DERIVADOS DE 2- ACILAMINO- 4- FENILETIAZOL, SU PREPARACION Y SU APLICACION EN TERAPEUTICA

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...

Full description

Saved in:
Bibliographic Details
Main Authors FLOUTARD, DANIEL, FRAISSE, PIERRE, LABEEUW, BERNARD, JEGHAM, SAMIR, CASELLAS, PIERRE
Format Patent
LanguageSpanish
Published 29.07.2008
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
Online AccessGet full text

Cover

More Information
Summary: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.
Bibliography:Application Number: CR20050008037