公开(公告)号：US20140350005A1

公开(公告)日：2014-11-27

申请号：US14184615

申请日：2014-02-19

Applicant: GARY W. LUEHR ,  ARATHI SUNDARAM ,  PRIYADARSHINI JAISHANKAR ,  PHILIP W. PAYNE ,  PASCAL DRUZGALA

Inventor： GARY W. LUEHR ,  ARATHI SUNDARAM ,  PRIYADARSHINI JAISHANKAR ,  PHILIP W. PAYNE ,  PASCAL DRUZGALA

IPC: C07D471/10 ,  A61K31/5377 ,  A61K31/439 ,  A61K31/435 ,  A61K45/06 ,  A61K31/4545 ,  A61K31/538 ,  A61K31/496

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/538 ,  A61K45/06 ,  C07D519/00 ,  Y02A50/475

Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.

Abstract translation: 提供D2或D3拮抗剂化合物和式I的药物组合物及其药学上可接受的盐或其异构体，其中R 1，R 2和R 3如本文所定义。 本发明还包括制备本发明化合物的方法和用于治疗由本发明化合物引起的多巴胺D2或D3受体介导的病症的方法。

公开(公告)号：USRE42412E1

公开(公告)日：2011-05-31

申请号：US11962592

申请日：2007-12-21

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。

公开(公告)号：US20100184815A1

公开(公告)日：2010-07-22

申请号：US12641954

申请日：2009-12-18

Applicant: Gary W. Luehr ,  Arathi Sundaram ,  Priya Jaishankar ,  Chhaya Bhakta ,  Pascal Druzgala

Inventor： Gary W. Luehr ,  Arathi Sundaram ,  Priya Jaishankar ,  Chhaya Bhakta ,  Pascal Druzgala

IPC: A61K31/4196 ,  C07D249/12 ,  C07D249/04 ,  C07D231/12 ,  A61K31/4192 ,  A61K31/415 ,  A61P9/10

CPC classification number: C07D233/56 ,  C07D249/04 ,  C07D249/06 ,  C07D249/12

Abstract: Disclosed are compounds of the formula: And pharmaceutically acceptable salts thereof, wherein the variables are as defined herein, which are useful in activating PPARα and in treating atherosclerosis hypercholesterolemia, primary hypercholesterolemia or mixed dyslipidemia, hypertriglyceridemia, Frederickson Types IV and V hyperlipidemia. Pharmaceutical compositions, intermediates useful in the preparation of the compounds of formula I and methods of making the compounds of formula I are also disclosed.

Abstract translation: 公开了下式的化合物及其药学上可接受的盐，其中变量如本文所定义，其可用于激活PPARα和用于治疗动脉粥样硬化高胆固醇血症，原发性高胆固醇血症或混合型血脂异常，高甘油三酯血症，腓特第克氏IV型和V型高脂血症。 还公开了药物组合物，可用于制备式I化合物的中间体和制备式I化合物的方法。

公开(公告)号：US07381735B2

公开(公告)日：2008-06-03

申请号：US11257323

申请日：2005-10-24

Applicant: Pascal Druzgala

Inventor： Pascal Druzgala

IPC: A01N43/40 ,  C07D211/56

CPC classification number: C07D211/58 ,  C07D211/66

Abstract: The subject invention concerns analogs of fentanyl opioids. The subject invention also concerns methods for synthesizing the compounds of the invention. The invention also concerns methods for treating pain in a patient by administering a compound of the invention to a person in need of such treatment.

Abstract translation: 本发明涉及芬太尼阿片样物质的类似物。 本发明还涉及合成本发明化合物的方法。 本发明还涉及通过向需要这种治疗的人施用本发明化合物来治疗患者疼痛的方法。

公开(公告)号：US07265142B2

公开(公告)日：2007-09-04

申请号：US10643699

申请日：2003-08-18

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。

公开(公告)号：US20070060640A1

公开(公告)日：2007-03-15

申请号：US11457719

申请日：2006-07-14

Applicant: Pascal Druzgala ,  Jien-Heh Tien ,  Arthur Cooper ,  Cyrus Becker

Inventor： Pascal Druzgala ,  Jien-Heh Tien ,  Arthur Cooper ,  Cyrus Becker

IPC: A61K31/366 ,  C07D493/02

CPC classification number: C07D307/80 ,  C07D493/04

Abstract: The invention comprises compounds of Formula 1: wherein, R1 is independently H or halogen; R2 is, for example, H or —R10—NR11R12, and wherein R10 is C1-C6 alkyl, and R11 and R12 are independently H, C1-C4 alkyl, and hydrates, solvates, salts and tautomers thereof. The invention further comprises methods for making the compounds of the invention and methods for making compounds useful in the treatment or prevention of cardiac arrhythmia from the compounds of the invention.

Abstract translation: 本发明包括式1的化合物：其中R 1独立地是H或卤素; R 2是例如H或-R 10 -NR 11 R 12，并且其中R 1， R 10是C 1 -C 6烷基，R 11和R 12是 独立地是H，C 1 -C 4烷基，以及其水合物，溶剂合物，盐和互变异构体。 本发明还包括制备本发明化合物的方法和用于制备化合物的方法，其用于治疗或预防本发明化合物的心律失常。

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.

公开(公告)号：US20050054676A1

公开(公告)日：2005-03-10

申请号：US10931586

申请日：2004-08-31

Applicant: Pascal Druzgala

Inventor： Pascal Druzgala

IPC: A61K31/165 ,  A61K31/192 ,  A61K31/215 ,  A61K31/221 ,  A61K31/277 ,  A61K31/4015 ,  C07C251/58 ,  A61K31/445 ,  A61K31/195 ,  A61K31/40

CPC classification number: C07C251/58 ,  A61K31/165 ,  A61K31/192 ,  A61K31/215 ,  A61K31/221 ,  A61K31/277 ,  A61K31/4015

Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Abstract translation: 本发明提供了易于被代谢药物解毒系统代谢的化合物。 特别地，教导了被设计为在化合物的结构内包括酯的氟伏沙明类似物。 还提供了治疗抑郁症和情感障碍（例如强迫症）的方法。 还教导了氟伏沙明类似物的药物组合物。

公开(公告)号：US06809116B2

公开(公告)日：2004-10-26

申请号：US10273702

申请日：2002-10-18

Applicant: Pascal Druzgala

Inventor： Pascal Druzgala

IPC: A61K3124

CPC classification number: A61K31/165 ,  A61K31/192 ,  A61K31/215 ,  A61K31/221 ,  A61K31/277 ,  A61K31/4015 ,  C07C251/58

Abstract: The subject invention provides compounds which are easily metabolized by the metobolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Abstract translation: 本发明提供了化合物，其易于被全身药物解毒系统代谢。 特别地，教导了被设计为在化合物结构内包括酯的氟伏沙明类似物。 还提供了治疗抑郁症和情感障碍（例如强迫症）的方法。 还教导了氟伏沙明类似物的药物组合物。

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。