摘要 |
<p>Piperazino alkyl anthranilic amides of formula (I), their salts and solvates, are new; where Ar = 6 - 14C mono- bi- or tricyclic aryl, or heteroaryl selected from pyridyl, pyrimidyl, pyrrolyl, furyl, thienyl, quinolyl, indolyl, benzothienyl, benzofuryl, benzopyranyl, benzothiopyranyl, dibenzofuryl, carbazolyl, or benzothiazinyl, all of these groups being optionally substituted by 1 - 3 groups selected from 1-8C alkyl or alkoxy, 3-8C cycloalkyl 1-6C alkyl, 3-8C cycloalkyloxy 1-6C alkyl, 3-8C cycloalkyl 1-6C alkoxy 1-6C alkyl, 3-8C cycloalkyloxy, 3-8C cycloalkyl 1-6C alkoxy, 1-6C alkoxy 1-6C alkyl, 6-14C aryl, 6-14C heteroaryl, 6-14C heteroaryl 1-6C alkyl, 6-14C aryl 1-6C alkyl, 6-14C aryl 1-6C alkyl 6-14C aryl, 6-14C aryloxy, 6-14C aryloxy 1-6C alkyl, 6-14C aryl 1-6C alkoxy, 6-14C aryl 1-6C alkoxy 1-6C alkyl, halogen, CF3, CF3O, CN, OH, NO2, NH2, COOH, 1-6C alkoxy carbonyl, carbamoyl, 1-8C alkylthio, 1-8C alkylsulphinyl, 1-8C alkylsulphonyl, sulphoamino, 1-8C alkyl sulphonyl amino, sulphamoyl, 1-8C alkyl carbonylamino, or two of these substituents may form a methylene dioxy group, with the exclusion from the definition of Ar of 4-carboxy phenyl and substituted 4- carboxy phenyl; R1, R2, and R3 = H, 1-8C alkyl, 1-6C alkoxy 1-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl 1-6C alkyl, 3-8C cycloalkyloxy 1-6C alkyl, or 3-8c cycloalkyl 1-6C alkoxy 1-6C alkyl, 6-14C aryl, 6-14C heteroaryl, 6-14C heteroaryl 1-6C alkyl, 6-14C aryl 1-6C alkyl, 6-14C aryl 1-6C alkyl 6-14C aryl, 6-14C aryl 1-6C alkoxy 1-6C alkyl, 6-14C aryloxy 1-6C alkyl, A, B, C, and D = =CH-or one or two of them may be =N-, R4, R5, and R6 = 1-8C alkyl or alkoxy, 3-8C cycloalkyl 1-6C alkyl, 3-8C cycloalkyloxy 1-6C alkyl, 3-8C cycloalkyl 1-6C alkoxy 1-6C alkyl, 1-6C alkoxy 1-6C alkyl, 6-14C aryl, 6 - 14C aryl 1-6C alkyl, 6-14C aryl 1-6C alkyl 6-14C aryl, 6-14C aryloxy, 6-14C aryloxy 1-6C alkyl, 1-14C aryl (sic) 1-6C alkoxy, 6-14C aryl 1-6C alkoxy 1-6C alkyl, halogen, CF3, CF3O, CN, OH, NO2, NH2, 1-6C alkoxy carbonyl, carbamoyl, 1-6C alkylthio, 1-8C alkylsulphinyl, 1-8C alkylsulphonyl, sulphoamino, 1-8C alkyl sulphonyl amino, sulphamoyl, 1-8C alkyl carbonyl amino, or two of these substituents may form a methylene dioxy group, or a phenyl ring condensed to the ring to which they are attached, the various aryl groups may themselves be substituted by 1-3 substituents selected from 1-8C alkyl or alkoxy, halogen, CF3, CF3O, OH, NO2, and NH2.</p> |