A61K031/353 ,  A61K031/19

    CPC分类号： A61K31/19 ,  A61K31/52 ,  A61K31/60 ,  A61K31/65 ,  A61K31/70

    摘要： Therapeutic methods for treatment of age associated memory impairment (AAMI), mild cognitive impairment (MCI), Alzheimer's disease (AD), cerebrovascular dementia (CVD), and related neurodegenerative conditions by administering an agent capable of inhibiting cell cycle progression, comprising administering one or more agents that are capable of inhibiting neuronal cell cycle progression at either an early cell cycle phase or generally, either alone or in combination with one or more agents capable of reducing mitogenic stimulation.

    摘要翻译： 通过施用能够抑制细胞周期进程的药物治疗年龄相关记忆障碍（AAMI），轻度认知障碍（MCI），阿尔茨海默病（AD），脑血管性痴呆（CVD）和相关神经变性病症的治疗方法，包括给予一种 或更多的能够在早期细胞周期阶段或通常单独或与一种或多种能够减少有丝分裂刺激的试剂组合的神经元细胞周期进程的试剂。

    GAL3 receptor antagonists for the treatment of affective disorders
    98.
    发明申请
    GAL3 receptor antagonists for the treatment of affective disorders 审中-公开
    GAL3受体拮抗剂用于治疗情感障碍

    公开(公告)号：US20040110821A1

    公开(公告)日：2004-06-10

    申请号：US10638242

    申请日：2003-08-07

    发明人： Michael J. Konkel ,  Thomas P. Blackburn ,  John M. Wetzel

    IPC分类号： A61K031/407 ,  A61K031/404

    CPC分类号： A61K31/407 ,  A61K31/404

    摘要： This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. This invention provides a method of treating a subject suffering from an affective disorder which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's affective disorder. This invention also provides a method of treating an affective disorder in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.

    摘要翻译： 本发明涉及作为GAL3受体的选择性拮抗剂的嘧啶和吲哚酮衍生物。 本发明提供了一种治疗患有情感障碍的受试者的方法，其包括给予受试者一定量的有效治疗受试者情感障碍的本发明化合物。 本发明还提供了治疗受试者的情感障碍的方法，其包括向受试者施用包含药学上可接受的载体和治疗有效量的GAL3受体拮抗剂的组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。

    Oxindoles which are inhibitors of CDK-1 and their application in therapeutics
    99.
    发明申请
    Oxindoles which are inhibitors of CDK-1 and their application in therapeutics 审中-公开
    作为CDK-1抑制剂的Oxindoles及其在治疗中的应用

    公开(公告)号：US20040110770A1

    公开(公告)日：2004-06-10

    申请号：US10644411

    申请日：2003-08-20

    申请人： AVENTIS PHARMA SA

    发明人： Jean-Francois Riou ,  Michel Maratrat ,  Lucile Grondard ,  Fabienne Thompson ,  Odile Petitgenet ,  Patrick Mailliet ,  Jacques Lavayre

    IPC分类号： A61K031/506 ,  A61K031/4439 ,  A61K031/4178 ,  A61K031/404 ,  C07D43/02

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D409/14

    摘要： The present invention relates to a compound of formula (I): 1 wherein R5 is selected from the group consisting of 3-pyridyl, 5-pyrimidinyl, nullCONHnull(C1-C4 alkyl), nullNHCOnull(C1-C4 alkyl), halogen, nullSO2NH2, nullNO2, nullCF3 or thien-2-ylcarbonyl 2 nulland nullCO2R where R can be hydrogen or C1-C4 alkyl; and Ar is selected from the group consisting of 5-imidazolyl, 2-pyrrolyl optionally substituted by a C1-C4 alkyl radical, 2-furyl or 2-thiazolyl, in the E or Z geometrical isomeric form or a mixture of the two geometrical isomeric forms. The invention is also directed to a method of treating primary and secondary tumours in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a compound of formula I. The invention is also directed to a method of using a compound of formula I to treat cancer, inhibit the proliferation of a cell and induce cell apoptosis, comprising contacting a cell with an effective amount of the compound of formula I., The invention is also directed to a method of preparing the compound of formula I.

    摘要翻译： 本发明涉及式（I）化合物：其中R5选自3-吡啶基，5-嘧啶基，-CONH-（C1-C4烷基），-NHCO-（C1-C4烷基）， 卤素，-SO 2 NH 2，-NO 2，-CF 3或噻吩-2-基羰基和-CO 2 R，其中R可以是氢或C 1 -C 4烷基; 并且Ar选自5-取代的咪唑基，任意被C1-C4烷基取代的2-吡咯基，2-呋喃基或2-噻唑基，E或Z几何异构形式或两个几何异构体的混合物 形式。 本发明还涉及在有需要的患者中治疗原发性和继发性肿瘤的方法，其包括向患者施用治疗有效量的式I化合物。本发明还涉及使用式 I治疗癌症，抑制细胞的增殖并诱导细胞凋亡，包括使细胞与有效量的式I化合物接触。本发明还涉及制备式I化合物的方法。