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    Combination
    1.
    发明申请
    Combination 审中-公开
    组合

    公开(公告)号：US20040242597A1

    公开(公告)日：2004-12-02

    申请号：US10489920

    申请日：2004-03-18

    发明人： Thomas Klein ,  Hans-Peter Kley

    IPC分类号： A61K031/522 ,  A61K031/513 ,  A61K031/4709

    CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K2300/00

    摘要： The invention relates to the combined administration of PDE4-inhibitors and NSAIDs for the treatment of an inflammatory disease and/or an inflammation associated disorder while minimizing gastrointesti-nal side effects, such as gastric erosions and ulcer, which are frequently associated with the use of NSAIDs.

    摘要翻译： 本发明涉及用于治疗炎性疾病和/或炎症相关疾病的PDE4抑制剂和NSAID的组合给药，同时最小化胃肠道侵蚀和溃疡的胃肠道副作用，其通常与使用 NSAIDs。

    Methods of treating patients suffering from movement disorders
    3.
    发明申请
    Methods of treating patients suffering from movement disorders 审中-公开
    治疗运动障碍患者的方法

    公开(公告)号：US20040198753A1

    公开(公告)日：2004-10-07

    申请号：US10353240

    申请日：2003-01-28

    发明人： Hiroshi Kase ,  Akihisa Mori ,  Yutaka Waki ,  Yutaka Ohsawa ,  Akira Karasawa ,  Yoshihisa Kuwana

    IPC分类号： A61K031/522

    CPC分类号： A61K31/522 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/48 ,  A61K31/198 ,  A61K45/06

    摘要： The present invention is directed to methods of treating movement disorders by administering an effective amount of one or more adenosine A2A receptor antagonists to a patient in need thereof. The present invention also provides methods of decreasing the adverse effects of L-DOPA in patients receiving L-DOPA therapy in the treatment of Parkinson's disease. The present invention further provides methods and compositions for treating Parkinson's disease patients with sub-clinically effective doses of L-DOPA by combining L-DOPA treatment with an effective amount of one or more adenosine A2A receptor antagonists (i.e., L-DOPA sparing effect). The present invention further provides methods of effective treatment of Parkinson's disease by co-administering at least one adenosine A2A receptor antagonist, L-DOPA and a dopamine agonist and/or a COMT inhibitor and/or a MAO inhibitor. The present invention further provides methods of prolonging effective treatment of Parkinson's disease by administering an adenosine A2A receptor antagonist singly or together with a dopamine agonist, and/or a COMT inhibitor, and/or a MAO inhibitor without prior or subsequent administration of L-DOPA, delaying or removing on-set of L-DOPA motor complication.

    摘要翻译： 本发明涉及通过向有需要的患者施用有效量的一种或多种腺苷A 2A受体拮抗剂来治疗运动障碍的方法。 本发明还提供降低L-DOPA在接受L-DOPA治疗的帕金森病治疗中的不良反应的方法。 本发明进一步提供了通过将L-DOPA治疗与有效量的一种或多种腺苷A 2A受体拮抗剂组合（即L-DOPA备用效应）来治疗具有亚临床有效剂量的L-DOPA的帕金森病患者的方法和组合物， 。 本发明还提供了通过共同施用至少一种腺苷A 2A受体拮抗剂，L-DOPA和多巴胺激动剂和/或COMT抑制剂和/或MAO抑制剂来有效治疗帕金森病的方法。 本发明还提供了延长帕金森病有效治疗的方法，通过单独或与多巴胺激动剂和/或COMT抑制剂和/或MAO抑制剂一起施用腺苷A2A受体拮抗剂，而无需先前或随后给予L-DOPA ，延迟或消除L-DOPA电机并发症。

    Marker
    4.
    发明申请
    Marker 审中-公开
    标记

    公开(公告)号：US20040186117A1

    公开(公告)日：2004-09-23

    申请号：US10632567

    申请日：2003-07-31

    发明人： Paul Workman ,  Steven R. Whittaker

    IPC分类号： A61K031/522

    CPC分类号： G01N33/502 ,  G01N33/5008 ,  G01N33/5011 ,  G01N33/5044 ,  G01N33/5047 ,  G01N33/5088

    摘要： The present invention relates to a pharmacodynamic marker for the candidate 2,6,9-tri-substituted purine known as roscovitine. The identity of this marker facilitates the convenient identification of roscovitine activity both in vitro and in vivo.

    摘要翻译： 本发明涉及称为roscovitine的候选2,6,9-三取代嘌呤的药效学标记。 该标记的身份有助于在体外和体内方便地鉴定roscovitine活性。

    Method for producing mixed crystal of disodium 5'-guanylate and disodium 5'-inosinate
    5.
    发明申请
    Method for producing mixed crystal of disodium 5'-guanylate and disodium 5'-inosinate 有权
    5'-鸟苷酸二钠和5'-肌苷酸二钠混合晶的方法

    公开(公告)号：US20040180909A1

    公开(公告)日：2004-09-16

    申请号：US10481893

    申请日：2004-01-05

    发明人： Toyokazu Kaneko ,  Yasuo Yonou ,  Naoto Hirano ,  Shigematsu Abe ,  Kunihiko Toumori

    IPC分类号： A61K031/522 ,  C07D473/02

    CPC分类号： C07H1/00 ,  C07H19/20

    摘要： Disclosed herein are a process for producing mixed crystals of disodium 5null-guanylate and disodium 5null-inosinate which comprises precipitating mixed crystals of disodium 5null-guanylate and disodium 5null-inosinate (InullG mixed crystals) by adding an aqueous mixed solution of disodium 5null-guanylate and disodium 5null-inosinate and a hydrophilic organic solvent at the same time into a crystallization vessel in such manner that the ratio of the hydrophilic organic solvent to the liquid phase in the crystallization vessel is maintained in a range of 30 to 70 vol %, as well as such process for producing InullG mixed crystals wherein said producing of InullG mixed crystals is carried out by seeding crystallization wherein crystals of 5null-IMP2Na or/and InullG mixed crystals are used as seed crystals. According to these production processes, the by-production of amorphous solids of 5null-GMP2Na which adversely affect separability of the crystals concerned, is inhibited, and therefore, such mixed crystals having a good separability without contamination of such amorphous solids, can be produced in a high productivity.

    摘要翻译： 本文公开了一种生产5'-鸟苷酸二钠和5'-肌苷酸二钠的混合晶体的方法，该方法包括通过加入含水混合物来沉淀5'-鸟苷酸二钠和5'-肌苷酸二钠（I + G混合晶体）的混合物 5'-鸟苷酸二钠和5'-肌苷酸二钠和亲水性有机溶剂的溶液同时放入结晶容器中，使得结晶容器中的亲水性有机溶剂与液相的比率保持在一定范围内 为30〜70体积％，以及这种I + G混合晶体的制造方法，其中所述I + G混晶的制造是通过晶种结晶进行的，其中5'-IMP2Na或/和I + G混合晶体的晶体为 用作晶种。 根据这些制造方法，抑制了对相关晶体的分离性有不利影响的5-GMP2Na的无定形固体的副产物，因此可以制备这种具有良好分离性而不会污染这种无定形固体的混合晶体 在高生产率。

    Compositions and methods for targeting cerebral circulation and treatment of headache
    6.
    发明申请
    Compositions and methods for targeting cerebral circulation and treatment of headache 有权
    用于靶向脑循环和头痛治疗的组合物和方法

    公开(公告)号：US20040171625A1

    公开(公告)日：2004-09-02

    申请号：US10483509

    申请日：2004-01-12

    发明人： Bruce Frome

    IPC分类号： A61K031/522 ,  A61K009/70

    CPC分类号： A61K47/10 ,  A61K9/0014 ,  A61K31/522 ,  A61K47/12 ,  A61K47/14 ,  A61K47/24

    摘要： Methods and compositions for targeting cerebral circulation and treatment of headache include formulations comprising a pharmacologically active substance in a transdermal formulation, which is topically applied to an area of skin superficial to a carotid artery, a temporal artery, a vertebral artery, or to a tender spot associated with a headache. Particularly preferred formulations include a xanthine derivative (e.g., theophylline, caffeine, aminophylline), and may further comprise ketoprofen. Contemplated methods further include methods of advertising use of contemplated compositions.

    摘要翻译： 用于靶向脑循环和头痛治疗的方法和组合物包括在透皮制剂中包含药理活性物质的制剂，其局部施用于颈动脉浅表的皮肤区域，颞动脉，椎动脉或嫩 斑点与头痛相关。 特别优选的制剂包括黄嘌呤衍生物（例如茶碱，咖啡因，氨茶碱），并且还可以包含酮洛芬。 考虑的方法还包括广泛使用预期组合物的方法。

    Combination therapy for the treatment of acute leukemia and myelodysplastic syndrome
    7.
    发明申请
    Combination therapy for the treatment of acute leukemia and myelodysplastic syndrome 审中-公开
    联合治疗急性白血病和骨髓增生异常综合征

    公开(公告)号：US20040152632A1

    公开(公告)日：2004-08-05

    申请号：US10700650

    申请日：2003-11-04

    申请人： Wyeth

    发明人： Jay Marshall Feingold

    IPC分类号： A61K038/17 ,  A61K031/704 ,  A61K031/7076 ,  A61K031/7072 ,  A61K031/513 ,  A61K031/522

    CPC分类号： A61K31/513 ,  A61K31/522 ,  A61K31/704 ,  A61K31/7072 ,  A61K31/7076 ,  A61K47/6803 ,  A61K47/6849 ,  A61K2300/00

    摘要： Methods of treatment and pharmaceutical combinations are provided for the treatment of acute leukemia, such as acute myelogenous leukemia, and myelodysplastic syndrome. The methods of treatment and pharmaceutical combinations employ an anti-CD33 cytotoxic conjugate in combination with at least one compound selected from the group consisting of an anthracycline and a pyrimidine or purine nucleoside analog. Preferred methods of treatment and pharmaceutical combinations employ gemtuzumab ozogamicin, daunorubicin, and cytarabine.

    摘要翻译： 提供治疗方法和药物组合用于治疗急性白血病，如急性骨髓性白血病和骨髓增生异常综合征。 治疗和药物组合的方法使用抗CD33细胞毒性缀合物与至少一种选自蒽环类和嘧啶或嘌呤核苷类似物的化合物组合。 优选的治疗方法和药物组合使用吉妥珠单抗奥佐霉素，柔红霉素和阿糖胞苷。

    Topical composition and method for treating occlusive wounds
    8.
    发明申请
    Topical composition and method for treating occlusive wounds 审中-公开
    用于治疗闭合性创伤的局部组合物和方法

    公开(公告)号：US20040147534A1

    公开(公告)日：2004-07-29

    申请号：US10350200

    申请日：2003-01-23

    发明人： Mary Ann Foote ,  Mark Harlan Mandel

    IPC分类号： A61K031/522 ,  A61K031/455

    CPC分类号： A61K31/522 ,  A61K9/0014 ,  A61K31/455 ,  A61K45/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/24 ,  A61K47/36

    摘要： The present invention provides a topical composition comprising about 6% to about 15% nifedipine and about 6% to about 15% pentoxifylline for treating severe vascular occlusive wounds. The present invention also provides a method and a kit for treating the vascular occlusive wound by applying the composition to the open wound, and cleaning and dressing the wound at least once daily.

    摘要翻译： 本发明提供了包含约6％至约15％硝苯吡啶和约6％至约15％己酮可可碱用于治疗严重血管闭塞性创伤的局部组合物。 本发明还提供了一种用于通过将组合物施用于开放性伤口来治疗血管闭塞性伤口并且每天至少清洁和敷裹伤口的方法和试剂盒。

    Use of an adenosine a3 receptor agonist for inhibition of viral replication
    9.
    发明申请
    Use of an adenosine a3 receptor agonist for inhibition of viral replication 有权
    使用腺苷a3受体激动剂抑制病毒复制

    公开(公告)号：US20040106572A1

    公开(公告)日：2004-06-03

    申请号：US10466263

    申请日：2004-01-15

    发明人： Pnina Fishman ,  Kamel Khalili

    IPC分类号： A61K031/7076 ,  A61K031/52 ,  A61K031/522

    CPC分类号： A61K31/00 ,  A61K31/52 ,  A61K31/522 ,  A61K31/7076

    摘要： The present invention concerns the use of an active ingredient selected from the group consisting of agonists of the adenosine receptor system, for inhibiting viral replication in cells. In particular, the invention provides a composition and method for inhibiting viral replication in cells, the method comprising presenting to the cells an effective amount of the active ingredient. According to one embodiment, the adenosine agonist is an A3 receptor agonist (A3RAg). The invention is particularly useful, for although not limited to, inhibiting the replication of HIV virus in human cells.

    摘要翻译： 本发明涉及使用选自腺苷受体系统的激动剂的活性成分，用于抑制细胞中的病毒复制。 特别地，本发明提供了抑制细胞中病毒复制的组合物和方法，所述方法包括向细胞呈递有效量的活性成分。 根据一个实施方案，腺苷激动剂是A3受体激动剂（A3RAg）。 本发明特别有用，因为虽然不限于抑制HIV病毒在人细胞中的复制。