公开(公告)号：US06492424B1

公开(公告)日：2002-12-10

申请号：US09744865

申请日：2001-04-09

申请人： Theresa Apelqvist ,  Patrick Goede ,  Erik Holmgren

发明人： Theresa Apelqvist ,  Patrick Goede ,  Erik Holmgren

IPC分类号： A61K3119

CPC分类号： C07D295/192 ,  C07C59/68 ,  C07C59/90 ,  C07C65/40 ,  C07C69/736 ,  C07C69/92 ,  C07C217/90 ,  C07C233/56 ,  C07C235/34

摘要： Novel glucocorticoid and thyroid receptor ligands as provided which have the general formula (I): in which R1 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano, or a pharmaceutically acceptable salt thereof. R2 and R3 are the same or different, and are hydrogen, halogen, alkyl of 1 to 4 carbons, or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen. X is carbonyl or methylene. R4 is an aliphatic, aromatic or heteroaromatic. Y is hydroxyl, methoxy, amino, or alkyl amino. n is an integer from 0 to 4. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid or thyroid receptor gene such as diabetes, hypercholesterolemia, or obesity using these compounds is also disclosed.

摘要翻译： 提供具有通式（I）的新型糖皮质激素和甲状腺受体配体：其中R 1是脂族烃，芳族烃，羧酸或其酯，链烯基羧酸或其酯，羟基，卤素或氰基，或 其药学上可接受的盐。 R2和R3相同或不同，为氢，卤素，1至4个碳的烷基或3至5个碳的环烷基，R2和R3中的至少一个不是氢。 X是羰基或亚甲基。 R 4是脂族，芳族或杂芳族。 Y是羟基，甲氧基，氨基或烷基氨基。 n是0至4的整数。还公开了用于治疗与代谢功能障碍相关的疾病或依赖于使用这些化合物的糖皮质激素或甲状腺受体基因如糖尿病，高胆固醇血症或肥胖症的表达的方法。