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Patent Searching and Data


Title:
ARYL AND HETEROARYL (PHOSPHINYLMETHYL)PHOSPHONATE AS SQUALENE SYNTHETASE INHIBITOR
Document Type and Number:
Japanese Patent JPH069668
Kind Code:
A
Abstract:

PURPOSE: To obtain the subject new compd. which suppresses biosynthesis of cholesterol and which is effective for hypocholesterolemia or useful as a drug for hyperlipoproteinemia or as a squalene synthetase inhibitor.

CONSTITUTION: This compd. is expressed by formula I [(m) is 0 to 3; (n) is 1 to 5; Y1, Y2 are each H or a halogen; R2 to R4 are each H, metal ions, a 1-8C alkyl, a 3-12C alkenyl or a prodrug ester; R1 is a (substd.)heterocyclic or a substd. phenyl group bonded to (CH2)n]. The compd. is, for example, (E)-(((((4-(2,6-dimethyl-1,5-heptadienyl)phenyl)methoxy)methyl)hydroxyphosphinyl) methyl)phosphonic acid. The compd. is produced from a compd. expressed by formula II (R2a is a 1-8C alkyl or a 3-12C alkenyl).


Inventors:
SUKOTSUTO EI BIRAA
Application Number:
JP11279193A
Publication Date:
January 18, 1994
Filing Date:
May 14, 1993
Export Citation:
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Assignee:
BRISTOL MYERS SQUIBB CO
International Classes:
A61K31/665; A61K31/67; A61P3/00; C07F9/38; C07F9/40; A61K31/66; (IPC1-7): C07F9/40; A61K31/66; A61K31/665; A61K31/67
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)