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1. 发明授权

US07265142B2 Materials and methods for the treatment of hypertension and angina 失效
标题翻译：用于治疗高血压和心绞痛的材料和方法
公开(公告)号：US07265142B2
公开(公告)日：2007-09-04
申请号：US10643699
申请日：2003-08-18
申请人： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Xiaoming Zhang
发明人： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Xiaoming Zhang
IPC分类号： A61K31/415 , C07D235/14
CPC分类号： C07D235/14
摘要： The subject invention provides useful and novel calcium channel blockers based upon mibefradil. The subject invention also provides methods for synthesizing the compounds of the invention. The invention also provides methods for the control or prevention of hypertension, angina pectoris, ischemia, arrhythmias, and cardiac insufficiency in a patient by administering a compound, or composition, of the invention to an individual in need of such treatment.
摘要翻译：本发明提供了基于米非司定的有用和新颖的钙通道阻滞剂。本发明还提供了合成本发明化合物的方法。本发明还提供了通过向需要这种治疗的个体施用本发明的化合物或组合物来控制或预防患者的高血压，心绞痛，缺血，心律失常和心脏功能不全的方法。

2. 发明授权

US06608097B2 Materials and methods for the treatment of hypertension and angina 失效
标题翻译：用于治疗高血压和心绞痛的材料和方法
公开(公告)号：US06608097B2
公开(公告)日：2003-08-19
申请号：US10269139
申请日：2002-10-10
申请人： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Xiaoming Zhang
发明人： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Xiaoming Zhang
IPC分类号： A61K314184
CPC分类号： C07D235/14
摘要： The subject invention provides useful and novel calcium channel blockers based upon mibefradil. The subject invention also provides methods for synthesizing the compounds of the invention. The invention also provides methods for the control or prevention of hypertension, angina pectoris, ischemia, arrhythmias, and cardiac insufficiency in a patient by administering a compound, or composition, of the invention to an individual in need of such treatment.
摘要翻译：本发明提供了基于米非司定的有用和新颖的钙通道阻滞剂。本发明还提供了合成本发明化合物的方法。本发明还提供了通过向需要这种治疗的个体施用本发明的化合物或组合物来控制或预防患者的高血压，心绞痛，缺血，心律失常和心脏功能不全的方法。

3. 发明授权

US06552046B2 Materials and methods for the treatment of gastroesophageal reflux disease 有权
公开(公告)号：US06552046B2
公开(公告)日：2003-04-22
申请号：US09876698
申请日：2001-06-07
申请人： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Cyrus Becker
发明人： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Cyrus Becker
IPC分类号： A61K31445
CPC分类号： C07D211/58 , A61K31/4468 , C07D211/46
摘要： The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.

4. 发明授权

US06768008B2 Materials and methods for the treatment of diabetes, hyperlipidemia, hypercholesterolemia, and atherosclerosis 失效
标题翻译：用于治疗糖尿病，高脂血症，高胆固醇血症和动脉粥样硬化的材料和方法
公开(公告)号：US06768008B2
公开(公告)日：2004-07-27
申请号：US09961542
申请日：2001-09-21
申请人： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
发明人： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
IPC分类号： C07D27734
CPC分类号： C07D277/20 , C07D261/12 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , Y10S514/866
摘要： The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.
摘要翻译：本发明提供了可用于治疗II型糖尿病的药物化合物。这些化合物是有利的，因为它们容易被代谢药物解毒系统代谢。特别地，提供了被设计为在化合物的结构内包含酯的噻唑烷二酮类似物。本发明还涉及治疗疾病如糖尿病的方法，其包括施用包含化合物的治疗有效组合物，所述化合物被设计为由血清或细胞内水解酶和酯酶代谢。还教导了含酯的噻唑烷二酮类似物的药物组合物。

5. 发明授权

US06362223B1 Enantiomeric compounds for treatment of cardiac arrhythmias and methods of use 有权
标题翻译：用于治疗心律失常的对映体化合物及其使用方法
公开(公告)号：US06362223B1
公开(公告)日：2002-03-26
申请号：US09684046
申请日：2000-10-06
申请人： Pascal Druzgala , Peter G. Milner
发明人： Pascal Druzgala , Peter G. Milner
IPC分类号： A61K31335
CPC分类号： C07D307/54 , Y10S514/821
摘要： The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.
摘要翻译：本发明涉及新颖的对映异构体纯的化合物和包含该化合物的组合物，用于治疗心律失常。本发明还涉及制备和纯化化合物的方法。与化合物的外消旋混合物相比，对映异构体纯化的化合物和这些化合物的组合物显示出意想不到的和有利的特征，例如显着优异的降低或抑制心室过早搏动的能力。

6. 发明授权

US6114344A Long-acting local anesthetics 失效
标题翻译：长效局麻药
公开(公告)号：US6114344A
公开(公告)日：2000-09-05
申请号：US356283
申请日：1999-07-16
申请人： Pascal Druzgala , Peter G. Milner
发明人： Pascal Druzgala , Peter G. Milner
IPC分类号： A61K31/245 , A61K31/435 , A61K31/135
CPC分类号： A61K31/245
摘要： The subject invention concerns novel compounds that are useful as long-acting local anesthetics. The compounds are N-acyl derivatives of the compound known as tetracaine.
摘要翻译：本发明涉及可用作长效局部麻醉剂的新化合物。化合物是被称为丁卡因的化合物的N-酰基衍生物。

7. 再颁专利

USRE41289E1 Ultrashort acting hypnotic barbiturates 失效
标题翻译：超短效催眠巴比妥类
公开(公告)号：USRE41289E1
公开(公告)日：2010-04-27
申请号：US12009446
申请日：2007-12-20
申请人： Pascal Druzgala , Peter G. Milner
发明人： Pascal Druzgala , Peter G. Milner
IPC分类号： C07D239/42 , C07D239/62 , A61K31/505 , A61K31/515 , A61P25/20
CPC分类号： C07D239/62 , C07D239/66
摘要： The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.
摘要翻译：本发明涉及可用作超短效催眠巴比妥酸盐的新型化合物。具体举例说明的是巴比妥酸和硫代巴比妥酸的衍生物。它们被血液和组织酶快速代谢，以形成无催眠活性的极性代谢物，并迅速消除。

8. 发明授权

US06958355B2 Materials and methods for the treatment of diabetes, hyperlipidemia, hypercholesterolemia, and atherosclerosis 失效
公开(公告)号：US06958355B2
公开(公告)日：2005-10-25
申请号：US10251522
申请日：2002-09-20
申请人： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
发明人： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
IPC分类号： A61P3/10 , C07D261/12 , C07D277/20 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , A61K31/421 , C07D263/58
CPC分类号： C07D277/20 , C07D261/12 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , Y10S514/866
摘要： The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

9. 发明授权

US06316487B1 Compounds for treatment of cardiac arrhythmia synthesis, and methods of use 有权
标题翻译：用于治疗心律失常合成的化合物及其使用方法
公开(公告)号：US06316487B1
公开(公告)日：2001-11-13
申请号：US09680880
申请日：2000-10-06
申请人： Pascal Druzgala , Peter G. Milner
发明人： Pascal Druzgala , Peter G. Milner
IPC分类号： A61K31405
CPC分类号： C07D307/80
摘要： The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
摘要翻译：本发明涉及用于治疗心律失常的新化合物和包含该化合物的组合物。本发明还涉及制备新化合物的方法。新化合物是胺碘酮的快速代谢类似物，其具有被代谢为较低亲油性化合物的独特且有利的特征。新化合物可用于治疗危及生命的室性快速性心律失常，特别是在患有充血性心力衰竭（CHF）的患者中。该产品还可以为室性心律失常和室上性心律失常提供有效的管理，包括心房颤动和涉及辅助途径的进入性快速性心律失常。

10. 再颁专利

USRE42412E1 Materials and methods for the treatment of gastroesophageal reflux disease 有权
标题翻译：用于治疗胃食管反流病的材料和方法
公开(公告)号：USRE42412E1
公开(公告)日：2011-05-31
申请号：US11962592
申请日：2007-12-21
申请人： Pascal Druzgala , Peter G. Milner , Jurg Pfister , Cyrus Becker
发明人： Pascal Druzgala , Peter G. Milner , Jurg Pfister , Cyrus Becker
IPC分类号： A61K31/445 , C07D211/56
CPC分类号： C07D211/58 , A61K31/4468 , C07D211/46
摘要： The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.
摘要翻译：本发明提供了用于安全有效地治疗胃食管反流和相关病症的新型化合物和组合物。在优选的实施方案中，本发明的组合物包含酯化的西沙必利衍生物。这些组合物在治疗胃食管反流疾病中具有有效的活性，并且显着减少与西沙必利施用相关的不良反应。这些不良影响包括但不限于腹泻，腹部绞痛和血压升高和心率升高。

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