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    • 3. 发明申请
    • THERAPY FOR COMPLICATIONS OF DIABETES
    • 治疗糖尿病的药物
    • WO2009026517A2
    • 2009-02-26
    • PCT/US2008074013
    • 2008-08-22
    • GILEAD COLORADO INCRODEN ROBERT LGORCZYNSKI RICHARD JGERBER MICHAEL J
    • RODEN ROBERT LGORCZYNSKI RICHARD JGERBER MICHAEL J
    • A61K31/505A61P13/12
    • A61K31/505A61K9/0053A61K31/4025A61K31/549A61K45/06
    • A selective ETA receptor antagonist for use in a method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome is disclosed. A selective ETA receptor antagonist for use in treating a complex of comorbidities in an elderly diabetic human subject, wherein the selective ETA receptor antagonist is for administration in combination or as adjunctive therapy with (a) at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension, and optionally (b) at least one antihypertensive other than a selective ETA receptor antagonist is disclosed. Further, a therapeutic combination comprising a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist is disclosed.
    • 公开了用于增加糖尿病性肾病和/或代谢综合征的人类受试者血糖控制和/或胰岛素敏感性的方法中的选择性ETA受体拮抗剂。 一种选择性ETA受体拮抗剂,其用于治疗老年糖尿病人受试者的合并症复合物,其中所述选择性ETA受体拮抗剂用于联合给药或作为辅助治疗,与(a)至少一种另外的药剂是(i)其它 公开了选择性ETA受体拮抗剂和(ii)有效治疗糖尿病和/或除了高血压之外的所述合并症中的至少一种,以及任选地(b)除了选择性ETA受体拮抗剂之外的至少一种抗高血压药。 此外,公开了包含选择性ETA受体拮抗剂和除选择性ETA受体拮抗剂之外的至少一种抗糖尿病,抗肥胖症或抗脂肪代谢剂的治疗组合。
    • 5. 发明申请
    • METHOD FOR TREATING RESISTANT HYPERTENSION
    • 治疗抗高血压的方法
    • WO2007098390A3
    • 2007-11-15
    • PCT/US2007062291
    • 2007-02-16
    • GILEAD COLORADO INCGERBER MICHAEL JGORCZYNSKI RICHARD JRODEN ROBERT L
    • GERBER MICHAEL JGORCZYNSKI RICHARD JRODEN ROBERT L
    • A61K31/435A61P9/12
    • A61K31/401A61K31/4184A61K31/455A61K31/505A61K31/549A61K31/554A61K45/06A61K2300/00
    • A new use of darusentan is provided in preparation of a pharmaceutical composition, for adjunctive administration with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers, to lower blood pressure in a patient having resistant hypertension; wherein the composition is orally deliverable and comprises darusentan in a daily dose effective, in combination with said regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.
    • 在制备药物组合物中提供了darusentan的新用途,用于用基线抗高血压药物方案辅助施用,该方法包括施用至少一种利尿剂和至少两种选自以下至少两种的抗高血压药物:(a)ACE抑制剂和血管紧张素II (b)β-肾上腺素受体阻断剂和(c)钙通道阻断剂,以降低患有顽固性高血压的患者的血压; 其中所述组合物是口服递送的并且包含与所述方案组合有效的每日剂量的达卢生坦,以在选自以下的一个或多个血压参数中提供至少约3mmHg的降低:坐位收缩期,坐位舒张期, 小时动态收缩压,24小时动态舒张压,最大昼夜收缩压和最大昼夜舒张压。
    • 7. 发明申请
    • ANTIHYPERTENSIVE THERAPY
    • 抗高血压治疗
    • WO2007098387A2
    • 2007-08-30
    • PCT/US2007/062288
    • 2007-02-16
    • GILEAD COLORADO, INC.GERBER, Michael, J.GORCZYNSKI, Richard, J.RODEN, Robert, L.
    • GERBER, Michael, J.GORCZYNSKI, Richard, J.RODEN, Robert, L.
    • A61P9/12
    • A61K31/435
    • A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.
    • 提供了达卢生坦的新用途,用于制备用于降低患有对一种或多种药物的基线抗高血压治疗抗性的患者的血压降低的药物组合物。 该组合物包含提供治疗有效日剂量的达卢生坦; (a)所述组合物可口服递送和/或(b)达卢生坦的日剂量有效提供至少约3mmHg的降低,所述一个或多个血压参数选自坐位收缩期,坐位舒张期槽,24 - 小时动态收缩压,24小时动态舒张压,最大昼夜收缩压和最大昼夜舒张压。 还提供了darusentan在制备用于降低对基线抗高血压治疗具有抗性的患者的血压降低的药物组合物中的新用途,其中该组合物与至少一种利尿剂和至少一种选自ACE抑制剂的抗高血压药物 ,血管紧张素II受体阻滞剂,β-肾上腺素受体阻滞剂和钙通道阻滞剂。
    • 8. 发明申请
    • METHODS FOR ADMINISTRATION OF RADIOTHERAPEUTIC AGENTS
    • 放射治疗药物的管理方法
    • WO2008140808A1
    • 2008-11-20
    • PCT/US2008/006040
    • 2008-05-09
    • PEAK BIOSCIENCES, INC.GERBER, Michael, J.WARREN, Stephen, L.MATSUURA, James, E.
    • GERBER, Michael, J.WARREN, Stephen, L.MATSUURA, James, E.
    • A01N43/42
    • A61K31/00A61K38/1703A61K38/18A61K38/1866A61K38/195A61K38/20A61K38/22A61K45/06A61K48/00A61K51/0491A61K2300/00
    • A method is provided for treatment of disorders involving hyperproliferative cells, such as malignancies, advanced stage solid tumors like glioblastoma multiforme, and non-malignant hyperproliferative pathological conditions such as adult macular degeneration. A short range, unselective cell killing radiotherapeutic substance is administered, optionally in a spatially defined volume of tissue, optionally in combination with a mitogenic agent that stimulates or induces DNA biosynthesis. In this way, the percentage of hyperproliferative that are susceptible to killing by the radiotherapeutic agent is increased. Cancer stem cells can be induced to enter S phase with the mitogenic agent, then killed with the radiotherapeutic agent. Thus, not only does the combination effectively kill the transit amplifying cell population, the most rapidly replicating type of cell in a tumor, but it also effectively kills the tumor stem cells, which give rise to the transit amplifying cells, for a longer lasting anticancer effect.
    • 提供了用于治疗涉及过度增殖细胞例如恶性肿瘤,晚期实体瘤如多形性成胶质细胞瘤的病症和非恶性过度增殖病理状况如成人黄斑变性的病症的方法。 任选地在空间上限定的组织体内施用短程,非选择性细胞杀伤放射治疗物质,任选与刺激或诱导DNA生物合成的促有丝分裂剂组合。 以这种方式,放射治疗剂易于杀死的过度增殖的百分比增加。 可以诱导癌干细胞与促有丝分裂剂进入S期,然后用放射治疗剂杀死。 因此,不仅组合有效地杀死了肿瘤中最快速复制型细胞的转运扩增细胞群,而且还有效地杀死了产生转运扩增细胞的肿瘤干细胞,以达到更持久的抗癌作用 影响。