公开(公告)号：EP1144370A2

公开(公告)日：2001-10-17

申请号：EP99962486.9

申请日：1999-12-23

申请人： KARO BIO AB ,  BRISTOL-MYERS SQUIBB COMPANY

发明人： HANGELAND, Jon ,  ZHANG, Minsheng ,  CARINGAL, Yolanda ,  RYONO, Denis ,  LI, Yi-Lin ,  MALM, Johan ,  LIU, Ye ,  GARG, Neeraj ,  LITTEN, Chris ,  GARCIA COLLAZO, Ana Maria ,  KOEHLER, Konrad

IPC分类号： C07C311/00

CPC分类号： C07D207/27 ,  C07C235/32 ,  C07C235/52 ,  C07C307/06 ,  C07C311/51 ,  C07C323/41 ,  C07C323/60 ,  C07D207/09 ,  C07D211/24 ,  C07D211/34 ,  C07D211/58 ,  C07D211/96 ,  C07D213/40 ,  C07D223/12 ,  C07D231/38 ,  C07D233/64 ,  C07D257/04 ,  C07D285/06 ,  C07D285/135 ,  C07D295/13 ,  C07D295/185 ,  C07D333/20

摘要： New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; 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 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR'R'') or an acylsulphonamide (CONHSO2R') derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR'R''). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H). 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.

公开(公告)号：EP1257526B1

公开(公告)日：2005-05-11

申请号：EP01903064.2

申请日：2001-01-12

申请人： Bristol-Myers Squibb Company

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