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1. 发明授权

US08642658B2 Treatment of neural diseases or conditions 有权
标题翻译：治疗神经疾病或病症
公开(公告)号：US08642658B2
公开(公告)日：2014-02-04
申请号：US12918787
申请日：2009-02-20
申请人： Danuta Radzioch , Samuel David , Ruben Lopez-Vales , Thomas Skinner
发明人： Danuta Radzioch , Samuel David , Ruben Lopez-Vales , Thomas Skinner
IPC分类号： A61K31/16 , C07C233/00
CPC分类号： A61K31/167 , A61K45/06 , A61K49/0008
摘要： Compounds, methods, uses, compositions, kits and packages for the prevention and/or treatment of neural injury or a neurodegenerative disease, based on the use of a retinoic acid derivative, such as fenretinide, and/or analogs, derivatives, pro-drugs, precursors thereof, and/or salts thereof, are described.
摘要翻译：基于视黄酸衍生物如芬维A胺和/或类似物衍生物，前药的用途，用于预防和/或治疗神经损伤或神经变性疾病的化合物，用途，组合物，试剂盒和包装，其前体和/或其盐。

2. 发明申请

US20100331417A1 TREATMENT OF NEURAL DISEASES OR CONDITIONS 有权
标题翻译：治疗神经疾病或病症
公开(公告)号：US20100331417A1
公开(公告)日：2010-12-30
申请号：US12918787
申请日：2009-02-20
申请人： Danuta Radzioch , Samuel David , Ruben Lopez-Vales , Thomas Skinner
发明人： Danuta Radzioch , Samuel David , Ruben Lopez-Vales , Thomas Skinner
IPC分类号： A61K31/164 , A61P25/00
CPC分类号： A61K31/167 , A61K45/06 , A61K49/0008
摘要： Compounds, methods, uses, compositions, kits and packages for the prevention and/or treatment of neural injury or a neurodegenerative disease, based on the use of a retinoic acid derivative, such as fenretinide, and/or analogs, derivatives, pro-drugs, precursors thereof, and/or salts thereof, are described.
摘要翻译：基于视黄酸衍生物如芬维A胺和/或类似物衍生物，前药的用途，用于预防和/或治疗神经损伤或神经变性疾病的化合物，用途，组合物，试剂盒和包装，其前体和/或其盐。

3. 发明授权

US08420852B2 Phospholipase A2 inhibitors and their use in treating neurological injury and disease 失效
标题翻译：磷脂酶A2抑制剂及其在治疗神经损伤和疾病中的应用
公开(公告)号：US08420852B2
公开(公告)日：2013-04-16
申请号：US12666773
申请日：2008-07-03
申请人： Edward A. Dennis , Daren Stephens , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokotou , Efrosini Barbayianni , Victoria Magrioti
发明人： Edward A. Dennis , Daren Stephens , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokotou , Efrosini Barbayianni , Victoria Magrioti
IPC分类号： C07C229/00 , A01N37/12 , A01N37/44
CPC分类号： C07C235/80
摘要： Phospholipase A2 (PLA2) forms are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2). Pharmaceutical compositions of compounds having cPLA2 inhibitory activity (but not iPLA2 or sPLA2 inhibitory activity) are useful in treating multiple sclerosis, while compositions of compounds having sPLA2 inhibitory activity (as well as iPLA2 and CPLA2 activity) are useful in treating spinal cord injuries (with related functional recovery).
摘要翻译：磷脂酶A2（PLA2）形式在脊髓中表达，其抑制诱导有效的抗痛觉过敏。提供PLA2抑制剂化合物，其包括由具有烃尾部的2-氧代酰胺和四碳系链组成的共同基序。化合物阻断IVA类钙依赖性PLA2（cPLA2）和/或VIA钙独立PLA2（iPLA2）和/或V组分泌的PLA2（sPLA2）。具有cPLA2抑制活性（但不是iPLA2或sPLA2抑制活性）的化合物的药物组合物可用于治疗多发性硬化，而具有sPLA2抑制活性的化合物（以及iPLA2和CPLA2活性）可用于治疗脊髓损伤（具有相关的功能恢复）。

4. 发明申请

US20110105610A1 Phospholipase A2 Inhibitors and their Use in Treating Neurological Injury and Disease 失效
标题翻译：磷脂酶A2抑制剂及其在治疗神经损伤和疾病中的应用
公开(公告)号：US20110105610A1
公开(公告)日：2011-05-05
申请号：US12666773
申请日：2008-07-03
申请人： Edward A. Dennis , Daren Stephen , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokoton , Efrosini Barbayianni , Victoria Magrioti
发明人： Edward A. Dennis , Daren Stephen , Samuel David , Ruben Lopez-Vales , Athena Kalyvas , George Kokotos , Violetta Constantinou-Kokoton , Efrosini Barbayianni , Victoria Magrioti
IPC分类号： A61K31/221 , C07C229/22 , C12N5/071 , A61K31/195 , A61P25/00
CPC分类号： C07C235/80
摘要： Phospholipase A2 (PLA2) forms are expressed in spinal cord whose inhibition induces a potent antihyperalgesia. PLA2 inhibitor compounds are provided that include a common motif consisting of a 2-oxoamide with a hydrocarbon tail and a four carbon tether. The compounds block Group IVA calcium dependent PLA2 (cPLA2) and/or Group VIA calcium independent PLA2 (iPLA2) and/or Group V secreted PLA2 (sPLA2). Pharmaceutical compositions of compounds having cPLA2 inhibitory activity (but not iPLA2 or sPLA2 inhibitory activity) are useful in treating multiple sclerosis, while compositions of compounds having sPLA2 inhibitory activity (as well as iPLA2 and CPLA2 activity) are useful in treating spinal cord injuries (with related functional recovery).
摘要翻译：磷脂酶A2（PLA2）形式在脊髓中表达，其抑制诱导有效的抗痛觉过敏。提供PLA2抑制剂化合物，其包括由具有烃尾部的2-氧代酰胺和四碳系链组成的共同基序。化合物阻断IVA类钙依赖性PLA2（cPLA2）和/或VIA钙独立PLA2（iPLA2）和/或V组分泌的PLA2（sPLA2）。具有cPLA2抑制活性（但不是iPLA2或sPLA2抑制活性）的化合物的药物组合物可用于治疗多发性硬化，而具有sPLA2抑制活性的化合物（以及iPLA2和CPLA2活性）可用于治疗脊髓损伤（具有相关的功能恢复）。

5. 发明申请

US20100048727A1 PERFLUOROKETONE COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：全氟酮酮化合物及其用途
公开(公告)号：US20100048727A1
公开(公告)日：2010-02-25
申请号：US12594579
申请日：2008-04-04
申请人： Samuel David , Athena Kalyvas , Ruben Lopez-Vales , George Kokotos , Violetta Constantinou-Kokotou , Constantinos Baskakis , Christoforos G. Kokotos , Edward A. Dennis , Daren Stephens
发明人： Samuel David , Athena Kalyvas , Ruben Lopez-Vales , George Kokotos , Violetta Constantinou-Kokotou , Constantinos Baskakis , Christoforos G. Kokotos , Edward A. Dennis , Daren Stephens
IPC分类号： A61K31/121 , C12N5/00 , A61K31/12 , C07C49/11 , C07C45/54 , C07C49/105 , C07C49/115 , C07C49/04 , A61P25/00 , A61P29/00
CPC分类号： C07C49/233 , C07C49/167 , C07C49/245 , C07C49/255
摘要： Novel perfluoroketone compounds of formula [I] and [Ia] are described. Also described are uses thereof, such as for inhibition of phospholipase A2 activity. Therapeutic uses thereof are also described, such as for the treatment of neural conditions and/or inflammatory conditions, such as demyelinating (e.g., multiple sclerosis) and neural injury (e.g., spinal cord injury).
摘要翻译：描述了式[I]和[Ia]的新型全氟酮化合物。还描述了其用途，例如用于抑制磷脂酶A2活性。还描述了其治疗用途，例如用于治疗神经病症和/或炎性病症，例如脱髓鞘（例如多发性硬化症）和神经损伤（例如脊髓损伤）。

6. 发明授权

US06946243B2 Method of identifying compounds suitable for treatment and/or prophylaxis of obesity 有权
标题翻译：鉴定适合于治疗和/或预防肥胖症的化合物的方法
公开(公告)号：US06946243B2
公开(公告)日：2005-09-20
申请号：US09907440
申请日：2001-07-18
申请人： Johannes Hebebrand , Jochen Antel , Ulf Preuschoff , Samuel David , Holger Sann , Michael Weske
发明人： Johannes Hebebrand , Jochen Antel , Ulf Preuschoff , Samuel David , Holger Sann , Michael Weske
IPC分类号： A61K31/34 , C12Q1/527 , G01N33/68 , C12Q1/00
CPC分类号： A61K31/34 , C12Q1/527 , G01N33/6893 , G01N2800/044
摘要： A method for the discovery of compounds suitable for the treatment and/or prophylaxis of obesity, in which the ability of the test compounds to inhibit de novo lipogenesis in mammals and/or man is determined. The use of compounds which are capable of inhibiting de novo lipogenesis in mammals, and which are substantially free of effects directed towards the CNS, for the preparation of pharmaceutical compositions for the treatment and/or prophylaxis of obesity, as well as for the treatment and/or inhibition of obesity, are also described.
摘要翻译：发现适用于治疗和/或预防肥胖症的化合物的方法，其中测定化合物在哺乳动物和/或人中抑制新生脂肪生成的能力。使用能够在哺乳动物中抑制从头脂肪生成并且基本上没有针对CNS的作用的化合物用于制备用于治疗和/或预防肥胖症的药物组合物，以及用于治疗和/ /或抑制肥胖。

7. 发明授权

US4714709A N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine derivatives and medical compositions thereof 失效
标题翻译： N-（2,10-二氧杂 - 三环 - [5,3,1,03,8] - 十一烷-5-基） - 色胺衍生物及其医药组合物
公开(公告)号：US4714709A
公开(公告)日：1987-12-22
申请号：US653707
申请日：1984-09-24
申请人： Peter W. Thies , Samuel David , Ulrich Kuehl , Gerd Buschmann , Peter Flecker
发明人： Peter W. Thies , Samuel David , Ulrich Kuehl , Gerd Buschmann , Peter Flecker
IPC分类号： A61K31/35 , A61K31/357 , A61P9/12 , C07D319/00 , C07D493/08 , A61K31/40 , C07D405/12
CPC分类号： C07D493/08
摘要： N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine compounds corresponding to the formula ##STR1## with blood-pressure lowering effects, a method of producing such compounds and pharmaceutical compositions incorporating such compounds, wherein R.sub.1 is hydrogen, a benzyl or lower alkyl group; R.sub.2 is a lower alkyl or lower alkanoyl group; R.sub.3 is hydrogen or a lower alkyl group; R.sub.4 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; R.sub.5 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; and A and B either are both hydrogen or together represent a bond between their respective carbons.
摘要翻译：对应于具有降血压效果的式“IMAGE”I的N-（2,10-二氧杂 - 三环 - [5,3,1,03,8] - 十一烷-5-基） - 色胺化合物，制备这样的化合物和掺入这种化合物的药物组合物，其中R 1是氢，苄基或低级烷基; R2是低级烷基或低级烷酰基; R3是氢或低级烷基; R4是氢，苄氧基，羟基或低级烷氧基; R5是氢，苄氧基，羟基或低级烷氧基; 并且A和B既可以是氢，也可以一起表示它们各自的碳之间的键。

8. 发明授权

US4207331A 2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives and pharmaceutical compositions thereof 失效
标题翻译： 2,9-二氧三环[4,3,1,03,7]癸烷衍生物及其药物组合物
公开(公告)号：US4207331A
公开(公告)日：1980-06-10
申请号：US904742
申请日：1978-05-11
申请人： Peter W. Thies , Akiji Asai , Samuel David
发明人： Peter W. Thies , Akiji Asai , Samuel David
IPC分类号： C07D493/08 , C07D319/08 , A61K31/335
CPC分类号： C07D493/08
摘要： New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group one of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygen one of R.sub.4 and R.sub.5 is hydrogen and the other represents alkyloxy or aralkyloxy y and y' each represent hydrogen or jointly form a bond and their pharmacologically acceptable salts, as well as pharmaceutical formulations thereof.
摘要翻译：公开了新的2,9-二氧杂三环[4,3,1,03,7]癸烷衍生物，其被C3位上的氨基甲基取代，并且其表现出镇静剂，特别是睡眠改善性质，图像（I）其中R1表示R2中的一个，R3是氢，另一个表示羟基酰氧基或氨基甲酰氧基或R2和R3共同表示氧，R4和R5之一是氢，另一个表示烷氧基或芳烷氧基y和y “各自表示氢或共同形成键及其药理学上可接受的盐，以及其药物制剂。

9. 发明申请

US20060058225A1 Used of inhibitors of phospholipase a2 for the treatment, prevention or diagnosis of neural inflammatory or demyelinating disease 审中-公开
标题翻译：用于磷脂酶a2的抑制剂用于治疗，预防或诊断神经性炎症或脱髓鞘疾病
公开(公告)号：US20060058225A1
公开(公告)日：2006-03-16
申请号：US10516241
申请日：2003-05-30
申请人： Samuel David , Athena Kalyvas
发明人： Samuel David , Athena Kalyvas
IPC分类号： A61K38/16 , A61K31/739 , A61K48/00 , A61K31/66 , A61K31/12
CPC分类号： G01N33/6896 , A61K31/20 , A61K38/1709 , C12Q1/44 , G01N2333/918 , G01N2500/00
摘要： The present invention provides methods of preventing and treating neural inflammatory or demyelinating disease, such as multiple sclerosis, via an inhibition of the activity or expression of phospholipase A2. The invention further relates to methods of identifying phospholipase A2 inhibitors and their use thereof for the prevention and/or treatment of neural inflammatory or demyelinating disease. An observed increase in the amount of phospholipase A2 in neural lesions in the EAE animal model system indicates that elevated phospholipase A2 activity or levels correlate with neural inflammatory or demyelinating disease. Therefore, in a further aspect the invention provides methods for the diagnosis and prognostication of neural inflammatory or demyelinating disease, such as multiple sclerosis.
摘要翻译：本发明通过抑制磷脂酶A 2活性或表达来提供预防和治疗神经性炎性或脱髓鞘疾病如多发性硬化的方法。本发明还涉及鉴定磷脂酶A 2抑制剂及其在预防和/或治疗神经性炎性或脱髓鞘疾病中的用途的方法。在EAE动物模型系统中观察到的神经损伤中磷脂酶A 2 N 2的量的增加表明升高的磷脂酶A 2活性或水平与神经性炎症或脱髓鞘疾病相关。因此，在另一方面，本发明提供了用于神经炎性或脱髓鞘疾病如多发性硬化症的诊断和预后的方法。

10. 发明授权

US6040303A 7-phenyl-1, 4-diazepane compounds, process for their preparation, and pharmaceutical compositions containing them 有权
标题翻译： 7-苯基-1,4-二氮杂环丁烷化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US6040303A
公开(公告)日：2000-03-21
申请号：US141312
申请日：1998-08-27
申请人： Samuel David , Jochen Antel , Reinhard Brueckner , Dieter Ziegler , Christian Eeckhout , Gerhard-Wilhelm Bielenberg , Michael Peck
发明人： Samuel David , Jochen Antel , Reinhard Brueckner , Dieter Ziegler , Christian Eeckhout , Gerhard-Wilhelm Bielenberg , Michael Peck
IPC分类号： A61K31/55 , A61P1/00 , A61P43/00 , C07D243/08
CPC分类号： C07D243/08 , Y02P20/55
摘要： Neurokinin-antagonistic compounds corresponding to formula I: ##STR1## in which R.sup.1 is hydrogen or lower alkyl,R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.3 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, orR.sup.2 and R.sup.3 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring,R.sup.4 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, andR.sup.5 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, orR.sup.4 and R.sup.5 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring,R.sup.6 is lower alkyl, halogen or trifluoromethyl,R.sup.7 is lower alkyl, halogen or trifluoromethyl,A is a --(CH.sub.2).sub.n -- group in which n represents an integer from 1 to 3, or an --NH--(CH.sub.2).sub.m -- group in which m represents an integer from 2 to 3, andB is an alkylene chain with 1 to 3 carbon atoms optionally substituted by lower alkyl,and physiologically acceptable salts thereof and processes for the preparation of these compounds.
摘要翻译：对应于式I的神经激肽拮抗化合物：其中R1是氢或低级烷基，R2是氢，低级烷基，低级烷氧基，卤素或三氟甲基，R3是氢，低级烷基，低级烷氧基，卤素或三氟甲基，或R2和 R3一起是具有1至2个碳原子的亚烷基二氧基，与苯环的相邻碳原子键合，R4是氢，低级烷基，低级烷氧基，卤素或三氟甲基，R5是氢，低级烷基，低级烷氧基，卤素或三氟甲基，或R4和R5一起是具有1至2个碳原子的亚烷基二氧基，与苯环的相邻碳原子键合，R6是低级烷基，卤素或三氟甲基，R7是低级烷基，卤素或三氟甲基，A是 - （CH2）n - 其中n表示1至3的整数的基团，或其中m表示2至3的整数的-NH-（CH 2）m - 基团，B是具有1至3个碳原子的亚烷基链，其任选被低级烷基和其生理上可接受的盐 d制备这些化合物的方法。

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