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    Pharmaceutical compositions comprising CB1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions
    1.
    发明授权
    Pharmaceutical compositions comprising CB1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions 有权
    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。

    Pharmaceutical compositions comprising CB1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions
    4.
    发明申请
    Pharmaceutical compositions comprising CB1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions 有权
    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：US20060128673A1

    公开(公告)日：2006-06-15

    申请号：US11257056

    申请日：2005-10-25

    申请人： Michael Firnges ,  Peter-Colin Gregory ,  Jochen Antel ,  Josephus Maria Lange ,  Harald Waldeck

    发明人： Michael Firnges ,  Peter-Colin Gregory ,  Jochen Antel ,  Josephus Maria Lange ,  Harald Waldeck

    IPC分类号： A61K31/655 ,  A61K31/4439 ,  A61K31/4152 ,  A61K31/454 ,  A61K31/5377

    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 的至少一个K ATP通道开放剂作为第一活性剂和至少一种作为第二活性剂的CB 1大麻素受体拮抗剂。 本发明进一步涉及这样的新型组合疗法，其中使用具有组合的K ATP通道开口和CB 1拮抗性质的双作用化合物。 本发明还涉及包含K ATP通道开放剂和CB 1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以及其并发症和/或继发性疾病或病症，特别是代谢综合征和/或综合征的预防，治疗，延迟发作和/或吸收 X和/或II型糖尿病。 本发明进一步涉及这样的新型药物组合物，其包含具有组合的K ATP通道开口和CB 1拮抗性质的双作用化合物。

    Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
    9.
    发明申请
    Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 审中-公开
    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。