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Title:
TETRAZOLE DERIVATIVE OF BILE ACID, PROCESS FOR ITS PREPARATION AND ITS USE AS MEDICAMENT
Document Type and Number:
Japanese Patent JP3476157
Kind Code:
B2
Abstract:

PURPOSE: To provide the subject new compound having an activity to inhibit absorption of bile acid in the small intestine and useful as a lipid level lowering agent to lower the level of cholesterol and the like by reacting bile acid with 5-aminotetrazole.
CONSTITUTION: By reacting a compound of formula G1-X in a reactive form {wherein G1 represents H, a (denatured) bile acid group of formula II [wherein R(1) represents H, formyl, acetyl, benzoyl or the like; R(2), R(3), R(4) and R(5) are each H, OH, O-formly, O-acetyl or the like] or the like; X represents a covalent bond or a group of formula II in a reactive form} with bile acids containing a tetrazolyl group in side chain of formula G2 {wherein G2 represents a group of formula IV [wherein V represents O or NH in a reactive form; W represents H; Z represents a group of formula III (wherein m is of 1 to 3; n is of 0 or 1; o is of 0, 1 or 2); R(6), R(7), R(8) or R(9) are each same as R(2)]}, the objective novel tetrazole derivatives of bile acids represented by formula G1-X-G2 useful as lipid level lowering medicaments are obtained.


Inventors:
Enhsen, Dr. Alfons
Glombik, Dr. Heiner
Kramer, Werner
Wess, Guenther
Application Number:
JP1994000094424
Publication Date:
December 10, 2003
Filing Date:
May 06, 1994
Export Citation:
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Assignee:
HOECHST AG
International Classes:
A61K31/575; A61K31/58; A61K31/675; A61P3/06; A61P9/10; C07J9/00; C07J17/00; C07J41/00; C07J43/00; (IPC1-7): C07J43/00; A61K31/58; A61K31/675; A61P3/06
Attorney, Agent or Firm:
高木 千嘉 (外2名)