公开(公告)号：US20060235035A1

公开(公告)日：2006-10-19

申请号：US10510907

申请日：2003-04-08

申请人： Thomas Hogberg ,  Emelie Bjurling ,  Jean-Marie Receveur ,  Trond Ulven ,  Paul Little ,  Christian Elling ,  Pia Norregaard

发明人： Thomas Hogberg ,  Emelie Bjurling ,  Jean-Marie Receveur ,  Trond Ulven ,  Paul Little ,  Christian Elling ,  Pia Norregaard

IPC分类号： A61K31/513 ,  A61K31/4747 ,  A61K31/4745 ,  A61K31/4035 ,  A61K31/4709 ,  A61K31/381 ,  A61K31/35 ,  A61K31/34

CPC分类号： C07D213/643 ,  C07C237/42 ,  C07C237/44 ,  C07C275/42 ,  C07C323/44 ,  C07C2601/14 ,  C07D207/09 ,  C07D207/14 ,  C07D211/26 ,  C07D211/58 ,  C07D213/75 ,  C07D233/32 ,  C07D295/13 ,  C07D317/58

摘要： Novel compounds of Formula (I) which modulate MCH activity are disclosed, in which A is a linker; Ar1 is an aryl or heteroaryl group; R1 is a lower alkoxy group; R2 is an R1 group or hydrogen, an OH or an NH2 group, Q together with the carbonyl forms an amide group, which is further substituted with an amine group; R5 is selected from hydrogen, halogen atoms, alkoxy groups, hydroxy, alkylamino groups, dialkylamino groups, hydroxylalkyl groups, carboxamido groups, acylamido groups, acyl groups, —CHO, nitrile, alkyl, alkenyl or alkynyl groups, —SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups such as —CH2CF3, —CF2CF3, —CF3, —OCF3, —SCF3; —SO2NH2, —SO2NHAlk, —SO2NAlk2, —SO2Alk; X is H, F, Cl, Br, I, —SCH3, —CF3, —OCF3, —SCF3, OCH3, or lower alkyl or alkenyl group; R8 is halogen atoms, alkyl, alkenyl or alkynyl groups, cycloalkyl groups, aryl groups, heteroaryl groups, heterocyclyl groups, alkylcycloalkyl groups, alkylaryl groups, alkylheterocyclyl groups, alkylheteroaryl groups, arylalkoxy groups, aryloxy groups, alkoxy groups, dialkylamino groups, —CONHAlk, —CONHAr, —CONAlk2, —NHCO-Alk, —NHCO—Ar, —CO-Alk, —CO—Ar, —SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups; or R8 is R6-Ar2—B—, in which B is a single bond or a connecting moiety; Ar2 is an Ar1 group; R6 is an R5 group; and which are useful in the treatment or prevention of e.g. obesity, depression, diabetes, bulimia etc.

公开(公告)号：US20060111357A1

公开(公告)日：2006-05-25

申请号：US10538455

申请日：2003-12-11

申请人： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Pia Norregaard ,  Paul Little ,  Jean-Marie Receveur

发明人： Thomas Frimurer ,  Trond Ulven ,  Thomas Hogberg ,  Pia Norregaard ,  Paul Little ,  Jean-Marie Receveur

IPC分类号： A61K31/519 ,  A61K31/517 ,  A61K31/498 ,  A61K31/4745 ,  A61K31/525 ,  A61K31/4709

CPC分类号： C07D401/04 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519

摘要： The present invention relates to the use of quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel quinoline compounds per se. The quinoline compounds have been found to interact with a melanin-concentrating hormone receptor, a MCH receptor. The compounds have modulating activity on the MCH receptor such as e.g. antagonistic, agonistic or allosteric activity and are useful for medicinal or cosmetic purposes such as, e.g. in the treatment or prevention of feeding disorders like obesity, metabolic syndrome, Type II diabetes, bulimia, etc. or in the treatment or prevention of depression.

摘要翻译： 本发明涉及喹啉化合物在制备药物和/或化妆品组合物中的用途，用于治疗，预防和/或诊断由黑色素浓缩激素引起或涉及的病症。 本发明还涉及新的喹啉化合物本身。 已发现喹啉化合物与黑色素浓缩激素受体MCH受体相互作用。 这些化合物对MCH受体具有调节活性，例如。 拮抗，激动或变构活性，并且可用于药物或化妆品目的，例如。 治疗或预防肥胖症，代谢综合征，II型糖尿病，食欲过盛等进食障碍，或治疗或预防抑郁症。