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公开(公告)号：US20070196510A1
公开(公告)日：2007-08-23
申请号：US11509895
申请日：2006-08-24
IPC分类号： A61K33/24 , A61K31/554 , A61K31/549 , A61K31/455 , A61K31/4184 , A61K31/41 , A61K31/401
CPC分类号： A61K31/401 , A61K31/4184 , A61K31/455 , A61K31/505 , A61K31/549 , A61K31/554 , A61K45/06 , A61K2300/00
摘要： A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively 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. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline 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.
摘要翻译： 提供了一种用于降低具有临床诊断为耐药性高血压的患者的血压的方法。 该方法包括以基线抗高血压方案辅助给予患者darusentan，所述方案包括给予至少一种利尿剂和至少两种抗高血压药物，所述药物选自（a）ACE抑制剂和血管紧张素II受体阻断剂中的至少两种，（b） 肾上腺素能受体阻断剂和（c）钙通道阻断剂。 darusentan以与基线方案组合的剂量和频率有效地口服施用，以在一个或多个血压参数中提供至少约3mmHg的减少，所述血压参数选自从坐位收缩期，低坐位舒张期，24小时动态 收缩期，24小时动态舒张期，最大昼间收缩期和最大昼夜舒张压。
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公开(公告)号：US20080145433A1
公开(公告)日：2008-06-19
申请号：US11935474
申请日：2007-11-06
CPC分类号： A61K31/505 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/2813 , A61K9/2853 , A61K9/2866
摘要： A solid discrete orally deliverable pharmaceutical dosage form comprises darusentan and one or more pharmaceutically acceptable excipients; wherein (a) the darusentan is in solid particulate form having a mean particle size of about 5 to about 200 μm and is present in the dosage form in an amount of about 1 to about 600 mg; and (b) the dosage form exhibits at least about 90% dissolution of the darusentan in 30 minutes in a standard in vitro dissolution test. A method for lowering blood pressure, for example in a patient having resistant hypertension, comprises administering such a dosage form once daily to the patient.
摘要翻译： 固体分散的口服递送药物剂型包含darusentan和一种或多种药学上可接受的赋形剂; 其中（a）所述darusentan是固体颗粒形式，其平均粒度为约5至约200μm，并且在剂型中以约1至约600mg的量存在; 和（b）在标准体外溶出试验中，剂型在30分钟内显示至少约90％的darusentan溶解。 一种降低血压的方法，例如在具有耐药性高血压的患者中，包括每天向患者施用这种剂型。
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公开(公告)号：US20090221549A1
公开(公告)日：2009-09-03
申请号：US12279037
申请日：2007-02-16
IPC分类号： A61K31/554 , A61K31/505 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/495 , A61P9/12
CPC分类号： A61K31/435
摘要： 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.
摘要翻译： 提供了一种新的使用darusentan来制备用于降低患有对一种或多种药物进行基线抗高血压治疗的抗性的患者的血压的药物组合物。 所述组合物包含提供治疗有效日剂量的darusentan; 其中（a）所述组合物可口服递送和/或（b）每日剂量的darusentan有效地在一个或多个血压参数中提供至少约3mmHg的降低，所述血压参数选自从坐位心脏收缩期，服用舒张期， - 动态收缩期，24小时动态舒张期，最大昼间收缩期和最大昼夜舒张压。 还提供了darusentan在制备用于降低基线抗高血压治疗抗性的患者中的血压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受体阻断剂，β-肾上腺素能受体阻断剂和钙通道阻断剂。
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公开(公告)号：US20090054473A1
公开(公告)日：2009-02-26
申请号：US12196635
申请日：2008-08-22
IPC分类号： A61K31/513 , A61P3/00
CPC分类号： A61K31/505 , A61K9/0053 , A61K31/4025 , A61K31/549 , A61K45/06 , A61K2300/00
摘要： A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with 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. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
摘要翻译： 在具有糖尿病性肾病和/或代谢综合征的人类受试者中增强血糖控制和/或胰岛素敏感性的方法包括在血糖控制和/或胰岛素敏感性增强有效量中向受试者施用选择性内皮素A（ETA）受体拮抗剂。 用于治疗老年糖尿病人受试者的合并症复合物的方法包括给予受试者组合的选择性ETA受体拮抗剂或作为辅助治疗与至少一种额外的药剂，所述另外的药剂是（i）除了选择性ETA受体拮抗剂和（ ii）有效治疗糖尿病和/或除高血压之外的所述合并症中的至少一种。 用于这种方法的治疗组合包括选择性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。
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