Methods and compositions for preventing and treating bone loss
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/58
A61K-031/56
A61K-031/44
출원번호
US-0984425
(1997-12-03)
발명자
/ 주소
Fuh Vivian L.
Kaufman Keith D.
Waldstreicher Joanne
출원인 / 주소
Merck & Co., Inc.
대리인 / 주소
Fitch
인용정보
피인용 횟수 :
40인용 특허 :
4
초록
Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for inhibiting bone loss and treating or preventing osteoporosis and osteopenia.
대표청구항▼
[ What is claimed is:] [1.] A method of inhibiting bone loss in a subject in need of such treatment comprising administration to the subject of an effective amount of a compound of structural formula I: [ STR 10 ] or a pharmaceutically acceptable salt or ester thereof wherein: the C1--C2 carbon-carb
[ What is claimed is:] [1.] A method of inhibiting bone loss in a subject in need of such treatment comprising administration to the subject of an effective amount of a compound of structural formula I: [ STR 10 ] or a pharmaceutically acceptable salt or ester thereof wherein: the C1--C2 carbon-carbon bond may be a single bond, or a double bond as indicated by the dashed line;R.sup.1 is selected from the group consisting of hydrogen and C.sub.1-10 alkyl;R.sup.2 is selected from the group consisting of hydrogen and C.sub.1-10 alkyl;one of R.sup.3 and R.sup.4 is selected from the group consisting of hydrogen and methyl, and the other is selected from the group consisting of:(a) amino;(b) cyano;(c) fluoro;(d) methyl;(e) OH;(f) --C(O)NR.sub.b R.sub.c, where R.sub.b and R.sub.c are independently H, C.sub.1-6 alkyl, aryl, or arylC.sub.1-6 alkyl; wherein the alkyl moiety can be substituted with 1-3 of: halo; C.sub.1-4 alkoxy; or trifluoromethyl; and the aryl moiety can be substituted with 1-3 of: halo; C.sub.1-4 alkyl; C.sub.1-4 alkoxy; or trifluoromethyl;(g) C.sub.1-10 alkyl--X--;(h) C.sub.2-10 alkenyl--X--;wherein the C.sub.1-10 alkyl in (g) and C.sub.2-10 alkenyl in (h) can be unsubstituted or substituted with one to three of:i) halo; hydroxy; cyano; nitro; mono-, di- or trihalomethyl; oxo; hydroxysulfonyl; carboxy;ii) hydroxyC.sub.1-6 alkyl; C.sub.1-6 alkyloxy; C.sub.1-6 alkylthio; C.sub.1-6 alkylsulfonyl; C.sub.1-6 alkyloxycarbonyl; in which the C.sub.1-6 alkyl moiety can be further substituted with 1-3 of: halo; C.sub.1-4 alkoxy; or trifluoromethyl;iii) arylthio; aryl; aryloxy; arylsulfonyl; aryloxycarbonyl; in which the aryl moiety can be further substituted with 1-3 of: halo; C.sub.1-4 alkyl; C.sub.1-4 alkoxy; or trifluoromethyl;iv) --C(O)NR.sub.b R.sub.c ; --N(R.sub.b)--C(O)--R.sub.c ; --NR.sub.b R.sub.c ; where R.sub.b and R.sub.c are defined above;(i) aryl--X--;(j) heteroaryl--X--, wherein heteroaryl is a 5, 6 or 7 membered heteroaromatic ring containing at least one member selected from the group consisting of: one ring oxygen atom, one ring sulfur atom, 1-4 ring nitrogen atoms, or combinations thereof; in which the heteroaromatic ring can also be fused with one benzo or heteroaromatic ring;wherein the aryl in (i) and heteroaryl in (j) can be unsubstituted or substituted with one to three of:v) halo; hydroxy; cyano; nitro; mono-, di- or trihalomethyl; mono-, di- or trihalomethoxy; C.sub.2-6 alkenyl; C.sub.3-6 cycloalkyl; formyl; hydrosulfonyl; carboxy; ureido;vi) C.sub.1-6 alkyl; hydroxy C.sub.1-6 alkyl; C.sub.1-6 alkyloxy; C.sub.1-6 alkyloxy C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkylsulfonyl; C.sub.1-6 alkylthio; C.sub.1-6 alkylsulfinyl; C.sub.1-6 alkylsulfonamido; C.sub.1-6 alkylarylsulfonamido; C.sub.1-6 alkyloxy-carbonyl; C.sub.1-6 alkyloxycarbonyl C.sub.1-6 alkyl; R.sub.b R.sub.c N--C(O)--C.sub.1-6 alkyl; C.sub.1-6 alkanoylamino C.sub.1-6 alkyl; aroylamino C.sub.1-6 alkyl; wherein the C.sub.1-6 alkyl moiety can be substituted with 1-3 of: halo; C.sub.1-4 alkoxy; or trifluoromethyl;vii) aryl; aryloxy; arylcarbonyl; arylthio; arylsulfonyl; arylsulfinyl; arylsulfonamido; aryloxycarbonyl; wherein the aryl moiety can be substituted with 1-3 of: halo; C.sub.1-4 alkyl; C.sub.1-4 alkoxy; or trifluoromethyl;viii) --C(O)NR.sub.b R.sub.c ; --O--C(O)--NR.sub.b R.sub.c ; --N(Rb)--C(O)--R.sub.c ; --NR.sub.b R.sub.c ; R.sub.b --C(O)--N(R.sub.c)--; where R.sub.b and R.sub.c are defined in (f) above; and --N(R.sub.b)--C(O)--OR.sub.g, wherein R.sub.g is C.sub.1-6 alkyl or aryl, in which the alkyl moiety can be substituted with 1-3 of: halo; C.sub.1-4 alkoxy; or trifluoromethyl, and the aryl moiety can be substituted with 1-3 of: halo; C.sub.1-4 alkyl; C.sub.1-4 alkoxy, or trifluoromethyl; --N(R.sub.b)--C(O) NR.sub.c R.sub.d, wherein R.sub.d is selected from H, C.sub.1-6 alkyl, and aryl; in which said C.sub.1-6 alkyl and aryl can be substituted as described above in (f) for R.sub.b and R.sub.c ;ix) a heterocyclic group, which is a 5, 6 or 7 membered ring, containing at least one member selected from the group consisting of: one ring oxygen atom, one ring sulfur atom, 1-4 ring nitrogen atoms, or combinations thereof; in which the heterocyclic ring can be aromatic, unsaturated, or saturated, wherein the heterocyclic ring can be fused with a benzo ring, andwherein said heterocyclic ring can be substituted with one to three substituents, as defined above for v), vi), vii) and viii), excluding ix) a heterocyclic group; and(k) R.sup.3 and R.sup.4 taken together can be carbonyl oxygen;(l) R.sup.3 and R.sup.4 taken together can be .dbd.CH--R.sub.g, wherein R.sub.g is defined in viii); and wherein:X is selected from the group consisting of:--O--; --S(O).sub.n --; --C(O)--; --CH(R.sub.e)--; --C(O)--O--.sup.* ; --C(O)--N(R.sub.e)--.sup.* ;--N(R.sub.e)--C(O)--O--.sup.* ; --O--C(O)--N(R.sub.e)--.sup.* ; --N(R.sub.e)C(O )--N(R.sub.e)--;--O--CH(R.sub.e)--.sup.* ; --N(R.sub.e)--; wherein R.sub.e is H, C.sub.1-3 alkyl, aryl, aryl- C.sub.1-3 alkyl, or unsubstituted or substituted heteroaryl, as defined above in (j); wherein the asterisk (.sup.*) denotes the bond which is attached to the 16-position in Structure I; and n is zero, 1 or 2.
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