公开(公告)号：US06768008B2

公开(公告)日：2004-07-27

申请号：US09961542

申请日：2001-09-21

Applicant: Pascal Druzgala ,  Peter G. Milner ,  Jurg R. Pfister

Inventor： Pascal Druzgala ,  Peter G. Milner ,  Jurg R. Pfister

IPC: C07D27734

CPC classification number: C07D277/20 ,  C07D261/12 ,  C07D277/34 ,  C07D311/70 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07J3/00 ,  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.

Abstract translation: 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。

公开(公告)号：US06362223B1

公开(公告)日：2002-03-26

申请号：US09684046

申请日：2000-10-06

Applicant: Pascal Druzgala ,  Peter G. Milner

Inventor： Pascal Druzgala ,  Peter G. Milner

IPC: A61K31335

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 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。

公开(公告)号：US6114344A

公开(公告)日：2000-09-05

申请号：US356283

申请日：1999-07-16

Applicant: Pascal Druzgala ,  Peter G. Milner

Inventor： Pascal Druzgala ,  Peter G. Milner

IPC: A61K31/245 ,  A61K31/435 ,  A61K31/135

CPC classification number: A61K31/245

Abstract: 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.

Abstract translation: 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。

公开(公告)号：USRE41289E1

公开(公告)日：2010-04-27

申请号：US12009446

申请日：2007-12-20

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.

Abstract translation: 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。

公开(公告)号：US06958355B2

公开(公告)日：2005-10-25

申请号：US10251522

申请日：2002-09-20

Applicant: Pascal Druzgala ,  Peter G. Milner ,  Jurg R. Pfister

Inventor： Pascal Druzgala ,  Peter G. Milner ,  Jurg R. Pfister

IPC: 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 classification number: C07D277/20 ,  C07D261/12 ,  C07D277/34 ,  C07D311/70 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07J3/00 ,  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.

公开(公告)号：US06316487B1

公开(公告)日：2001-11-13

申请号：US09680880

申请日：2000-10-06

Applicant: Pascal Druzgala ,  Peter G. Milner

Inventor： Pascal Druzgala ,  Peter G. Milner

IPC: A61K31405

CPC classification number: C07D307/80

Abstract: 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.

Abstract translation: 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。

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.

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.

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.

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。