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Title:
抗寄生虫活性を有する化合物及びそれを含有する医薬
Document Type and Number:
Japanese Patent JP5063860
Kind Code:
B2
Abstract:
Diamidine derivatives of formula (I) and their salts are new. Amidine derivatives of formula (I) and their salts are new. [Image] X : a group of formula (ii) or R 4; Z : -(CH 2) m-; m : 8 - 21; n : 0 or 1; Y : R 3 or a group of formula (iii); R 1 and R' 1H, alkyl, aryl, OH, O-alkyl, O-aryl, OCO-alkyl, OCO-aryl, O-CO-O-(or S or NH)-alkyl, O-CO-O-(or S or NH)-aryl, PO-(O-alkyl or O-aryl) 2, CO-O-CH 2-aryl, or cycloalkyl; R 2 and R' 2H, alkyl, CO-O-CH 2-aryl, CO-O-alkyl, or cycloalkyl; R 3 and R' 3H, alkyl, aryl, CO-O-alkyl, CO-O-aryl, COO-CH(R)-O-CO-alkyl, PO(O-alkyl, or O-aryl, or ONa) 2, or CO-O-CH(R)-aryl; R : H or alkyl; NR 1R 2, NR' 1R' 2, NR 2R 3, NR' 2R' 3a heterocycle, in which R 2 and R 3 and/or R' 2 and R' 3 may be doubly bonded to the nitrogen atom; R 4 and R' 4H or alkyl; R 1R 4, R' 1R' 4-(CH 2) p-; R 4R 2, R' 4R' 2-(CH 2) p; p : 3 - 5; and provided that: (1) when X is a group of formula (ii), then Y is R 3; and (2) when X is R 4, then Y is a group of formula (iii). [Image] Independent claims are also included for the preparation of compounds of formulae (V), (X), (VI) and (VIII). [Image] R anot defined. ACTIVITY : Protozoacide. 1,12-bis(imidazolin-2-yl) dodecane (Ib) was given orally and intraperitoneally to mice infected with Plasmodium vinckei. The dose that cleared 50 % of the infection (ED50) was 3.4 mg/kg i.p and 62 mg/kg p.o. MECHANISM OF ACTION : Not given in source material.

Inventors:
Henri, Vial
Kara, Michelle
Escale, Roger
Vidal, Valeri
Brusol, Francoise
Anslan, Mali-Roll
Application Number:
JP2004522264A
Publication Date:
October 31, 2012
Filing Date:
July 18, 2003
Export Citation:
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Assignee:
Saint-El-Nacional de la Ruché-Cheautyfique (Seienne Ales)
International Classes:
C07C257/14; A61K31/155; A61K31/27; A61K31/4025; A61K31/41; A61K31/4178; A61K31/4245; A61K31/433; A61K31/4523; A61K31/506; A61K31/664; A61P31/00; A61P33/00; A61P33/06; C07C257/20; C07C259/14; C07C269/02; C07C271/60; C07C279/24; C07C303/28; C07C309/66; C07C329/06; C07D233/24; C07D233/48; C07D239/06; C07D239/12; C07D271/06; C07D285/08; C07D291/04; C07D295/12; C07D403/12; C07F9/09; C07F9/24; C07F9/6506
Domestic Patent References:
JP2003505357A
JP2002541144A
JP2000247971A
JP2000191531A
JP10237761A
JP53125409A
JP10507446A
JP8502476A
JP52035300A
Foreign References:
GB1197929B
WO1997005182A1
US3639478
US2364075
Other References:
Journal of the Chemical Society, Chemical Communications,1976年,(7),p.240-241
Journal of Medicinal Chemistry ,1968年,11(3),p.430-441
Journal of the Chemical Society,1939年,p.1253-1257
Ann. Trop. Med. ,1938年,32,p.103-107
Lancet,1937年,II,p.1360-1363
Journal of Pharmaceutical and Biomedical Analysis,1998年,17(3),p.375-378
Collection of Czechoslovak Chemical Communications ,1995年,60(5),p.903-909
Journal of Fluorine Chemistry,1993年,65(1-2),p.157-164
Attorney, Agent or Firm:
Eiichiro Shimazaki
Naotaka Kono
Kanji Arai