DIISUBSTITUTEDDINDENE DERIVATIVE

Japanese Patent JPS5444651

A

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.

AAKE NIRUSU IENSON
TOOMASU GERAN KEMUPE
REMUBITSUTO MIKIBUAA
BENKUTO AAKE SUPARUFU

JP9500278A

April 09, 1979

August 03, 1978

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KABI AB

A61K31/14; A61K31/40; A61K31/445; A61P9/00; A61K31/135; A61P9/12; A61P25/02; A61P25/26; C07C17/10; C07C47/453; C07C67/00; C07C213/00; C07C215/38; C07C215/40; C07C217/74; C07C291/02; C07C291/04; C07D295/08; C07D295/084; (IPC1-7): A61K31/135; C07C91/24; C07C93/14; C07D295/08

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