| 摘要 |
2-phenylcarbonylamino-4-phenylthiazole derivatives (I), as free base, acid addition salts, hydrates and solvates are new. 2-phenylcarbonylamino-4-phenylthiazole derivatives of formula (I), as free base, acid addition salts, hydrates and solvates are new. [Image] R 1hydrogen, halo, 1-4C alkyl, alkoxy or alkylthio, trifluoroethyl, hydroxy, trifluoromethoxy, trifluoroethoxy, 3-8C cycloalkoxy, allyloxy or cyclopropylmethoxy; R 2hydrogen, halo, 1-8C alkyl or alkoxy, trifluoroethyl, perfluoro(1-4C)alkyl, 3-10C cycloalkyl, phenyl, trifluoromethoxy, trifluoroethoxy, allyloxy, 3-8C cycloalkylmethoxy, 3-8C cycloalkoxy or 3-8C cycloalkylmethyl; R 3any of 16 specified groups; proviso:R 1 and R 2 are not both hydrogen The full definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are also included for the following: (1) method for preparing (I) by reacting the carboxylic acid (II) with a 2-amino-4-phenylthiazole (III), optionally followed by conversion of precursor groups to final groups; and (2) intermediates of formulae (IIb), (IIe), (XXXXV) (all 3 optionally as 1-4C aliphatic or benzyl (optionally ring-substituted by methoxy) esters), (XXXXVIII) (optionally with free amino protected by Fmoc, benzyl, tert-butoxycarbonyl, benzyloxycarbonyl or 1-4C alkanoyl) and (IV) as new compounds. [Image] [Image] The full definitions are given in the DEFINITIONS (Full Definitions) Field. ACTIVITY : Antiarteriosclerosis; Antiinflammatory; Vasotropic; Virucide; Anti-HIV; Antibacterial: Protozoacide; Immunosuppressant; Osteopathic; Dermatological; Antiulcer; Antiarthritic; Antirheumatic; Neuroprotective; Antipsoriatic; Antiparkinsonian; Nootropic; Cytostatic; Cardiant. MECHANISM OF ACTION : (I) modulate the activity of chemokine receptors, particularly the CCR2b receptor, a target for monocyte chemotactic protein-1, with IC50 below 0.1 mu M. |
