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公开(公告)号：EP1751126A1
公开(公告)日：2007-02-14
申请号：EP05716736.3
申请日：2005-02-18
发明人： WALDECK, Harald , ANTEL, Jochen , EYTING, Sabine , WURL, Michael , GREGORY, Peter-Colin , WOLFF, Maike
IPC分类号： C07D305/12 , A61K31/335 , A61P3/00
CPC分类号： C07D305/12
摘要： The invention relates to substituted β-lactones (oxetanones) of general formula (I), in which R1, R2 and n have the meanings cited in the description, and to medicaments, which contain these compounds and which have a pancreas lipase-inhibiting effect. The invention also relates to a method for producing the compounds of formula (I) and to intermediate products of this method.
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2.发明公开COMBINATION TREATMENT OF OBESITY INVOLVING SELECTIVE CB1-ANTAGONISTS AND LIPASE INHIBITORS 审中-公开肥胖选择性CB1拮抗剂与脂肪酶抑制剂联合应用
公开(公告)号：EP1680116A1
公开(公告)日：2006-07-19
申请号：EP04791298.5
申请日：2004-10-22
IPC分类号： A61K31/454 , A61K31/5355 , A61K31/343 , A61K31/05 , A61K31/352 , A61K31/353 , A61K31/16 , A61K31/165 , A61K31/4164 , A61K31/397 , A61K31/4965 , A61K31/497 , A61K31/4166 , A61K31/365 , A61K31/785
CPC分类号： A61K45/06 , A61K31/05 , A61K31/16 , A61K31/165 , A61K31/343 , A61K31/352 , A61K31/353 , A61K31/365 , A61K31/397 , A61K31/4164 , A61K31/4166 , A61K31/454 , A61K31/4965 , A61K31/497 , A61K31/5355 , A61K31/785 , A61K2300/00
摘要： The present invention relates to a novel medical use of selective CB1 receptor antagonistic compounds 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 CB1 receptor antagonistic compounds suitable according to the invention are elucidated in more detail in the description. Preferred lipase inhibitors are orlistat, panclicins, ATL-962 and/or lipstatin.
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公开(公告)号：EP1513811A1
公开(公告)日：2005-03-16
申请号：EP03757007.4
申请日：2003-05-30
发明人： WEBER, Dirk , KESSLER, Horst , BERGER, Claudia , ANTEL, Jochen , HEINRICH, Timo
IPC分类号： C07D209/20 , C07K5/087 , A61K31/405 , A61K38/05 , A61K38/06 , A61P3/04 , A61P3/10 , A61P9/00 , C07K5/062 , C07K5/078 , C07K5/072 , C07D401/12 , C07D405/12
CPC分类号： C07D401/12 , A61K38/00 , C07D209/20 , C07D405/12 , C07K5/06026 , C07K5/06078 , C07K5/06191 , C07K5/0812
摘要： The invention relates to novel compounds having a selective BRS-3 agonistic action and corresponding to general formula (I) wherein A , A , A , R , R , R , Ar , Ar , Ar , m and n have the designations cited in the description. The invention also relates to pharmaceuticals containing said compounds and to methods for producing compounds of formula (I).
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4.发明公开VERWENDUNG VON TRIFLUORACETYLALKYL-SUBSTITUIERTER PHENYL-, PHENOL- UND BENZOYLDERIVATE IN DER BEHANDLUNG UND/ODER PROPHYLAXE VON OBESITAS UND DEREN BEGLEIT- UND/ODER FOLGEERKRANKUNGEN 有权USE TRIFLUORACETYLALKYL取代的用于治疗和/或预防肥胖症的苯基，苯酚基和苯甲酰基衍生物和它们的意外和/或继发性疾病
公开(公告)号：EP1420771A2
公开(公告)日：2004-05-26
申请号：EP02764680.1
申请日：2002-07-12
IPC分类号： A61K31/00 , A61K31/12 , A61K31/122 , C07C49/255 , C07C49/233 , C07C49/35 , C07C49/333 , A61P3/04 , A61P9/00 , A61P3/00 , A61P9/12 , A61P3/10 , A61P3/06 , A61P9/10
CPC分类号： A61K31/00 , A61K31/12 , A61K31/122
摘要： The invention relates to the use of novel and known lipase-inhibitorily active compounds of general formula (I), wherein Al, A2, R2 and Z have the meanings as cited in the description, for the treatment and/or prophylaxis of obesity as well as accompanying diseases and/or secondary diseases associated with obesity.
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5.发明公开NOVEL N-SULFAMOYL-PIPERIDINEAMIDES FOR THE PROPHYLAXIS OR TREATMENT OF OBESITY AND RELATED CONDITIONS 审中-公开新的N- SULFAMOYLPIPERIDINAMIDE为防止及肥胖症的治疗及类似LEIDEN
公开(公告)号：EP1960359A1
公开(公告)日：2008-08-27
申请号：EP06830478.1
申请日：2006-12-08
发明人： ANTEL, Jochen , SCHOEN, Uwe , WALDECK, Harald , WURL, Michael , FIRNGES, Michael , REICHE, Dania , GREGORY, Peter-Colin
IPC分类号： C07D211/58 , C07D401/04 , C07D409/12 , C07D401/12 , A61K31/4545 , A61P3/04
CPC分类号： C07D409/12 , C07D211/58 , C07D401/04 , C07D401/12
摘要： The present invention relates to novel N-sulfamoyl-piperidineamides of general 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/or related conditions.
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6.发明公开
公开(公告)号：EP1951725A1
公开(公告)日：2008-08-06
申请号：EP06829983.3
申请日：2006-11-14
发明人： ANTEL, Jochen , WALDECK, Harald , SCHOEN, Uwe , GREGORY, Peter-Colin , WURL, Michael , FIRNGES, Michael , REICHE, Dania , REINECKER, Uwe , SANN, Holger
IPC分类号： C07D491/10 , C07D491/20 , A61K31/438 , A61P27/06 , A61P25/00 , A61P3/00 , A61P35/00
CPC分类号： C07D491/10
摘要： The present invention relates to novel N-sulfamoyl-N'-benzopyranpiperidines of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the prophylaxis and/or treatment and/or prevention and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and its concomitant and/or secondary diseases or conditions.
摘要翻译： 本发明涉及通式（I）的新型N-氨磺酰基-N'-苯并吡喃哌啶及其生理学上可接受的酸加成盐，包含它们的药物组合物，其制备方法，以及它们用于预防和/或治疗和 /或预防和/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，酒精依赖和/或癌症及其并发和/或继发性疾病或病症。
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7.发明授权VERWENDUNG TRIFLUORACETYLALKYL-SUBSTITUIERTER PHENYL-, PHENOL- UND BENZOYLDERIVATE IN DER BEHANDLUNG UND/ODER PROPHYLAXE VON OBESITAS UND DEREN BEGLEIT- UND/ODER FOLGEERKRANKUNGEN 有权USE TRIFLUORACETYLALKYL取代的用于治疗和/或预防肥胖症的苯基，苯酚基和苯甲酰基衍生物和它们的意外和/或继发性疾病
公开(公告)号：EP1420771B9
公开(公告)日：2007-10-17
申请号：EP02764680.1
申请日：2002-07-12
IPC分类号： A61K31/00 , A61K31/12 , A61K31/122 , C07C49/255 , C07C49/233 , C07C49/35 , C07C49/333 , A61P3/04 , A61P3/00 , A61P9/12 , A61P3/10 , A61P3/06
CPC分类号： A61K31/00 , A61K31/12 , A61K31/122
摘要： The invention relates to the use of novel and known lipase-inhibitorily active compounds of general formula (I), wherein Al, A2, R2 and Z have the meanings as cited in the description, for the treatment and/or prophylaxis of obesity as well as accompanying diseases and/or secondary diseases associated with obesity.
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8.发明公开
公开(公告)号：EP1807063A2
公开(公告)日：2007-07-18
申请号：EP05801545.4
申请日：2005-10-25
发明人： FIRNGES, Michael , GREGORY, Peter-Colin , ANTEL, Jochen , LANGE, Josephus, Hubertus, Maria , WALDECK, Harald
IPC分类号： A61K31/00 , A61K31/54 , A61K31/40 , A61K31/44 , A61K31/415 , A61K31/427 , C12Q1/68 , A61P3/04 , G01N33/00
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 I, and the prophylaxis and treatment, of obesity as well as the prophylaxis, treatment, delayed onset and/or inhibition 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.
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9.发明公开MEDICAMENTS CONTAINING N-SULFAMOYL-N'-ARYLPIPERAZINES FOR THE PROPHYLAXIS OR TREATMENT OF OBESITY AND RELATED CONDITIONS 审中-公开N-二氨磺酰基-N'-苯基包含预防和肥胖症的治疗和相关疾病药物
公开(公告)号：EP1750712A2
公开(公告)日：2007-02-14
申请号：EP05749492.4
申请日：2005-05-18
发明人： ANTEL, Jochen , GREGORY, Peter-Colin , REINECKER, Uwe , WURL, Michael , SCHOEN, Uwe , WALDECK, Harald , FIRNGES, Michael , REICHE, Dania
IPC分类号： A61K31/495 , A61P3/04 , A61P3/00 , A61P3/10 , A61P3/06 , A61P9/12 , A61P9/00 , A61P9/10 , C07D295/22 , A61K45/06
CPC分类号： A61K31/495 , 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 and their physiologically compatible acid addition salts for the prophylaxis or treatment of obesity and related conditions.
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公开(公告)号：EP1513811B1
公开(公告)日：2009-04-08
申请号：EP03757007.4
申请日：2003-05-30
发明人： WEBER, Dirk , KESSLER, Horst , BERGER, Claudia , ANTEL, Jochen , HEINRICH, Timo
IPC分类号： C07D209/20 , C07K5/087 , A61K31/405 , A61K38/05 , A61K38/06 , A61P3/04 , A61P3/10 , A61P9/00 , C07K5/062 , C07K5/078 , C07K5/072 , C07D401/12 , C07D405/12
CPC分类号： C07D401/12 , A61K38/00 , C07D209/20 , C07D405/12 , C07K5/06026 , C07K5/06078 , C07K5/06191 , C07K5/0812
摘要： The invention relates to novel compounds having a selective BRS-3 agonistic action and corresponding to general formula (I) wherein A , A , A , R , R , R , Ar , Ar , Ar , m and n have the designations cited in the description. The invention also relates to pharmaceuticals containing said compounds and to methods for producing compounds of formula (I).
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