New hexahydropyridazine-3-carboxylic hydrazide or hydrazone derivatives are protease and kinase inhibitors, useful for treating cancer and cardiovascular, CNS, inflammatory, infectious or bone diseases

• Main Authors: GOURVEST JEAN FRANCOIS, BHATNAGAR NEERJA, MAUGER JACQUES, BROTO PIERRE
• Format: Patent
• Language: English; French
• Published: 19.12.2003
• Edition: 7
• Subjects: APPARATUS THEREFOR; CHEMISTRY; GENERAL METHODS OF ORGANIC CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; TESTING

2-(N-Substituted aminoalkanoyl or carbamoyl)-hexahydropyridazine-3-carboxylic hydrazide or hydrazone derivatives (I) are new. Hexahydropyridazine derivatives of formula (I), including all possible isomers, racemates, enantiomers and diastereomers, and their mineral or organic acid or base addition salts are new. n = 0-6; R1 = -CO-(CH2)m-R, -CO-NH-(CH2)m-R, -CS-NH-(CH2)m-R or -SO2-(CH2)m-R; m = 0-6, a double bond optionally being present in (CH2)m if m is more than 2; R = H (provided that m is other than 0), OH, SH, CN, OT, aryloxy, aralkoxy or 3-6C cycloalkyl; mono- or bicyclic, saturated or unsaturated heterocyclyl (optionally substituted by 1-3 groups Q); 6-10C aryl or 7-11C aralkyl (both optionally ring-substituted by 1-3 groups Q'); or NR4R5; T = 1-6C alkyl; Q = OH, SH, NH2, NO2, CN, COOH, CONH2, halo, CF3, T, OT, 2-6C acyl, aryl, aralkyl or mono- or bicyclic, saturated or unsaturated heterocyclyl (T, aryl, aralkyl or heterocyclyl being themselves optionally substituted by 1-3 of OH, SH, NH2, NO2, CN, COOH, CONH2, halo or CF3); Q' = as Q but not optionally substituted aryl or aralkyl; R4 = H or T; R5 = H, T or aryl; R2 = H or as for R1; N = R3 = N-R'3 or N=R''3; R'3 = as R1; and R''3 = as R. Independent claims are also included for: (1) Combinatorial libraries of compounds (I), in the form of a row matrix comprising at least two rows each containing at least 2 (preferably at least 5) individual compounds and/or containing at least 4 individual compounds; and (2) The preparation of (I) (optionally in combinatorial library form). L'invention a pour objet un composé de formule générale (I): L'invention a aussi pour objet les chimiothèques les contenant, leur utilisation comme médicaments, compositions pharmaceutiques et leurs procédés de préparation.