2-Phenylindole, Verfahren zu deren Herstellung, diese enthaltende pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln

Novel 2-phenyl indoles are disclosed of general formula (I), wherein: R represents one of the rests -(CH2)n-S(O)m-R , -(CH2)n-NR -SO2-R , (a), and n' being integers between 4 and 12 and m and m' are 0, 1 or 2; X represents a methylene group, an imino group = NR , or an oxygen or sulphur at...

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Hauptverfasser: ANGERER, ERWIN VON, DR., 93080 PENTLING, DE, BIBERGER, CHRISTIAN, 93342 SAAL, DE, SCHNEIDER, MARTIN, DR., 13469 BERLIN, DE
Format: Patent
Sprache:ger
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Zusammenfassung:Novel 2-phenyl indoles are disclosed of general formula (I), wherein: R represents one of the rests -(CH2)n-S(O)m-R , -(CH2)n-NR -SO2-R , (a), and n' being integers between 4 and 12 and m and m' are 0, 1 or 2; X represents a methylene group, an imino group = NR , or an oxygen or sulphur atom; R and R independently of one another represent a hydrogen atom, a C1-C10 alkyl group, a benzyl, alkanoyl or alkanoyloxy, or carbamoyl rest of formula -C(O)R or -C(O)NR R or a tetrahydropyranyl group; R represents a hydrogen atom, a C1-C10 alkyl, a completely or partially fluorinated alkyl group -(CH2)o-(CF2)pCF3, o and p being independently of one another integers between 0 and 6, an (alkyl)amino or (alkyl)carbamoyl group of formula (CH2)q-Y-NR R , q being an integer between 0 and 6 and Y representing a direct bond, a methylene or carbamoyl group (a condition being that q cannot be 0 when Y is a carbonyl group and m is 2), an aryl, aralkyl or heteroaryl group; R represents a C1-C10 alkyl group or a C1-C10 alkoxy group, a phenyl or benzyl group; R , R , R and R independently of one another represent a hydrogen atom, a C1-C10 alkyl group, or a benzyl group; and R represents a methyl group and R represents a hydrogen atom, or R and R both represent a di-, tri- or tetramethylene bridge which can also have a C-C double bond at any location in the bridge. These novel compounds have strong and selective anti-oestrogen properties and are suitable for use in particular in the treatment of oestrogen-related diseases.