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9 results about "Demethylating agent" patented technology

Demethylating agents are chemical substances that can inhibit methylation, resulting in the expression of the previously hypermethylated silenced genes (see Methylation#Cancer for more detail). Cytidine analogs such as 5-azacytidine (azacitidine) and 5-azadeoxycytidine (decitabine) are the most commonly used demethylating agents. They work by inhibiting DNA methyltransferases. Both compounds have been approved in the treatment of myelodysplastic syndrome (MDS) by Food and Drug Administration (FDA) in United States. Azacitidine and decitabine are marketed as Vidaza and Dacogen respectively. Azacitidine is the first drug to be approved by FDA for treating MDS and has been given orphan drug status. Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells.

A method for preparing raloxifene EP impurity B

This invention discloses a method for preparing raloxifene EP impurity B, comprising the following steps: dissolving 6-methoxy-2-(4-methoxyphenyl)benzothiophene (Ⅰ) as a raw material in solvent one, adding NIS, and then adding a free radical initiator to react and obtain intermediate III; dissolving 4-[2-(1-pyrrolidinyl)ethoxy]benzoate salt (II) in solvent two, adding solvent two or not, and then adding a chlorinating agent to react and generate intermediate IV; dissolving intermediate III in solvent three, adding a Lewis acid, and then adding intermediate IV, and performing a Friedel-Crafts acylation reaction to generate intermediate V; dissolving intermediate V in solvent four, adding a demethylating agent, and generating bisphenol hydroxyl intermediate VI under demethylation conditions; dissolving intermediate VI in solvent five, adding a reducing agent, and generating intermediate VII through a reduction reaction; dissolving intermediate VII in formic acid, stirring, evaporating, and finally lyophilizing to generate the formate target product VIII.
Owner:SHENZHEN FEITH BIOTECHNOLOGY CO LTD

Enhancing anti-tumor response in melanoma cells with defective sting signaling

Disclosed herein is a method for enhancing antitumor T cell responses in subjects. The method involves administering to the subject in need thereof a composition comprising a demethylating agent in an amount effective to demethylate STING proteins in the tumor cells. This method is particularly useful in subjects with deficient STING expression in the tumor cells. Therefore, also disclosed is a method for treating a tumor in a subject that involves detecting in a biopsy sample from the subject reduced STING expression, reduced cGAS expression, or a combination thereof; and then administering to the subject a demethylating agent in an amount effective to demethylate STING proteins in the tumor cells. The method can further involve administering to the subject a therapeutically effective amount of a STING agonist. The method can further involve administering to the subject tumor infiltrating lymphocytes (TILs), such as HLA-matched TILs.
Owner:H LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE INC +1

Deuterium labeled psychoactive substances, methods of making and uses thereof

The present application relates to a deuterium-labeled psychoactive substance, which has a chemical structural formula as shown in the description.The present application also provides a preparation method of the deuterium-labeled psychoactive substance, which comprises the following steps: (1) removing the methyl group of sufentanil under the action of a demethylating agent to generate a demethylated intermediate; (2) reacting the demethylated intermediate with a deuterated methyl reagent to generate the deuterium-labeled sufentanil.The present application also provides the use of the deuterium-labeled sufentanil in detecting the content of sufentanil in biological samples or environmental samples.
Owner:THE THIRD RES INST OF MIN OF PUBLIC SECURITY

Method for preparation of cytotoxic t lymphocytes with broad tumour-specific reactivity and characteristics of early differentiation cells

Provided is a method for preparation of a composition comprising activated human CD8+ lymphocytes with phenotype of stem cell-like memory cells and natural killer (NK) lymphocytes. The method entails use of short-term activation of lymphocytes by CD3 / CD28 activating agents followed by treatment with DNA-demethylating agent. The invention also provides a version of the method where addition of a CD3 / CD28 activating agent is made a few days after initiation of CD4+ mediated activation of the CD8+ cells; this step is also disclosed as an improvement of related methods where autologous dendritic cells have been used to activate the lymphocytes. Also provided is a method for treatment of cancer using the cells obtained from the process.
Owner:CYTOVAC

Preparation method and application of pyridyl piperazine modified quinazolinyl-aryl urea derivative

The invention discloses a preparation method and application of a pyridylpiperazine modified quinazolinyl-aryl urea derivative, and the method comprises the following steps: taking 4-chloro-6, 7-dimethoxy quinazoline as a raw material, reacting with 3-nitrobenzylamine hydrochloride to obtain an intermediate 2, adopting a demethylation reagent to remove methyl at the 6-position of a quinazoline ring with high selectivity to obtain the pyridylpiperazine modified quinazolinyl-aryl urea derivative. The preparation method comprises the following steps: firstly, preparing a key intermediate 3, modifying a hydrophilic group pyridyl piperazine unit and a lipophilic group (alkyl with four carbon atoms) on the basis of the intermediate, then reducing, and finally reacting with phenyl isocyanate (or phenyl isocyanate derivative) to obtain a target product. The method is simple, efficient and high in yield, a plurality of compounds in the product obtained by adopting the method show good proliferation inhibition effects on tumor cells of human bladder cancer, osteosarcoma, pancreatic cancer, breast cancer, cervical cancer and the like, and the product is good in water solubility and fat solubility and has the potential to become a tumor molecular targeting drug.
Owner:GUANGXI NORMAL UNIV

Enhancing anti-tumor response in melanoma cells with defective sting signaling

Disclosed herein is a method for enhancing antitumor T cell responses in subjects. The method involves administering to the subject in need thereof a composition comprising a demethylating agent in an amount effective to demethylate STING proteins in the tumor cells. This method is particularly useful in subjects with deficient STING expression in the tumor cells. Therefore, also disclosed is a method for treating a tumor in a subject that involves detecting in a biopsy sample from the subject reduced STING expression, reduced cGAS expression, or a combination thereof; and then administering to the subject a demethylating agent in an amount effective to demethylate STING proteins in the tumor cells. The method can further involve administering to the subject a therapeutically effective amount of a STING agonist. The method can further involve administering to the subject tumor infiltrating lymphocytes (TILs), such as HLA-matched TILs.
Owner:H LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE INC +1

A nano-drug composition for photo-triggered pyroptosis and a preparation method and application thereof

This invention proposes a photo-triggered pyroptosis nanomedicine composition, its preparation method, and its application, belonging to the field of pharmaceutical technology. The nanomedicine composition consists of spherical nanoparticles with a core-shell structure: an outer carrier (bovine serum albumin); a middle photothermal agent (poly(dithiophene-pyrrolopyrroledione); and a core demethylating agent (lipophilic demethylating agent RG108). This invention achieves successful triggering of pyroptosis and a sustained anti-tumor immune cycle with only a single dose and minimal light exposure, significantly improving the response rate of immunotherapy and providing a novel and highly innovative strategy for photo-immunotherapy of tumors.
Owner:UNIV OF SHANGHAI FOR SCI & TECH

A combined preparation for ph+ all and use thereof

This invention belongs to the field of biomedicine, specifically relating to a combination drug composition for Ph+ALL and its application. This invention discloses a combination drug composition for Ph+ALL, characterized by comprising a BCL-2 inhibitor, a demethylating agent, and a TKI. The technical solution of this invention expands the chemotherapy-free treatment modality for Ph+ALL, not only enabling patients to achieve rapid and deep remission while observing no unacceptable treatment-related toxicities, but also significantly improving the quality of life of treatment-naïve patients, reducing treatment-related complications, decreasing the consumption of blood products, shortening hospital stays, and significantly reducing medical insurance expenditures.
Owner:THE FIRST AFFILIATED HOSPITAL OF SOOCHOW UNIV