7 results about "Minodronic acid" patented technology

The invention belongs to the technical field of drug synthesis, and particularly provides a hypoxia activated prodrug derivative and a synthesis method thereof. The method comprises the following steps: by taking benzimidazole as a raw material, carrying out ring opening, decarboxylation, esterification, iodination, bromine substitution, reduction and cyano substitution to obtain (1-methyl-1H-imidazole-2-nitrile-5-yl) methanol and (1-methyl-1H-imidazole-2-nitrile-4-yl) methanol; then, the N, N '-bis (2-bromoethyl) diamino phosphonic acid (1-methyl-1H-imidazole-2-nitrile-5-yl) methyl ester and bromoisophosphamide nitrogen mustard are subjected to condensation reaction to obtain N, N'-bis (2-bromoethyl) diamino phosphonic acid (1-methyl-1H-imidazole-2-nitrile-5-yl) methyl ester or N, N '-bis (2-bromoethyl) diamino phosphonic acid (1-methyl-1H-imidazole-2-nitrile-4-yl) methyl ester. Through the test on the cell inhibition rate of ovarian cancer cells, the inhibition rate of the N, N '-bis (2-bromoethyl) diamino phosphonic acid (1-methyl-1H-imidazole-2-nitrile-5-yl) methyl ester is equivalent to that of TH-302.

The application belongs to the technical field of pharmaceutical preparations, and discloses a minodronic acid tablet and a preparation method thereof.The tablet provided by the application contains minodronic acid with a specific particle size, hydroxypropyl cellulose and pharmaceutically acceptable excipients, and the synergistic adaptation of the raw materials and the excipients is realized by controlling the particle size of minodronic acid and the suitable weight ratio of minodronic acid and hydroxypropyl cellulose.The application effectively solves the problems of sticking and bumping in the production of minodronic acid tablets, poor dissolution and low bioavailability, and the quality of the preparation is stable and the content is uniform, the preparation process is simple and easy to implement, is suitable for large-scale production, and has biological equivalence with the original research drug, and has a good clinical application prospect.

The application belongs to the technical field of pharmaceutical preparations, and discloses a minodronic acid tablet and a preparation method thereof.The tablet provided by the application contains minodronic acid with a specific particle size, hydroxypropyl cellulose and pharmaceutically acceptable excipients, and the synergistic adaptation of the raw materials and the excipients is realized by controlling the particle size of minodronic acid and the suitable weight ratio of minodronic acid and hydroxypropyl cellulose.The application effectively solves the problems of sticking and bumping in the production of minodronic acid tablets, poor dissolution and low bioavailability, and the quality of the preparation is stable and the content is uniform, the preparation process is simple and easy to implement, is suitable for large-scale production, and has biological equivalence with the original research drug, and has a good clinical application prospect.

The present invention belongs to the field of drug synthesis technology, and specifically provides a hypoxia-activated prodrug derivative and a synthesis method thereof. Using benzimidazole as raw material, (1-methyl-1H-imidazole-2-nitrile-5-yl)methanol and (1-methyl-1H-imidazole-2-nitrile-4-yl)methanol are obtained by ring opening, decarboxylation, esterification, iodination, bromine substitution, reduction, and cyano substitution; then it is condensed with bromoisophosphoramide nitrogen mustard to obtain N, N'-bis (2-bromoethyl) diaminophosphonic acid (1-methyl-1H-imidazole-2-nitrile-5-yl) methyl ester or N, N'-bis (2-bromoethyl) diaminophosphonic acid (1-methyl-1H-imidazole-2-nitrile-4-yl) methyl ester. After testing the inhibition rate of ovarian cancer cells, the inhibition rate of N, N'-bis (2-bromoethyl) diaminophosphonic acid (1-methyl-1H-imidazole-2-nitrile-5-yl) methyl ester of the present invention is comparable to that of TH-302.

The invention discloses an application of a bisphosphonate compound in preparation of an antigen-specific activated T cell preparation. The bisphosphonate compound is etidronate sodium as shown in a formula I; the clodronate sodium is shown as a formula II; the pamidronate sodium is shown as a formula III; the alendronate sodium trihydrate is as shown in a formula IV; zoledronic acid is as shown in formula V; the ibandronic acid is as shown in a formula VI; the risedronate sodium is shown as a formula VII; minodronic acid is shown as a formula VIII. The bisphosphonate compound can specifically activate T cells and remove target cells, and the target cells comprise various tumor cells, aging cells and infected cells.

The application belongs to the field of medicine synthesis, and specifically provides a synthesis method of alovudine isomer derivative. 4-nitro-1H-imidazole is used as raw material, substitution, elimination and reduction reaction are carried out to generate (1-alkyl-4-nitro-1H-imidazol-5-yl)methanol; then 2-haloethylamine halide acid salt and phosphorus oxychloride are reacted to generate N,N'-bis(2-haloethyl) diaminophosphonic acid; finally, (1-alkyl-4-nitro-1H-imidazol-5-yl)methanol, N,N'-bis(2-haloethyl) diaminophosphonic acid, triphenylphosphine and anhydrous tetrahydrofuran are added into a reaction bottle, the system is reduced to 0 DEG C, diisopropyl azodicarboxylate (DIAD) is added dropwise, the temperature is increased to 25 DEG C, reaction is carried out for 3h, and then the crude product is obtained through concentration under reduced pressure, and alovudine isomer derivative is obtained through purification through a silica gel column.

This invention belongs to the field of pharmaceutical formulation technology and discloses a minodronic acid tablet and its preparation method. The tablet provided by this invention contains minodronic acid of a specific particle size, hydroxypropyl cellulose, and pharmaceutically acceptable excipients. By controlling the particle size of minodronic acid and its appropriate weight ratio with hydroxypropyl cellulose, synergistic compatibility between the raw materials and excipients is achieved. This invention effectively solves the problems of sticking, poor dissolution, and low bioavailability in minodronic acid tablet production. The formulation has stable quality and uniform content. The preparation process is simple and easy to implement, suitable for large-scale production, and exhibits bioequivalence to the original drug, showing good prospects for clinical application.