Title:
ニコチン性アセチルコリンレセプターに於けるコリン作動性リガンドとしてのヘテロアリールジアザシクロアルカン
Document Type and Number:
Japanese Patent JP4570773
Kind Code:
B2
Abstract:
Heteroaryl diazacycloalkane derivatives (I) are new. Heteroaryl diazacycloalkane derivatives of formula (I) and their enantiomers or mixtures, isotopes and salts are new. [Image] n : 1-3 m : 0-2; R : H, alkyl, cycloalkyl, cycloalkylalkyl or aralkyl; R 1>aminophenyl; nitrophenyl; hydroxyphenyl; alkoxyphenyl; monocyclic 5-6 membered heterocyclyl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino, NO 2, COOR 3, CONR 2R 3, NHCO 2R 2and/or OCONR 2R 3); aryl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2); X-alkyl-Y-alkyl (optionally alkyl substituted by alkoxy or thioalkoxy); X-(alkyl) o-aryl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylene-dioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2); X-(alkyl) o-Z (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2), monocyclic 5-6 membered heterocyclyl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2) (sic), bicyclic heterocyclyl comprising a 5-6 membered monocyclic heterocyclyl fused to a benzene ring (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, alkoxy-alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino, NO 2, aryl optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amine and/or NO 2) or monocyclic 5-6 membered heterocyclyl (optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, alkenoxy, alkynoxy, methylenedioxy, halo, CF 3, OCF 3, CN, amino and/or NO 2); X, Y : O, S or NH, N-alkyl or Se; o : 0 or 1 and Z : 5-6 membered monocyclic heterocyclyl. ACTIVITY : Analgesic; Neuroprotective; Nootropic; Tranquilizer; Antiinflammatory; Antiaddictive; Antismoking; Anticonvulsant; Neuroleptic; Antidepressant; Antiasthmatic; Antianginal; Antimigraine. The affinity of 1-(6-chloro-5-methoxy-3-pyridyl)-homopiperazine fumaric acid salt for nicotinic Ach receptors was investigated in a test for in vitroinhibition of 3H-cytisine binding. The compound exhibited and IC 50value of 0.0007 mu M. MECHANISM OF ACTION : Nicotinic acetyl choline receptor ligand.
Inventors:
Peters Dunn
Olsen Gunnar Em
Nielsen Simon Feldbake
Nielsen Elsebeto Astergoll
Olsen Gunnar Em
Nielsen Simon Feldbake
Nielsen Elsebeto Astergoll
Application Number:
JP2000517946A
Publication Date:
October 27, 2010
Filing Date:
October 27, 1998
Export Citation:
Assignee:
NEUROSEARCH A/S
International Classes:
C07D213/74; A61K31/4406; C07D217/22; A61K31/4418; A61K31/4425; A61K31/4427; A61K31/443; A61K31/4433; A61K31/495; A61K31/496; A61K31/497; A61K31/501; A61K31/551; A61P1/12; A61P9/10; A61P11/06; A61P21/02; A61P25/00; A61P25/08; A61P25/14; A61P25/16; A61P25/28; A61P25/30; A61P29/00; C07D213/22; C07D215/38; C07D243/08; C07D401/04; C07D401/14; C07D403/04; C07D405/04; C07D409/04; C07D409/14; C07D417/04; C07D417/14
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Other References:
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XU,P. et al,STUDIES ON SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 3-SUBSTITUTED PIPERAZINO -S- (SUBSTITUTED-PHENYL)PYRIDAZINE,JOURNAL OF BEIJING MEDICAL UNIVERSITY,1991年,Vol.23, No.6,p.477-480
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SHOENEN,B. et al,Synthesis and Chemical Properties of 3-Aminoquinoline,Archiv der pharmazie,1981年,Vol.314, No.5,p.464-470
Attorney, Agent or Firm:
Mitsufumi Esaki
Blacksmith
Blacksmith