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Details for Patent: 7,053,080

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Details for Patent: 7,053,080

Title:Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
Abstract: The present invention provides methods for the treatment of obesity using sterol or 5.alpha.-stanol absorption inhibitors and compositions and therapeutic combinations including sterol or 5.alpha.-stanol absorption inhibitors and at least one obesity control medication.
Inventor(s): Davis; Harry R. (Berkeley Heights, NJ), Ress; Rudyard J. (Flemington, NJ), Strony; John T. (Lebanon, NJ), Veltri; Enrico P. (Princeton, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Filing Date:Sep 19, 2002
Application Number:10/247,397
Claims:1. A composition comprising: (a) at least one obesity control medication; and (b) at least one sterol absorption inhibitor or at least one 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 sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (I): ##STR00062## 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.sub.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.

3. The composition according to claim 2, wherein the sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (II) below: ##STR00063##

4. The composition according to claim 1, wherein the at least one sterol absorption inhibitor is represented by Formula (III): ##STR00064## 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.

5. The composition according to claim 1, wherein the at least one sterol absorption inhibitor is represented by Formula (IV): ##STR00065## 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 ##STR00066## 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: ##STR00067## 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: ##STR00068## 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.13are 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.13together 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 ##STR00069## 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.18R.sup.18, ##STR00070## 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.17are 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.

6. The composition according to claim 1, wherein the at least one sterol absorption inhibitor is represented by Formula (V): ##STR00071## 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.

7. The composition according to claim 1, where the at least one sterol absorption inhibitor is represented by Formula (VI): ##STR00072## or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein: R.sub.1 is ##STR00073## 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.sub.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.f13 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 s is 0, 1, 2, 3, 4, 5 or 6; or R.sub.1 and R.sub.4 together form the group ##STR00074## B is selected from indanyl, indenyl, naphthyl, tetrahydronaphthyl, heteroaryl or W-substituted beteroaryl, 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 ##STR00075## 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 ##STR00076## 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, ##STR00077## --N(R.sub.8)(R.sub.9), lower alkyl, phenyl or R.sub.7-phenyl; R.sub.13is 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.17are independently selected from the group consisting of H and the groups defined for W; or R.sub.15 is 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.

8. The composition according to claim 1, wherein the at least one sterol absorption inhibitor is represented by Formula (VIIA) or (VIIB): ##STR00078## 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; B is ##STR00079## 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 ##STR00080## 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.

9. The composition according to claim 1, wherein the at least one sterol absorption inhibitor is represented by Formula (VIII): ##STR00081## 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 ##STR00082## 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, iosthiazolyl, 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 ##STR00083## 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 ##STR00084## R.sup.13and 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.13is --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: ##STR00085## 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.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.17and 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 ##STR00086## 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.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 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.

10. The composition according to claim 1, wherein the at least one sterol absorption inhibitor is represented by Formula (IX): ##STR00087## 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, ##STR00088## 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 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 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: ##STR00089## 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--, ##STR00090## 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: ##STR00091## 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 f) ##STR00092## wherein M is --O--, --S--, --S(O)--or --S(O).sub.2--; X, Y 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.6alkylene)--COOR.sup.19, --CH.dbd.CH--COOR.sup.19, --CF.sub.3, --CN, --NO.sub.2 and halo; R.sup.15 and R.sup.17are 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.18are 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.16 together are .dbd.O, or R.sup.17and 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 ##STR00093## wherein R.sup.12 is ##STR00094## 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.13is --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 ##STR00095## 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.

11. The composition according to claim 1, wherein the at least one obesity medication is selected from the group consisting of noradrenergic agents, serotonergic agents, thermogenic agents and combinations thereof.

12. The composition according to claim 11, wherein the noradrenergic agent is selected from the group consisting of diethylpropion, mazindol, phenylpropanolamine, phentermine, phendimetrazine, phendamine tartrate, methamphetamine, phendimetrazine tartrate and combinations thereof.

13. The composition according to claim 11, wherein the serotonergic agent is selected from the group consisting of sibutramine, fenfluramine, dexfenfluramine, fluoxetine, fluvoxamine, paroxtine and combinations thereof.

14. The composition according to claim 11, wherein the thermogenic agent is selected from the group consisting of ephedrine, caffeine, theophylline, selective .beta.3-adrenergic agonists and combinations thereof.

15. The composition according to claim 1, wherein the at least one obesity control medication is administered to a mammal in an amount ranging from about 1 to about 1000 milligrams of obesity medication per day.

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

17. The composition according to claim 1, wherein the at least one obesity control medication is an alpha-blocking agent.

18. The composition according to claim 1, wherein the at least one obesity control medication is a kainite or D,L-a-amino-3-hydroxy-5-methyl-isoxazole propionic acid (AMPA) receptor antagonist.

19. The composition according to claim 1, wherein the at least one obesity control medication is a leptin-lipolysis stimulated receptor.

20. The composition according to claim 1, wherein the at least one obesity control medication is a phosphodiesterase enzyme inhibitor.

21. The composition according to claim 1, wherein the at least one obesity control medication is a compound having nucleotide sequences of the mahogany gene.

22. The composition according to claim 1, wherein the at least one obesity control medication is a fibroblast growth factor-10 polypeptide.

23. The composition according to claim 1, wherein the at least one obesity control medication is a monoamine oxidase inhibitor.

24. The composition according to claim 23, wherein the monoamine oxidase inhibitor is selected from the group consisting of befloxatone, moclobemide, brofaromine, phenoxathine, esuprone, befol, toloxatone, pirlindol, amiflamine, sercloremine, bazinaprine, lazabemide, milacemide, caroxazone and combinations thereof.

25. The composition according to claim 1, wherein the at least one obesity control medication is a compound for increasing lipid metabolism.

26. The composition according to claim 1, wherein the at least one obesity control medication is a lipase inhibitor.

27. A pharmaceutical composition for the treatment or of obesity or lowering a concentration of a sterol or 5.alpha.-stanol in plasma of a mammal, comprising a therapeutically effective amount of the composition of claim 1 and a pharmaceutically acceptable carrier.

28. A method of treating or obesity or lowering a concentration of a sterol or 5.alpha.-stanol in plasma of a mammal, comprising the step of administering to a mammal in need of such treatment an effective amount of the composition of claim 1.

29. A therapeutic combination comprising: (a) a first amount of at least one obesity control medication, and (b) a second amount of at least one sterol absorption inhibitor or 5.alpha.-stanol absorption inhibitor; wherein the first amount and the second amount together comprise a therapeutically effective amount for the treatment or of obesity or lowering a concentration of a sterol or 5.alpha.-stanol in plasma of a subject.

30. The therapeutic combination of claim 29, wherein the at least one sterol or 5.alpha.-stanol absorption inhibitor is represented by Formula (I): ##STR00096## 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.3is 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.

31. The therapeutic combination according to claim 29, wherein the at least one obesity medication is administered concomitantly with the at least one sterol or 5.alpha.-stanol absorption inhibitor.

32. The therapeutic combination according to claim 29, wherein the at least one obesity medication and the at least one sterol or 5.alpha.-stanol absorption inhibitor are present in separate treatment compositions.

33. A method of treating or obesity or lowering a concentration of a sterol in plasma of a subject, comprising the step of administering to a subject in need of such treatment an effective amount of the composition of claim 29.

34. A method of treating or obesity comprising the step of administering to a subject in need of such treatment an effective amount of a composition comprising at least one sterol or 5.alpha.-stanol absorption inhibitor.

35. A method of treating or obesity comprising the step of administering to a subject in need of such treatment an effective amount of a composition comprising at least one sterol absorption inhibitor represented by Formula (II) below: ##STR00097##
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