公开(公告)号：US20060025344A1

公开(公告)日：2006-02-02

申请号：US11158348

申请日：2005-06-20

申请人： Birgitte Lange ,  Thue Schwartz ,  Thomas Frimurer ,  Oystein Rist

发明人： Birgitte Lange ,  Thue Schwartz ,  Thomas Frimurer ,  Oystein Rist

IPC分类号： A61K38/22 ,  C07K14/575

CPC分类号： G01N33/74 ,  A61K31/00 ,  A61K38/046 ,  G01N2333/726 ,  G01N2500/02

摘要： Compounds of the invention act as inverse agonist ghrelin receptors. Some of the compounds of the invention may have both inverse agonistic and antagonistic properties as they both decrease or eliminate the constitutive activity of he ghrelin receptor and block the effect of ghrelin. Other preferred compounds of the invention have inverse agonistic properties but have little or no antagonistic activity. The compounds are suitable for medical and/or cosmetic use in connection with modulation of feeding behaviors, body composition and reduction of body mass. The invention also relates to methods for identifying inverse agonists for the ghrelin receptor and for monitoring the further development of such compounds.

摘要翻译： 本发明的化合物作为反向激动剂ghrelin受体。 本发明的一些化合物可以具有反向激动和拮抗性质，因为它们都降低或消除了生长素释放肽受体的组成型活性并阻断了生长素释放肽的作用。 本发明的其它优选化合物具有反向激动性质但具有很少或没有拮抗活性。 该化合物适用于与调节进食行为，身体组成和减少体重有关的医疗和/或化妆品用途。 本发明还涉及用于鉴定生长素释放肽受体的反向激动剂并监测这些化合物的进一步发展的方法。

公开(公告)号：US20070037751A1

公开(公告)日：2007-02-15

申请号：US10567406

申请日：2004-08-06

申请人： Birgitte Lange ,  Christian Hansen ,  Henrik Nilsson

发明人： Birgitte Lange ,  Christian Hansen ,  Henrik Nilsson

IPC分类号： A61K38/08 ,  A61K38/05 ,  A61K38/06

CPC分类号： C07K14/575 ,  A61K38/00

摘要： The present invention relates, in one aspect, to the use of a secretagogue compound for the preparation of a medicament for the prophylaxis or treatment of cancer cachexia in an individual in need of such treatment. In another aspect, the present invention relates to the use of a ghrelin-like compound for the preparation of a medicament for prophylaxis or treatment of cachexia in an individual by administering a subcutaneous dosage of said medicament to the individual. In a further aspect, the present invention relates to the use of a ghrelin-like compound or a pharmaceutically acceptable salt thereof for the preparation of a medicament for stimulation of appetite in an individual by administering a subcutaneous dosage of said medicament to the individual. Furthermore, the present invention relates to a number of new ghrelin-like compounds and uses thereof, as well as to pharmaceutical compositions and medical packaging comprising the new ghrelin-like compounds.

摘要翻译： 本发明在一个方面涉及促分泌素化合物在制备用于预防或治疗需要这种治疗的个体中的癌症恶病质的药物中的用途。 另一方面，本发明涉及生长素释放肽样化合物在制备用于预防或治疗个体中恶病质的药物中的用途，其通过向个体施用皮下剂量的所述药物。 在另一方面，本发明涉及生长素释放肽样化合物或其药学上可接受的盐在制备用于通过向个体施用所述药物的皮下剂量来刺激个体中的食欲的药物中的用途。 此外，本发明涉及许多新的生长素释放肽样化合物及其用途，以及包含新的生长素释放肽样化合物的药物组合物和医药包装。