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1. 发明授权

US07273860B2 Method and pharmaceutical compositions for treating or inhibiting renal dysfunctions, diseases or disorders, particularly in diabetic patients 失效
标题翻译：用于治疗或抑制肾功能异常，疾病或病症，特别是糖尿病患者的方法和药物组合物
公开(公告)号：US07273860B2
公开(公告)日：2007-09-25
申请号：US10988847
申请日：2004-11-16
申请人： Dirk Thormaehlen , Berthold Hocher , Harald Waldeck
发明人： Dirk Thormaehlen , Berthold Hocher , Harald Waldeck
IPC分类号： A61K31/55
CPC分类号： A61K31/55
摘要： Treatment and/or inhibition of renal dysfunction, disease or disorder in larger mammals, and particularly in humans, especially in human patients suffering from diabetes, using benzazepine-N-acetic acid derivatives which contain an oxo-group in the α-position to the nitrogen atom and are substituted in position 3 by a 1-(carboxyalkyl)cyclopentylcarbonylamino radical, and/or salts or biolabile esters or physiologically acceptable solvates thereof, and production of pharmaceutical compositions and products suitable for treatment and/or inhibition of renal dysfunction, disease or disorder, particularly in diabetic patients, but also in patients with syndrome X or in patients with a renal dysfunction, disease and/or disorder, which patients are additionally hypertensive, obese, hyperglycemic and/or subject to a metabolic disorder.
摘要翻译：在大型哺乳动物，特别是人，特别是患有糖尿病的人类患者中，使用含有氧代基的苯并氮杂-N-乙酸衍生物，在α位置的治疗和/或抑制肾功能障碍，疾病或病症氮原子，并且在3位上被1-（羧基烷基）环戊基羰基氨基取代，和/或其盐或生物不稳定酯或其生理学上可接受的溶剂合物，以及适于治疗和/或抑制肾功能障碍的药物组合物和产品的生产或障碍，特别是在糖尿病患者中，而且在患有综合征X或患有肾功能障碍，疾病和/或障碍的患者中，该患者另外是高血压，肥胖，高血糖和/或经历代谢紊乱。

2. 发明申请

US20050261292A1 Pharmaceutical composition containing N-sulfamoyl-N'-arylpiperazines for the treatment or inhibition of obesity and related conditions 审中-公开
标题翻译：含有N-氨磺酰基-N'-芳基哌嗪的药物组合物用于治疗或抑制肥胖症及相关病症
公开(公告)号：US20050261292A1
公开(公告)日：2005-11-24
申请号：US11130268
申请日：2005-05-17
申请人： Jochen Antel , Michael Firnges , Peter-Colin Gregory , Uwe Reinecker , Uwe Schoen , Harald Waldeck , Michael Wurl , Dania Reiche
发明人： Jochen Antel , Michael Firnges , Peter-Colin Gregory , Uwe Reinecker , Uwe Schoen , Harald Waldeck , Michael Wurl , Dania Reiche
IPC分类号： A61K31/496 , A61K31/497 , A61K31/501 , A61K31/519 , A61K31/53 , C07D213/74 , C07D295/26 , C07D43/02
CPC分类号： A61K31/496 , A61K31/497 , A61K31/501 , A61K31/519 , A61K31/53 , C07D213/74 , C07D295/26
摘要： The present invention relates to the use of known and novel N-sulfamoyl-N′-arylpiperazines corresponding to Formula I and their physiologically compatible acid addition salts for the treatment or inhibition of obesity and related conditions.
摘要翻译：本发明涉及对应于式I的已知和新型N-氨磺酰基-N'-芳基哌嗪及其生理相容的酸加成盐在治疗或抑制肥胖症及相关病症中的用途。

3. 发明申请

US20050137183A1 Method and pharmaceutical compositions for treating or inhibiting renal dysfunctions, diseases or disorders, particularly in diabetic patients 失效
标题翻译：用于治疗或抑制肾功能异常，疾病或病症，特别是糖尿病患者的方法和药物组合物
公开(公告)号：US20050137183A1
公开(公告)日：2005-06-23
申请号：US10988847
申请日：2004-11-16
申请人： Dirk Thormaehlen , Berthold Hocher , Harald Waldeck
发明人： Dirk Thormaehlen , Berthold Hocher , Harald Waldeck
IPC分类号： A61K31/55
CPC分类号： A61K31/55
摘要： Treatment and/or inhibition of renal dysfunction, disease or disorder in larger mammals, and particularly in humans, especially in human patients suffering from diabetes, using benzazepine-N-acetic acid derivatives which contain an oxo-group in the α-position to the nitrogen atom and are substituted in position 3 by a 1-(carboxyalkyl)cyclopentylcarbonylamino radical, and/or salts or biolabile esters or physiologically acceptable solvates thereof, and production of pharmaceutical compositions and products suitable for treatment and/or inhibition of renal dysfunction, disease or disorder, particularly in diabetic patients, but also in patients with syndrome X or in patients with a renal dysfunction, disease and/or disorder, which patients are additionally hypertensive, obese, hyperglycemic and/or subject to a metabolic disorder.
摘要翻译：在大型哺乳动物，特别是人，特别是患有糖尿病的人类患者中，使用含有氧代基的苯并氮杂-N-乙酸衍生物，在α位置的治疗和/或抑制肾功能障碍，疾病或病症氮原子，并且在3位上被1-（羧基烷基）环戊基羰基氨基取代，和/或其盐或生物不稳定酯或其生理学上可接受的溶剂合物，以及适于治疗和/或抑制肾功能障碍的药物组合物和产品的生产或障碍，特别是在糖尿病患者中，而且在患有综合征X或患有肾功能障碍，疾病和/或病症的患者中，该患者另外是高血压，肥胖，高血糖和/或经历代谢紊乱。

4. 发明授权

US5952327A Phosphonic acid-substituted benzazepinone-n-acetic acid derivatives process for their preparation and pharmaceutical compositions comprising them 有权
标题翻译：膦酸取代的苯并氮杂-乙酸衍生物的制备方法和包含它们的药物组合物
公开(公告)号：US5952327A
公开(公告)日：1999-09-14
申请号：US189796
申请日：1998-11-12
申请人： Harald Waldeck , Joerg Meil , Dirk Thormaehlen , Michael Wurl
发明人： Harald Waldeck , Joerg Meil , Dirk Thormaehlen , Michael Wurl
IPC分类号： A61K31/675 , A61K31/00 , A61K31/55 , A61K38/00 , A61P9/00 , A61P9/04 , A61P9/12 , C07D223/16 , C07F9/38 , C07F9/40 , C07F9/553 , C07K5/06 , C07D223/32
CPC分类号： C07K5/06191 , A61K38/00 , Y02P20/55
摘要： Compounds having NEP-inhibitory activity, corresponding to the formula I in whichR.sup.1 is hydrogen or a group forming a biolabile phosphonic acid ester,R.sup.2 is hydrogen or a group forming a biolabile phosphonic acid ester andR.sup.3 is hydrogen or a group forming a biolabile carboxylic acid esterand physiologically acceptable salts of acids of formula I, and pharmaceutical compositions comprising these compounds.
摘要翻译：具有NEP-抑制活性的化合物，其对应于其中R 1是氢的式I或形成可生物不稳定的膦酸酯的基团，R 2是氢或形成可生物不稳定的膦酸酯的基团，并且R 3是氢或形成生物不稳定羧酸的基团酸酯和式I的酸的生理上可接受的盐，以及包含这些化合物的药物组合物。

5. 发明授权

US5783573A Pharmaceuticals which promote gastrointestinal blood circulation 失效
标题翻译：促进胃肠道血液循环的药物
公开(公告)号：US5783573A
公开(公告)日：1998-07-21
申请号：US929114
申请日：1997-09-15
申请人： Susanna Rozsa , Julius Gy. Papp , Dirk Thormaehlen , Harald Waldeck
发明人： Susanna Rozsa , Julius Gy. Papp , Dirk Thormaehlen , Harald Waldeck
IPC分类号： C07D223/16 , A61K31/55 , A61P1/00
CPC分类号： A61K31/55
摘要： The use is described of compounds of the general formula I ##STR1## wherein R.sup.1 represents a phenyl-lower alkyl group which can optionally be substituted in the phenyl ring by lower alkyl, lower alkoxy or halogen, or represents a naphthyl-lower alkyl group, R.sup.2 denotes hydrogen or a biolabile ester-forming group, and R.sup.3 denotes hydrogen or a biolabile ester-forming group, and physiologically acceptable salts of the acids of formula I for preparing pharmaceutical compositions for the treatment and/or prophylaxis of gastrointestinal blood circulation disturbances.
摘要翻译：描述了通式I的化合物，其中R 1表示苯基 - 低级烷基，其可以在苯环中被低级烷基，低级烷氧基或卤素任意取代，或表示萘基 - 低级烷基， R2表示氢或不生物不稳定酯形成基团，R 3表示氢或不可生物酯形成基团，以及用于制备用于治疗和/或预防胃肠道血液循环障碍的药物组合物的式I的酸的生理学上可接受的盐。

6. 发明授权

US5677297A Benzazepine-, benzoxazepine- and benzothiazepine-n-acetic acid derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：苯扎西平 - ，苯并氧氮杂和苯并硫氮杂_-乙酸衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5677297A
公开(公告)日：1997-10-14
申请号：US620213
申请日：1996-03-22
申请人： Harald Waldeck , Dagmar Hoeltje , Josef Messinger , Jochen Antel , Michael Wurl , Dirk Thormaehlen
发明人： Harald Waldeck , Dagmar Hoeltje , Josef Messinger , Jochen Antel , Michael Wurl , Dirk Thormaehlen
IPC分类号： C07D223/16 , A61K31/33 , A61K31/423 , A61K31/428 , A61K31/55 , A61K31/554 , A61K38/00 , A61K38/05 , A61P7/10 , A61P9/00 , A61P43/00 , C07D267/14 , C07D281/10 , C07K5/078 , C07D487/00
CPC分类号： C07K5/06139 , A61K38/00
摘要： Compounds with neutral endopeptidase (NEP) inhibitory activity corresponding to the formula I ##STR1## in which R.sup.1 is a lower alkoxy-lower-alkyl group whose lower alkoxy radical is substituted by a lower alkoxy group, or a phenyl-lower-alkyl or phenyloxy-lower-alkyl group which can optionally be substituted in the phenyl ring by lower alkyl, lower alkoxy or halogen, or a naphthyl-lower-alkyl group, A is CH.sub.2, O or S, R.sup.2 is hydrogen or halogen, R.sup.3 is hydrogen or halogen, R.sup.4 is hydrogen or a group forming a biolabile ester, and R.sup.5 is hydrogen or a group forming a biolabile ester, and the physiologically acceptable acid addition salts thereof.
摘要翻译：具有对应于式I的中性内肽酶（NEP）抑制活性的化合物其中R1是低级烷氧基被低级烷氧基取代的低级烷氧基 - 低级烷基或苯基 - 低级烷基或苯基氧基 - 低级烷基，其可以被苯环中的低级烷基，低级烷氧基或卤素或萘基 - 低级烷基任意取代，A是CH 2，O或S，R 2是氢或卤素，R 3是氢或卤素，R 4为氢或形成不可生物酯的基团，R 5为氢或形成不可生物酯的基团及其生理上可接受的酸加成盐。

7. 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。

8. 发明授权

US07772225B2 N-sulfamoyl-piperidineamides for the treatment or inhibition of obesity and related conditions 有权
标题翻译： N-氨磺酰基 - 哌啶酰胺，用于治疗或抑制肥胖症和相关病症
公开(公告)号：US07772225B2
公开(公告)日：2010-08-10
申请号：US11635514
申请日：2006-12-08
申请人： Jochen Antel , Michael Firnges , Uwe Schoen , Harald Waldeck , Michael Wurl , Dania Reiche , Peter-Colin Gregory
发明人： Jochen Antel , Michael Firnges , Uwe Schoen , Harald Waldeck , Michael Wurl , Dania Reiche , Peter-Colin Gregory
IPC分类号： A01N43/00 , A01N43/58 , A01N43/40 , A61K31/55 , A61K31/54 , A61K31/535 , A61K31/50 , A61K31/497 , A61K31/445 , C07D223/14 , C07D279/12 , C07D295/00 , C07D265/28 , C07D239/00 , C07D239/70 , C07D471/00 , C07D487/00 , C07D241/04 , C07D211/00
CPC分类号： C07D211/96 , C07D401/04 , C07D401/12 , C07D409/12 , C07D413/04
摘要： The present invention relates to novel N-sulfamoyl-piperidineamides of Formula I and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment of obesity and its concomitant and/or secondary diseases and related or other conditions.
摘要翻译：本发明涉及式I的新型N-氨磺酰 - 哌啶酰胺及其生理上可接受的酸加成盐，包括它们的药物组合物，其制备方法及其用于治疗肥胖及其伴随和/或继发性疾病的用途，以及相关或其他条件。

9. 发明授权

US07547708B2 N-sulfamoyl-N′-benzopyranpiperidine compounds and uses thereof 有权
标题翻译： N-氨磺酰基-N'-苯并吡喃哌啶化合物及其用途
公开(公告)号：US07547708B2
公开(公告)日：2009-06-16
申请号：US11598684
申请日：2006-11-14
申请人： Jochen Antel , Harald Waldeck , Uwe Schoen , Peter-Colin Gregory , Michael Wurl , Michael Firnges , Dania Reiche , Uwe Reinecker , Holger Sann
发明人： Jochen Antel , Harald Waldeck , Uwe Schoen , Peter-Colin Gregory , Michael Wurl , Michael Firnges , Dania Reiche , Uwe Reinecker , Holger Sann
IPC分类号： A61K31/438 , C07D491/10
CPC分类号： C07D491/10
摘要： N-sulfamoyl-N′-benzopyranpiperidine compounds of formula I and their physiologically acceptable acid addition salts, pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and related concomitant and/or secondary diseases or conditions
摘要翻译：式I的N-氨磺酰基-N'-苯并吡喃哌啶化合物及其生理上可接受的酸加成盐，包含它们的药物组合物，其制备方法及其用于治疗和/或抑制青光眼，癫痫，双相性精神障碍，偏头痛，神经性疼痛，肥胖症，II型糖尿病，代谢综合征，酒精依赖性和/或癌症，以及相关并发症和/或继发性疾病或病症

10. 发明申请

US20050143441A1 Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 审中-公开
标题翻译：涉及具有CB1拮抗作用的4,5-二氢-1H-吡唑衍生物的肥胖症的新型医疗联合治疗
公开(公告)号：US20050143441A1
公开(公告)日：2005-06-30
申请号：US11005486
申请日：2004-12-07
申请人： Jochen Antel , Gunter Krause , Peter-Colin Gregory , Michael Wurl , Harald Waldeck , Josephus Lange , Cornelis Kruse
发明人： Jochen Antel , Gunter Krause , Peter-Colin Gregory , Michael Wurl , Harald Waldeck , Josephus Lange , Cornelis Kruse
IPC分类号： A61K31/365 , A61K31/4152
CPC分类号： A61K31/4152 , A61K31/365 , A61K2300/00
摘要： The present invention relates to a novel medical use of e.g. 4,5-dihydro-1H-pyrazole compounds which are potent antagonists of the cannabis CB1-receptor in combination with lipase inhibitors. Said compounds are particularly suitable in combination with lipase inhibitors in the manufacture of medicaments for the treatment and/or prophylaxis of obesity in adolescent or in juvenile patients and/or for the treatment and/or prophylaxis of drug induced obesity in juvenile as well as in adolescent patients. The compounds have the general formula (I) wherein the group Bb represents sulfonyl or carbonyl, and the substituents R, R1, R2 and R3, and the group Aa are defined as shown in the description. Preferred lipase inhibitors are orlistat, panclicins, ATL-962 and/or lipstatin.
摘要翻译：本发明涉及一种新的医疗用途。 4,5-二氢-1H-吡唑化合物，其是大麻CB 1 - 受体与脂肪酶抑制剂组合的有效拮抗剂。所述化合物在制备用于治疗和/或预防青少年或青少年患者肥胖症的药物和/或用于治疗和/或预防青少年药物诱导的肥胖症以及青少年患者。化合物具有通式（I），其中基团Bb表示磺酰基或羰基，取代基R 1，R 1，R 2和R 3， SUB>，并且组Aa如说明书所示定义。优选的脂肪酶抑制剂是奥利司他，胰蛋白酶，ATL-962和/或脂抑素。

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