Claims
- 1. Sulfur-containing phosphonate compound, or a pharmaceutically-acceptable phosphonic acid salt or ester thereof, having the following structure: ##STR38## wherein m and n are integers 0 to 10 and m+n equals 0 to 10, and wherein (a) X is O or S;
- (b) Z is a covalent bond or a monocyclic or polycyclic carbocyclic ring moiety;
- (c) Q is a covalent bond; O; or S;
- (d) R is �COOH, SO.sub.3 H,!PO.sub.3 H.sub.2 or P(O)(OH)R.sup.4, wherein R.sup.4 is a substituted or unsubstituted C.sub.1 -C.sub.8 alkyl;
- (e) each R.sup.1 is independently selected from --SR.sup.6 ; --R.sup.8 SR.sup.6 ; nil; hydrogen; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; monocyclic or polycyclic carbocyclic ring moiety; unsubstituted or substituted aryl; substituted or unsubstituted thiophene; substituted or unsubstituted oxathiazole; substituted or unsubstituted pyranone; substituted or unsubstituted furan; hydroxy; amido; --CO.sub.2 R.sup.3 ; --O.sub.2 CR.sup.3 ; --NR.sup.3.sub.2 ; --OR.sup.3 ; --N(R.sup.3)C(O)R.sup.3 ; --C(O)N(R.sup.3).sub.2 ; substituted or unsubstituted benzyl; nitro; or combinations thereof;
- (f) R.sup.2 is independently selected from --SR.sup.6 ; --R.sup.8 SR.sup.6 ; --CO.sub.2 R.sup.3 ; --O.sub.2 CR.sup.3 ; --C(O)N(R.sup.3).sub.2 ; --N(R).sup.3 C(O)R.sup.3 ; --OR.sup.3 ; nil; hydrogen; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; unsubstituted or substituted aryl; hydroxy; substituted or unsubstituted benzyl; nitro; or combinations thereof;
- (g) each R.sup.3 is independently selected from hydrogen; substituted or unsubstituted C.sub.1 -C.sub.8 alkyl; or �R.sup.8 SR.sup.6 ! --R.sup.8 SR.sup.6 ;
- (h) R.sup.5 is selected from --SR.sup.6 ; �R.sup.8 SR.sup.6 ! --R.sup.8 SR.sup.6 ; hydrogen; hydroxy; amino; halogen; or unsubstituted or substituted C.sub.1 -C.sub.8 alkyl;
- (i) R.sup.6 is independently selected from H, --C(O)R.sup.7 ; or C(O)N(R.sup.7).sub.2 ; where R.sup.7 is hydrogen, or unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; and
- (j) R.sup.8 is substituted or unsubstituted C.sub.1 -C.sub.8 alkyl;
- provided that if Z is a covalent bond and m is 0, then R.sup.2 is other than nil.
- 2. A compound according to claim 1, wherein Z is selected from the group consisting of phenyl, cyclopentyl, cyclohexyl and cycloheptyl.
- 3. A compound, according to claim 1, wherein R.sup.1 is independently selected from the group consisting of hydrogen; substituted or unsubstituted C.sub.1 -C.sub.8 alkyl; --NR.sup.3.sub.2 ; or --CO.sub.2 R.sup.3.
- 4. A compound, according to claim 1, wherein R.sup.2 is independently selected from the group consisting of hydrogen; hydroxy, substituted or unsubstituted C.sub.1 -C.sub.8 alkyl; --C(O)N(R.sup.3).sub.2 ; or --CO.sub.2 R.sup.3.
- 5. A pharmaceutical composition comprised of a safe and effective amount of a compound according to claim 1 and pharmaceutically-acceptable excipients.
- 6. A composition according to claim 5 comprised of 0.1% to 99.9% by weight of the compound according to claim 1.
- 7. A composition according to claim 6 comprised of 20% to 80% by weight of the compound according to claim 1.
- 8. A composition according to claim 6 comprised of 15% to 95% of a compound according to claim 1; 0-2% flavoring agents; 0-50% co-solvents; 0-5% buffer system; 0-2% surfactants; 0-2% preservatives; 0-5% sweeteners; 0-5% viscosity agents; 0-75% fillers; 0.5-2% lubricants; 1-5% glidants; 4-15% disintegrants; and 1-10% binders.
- 9. A method of treating or preventing disorders associated with abnormal calcium and phosphate metabolism wherein a safe and effective amount of a compound according to claim 1 is administered to a human or other mammal in need of such treatment.
- 10. A method according to claim 9 wherein said human or other mammal is suffering from osteoporosis.
- 11. A method according to claim 9 wherein said human or other mammal is suffering from arthritis.
- 12. A method according to claim 9 wherein said human or other mammal is suffering from osteoarthritis.
- 13. A method according to claim 9 wherein said human or other mammal is suffering from rheumatoid arthritis.
- 14. A method of treating or preventing disorders associated with abnormal calcium and phosphate metabolism wherein a human or other mammal in need of such treatment is administered a pharmaceutical composition according to claim 5.
Parent Case Info
This is a continuation of application Ser. No. 07/891,309, filed on May 29, 1992, now abandoned.
US Referenced Citations (17)
Foreign Referenced Citations (1)
Number |
Date |
Country |
A-2673888 |
Jun 1989 |
AUX |
Continuations (1)
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Number |
Date |
Country |
Parent |
891309 |
May 1992 |
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