Title:
STEROIDAL DERIVATIVES
Document Type and Number:
WIPO Patent Application WO2002062302
Kind Code:
A3
Abstract:
A compound of formula (1), wherein each of R1, R2, R4, R4', R7, R11, R12, R15, R16, R17', independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, -O-sulfonic acid, or alkyl that is optionally inserted with -NH-, -N(alkyl)-, -O-, -S-, -SO-, -SO2, -O-SO2, -SO2-O-, -SO3-O-, -CO-, -CO-O-, -O-CO-, -CO-NH-, -CO-N(alkyl)-, -NH-CO-, or-N(alkyl-CO-, and further optionally substituted with hydroxy, halo, amino, carboxyl, sulfonic acid, or -O-sulfonic acid; R3 is X-Y-, wherein X is hydrogen, amino, carboxyl, halo, sulfonic acid, -O-sulfonic acid, or alkyl; Y is -S-, -NH-, -N(alkyl)-, -SO-, -SO2, -O-SO2-, -SO2-O-, -SO3-O-, -CO-, -CO-O-, -O-CO-, -CO-N(alkyl)-CO-; R5 and R6, together, are -O-; or R5 and R6, together, are a double bond between C-5 and C-6, and R7 is oxo; each of R8, R9, R10, R13, and R14, independently, is hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, or amino; and n is 0, 1, or 2. Also disclosed are a method of treating hypocholesterolemia and a method of screening for an LXR agonist by administering a compound described above, a pharmaceutical composition containing at least one the compounds described above, and an antibody against 5alpha, 6alpha-epoxycholesterol-3-sulfate or 7-ketocholesterol-3-sulfate.
Inventors:
LIAO SHUTSUNG (US)
SONG CHING (US)
SONG CHING (US)
Application Number:
PCT/US2002/003826
Publication Date:
November 27, 2003
Filing Date:
February 07, 2002
Export Citation:
Assignee:
UNIV CHICAGO (US)
LIAO SHUTSUNG (US)
SONG CHING (US)
LIAO SHUTSUNG (US)
SONG CHING (US)
International Classes:
A61K31/56; A61K31/565; A61K31/575; A61K31/58; A61P3/00; A61P3/06; C07J1/00; C07J9/00; C07J31/00; C07J41/00; C07J71/00; C07K16/44; G01N33/566; A61K; (IPC1-7): C07J41/00; A61K31/56
Foreign References:
| US4125544A | 1978-11-14 | |||
| US4304726A | 1981-12-08 | |||
| US4193930A | 1980-03-18 | |||
| US5424463A | 1995-06-13 |
Other References:
DATABASE HCAPLUS [online] BLEAU G. ET AL.: "Cholesterol sulfate, occurrence and possible biological function as an amphipathic lipid in the membrane of the human erythrocyte", XP002963850, Database accession no. 1974:461503
See also references of EP 1385868A4
See also references of EP 1385868A4
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