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1. 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.

2. 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。

3. 发明申请

US20130040987A1 Stereoisomeric Compounds and Methods for the Treatment of Gastrointestinal and Central Nervous System Disorders 有权
标题翻译：立体异构化合物和治疗胃肠道和中枢神经系统疾病的方法
公开(公告)号：US20130040987A1
公开(公告)日：2013-02-14
申请号：US13370853
申请日：2012-02-10
申请人： Ian Irwin , Monica Palme , Cyrus Becker , Pascal Druzgala
发明人： Ian Irwin , Monica Palme , Cyrus Becker , Pascal Druzgala
IPC分类号： A61K31/439 , A61P1/08 , A61P1/00 , A61P1/10 , A61P1/04 , C07D453/02 , A61P1/14
CPC分类号： C07D453/02 , C07D401/04
摘要： The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.
摘要翻译：本发明提供式（X）的立体异构体化合物：其中变量如本文所定义，以及用于安全和有效治疗各种胃肠道疾病的组合物，包括但不限于胃轻瘫，胃食管反流和相关病症。本发明的化合物还可用于治疗涉及中枢神经系统的多种病症。

4. 发明授权

US08093237B2 Dibenzo[b,f][1,4]oxazapine compounds 有权
标题翻译：二苯并[b，f] [1,4]恶唑氮化合物
公开(公告)号：US08093237B2
公开(公告)日：2012-01-10
申请号：US12047858
申请日：2008-03-13
申请人： Cyrus Becker , Courtney Rubens , Jason Adams , Monica Palme , Pascal Druzgala
发明人： Cyrus Becker , Courtney Rubens , Jason Adams , Monica Palme , Pascal Druzgala
IPC分类号： A61P25/00 , A61K31/553 , C07D267/02
CPC分类号： C07D413/04 , C07D405/14 , C07D453/02
摘要： The present invention relates to 11-(piperazin-1-yl)dibenzo[b,f][1,4 ]oxazapine compounds of the formula: where the variables are as defined herein, their salts and pharmaceutically acceptable compositions thereof. Methods of preparing these compounds are also described. These compounds may be used in the treatment of disorders such as schizophrenia, treatment resistant schizophrenia, bipolar disorder, psychotic depression, treatment resistant depression, schizophrenia-associated depression, treatment resistant OCD, autism, senile psychosis, psychotic dementia, L-DOPA induced psychosis, psychogenic polydipsia, psychotic symptoms of neurological disorders, sleep disorders.
摘要翻译：本发明涉及下式的11-（哌嗪-1-基）二苯并[b，f] [1,4]恶唑氮化合物：其中变量如本文所定义，其盐和药学上可接受的组合物。还描述了制备这些化合物的方法。这些化合物可用于治疗精神分裂症，治疗耐药性精神分裂症，双相性精神障碍，精神病抑郁症，治疗耐药性抑郁症，精神分裂症相关抑郁症，治疗耐药性OCD，孤独症，老年性精神病，精神病性痴呆，L-DOPA诱发的精神病，心理性多饮，精神病性神经障碍症状，睡眠障碍。

5. 发明申请

US20050245603A1 Materials and methods for treating coagulation disorders 有权
标题翻译：用于治疗凝血障碍的材料和方法
公开(公告)号：US20050245603A1
公开(公告)日：2005-11-03
申请号：US11101714
申请日：2005-04-08
申请人： Pascal Druzgala , Cyrus Becker
发明人： Pascal Druzgala , Cyrus Becker
IPC分类号： C07D311/56 , A61K31/366 , C07D311/02
CPC分类号： C07D311/56
摘要： The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.
摘要翻译：本发明提供式I的抗凝血剂化合物及其药学上可接受的盐，其中R 1，R 3，n和Ar如本文所定义。本发明的化合物可用于治疗危险人群，从而缓解症状，改善生活质量，预防急性和长期并发症，降低死亡率和治疗伴随的疾病。本发明还包括包含本发明化合物和盐的药物组合物，以及使用本发明化合物，盐和组合物的方法。

6. 发明授权

US07501436B2 5-HT3 receptor antagonists and methods of use 失效
标题翻译： 5-HT 3受体拮抗剂和使用方法
公开(公告)号：US07501436B2
公开(公告)日：2009-03-10
申请号：US11551562
申请日：2006-10-20
申请人： Xiaoming Zhang , Jurg R. Pfister , Cyrus Becker , Pascal Druzgala
发明人： Xiaoming Zhang , Jurg R. Pfister , Cyrus Becker , Pascal Druzgala
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D403/06 , C07D451/14 , C07D471/04
摘要： The subject invention provides useful and novel 5-HT3 antagonists. The subject invention also provides methods for synthesizing the compounds of invention. The invention also provides methods for the treatment of irritable bowel syndrome and other such conditions.
摘要翻译：本发明提供有用的和新颖的5-HT 3拮抗剂。本发明还提供了合成本发明化合物的方法。本发明还提供了治疗肠易激综合征和其他此类病症的方法。

7. 发明授权

US07285671B2 Materials and methods for treating coagulation disorders 有权
标题翻译：用于治疗凝血障碍的材料和方法
公开(公告)号：US07285671B2
公开(公告)日：2007-10-23
申请号：US11467813
申请日：2006-08-28
申请人： Pascal Druzgala , Cyrus Becker
发明人： Pascal Druzgala , Cyrus Becker
IPC分类号： C07D311/002
CPC分类号： C07D311/56
摘要： The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.
摘要翻译：本发明提供式I的抗凝血剂化合物及其药学上可接受的盐，其中R 1，R 3，n和Ar如本文所定义。本发明的化合物可用于治疗危险人群，从而缓解症状，改善生活质量，预防急性和长期并发症，降低死亡率和治疗伴随的疾病。本发明还包括包含本发明化合物和盐的药物组合物，以及使用本发明化合物，盐和组合物的方法。

8. 发明申请

US20070060640A1 Antiarrhythmic Precursor Compounds, Methods Of Synthesis And Methods Of Use 有权
标题翻译：抗心律失常前体化合物，合成方法和使用方法
公开(公告)号：US20070060640A1
公开(公告)日：2007-03-15
申请号：US11457719
申请日：2006-07-14
申请人： Pascal Druzgala , Jien-Heh Tien , Arthur Cooper , Cyrus Becker
发明人： Pascal Druzgala , Jien-Heh Tien , Arthur Cooper , Cyrus Becker
IPC分类号： A61K31/366 , C07D493/02
CPC分类号： C07D307/80 , C07D493/04
摘要： 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.
摘要翻译：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。

9. 发明授权

US08138204B2 Stereoisomeric compounds and methods for the treatment of gastrointestinal and central nervous system disorders 有权
标题翻译：立体异构化合物和治疗胃肠道和中枢神经系统疾病的方法
公开(公告)号：US08138204B2
公开(公告)日：2012-03-20
申请号：US11778315
申请日：2007-07-16
申请人： Ian Irwin , Monica Palme , Cyrus Becker , Pascal Druzgala
发明人： Ian Irwin , Monica Palme , Cyrus Becker , Pascal Druzgala
IPC分类号： A61K31/4468 , A61K31/439
CPC分类号： C07D453/02 , C07D401/04
摘要： The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.
摘要翻译：本发明提供式（X）的立体异构体化合物：其中变量如本文所定义，以及用于安全和有效治疗各种胃肠道疾病的组合物，包括但不限于胃轻瘫，胃食管反流和相关病症。本发明的化合物还可用于治疗涉及中枢神经系统的多种病症。

10. 发明授权

US07932405B2 Halogenated ester derivatives of coumarins for the treatment of coagulation disorders 有权
标题翻译：香豆素的卤代酯衍生物用于治疗凝血障碍
公开(公告)号：US07932405B2
公开(公告)日：2011-04-26
申请号：US12268109
申请日：2008-11-10
申请人： Pascal Druzgala , Cyrus Becker
发明人： Pascal Druzgala , Cyrus Becker
IPC分类号： C07D311/56 , A61K31/352
CPC分类号： C07D311/56
摘要： The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.
摘要翻译：本发明提供了式I的抗凝血剂化合物及其药学上可接受的盐，其中R 1，R 3，n和Ar如本文所定义。本发明的化合物可用于治疗危险人群，从而缓解症状，改善生活质量，预防急性和长期并发症，降低死亡率和治疗伴随的疾病。本发明还包括包含本发明化合物和盐的药物组合物，以及使用本发明化合物，盐和组合物的方法。

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