50 results about "Purine derivative" patented technology

The present application relates to a kind of purine derivatives as the use of NSD2 and NSD3 inhibitor, the structural formula of the derivative is as shown in formula (I) or formula (II).The compound shows good NSD2, NSD3 inhibitory activity, can effectively reduce the methylation level of H3K36 in cell, and cause the reduction of cell proliferation activity of NSD2, NSD3 high expression tumor cell strain.

The present invention relates to a novel purine derivative compound and a composition for enhancing an immune response comprising same as an active ingredient. The compound of the present invention not only has a nanomolar EC50 value for TLR7, which is an intracellular membrane receptor of immune cells, but also has high selectivity for TLR7 compared to TLR8, which has a similar structure and is mainly distributed in the endoplasmic reticulum (ER), thereby being able to induce sustained immune activation. Therefore, the compound of the present invention can be effectively used as an efficient vaccine adjuvant composition against various RNA viruses including influenza virus, SARS-CoV-2, and hepatitis C virus.

The invention relates to a preparation method of an 8-hydroxyguanine (8-Hydroxyguanine) detection kit based on a chemiluminescence immunoassay technology. The 8-Hydroxyguanine (8-Hydroxyguanine) detection kit is used for detecting 8-Hydroxyguanine. As 8-hydroxyguanine is small in molecular weight and poor in immunogenicity, when a corresponding antibody is prepared, firstly, a proper derivative site needs to be selected, and a derived hapten is coupled with a specific macromolecular carrier to prepare a complete antigen. According to the invention, the antibody with good specificity and high affinity is successfully prepared by designing and transforming the hapten. The invention mainly relates to design and synthesis of an 8-hydroxyguanine hapten, preparation of an 8-hydroxyguanine complete antigen and an anti-8-hydroxyguanine antibody, a method for determining the concentration of 8-hydroxyguanine, and composition and components of a reagent. The design and synthesis of the hapten mainly comprise design and chemical synthesis of 8-hydroxyguanine derivatives. The 8-hydroxyguanine derivative disclosed by the invention has a structure as shown in a formula (I),

The present invention provides a salt of an aromatic amino purine derivative shown in Formula 2, and a preparation method and application thereof. The salt obtained by the present invention has good crystallinity and significantly improved solubility relative to the free form. The salt and the crystal form preferably have low hygroscopicity and can exist stably, so it is easier to make medicine than the free form of aromatic amino purine derivatives or other salts. (2).

The invention discloses a method for synthesizing 6-thiopurine derivatives by a copper-catalyzed three-component coupling reaction, using 6-chloropurine compounds, sodium sulfide and iodide as raw materials, in an alkali-free system, using polyethylene glycol as a reaction medium, under the action of a copper catalyst, a three-component coupling reaction forming two C-S bonds occurs, and a one-pot method efficiently prepares 6-thiopurine derivatives. The present invention saves the pre-synthesis step of 6-mercaptopurine, and is highly economical; using odorless inorganic salt sodium sulfide as a sulfur source, the use of thiol with a foul odor is avoided, there is no special requirement for the environment, the operation is simple, and it is suitable for industrial large-scale production; using polyethylene glycol as a reaction medium, the use of volatile organic solvents is avoided, and it is green and environmentally friendly; without the addition of alkaline additives, the reaction conditions are mild; the copper catalyst used is low-toxic, cheap and easy to obtain, and has good stability; with good substrate applicability, it is applicable to 6-chloropurine and iodide containing different substituents.

A Toll-like receptor (TLR) is an indispensable component of an innate immune system and plays a key role in identifying and coping with microbial pathogens. TLR7, TLR8, and TLR9 are located in the endosome-lysosome compartment within the cell and then exclusively used to detect nucleic acids of a microorganism after the microorganism is swallowed and reaches the endosome compartment. The biological importance of the TLR agonists lies in that they can be used as powerful tools for studying innate immune responses, developing vaccines and potential therapeutic applications. In addition, TLR agonists have been explored for use as immunotherapy, while these TLR antagonists can be used as new pathogenic nodes in the context of different autoimmune diseases. Therefore, the agonists and antagonists of the endosomal TLR have therapeutic significance in different clinical backgrounds. The previous study on 8-oxo adenines shows that the C-6-site-NH2 group is extremely important for the recognition of agonistic active sites and the subsequent induction of interferon (IFN). The present invention explores the ability of a hydrogen-substituted 8-oxopurine derivative that does not contain an essential C-6 amine group. The C-6 amino group in the 8-oxopurine derivative is substituted by hydrogen (H), providing an exciting opinion for regulating the endosome TLRs (Toll-Like Receptors). The ability of 8-oxopurine derivatives to modulate the endosomal TLR has been reported, which derivatives are related / interrelated to various substitutions at N-7, N-9 and C-2, all derivatives containing hydrogen at C-6. Structure 1

An object of the present invention is to provide a semiconductor treatment liquid which has excellent anticorrosion properties against at least one metal selected from the group consisting of Cu and Co in a case of being brought into contact with an object containing, and in which defects are less likely to remain on a surface of the object to be treated after the object to be treated is subjected to water cleaning; a treatment method for an object to be treated; and a manufacturing method of an electronic device. The semiconductor treatment liquid of the present invention contains at least one purine compound selected from the group consisting of purine and a purine derivative, at least one specific compound selected from the group consisting of an organic sulfonic acid compound having 10 or less carbon atoms, sulfuric acid, and a salt of these compounds, and water, in which a pH is more than 7.0.

The invention belongs to the technical field of medicine synthesis, and relates to a synthetic method of a fluorescent 2-aminopurine derivative. In particular to a synthetic method of 2-amino-6-cyanopurine, which is characterized in that cyanamide (SM-1) and 5-amino-4-(cyanoformyl imidogen) imidazole (SM-2) are used as raw materials to synthesize the 2-amino-6-cyanopurine. The problems of complex operation, long reaction time, unstable yield and the like in the prior art can be effectively avoided.

The present invention disclosures a novel purine derivatives represented by formula (I) or a pharmaceutically acceptable salt thereof, intermediate and application thereof inpreparation of a medicament for treating or preventing a cancer. This compound is a novel PI3K inhibitor with an excellent inhibitory activity, and may be useful for treating a variety of malignant tumors.

Disclosed are purine derivatives of formulae (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods involving the inventive compounds or compositions for treating and / or preventing cell proliferative diseases including certain cancers of breast, brain, ovarian, lung, colorectal cancer, leukemias, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma and inflammatory and myotonic dystrophy type 1 diseases in a mammal. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of kinases, such as a cyclin-dependent kinases (CDK) (e.g., CDK12 / 13), and therefore, induce potent antiproliferative and apoptotic effects and / or inhibit transcription in the subject.

The invention belongs to the technical field of medicine preparation, and particularly relates to 6-phenyl-purine derivatives as well as a preparation method and medical application thereof. The structural formula of the 6-phenyl-purine derivative is shown in the specification. The preparation method of the 6-phenyl-purine derivative comprises the following steps: S1, carrying out substitution reaction on R1-CH2NH2 and a compound 1 under the catalysis of organic base to obtain a compound 2; s2, carrying out Dieckmann condensation reaction on the compound 2 and excessive CDI to obtain a compound 3; s3, the compound 3 and phenylboronic acid are subjected to a Suzuki coupling reaction under catalysis of sodium carbonate, Pd (OAc) 2 and TPPTS, and the 6-phenyl-purine derivative with the structure shown in the general formula I is obtained. The 6-phenyl-purine derivative has antineoplastic activity and can be applied to preparation of antineoplastic drugs.

The present invention relates to a multilayer pharmaceutical or nutraceutical solid dosage form comprising at least one pyrimidine derivative, purine derivative or any salt or solvate thereof and least one B-group vitamin. It also provides three methods for producing said multilayer pharmaceutical or nutraceutical solid dosage forms. Furthermore, the present invention is also related to therapeutic uses of said multilayer pharmaceutical or nutraceutical solid dosage forms, particularly for the treatment and / or prevention of peripheral neuropathy.

An object of the present invention is to provide a semiconductor treatment liquid which has excellent anticorrosion properties against at least one metal selected from the group consisting of Cu and Co in a case of being brought into contact with an object containing the metal, and also has excellent cleanability for organic residues on a surface of the object to be treated; and to provide a treatment method for an object to be treated and a manufacturing method of an electronic device. The treatment liquid of the present invention contains a purine compound and an amine compound, in which the purine compound includes at least one selected from the group consisting of purine and a purine derivative, the amine compound includes at least two of one amine compound A and one or two or more amine compounds B different from the amine compound A, the amine compound A is a tertiary amine compound, and a mass ratio of a content of the purine compound to a content of the amine compound is 0.0001 to 0.1.

The present invention relates to novel inhibitors of salt-inducible kinase-3 (SIK3), methods of preparing them, pharmaceutical compositions containing them and methods for the treatment and / or prevention of kinase mediated diseases or disorders using them.

Provided are a bicyclic fused ring such as for example, benzo[d]imidazole, benzo[d][1,2,3]triazole, or 8-oxo-8,9-dihydro-7H-purine derivatives or pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical composition comprising the same and a use thereof, wherein the bicyclic fused ring derivative or pharmaceutically acceptable salt thereof has an inhibitory activity against the lysyl oxidase family and can be usefully applied for preventing or treating various diseases associated with the lysyl oxidase family, such as idiopathic pulmonary fibrosis (IPF), non-alcoholic steatohepatitis (NASH), chronic kidney disease (CKD), or liver cirrhosis.

The present invention relates to a multilayer pharmaceutical or nutraceutical solid dosage form comprising at least one pyrimidine derivative, purine derivative or any salt or solvate thereof and least one B-group vitamin. It also provides three methods for producing said multilayer pharmaceutical or nutraceutical solid dosage forms. Furthermore, the present invention is also related to therapeutic uses of said multilayer pharmaceutical or nutraceutical solid dosage forms, particularly for the treatment and / or prevention of peripheral neuropathy.

The present invention discloses a method for synthesizing 6-alkyl purine nucleosides by light-promoting them in an aqueous system, belonging to the field of pharmaceutical synthesis technology. Using an organic solvent and water as a mixed solvent, an organic base and a photocatalyst are added. Under visible light irradiation, a purine derivative A and an iodinated alkane react at room temperature to obtain 6-alkyl purine nucleoside B. The synthesis method of the present invention shortens the reaction steps, avoids the use of metal reagents, ligands, and heavy metal catalysts, and enriches the structural diversity of 6-alkyl purine nucleosides, providing a reference for optimizing their synthesis process and expanding their scope of application.

The present invention relates to a purine derivative for use in the treatment of a disease due to a nonsense mutation in a gene leading to the premature introduction of a UGA stop codon.

Disclosed are purine derivative compounds of general formula (I) wherein X is O or NH; y is CH or N; r1 is an optionally substituted alkyl group; n is 1 to 4; m is 0 to 4, and R2 is H, halogen, alkyl or alkoxy; each of R3 and R1 is H, OH, NR6R7, optionally substituted alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or R3, R4 and N together may form a ring. Also disclosed are immunostimulatory antibody conjugates (ISACs) comprising such compounds, and methods for producing and using such compounds, for example, in the treatment of diseases such as cancer. # imgabs0 #

There is disclosed a purine derivative compound of general formula (I) (wherein X is O or NH; Y is CH or N; R 1 is optionally substituted alkyl; n is from 1 to 4; m is from 0 to 4; R 2 is H, halogen, alkyl or alkoxy; R 3 and R 1 are each H, OH, NR 6 R 7 optionally substituted alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, or R 3 and R 4 and N may together form a ring). Also disclosed are immunopotentiating antibody conjugates (ISAC) containing such compounds, and methods for producing and using such compounds for the treatment of diseases such as cancer, for example. TIFF2025524965000338.tif48164

Provided is a negative photosensitive resin composition containing (A) a polyimide precursor or polyimide, (B) a photopolymerization initiator, (C) a radically polymerizable monomer having one photopolymerizable group, and (D) a nitrogen-containing heterocyclic compound, wherein the component (C) is a liquid at 25°C and 1 atm, the component (D) is a tetrazole derivative, a triazole derivative, a triazine derivative, or a purine derivative, and the purine derivative has an acyl group, an alkoxy group, an alkyl group, a hydroxyalkyl group, or a heteroaryl group.

The present invention relates to a purine derivative and use thereof in medicine, and in particular to a pyrimidine derivative shown as general formula (I) or a stereoisomer, solvate, metabolite, prodrug, deuteride, pharmaceutically acceptable salt or cocrystal thereof, a pharmaceutical composition comprising the same, and use of the compound or composition of the present invention in the field of preparation of a DNA-PK inhibitor, wherein the substituents in general formula (I) are defined in the same way as in the specification

Compounds and pharmaceutically acceptable salts thereof of Formula (I) are disclosed. Certain compounds and salts of Formula (I) are active as TDP1 inhibitors and radiosensitizers of cancer cells. The disclosure provides pharmaceutical compositions containing a compound of Formula (I) as the only active agent, or optionally containing one or more additional active agents. Methods of using compounds of Formula (I) to treat a cancer are provided in this disclosure. The disclosed compounds of Formula (I) may be used alone to treat cancer, but may also be used in combination with another active agent, such as a TOPI inhibitor, for example, camptothecin or a camptothecin analogue, and / or ionizing radiation.

The present invention belongs to the field of biomedicine and specifically relates to a purine derivative, its synthesis method, and application. The structure of the purine derivative is shown in Formula I, wherein R1 is a saturated hydrocarbon group, alkenyl group, alkynyl group, cycloalkyl group, aryl group, heterocyclic group, or alkoxycarbonyl group; R2 is hydrogen, halogen, alkyl group, aryl group, amino group, hydrocarbon amino group, or alkoxy group; R3 is hydrogen, alkyl group, amino group, hydrocarbon amino group, alkoxy group, aminosulfonyl group, sulfanyl group, aryl group, heterocyclic group, or carboxyl group; and n is 1, 2, 3, 4, 5, or 6. The purine derivative has excellent inhibitory activity against 5-lipoxygenase and 5-lipoxygenase, can be used to prepare lipoxygenase inhibitors, and can also be used to prepare drugs for treating lipoxygenase-mediated diseases, and has good clinical application prospects.

The present invention relates to novel inhibitors of salt-inducible kinase-3 (SIK3), methods of preparing them, pharmaceutical compositions containing them and methods for the treatment and / or prevention of kinase mediated diseases or disorders using them.

The present invention discloses an induction method for efficiently producing triploid male Nibea albiflora, belonging to the technical field of triploid induction of male Nibea albiflora, and specifically relates to nutritional regulation and photothermal regulation of sexually mature pseudo-male Nibea albiflora and female Nibea albiflora, sperm and eggs collection; artificial insemination to obtain fertilized eggs, which are immersed in seawater for treatment and then incubated, and finally triploid male Nibea albiflora is induced and cultivated; when the fertilized eggs are immersed in seawater during artificial insemination and incubation, purine derivatives can be added to the seawater to treat the fertilized eggs, thereby improving the success rate of triploid induction of Nibea albiflora. The method of the present invention has a high success rate of triploid induction of Nibea albiflora, and triploid male Nibea albiflora is successfully obtained under subsequent induction.

The invention relates to a 2, 6, 9-trisubstituted purine derivative and a synthesis method thereof, and belongs to the technical field of chemistry. The compound comprises a structure as shown in a general formula I, wherein R1 is at least one of hydrogen, C1-C6 alkyl and C3-C6 cycloalkyl; r2 and R3 are at least one of hydrogen, fluorine, chlorine, bromine, iodine, hydroxyl, amino, amino containing one or more substituent groups, cyano, C1-C6 alkoxy containing one or more substituent groups, C1-C6 alkyl acyl, C1-C6 alkyl sulfonyl, C1-C6 alkyl phosphonyl, C3-C6 heterocyclic radical and C3-C6 heterocyclic radical containing one or more substituent groups; x is an oxygen atom or a nitrogen atom. The compound disclosed by the invention is simple in synthesis step and has the characteristic of remarkably inhibiting cancer cell proliferation; the method has the advantages of high cost benefit, obvious treatment effect and low toxicity, and in the synthesis route, the yield of the intermediate is higher, and the resource consumption is effectively reduced, so that the overall cost is favorably reduced.

Compounds and pharmaceutically acceptable salts thereof of Formula (I) are disclosed. Certain compounds and salts of Formula (I) are active as TDP1 inhibitors and radiosensitizers of cancer cells. The disclosure provides pharmaceutical compositions containing a compound of Formula (I) as the only active agent, or optionally containing one or more additional active agents. Methods of using compounds of Formula (I) to treat a cancer are provided in this disclosure. The disclosed compounds of Formula (I) may be used alone to treat cancer, but may also be used in combination with another active agent, such as a TOPI inhibitor, for example, camptothecin or a camptothecin analogue, and / or ionizing radiation.