摘要:
The invention relates to a bisphosphonate (BP) compound, or a pharmaceutically acceptable salt or solvate or pro-drug thereof, for use as a cytoprotectant for protecting non-cancerous cells of a subject against radiation-induced damage and/or damage induced by a chemical agent.
摘要:
The invention relates to quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds, processes for preparing quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds, antimicrobial coating compositions comprising quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds and method of treating a surface with said compositions to provide a durable, antimicrobial-treated surface.
摘要:
The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side–effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
摘要:
The present invention discloses a new and an improved process for preparation of Ibandronate sodium monohydrate. According to the process pentylamine is reacted with ethylacrylate to give N-pentyl-ß-alanine ethyl ester (XXIV), which on methylation provided N-methyl-N-pentyl-ß-alanine ethylester formula (XXV). The reresulting ester on hydrolysis and subsequent treatment with hydrochloric acid furnished 3-(N-methyl-N-pentylamino)propionic acid hydrochloride formula (II). Bisphosphorylation of 3-(N-methyl-N-pentylamino)propionic acid hydrochloride formula (II) with phosphorous acid and phosphorous trichloride followed by hydrolysis and subsequent treatment with a base provided Ibandronate monosodium monohydrate of formula (I).
摘要:
La présente invention concerne un procédé de préparation d'un dérivé d'acide hydroxy-bisphosphonique ou d'un sel de celui-ci à partir de l'acide carboxylique correspondant comprenant les étapes suivantes : - activation de la fonction acide carboxylique sous la forme de son dérivé boronate par action d'un borane, puis - réaction dans les conditions d'Arbuzov avec le tris (triméthylsilyl) phosphite, - traitement avec un alcool, choisi notamment parmi un alcool aliphatique ou le trif luorométhanol, et - séparation du dérivé d'acide hydroxy-bisphosphonique formé du milieu réactionnel.
摘要:
Polymorphic crystalline forms of Ibandronate sodium were found, referred to hereinafter as polymorphic Form α, Form β, Form ε, Form δ, Form γ and Form ζ. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms, to pharmaceutical compositions comprising them, as well as their use.
摘要:
A crystalline ibandronic acid characterized by data selected from the group consisting of at least one of a powder x-ray diffraction pattern having peaks at about 4.1, 12.3 and 13.4 ± 0.2 degrees two-theta and at least two more peaks selected from the group consisting of: 8.2, 11.3, 16.2 and 16.9 and 20.8 ± 0.2 degrees two-theta, and by a powder X-ray diffraction pattern depicted in Figure 1 is provided. Also provided is a crystalline ibandronic acid characterized by data selected from the group consisting of at least one of a powder x-ray diffraction pattern having peaks at about peaks at about 5.2, 11.7, and 18.7 ± 0.2 degrees two- theta and at least two more peaks selected from the group consisting of: 5.8, 10.1, 12.0, 17.1, and 20.0 ± 0.2 degrees two-theta and a powder X-ray diffraction pattern as depicted in Figure 2. Methods of preparing the crystalline forms are also provided.
摘要:
The present invention provides for methods of administering a bisphosphonate active agent to a subject in need thereof. Aspects of the invention include administering the bisphosphonate active agent to the subject by a pulmonary route, where the bisphosphonate active agent is bonded, either directly or through an intervening linking group, to a non-peptide polymer, such that the bisphosphonate active agent is a polymer-linked-bisphosphonate active agent. Also provided are compositions for use in practicing methods according to embodiments of the invention. Methods and compositions according to embodiments of the invention find use in a variety of different applications, including but not limited to, the treatment of bone adsorption disease conditions.
摘要:
The present invention provides an improved process for the preparation of bisphosphonic acids or salts thereof, e.g alendronic acid, by reacting a carboxylic acid, phosphorus acid and a halophosphorus compound in presence of phenolic compounds as diluent/solvent.
摘要:
A manufacturing process for the preparation of bisphosphonic acids and in particular zoledronic acid is provided wherein diglyme, monoglyme, or a mixture thereof, is utilized to produce a homogenous, water soluble, solid reaction mass that upon cooling, dissolving in water and stripping results in a high purity product and comparatively good yield.