PHARMACEUTICAL PREPARATION
    21.
    发明申请
    PHARMACEUTICAL PREPARATION 审中-公开
    药物制剂

    公开(公告)号:US20110111021A1

    公开(公告)日:2011-05-12

    申请号:US12918993

    申请日:2009-02-23

    摘要: The present invention provides a pharmaceutical preparation including a compartment containing a renin inhibitor as a pharmacologically active ingredient, and a compartment containing an HMG-CoA reductase inhibitor as a pharmacologically active ingredient, wherein one compartment is a prior-release compartment and the other compartment is a delayed-release compartment. The combination preparation of the present invention can deliver a renin inhibitor and an HMG-CoA reductase inhibitor with a time interval at a specific speed, thus reducing undesirable side-effects, improving the drug efficacy and promoting the patient compliance. Further, the pharmaceutical preparation of the present invention has pharmacological, clinical, scientific and economical advantages in the prevention or treatment of metabolic syndromes, cardiovascular diseases, renal diseases and the like, as compared with the complex drug regimens in which medicament ingredients are taken individually or simultaneously.

    摘要翻译: 本发明提供一种药物制剂,其包含含有作为药理活性成分的肾素抑制剂的隔室,以及含有作为药理活性成分的HMG-CoA还原酶抑制剂的隔室,其中一个隔室为先前释放室,另一隔室为 延迟释放室。 本发明的组合制剂可以以特定速度的时间间隔递送肾素抑制剂和HMG-CoA还原酶抑制剂,从而减少不期望的副作用,改善药物功效并促进患者依从性。 此外,与复合药物方案相比,本发明的药物制剂在预防或治疗代谢综合征,心血管疾病,肾脏疾病等方面具有药理,临床,科学和经济优势,其中药物成分单独服用 或同时。

    COMPOSITE PREPARATION
    22.
    发明申请
    COMPOSITE PREPARATION 审中-公开
    复合制剂

    公开(公告)号:US20110038931A1

    公开(公告)日:2011-02-17

    申请号:US12919000

    申请日:2009-02-21

    摘要: The present invention provides a combination preparation which comprises: a prior-release section comprising aspirin or a pharmaceutically acceptable salt thereof as a pharmacologically active component; and a delayed-release section comprising clopidogrel, an isomer thereof or a pharmaceutically acceptable salt thereof as a pharmacologically active component. The combination preparation of the present invention exhibits a far better effect in preventing platelet aggregation than does simultaneous oral therapy or treatment with the respective single preparations, and not only can it improve the patient's drug-taking compliance by administration once a day but it can also reduce the adverse reactions which follow long-term administration of aspirin. The combination preparation of the present invention is also advantageous in that it exhibits an outstanding effect in inhibiting blood platelet aggregation despite a reduction in the amount of aspirin ingested, and in that it converts clopidogrel resistance into susceptibility and prevents serious adverse reactions caused by clopidogrel resistance and in that it can be stored over the longer term since it is stable under common storage conditions.

    摘要翻译: 本发明提供了一种组合制剂,其包含:包含阿司匹林或其药学上可接受的盐作为药理活性成分的先前释放部分; 以及包含氯吡格雷,其异构体或其药学上可接受的盐作为药理活性成分的延迟释放部分。 本发明的组合制剂表现出比同时口服治疗或用单一制剂治疗的预防血小板聚集效果好得多,并且不仅可以通过一天一次的给药来改善患者的药物依从性,而且还可以 减少长期服用阿司匹林后的不良反应。 本发明的组合制剂的优点还在于尽管阿司匹林的摄取量减少,但是其表现出抑制血小板聚集的突出效果,并且将氯吡格雷耐药性转化为易感性并防止由氯吡格雷抗性引起的严重不良反应 并且由于它在常见的储存条件下是稳定的,因此可以长期储存。

    CONTROLLED RELEASE COMPLEX COMPOSITION COMPRISING ANGIOTENSIN-II-RECEPTOR BLOCKERS AND HMG-COA REDUCTASE INHIBITORS
    24.
    发明申请
    CONTROLLED RELEASE COMPLEX COMPOSITION COMPRISING ANGIOTENSIN-II-RECEPTOR BLOCKERS AND HMG-COA REDUCTASE INHIBITORS 有权
    包含血管紧张素II受体阻断剂和HMG-COA还原酶抑制剂的受控释放复合组合物

    公开(公告)号:US20100074951A1

    公开(公告)日:2010-03-25

    申请号:US12513054

    申请日:2007-10-30

    摘要: Disclosed herein is a lag time delayed-release combination pharmaceutical composition comprising of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor, as well as a preparation method thereof. The composition is designed based on chronotherapy in which active ingredients are administered to have different onset times, such that the release of each active ingredient of the composition in body can be lag time delayed to a specific rate. Also, the composition is very effective for the treatment of hypertension and the prevention of complications in patients having metabolic syndromes which show diabetes, obesity, hyperlipidemia, coronary artery diseases and the like. More specifically, the composition is a drug delivery system designed such that the release of each drug is controlled to a specific rate, and it can show the most ideal effect, when it is absorbed in body.

    摘要翻译: 本文公开了包含血管紧张素-II-受体阻断剂和HMG-CoA还原酶抑制剂的滞后时间延迟释放组合药物组合物及其制备方法。 该组合物是基于治疗时间来设计的,其中施用活性成分具有不同的起始时间,使得组合物的每种活性成分在体内的释放可延迟到特定的速率。 此外,该组合物对于治疗高血压和预防具有显示糖尿病,肥胖症,高脂血症,冠状动脉疾病等的代谢综合征的患者的并发症非常有效。 更具体地,组合物是药物递送系统,其被设计成使得每种药物的释放被控制到特定的速率,并且当其被吸收在体内时它可以显示出最理想的效果。

    N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative, preparation method thereof, and pharmaceutical composition containing same
    28.
    发明授权
    N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative, preparation method thereof, and pharmaceutical composition containing same 失效
    N1-苯并[1,3]二氧杂环戊烯-5-基甲基-N2-取代双胍衍生物,其制备方法和含有它们的药物组合物

    公开(公告)号:US08642647B2

    公开(公告)日:2014-02-04

    申请号:US13123417

    申请日:2009-10-13

    IPC分类号: C07D317/44 A61K31/36

    CPC分类号: C07D317/58

    摘要: The present invention provides an N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.

    摘要翻译: 本发明提供式(I)的1,3-苯并[1,3]二氧杂环戊烯-5-基甲基-N 2取代双胍衍生物或其药学上可接受的盐,其制备方法,以及包含其的药物组合物 有效成分。 本发明的N1-苯并[1,3]二氧杂环戊烯-5-基甲基-N2-取代的双胍衍生物即使与常规药物相比也显示出降低剂量的血糖水平和脂质降低水平的效果,因此它是有用的 用于预防或治疗糖尿病,代谢综合征如胰岛素不依赖性糖尿病,肥胖症和动脉粥样硬化,或P53基因缺陷相关癌症。

    Controlled release complex composition comprising angiotensin-II-receptor blockers and HMG-CoA reductase inhibitors
    29.
    发明授权
    Controlled release complex composition comprising angiotensin-II-receptor blockers and HMG-CoA reductase inhibitors 有权
    包含血管紧张素-II受体阻断剂和HMG-CoA还原酶抑制剂的控制释放复合物组合物

    公开(公告)号:US08642083B2

    公开(公告)日:2014-02-04

    申请号:US12513054

    申请日:2007-10-30

    摘要: Disclosed herein is a lag time delayed-release combination pharmaceutical composition comprising of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor, as well as a preparation method thereof. The composition is designed based on chronotherapy in which active ingredients are administered to have different onset times, such that the release of each active ingredient of the composition in body can be lag time delayed to a specific rate. Also, the composition is very effective for the treatment of hypertension and the prevention of complications in patients having metabolic syndromes which show diabetes, obesity, hyperlipidemia, coronary artery diseases and the like. More specifically, the composition is a drug delivery system designed such that the release of each drug is controlled to a specific rate, and it can show the most ideal effect, when it is absorbed in body.

    摘要翻译: 本文公开了包含血管紧张素-II-受体阻断剂和HMG-CoA还原酶抑制剂的滞后时间延迟释放组合药物组合物及其制备方法。 该组合物是基于治疗时间来设计的,其中施用活性成分具有不同的起始时间,使得组合物的每种活性成分在体内的释放可延迟到特定的速率。 此外,该组合物对于治疗高血压和预防具有显示糖尿病,肥胖症,高脂血症,冠状动脉疾病等的代谢综合征的患者的并发症非常有效。 更具体地,组合物是药物递送系统,其被设计成使得每种药物的释放被控制到特定的速率,并且当其被吸收在体内时它可以显示出最理想的效果。