| 摘要 |
<p>Sulfonylindoline compounds (I) and their salts are new. Sulfonylindoline compounds of formula (I) and their salts are new. R 1 : H, halo, 1-4C alkyl, 3-4C cycloalkyl, 1-3C alkoxy, CF 3or OCF 3; R 2 : H or halo; R 3 : H or CF 3; R 4 : H or 1-3C alkoxy; Y 1 : 1-8C alkylene (optionally substituted by phenyl), a partially cyclized moiety or -(CH 2) n-W 1; W 1 : O or S; n : 2-4; Z : 1-4C alkyl, 3-4C cycloalkyl, CF 3, COR a, (hetero)aryl or heterocyclic e.g. phenyl, pyrrolidinyl, pyrrolidinylone, imidazolyl, pyridinyl, piperidinyl, piperazinyl or morpholinyl (all optionally substituted by 1-2 of halo, 1-4C alkyl, 3-4C cycloalkyl, 1-4C alkoxy, CF 3, nitro, N(R) 2, -CH 2-N(R) 2, OH, CN or -X-(C(R) 2) p-COR a); X : bond, O, S or NH; R a : OR or N(R) 2; R : H or 1-4C alkyl; and p : 0-4. Provided that simultaneously, R 1and R 3are not hydrogen. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Neuroprotective; Cardiovascular-Gen.; Antiinflammatory; Antilipemic; Anorectic; Antidiabetic. MECHANISM OF ACTION : Liver X receptor modulator. The ability of (I) to transactivate Gal4-liver X receptor after the transitory transfection in COS7 cells was tested. The results showed that (I) exhibited an EC 50value of less than 1 mu M.</p> |
