150250-33-2Relevant academic research and scientific papers
PHOSPHONATED RIFAMYCINS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS
-
Page/Page column 81, (2011/11/06)
The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
PHOSPHONATED RIFAMYCINS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS
-
Page/Page column 125-126, (2010/04/03)
The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
PHOSPHONATED GLYCOPEPTIDE AND LIPOGLYCOPEPTIDE ANTIBIOTICS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS
-
, (2010/05/13)
The present invention is directed to antimicrobial compounds which have an affinity for binding bones. More particularly, the invention is directed to phosphonated derivatives of glycopeptide or lipoglycopeptide antibiotics. These compounds are useful as antibiotics for the prevention or treatment of bone and joint infections, especially for the prevention and treatment of osteomyelitis.
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis
Tanaka, Kelly S.E.,Houghton, Tom J.,Kang, Ting,Dietrich, Evelyne,Delorme, Daniel,Ferreira, Sandra S.,Caron, Laurence,Viens, Frederic,Arhin, Francis F.,Sarmiento, Ingrid,Lehoux, Dario,Fadhil, Ibtihal,Laquerre, Karine,Liu, Jing,Ostiguy, Valerie,Poirier, Hugo,Moeck, Gregory,Parr Jr., Thomas R.,Rafai Far, Adel
experimental part, p. 9217 - 9229 (2009/04/11)
Osteomyelitis is a difficult to treat bacterial infection of the bone. Delivering antibacterial agents to the bone may overcome the difficulties in treating this illness by effectively concentrating the antibiotic at the site of infection and by limiting the toxicity that may result from systemic exposure to the large doses conventionally used. Using bisphosphonates as osteophilic functional groups, different forms of fluoroquinolone esters were synthesized and evaluated for their ability to bind bone and to release the parent antibacterial agent. Bisphosphonated glycolamide fluoroquinolone esters were found to present a profile consistent with effective and rapid bone binding and efficient release of the active drug moiety. They were assessed for their ability to prevent bone infection in vivo and were found to be effective when the free fluoroquinolones were not.
Linking bisphosphonates to the free amino groups in fluoroquinolones: Preparation of osteotropic prodrugs for the prevention of osteomyelitis
Houghton, Tom J.,Tanaka, Kelly S. E.,Kang, Ting,Dietrich, Evelyne,Lafontaine, Yanick,Delorme, Daniel,Ferreira, Sandra S.,Viens, Frederic,Arhin, Francis F.,Sarmiento, Ingrid,Lehoux, Dario,Fadhil, Ibtihal,Laquerre, Karine,Liu, Jing,Ostiguy, Valérie,Poirier, Hugo,Moeck, Gregory,Parr Jr., Thomas R.,Far, Adel Rafai
experimental part, p. 6955 - 6969 (2009/11/30)
Osteomyelitis is an infection located in bone and a notoriously difficult disease to manage, requiring frequent and heavy doses of systemically administered antibiotics. Targeting antibiotics to the bone after systemic administration may provide both grea
Phosphonated Fluoroquinolones, Antibacterial Analogs Thereof, and Methods for the Prevention and Treatment of Bone and Joint Infections
-
Page/Page column 59, (2008/12/09)
The present invention relates to phosphonated fluoroquinolones, antibacterial analogs thereof, and methods of using such compounds. These compounds are useful as antibiotics for prevention and/or the treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis.
A new efficient synthesis of ω-aminoalkylidene-1,1-bisphosphonate tetraethylesters
Gourves, Jean-Philippe,Couthon, Helene,Sturtz, Georges
, p. 219 - 229 (2007/10/03)
Bisphosphonates are interesting therapeutic agents in the management of bone diseases and since several years our laboratory has been developing the chemistry of 1,1-bisphosphonates. This paper describes an original synthesis of two aminoalkylidenebisphosphonates by first preparing the intermediate hydroxyalkylidenebisphosphonates which are transformed into amines via the azides.
