FOERFARANDE FOER FRAMSTAELLNING AV NYA TERAPEUTISKT ANVAENDBARA GEMINALT DISUBSTITUERADE INDENFOERENINGAR
New geminally disubstituted indenes are of general formula I (I) wherein each of R1 and R2 is hydrogen or R1 and R2 together form a direct bond or an alkylene group -(CH2)n-, in which n is an integer from 1 to 4, R3 is hydrogen, C1-3-alkoxy or halogen, and each of R4 and R5 is hydrogen or C1-4-lower...
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Zusammenfassung: | New geminally disubstituted indenes are of general formula I (I) wherein each of R1 and R2 is hydrogen or R1 and R2 together form a direct bond or an alkylene group -(CH2)n-, in which n is an integer from 1 to 4, R3 is hydrogen, C1-3-alkoxy or halogen, and each of R4 and R5 is hydrogen or C1-4-lower alkyl, or R4 and R5 together form an alkylene group -(CH2)m-, in which m is an integer from 3 to 6; and the corresponding amine oxides, quaternary ammonium compounds and salts with physiologically acceptable acids. The indenes find use in treating incontinence, as a mucous membrane decongestant, as a blood pressure reducing agent, as vasocostrictor or as an anti-reserpine agent. The indenes may be prepared by processes known per se involving (a) synthesing the side chain -CH(OH)CH2NR4R5 by a method known per se in an indenyl precursor of a formula I compound in which the side chain is incomplete or (b) introducing the double bond into an indanyl precursor of a formula I compound in which the double bond is absent or (c) releasing the terminal amino group in a precursor of a formula I compound in which the terminal amino group is protected. |
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