Steroidal derivatives

Details Steroidal derivatives Steroidal derivatives

C - Chemistry, Metallurgy

07

J

C07J 71/00 (2006.01) A61K 31/56 (2006.01) A61K 31/565 (2006.01) A61K 31/575 (2006.01) A61K 31/58 (2006.01) A61P 3/00 (2006.01) A61P 3/06 (2006.01) C07J 1/00 (2006.01) C07J 9/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07K 16/26 (2006.01) C07K 16/44 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2438221

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 5.alpha., 6.alpha.-epoxycholesterol-3-sulfate or 7-ketocholesterol-3-sulfate.

La présente invention concerne un composé de la formule (1), dans laquelle R¿1?, R¿2?, R¿4?, R¿4'?, R¿7?, R¿11?, R¿12?, R¿15?, R¿16?, R¿17'? sont, chacun indépendamment, hydrogène, hydroxy, amino, carboxyle, oxo, halo, acide sulfonique, acide -O-sulfonique ou un alkyle dans lequel a été facultativement inséré -NH-, -N(alkyl)-, -O-, -S-, -SO-, -SO¿2?, -O-SO¿2?, -SO¿2?-O-, -SO¿3?-O-, -CO-, -CO-O-, -O-CO-, -CO-NH-, -CO-N(alkyl)-, -NH-CO-, ou-N(alkyl)-CO-, et encore facultativement substitué par hydroxy, halo, amino, carboxyle, acide sulfonique ou acide -O-sulfonique; R¿3? est X-Y-, où X est hydrogène, amino, carboxyle, halo, acide sulfonique, acide -O-sulfonique ou alkyle; Y est -S-, -NH-, -N(alkyl)-, -SO-, -SO¿2?, -O-SO¿2?-, -SO¿2?-O-, -SO¿3?-O-, -CO-, -CO-O-, -O-CO-, -CO-N(alkyl)-CO-; R¿5? et R¿6 ?sont, ensemble, -O-; ou R¿5? et R¿6 ?sont, ensemble, une double liaison entre C-5 et C-6, et R¿7? est oxo; R¿8?, R¿9?, R¿10?, R¿13? et R¿14? sont, chacun indépendamment, hydrogène, alkyle, haloalkyle, hydroxyalkyle, alcoxy, hydroxy ou amino; et n est 0, 1, ou 2. L'invention concerne également un procédé qui permet de traiter l'hypocholestérolémie et un procédé qui permet de cribler un agoniste du LXR en administrant un des composés décrits ci-dessus, une composition pharmaceutique contenant au moins l'un des composés précités, et un anticorps dirigé contre le 5.alpha.,6.alpha.-epoxycholestérol-3-sulfate ou le 7-cétocholestérol-3-sulfate.

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