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US 6,660,724 B1Granted
Compounds and pharmaceutical compositions containing them
AssigneeIlex Products, Inc.
InventorsLan Mong Nguyen, Eric Niesor, Craig Leigh Bentzen, Hieu Trung Phan, Vinh Van Diep, Simon Floret, Raymond Azoulay, Alexandre Bulla, Yves Guyon-Gellin, Robert John Ife
Life of this patent
Estimating the term…
Abstract
Aminophosphonates alpha substituted by phenol groups of formula (I) have lipoprotein(a) lowering activity.
Claims8
A process for preparing a compound of formula (Ia):
- wherein X1 is H, C(1-3)alkyl, hydroxy or C(1-4)alkoxy;
- X2 is C(1-3)alkyl or C(1-4)alkoxy;
- X3 is H or C(1-4)alkyl;
- R1, R2, which may be identical or different, are H or C(1-3)alkyl;
- B is CH2CH2, CH═CH, or CH2;
- n is zero or 1;
- Z is H;
- m is an integer from 1 to 5;
- X4 is H, or C(1-8)alkyl, C(1-8)alkoxy or halo;
- and the pyridyl ring is attached by the ring carbon α- or β- to the nitrogen (2- or 3-pyridyl);
- which process comprises
- (a) treating an amine of formula (VII)
- in which B, R1, R2, X1, X2, X3 and n are as hereinbefore defined;
- with an aldehyde of formula (IX):
- in which m and X4 are as hereinbefore defined;
- under reductive amination conditions.
13 more elements
A compound selected from the group consisting of:
- diisopropyl α-(4-hydroxy-3-methoxy-5-methylphenyl)-N-(3-pyridyl)-aminomethylphosphonate;
- dimethyl α-(3,5-dimethoxy-4-hydroxyphenyl)-N-(3-pyridyl)-aminomethylphosphonate;
- diethyl α-(3,5-dimethoxy-4-hydroxyphenyl)-N-(3-pyridyl)-aminomethylphosphonate;
- diisopropyl α-(3,5-dimethoxy-4-hydroxyphenyl)-N-(3-pyridyl)-aminomethylphosphonate;
- diethyl α-(3,5-dimethyl-4-hydroxyphenyl)-N-(3-pyridyl)-aminomethylphosphonate;
- and
- dimethyl α-(3-methyl-4-hydroxyphenyl-5-tert-butyl)-N-(3-pyridyl)-aminomethylphosphonate.
4 more elements
Dependencies are inferred from the claim text.