公开(公告)号：EP1257526A1

公开(公告)日：2002-11-20

申请号：EP01903064.2

申请日：2001-01-12

申请人： Bristol-Myers Squibb Co.

发明人： FRIENDS, Todd, Jason ,  RYONO, Dennis, E. ,  ZHANG, Minsheng

IPC分类号： C07C235/74 ,  C07C235/76 ,  A61K31/167

CPC分类号： C07C233/27 ,  A61K31/167 ,  A61K45/06 ,  C07C233/25 ,  A61K2300/00

摘要： New thyroid receptor ligands are provided which have the general formula (I) in which X is -O-, -S-, -CH2-, -CO-, or -NH-; Y is -(CH2)n- where n is an integer from 1 to 5, or cis- or trans-ethylene; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.