INHIBIDORES NO PEPTIDILICOS DE LA UNION A LAS CELULAS DEPENDIENTES DE VLA- 4 UTILES EN EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS, AUTOINMUNES Y RESPIRATORIAS

• Main Authors: ALLEN JACOB DUPLANTIER, LOUIS STANLEY CHUPAK, JHONY JOHN MILICI
• Format: Patent
• Language: Spanish
• Published: 11.11.1999
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

LA PRESENTE INVENCION SE REFIERE A COMPUESTOS QUE TIENEN UNA ESTRUCTURA NO PEPTIDILICA Y SON ACTIVOS COMO POTENTES INHIBIDORES DE LA UNION DEL ANTIGENO-4 MUY TARDIO A PROTEINAS COMO LA MOLECULA DE ADHESION CELULAR 1 (VCAM-1), EL DOMINIO HepII/IIICS (regi¢n CS-1) DE FIBRONECTINA Y OSTEOPONTINA. Compounds of Formula (1.0.0):are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably -C(=O)-; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6):and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0):where R1a is hydrogen when R1 has the meaning of a mono-valent substituent; and R1a is a single bond when R1 has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.