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1. 发明申请

US20110144199A1 METHODS FOR TREATING ATRIAL FIBRILLATION 审中-公开
标题翻译：治疗急性心肌梗死的方法
公开(公告)号：US20110144199A1
公开(公告)日：2011-06-16
申请号：US12952696
申请日：2010-11-23
申请人： Peter G. Milner , David Jack Ellis
发明人： Peter G. Milner , David Jack Ellis
IPC分类号： A61K31/343 , A61P9/00
CPC分类号： A61K31/343
摘要： The subject invention provides methods for reducing atrial fibrillation (AF) episode duration, methods for reducing stroke rate, methods for increasing time in normal sinus rhythm (NSR), methods for preventing atrial remodeling, and methods for reversing atrial remodeling, all comprising administering an amount of budiodarone effective to reduce AF episode duration.
摘要翻译：本发明提供减少心房颤动（AF）发作持续时间的方法，降低卒中率的方法，增加正常窦性心律（NSR）时间的方法，预防心房重构的方法，以及逆转心房重构的方法，所有方法均包括给予有效减少AF发作持续时间的剂量的量。

2. 发明申请

US20110269762A1 METHODS FOR TREATING ATRIAL FIBRILLATION AND REDUCING STROKE RATE IN ATRIAL FIBRILLATION PATIENTS 审中-公开
标题翻译：治疗急性心肌梗死的方法和降低急性心肌梗死患者的卒中率
公开(公告)号：US20110269762A1
公开(公告)日：2011-11-03
申请号：US12952666
申请日：2010-11-23
申请人： Peter G. Milner , David Jack Ellis
发明人： Peter G. Milner , David Jack Ellis
IPC分类号： A61K31/5377 , A61K31/4439 , A61P25/00 , A61K31/343 , A61P9/00 , A61K31/437 , A61K31/352
CPC分类号： A61K31/437 , A61K31/343 , A61K31/352 , A61K31/4439 , A61K31/4545 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling. In some methods of the invention, budiodarone is administered 400 mg BID or more preferably 600 mg BID.
摘要翻译：本发明提供了降低卒中发生率的方法，用于预防心房重塑的方法，以及通过施用贝碘酮以减少心房颤动（AF）发作持续时间和抗凝血剂（AC）来逆转心房重塑的方法。根据本发明的一些方法，平均AF发作持续时间可以减少到小于约24,5,3或1小时，并且最大AF发作持续时间可以减少到小于约20,10或5 小时。根据本发明的一些方法，给予布洛诺酮和AC时降低的卒中率小于年龄调整后的总卒中率。此外，一些方法提供可以治疗在给予他莫达酮之前对一种或多种抗心律失常药物难治的患者。一些方法可用于预防心房重塑，另一些方法用于预防房颤重建，包括量化逆转心房重塑的方法。在本发明的一些方法中，给予他达洛酮400mg BID或更优选600mg BID。

3. 发明申请

US20110136779A1 METHODS FOR STROKE REDUCTION IN ATRIAL FIBRILLATION PATIENTS 审中-公开
标题翻译：方法减少ATRIAL FIBRILLATION患者
公开(公告)号：US20110136779A1
公开(公告)日：2011-06-09
申请号：US12952683
申请日：2010-11-23
申请人： Peter G. Milner , David Jack Ellis
发明人： Peter G. Milner , David Jack Ellis
IPC分类号： A61K31/397 , A61K31/40 , A61K31/4439 , A61K31/4709 , A61K31/4545 , A61K31/5377 , A61K31/444 , A61K31/4418 , A61K31/37 , A61K31/4402 , A61K31/445 , A61K31/439 , A61P9/00 , A61P7/02
CPC分类号： A61K31/37 , A61K31/397 , A61K31/40 , A61K31/439 , A61K31/4402 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4545 , A61K31/4709 , A61K31/5377
摘要： The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering a multiple ion channel blocker anti-arrhythmic to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of multiple ion channel blocker and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of the multiple ion channel blocker may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling. In some methods of the invention, budiodarone is administered 400 mg BID or more preferably 600 mg BID.
摘要翻译：本发明提供了降低卒中发生率的方法，用于预防心房重塑的方法，以及通过施用多重离子通道阻断剂抗心律不齐以减少心房颤动（AF）发作持续时间和抗凝血剂（AC）来逆转心房重构的方法。根据本发明的一些方法，平均AF发作持续时间可以减少到小于约24,5,3或1小时，并且最大AF发作持续时间可以减少到小于约20,10或5 小时。根据本发明的一些方法，施用多个离子通道阻滞剂和AC时降低的卒中率小于经年龄调整的总卒中率。此外，一些方法提供了在给予多重离子通道阻断剂之前对一种或多种抗心律失常药物难治的患者也可以进行治疗。一些方法可用于预防心房重塑，另一些方法用于预防房颤重建，包括量化逆转心房重塑的方法。在本发明的一些方法中，给予他达洛酮400mg BID或更优选600mg BID。

4. 发明申请

US20080194486A1 Novel Anti-Obesity Agents 失效
标题翻译：新型抗肥胖剂
公开(公告)号：US20080194486A1
公开(公告)日：2008-08-14
申请号：US11923222
申请日：2007-10-24
申请人： Dominique P. Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter G. Milner
发明人： Dominique P. Bridon , Roger Leger , Xicai Huang , Karen Thibaudeau , Martin Robitaille , Peter G. Milner
IPC分类号： A61K38/03 , C07K4/00 , G01N33/567 , C07K14/00
CPC分类号： C07K14/57545 , A61K38/00 , C07K19/00 , C07K2319/01
摘要： The present invention relates to a compound comprising a PYY peptide or a functional derivative thereof, which is coupled to a reactive group. Such a reactive group is capable of reacting on a blood component so as to form a stable covalent bond therewith. The present invention also relates to a conjugate comprising such a compound which is covalently bonded to a blood component. Moreover, the invention also relates to a method of enhancing, in a patient, the anti-obesity activity of a PYY peptide or functional derivative thereof.
摘要翻译：本发明涉及包含与反应性基团偶联的PYY肽或其功能性衍生物的化合物。这样的反应性基团能够对血液成分进行反应，与其形成稳定的共价键。本发明还涉及包含共价键合到血液成分上的化合物的缀合物。此外，本发明还涉及在患者中增强PYY肽或其功能性衍生物的抗肥胖活性的方法。

5. 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。

6. 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。

7. 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。

8. 发明授权

US5998387A Method for using A.sub.1 adenosine receptor agonists 失效
标题翻译：使用A1腺苷受体激动剂的方法
公开(公告)号：US5998387A
公开(公告)日：1999-12-07
申请号：US56195
申请日：1998-04-06
申请人： Luiz Belardinelli , Ray Olsson , Stephen Baker , Peter J. Scammells , Peter G. Milner , Jurg R. Pfister
发明人： Luiz Belardinelli , Ray Olsson , Stephen Baker , Peter J. Scammells , Peter G. Milner , Jurg R. Pfister
IPC分类号： C07H19/167 , A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61P9/00 , A61P9/06 , C07D473/06 , C07D519/00 , C07H19/16 , C07C229/04
CPC分类号： C07H19/16 , C07D473/06 , Y10S514/821
摘要： Adenosine and xanthine deriviatives, and compositions comprising those compounds, are potent selective agonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias.
摘要翻译：腺苷和黄嘌呤衍生物以及包含这些化合物的组合物是腺苷受体的有效选择性激动剂。衍生物和组合物用于治疗包括某些心律失常的病症。

9. 发明授权

US07608271B2 Modified human immunodeficiency virus anti-fusogenic GP41 peptides comprising a maleimide-containing group 失效
标题翻译：包含含马来酰亚胺基团的修饰的人免疫缺陷病毒抗融合GP41肽
公开(公告)号：US07608271B2
公开(公告)日：2009-10-27
申请号：US10950010
申请日：2004-09-24
申请人： Dominique P. Bridon , Robert S. Dufresne , Nisssab Boudjellab , Martin Robitaille , Peter G. Milner
发明人： Dominique P. Bridon , Robert S. Dufresne , Nisssab Boudjellab , Martin Robitaille , Peter G. Milner
IPC分类号： A61K39/385 , A61K39/21
CPC分类号： C07K14/005 , A61K38/00 , C12N2740/16122
摘要： Peptides exhibiting anti-viral and anti-fusogenic activity are modified to provide greater stability and improved half-life in vivo. The selected peptides include fusion inhibitors DP178 and DP107 and related peptides and analogs thereof. The modified peptides are capable of forming covalent bonds with one or more blood components, preferably a mobile blood component.
摘要翻译：展示抗病毒和抗融合活性的肽被修饰以提供更大的稳定性和改善的体内半衰期。所选择的肽包括融合抑制剂DP178和DP107及其相关肽及其类似物。修饰的肽能够与一种或多种血液成分，优选移动血液成分形成共价键。

10. 发明授权

US07256253B2 Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components 失效
标题翻译：通过与血液成分缀合，保护内源性治疗肽免受肽酶活性的影响
公开(公告)号：US07256253B2
公开(公告)日：2007-08-14
申请号：US11066697
申请日：2005-02-25
申请人： Dominique P. Bridon , Alan M. Ezrin , Peter G. Milner , Darren L. Holmes , Karen Thibaudeau
发明人： Dominique P. Bridon , Alan M. Ezrin , Peter G. Milner , Darren L. Holmes , Karen Thibaudeau
IPC分类号： A61K38/00 , C07K14/00
CPC分类号： C07K19/00
摘要： A secretin or secretin derivative protected against peptidase activity. The secretin or derivative comprises a peptidic sequence and a reactive group selected from the group consisting of succinimidyl and maleimido groups capable of reacting with an amino group, hydroxyl group or thiol group on a blood component to form a stable covalent bond. The reactive group is attached at a position along the peptidic sequence that provides, when conjugated to a blood component, a higher stability against peptidase degradation than the unconjugated secretin or derivative, and therefore an increased maintenance of the therapeutic activity compared to the unconjugated secretin or derivative. Such a compound is thus effective to provide a source of secretin having a high stability against peptidases. A method for synthesizing such a compound is also described.
摘要翻译：保护蛋白酶活性的促胰液素或促胰液素衍生物。分泌素或衍生物包含肽类序列和选自能够与血液成分上的氨基，羟基或硫醇基反应形成稳定的共价键的琥珀酰亚胺基和马来酰亚胺基的反应性基团。反应性基团连接在沿着肽序列的位置，当与血液成分缀合时，其比非共轭分泌素或衍生物具有比肽酶降解更高的稳定性，因此与未缀合的促胰液素相比，治疗活性的维持得到增加衍生物。因此，这样的化合物有效地提供对肽酶具有高稳定性的促胰液素来源。还描述了合成这种化合物的方法。

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