Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-10-14
1998-12-08
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514423, 514451, 514460, 514510, 514824, A61K 31395, A61K 3140, A61K 3135, A61K 3121
Patent
active
058469664
ABSTRACT:
Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 and Ar.sup.2 are aryl or R.sup.4 -substituted aryl;
Ar.sup.3 is aryl or R.sup.5 -substituted aryl;
X, Y and Z are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;
R and R.sup.2 are --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ;
R.sup.1 and R.sup.3 are H or lower alkyl;
q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is 0 and r is 1, the sum of m, q and n is 1-5;
R.sup.4 is selected from lower alkyl, R.sup.5, --CF.sub.3, --CN, --NO.sub.2 and halogen;
R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;
R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl;
R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl;
are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them, and a process for preparing them.
REFERENCES:
patent: 4375475 (1983-03-01), Willard et al.
patent: 4983597 (1991-01-01), Yang et al.
patent: 5099034 (1992-03-01), Yoshida
patent: 5350868 (1994-09-01), Yoshida
patent: 5631365 (1997-05-01), Rosenblum et al.
patent: 5661145 (1997-08-01), Davis
Ram et al, Indian J. Chem., Sect B, 29B, 12 (1990), pp. 1134-1137.
Hoekman et al, J. Agric. Food Chem., 30 (1982), pp. 920-924.
Durst et al, Can. J. Chem., 50 (1972), pp. 3196-3201.
Otto et al, Liebigs Ann. Chem., (1983), pp. 1152-1161.
Panfil, et al., Heterocycles, 24, 6 (1986), pp. 1609-1617.
Schnitzer-Polokoff, et al, Comp. Biochem. Physiol., 99A (1991), pp. 665-670.
Witzum, Circulation, 80, 5 (1989), pp.1101-1114.
Illingworth, Drugs, 36(Supp. 3) (1988), pp. 63-71.
Allain, et al., Clin. Chem., 20, (1974), pp. 470-475.
Horie, et al, Atherosclerosis, 88 (1991), pp. 183-192.
Baxter, er al, J. Biological Chem., 267, 17 (1992), pp. 11705-11708.
Current Drugs: Anti-Atheroscierotic Agents--Summary Factfile, May, 1992.
Georg et al, Tet. Letters, 26, 45 (1985), pp. 3903-3906.
Hart et al, Tet. Letters, 26, 45 (1985), pp. 5493-5496.
Burnett Duane A.
Clader John W.
Dugar Sundeep
McKittrick Brian A.
Rosenblum Stuart B.
Jordan Kimberly
Magatti Anita W.
Schering Corporation
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