Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1994-04-14
1995-08-15
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
514553, 514 79, 514 80, 514 82, 562 11, 562 13, 546 22, 548113, 548413, 540450, 540480, 540542, A61K 3166, C07F 940, C07F 944
Patent
active
054419468
ABSTRACT:
This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
REFERENCES:
patent: 5317015 (1994-05-01), Ullrich et al.
J. Med. Chem., vol. 31, No. 10, pp. 1869-1871 (Oct. 1988), Biller, et al., Isoprenoid (Phosphinylmethyl)phosphonates as Inhibitors of Squalene Synthetase, English Original.
J. Am. Chem. Soc., vol. 111, No. 10, pp. 3734-3739 (1989), Poulter, et al., Squalene Synthetase. Inhibition by Ammonium Analogues of Carbocationic Intermediates in e Conversion, English Original.
J. Am. Chem. Soc., vol. 104, No. 25, pp. 7346-7378 (1982), Sandifer, et al., Squalene Synthetase. Inhibition by an Ammonium Analogue of a Carbocationic Intermediate in the Conversion, English Original.
Amin Dilip V.
Choi Yong-Mi
Pauls Henry W.
Ivy C. Warren
Nicholson James A.
Owens A. A.
Rhone-Poulenc-Rorer Pharmaceuticals, Inc.
Savitzky Martin F.
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