Title:
BENZAMIDE LIGANDS FOR THE THYROID RECEPTOR
Document Type and Number:
WIPO Patent Application WO2001094293
Kind Code:
A3
Abstract:
New thyroid receptor ligands are provided which have the general formula (I) in which: X is -0-, -S-, -CH2-, -CO-, or -NH-; 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 methyl, ethyl, n-propyl or trifluoromethyl; 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.
Inventors:
RYONO DENIS E (US)
Application Number:
PCT/US2001/017742
Publication Date:
June 06, 2002
Filing Date:
June 01, 2001
Export Citation:
Assignee:
BRISTOL MYERS SQUIBB CO (US)
RYONO DENIS E (US)
RYONO DENIS E (US)
International Classes:
A61K45/00; A61K31/07; A61K31/166; A61K31/195; A61K31/22; A61K31/351; A61K31/40; A61K31/404; A61K31/4418; A61K31/455; A61K31/592; A61K38/28; A61P3/00; A61P3/04; A61P3/06; A61P5/14; A61P5/16; A61P9/04; A61P9/06; A61P9/10; A61P17/00; A61P17/02; A61P17/10; A61P17/16; A61P19/10; A61P25/24; A61P27/06; A61P35/00; C07C235/52; (IPC1-7): C07C235/52; A61K31/166
Domestic Patent References:
| WO2000039077A2 | 2000-07-06 | |||
| WO1999000353A1 | 1999-01-07 |
Foreign References:
| DE1078582B | 1960-03-31 |
Other References:
YOKOYAMA N: "Synthesis and structure-activity relationships of oxamic acid and acetic acid derivatives related to L-thyronine", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 38, 1995, pages 695 - 707, XP002080908, ISSN: 0022-2623
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