TERTIARY ARYLETHYLAMINE DERIVATIVE HAVING OPIUM DERIVATIVE-ANTAGONIC ACTIVITY

Japanese Patent JPS63290848

A

The invention relates to a group of tertiary arylethyl amine derivatives having opiate-antagonistic activity. The compounds have the general formula 1 wherein R1 is hydrogen, an optionally esterified hydroxyl group or mercapto group, a group -NHR9 or -CONHR9, wherein R9 is hydrogen, alkyl having 1-6 C-atoms or alkylcarbonyl having 1-7 C-atoms; R2 is hydrogen or, when R1 is hydrogen, one of the other meanings of R1, or R1 and R2 together with the 2 carbon atoms of the benzene ring constitute a heterocyclic group which consists of five or six ring atoms and which comprises a group -NH- and, optionally may comprise an oxygen atom, sulphur atom or nitrogen atom as a second hetero atom; R3 is hydrogen, alkyl, alkoxy or alkylthio having 1-4 C-atoms, amino, mono- or dialkylamino having 1-4 C-atoms per alkyl group, hydroxyalkyl, alkyl-, alkylamino- or alkoxycarbonyl having 1-4 C-atoms in the alkyl group, nitro, cyano, halogen, trifluoromethyl, trifluoromethoxy, alkylsulphonyl having 1-4 C-atoms, or aminosulphonyl; m has the value 1, 2 or 3; R4 is hydrogen, alkyl or alkoxy having 1-3 C-atoms, or hydroxyl; R5 is hydrogen; alkyl, phenylalkyl, hydroxyalkyl, methoxyalkyl, alkylcarbonyl, alkoxycarbonyl or alkylaminocarbonyl having 1-6 C-atoms in the optionally branched alkyl group; R6 is straight or branched alkyl, alkenyl or cycloalkylalkyl or cycloalkyl, having at most 8 C-atoms; Y is a group R7-X-R8, wherein R7 is a straight or branched alkylene chain having 3-8 C-atoms with at least 3 C-atoms between the nitrogen atom and group X; X is the carbonyl group or ketalised carbonyl group, or the group CHOH, CHC6H5, CH2, -CONH- or -CO-NCH3 or an oxygen atom or sulphur atom; and R8 is an alkyl group, cycloalkyl group or cycloalkylalkyl group having at most 10 C-atoms a phenyl group or phenylalkyl group having 1-4 C-atoms in the alkyl group, which groups R8 can be substituted with one or more groups R3; or Y is a group of the formula 2a-2e wherein R10 may have the meanings given for R3. a

INEKE FUAN UIEINFUARUDEN
YAKOBUSU ANTONIUSU YOSEFU DEN
MARUTEINUSU TEODORUSU MARIA TO
MARINUSU UIREMU ROOBEZOO

JP8237388A

November 28, 1988

April 05, 1988

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DUPHAR INT RES

A61K31/135; A61K31/215; A61K31/33; A61K31/34; A61K31/341; A61K31/38; A61K31/381; A61P25/04; A61P25/30; A61P43/00; C07C67/00; C07C209/00; C07C209/08; C07C209/16; C07C211/27; C07C211/54; C07C213/00; C07C215/08; C07C215/12; C07C215/28; C07C215/30; A61K31/165; C07C215/52; C07C215/56; C07C215/60; C07C217/60; C07C217/64; C07C217/70; C07C225/06; C07C225/10; C07C225/16; C07C231/00; C07C231/02; C07C231/12; C07C237/04; C07C237/06; C07C237/20; C07C237/30; C07C237/52; C07C253/00; C07C255/58; C07C255/60; C07C313/00; C07C323/34; C07C323/62; C07C323/65; C07C323/67; C07D207/335; C07D231/12; C07D307/52; C07D333/20; C07D521/00; (IPC1-7): A61K31/135; A61K31/165; A61K31/215; A61K31/33; A61K31/34; A61K31/38; C07C87/28; C07C87/50; C07C91/04; C07C93/02; C07C97/10; C07C103/28; C07C103/29; C07C103/76; C07C103/92; C07C121/78; C07C149/42; C07D207/335; C07D307/52; C07D333/20; C07D521/00

Akihide Sugimura (1 outside)

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