52 results about "Amifostine" patented technology

The present invention is directed to methods of treating or protecting mucosal tissue from damage associated with radiation and / or chemotherapeutic treatment of cancers, by the topical application of amifostine and related compounds. These methods avoid the side effects of systemically applied radio / chemo protectants. The invention is also directed to treatment and prevention of infections associated with mucositis by topical application of amifostine and related compounds.

The present invention relates to a sterile, stable dosage forms suitable for reconstitution and parenteral administration to a patient, said dosage form comprising an amorphous aminoalkyl dihydrogen phosphorothioate, and of amifostine in particular. The invention further relates to a method of preparing such a dosage form, which typically exhibits enhanced thermal stability as compared to existing vacuum dried amorphous amifostine.

The invention provides, in a general sense, a new labeling strategy employing compounds that are are N2S2 chelates conjugated to a targeting ligand, wherein the targeting ligand is a disease cell cycle targeting compound, a tumor angiogenesis targeting ligand, a tumor apoptosis targeting ligand, a disease receptor targeting ligand, amifostine, angiostatin, monoclonal antibody C225, monoclonal antibody CD31, monoclonal antibody CD40, capecitabine, a COX-2 inhibitor, deoxycytidine, fullerene, herceptin, human serum albumin, lactose, leuteinizing hormone, pyridoxal, quinazoline, thalidomide, transferrin, or trimethyl lysine. The present invention also pertains to kits employing the compounds of interest, and methods of assessing the pharmacology of an agent of interest using the present compounds.

The present invention provides methods of administering aminoalkyl phosphorothioate and / or aminoalkyl thiol compounds to patients receiving radiation therapy in a manner that significantly reduces or decreases the adverse or undesirable side-effects of the compounds as compared with conventional intravenous administration.

A method for the prevention or treatment of human immunodeficiency virus infection by administering an effective amount of amifostine, phosphonol, or similar compound to an individual in need is provided.

Methods and pharmaceuticals for inhibiting or preventing metastasis formation in animals, including humans, having primary tumors, through the administration of phosphorothioates including their thiol and disulfide metabolites are disclosed. These compounds stimulate angiostatin levels, inhibit matrix metalloproteinases (MMPs), and stimulate manganese superoxidase dismutase (MnSOD). Phosphorothioates, of which amifostine is an example, can be administered as a combination therapy with traditional cancer therapies, including chemotherapy, radiotherapy, surgery, immunotherapy, hormone therapy and gene-therapy. Inhibition or prevention of metastasis by phosphorothioates is independent of tumor type, including adenocarcinomas and sarcomas.

The present invention provides methods of administering aminoalkyl phosphorothioate and / or aminoalkyl thiol compounds to patients in a manner that significantly reduces or decreases the adverse or undesirable side-effects of the compounds as compared with conventional intravenous administration.

The present invention is directed to methods of treating or protecting mucosal tissue from damage associated with radiation and / or chemotherapeutic treatment of cancers, by the topical application of amifostine and related compounds. These methods avoid the side effects of systemically applied radio / chemo protectants. The invention is also directed to treatment and prevention of infections associated with mucositis by topical application of amifostine and related compounds.

The present invention relates to new uses of S-2-(3-aminopropylamino)ethyl dihydrogen phosphorothioate, (amifostine) and other aminothiol compounds to treat and reverse toxicities caused by therapeutic agents, radiation treatment or diabetes. In particular, the invention provides a method for treating neurotoxicity and nephrotoxicity associated with the administration of chemotherapeutic agents.

The present invention relates to processes for the preparation of (Omega-aminoalkylainino)alkyl halides, their conversion to S-Omega-(Omega-aminoalkylamino)alkyl phosphothioates, and purification of the crystalline products of the reaction. The preparation process for the (Omega-aminoalkylamino)alkyl halides comprises contacting an appropriate alcohol with a brominating agent in the presence of a sulfone solvent under temperature and pressure conditions suitable to effect salt formation without subsequent premature precipitation. The process is especially useful for converting (Omega-aminoalkylamino) ethyl alcohol to amifostine.

A storage stable aqueous solution of amifostine at a pH of at least 10.0, in an amifostine concentration of about 50 to about 250 mg / l, which formulation is storage stable under refrigerated conditions.

The present invention relates to sterile, stable dosage forms suitable for reconstitution and parenteral administration to a patient, said dosage form comprising an amorphous aminoalkyl dihydrogen phosphorothioate, and amifostine in particular. The invention further relates to a method of preparing such a dosage form, which typically exhibits enhanced thermal stability as compared to existing vacuum dried amorphous amifostine.

The invention discloses a treatment medicine capable of degrading high-polymer tumor and a sustained-release medicine for normal cell protective agent. The sustained-release medicine comprises one or more of the following sustained-release systems: (1) a tumor tissue and peripheral implanted medicine sustained-release system; (2) an absorbable nanometer medicine sustained-release system containing a lymphaden tracking medicine in lymph; (3) a nanometer medicine sustained-release system in blood or body fluid; (4) a nanometer medicine sustained-release system in a specific tissue, wherein, the specific tissue can be a liver, a spleen, a lung or marrow. The treatment medicine for tumor comprises one or more of chemotherapeutic medicine, chemotherapeutic sensitizer and tumor targeting medicine, and uses amifostine as the normal cell protective agent. The range of tumor treatment is applicable to any tumor through changing different treatment medicines. The invention is a novel medicine application platform, can be used by any new medicine besides the existing medicines, and plays a role in conquering cancer finally.

The invention relates to a method for preparing amifostine, comprising the following steps: a) reacting phthalimide with 1,3-dibromopropane in dipolar aprotic solvents to genenrate N-(3-bromopropyl) phthalimide; and b)reacting N-(3-bromopropyl) phthalimide with 2-oxazolidinone in dipolar aprotic solvents to generate 2,2-[3-(2-carbonyl-3-oxazole)propyl]-1H-isoindole-1,3(2H)-diketone; and using the one-pot process to prepare the amifostine directly from the intermediate 2,2-[3-(2-carbonyl-3-oxazole)propyl]-1H-isoindole-1,3(2H)-diketone, thus the production process can be simplified, and the production cost can be saved. In addition, primary amine is obtained by hydrazinolysis, thus the reaction conditions are mild, the side effect is low, and the post-treatment is simple. The method has the characteristics of easy obtainment of raw materials, low price, safe and convenient usage, little pollution, easy transportation, and the like.

A freeze-dried amifostine is prepared from amifostine, acetone and the solution of pharmacologically acceptable excipient through prefreezing, sublimated drying, and drying again.

The present invention provides methods of administering amifostine, WR-1065, or a combination thereof, to patients receiving radiation therapy in a manner that significantly reduces or decreases the adverse or undesirable side-effects of the compounds as compared with conventional intravenous administration.

The invention discloses amifostine slow-release microspheres for subcutaneous injection and a preparation method thereof. A unique two-way emulsion-solution evaporation technology is adopted, the prepared amifostine slow-release microspheres for subcutaneous injection can reach relative constant and long-acting drug release in a subcutaneous injection scene, in-vitro release is even, release time can be as long as 300 hours or above, the protection function is stable, adverse factors brought by the fact that existing amifostine can only adopt an intravenous injection drug application mode are avoided, and the problem that drug release is not uniform and lasting through subcutaneous injection is also solved.

The present invention relates to a sterile, stable dosage forms suitable for reconstitution and parenteral administration to a patient, said dosage form comprising an amorphous aminoalkyl dihydrogen phosphorothioate, and of amifostine in particular. The invention further relates to a method of preparing such a dosage form, which typically exhibits enhanced thermal stability as compared to existing vacuum dried amorphous. amifostine.

The invention relates to the technical field of in-vitro tissue cell separation, and particularly relates to a method for quickly and efficiently separating cartilage cells. A human serum albumin is added in the early digestion stage to buffer the decomposition effect of other extrinsic protease on type II collagenase, thus ensuring that the type II collagenase is not damaged and has high activity; and an amifostine solution is further added in the late digestion stage to favorably protect cartilage cells and effectively prevent the cartilage cells from being damaged in the digestion process, thereby being beneficial to obtaining more primary cartilage cells with higher activity.

The invention discloses an amifostine soluble armored microneedle patch. The microneedle patch is composed of an amifostine soluble armored microneedle array and a substrate layer. The amifostine soluble armor microneedle structurally comprises a needle and an armor layer. The armored microneedle can greatly improve the drug dosage, does not influence the mechanical strength, can be smoothly inserted into the skin to implement transdermal drug delivery, achieves a long-time and high-efficiency cell protection effect, and can be used for radiation protection and chemotherapy protection.

The invention provides a PEGylation modified amifostine as well as a preparation method and use of the PEGylation modified amifostine. The polymer is of a structure formed by connecting the micromolecular medicine amifostine with polyethylene glycol (PEG) by use of a covalent bond, wherein the amino on the amifostine is in covalent linkage with the long chain of a PEG derivative by use of an amido bond. The invention also provides a preparation method of the PEGylation modified amifostine. The PEGylation modified amifostine also has an enhanced oxidation effect at the cellular level.

The invention belongs to the field of medicine and particularly relates to a transdermal preparation for treating oral mucositis caused by radiotherapy of tumor. The transdermal preparation comprisesactive ingredients of 109-237 parts by weight of amifostine and 42-85 parts by weight of uridine triacetate. The transdermal preparation is administered externally at a daily dose level of milligrams,has a markedly improved effect on the oral mucositis caused by the radiotherapy, and can avoid the drop of blood pressure caused by large doses of amifostine hydrochloride to affect the health of patients with normal blood pressure or hypotension.

The present invention relates to sterile, stable dosage forms suitable for reconstitution and parenteral administration to a patient, said dosage form comprising an amorphous aminoalkyl dihydrogen phosphorothioate, and amifostine in particular. The invention further relates to a method of preparing such a dosage form, which typically exhibits enhanced thermal stability as compared to existing vacuum dried amorphous amifostine.

The invention discloses an application of AMF (amifostine) in treatment of tumors with high Cyclin D1 expression. According to research, AMF inhibits tumor cell growth by inhibiting cancer gene CyclinD1 expression in a targeted manner and resists the tumors by inhibiting the CyclinD1 expression in a targeted manner, and the functions are successfully verified through megakaryocyte leukemia cell lines Dami; and AMF successfully cures mantle cell lymphoma with high Cyclin D1 expression and high leukocyte expression as characteristics in clinical practice.

A freeze-dried amifostine is prepared from amifostine, acetone and the solution of pharmacologically acceptable excipient through prefreezing, sublimated drying, and drying again.