COMPOUNDS AND METHODS OF TREATING CELL PROLIFERATIVE DISEASES, RETINOPATHIES AND ARTHRITIS

• Main Authors: LEBLOND, BERTRAND, PETIT, SILVERE, TAVERNE, THIERRY, SCHWEIGHOFFER, FABIEN, PICARD, VIRGINIE
• Format: Patent
• Language: English; French; German
• Published: 23.11.2005
• Edition: 7
• Subjects: 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

Quinoline derivatives (I) and their tautomers, optical and geometrical isomers, racemates, salts, hydrates or mixtures are new. Quinoline derivatives of formula (I) and their tautomers, optical and geometrical isomers, racemates, salts, hydrates or mixtures are new. [Image] R 1pyran derivative of formula (a1), piperdine derivative of formula (a2), dihydropyrrole derivative of formula (a3), alkane derivative of formula (a4) or amine derivative of formula (a5); R 2H, 3-6C alkyl or 3-6C alkenyl; B : halo, preferably chlorine, hydroxyl, O-CH 2-O-CH 3(MOM), O-CH 2-O-CH 2-CH 2-O-CH 3(MEM), OSO 2-alkyl or OSi(CH 3) 2tBu; D : O, NR 3, CR'R'' or S; X, Y : O, S or a radical NR 4; R 3H, alkyl, carboxylate, acyl, carboxamide or SO 2-alkyl; R', R'' : H or alkyl radical; R 4H, 1-10C alkyl, aryl or aralkyl; linker : (CH 2) n; n : 1-10; (optionally interrupted by an heteroatom (preferably N, O , S and P) or a carbonyl group, or an aryldialkyl (preferably xylenyl); and A : quinoline derivative of formulae (a6-a7), benzopyrimidine derivative of formula (a8) or benzothiophene derivative of formula (a9) (all optionally substituted). [Image] ACTIVITY : Cytostatic; Antiangiogenic; Vasotropic; Antiarthritic; Antidiabetic; Ophthalmological. MECHANISM OF ACTION : None given.