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1.再颁专利公开(公告)号：USRE42412E1
公开(公告)日：2011-05-31
申请号：US11962592
申请日：2007-12-21
Applicant: Pascal Druzgala , Peter G. Milner , Jurg Pfister , Cyrus Becker
Inventor： Pascal Druzgala , Peter G. Milner , Jurg Pfister , Cyrus Becker
IPC: A61K31/445 , C07D211/56
CPC classification number: C07D211/58 , A61K31/4468 , C07D211/46
Abstract: 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.
Abstract translation: 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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公开(公告)号：US07265142B2
公开(公告)日：2007-09-04
申请号：US10643699
申请日：2003-08-18
Applicant: Pascal Druzgala , Peter G. Milner , Jürg Pfister , Xiaoming Zhang
Inventor： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Xiaoming Zhang
IPC: A61K31/415 , C07D235/14
CPC classification number: C07D235/14
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US07022722B2
公开(公告)日：2006-04-04
申请号：US10759617
申请日：2004-01-16
Applicant: Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
Inventor： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
IPC: A61K31/426 , A61K31/427
CPC classification number: C07D277/20 , C07D261/12 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , Y10S514/824 , Y10S514/866
Abstract: 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.
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4.发明授权Enantiomeric compounds for treatment of cardiac arrhythmias and methods of use 有权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：US06683195B2
公开(公告)日：2004-01-27
申请号：US10123573
申请日：2002-04-15
Applicant: Pascal Druzgala , Peter G. Milner
Inventor： Pascal Druzgala , Peter G. Milner
IPC: C07D30778
CPC classification number: C07D307/54 , C07D307/80
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US06552046B2
公开(公告)日：2003-04-22
申请号：US09876698
申请日：2001-06-07
Applicant: Pascal Druzgala , Peter G. Milner , Jürg Pfister , Cyrus Becker
Inventor： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Cyrus Becker
IPC: A61K31445
CPC classification number: C07D211/58 , A61K31/4468 , C07D211/46
Abstract: 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.
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Patent Agency Ranking
6.发明授权Enantiomeric compounds for treatment of cardiac arrhythmias and methods of use 有权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：US06372783B1
公开(公告)日：2002-04-16
申请号：US09680873
申请日：2000-10-06
Applicant: Pascal Druzgala , Peter G. Milner
Inventor： Pascal Druzgala , Peter G. Milner
IPC: A61K3134
CPC classification number: C07D307/54 , Y10S514/821
Abstract: 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 isolated 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.
Abstract translation: 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，分离的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，例如显着优异的减少或抑制心室过早搏动的能力。
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公开(公告)号：US07041673B2
公开(公告)日：2006-05-09
申请号：US10763904
申请日：2004-01-23
Applicant: Pascal Druzgala , Peter G. Milner
Inventor： Pascal Druzgala , Peter G. Milner
IPC: C07D239/42 , C07D239/62 , A61K31/505 , A61K31/515 , A61P25/20
CPC classification number: C07D239/62 , C07D239/66
Abstract: 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.
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公开(公告)号：US06818782B2
公开(公告)日：2004-11-16
申请号：US10697683
申请日：2003-10-29
Applicant: Pascal Druzgala , Peter G. Milner
Inventor： Pascal Druzgala , Peter G. Milner
IPC: C07D30778
CPC classification number: C07D307/54 , C07D307/80
Abstract: 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.
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公开(公告)号：US06680387B2
公开(公告)日：2004-01-20
申请号：US09841351
申请日：2001-04-24
Applicant: Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
Inventor： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
IPC: C07D41700
CPC classification number: C07D277/20 , C07D261/12 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , Y10S514/824 , Y10S514/866
Abstract: 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.
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公开(公告)号：US06608097B2
公开(公告)日：2003-08-19
申请号：US10269139
申请日：2002-10-10
Applicant: Pascal Druzgala , Peter G. Milner , Jürg Pfister , Xiaoming Zhang
Inventor： Pascal Druzgala , Peter G. Milner , Jürg Pfister , Xiaoming Zhang
IPC: A61K314184
CPC classification number: C07D235/14
Abstract: 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.
Abstract translation: 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。
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