BENZOTHIAZOLONE COMPOUNDS, METHODS AND INTERMEDIATE COMPOUNDS FOR THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel derivatives of benzothiazolone of the general formula (I) β₂- where X means or -SO₂NH-; p, q and r = 2 or 3 being independently each of other; Y means thienyl optionally substituted with -NHSO₂--alkyl or halogen atom or phenylthio-group or phenyl optionally substituted with C_1-6-alkyl or halogen atom; each of R means independently H or C_1-6-alkyl, its optical isomers and pharmaceutically acceptable salts. Method of synthesis of compound of the formula (I) or its pharmaceutically acceptable salt involves selective reductive alkylation of compound of the formula (II) C_1-6 with compound of the formula (III) in the presence of reducing agent or by selective reduction of compound of the formula (IV) . Amide of the formula (VI) , acid of the formula (V) and aldehyde of the formula (III) are used as intermediate compounds for synthesis of benzothiazolone of the formula (I). Invention relates to also a pharmaceutical composition eliciting agonistic effect with respect to DA₂-receptors and β₂-adrenoreceptors and containing compound of the formula (I) or its pharmaceutically acceptable salt dispersed in propellant optionally containing vehicle, lubricating agents or stabilizing agents or as dry powder for inhalation optionally including pharmaceutically acceptable carrier. EFFECT: new derivatives of benzothiazolone indicated above, improved methods of synthesis, valuable pharmacological properties. 18 cl, 9 ex