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Title:
AMIDINE DERIVATIVE AND DRUG CARRIER CONTAINING THE SAME AS CONSTITUENT
Document Type and Number:
Japanese Patent JP2000319200
Kind Code:
A
Abstract:

To obtain a new amidine derivative useful as a constituent of drug carrier capable of efficiently and safely carrying out the transfection of nucleic acids, polypeptides, genes and their analogues to cells.

The compound of the formula [A is an aromatic ring; X is -OCOO- or -(CH2)i-O-; (m) and (n) are each 0 or 1; (i) is 0-6; Y is a steroid], e.g. α-(5-cholesten-3β-oxy)-4-amidino-toluene hydrochloride, is obtained by condensing a compound of the formula: Z-(CH2)m-A-X [X is -OH or -(CH2)ii-Y (Y is a halogen; Z is a halogen, CN or a protected amidino)] to a steroid and then introducing thiourea into the part of Z when Z is a halogen, transforming Z to an amidino group when Z is CN or deprotecting Z when Z is a protected amidino group.


Inventors:
SHIMIZU KAZUHIRO
KOIWAI KAZUMICHI
ISOZAKI MASASHI
Application Number:
JP12946099A
Publication Date:
November 21, 2000
Filing Date:
May 11, 1999
Export Citation:
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Assignee:
TERUMO CORP
International Classes:
A61K47/28; A61K9/107; A61K9/127; A61K31/70; A61K31/702; A61K31/715; A61K31/726; A61K45/00; A61K48/00; A61K49/00; A61K49/04; A61K51/00; C07J1/00; (IPC1-7): A61K47/28; A61K9/107; A61K9/127; A61K31/702; A61K31/715; A61K31/726; A61K45/00; A61K48/00; A61K49/00; A61K49/04; A61K51/00; C07J1/00