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11. 发明申请

US20070254862A1 Pharmaceutical compositions comprising CBx cannabinoid receptor modulators and potassium channel modulators 有权
标题翻译：包含CBx大麻素受体调节剂和钾通道调节剂的药物组合物
公开(公告)号：US20070254862A1
公开(公告)日：2007-11-01
申请号：US11796716
申请日：2007-04-26
申请人： Jochen Antel , Peter-Colin Gregory , Josephus Lange , Michael Firnges , Dania Reiche
发明人： Jochen Antel , Peter-Colin Gregory , Josephus Lange , Michael Firnges , Dania Reiche
IPC分类号： A61K31/5377 , A61K31/55 , A61K31/535 , A61K31/454 , A61K31/4152 , A61K31/397 , A61K31/396
CPC分类号： A61K31/535 , A61K31/396 , A61K31/397 , A61K31/4152 , A61K31/454 , A61K31/5377 , A61K31/55 , A61K45/06 , Y10S514/866 , A61K2300/00
摘要： Described herein are pharmaceutical compositions comprising therapeutically effective quantities of (i) a KATP channel modulator; and (ii) a CBx modulator. Also described herein are methods of making and using these compositions.
摘要翻译：本文描述的是包含治疗有效量的（i）K ATP通道调节剂的药物组合物; 和（ii）CB 调制器。本文还描述了制备和使用这些组合物的方法。

12. 发明申请

US20070191357A1 METHODS OF USING POTASSIUM CHANNEL INHIBITING COMPOUNDS 审中-公开
标题翻译：使用钾通道抑制化合物的方法
公开(公告)号：US20070191357A1
公开(公告)日：2007-08-16
申请号：US11465258
申请日：2006-08-17
申请人： Jochen Antel , Peter-Colin Gregory , Michael Firnges , Dania Reiche
发明人： Jochen Antel , Peter-Colin Gregory , Michael Firnges , Dania Reiche
IPC分类号： A61K31/425
CPC分类号： A61K31/425 , A61K31/085 , A61K31/415 , A61K31/4155 , A61K31/4439 , A61K31/5383 , A61K31/549 , A61K45/06 , A61K2300/00
摘要： Described herein are methods of treating, preventing or inhibiting a variety of medical conditions by administering to subjects in need thereof an effective amount of at least one potassium Kv1.3 channel inhibiting compound which can optionally also have either or both CBx modulating properties and/or potassium K(atp) channel opening properties. Also described is the use of potassium Kv1.3 channel inhibiting compounds in a pharmaceutical composition for the prophylaxis, treatment, delayed progression, delayed onset and/or inhibition of a variety of medical conditions.
摘要翻译：本文描述的是通过向有需要的受试者施用有效量的至少一种钾K1-3.3通道抑制化合物来治疗，预防或抑制多种医学病症的方法，其可任选地还可以具有或两个CB x调制性质和/或钾（atp）通道开口性质。还描述了在药物组合物中用于预防，治疗，延迟进展，延迟发作和/或抑制各种医学病症的钾通道抑制化合物的用途。

13. 发明授权

US07763607B2 Pharmaceutical compositions comprising CBx cannabinoid receptor modulators and potassium channel modulators 有权
标题翻译：包含CBx大麻素受体调节剂和钾通道调节剂的药物组合物
公开(公告)号：US07763607B2
公开(公告)日：2010-07-27
申请号：US11796716
申请日：2007-04-26
申请人： Jochen Antel , Peter-Colin Gregory , Josephus Hubertus Maria Lange , Michael Firnges , Dania Reiche
发明人： Jochen Antel , Peter-Colin Gregory , Josephus Hubertus Maria Lange , Michael Firnges , Dania Reiche
IPC分类号： A61K31/54 , A61K31/44 , A61K31/425
CPC分类号： A61K31/535 , A61K31/396 , A61K31/397 , A61K31/4152 , A61K31/454 , A61K31/5377 , A61K31/55 , A61K45/06 , Y10S514/866 , A61K2300/00
摘要： Described herein are pharmaceutical compositions comprising therapeutically effective quantities of (i) a KATP channel modulator; and (ii) a CBx modulator. Also described herein are methods of making and using these compositions.
摘要翻译：本文描述的是药物组合物，其包含治疗有效量的（i）KATP通道调节剂; 和（ii）CBx调节剂。本文还描述了制备和使用这些组合物的方法。

14. 发明申请

US20070254863A1 Use of CBx cannabinoid receptor modulators as potassium channel modulators 审中-公开
标题翻译：使用CBx大麻素受体调节剂作为钾通道调节剂
公开(公告)号：US20070254863A1
公开(公告)日：2007-11-01
申请号：US11796740
申请日：2007-04-26
申请人： Jochen Antel , Peter-Colin Gregory , Josephus Lange , Michael Firnges , Dania Reiche
发明人： Jochen Antel , Peter-Colin Gregory , Josephus Lange , Michael Firnges , Dania Reiche
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/454
CPC分类号： A61K31/454 , A61K31/5377 , A61K31/55
摘要： Methods of treating one or more medical conditions by administering to a subject in need thereof an effective amount of a CBx modulator having KATP channel modulating properties are described herein. Also described are methods of using a CBx modulator having KATP channel modulating properties to treat one or more medical conditions.
摘要翻译：本文描述了通过向有需要的受试者施用有效量的具有K ATP通道调节特性的CB调节剂来治疗一种或多种医学病症的方法。还描述了使用具有K + ATP通道调节性质的CB调节剂治疗一种或多种医学病症的方法。

15. 发明授权

US06001833A Urea derivatives 有权
标题翻译：尿素衍生物
公开(公告)号：US06001833A
公开(公告)日：1999-12-14
申请号：US141623
申请日：1998-08-27
申请人： Daniel Jasserand , Samuel David , Jochen Antel , Reinhard Brueckner , Christian Eeckhout , Gerhard-Wilhelm Bielenberg
发明人： Daniel Jasserand , Samuel David , Jochen Antel , Reinhard Brueckner , Christian Eeckhout , Gerhard-Wilhelm Bielenberg
IPC分类号： C07D403/06 , A61K31/495 , A61K31/496 , A61P1/00 , A61P29/00 , A61P43/00 , C07D209/00 , C07D209/14 , C07D241/00 , A61K31/47
CPC分类号： C07D209/14 , Y02P20/55
摘要： Compounds of Formula I ##STR1## wherein R.sup.1 is hydrogen or lower alkyl,R.sup.2 is hydrogen or halogen andR.sup.3 is hydrogen or lower alkoxy,and their pharmacologically acceptable acid addition salts and pharmaceutical compositions containing these compounds and also processes for the preparation of these compounds. Pharmaceutical composition containing these compounds are suitable, for example, for treating functional and inflammatory disorders of the gastrointestinal tract.
摘要翻译：式Ⅰ化合物，其中R 1是氢或低级烷基，R 2是氢或卤素，R 3是氢或低级烷氧基，以及它们的药学上可接受的酸加成盐和含有这些化合物的药物组合物，以及制备这些化合物的方法。含有这些化合物的药物组合物适用于例如治疗胃肠道的功能性和炎症性疾病。

16. 发明授权

US07238470B2 Method of treating or inhibiting obesity 有权
标题翻译：治疗或抑制肥胖症的方法
公开(公告)号：US07238470B2
公开(公告)日：2007-07-03
申请号：US10785042
申请日：2004-02-25
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： 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。

17. 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。

18. 发明授权

US08058264B2 Pharmaceutical compositions comprising CB1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions 有权
标题翻译：包含CB1大麻素受体拮抗剂和用于治疗肥胖症和相关病症的钾通道开放剂的药物组合物
公开(公告)号：US08058264B2
公开(公告)日：2011-11-15
申请号：US11257056
申请日：2005-10-25
申请人： Michael Firnges , Peter-Colin Gregory , Jochen Antel , Josephus Hubertus Maria Lange , Harald Waldeck
发明人： Michael Firnges , Peter-Colin Gregory , Jochen Antel , Josephus Hubertus Maria Lange , Harald Waldeck
IPC分类号： A01N33/26 , A61K31/535
CPC分类号： A61K31/00 , A61K31/40 , A61K31/415 , A61K31/4152 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/54 , A61K31/655 , A61K45/06 , G01N33/6872 , G01N33/948 , G01N2500/00 , G01N2800/042 , G01N2800/044 , A61K2300/00
摘要： Described is a novel combination therapy for diabetes mellitus type I and/or for obesity and its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, by administering a combination of at least one KATP channel opener as a first active agent and at least one CB1 cannabinoid receptor antagonist as a second active agent. The invention is further directed to such novel combination therapy wherein a dually acting compound with combined KATP channel opening and CB1 antagonistic properties is used. The invention also relates to novel pharmaceutical compositions comprising KATP channel openers and CB1 antagonists and the use of said pharmaceutical compositions in the treatment, delayed progression, delayed onset of and/or inhibition of diabetes mellitus type 1, and the prophylaxis and treatment, of obesity as well as the prophylaxis, treatment, delayed onset and/or inhbition of its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, in mammals and humans. The invention is further directed to such novel pharmaceutical compositions comprising a dually acting compound with combined KATP channel opening and CB1 antagonistic properties.
摘要翻译：描述了通过施用组合来描述I型糖尿病和/或用于肥胖及其伴随和/或继发疾病或病症，特别是代谢综合征和/或综合征X和/或II型糖尿病的新型联合治疗的至少一种KATP通道开放剂作为第一活性剂和至少一种CB1大麻素受体拮抗剂作为第二活性剂。本发明进一步涉及这种新型联合治疗，其中使用具有组合的KATP通道开放和CB1拮抗性质的双作用化合物。本发明还涉及包含KATP通道开放剂和CB1拮抗剂的新型药物组合物，以及所述药物组合物在治疗，延迟进展，延迟发作和/或抑制1型糖尿病以及预防和治疗肥胖症中的用途以及其伴随和/或继发疾病或病症，特别是哺乳动物和人类的代谢综合征和/或综合征X和/或II型糖尿病的预防，治疗，延迟发作和/或吸收。本发明还涉及这种新型药物组合物，其包含具有组合的KATP通道开口和CB1拮抗性质的双作用化合物。

19. 发明授权

US07282325B2 Method of preparing pharmaceutical compositions 有权
标题翻译：制备药物组合物的方法
公开(公告)号：US07282325B2
公开(公告)日：2007-10-16
申请号：US10785043
申请日：2004-02-25
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： 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。

20. 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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