Invention Grant
- Patent Title: Thyroid receptor ligands and method II
- Patent Title (中): 甲状腺受体配体及方法二
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Application No.: US11189654Application Date: 2005-07-26
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Publication No.: US07288571B2Publication Date: 2007-10-30
- Inventor: Jon Hangeland , Minsheng Zhang , Yolanda Caringal , Denis Ryono , Yi-Lin Li , Johan Malm , Ye Liu , Neeraj Garg , Chris Litten , Ana Maria Garcia Collazo , Konrad Koehler
- Applicant: Jon Hangeland , Minsheng Zhang , Yolanda Caringal , Denis Ryono , Yi-Lin Li , Johan Malm , Ye Liu , Neeraj Garg , Chris Litten , Ana Maria Garcia Collazo , Konrad Koehler
- Applicant Address: SE Huddinge
- Assignee: Karo Bio AB
- Current Assignee: Karo Bio AB
- Current Assignee Address: SE Huddinge
- Agency: Wiggin and Dana LLP
- Agent Todd E. Garabedian; Elizabeth A. Galletta
- Priority: GB9828442.5 19981224
- Main IPC: A61K31/18
- IPC: A61K31/18 ; C07C311/50

Abstract:
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 stereolsom thereof; or when n is equal to or greater than one, R4 may be 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 dependant 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.
Public/Granted literature
- US20050282872A1 Novel thyroid receptor ligands and method II Public/Granted day:2005-12-22
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