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Last Updated: March 29, 2024

Details for Patent: 7,056,906


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Title:Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
Abstract: The present invention provides compositions, therapeutic combinations and methods including: (a) at least one hormone replacement therapy composition; and (b) at least one sterol absorption inhibitor which can be useful for treating vascular conditions in post-menopausal women and lowering plasma levels of sterols or 5.alpha.-stanols.
Inventor(s): Strony; John T. (Lebanon, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Filing Date:Sep 19, 2002
Application Number:10/247,085
Claims:1. A composition comprising: (a) at least one hormone replacement therapy composition; and (b) at least one sterol or 5.alpha.-stanol absorption inhibitor or a pharmaceutically acceptable salt thereof or a solvate thereof.

2. The composition according to claim 1, wherein the at least one hormone replacement therapy composition comprises one or more agents selected from the group consisting of androgens, estrogens, phytoestrogens, progestins, and their pharmaceutically acceptable salts.

3. The composition according to claim 2, wherein the androgens are selected from the group consisting of methyltestosterone (17-hydroxy-17-methyl-, (17B)-androst-4-en-3-one) and combinations thereof.

4. The composition according to claim 2, wherein the estrogens are selected from the group consisting of sodium estrone sulfate, sodium equilin sulfate, sodium 17.alpha.-dihydroequilin sulfate, sodium 17.alpha.-estradiol sulfate, sodium 17.beta.-dihydroequilin sulfate, sodium 17.alpha.-dihydroequilenin sulfate, sodium 17.beta.-dihydroequilenin sulfate, sodium equilenin sulfate and sodium 17.beta.-estradiol sulfate, ethinyl estradiol (19-nor-17.alpha.-pregna-1,3,5(10)-trien-20-yne-3,17-diolestropipate (piperazine estra-1,3,5(10)-trien-17-one, 3-(sulfoxy)-estrone sulfate); and combinations thereof.

5. The composition according to claim 2, wherein the phytoestrogens comprises one or more soy isoflavones.

6. The composition according to claim 2, wherein the progestins are selected from the group consisting of norethindrone, norgestrel, micronized progesterone (pregn-4-ene-3, 20-dione), medroxyprogesterone and combinations thereof.

7. The composition according to claim 2, wherein the hormone replacement therapy composition comprises a combination of progestins and estrogens selected from the group consisting of the combination of estradiol (estra-1, 3, 5 (10)-triene-3, 17.beta.-diol hemihydrate) and norethindrone (17.beta.-acetoxy-19-nor-17.alpha.-pregn-4-en-20-yn-3-one), the combination of levonorgestrel (d(-)-13.beta.-ethyl-17.alpha.-ethinyl-17.beta.-hydroxygon-4-en-3-one), the combination of ethynodiol diacetate (19-nor-17.alpha.-pregn-4-en-20-yne-3.beta.,17-diol diacetate) and ethinyl estradiol, the combination of desogestrel (13-ethyl-11-methylene-18,19-dinor-17 .alpha.-pregn-4-en-20-yn-17-ol) and ethinyl estradiol, the combination of norethindrone and ethinyl estradiol, the combination of norgestrel ((.+-.)-13-ethyl-17-hydroxy-18, 19-dinor-17.alpha.-preg-4-en-20-yn-3-one) and ethinyl estradiol, the combination of norethindrone, ethinyl estradiol, mestranol (3-methoxy-19-nor-17.alpha.-pregna-1,3,5(10)-trien-20-yn-17-ol), the combination of 17.beta.-estradiol (estra-1,3,5(10)-triene-3, 17.beta.-diol) and micronized norgestimate (17.alpha.-17-(Acetyloxyl)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one3-ox- ime), the combination of norgestimate (18,19-dinor-17-pregn-4-en-20-yn-3-one, 17-(acetyloxy)-13-ethyl-, oxime, (17(.alpha.)-(+)-) and ethinyl estradiol, and the combination of conjugated estrogens sodium estrone sulfate and sodium equilin sulfate and medroxyprogesterone acetate (20-dione, 17-(acetyloxy)-6-methyl-, (6(.alpha.))-pregn-4-ene-3).

8. The composition according to claim 2, wherein the hormone replacement therapy composition is an androgen and estrogen combination selected from the group consisting of the combination of esterified estrogens sodium estrone sulfate and sodium equilin sulfate and methyltestosterone (17-hydroxy-17-methyl-, (17B)-androst-4-en-3-one).

9. The composition according to claim 1, wherein the at least one hormone replacement therapy composition is administered to a subject in an amount ranging from about 0.1 to about 3000 milligrams of hormone replacement therapy composition per day.

10. The composition of claim 1, wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (I): ##STR00058## or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein: Ar.sup.1 and Ar.sup.2 are independently selected from the group consisting of aryl and R.sup.4-substituted aryl; Ar.sup.3 is aryl or R.sup.5-substituted aryl; X, Y and Z are independently selected from the group consisting of --CH.sub.2--, --CH(lower alkyl)- and --C(dilower alkyl)-; R and R.sup.2 are independently selected from the group consisting of --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 and --O(CO)NR.sup.6R.sup.7; R.sup.1 and R.sup.3 are independently selected from the group consisting of hydrogen, lower alkyl and aryl; q is 0 or 1; r is 0 or 1; m, n and p are independently selected from 0, 1, 2, 3 or 4; provided that at least one of q and r is 1 and the sum of m, n, p, q and r is 1, 2, 3, 4, 5 or 6; and provided that when p is 0 and r is 1, the sum of m, q and n is 1, 2, 3, 4 or 5; R.sup.4 is 1 5 substituents independently selected from the group consisting of lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5OR.sup.6, --O(CO)NR.sup.6R.sup.7, --NR.sup.6R.sup.7, --NR.sup.6(CO)R.sup.7, --NR.sup.6(CO)OR.sup.9, --NR.sup.6(CO)NR.sup.7R.sup.8, --NR.sup.6SO.sub.2R.sup.9, --COOR.sup.6, --CONR.sup.6R.sup.7, --COR.sup.6, --SO.sub.2NR.sup.6R.sup.7, S(O).sub.0-2R.sup.9, --O(CH.sub.2).sub.1-10--COOR.sup.6, --O(CH.sub.2).sub.1-10CONR.sup.6R.sup.7, -(lower alkylene)COOR.sup.6, --CH.dbd.CH--COOR.sup.6, --CF.sub.3, --CN, --NO.sub.2 and halogen; R.sup.5 is 1 5 substituents independently selected from the group consisting of --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5OR.sup.6, --O(CO)NR.sup.6R.sup.7, --NR.sup.6R.sup.7, --NR.sup.6(CO)R.sup.7, --NR.sup.6(CO)OR.sup.9, --NR.sup.6(CO)NR.sup.7R.sup.8, --NR.sup.6SO.sub.2R.sup.9, --COOR.sup.6, --CONR.sup.6R.sup.7, --COR.sup.6, --SO.sub.2NR.sup.6R.sup.7, S(O).sub.0-2R.sup.9, --O(CH.sub.2).sub.1-10--COOR.sup.6, --O(CH.sub.2).sub.1-10CONR.sup.6R.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 independently selected from the group consisting of hydrogen, lower alkyl, aryl and aryl-substituted lower alkyl; and R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl.

11. The composition according to claim 10, wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (II) below: ##STR00059##

12. The composition of claim 1, wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (III): ##STR00060## or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein, in formula (III) above: Ar.sup.1 is R.sup.3-substituted aryl; Ar.sup.2 is R.sup.4-substituted aryl; Ar.sup.3 is R.sup.5-substituted aryl; Y and Z are independently selected from the group consisting of --CH.sub.2--, --CH(lower alkyl)- and --C(dilower alkyl)-; A is selected from --O--, --S--, --S(O)-- or --S(O).sub.2--; R.sup.1 is selected from the group consisting of --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 and --O(CO)NR.sup.6R.sup.7; R.sup.2 is selected from the group consisting of hydrogen, lower alkyl and aryl; or R.sup.1 and R.sup.2 together are .dbd.O; q is 1, 2 or 3; p is 0, 1, 2, 3 or 4; R.sup.5 is 1 3 substituents independently selected from the group consisting of --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5OR.sup.9, --O(CO)NR.sup.6R.sup.7, --NR.sup.6R.sup.7, --NR.sup.6(CO)R.sup.7, --NR.sup.6(CO)OR.sup.9, --NR.sup.6(CO)NR.sup.7R.sup.8, --NR.sup.6SO.sub.2-lower alkyl, --NR.sup.6SO.sub.2-aryl, --CONR.sup.6R.sup.7, --COR.sup.6, --SO.sub.2NR.sup.6R.sup.7, S(O).sub.0-2-alkyl, S(O).sub.0-2-aryl, --O(CH.sub.2).sub.1-10--COOR.sup.6, --O(CH.sub.2).sub.1-10CONR.sup.6R.sup.7, o-halogeno, m-halogeno, o-lower alkyl, m-lower alkyl, -(lower alkylene)-COOR.sup.6, and --CH.dbd.CH--COOR.sup.6; R.sup.3 and R.sup.4 are independently 1 3 substituents independently selected from the group consisting of R.sup.5, hydrogen, p-lower alkyl, aryl, --NO.sub.2, --CF.sub.3 and p-halogeno; R.sup.6, R.sup.7 and R.sup.8 are independently selected from the group consisting of hydrogen, lower alkyl, aryl and aryl-substituted lower alkyl; and R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl.

13. The composition of claim 1 wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (IV): ##STR00061## or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein, in Formula (IV) above: A is selected from the group consisting of R.sup.2-substituted heterocycloalkyl, R.sup.2-substituted heteroaryl, R.sup.2-substituted benzofused heterocycloalkyl, and R.sup.2-substituted benzofused heteroaryl; Ar.sup.1 is aryl or R.sup.3-substituted aryl; Ar.sup.2 is aryl or R.sup.4-substituted aryl; Q is a bond or, with the 3-position ring carbon of the azetidinone, forms the spiro group ##STR00062## and R.sup.1 is selected from the group consisting of: --(CH.sub.2).sub.q--, wherein q is 2 6, provided that when Q forms a spiro ring, q can also be zero or 1; --(CH.sub.2).sub.e--G--(CH.sub.2).sub.r--, wherein G is --O--, --C(O)--, phenylene, --NR.sup.8-- or --S(O).sub.0-2--, e is 0 5 and r is 0 5, provided that the sum of e and r is 1 6; --(C.sub.2 C.sub.6 alkenylene)-; and --(CH.sub.2).sub.f--V--(CH.sub.2).sub.g--, wherein V is C.sub.3 C.sub.6 cycloalkylene, f is 1 5 and g is 0 5, provided that the sum of f and g is 1 6; R.sup.5 is selected from: ##STR00063## R.sup.6 and R.sup.7 are independently selected from the group consisting of --CH.sub.2--, --CH(C.sub.1 C.sub.6 alkyl)-, --C(di-(C.sub.1 C.sub.6) alkyl), --CH.dbd.CH-- and --C(C.sub.1 C.sub.6 alkyl).dbd.CH--; or R.sup.5 together with an adjacent R.sup.6, or R.sup.5 together with an adjacent R.sup.7, form a --CH.dbd.CH-- or a --CH.dbd.C(C.sub.1 C.sub.6 alkyl)- group; a and b are independently 0, 1, 2 or 3, provided both are not zero; provided that when R.sup.6 is --CH.dbd.CH-- or --C(C.sub.1 C.sub.6 alkyl).dbd.CH--, a is 1; provided that when R.sup.7 is --CH.dbd.CH-- or --C(C.sub.1 C.sub.6 alkyl).dbd.CH--, b is 1; provided that when a is 2 or 3, the R.sup.6's can be the same or different; and provided that when b is 2 or 3, the R.sup.7's can be the same or different; and when Q is a bond, R.sup.1 also can be selected from: ##STR00064## where M is --O--, --S--, --S(O)-- or --S(O).sub.2--; X, Y and Z are independently selected from the group consisting of --CH.sub.2--, --CH(C.sub.1 C.sub.6 alkyl)- and --C(di-(C.sub.1 C.sub.6)alkyl); R.sup.10 and R.sup.12 are independently selected from the group consisting of --OR.sup.14, --O(CO)R.sup.14, --O(CO)OR.sup.16 and --O(CO)NR.sup.14R.sup.15; R.sup.11 and R.sup.13 are independently selected from the group consisting of hydrogen, (C.sub.1 C.sub.6)alkyl and aryl; or R.sup.10 and R.sup.11 together are .dbd.O, or R.sup.12 and R.sup.13 together are .dbd.O; d is 1, 2 or 3; h is 0, 1, 2, 3 or 4; s is 0 or 1; t is 0 or 1; m, n and p are independently 0 4; provided that at least one of s and t is 1, and the sum of m, n, p, s and t is 1 6; provided that when p is 0 and t is 1, the sum of m, s and n is 1 5; and provided that when p is 0 and s is 1, the sum of m, t and n is 1 5; v is 0 or 1; j and k are independently 1 5, provided that the sum of j, k and v is 1 5; R.sup.2 is 1 3 substituents on the ring carbon atoms selected from the group consisting of hydrogen, (C.sub.1 C.sub.10)alkyl, (C.sub.2 C.sub.10)alkenyl, (C.sub.2 C.sub.10)alkynyl, (C.sub.3 C.sub.6)cycloalkyl, (C.sub.3 C.sub.6)cycloalkenyl, R.sup.17-substituted aryl, R.sup.17-substituted benzyl, R.sup.17-substituted benzyloxy, R.sup.17- substituted aryloxy, halogeno, --NR.sup.14R.sup.15, NR.sup.14R.sup.15(C.sub.1 C.sub.6 alkylene)-, NR.sup.14R.sup.15C(O)(C.sub.1 C.sub.6 alkylene)-, --NHC(O)R.sup.16, OH, C.sub.1 C.sub.6 alkoxy, --OC(O)R.sup.16, --COR.sup.14, hydroxy(C.sub.1 C.sub.6)alkyl, (C.sub.1 C.sub.6)alkoxy(C.sub.1 C.sub.6)alkyl, NO.sub.2, --S(O).sub.0-2R.sup.16, --SO.sub.2NR.sup.14R.sup.15 and --(C.sub.1 C.sub.6 alkylene)COOR.sup.14; when R.sup.2 is a substituent on a heterocycloalkyl ring, R.sup.2 is as defined, or is .dbd.O or ##STR00065## and, where R.sup.2 is a substituent on a substitutable ring nitrogen, it is hydrogen, (C.sub.1 C.sub.6)alkyl, aryl, (C.sub.1 C.sub.6)alkoxy, aryloxy, (C.sub.1 C.sub.6)alkylcarbonyl, arylcarbonyl, hydroxy, --(CH.sub.2).sub.1-6CONR.sup.16R.sup.18; ##STR00066## wherein J is --O--, --NH--, --NR.sup.18-- or --CH.sub.2--; R.sup.3 and R.sup.4 are independently selected from the group consisting of 1 3 substituents independently selected from the group consisting of (C.sub.1 C.sub.6)alkyl, --OR.sup.14, --O(CO)R.sup.14, --O(CO)OR.sup.16, --O(CH.sub.2).sub.1-5OR.sup.14, --O(CO)NR.sup.14R.sup.15, --NR.sup.14R.sup.15, --NR.sup.14(CO)R.sup.15, --NR.sup.14(CO)OR.sup.16, --NR.sup.14(CO)NR.sup.15R.sup.19, --NR.sup.14SO.sub.2R.sup.16, --COOR.sup.14, --CONR.sup.14R.sup.15, --COR.sup.14, SO.sub.2NR.sup.14R.sup.15, S(O).sub.0-2R.sup.16, --O(CH.sub.2).sub.1-10--COOR.sup.14, --O(CH.sub.2).sub.1-10CONR.sup.14R.sup.15, --(C.sub.1 C.sub.6 alkylene)-COOR.sup.14, --CH.dbd.CH--COOR.sup.14, --CF.sub.3, --CN, --NO.sub.2 and halogen; R.sup.8 is hydrogen, (C.sub.1 C.sub.6)alkyl, aryl (C.sub.1 C.sub.6)alkyl, --C(O)R.sup.14 or --COOR.sup.14; R.sup.9 and R.sup.17 are independently 1 3 groups independently selected from the group consisting of hydrogen, (C.sub.1 C.sub.6)alkyl, (C.sub.1 C.sub.6)alkoxy, --COOH, NO.sub.2, --NR.sup.14R.sup.15, OH and halogeno; R.sup.14 and R.sup.15 are independently selected from the group consisting of hydrogen, (C.sub.1 C.sub.6)alkyl, aryl and aryl-substituted (C.sub.1 C.sub.6)alkyl; R.sup.16 is (C.sub.1 C.sub.6)alkyl, aryl or R.sup.17-substituted aryl; R.sup.18 is hydrogen or (C.sub.1 C.sub.6)alkyl; and R.sup.19 is hydrogen, hydroxy or (C.sub.1 C.sub.6)alkoxy.

14. The composition of claim 1, wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (V): ##STR00067## or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein, in Formula (V) above: Ar.sup.1 is aryl, R.sup.10-substituted aryl or heteroaryl; Ar.sup.2 is aryl or R.sup.4-substituted aryl; Ar.sup.3 is aryl or R.sup.5-substituted aryl; X and Y are independently selected from the group consisting of --CH.sub.2--, --CH(lower alkyl)-, and --C(dilower alkyl)-; R is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6R.sup.7; R.sup.1 is hydrogen, lower alkyl or aryl; or R and R.sup.1 together are .dbd.O; q is 0 or 1; r is 0, 1 or 2; m and n are independently 0, 1, 2, 3, 4 or 5; provided that the sum of m, n and q is 1, 2, 3, 4 or 5; R.sup.4 is 1 5 substituents independently selected from the group consisting of lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5OR.sup.6, --O(CO)NR.sup.6R.sup.7, --NR.sup.6R.sup.7, --NR.sup.6(CO)R.sup.7, --NR.sup.6(CO)OR.sup.9, --NR.sup.6(CO)NR.sup.7R.sup.8, --NR.sup.6SO.sub.2R.sup.9, --COOR.sup.6, --CONR.sup.6R.sup.7, --COR.sup.6, --SO.sub.2NR.sup.6R.sup.7, S(O).sub.0-2R.sup.9, --O(CH.sub.2).sub.1-10--COOR.sup.6, --O(CH.sub.2).sub.1-10CONR.sup.6R.sup.7, -(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6; R.sup.5 is 1 5 substituents independently selected from the group consisting of --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5OR.sup.6, --O(CO)NR.sup.6R.sup.7, --NR.sup.6R.sup.7, --NR.sup.6(CO)R.sup.7, --NR.sup.6(CO)OR.sup.9, --NR.sup.6(CO)NR.sup.7R.sup.8, --NR.sup.6SO.sub.2R.sup.9, --COOR.sup.6, --CONR.sup.6R.sup.7, --COR.sup.6, --SO.sub.2NR.sup.6R.sup.7, S(O).sub.0-2R.sup.9, --O(CH.sub.2).sub.1-10--COOR.sup.6, --O(CH.sub.2).sub.1-10CONR.sup.6R.sup.7, --CF.sub.3, --CN, --NO.sub.2, halogen, -(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6; R.sup.6, R.sup.7 and R.sup.8 are independently selected from the group consisting of hydrogen, lower alkyl, aryl and aryl-substituted lower alkyl; R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; and R.sup.10 is 1 5 substituents independently selected from the group consisting of lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5OR.sup.6, --O(CO)NR.sup.6R.sup.7, --NR.sup.6R.sup.7, --NR.sup.6(CO)R.sup.7, --NR.sup.6(CO)OR.sup.9, --NR.sup.6(CO)NR.sup.7R.sup.8, --NR.sup.6SO.sub.2R.sup.9, --COOR.sup.6, --CONR.sup.6R.sup.7, --COR.sup.6, --SO.sub.2NR.sup.6R.sup.7, --S(O).sub.0-2R.sup.9, --O(CH.sub.2).sub.1-10--COOR.sup.6, --O(CH.sub.2).sub.1-10CONR.sup.6R.sup.7, --CF.sub.3, --CN, --NO.sub.2 and halogen.

15. The composition of claim 1, wherein the sterol or 5.alpha.-stanol absorption inhibitor selected is represented by Formula (VI): ##STR00068## or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein: R.sub.1 is ##STR00069## R.sub.2 and R.sub.3 are independently selected from the group consisting of: --CH.sub.2--, --CH(lower alkyl)-, --C(di-lower alkyl)-, --CH.dbd.CH-- and --C(lower alkyl).dbd.CH--; or R.sub.1 together with an adjacent R.sub.2, or R.sub.1 together with an adjacent R.sub.3, form a --CH.dbd.CH-- or a --CH.dbd.C(lower alkyl)- group; u and v are independently 0, 1, 2 or 3, provided both are not zero; provided that when R.sub.2 is --CH.dbd.CH-- or --C(lower alkyl).dbd.CH--, v is 1; provided that when R.sub.3 is --CH.dbd.CH-- or --C(lower alkyl).dbd.CH--, u is 1; provided that when v is 2 or 3, the R.sub.2's can be the same or different; and provided that when u is 2 or 3, the R.sub.3's can be the same or different; R.sub.4 is selected from B-(CH.sub.2).sub.mC(O)--, wherein m is 0, 1, 2, 3, 4 or 5; B--(CH.sub.2).sub.q--, wherein q is 0, 1, 2, 3, 4, 5 or 6; B--(CH.sub.2).sub.e--Z--(CH.sub.2).sub.r--, wherein Z is --O--, --C(O)--, phenylene, --N(R.sup.8)-- or --S(O).sub.0-2--, e is 0, 1, 2, 3, 4 or 5 and r is 0, 1, 2, 3, 4 or 5, provided that the sum of e and r is 0, 1, 2, 3, 4, 5 or 6; B--(C.sub.2 C.sub.6 alkenylene)-; B--(C.sub.4 C.sub.6 alkadienylene)-; B--(CH.sub.2).sub.t--Z--(C.sub.2 C.sub.6 alkenylene)-, wherein Z is as defined above, and wherein t is 0, 1, 2 or 3, provided that the sum of t and the number of carbon atoms in the alkenylene chain is 2, 3, 4, 5 or 6; B--(CH.sub.2).sub.f--V--(CH.sub.2).sub.g--, wherein V is C.sub.3 C.sub.6 cycloalkylene, f is 1, 2, 3, 4 or 5 and g is 0, 1, 2, 3, 4 or 5, provided that the sum of f and g is 1, 2, 3, 4, 5 or 6; B--(CH.sub.2).sub.t--V--(C.sub.2 C.sub.6 alkenylene)- or B--(C.sub.2 C.sub.6 alkenylene)-V--(CH.sub.2).sub.t--, wherein V and t are as defined above, provided that the sum of t and the number of carbon atoms in the alkenylene chain is 2, 3, 4, 5 or 6; B--(CH.sub.2).sub.a--Z--(CH.sub.2).sub.b--V--(CH.sub.2).sub.d--, wherein Z and V are as defined above and a, b and d are independently 0, 1, 2, 3, 4, 5 or 6, provided that the sum of a, b and d is 0, 1, 2, 3, 4, 5 or 6; or T--(CH.sub.2).sub.s--, wherein T is cycloalkyl of 3 6 carbon atoms and a is 0, 1, 2, 3, 4, 5 or 6; or R.sub.1 and R.sub.4 together form the group ##STR00070## B is selected from indanyl, indenyl, naphthyl, tetrahydronaphthyl, heteroaryl or W-substituted heteroaryl, wherein heteroaryl is selected from the group consisting of pyrrolyl, pyridinyl, pyrimidinyl, pyrazinyl, triazinyl, imidazolyl, thiazolyl, pyrazolyl, thienyl, oxazolyl and furanyl, and for nitrogen-containing heteroaryls, the N-oxides thereof, or ##STR00071## W is 1 to 3 substituents independently selected from the group consisting of lower alkyl, hydroxy lower alkyl, lower alkoxy, alkoxyalkyl, alkoxyalkoxy, alkoxycarbonylalkoxy, (lower alkoxyimino)-lower alkyl, lower alkanedioyl, lower alkyl lower alkanedioyl allyloxy, --CF.sub.3, --OCF.sub.3, benzyl, R.sub.7-benzyl, benzyloxy, R.sub.7-benzyloxy, phenoxy, R.sub.7-phenoxy, dioxolanyl, NO.sub.2, --N(R.sub.8)(R.sub.9), N(R.sub.8)(R.sub.9)-lower alkylene-, N(R.sub.8)(R.sub.9)-lower alkylenyloxy-, OH, halogeno, --CN, --N.sub.3, --NHC(O)OR.sub.10, --NHC(O)R.sub.10, R.sub.11O.sub.2SNH--, (R.sub.11O.sub.2S).sub.2N--, --S(O).sub.2NH.sub.2, --S(O).sub.0-2R.sub.8, tert-butyldimethyl-silyloxymethyl, --C(O)R.sub.12, --COOR.sub.19, --CON(R.sub.8)(R.sub.9), --CH.dbd.CHC(O)R.sub.12, -lower alkylene-C(O)R.sub.12, R.sub.10C(O)(lower alkylenyloxy)-, N(R.sub.8)(R.sub.9)C(O)(lower alkylenyloxy)- and ##STR00072## for substitution on ring carbon atoms, and the substituents on the substituted heteroaryl ring nitrogen atoms, when present, are selected from the group consisting of lower alkyl, lower alkoxy, --C(O)OR.sub.10, --C(O)R.sub.10, OH, N(R.sub.8)(R.sub.9)lower alkylene-, N(R.sub.8)(R.sub.9)-lower alkylenyloxy-, --S(O).sub.2NH.sub.2 and 2-(trimethylsilyl)-ethoxymethyl; R.sub.7 is 1 3 groups independently selected from the group consisting of lower alkyl, lower alkoxy, --COOH, NO.sub.2, --N(R.sub.8)(R.sub.9), OH, and halogeno; R.sub.8 and R.sub.9 are independently selected from H or lower alkyl; R.sub.10 is selected from lower alkyl, phenyl, R.sub.7-phenyl, benzyl or R.sub.7-benzyl; R.sub.11 is selected from OH, lower alkyl, phenyl, benzyl, R.sub.7-phenyl or R.sub.7-benzyl; R.sub.12 is selected from H, OH, alkoxy, phenoxy, benzyloxy, ##STR00073## --N(R.sub.8)(R.sub.9), lower alkyl, phenyl or R.sub.7-phenyl; R.sub.13 is selected from --O--, --CH.sub.2--, --NH--, --N(lower alkyl)- or --NC(O)R.sub.19; R.sub.15, R.sub.16 and R.sub.17 are independently selected from the group consisting of H and the groups defined for W; or R.sub.15 hydrogen and R.sub.16 and R.sub.17, together with adjacent carbon atoms to which they are attached, form a dioxolanyl ring; R.sub.19 is H, lower alkyl, phenyl or phenyl lower alkyl; and R.sub.20 and R.sub.21 are independently selected from the group consisting of phenyl, W-substituted phenyl, naphthyl, W-substituted naphthyl, indanyl, indenyl, tetrahydronaphthyl, benzodioxolyl, heteroaryl, W-substituted heteroaryl, benzofused heteroaryl, W-substituted benzofused heteroaryl and cyclopropyl, wherein heteroaryl is as defined above.

16. The composition of claim 1, wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (VIIA) or (VIIB): ##STR00074## or a pharmaceutically acceptable salt or solvate thereof, wherein: A is --CH.dbd.CH--, --C.ident.C-- or --(CH.sub.2).sub.p-- wherein p is 0, 1 or 2; ##STR00075## D is --(CH.sub.2).sub.mC(O)-- or --(CH.sub.2).sub.q-- wherein m is 1, 2, 3 or 4 and q is 2, 3 or 4; E is C.sub.10 to C.sub.20 alkyl or --C(O)--(C.sub.9 to C.sub.19)-alkyl, wherein the alkyl is straight or branched, saturated or containing one or more double bonds; R is hydrogen, C.sub.1 C.sub.15 alkyl, straight or branched, saturated or containing one or more double bonds, or B--(CH.sub.2).sub.r--, wherein r is 0, 1, 2, or 3; R.sub.1, R.sub.2, R.sub.3, R.sub.1', R.sub.2', and R.sub.3' are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, carboxy, NO.sub.2, NH.sub.2, OH, halogeno, lower alkylamino, dilower alkylamino, --NHC(O)OR.sub.5, R.sub.6O.sub.2SNH-- and --S(O).sub.2NH.sub.2; R.sub.4 is ##STR00076## wherein n is 0, 1, 2 or 3; R.sub.5 is lower alkyl; and R.sub.6 is OH, lower alkyl, phenyl, benzyl or substituted phenyl wherein the substituents are 1 3 groups independently selected from the group consisting of lower alkyl, lower alkoxy, carboxy, NO.sub.2, NH.sub.2, OH, halogeno, lower alkylamino and dilower alkylamino; or a pharmaceutically acceptable salt thereof or a prodrug thereof.

17. The composition of claim 1, wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (VIII): ##STR00077## or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein, in Formula (VIII) above, R.sup.26 is H or OG.sup.1; G and G.sup.1 are independently selected from the group consisting of ##STR00078## provided that when R.sup.26 is H or OH, G is not H; R, R.sup.a and R.sup.b are independently selected from the group consisting of H, --OH, halogeno, --NH.sub.2, azido, (C.sub.1 C.sub.6)alkoxy(C.sub.1 C.sub.6)-alkoxy or --W--R.sup.30; W is independently selected from the group consisting of --NH--C(O)--, --O--C(O)--, --O--C(O)--N(R.sup.31)--, --NH--C(O)--N(R.sup.31)-- and --O--C(S)--N(R.sup.31)--; R.sup.2 and R.sup.6 are independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl, aryl and aryl(C.sub.1 C.sub.6)alkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.3a and R.sup.4a are independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl, aryl(C.sub.1 C.sub.6)alkyl, --C(O)(C.sub.1 C.sub.6)alkyl and --C(O)aryl; R.sup.30 is selected from the group consisting of R.sup.32-substituted T, R.sup.32-substituted-T--(C.sub.1 C.sub.6)alkyl, R.sup.32-substituted-(C.sub.2 C.sub.4)alkenyl, R.sup.32-substituted-(C.sub.1 C.sub.6)alkyl, R.sup.32-substituted-(C.sub.3 C.sub.7)cycloalkyl and R.sup.32-substituted-(C.sub.3 C.sub.7)cycloalkyl(C.sub.1 C.sub.6)alkyl; R.sup.31 is selected from the group consisting of H and (C.sub.1 C.sub.4)alkyl; T is selected from the group consisting of phenyl, furyl, thienyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzothiazolyl, thiadiazolyl, pyrazolyl, imidazolyl and pyridyl; R.sup.32 is independently selected from 1 3 substituents independently selected from the group consisting of halogeno, (C.sub.1 C.sub.4)alkyl, --OH, phenoxy, --CF.sub.3, --NO.sub.2, (C.sub.1 C.sub.4)alkoxy, methylenedioxy, oxo, (C.sub.1 C.sub.4)alkylsulfanyl, (C.sub.1 C.sub.4)alkylsulfinyl, (C.sub.1 C.sub.4)alkylsulfonyl, --N(CH.sub.3).sub.2, --C(O)--NH(C.sub.1 C.sub.4)alkyl, --C(O)--N((C.sub.1 C.sub.4)alkyl).sub.2, --C(O)--(C.sub.1 C.sub.4)alkyl, --C(O)--(C.sub.1 C.sub.4)alkoxy and pyrrolidinylcarbonyl; or R.sup.32 is a covalent bond and R.sup.31, the nitrogen to which it is attached and R.sup.32 form a pyrrolidinyl, piperidinyl, N-methyl-piperazinyl, indolinyl or morpholinyl group, or a (C.sub.1 C.sub.4)alkoxycarbonyl-substituted pyrrolidinyl, piperidinyl, N-methylpiperazinyl, indolinyl or morpholinyl group; Ar.sup.1 is aryl or R.sup.10-substituted aryl; Ar.sup.2 is aryl or R.sup.11-substituted aryl; Q is a bond or, with the 3-position ring carbon of the azetidinone, forms the spiro group ##STR00079## and R.sup.1 is selected from the group consisting of --(CH.sub.2).sub.q--, wherein q is 2 6, provided that when Q forms a spiro ring, q can also be zero or 1; --(CH.sub.2).sub.e--E--(CH.sub.2).sub.r--, wherein E is --O--, --C(O)--, phenylene, --NR.sup.22-- or --S(O).sub.0-2--, e is 0 5 and r is 0 5, provided that the sum of e and r is 1 6; --(C.sub.2 C.sub.6)alkenylene-; and --(CH.sub.2).sub.f--V--(CH.sub.2).sub.g--, wherein V is C.sub.3 C.sub.6 cycloalkylene, f is 1 5 and g is 0 5, provided that the sum of f and g is 1 6; R.sup.12 is ##STR00080## R.sup.13 and R.sup.14 are independently selected from the group consisting of --CH.sub.2--, --CH(C.sub.1 C.sub.6 alkyl)-, --C(di-(C.sub.1 C.sub.6)alkyl), --CH.dbd.CH-- and --C(C.sub.1 C.sub.6 alkyl).dbd.CH--; or R.sup.12 together with an adjacent R.sup.13, or R.sup.12 together with an adjacent R.sup.14, form a --CH.dbd.CH-- or a --CH.dbd.C(C.sub.1 C.sub.6 alkyl)- group; a and b are independently 0, 1, 2 or 3, provided both are not zero; provided that when R.sup.13 is --CH.dbd.CH-- or --C(C.sub.1 C.sub.6 alkyl).dbd.CH--, a is 1; provided that when R.sup.14 is --CH.dbd.CH-- or --C(C.sub.1 C.sub.6 alkyl).dbd.CH--, b is 1; provided that when a is 2 or 3, the R.sup.13's can be the same or different; and provided that when b is 2 or 3, the R.sup.14's can be the same or different; and when Q is a bond, R.sup.1 also can be: ##STR00081## M is --O--, --S--, --S(O)-- or --S(O).sub.2--; X, V and Z are independently selected from the group consisting of --CH.sub.2--, --CH(C.sub.1 C.sub.6)alkyl- and --C(di-(C.sub.1 C.sub.6)alkyl); R.sup.10 and R.sup.11 are independently selected from the group consisting of 1 3 substituents independently selected from the group consisting of (C.sub.1 C.sub.6)alkyl, --OR.sup.19, --O(CO)R.sup.19, --O(CO)OR.sup.21, --O(CH.sub.2).sub.1-5OR.sup.19, --O(CO)NR.sup.19R.sup.20, --NR.sup.19R.sup.20, --NR.sup.19(CO)R.sup.20, --NR.sup.19(CO)OR.sup.21, --NR.sup.19(CO)NR.sup.20R.sup.25, --NR.sup.19SO.sub.2R.sup.21, --COOR.sup.19, --CONR.sup.19R.sup.20, --COR.sup.19, --SO.sub.2NR.sup.19R.sup.20, S(O).sub.0-2R.sup.21, --O(CH.sub.2).sub.1-10--COOR.sup.19, --O(CH.sub.2).sub.1-10CONR.sup.19R.sup.20, --(C.sub.1 C.sub.6 alkylene)-COOR.sup.19, --CH.dbd.CH--COOR.sup.19, --CF.sub.3, --CN, --NO.sub.2 and halogen; R.sup.15 and R.sup.17 are independently selected from the group consisting of --OR.sup.19, --O(CO)R.sup.19, --O(CO)OR.sup.21 and --O(CO)NR.sup.19R.sup.20; R.sup.16 and R.sup.18 are independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl and aryl; or R.sup.15 and R.sup.16 together are .dbd.O, or R.sup.17 and R.sup.18 together are .dbd.O; d is 1, 2 or 3; h is 0, 1, 2, 3 or 4; s is 0 or 1; t is 0 or 1; m, n and p are independently 0 4; provided that at least one of s and t is 1, and the sum of m, n, p, s and t is 1 6; provided that when p is 0 and t is 1, the sum of m, s and n is 1 5; and provided that when p is 0 and s is 1, the sum of m, t and n is 1 5; V is 0 or 1; j and k are independently 1 5, provided that the sum of j, k and v is 1 5; and when Q is a bond and R.sup.1 is ##STR00082## Ar.sup.1 can also be pyridyl, isoxazolyl, furanyl, pyrrolyl, thienyl, imidazolyl, pyrazolyl, thiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl; R.sup.19 and R.sup.20 are independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl, aryl and aryl-substituted (C.sub.1C.sub.6)alkyl; R.sup.21 is (C.sub.1 C.sub.6)alkyl, aryl or R.sup.24-substituted aryl; R.sup.22 is H, (C.sub.1 C.sub.6)alkyl, aryl (C.sub.1 C.sub.6)alkyl, --C(O)R.sup.19 or --COOR.sup.19; R.sup.23 and R.sup.24 are independently 1 3 groups independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl, (C.sub.1 C.sub.6)alkoxy, --COOH, NO.sub.2, --NR.sup.19R.sup.20, --OH and halogeno; and R.sup.25 is H, --OH or (C.sub.1 C.sub.6)alkoxy.

18. The composition of claim 1, wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (IX): ##STR00083## or a pharmaceutically acceptable salt or solvate thereof, wherein in Formula (IX): R.sup.1 is selected from the group consisting of H, G, G.sup.1, G.sup.2, --SO.sub.3H and --PO.sub.3H; G is selected from the group consisting of: H, ##STR00084## wherein R, R.sup.a and R.sup.b are each independently selected from the group consisting of H, --OH, halo, --NH.sub.2, azido, (C.sub.1 C.sub.6)alkoxy(C.sub.1 C.sub.6)alkoxy or --W--R.sup.30; W is independently selected from the group consisting of --NH--C(O)--, --O--C(O)--, --O--C(O)--N(R.sup.31)--, --NH--C(O)--N(R.sup.31)-- and --O--C(S)--N(R.sup.31)--; R.sup.2 and R.sup.6 are each independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl, acetyl, aryl and aryl(C.sub.1 C.sub.6)alkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.3a and R.sup.4a are each independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl, acetyl, aryl(C.sub.1 C.sub.6)alkyl, --C(O)(C.sub.1 C.sub.6)alkyl and --C(O)aryl; R.sup.30 is independently selected from the group consisting of R.sup.32-substituted T, R.sup.32-substituted-T-(C.sub.1 -C.sub.6)alkyl, R.sup.32-substituted-(C.sub.2 C.sub.4)alkenyl, R.sup.32-substituted-(C.sub.1 C.sub.6)alkyl, R.sup.32-substituted-(C.sub.3-C7)cycloalkyl and R.sup.32-substituted-(C.sub.3-C7)cycloalkyl(C.sub.1 C.sub.6)alkyl; R.sup.31 is independently selected from the group consisting of H and (C.sub.1 C.sub.4)alkyl; T is independently selected from the group consisting of phenyl, furyl, thienyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzothiazolyl, thiadiazolyl, pyrazolyl, imidazolyl and pyridyl; R.sup.32 is independently selected from 1 3 substituents which are each independently selected from the group consisting of H, halo, (C.sub.1 C.sub.4)alkyl, --OH, phenoxy, --CF.sub.3, --NO.sub.2, (C.sub.1 C.sub.4)alkoxy, methylenedioxy, oxo, (C.sub.1 C.sub.4)alkylsulfanyl, (C.sub.1 C.sub.4)alkylsulfinyl, (C.sub.1 C.sub.4)alkylsulfonyl, --N(CH.sub.3).sub.2, --C(O)--NH(C.sub.1 C.sub.4)alkyl, --C(O)--N((C.sub.1 C.sub.4)alkyl).sub.2, --C(O)--(C.sub.1 C.sub.4)alkyl, --C(O)--(C.sub.1 C.sub.4)alkoxy and pyrrolidinylcarbonyl; or R.sup.32 is a covalent bond and R.sup.31, the nitrogen to which it is attached and R.sup.32 form a pyrrolidinyl, piperidinyl, N-methyl-piperazinyl, indolinyl or morpholinyl group, or a (C.sub.1 C.sub.4)alkoxycarbonyl-substituted pyrrolidinyl, piperidinyl, N-methylpiperazinyl, indolinyl or morpholinyl group; G.sup.1 is represented by the structure: ##STR00085## wherein R.sup.33 is independently selected from the group consisting of unsubstituted alkyl, R.sup.34-substituted alkyl, (R.sup.35)(R.sup.36)alkyl-, ##STR00086## R.sup.34 is one to three substituents, each R.sup.34 being independently selected from the group consisting of HOOC--, HS--, (CH.sub.3)S--, H.sub.2N--, (NH.sub.2)(NH)C(NH)--, (NH.sub.2)C(O)-- and HOOCCH(NH.sub.3.sup.+)CH.sub.2SS--; R.sup.35 is independently selected from the group consisting of H and NH.sub.2--; R.sup.36 is independently selected from the group consisting of H, unsubstituted alkyl, R.sup.34-substituted alkyl, unsubstituted cycloalkyl and R.sup.34-substituted cycloalkyl; G.sup.2 is represented by the structure: ##STR00087## wherein R.sup.37 and R.sup.38 are each independently selected from the group consisting of (C.sub.1 C.sub.6)alkyl and aryl; R.sup.26 is one to five substituents, each R.sup.26 being independently selected from the group consisting of: a) H; b) --OH; c) --OCH.sub.3; d) fluorine; e) chlorine; f) --O--G; g) --O--G.sup.1; --h) --O--G.sup.2; i) --SO.sub.3H; and j) --PO.sub.3H; provided that when R.sup.1 is H, R.sup.26 is not H, --OH, --OCH.sub.3 or --O--G; Ar.sup.1 is aryl, R.sup.10-substituted aryl, heteroaryl or R.sup.10-substituted heteroaryl; Ar.sup.2 is aryl, R.sup.11-substituted aryl, heteroaryl or R.sup.11-substituted heteroaryl; L is selected from the group consisting of: a) a covalent bond; b) --(CH.sub.2).sub.q--, wherein q is 1 6; c) --(CH.sub.2).sub.e--E--(CH.sub.2).sub.r--, wherein E is --O--, --C(O)--, phenylene, --NR.sup.22-- or --S(O).sub.0-2--, e is 0 5 and r is 0 5, provided that the sum of e and r is 1 6; d) --(C.sub.2 C.sub.6)alkenylene-; e) --(CH.sub.2).sub.f--V--(CH.sub.2).sub.g--, wherein V is C.sub.3 C.sub.6cycloalkylene, f is 1 5 and g is 0 5, provided that the sum of f and g is 1 6; and ##STR00088## wherein M is --O--, --S--, --S(O)-- or --S(O).sub.2--; X, V and Z are each independently selected from the group consisting of --CH.sub.2--, --CH(C.sub.1 C.sub.6)alkyl- and --C(di-(C.sub.1 C.sub.6)alkyl)-; R.sup.8 is selected from the group consisting of H and alkyl; R.sup.10 and R.sup.11 are each independently selected from the group consisting of 1 3 substituents which are each independently selected from the group consisting of (C.sub.1 C.sub.6)alkyl, --OR.sup.19, --O(CO)R.sup.19, --O(CO)OR.sup.21, --O(CH.sub.2).sub.1-5OR.sup.19, --O(CO)NR.sup.19R.sup.20, --NR.sup.19R.sup.20, --NR.sup.19(CO)R.sup.20, --NR.sup.19(CO)OR.sup.21, --NR.sup.19(CO)NR.sup.20R.sup.25, --NR.sup.19SO.sub.2R.sup.21, --COOR.sup.19, --CONR.sup.19R.sup.20, --COR.sup.19, --SO.sub.2NR.sup.19R.sup.20, S(O).sub.0-2R.sup.21, --O(CH.sub.2).sub.1-10--COOR.sup.19, --O(CH.sub.2).sub.1-10CONR.sup.19R.sup.20, --(C.sub.1 C.sub.6 alkylene)-COOR.sup.19, --CH.dbd.CH--COOR.sup.19, --CF.sub.3, --CN, --NO.sub.2 and halo; R.sup.15 and R.sup.17 are each independently selected from the group consisting of --OR.sup.19, --OC(O)R.sup.19, --OC(O)OR.sup.21, --OC(O)NR.sup.19R.sup.20; R.sup.16 and R.sup.18 are each independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl and aryl; or R.sup.15 and R.sup.18 together are .dbd.O, or R.sup.17 and R.sup.18 together are .dbd.O; d is 1, 2 or 3; h is 0, 1, 2, 3 or 4; s is 0 or 1; t is 0 or 1; m, n and p are each independently selected from 0 4; provided that at least one of s and t is 1, and the sum of m, n, p, s and t is 1 6; provided that when p is 0 and t is 1, the sum of m, n and p is 1 5; and provided that when p is 0 and s is 1, the sum of m, t and n is 1 5; v is 0 or 1; j and k are each independently 1 5, provided that the sum of j, k and v is 1 5; Q is a bond, --(CH.sub.2).sub.q--, wherein q is 1 6, or, with the 3-position ring carbon of the azetidinone, forms the spiro group ##STR00089## wherein R.sup.12 is ##STR00090## R.sup.13 and R.sup.14 are each independently selected from the group consisting of --CH.sub.2--, --CH(C.sub.1 C.sub.6 alkyl)-, --C(di-(C.sub.1 C.sub.6)alkyl), --CH.dbd.CH-- and --C(C.sub.1 C.sub.6 alkyl).dbd.CH--; or R.sup.12 together with an adjacent R.sup.13, or R.sup.12 together with an adjacent R.sup.14, form a --CH.dbd.CH-- or a --CH.dbd.C(C.sub.1 C.sub.6 alkyl)- group; a and b are each independently 0, 1, 2 or 3, provided both are not zero; provided that when R.sup.13 is --CH.dbd.CH-- or --C(C.sub.1 C.sub.6 alkyl).dbd.CH--, a is 1; provided that when R.sup.14 is --CH.dbd.CH-- or --C(C.sub.1 C.sub.6 alkyl).dbd.CH--, b is 1; provided that when a is 2 or 3, the R.sup.13's can be the same or different; and provided that when b is 2 or 3, the R.sup.14's can be the same or different; and when Q is a bond and L is ##STR00091## then Ar.sup.1 can also be pyridyl, isoxazolyl, furanyl, pyrrolyl, thienyl, imidazolyl, pyrazolyl, thiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl; R.sup.19 and R.sup.20 are each independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl, aryl and aryl-substituted (C.sub.1 C.sub.6)alkyl; R.sup.21 is (C.sub.1 C.sub.6)alkyl, aryl or R.sup.24-substituted aryl; R.sup.22 is H, (C.sub.1 C.sub.6)alkyl, aryl (C.sub.1 C.sub.6)alkyl, --C(O)R.sup.19 or --COOR.sup.19; R.sup.23 and R.sup.24 are each independently selected from the group consisting of 1 3 substituents which are each independently selected from the group consisting of H, (C.sub.1 C.sub.6)alkyl, (C.sub.1 C.sub.6)alkoxy, --COOH, NO.sub.2, --NR.sup.19R.sup.20, --OH and halo; and R.sup.25 is H, --OH or (C.sub.1 C.sub.6)alkoxy.

19. The composition according to claim 1, wherein the at least one sterol or 5.alpha.-stanol absorption inhibitor is administered to a subject in an amount ranging from about 0.1 to about 1000 milligrams of sterol absorption inhibitor per day.

20. The composition according to claim 19, wherein the subject is a post menopausal woman.

21. The composition according to claim 1, further comprising at least one cholesterol biosynthesis inhibitor.

22. The composition according to claim 21, wherein the at least one cholesterol biosynthesis inhibitor comprises at least one HMG CoA reductase inhibitor.

23. The composition according to claim 22, wherein the at least one HMG CoA reductase inhibitor is selected from the group consisting of lovastatin, pravastatin, fluvastatin, simvastatin, atorvastatin, cerivastatin and mixtures thereof.

24. The composition according to claim 23, wherein the at least one HMG CoA reductase inhibitor is simvastatin.

25. The composition according to claim 1, further comprising at least one peroxisome proliferator-activated receptor (PPAR) activator.

26. The composition according to claim 1, further comprising at least one bile acid sequestrant.

27. The composition according to claim 1, further comprising nicotinic acid or a compound comprising a pyridine-3-carboxylate structure or a pyrazine-2-carboxylate structure, and acids, salts, esters, zwitterions and tautomers thereof.

28. The composition according to claim 1, further comprising at least one AcylCoA:Cholesterol O-acyltransferase Inhibitor.

29. The composition according to claim 1, further comprising probucol or [mono[4-[[1-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]thio]1-methyleth- yl]thio]-2,6-bis(1,1-dimethylethyl)phenyl]ester](butanedioc acid).

30. The composition according to claim 1, further comprising at least one low-density lipoprotein receptor activator.

31. The composition according to claim 1, further comprising at least one Omega 3 fatty acid.

32. The composition according to claim 1, further comprising at least one natural water soluble fiber.

33. The composition according to claim 1, further comprising at least one of plant sterols, plant stanols or fatty acid esters of plant stanols.

34. The composition according to claim 1, further comprising at least one antioxidant or vitamin.

35. A pharmaceutical composition for the treatment or of a hyperlipidemia, vascular inflammation, stroke, hypertension, diabetes, obesity, lowering a concentration of a sterol or 5.alpha.-stanol in plasma of a subject, or as a hormone replacement therapy/hyperlipidemia, vascular inflammation, stroke treatment for a subject comprising a therapeutically effective amount of the composition of claim 1 and a pharmaceutically acceptable carrier.

36. A method of treating hyperlipidaemia, vascular inflammation, stroke, hypertension, diabetes, obesity, lowering a concentration of a sterol or 5.alpha.-stanol in plasma of a subject, or as a hormone replacement therapy/hyperlipidemia, vascular inflammation, stroke treatment for a subject, comprising the step of administering to a mammal in need of such treatment an effective amount of the composition of claim 1.

37. The method according to claim 36, wherein the condition is hyperlipidemia.

38. A therapeutic combination comprising: (a) a first amount of at least one hormone replacement therapy composition; and (b) a second amount of at least one sterol or 5.alpha.-stanol absorption inhibitor or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein the first amount and the second amount together comprise a therapeutically effective amount for the treatment or prevention of a vascular condition, hypertension, diabetes, obesity, lowering a concentration of a sterol or 5.alpha.-stanol in plasma of a subject or as a hormone replacement therapy/vascular condition treatment for a subject.

39. A therapeutic combination according to claim 38, wherein the at least one hormone replacement therapy composition is administered concomitantly with the at least one sterol or 5.alpha.-stanol absorption inhibitor.

40. A therapeutic combination according to claim 38, wherein the at least one hormone replacement therapy composition and the at least one sterol or 5.alpha.-stanol sterol absorption inhibitor are present in separate treatment compositions.

41. A method of treating hyperlipidaemia, vascular inflammation, stroke, hypertension, obesity, lowering a concentration of a sterol or 5.alpha.-stanol in plasma of a subject or as a hormone replacement therapy/hyperlipidemia, vascular inflammation, stroke treatment for a mammal, comprising the step of administering to a subject in need of such treatment an effective amount of the therapeutic combination of claim 38.

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