Patent DE-10050236-A1 (DE)
Title: Use of specified compounds as sigma-receptor ligands, useful for treating carcinomas and sarcomas
Inventor: AMSTERDAM CHRISTOPH VAN
IPC: A61K31/404
Filed: 2000-10-11
Abstract: Compounds (I) selected from a list of 49 named compounds are used as sigma -receptor ligands.  Compounds (I) selected from the following compounds or the corresponding acids, bases or salts are used as sigma -receptor ligands: (a) 3-(4-(4-Phenyl-1,2,3,6-tetrahydro-1-pyridyl)-butyl)-indol-5-ol; (b) 1-(2-(Bis-(4-fluorophenyl)methoxy)ethyl)-4-(3-phenylpropyl)piperazine; (c) 1-(4-Hydroxyphenyl)-2-(4-benzyl-1-piperidinyl)-propanol; (d) 3-(4-((3S)-3-Benzyl-1-piperidyl)-butyl)-indole-5-carbonitrile; (e) 3-(4-((3R)-3-Benzyl-1-piperidyl)-butyl)-indole-5-carbonitrile; (f) 6-(4-(4-(5-Fluoro-3-indolyl)-butyl)-1-piperazinyl)-2H-1-benzopyran-2-one; (g) (5S)-(-)-5-(4-(4-Aminobenzyl)-1-piperidylmethyl)-3-(4-ethylphenyl)-oxa zolidin-2-one; (h) 6-(3-(4-(2,4-Difluorobenzyl)-1-piperidyl)-1-oxopropyl)-2,3-dihydrobenz oxazol-2-one; (i) 3-(4-(3-(4-Fluorophenyl-hydroxymethyl)piperidin-1-yl) butyl)-5-indolcarbonitrile; (j) 2-(4-(3-(5H-Dibenz(b,f)azepin-5-yl)-propyl)-1-piperazinyl)-ethanol; (k) 1-(2-(3,4-Dimethoxyphenyl)-ethyl)-4-(3-phenylpropyl)-piperazine; (l) (5S)-(-)-5-(4-Benzyl-1-piperidylmethyl)-3-(4-chlorophenyl)oxazolidin-2 -one; (m) 6-(3-(4-(4-Fluorobenzyl)-1-piperidyl)-2-methylpropionyl)-2,3-dihydrobe nzoxazol-2-one; (n) (1R,2S)-(+)-4-(3-(4-benzyl-piperidin-1-yl)-1-hydroxy-2-methylpropyl)-p henol; (o) (E)-4-(3-(4-benzyl-piperidin-1-yl)-2-methyl propenyl)-phenol; (p) 3-(4-(4-(2,1,3-Benzothiadiazol-5-yl)-1-piperazinyl)-butyl)-indole-5-ca rbonitrile; (q) 6-(3-(4-(4-Fluorobenzyl)-1--piperidyl)-2-propenyl)-2,3-dihydrobenzoxaz ol-2 one; (r) 3-(4-Trifluoromethylphenoxymethyl)-pyrrolidine; (s) 6-(3-(4-(4-Fluorobenzyl)-1-piperidyl)-propionyl)-3H-benzothiazol-2-one ; (t) 4-(3-(4-(4-Fluorobenzyl)-piperidin-1-yl)-propoxy)-phenol; (u) (2-(4-Methoxy-3-phenethyloxy-phenyl)-ethyl)-dipropylamine; (v) (1S,5R)-3-(2-(2-Adamantyl)ethyl)-1,6,6-trimethyl-3-azabicyclo(3.2.1)oc tane; (w) 6-(3-(4-(2,4-Difluorobenzyl)-piperidin-1-yl)propionyl)-3H-benzothiazol -2-one; (x) 1-(1-(2-(4-Fluoro-phenyl)-ethyl)-piperidin-4-yl)-indan-1-ol; (y) 1-(lndol-4-yl)-4-(4-(4-fluorophenyl)-butyl)-piperazine; (z) 1-(2 (4 Fluorophenyl)-ethyl)-4-(naphthalene-2-sulfinyl)-piperidine; (a') 3-(4-(2-(2-Phenylethyl)-1-piperidyl-1-butyl)-indole; (b') 2-(4-(4-(3-lndolyl)-butyl)-1-piperazinyl)-benzonitrile; (c') (S)-(-)-5-(4-Hydroxy-4-(3,4-methylendioxyphenyl)-piperidin-1-ylmethyl) -3-(4-methoxyphenyl)-oxazolidin-2-one; (d') 5-Fluoro-3-((4-phenyl-1-piperidyl)-butyl)-indole; (e') 3-(1-Phenethyl-1,2,3,6-tetrahydro-4-pyridyl)-indole-5-carbonitrile; (f') 3-(2 Phenylethyl)-1,2,3,4,5,6-hexahydrobenz(f)isoquinoline; (g') 5-Fluoro-3-(1-phenethyl-4-piperidyl)-indole; (h') N-(1-Benzyl-4-piperidyl)-6-fluoro-1,2,3,4-tetrahydrocarbazol-3-carboxa mide; (i') 3-(4-(4-(4-Cyanophenyl)-1-piperazinyl)-butyl)-indole-5-carbonitrile; (j') 3-(3-(4-(2-Carbamoyl-5-benzofuranyl)-1-piperazinyl)-propyl)-indole-5-c arbonitrile; (k') 3-(4-(4-(4-Fluorophenyl)-1-piperazinyl)-butyl)-indole-5-carbonitrile; (l') 3-(4-(4-(2-Cyanophenyl)-piperazinyl)-butyl)-indole-5-carbonitrile; (m') 5-(3-(4-(-Fluorobenzyl)-1-piperidyl)-1-oxopropyl)-6-fluoro-2,3-dihydro -1H-benzimidazol-2-one; (n') 6-(3-(4-(4-Fluorobenzyl)-1-piperidyl)-1-oxopropyl)-2,3-dihydrobenzoxaz ol-2-one; (o') 3-(4-Benzyl-1-piperidyl)-1-(4-hydroxyphenyl)-1-propanone; (p') 3-(4-(4-(4-Fluorophenyl)-1-piperazinyl)-butyl)indole-5-carbonitrile; (q') 6-(3-(4-(4-Fluorobenzyl)-1-piperidyl)-1-hydroxypropyl)-2,3-dihydrobenz oxazol-2-one; (r') 1-(2-Methoxyphenyl)-4-(2-(6,7,8,9-tetrahydro-5H-benzocyclohepten-6-yli den)-ethyl) -piperazine; (s') 3-(1-(2-(4 Fluorophenoxy)-ethyl)-4-piperidyl)-4,5-dihydro-2H benz(g)indazole; (t') (5S)-(-)-5-(4-(4-Fluorobenzyl)-1-piperidylmethyl)-3-(4-fluorophenyl)ox azolidin-2-one; (u') 3-(4-((3R)-3-Benzyl-1-piperidyl)butyl)-5-fluoroindole; and (v') 3-(4-((3S)-3-Benzyl-1-piperidyl)butyl)-5-fluoroindole.