Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-04-23
1999-03-23
Huang, Evelyn
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142355, 514248, 514252, 514290, 514292, 514314, 514340, 514367, 514374, 514378, 514397, 514403, 514406, 514414, 548180, 548215, 548248, 548314, 5483625, 5483641, 548467, 548930, 548935, 546 85, 546111, 546156, 546169, 5462681, 544168, 544235, 544238, 544277, 544406, 544407, A61K 31395, A61K 3141, A61K 31435, A61K 31495, C07D20504
Patent
active
058859837
ABSTRACT:
Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.6, Q, and X are as defined herein.
REFERENCES:
patent: 3910931 (1975-10-01), Cavalla et al.
patent: 4123527 (1978-10-01), Melloni
patent: 4289781 (1981-09-01), Bengtsson et al.
patent: 4367232 (1983-01-01), Boix-Igleasias et al.
patent: 4576940 (1986-03-01), Tahara et al.
patent: 4581355 (1986-04-01), Tahara et al.
patent: 4607042 (1986-08-01), Pierce
patent: 4826975 (1989-05-01), Picciola et al.
patent: 5026858 (1991-06-01), Vega-Noverola et al.
patent: 5028616 (1991-07-01), Desai et al.
patent: 5032598 (1991-07-01), Baldwin et al.
patent: 5087621 (1992-02-01), Pinol
patent: 5098915 (1992-03-01), Desai et al.
patent: 5130333 (1992-07-01), Pan et al.
patent: 5189045 (1993-02-01), Peglion et al.
patent: 5212182 (1993-05-01), Musser et al.
patent: 5215989 (1993-06-01), Baldwin et al.
patent: 5292883 (1994-03-01), Martin et al.
patent: 5410057 (1995-04-01), Baroni
patent: 5527801 (1996-06-01), Masuda et al.
Frigola J et al. J. Med. Chem. 36(7), 801-10, 1993.
Nisato D and Frigerio M. J. Heterocycl. Chem. 22(4), 961-3, 1985.
Masuda K et al. Takeda Kenkyusho Ho. 31(4), 453-9, 1972.
Hirata M et al. Takeda Kenkyusho Ho. 31(2), 206-20, 1972.
Chen TY et al. Bull. Chem. Soc. Jap. 41(3), 712-6, 1968.
Melloni P et al. J. Med. Chem. 22(2), 183-91, 1978.
Bulleid & Freedman, Nature 335, 649-651 (1988). "Defective co-translational formation of disulphide bonds in protein disulphideisomerase-deficient microsomes".
Koivu et al., J. Biol. Chem. 262, 6447-6449 (1987). "A Single Polypeptide Acts Both as the .beta. Subunit of Prolyl 4-Hydroxylase and as a Protein Disulfide-Isomerase*".
Kane & Havel in the Metabolic Basis of Inherited Disease, Sixth Edition, 1139-1164 (1989). "Disorders of the Biogenesis and Secretion of Lipoproteins Containing The B Apolipoproteins".
Schaefer et al., Clin. Chem. 34, B9-B12 (1988), "Genetics and Abnormalties in Metabolism of Lipoproteins".
Drayna et al., Nature 327, 632-634 (1987). "Cloning and sequencing of human cholesteryl ester transfer protein cDNA.".
Pihlajaniemi et al., EMBO J. 6, 643-649 (1987). "Molecular cloning of the .beta.-subunit of human prolyl-4-hydroxylase. This subunit and protein disulphide isomerase are products of the same gene".
Yamaguchi et al., Biochem. Biophys. Res. Comm. 146, 1485-1492 (1987). "Sequence of Membrane-Associated Thyroid Hormone Binding Protein From Bovine Liver: Its Identity with Protein Disulphide Isomerase".
Edman et al., Nature 317, 267-270 (1985). Sequence of protein disulphide isomerase and implications of its relationship to thioredoxin.
Kao et al., Connective Tissue Research 18, 157-174 (1988). "Isolation of cDNA Clones and Genomic DNA Clones of .beta.-Subunit of Chicken Proplyl 4-Hydroxylase*".
Wetterau, J. et al., Biochem 30, 9728-9735 (1991). "Protein Disulfide Isomerase Appears Necessary To Maintain the Catalytically Active Structure of the Microsomal Triglyceride Transfer Protein".
Morton, R.E. et al., J. Biol. Chem. 256, 1992-1995 (1981), "A Plasma Inhibitor of Triglyceride and Chloesteryl Ester Transfer Activities".
Wetterau, J. et al., Biochem: 30, 4406-4412 (1991): "Structural Properties of the Microsomal Triglyceride-Transfer Protein Complex".
Wetterau, J. et al., J. Biol. Chem. 265, 9800-9807 (1990). "Protein Disulfide Isomerase Is a Component of the Microsomal Triglyceride Transfer Protein Complex".
Wetterau, J. and Zilversmit, D.B., Chem., and Phys. of Lipids 38, 205-22 (1985). "Purification and Characterization of Microsomal Triglyceride and Cholesteryl Ester Transfer Protein From Bovine Liver Microsomes".
Wetterau, J. and Zilversmit, D.B., Biochimicia et Biophysica Acta 875, 610-617 (1986). "Localization of intracellular triacylglycerol and cholesteryl ester transfer activity in rat tissues".
Wetterau, J. and Zilversmit, D.B., J. Biol. Chem. 259, 10863-10866 (1984) "A Triglyceride and Cholesteryl Ester Transfer Protein Associated with Liver Microsomes".
Wetterau, J., Grant Application entitled: "Intracellular Triglyceride Transport and Metabolism".
Presentation Materials, Aspen Bile Acid/Cholesterol Conference, Aug. 15, 1992.
Wetterau, J. R., et al., Science, vol. 258, 999-1001, Nov. 6, 1992, "Absence of Microsomal Triglyceride Transfer Protein in Individuals with Abetalipoproteinemia".
Archibald, J. L., et al., Journal of Medicinal Chemistry, vol. 14, No. 11, pp. 1054-1059.
Cortizo, L. et al., J. Med. Chem., 34, pp. 2242-2247, 1991.
Hall, I. H. et al., Pharmaceutical Research, vol. 9, No. 10, pp. 1324-1329, 1992.
Hall, I. H., et al., Pharmacological Research Communications, vol. 19, No. 12, pp. 839-858, 1987.
Murthy et al., Eur. J. Med. Chem.--Chim. Ther., vol. 20, No. 6, pp. 547-550, 1985.
Biller Scott A.
Dickson, Jr. John K.
Bristol--Myers Squibb Company
Huang Evelyn
Rodney Burton
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