Claims
- 1. A compound of formula (1):
- 2. The compound of claim 1, wherein R4 and R5 taken together comprise a substituted or unsubstituted aryl, heteroryl, or cycloalkyl moiety, and wherein said aryl, heteroaryl, or cycloalkyl moiety is a substituted single or polycyclic ring.
- 3. The compound of claim 2, wherein said substituted single or polycyclic ring is substituted with methyl or alkoxy.
- 4. The compound of claim 1, wherein a bone targeting moiety comprises formula (II)
- 5. The compound of claim 4, wherein R1, R3 and R4 are each hydrogen; wherein R2 is a bone targeting moiety, wherein for L, n is 0 and He is either NR′, wherein R′ is hydrogen or lower alkyl, or O; wherein X2 is NH, wherein Hc is
- 6. The compound of claim 4, wherein R1 and R3 are each hydrogen; wherein R4 is alkoxy; wherein R2 is the bone targeting group; wherein for L n is 0 and Hc is NR′, wherein R′ is hydrogen or lower alkyl, or O; wherein X1 is CH; wherein X2 is NH; wherein Hc is
- 7. The compound of claim 4, wherein R1 and R3 are each independently a lower alkyl or hydrogen; wherein R4 is hydrogen; wherein R2 is the bone targeting moiety; wherein for L, n is 0 and He is NH or O; wherein X1 is N; wherein X2 is NH; wherein Hc is
- 8. The compound of claim 7, wherein R6 and R7 taken together comprise a substituted phenyl group, wherein said phenyl group is substituted with an electron donating moiety.
- 9. A pharmaceutical composition comprising:
a compound of any one of claims 1, 2, 3, 4, 5, 6, 7 or 8; and a pharmaceutically acceptable carrier or excipient.
- 10. A method for the prevention or treatment of a disease or secondary condition associated with overactivity of osteoclasts in a subject which method comprises the administration of an effective non-toxic amount of a selective inhibitor of mammalian osteoclasts to a subject in need thereof.
- 11. The method of claim 10, wherein said method comprises the administration of any one of claims 1, 2, 3, 4, 5 , 6, 7, or 8 to a subject in need thereof.
- 12. The method of claim 10, wherein said disease or secondary condition is selected from the group consisting of osteoporosis, Paget's Disease, hypercalcemia, rheumatoid arthritis, metastatic bone destruction, cancer, and immune disorder.
PRIORITY INFORMATION
[0001] The present application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Patent Application No. 60/172,510, filed Dec. 17, 1999, entitled “Bone Targeting Agents”, U.S. Provisional Patent Application No. 60/172,161, filed Dec. 17, 1999, entitled “Proton Pump Inhibitors”, and U.S. Provisional Patent Application No. 60/240,788, filed Oct. 16, 2000 entitled “Bone Targeting Agents”, and the entire contents of each of these applications are hereby incorporated by reference.
[0002] The application further claims priority to U.S. National patent application No. ______, entitled “Novel Heterocycles”, and U.S. National patent application No. ______, entitled “Novel Purines”, each of which is filed on even date herewith and is hereby incorporated by reference.
Provisional Applications (3)
|
Number |
Date |
Country |
|
60172510 |
Dec 1999 |
US |
|
60172161 |
Dec 1999 |
US |
|
60240788 |
Oct 2000 |
US |