Title:
【発明の名称】エストロゲン作用薬/拮抗薬
Document Type and Number:
Japanese Patent JP2972347
Kind Code:
B2
Abstract:
Heterocyclic derivs. of formula (I) and their optical and geometric isomers and acid addn. salts, esters, N-oxides and quat. ammonium salts are new. A = CH2 or NR; B, D, E = CH or N; Y = phenyl, naphthyl, a 5- or 6-membered heterocycle contg. up to two of O, NR2 or S(O)n (opt benzo-fused) (all opt. substd. by 1-3 R4) or 3-8C cycloalkyl or cycloalkenyl (both opt. substd. by 1-2 R4); Z1 = (CH2)pW(CH2)q, O(CH2)pCR5R6, O(CH2)pN(CH2)q, OCHR2CHR3 or SCHR2CHR3; G = NR7R8, a bicyclic amine contg. 5-12C either bridge or fused (opt. substd. by 1-3 R4); or a gp. of formula (a) (opt. fused with 1-2 Ph and opt. substd. by 1-3 R4 on C and R4 on N); n = 0-2; m = 1-3; Z2 = NH, O, S or CH2; or Z1+G = a gp. of formula (b); W = CH2, CH=CH, O, NR2, S(O)n, CO, CH2OH, CONR2, NR2CO, Ctriple boundC or a gp. of formula (c); R = H or 1-6C alkyl; R2, R3 = H or 1-4C alkyl; R4 = H, halo, 1-6C alkyl, 1-4C alkoxy, 1-4C acyloxy, 1-4C alkylthio, 1-4C alkylsulphinyl, 1-4C alkylsulphonyl, 1-4C hydroxyalkyl, aryl(1-4C alkyl), CO2H, CN, CONHOR, SO2NHR, NH2, 1-4C alkylamino, 1-4C dialkylamino, NHSO2R, NO2, aryl or OH; R5, R6 = 1-8C alkyl; or R5+R6 = 3-10C ring; R7, R8 = Ph, opt. unsatd. 3-10C carbocycle, or 3-10C heterocycle contg. up to 2 or O, N or S; H, 1-6C alkyl; or with R5 or R6 form a 3-8 membered N-contg. ring; (all opt. substd. by 1-3 of 1-6C alkyl, halo, OH, alkoxy or COOH); any ring formed by R7 and R8 is opt. benzo fused; l = 0-2; p, q = 0-3. The intermediates 1-(2-(4-(6-methoxy-3-4-dihydro-naphthalen-1-yl) phenoxy) ethyl) pyrrolidine (IIa) and 1-(2-(4-(2-bromo-6-methoxy-3,'4-dihydro-naphthalen-1-yl) phenoxy) ethyl) pyrrolidine (III) are also new.
Inventors:
KAMERON KINBARII OO
JAADEIN HOORU EI DASHIRUA
ROSATEI ROBAATO ERU
JAADEIN HOORU EI DASHIRUA
ROSATEI ROBAATO ERU
Application Number:
JP52152896A
Publication Date:
November 08, 1999
Filing Date:
April 24, 1995
Export Citation:
Assignee:
FUAIZAA INC
International Classes:
A61K31/00; A61K31/395; A61K31/40; A61K31/425; A61K31/426; A61K31/428; A61K31/44; C07D295/06; A61K31/4418; A61K31/4427; A61K31/445; A61K31/47; A61K31/4709; A61K31/472; A61K31/4725; A61P3/06; A61P5/30; A61P5/32; A61P9/00; A61P35/00; C07C35/36; C07D213/64; C07D217/00; C07D217/04; C07D217/16; C07D237/02; C07D237/06; C07D275/02; C07D277/02; C07D277/62; C07D295/00; C07D295/08; C07D295/092; C07D401/04; C07D401/10; C07D401/12; C07D403/04; A61K; C07D; (IPC1-7): C07D213/64; C07D217/16; C07D295/06; C07D295/08; C07D401/12
Other References:
【文献】米国特許3234090(US,A)
【文献】米国特許3274213(US,A)
【文献】米国特許3277106(US,A)
【文献】米国特許3274213(US,A)
【文献】米国特許3277106(US,A)
Attorney, Agent or Firm:
Kazuo Shamoto (4 outside)