Title:
ベンズイミダゾール誘導体及びGNRH拮抗剤としてのそれらの使用
Document Type and Number:
Japanese Patent JP4418679
Kind Code:
B2
Abstract:
2-(Alkylamino or alkylthio)-5-(aminocarbonyl or aminomethyl)-benzimidazole derivatives (I) are new. 2-(Alkylamino or alkylthio)-5-(aminocarbonyl or aminomethyl)-benzimidazole derivatives of formula (I), in racemic or enantiomer form or any combination of these forms, and their salts are new. A = CH2 or CO; Y = S or NH; R1, R2 = H, 1-8C alkyl, 5-9C bicycloalkyl (optionally substituted (os) by one or more T) or -(CH2)a-X; or NR1R2 = heterocycloalkyl, heterobicycloalkyl or a spiro or fused piperidine group of formula (i), (ii), (iii) or (iv) (all os by one or more of -(CH2)c-X''-Y'', oxo, hydroxy, halo, nitro or cyano); T = 1-6C alkyl; X = NH2, NHT, NT2, adamantyl, arylcarbonyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, indanyl or tetralinyl or 3-7C cycloalkyl, heterocycloalkyl, aryl or heteroaryl (os by one or more of -(CH2)b-X'-Y', halo, oxo, NO2, CN, NH2, NHT, NT2, OH or N3); X' = O, S, C(O), C(O)O, NHC(O), NHSO2 or direct bond; Y' = T (os by one or more halo) or heteroaryl, aryl or heterocycloalkyl (all os by one or more of T, OT, halo, NO2, CN, NH2, CF3, OCF3, OH, N3, NHT or NT2); X'' = O, C(O), C(O)O or direct bond; Y'' = T, NH2, NHT, NT2, 3-7C cycloalkyl, heterocycloalkyl or aralkyl; aryl or heteroaryl (both os by one or more of T, OT, COT, halo, OH, NO2, CN, CF3, OCF3, NH2, NHT or NT2); or 1,4-benzodioxanyl, 1,3-benzodioxolyl or benzimidazol-2-on-1-yl; a = 0-6; b = 0-2; c = 0-4; R3 = -(CH2)c-W3-(CH)2d-Z3; W3 = direct bond, CH(OH) or C(O); Z3 = T, adamantyl, aryl, heteroaryl, 1,4-benzodioxanyl, 1,3-benzodioxolyl or anthraquinonyl (where all aryl groups are os by one or more of -(CH2)e-V3-Y3, halo, NO2, CN, N3 or OH; V3 = O, S, C(O), C(O)O, SO2 or direct bond; Y3 = T, os by one or more halo, NH2, NHT, NT2, CH2COPh, heterocycloalkyl or aryl; c, d, e = 0-4; R4 = -(CH2)f-R''4; R''4 = heterocycloalkyl containing at least one N (os by T or aralkyl); heteroaryl containing at least one N (os by T); or -NW4W'4; W4 = H, T or cycloalkyl; W'4 = -(CH2)g-Q4-Z4; Q4 = -CH2CH(OH)-(CH2)h-(O)i-(CH2)j or -C(O)O; Z4 = H, 1-8C alkyl (os by one or more of OT, ST, SST and OH), 2-6C alkenyl, 2-6C alkynyl, 3-7C cycloalkyl (os by one or more alkyl, COOT or -T-OH), cyclohexenyl, adamantyl, heteroaryl, aryl (os by one or more of -(CH2)k-V4-Y4, OH, NO2, halo or CN), 1,4-benzodioxanyl or 1,3-benzodioxolyl; V4 = O, S, NHC(O) or direct bond; Y4 = T (os by NT2 or one or more halo), NH2, NHT, NT2, aralkyl or heterocycloalkyl; f, g = 0-4; h, i, j = 0 or 1; and k = 0-4.
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Inventors:
Poitou, reddy
Brawl, Valery
Eric, Felandes
Treeau, christophe
Brawl, Valery
Eric, Felandes
Treeau, christophe
Application Number:
JP2003554655A
Publication Date:
February 17, 2010
Filing Date:
December 20, 2002
Export Citation:
Assignee:
Société de Conseille de Le Sherche et d'Apcursion Chantique S a S
International Classes:
C07D235/28; A61K31/4184; A61K31/427; A61K31/437; A61K31/438; A61K31/4439; A61K31/444; A61K31/454; A61K31/4545; A61K31/4725; A61K31/496; A61K31/497; A61K31/5377; A61K31/551; A61P5/24; A61P13/08; A61P15/00; A61P35/00; A61P43/00; C07D235/30; C07D401/04; C07D401/06; C07D401/12; C07D401/14; C07D403/04; C07D403/12; C07D403/14; C07D405/12; C07D405/14; C07D409/12; C07D409/14; C07D413/12; C07D417/04; C07D417/06; C07D471/04; C07D471/10; C07D521/00
Domestic Patent References:
| JP2000095767A | ||||
| JP11504040A |
Foreign References:
| WO2003041708A1 |
Attorney, Agent or Firm:
Takao Hamano
Teruichi Hirai
Teruichi Hirai