73 results about "Hypoxic tumor" patented technology

The present invention relates to the use of adenosine receptor antagonists, preferably A3 receptor antagonists, either alone or in combination with other agents for the treatment, prevention and / or management of diseases or disorders associated with overexpression of HIF-1α and / or increased HIF-1α activity (e.g., cancer, respiratory disease). The methods and compositions of the invention are particularly useful for preventing, treating, or ameliorating symptoms associated with a cancer, disease or disorder associated with hypoxia-inducible factor 1α (HIF-1α) using the A3 receptor antagonists of the invention. The present invention provides methods to inhibit the growth of tumors, particularly solid tumors and more particularly hypoxic tumors.

The invention provides a nitroreductase-specific fluorescent probe and the preparation thereof and a reagent for applying the nitroreductase-specific fluorescent probe to tumor-targeted fluorescence imaging and monitoring of tumor hypoxia. The reagent is connected by tumor biomarker identifying groups (sensor), tumor targeted groups (target) and fluorescent groups (dye) via chemical bonds. The reagent can be used in the tumors with hypoxic microenvironment and high expression of nitroreductase based on tumor hypoxia and the high expression of nitroreductase in hypoxic tumors. Combined with a fluorescence imager, the reagent can be used in tumor targeted fluorescence imaging, tumor hypoxia monitoring and the monitoring of tumor metastasis, etc. The reagent realizes high sensitivity and high specificity in application and provides an effective tool for medical study of cancer and clinical monitoring and treatment of tumor metastasis, thereby having a good application prospect in tumor-targeted fluorescence imaging, tumor hypoxia monitoring and monitoring of tumor metastasis.

The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.

The invention discloses a hypoxia-activated prodrug based on 2-nitroimidazole-1-alkanol. The 2-nitroimidazole-1-alkanol of the prodrug is connected to an antineoplastic drug through a carbonate bond. The prodrug has a structure shown in the formula I and in the formula, n represents 0, 1, 2 or 3, and R1, R2, R3 and R4 include but not limited to hydrogen, hydroxyl, chlorine, bromine, fluorine, C1-C6 alkyl, C1-C6 alkyl containing alkenyl and C1-C6 alkyl containing alkynyl. The prodrug can target the hypoxia region of the tumor and is reduced by the high expressed specific enzyme in the hypoxic tumor tissue so that the original drug is released. The prodrug is stable in vitro and in vivo, and the released drug can be specifically reduced in hypoxic tumor tissue so that the targeting of the anti-tumor drug is improved, toxic or side effects are reduced and the curative effect is improved.

Methods and systems for treatment of hypoxic tumors are provided, including the steps of positioning a delivery device in a bodily cavity adjacent to tumor tissue, delivering an oxygenating agent to the tumor tissue via the delivery device and radiating the tumor tissue with radiation. Methods and systems of treatment of tumors are also provided, including the steps of positioning a delivery device in a bodily cavity adjacent to tumor tissue, delivering a photosensitizing agent to the tumor tissue via the delivery device, and radiating the tumor tissue with light.

Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy.where R is C1-C10 alkyl or haloalkyl;R′ and R″ are each independently C1-C10 alkyl;R1 is CH3; andX is O;or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.

Therapeutic ureido-sulfonamide compositions having compounds with the formulaR-Q-Ar—SO2NH2 are disclosed, which compounds selectively inhibit CAIX and CAXII, and which are effective to inhibit hypoxic tumor growth, suppress metastases, and impair and deplete cancer stem cells in mammals.

The invention discloses a delivery system based on nano-liposome, a preparation method and an application thereof. The nano-liposome is of a granular structure composed of a shell layer and emulsion in the shell layer. The shell layer is composed of lecithin and cholesterol, and the emulsion is composed of perfluorocarbon and Tween-80; wherein the mass ratio of lecithin to cholesterol is (1-4): (0.5-1); the volume ratio of the perfluorinated carbon to the tween-80 is (1-6): (0.5-1.5); and the average particle size of the liposome is 100 nm to 300 nm. The preparation method comprises the following steps: firstly, perfluorocarbon is prepared into an emulsion, and then the emulsion is wrapped in a liposome; when the liposome is combined with ozone, the ozone is coated in the liposome, so that the stability of the ozone and the concentration of the carried ozone are improved; the nano-liposome loaded ozone is specifically delivered into a tumor microenvironment, under the action of rays, the ozone can be decomposed into hydroxyl radicals with higher concentration compared with oxygen, the effect of directly killing tumor cells is achieved, meanwhile, the ozone can also be decomposed to generate oxygen, and the killing sensitivity of radioactive rays to the tumor cells is enhanced by improving the hypoxic tumor microenvironment.

Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formulas (I), (II), (III) and (IV). Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. Where R = C1-10 alkyl, or C1-10 haloalkyl (preferably containing no more than 5 halogen groups, preferably 2-chloroethyl); R' and R'' are independently C1-10 alkyl, or C5-20 aryl or heteroaryl (preferably methyl); R1 is H, C1-10 alkyl, C1-10 alkoxyl, C5-20 aryl or heteroaryl or C5-20 aroxyl or heteroaroxyl (preferably methyl and ethyl); X is O, NH, or NR (preferably O); Y is (CH2)n , where n = 1, 2, 3, 4 or 5 (preferably n = 2 and 3); or Y = aryl or heteroaryl (preferably para-phenyl); A = CH, or N (preferably CH); and B = CH=CH, O, S, NH, or NR (preferably CH=CH); or pharmaceutically acceptable salts, solvates, polymorphs or metabolites, thereof.

The present invention provides a composition and method for targeting hypoxic tumor areas for detection or treatment or a treatment adjuvant for cancer. Specifically, a hypoxia targeting moiety is conjugated to a polymeric micelle containing imaging agents, therapeutic agents, or therapeutic adjuvants.