DERIVATIVES OF ANTHRANILIC ACID OR THEIR PHARMACOLOGICALLY ACCEPTABLE SALTS, INTERMEDIATE COMPOUNDS USED FOR THEIR SYNTHESIS AND DRUG Russian patent published in 1999 - IPC

Abstract RU 2128644 C1

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to new derivatives of anthranilic acid of the general formula (I) or their pharmacologically acceptable salts where R1, R2, R3 and R4 are similar or distinct and mean hydrogen atom, halogen atom, optionally halogenated lower alkoxy-group, nitro-, cyano-group, pyrazolyl group, group of the formula (II) where R9 and R10 are similar or distinct and mean hydrogen atom, lower alkyl group and p = 0-6; group of the formula (III) where R13 means hydrogen atom, lower alkyl group; q = 0-2; R2 can be 1,2,4- -triazolyl group; R5 and R6 are similar or distinct and mean hydrogen atom, halogen atom, cyano-group, lower alkoxy-group, or R5 and R6 together with carbon atoms to which they are bound form oxolane, 1,3-dioxolane or 1,4-dioxolane ring; W means a group -N= or -CH= ; R7 and R8 are similar or distinct and mean hydrogen atom, lower alkyl group, or R1 and R7 together with carbon and nitrogen atoms, respectively, to which they are bound form piperidine or pyrrolidine ring; A means hydrogen atom, optionally halogenated lower alkyl group or a group of the formula: -X-(CH2)m-Z where X means -CO-, -CH2- or S(O)2-; Z means hydrogen, halogen atom, phenyl group that can be substituted with lower alkyl, lower alkoxy-, carboxy- or lower alkoxycarbonyl-group, pyridyl group, a group of the formula NR11R12 where R11 and R12 together with nitrogen atom to which they are bound form piperidine or pyrrolidine ring and the latter can be substituted with lower alkyl group, hydroxy-, carboxy-, lower alkoxycarbonyl-, cycloalkyl-group containing 3-8 carbon atoms that can be substituted with hydroxy-, cyano-, lower alkylcarbonylhydroxy-, carboxy- or lower alkoxycarbonyl-, piperidyl-group; m = 0-6; Y - oxygen atom; n = 0-6. Invention describes also a drug eliciting inhibiting activity with respect to cyclic GMP-phosphodiesterase based on compound of the formula (I). EFFECT: improved method of synthesis, enhanced effectiveness of drug. 5 cl, 143 ex

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RU 2 128 644 C1

Authors

Fumikhiro Ozaki

Kejdzhi Isibasi

Khironori Ikuta

Khiroki Isikhara

Sigeru Souda

Dates

1999-04-10Published

1994-12-27Filed