Methods of inhibiting bone loss
AssigneeEli Lilly and Company
InventorsJill A. Panetta, Masahiko Sato
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Abstract
Rhodanine derivatives are utilized as inhibitors of bone loss/bone resorption and cartilage degradation.
Claims5
A method of inhibiting bone resorption in a subject comprising administering to said subject a pharmaceutically effective dose of a compound of the structure ##STR11## wherein R.sup.1 and R.sup.2 are independently hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, ##STR12## where n is an integer from 0 to 6, inclusive;
- R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl
- R.sup.4 and R.sup.5 are hydrogen or when taken together form a bond
- R.sup.6 and R.sup.7 are independently hydrogen or when taken together from .dbd.S or .dbd.O, or when one of R.sup.6 or R.sup.7 is hydrogen, the other is --OH or --SCH.sub.3 ;
- X is ##STR13## wherein m is 0,1, or 2;
- and Q is --CH.sub.2 --, --O--, or --NR.sup.8 where R.sup.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, --SO.sub.2 CH.sub.3 or --(CH.sub.2).sub.t --Y where t is 0,1,2, or 3, and Y is cyano, ##STR14## tetrazolyl, --NR.sup.11 R.sup.12, --SH, --S(C.sub.1 -C.sub.4 alkyl) or ##STR15## where R.sup.9 is hydrogen, C.sub.1 -C.sub.4 alkyl, tosyl, or ##STR16## R.sup.10 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or --NH.sub.2 ;
- R.sup.11 and R.sup.12 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, --(CH.sub.2).sub.n OH, --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.4 alkyl).sub.2, --(CH.sub.2).sub.n S(C.sub.1 -C.sub.4 alkyl), or ##STR17## where n is an integer from 0 to 6, inclusive, and t is 0,1,2, or 3;
- or R.sup.11 and R.sup.12 taken together form a morpholinyl, piperidinyl, piperazinyl or an N-methyl piperazinyl ring;
- and pharmaceutically acceptable salts and solvates thereof.
A method of inhibiting bone resorption in a subject comprising administering to said subject a pharmaceutically effective dose of a compound of the structure ##STR18## wherein R.sup.1a and R.sup.2a are independently hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, ##STR19## where n is an integer from 0 to 6, inclusive;
- R' is hydrogen, methyl, C.sub.1 -C.sub.6 alkyl, or C.sub.3 -C.sub.8 cycloalkyl;
- X.sup.a is --CH.sub.2 -- or S;
- and pharmaceutically acceptable salts and solvates thereof.
Dependencies are inferred from the claim text.