Patent TW-I254044-B (TW)
Title: Benzodiazepine derivatives
Inventor: ADAM GEO
IPC: A61P25/36
Filed: 2000-10-07
Granted: 2006-05-01
Abstract: The present invention relates to compounds of general formula, wherein X is a single bond or an ethynediyl group, wherein, in case X is a single bond, R1 is hydrogen; halogen; nitro; lower alkyl; halo-lower alkyl; alkoxycarbonyl; lower cycloalkyl, optionally substituted with oxygen; benzoyl, optionally substituted with lower alkyl, halo-lower alkyl, or halogen; phenyl, optionally substituted with halogen, hydroxy, lower alkyl, halo-lower alkyl, lower cycloalkyl, or lower alkoxy, halo-lower alkoxy, or cyano; styrenyl; phenylethyl; naphthyl; biphenyl; benzofuranyl; or 5 or 6 membered heterocyclic ring, optionally substituted with oxo, benzyloxy, benzoyl, methanesulfonyl, benzenesulfonyl, or acetyl; in case X is an ethynediyl group, R1 is hydrogen; lower alkyl, optionally substituted with hydroxy; halo-lower alkyl; lower cycloalkyl, optionally substituted with hydroxy, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, or halogen; lower cycloalkenyl, optionally substituted with lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, halogen, or oxo; lower alkenyl; phenyl, optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower cycloalkyl, lower alkoxy, halo; 5 or 6 membered heterocyclic ring, optionally substituted with lower alkyl, halogen, oxo, benzyloxy, benzoyl, methanesulfonyl, benzenesulfonyl, acetyl, pivaloyl, tert. butoxycarbonyl, or tert. butylcarbonyl; or benzofuranyl; R3 is phenyl; pyridine; thiophenyl or thiazolyl, which are optionally substituted by halogen, cyano, nitro, azido, hydroxy, carboxy, morpholine-4-carbonyl, carbamoyl, thiocarbamoyl, N-hydroxycarbamoyl, trimethylsilyl-ethynyl, or from lower alkyl, lower alkynyl, lower alkoxy, halo-lower alkyl, 4-lower alkyl-piperazine-1-carbonyl, lower alkylaminocarbonyl, which are optionally substituted by amino, lower alkylamino, acylamino, oxo, hydroxy; lower alkoxy, lower alkylthio, or carboxy which is optionally esterified or amidated; or a 5-membered aromatic heterocycle which is optionally substituted by amino, lower alkylamino, acylamino, oxo, hydroxy, lower alkoxy, lower alkylthio, carboxy which is optionally esterified with lower alkyl or amidated with lower alkylamino which is eventually substituted by hydroxy, or lower alkyl which is optionally substituted by halogen, hydroxy, amino, lower alkylamino, acylamino, or amidino, which is optionally substituted by lower alkyl, -C(NRR')=NR"" (where R, R' and R"" are hydrogen or lower alkyl), hydroxy, lower alkoxy, lower alkylthio, acyloxy, lower alkylsulfinyl, lower alkylsulfonyl, lower alkoxy-lower alkylsulfanyl, lower alkylsulfanyl, cycloalkylsulfinyl, cycloalkylsulfonyl, hydroxyimino, or lower alkoxyimino, which is optionally esterified or amidated, lower alkenyl, oxo, cyano, carbamoyloxy, or sulfamoyl which is optionally substituted by lower alkyl, with the proviso that, if X is a single bond and R3 is pyridinyl, R1 is not hydrogen, or methyl; and their pharmaceutically acceptable acid addition salts. The compounds according to the present invention can be used for treating or preventing acute and/or chronic neurological disorders such as psychosis, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits.