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    Novel medical combination treatment of obesity involving 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
    1.
    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。

    Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds
    2.
    发明申请
    Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds 审中-公开
    显示CB1拮抗活性的化合物的新型医疗用途和涉及所述化合物的组合治疗

    公开(公告)号：US20050124660A1

    公开(公告)日：2005-06-09

    申请号：US10969840

    申请日：2004-10-22

    申请人： Jochen Antel ,  Peter-Colin Gregory ,  Harald Waldeck ,  Gunter Krause ,  Josephus Lange ,  Cornelis Kruse

    发明人： Jochen Antel ,  Peter-Colin Gregory ,  Harald Waldeck ,  Gunter Krause ,  Josephus Lange ,  Cornelis Kruse

    IPC分类号： A61K31/4196 ,  A61K31/426 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/541

    CPC分类号： A61K31/4439 ,  A61K31/4196 ,  A61K31/426 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/541

    摘要： The present invention relates to a novel medical use of compounds with CB1-receptor activity selected from the group of 4,5-dihydro-1H-pyrazole derivatives, 1H-Imidazole derivatives, thiazole derivatives and/or 1H-1,2,4-triazole-3-carboxamide derivatives, as each defined in the specification, or of a prodrug thereof, a tautomer thereof or a salt thereof, in the manufacture of medicaments for the treatment and/or prophylaxis of CB1 receptor related diseases in juvenile patients and/or for the treatment and/or prophylaxis of drug induced obesity in juvenile, as well as in adolescent, patients. Furthermore, the invention pertains to the use of said compounds with CB1-receptor activity 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. Preferred lipase inhibitors are orlistat, panclicins, ATL-962 and/or lipstatin.

    摘要翻译： 本发明涉及一种具有选自4,5-二氢-1H-吡唑衍生物，1H-咪唑衍生物，噻唑衍生物和/或其中之一种具有CB 1 - 1 - 受体活性的化合物的新型医疗用途 在制备用于治疗和/或预防CB的药物中的1H-1,2,4-三唑-3-甲酰胺衍生物，如说明书中所定义，或其前药，其互变异构体或其盐 少年患者中的受体相关疾病和/或用于治疗和/或预防青少年以及青少年患者的药物诱导的肥胖症。 此外，本发明涉及具有CB 1/2受体活性的所述化合物与脂肪酶抑制剂的组合的用途。 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。 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。

    NOVEL MEDICAL USES OF 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1- ANTAGONISTIC ACTIVITY
    3.
    发明申请
    NOVEL MEDICAL USES OF 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1- ANTAGONISTIC ACTIVITY 审中-公开
    具有CB1-拮抗活性的4,5-二氢-1H-吡唑衍生物的新医学用途

    公开(公告)号：US20050239859A2

    公开(公告)日：2005-10-27

    申请号：US10929377

    申请日：2004-08-31

    申请人： Jochen Antel ,  Gunter Krause ,  Josephus Lange ,  Cornelis Kruse ,  Peter-Colin Gregory ,  Cathaline Den Besten

    发明人： Jochen Antel ,  Gunter Krause ,  Josephus Lange ,  Cornelis Kruse ,  Peter-Colin Gregory ,  Cathaline Den Besten

    IPC分类号： A61K31/415

    CPC分类号： A61K31/415

    摘要： Abstract of the DisclosureThe present invention relates to a novel medical use of 4,5-dihydro-1H-pyrazole compounds which are potent antagonists of the cannabis CB1-receptor. Said compounds are particularly suitable in the manufacture of medicaments for the treatment and/or prophylaxis of CB1 receptor related diseases 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.

    摘要翻译： 本发明摘要本发明涉及作为大麻CB 1受体的有效拮抗剂的4,5-二氢-1H-吡唑化合物的新型医疗用途。 所述化合物特别适用于制备用于治疗和/或预防少年患者中CB 1受体相关疾病的药物和/或用于治疗和/或预防未成年人药物诱导的肥胖的药物 就像青少年患者一样。 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。