| 摘要 |
N-Phenyl-imidazo[1,2-a]pyridine-2-carboxamide compounds (I) and their acid or base addition salts are new. N-Phenyl-imidazo[1,2-a]pyridine-2-carboxamide compounds of formula (I) and their acid or base addition salts are new. X : phenyl optionally substituted by 1-6C alkoxy, 1-6C alkyl (both optionally substituted by halo), halo or NR aR b; R 1H, halo, 1-6C alkoxy, 1-6C alkyl or NR cR d, where the alkyl or alkoxy is optionally substituted by one or more halo, OH, amino or 1-6C alkoxy; R 2NHCH 2CH 2OCH 3, NR cR d, hydroxyiminoalkyl, alkoxyiminoalkyl, 1-6C alkylthio, 1-6C alkylsulfinyl, 1-6C alkylsulfonyl, ((1-6C alkyl) 3)silylethynyl or -SO 2-NR 5R 6; R 3H, 1-6C alkyl, 1-6C alkoxy or halo; R 4H, 1-4C alkyl, 1-4C alkoxy or F; R 5, R 6H or 1-6C alkyl; either R aR bH or 1-6C alkyl; or NR aR b4-7 membered ring; R cH; and R dH or 1-6C alkyl. An independent claim is included for intermediate compounds (A) of 5-ethylaminopyridine-2-amine and 5-(2-methoxyethylamino)pyridine-2-amine. [Image] ACTIVITY : Neuroprotective; Cerebroprotective; Anticonvulsant; Neuroleptic; Antiinflammatory; Osteopathic; Cytostatic; Antiparkinsonian; Nootropic; Antidepressant; Antiaddictive; Tranquilizer; CNS-Gen.; Vasotropic; Antiarteriosclerotic; Antiarthritic; Antirheumatic; Gastrointestinal-Gen; Antiulcer; Gastrointestinal-Gen.; Antiallergic; Antiasthmatic; Immunosuppressive; Antidiabetic; Dermatological; Endocrine-Gen; Immunusuppressant; Immunomodulator. MECHANISM OF ACTION : Nuclear receptor related protein 1 (NURR1) modulator; Hippocampus zinc finger protein 3 (HZF-3) modulator; Nuclear receptor of T-cells (NOT) modulator; Regenerating liver nuclear receptor 1 (RNR1) modulator; Transcriptionally inducible nuclear receptor (TINUR) modulator; Nuclear receptor subfamily 4, group A, member 2 (NR4A2) modulator. The ability of (I) to modulate nuclear receptor related protein 1 was tested using N2A cell lines. The results showed that the hydrochloride of 7-(isopropylamino)-N-phenylimidazo[1,2-a]pyridine-2-carboxamide exhibited an EC 5 0value of 1.6 nM. |
