Title:
新規な甲状腺レセプターリガンドおよび方法II
Document Type and Number:
Japanese Patent JP4405088
Kind Code:
B2
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 differential 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 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.
Inventors:
John Hangerland
Jean, Minsheng
Karingal, Yolanda
Rhino, Dennis
Li, Irin
Marum, Joan
Liu, Ye
Niraj, Guarg
Ritten, chris
Garcia Colazo, Anna Maria
Caller, Conrad
Jean, Minsheng
Karingal, Yolanda
Rhino, Dennis
Li, Irin
Marum, Joan
Liu, Ye
Niraj, Guarg
Ritten, chris
Garcia Colazo, Anna Maria
Caller, Conrad
Application Number:
JP2000590990A
Publication Date:
January 27, 2010
Filing Date:
December 23, 1999
Export Citation:
Assignee:
Caro Bio Actebrague
International Classes:
C07C235/34; A61K31/381; C07D233/88; A61K31/40; A61K31/41; A61K31/415; A61K31/4168; A61K31/433; A61K31/44; A61K31/4409; A61K31/495; A61K31/55; A61K45/00; A61P3/04; A61P3/06; A61P5/14; A61P9/06; A61P9/10; A61P17/00; A61P17/02; A61P17/04; A61P17/06; A61P19/10; A61P25/24; A61P27/06; A61P35/00; C07C235/32; C07C235/52; C07C237/22; C07C271/22; C07C279/12; C07C307/06; C07C311/00; C07C311/51; C07C323/41; C07C323/59; C07C323/60; C07D207/09; C07D207/26; C07D207/27; C07D209/20; C07D211/24; C07D211/34; C07D211/58; C07D211/60; C07D211/96; C07D213/38; C07D213/40; C07D213/74; C07D223/12; C07D231/38; C07D233/54; C07D241/04; C07D257/04; C07D285/06; C07D285/125; C07D285/135; C07D295/13; C07D295/185; C07D333/20; C07D333/34; C07D285/12
Domestic Patent References:
| JP2000502086A |
Foreign References:
| GB1133675B | ||||
| US4741897 |
Attorney, Agent or Firm:
Yoshiyuki Kawaguchi
Hidemi Matsukura
Mayuko Wakuda
Tsutomu Toyama
Hidemi Matsukura
Mayuko Wakuda
Tsutomu Toyama