C07F9/3873

Phosphate derivatives and use thereof

The present invention discloses a compound with the following formula (I), or a tautomer, mesomer, racemate, enantiomer, and diastereoisomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt thereof, or a prodrug molecule thereof, wherein D is selected from: ##STR00001##
invention further discloses the use of the compound in the preparation of drugs for preventing and/or treating cancers, and the use of the compound in the preparation of drugs for inhibiting cancer metastasis. The compound of the present invention can effectively inhibit the proliferation and metastasis of cancer cells by adjusting the acidity of a tumor microenvironment to achieve a better effect in clinical cancer treatment, and has broad application prospects. ##STR00002##

Method of treating urolithiasis

The present disclosure provides phospholipid-containing compounds, pharmaceutical compositions and microspheres that exhibit high affinity for mineralized metals. The present disclosure also provides strategies for using said compounds, compositions and microspheres in the treatment of nephrolithiasis or kidney stone disease, and methods of manufacturing and preparing said compounds and compositions.

Flame retardant and flame retardant uses
10501602 · 2019-12-10 ·

The flame-retardants of this invention were formed by the direct reaction of ethyleneamines and commercial polyphosphoric acid at an elevated temperature. It was unexpected that a high temperature had to be used to overcome reaction barrier to formation. These compounds are found to be efficient flame retardants.

Bisphosphonate-based coordination complexes as enhanced pharmaceutical formulations and method of preparing the same

The hydrothermal reaction between bioactive metals (Ca.sup.2+, Zn.sup.2+, and Mg.sup.2+) salts and clinically utilized bisphosphonate (BP) alendronic acid (ALEN) were performed to prepare several bisphosphonate-based biocompatible coordination complexes (pBioCCs). The invention describes the effect of three variables M.sup.2+/BP molar ratio, reaction temperature, and pH on the reaction outcomes yields an unprecedented number of crystalline materials of enough crystal quality for structural elucidation. The crystal structure was unveiled by single crystal X-ray diffraction at 100 K and their solid-state properties revealed in tandem with other characterization techniques: thermogravimetry, vibrational spectroscopy, and elemental analysis. The invention provides materials with high structural stability and dissolution properties paving the way for better formulation strategies for alendronic acid (ALEN) through the design of pBioCCs for the treatment of bone-related diseases.

AMIDE-LINKED EP4 AGONIST-BISPHOSPHONATE COMPOUNDS AND USES THEREOF
20190345179 · 2019-11-14 ·

The present invention relates to EP4 agonist-bisphosphonate conjugates or related compounds and uses thereof. Said conjugates or related compounds may be used to provide delivery of an EP4 agonist or related compound to a desired site of action, such as a bone. Bisphosphonate moieties, linked to the EP4 agonists via amide linkers, have been implicated in the inhibition of bone resorption and bone targeting.

POLYMORPH OF SODIUM NERIDRONATE AND PREPARATION PROCESS THEREOF

The present invention relates to a novel crystalline hemihydrate polymorph of neridronic acid sodium salt, and a novel process for the preparation thereof comprising the steps of: 1) dissolving solid sodium neridronate in any crystalline form in water, at a temperature in the range from 70 to 90 C., to obtain an aqueous solution of sodium neridronate; 2) adding a solvent selected from the group consisting in ethanol, 1-propanol, and 2-propanol to the aqueous solution obtained from step (1), so that the final water:solvent volume ratio is in the range from 1:0.5 to 1:1, thus obtaining a suspension; 3) placing the suspension obtained from step (2) under mechanical stirring, at a temperature in the range from 60 to 95 C.; 4) recovering the crystalline hemihydrate form F of sodium neridronate formed in the previous step (3). The crystalline hemihydrate form F of sodium neridronate, particularly stable, may be employed in the preparation of solid oral pharmaceutical forms for use in the treatment of musculoskeletal and calcium metabolism disorders.

Dosage forms for oral administration of zoledronic acid or related compounds for treating disease
10420782 · 2019-09-24 · ·

Oral dosage forms of osteoclast inhibitors, such as zoledronic acid, in an acid or a salt form, can be used to treat or alleviate pain or related conditions, such as arthritis.

Amide-linked EP4 agonist-bisphosphonate compounds and uses thereof

The present invention relates to conjugate compounds and methods of making and using same.

NERIDRONIC ACID AND OTHER BISPHOSPHONATES FOR TREATING COMPLEX REGIONAL PAIN SYNDROME AND OTHER DISEASES
20190216832 · 2019-07-18 ·

Oral dosage forms of osteoclast inhibitors, such as neridronic acid, in an acid or a salt form, can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.

Phosphonate functional antimicrobial coatings for metal surfaces

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.