35 results about "Biphosphonate" patented technology

The invention discloses a method for preparing a monophosphonate and biphosphonate mixed fire retardant, which comprises the following steps of: (1) heating tris phosphite and dihalide in the presence of a catalyst: (2) refluxing the mixture after the temperature rises to 110 to130 DEG C and continuously heating the refluxed mixture, wherein the optimal refluxing temperature of 120 DEG C; (3) allowing the refluxing speed to reduce obviously when the temperature is 160 and 180 DEG C, wherein the optimal temperature is 170 DEG C; (4) continuing a reaction, keeping the temperature between 170 and 200 DEG C to perform a reaction for 1 hour when the reflux phenomenon basically disappears, wherein the reaction is performed at 180 to190 DEG C optimally; (5) distilling the reacting product under normal pressure and filtering the distilled product to obtain a colorless transparent product. The total product yield of the monophosphonate and biphosphonate mixed fire retardant is over 90 percent; and the reaction time is shortened, the product has good color and luster, the acid value is low, the viscosity is low and no additional de-coloration treatment is required. Serving as the additive-type phosphine fire retardant, the monophosphonate and biphosphonate mixed fire retardant has higher performance. The monophosphonate and biphosphonate mixed fire retardant has the advantages of high economy, high product utilization efficiency, zero emission in a production process and environmental protection.

The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.

Synthesis of biphosphonate compounds can be advantageously carried out in a solvent/diluent comprising a compound of formula (3)

wherein R is hydrogen or a C1-C6 alkyl group; each of R1 is a C1-C6 alkyl group or both R1 groups are linked to form a C1-C3 alkylene group; and R2 is hydrogen, a C1-C6 alkyl group, a C1-C6 alkoxy group, or is linked together with R to form a C3-C7 carbon ring.

The invention relates to the use of a derivative with C-O-P bonds in the form of controlled release for the treatment of patients with renal failure. The invention also relates to the use of said derived compounds together with other active substances, that can particularly be selected from the list comprising a calcimimetic, a vitamin, a phosphorus chelator, thiosulfate, biphosphonate, pyrophosphate, citrate, a diuretic, an antihypertensive and an anticholesterolemic agent.

The invention provides a preparation method of 2,7-dimethyl-2,4,6-octa-triene-1,8-diethylester biphosphonate, which comprises the following steps of: preparing 2,7-dimethyl-2,4,6-octa-triene-1,8-diol by using 2,7-dimethyl-2,4,6-octa-triene-1,8-dialdehyde as an initiative raw material, adopting methanol, ethanol, dimethyl-tetrahydrofuran or isopropanol as a solvent, and using aluminum isopropoxide, potassium borohydride or sodium borohydride as a reducing agent for reduction; preparing 2,7-dimethyl-2,4,6-octa-triene-1,8-dihalide by using phosphorus tri-halide or thionyl chloride for halogenation; and finally, heating the 2,7-dimethyl-2,4,6-octa-triene-1,8-dihalide together with triethyl phosphate to remove chloroethane or bromoethane to obtain the target compound. While achieving the aims of facilitating industrial application and making reaction easily controlled, the preparation method provided by the invention ensures that the yield of the reaction of each step exceeds 60 percent.

The invention relates to medicine and pharmacology, and represents a pharmaceutical composition for the treatment of bone resorption of various etiology comprising, as the biologically active ingredient, liposomes with biphosphonates in gel dosage form suitable for transdermal delivery of biphosphonates and effective local therapy. Using this composition, methods for the prevention and treatment of osteoporosis, Paget's disease, patoplogical fractures associated with oncological diseases, and some other pathological processes associated with bone resorption and reparation are proposed.

A novel method for rapidly and efficiently introducing fluorine into the P-C-P backbone of bisphosphonates starting from readily accessible diazomethylenebisphosphonate esters is provided. The method is applied successfully to create novel [¹⁸F]-labeled bisphosphonates for positron emission tomography imaging. Some versions of the method include reacting a diazomethylenebisphosphonate tetraalkyl ester with a fluorinating agent in the presence of an acidic HF/base complex and a t-butyl hypohalite to produce a halofluoromethylenebisphosphonate tetraalkyl ester, and dealkylating the halofluoromethylenebisphosphonate alkyl ester to produce a halofluoromethylenebis(phosphonic acid). Methods of replacing the halogen group with hydrogen are further provided. ¹⁸F-labeled bisphosphonates prepared by the methods, and methods of using such compounds for positron emission tomography imaging in patients and animal models, are also provided.

A phosphonate medicine for treating osteoporosis and bone cancer transfer contains one of methylene biphosphonate, hydroxymethylene biphosphonate or ethyldiamine tetramethylene phosphonate. Its advantages are high curative effect and low by-effect.