29-04-2021 дата публикации
Номер: US20210121485A1
Принадлежит:
Disclosed herein are methods and compositions for removing or displacing bisphosphonates in skeletal tissue. 1. A method of removing or displacing an active bisphosphonate in a skeletal tissue , which comprises administering to the skeletal tissue one or more inactive bisphosphonates , wherein the one or more inactive bisphosphonates is methylene hydroxyl bisphosphonate (MHDP), or', 'ethylene hydroxyl bisphosphonate (EHDP), wherein the EHDP is locally administered;, '(a) an alkyl hydroxyl bisphosphonate which is'} 2-hydroxy-3-(imidazo[1,2-a]pyridin-3-yl)-2-phosphonopropanoic acid (3-IPEHPC),', '2-hydroxy-2-phosphono-3-(pyridin-3-yl)propanoic acid (3-PEHPC),', '5-FAM-RISPC,', '6-FAM-RISPC,', '5(6)-FAM-RISPC,', '5 (6)-RhR-RISPC,', '5-ROX-RISPC,', '5(6)-ROX-RISPC,', '800CW-RISPC,', 'AF647-RISPC, and', 'ICG-RISPC,, '(b) a phosphonocarboxylate compound selected from the group consisting of'} 5-ROX-RIS,', '5(6)-ROX-RIS,', '5-FAM-RIS,', '6-FAM-RIS,', '800CW-RIS,', 'AF647-RIS, and', 'ICG-RIS; or, '(c) a fluorescent risedronate compound selected from the group consisting of'} 5-FAM-ZOL,', '800CW-ZOL,', 'AF647-ZOL, and', 'ICG-ZOL., '(d) a fluorescent zoledronate compound selected from the group consisting of'}2. (canceled)3. The method according to claim 1 , wherein the inactive bisphosphonates has a detectable label attached thereto.4. The method according to claim 1 , wherein the inactive bisphosphonates comprises a bisphosphonate conjugated to a fluorescent compound.5. The method according to claim 4 , wherein the fluorescent compound is selected from the group consisting of: ROX claim 4 , FAM claim 4 , AF647 claim 4 , ICG claim 4 , ICG analogs claim 4 , Cy5 claim 4 , Sulfo-Cy5 claim 4 , Cy7 claim 4 , and IRDye 800CW.6. The method according to claim 4 , wherein the one or more inactive bisphosphonates is selected from the group consisting of: 5(6)-FAM-RIS claim 4 , 5(6)-FAM-RISPC claim 4 , 5(6)-RhR-RIS claim 4 , 5(6)-RhR-RISPC claim 4 , 5(6)-ROX-RIS claim 4 , 5(6)-ROX- ...
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