6results about How to "High metabolic stability" patented technology

The invention relates to the technical field of metabonomics analysis, in particular to application of a metabolic marker in preparation of a head and neck squamous cell carcinoma diagnostic product, a kit, a screening method of the metabolic marker of the head and neck squamous cell carcinoma, a diagnostic model and a construction method and application of the diagnostic model. The metabolic marker comprises at least one of lactic acid, sphingosine, cadaverine, uridine diphosphate, allantoic acid, hydroxyproline, sphingosine-1-phosphoric acid, indole-3-acetaldehyde, pantothenic acid, fumaric acid, malic acid, prostaglandin or ornithine in red blood cells and / or plasma. The screened red blood cells and plasma metabolism markers can be used for predicting or diagnosing the head and neck squamous cell carcinoma respectively or independently, particularly, the red blood cell metabolism markers can provide more stable tumor microenvironment information, and the metabolism stability is high and is not easily influenced by diet and circadian rhythm.

This invention discloses a highly efficient oxygen removal reagent and its application in the deoxygenation reconstruction of carbon resource molecular skeletons, comprising a pivot reagent, a phosphine reagent, an azo reagent, a reducing agent, an acid reagent, a base reagent, a photosensitizer, and an organic solvent; wherein, X in the pivot reagent includes a hydrazine group or a sulfone group; PG is a protecting group; LG is a leaving group; by using natural oxygen-containing functional groups such as alcohols, aldehydes, and ketones as direct coupling precursors, an integrated in-situ activation-deoxygenation coupling process is achieved, significantly reducing reaction steps.

The present application relates to the technical field of biological medicine, in particular to a gemcitabine-indoleamine 2,3-dioxygenase inhibitor conjugate, a prodrug nanomicelle, a preparation method and an application. The conjugate covalently connects gemcitabine and NLG919 through a connecting arm containing a triazole structure, forms an amphiphilic molecule with a hydrophilic-hydrophobic structure, and can self-assemble into stable small-size nanomicelles in an aqueous solution. The nanomicelle has a pH and enzyme dual-responsive drug release property, can improve the stability and delivery efficiency of gemcitabine, promote cell uptake, and enhance the synergistic antitumor effect of chemotherapy and immunomodulation. The present application also provides an application of the nanomicelle in the preparation of an antitumor drug.

The invention discloses a tanshinone IIA derivative as well as a preparation method and application thereof, and provides a set of systematic chemical synthesis route for overcoming the defects that tanshinone IIA is poor in water solubility and low in bioavailability and the antitumor activity needs to be improved. A series of novel derivatives with various structures and general formula structures and pharmaceutical salts thereof are prepared. The core of the technical scheme is that after a specific functional group is introduced into the derivative, the water solubility and the stability of the compound are remarkably improved, and the derivative particularly shows excellent anti-colorectal cancer activity, can effectively inhibit tumor cell proliferation and tumor growth in an animal model, and does not have obvious toxic or side effects. The invention also provides a pharmaceutical composition containing the derivative and application of the pharmaceutical composition in preparation of medicines for preventing, relieving or treating colorectal cancer, and provides an important candidate compound for developing a high-efficiency and low-toxicity novel anti-colorectal cancer medicine.

The invention discloses an N-methyl nitrosamide compound as well as a pharmaceutical composition and application thereof. The compound (formula I) is a hypoxia-activated NO donor drug, has the characteristic of effectively releasing NO under a high-selectivity hypoxia condition, so that the activity of myocardial cells is remarkably improved, the in-vivo and in-vitro activity is excellent, and the compound can be used for preventing or treating myocardial hypoxia injury. Meanwhile, the metabolic stability of the compound is improved by an ether bond connection structure, so that the compound has in-vivo metabolic properties beneficial to patent medicines.

The invention discloses a method for preparing carbon isotope labeled levodopa through asymmetric synthesis. The method comprises the following steps: carrying out nucleophilic addition reaction on carbon isotope labeled CO2 and an aryl nucleophilic reagent to obtain carbon isotope labeled pepper acid; carrying out reduction and bromination reaction on piperic acid to synthesize a carbon isotope labeled aryl bromide fragment; the aryl bromide fragment and a chiral auxiliary Schiff base fragment are connected through an asymmetric alkylation reaction, and the carbon isotope labeled levodopa is obtained by removing an auxiliary and a protecting group from a connection product. According to the method, cheap and easily available raw materials are adopted, the cost is low, the yield is high, and the chiral center stereo enantioselectivity is high; according to the method, the L-DOPA can be accurately and stably labeled at the levodopa 3 site at a fixed point, the metabolic stability of the carbon isotope labeled L-DOPA is improved, the asymmetric synthesis of the carbon isotope labeled L-DOPA at the levodopa 3 site is completed for the first time, and a material support is provided for metabolism research related to the levodopa.