24 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 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),

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.

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.

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 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 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 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.

This invention relates to purine derivative G4-targeting protein chimeras, and more particularly to a class of purine derivative G4-targeting protein chimeras synthesized using PROTAC technology and possessing antitumor activity. The general structural formula of the targeting chimera is as follows: where R is a linker, representing triethylene glycol, tetraethylene glycol, pentaethylene glycol, a four-carbon chain, a five-carbon chain, a six-carbon chain, a seven-carbon chain, an eight-carbon chain, a nine-carbon chain, azacyclobutane, tetrahydropyrrole, piperidine, or 1-phenylpiperazine. Spectroscopic and mass spectrometric data analysis show that the synthesized purine derivative G4-targeting protein chimeras are novel compounds. In vitro antitumor activity studies have demonstrated that the purine derivative G4-targeting protein chimeras provided by this invention exhibit strong antitumor activity against human triple-negative breast cancer cells MDA-MB-231, human gastric adenocarcinoma cells MGC803, human liver cancer cells HepG2, and human colon cancer cells HCT-116. This is an excellent new antitumor compound with the potential to be developed into a new antitumor drug.

The application discloses a 7,9-dihydropurine derivative and a pharmaceutical application thereof. Specifically provided are a compound shown in formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof. Experiments show that the compound provided by the application has good inhibitory activity on DNA-PK, and especially, the inhibitory activity of compounds CLJ1, 4, 8, 15, 22-25, 56 and 59 is even superior to that of a known DNA-PK inhibitor AZD-7648. The compound provided by the application has a wide application prospect in preparation of a DNA-PK inhibitor. The application provides a new selection for an anti-tumor drug sensitizer, a radiotherapy sensitizer and a tumor treatment drug, and also provides a new selection for a tumor treatment method.

A compound of formula (I), for use in the treatment of non-traumatic acquired brain injury,in which M represents a NR1R2 group, an OR1 group or a SR1 group, A represents a NR4R5 group, an OR10 group or a hydrogen atom, R3 is a (C1-C6)alkyl group, a (C1-C6)cycloalkyl group, an aryl group, a —CH2-aryl group, a CH2-(C1-C6)cycloalkyl group or a —CH2-heteroaryl group, and its addition salts with pharmaceutically acceptable acids. A compound of formula (I) wherein R5 is a (C1-C8)alkyl group or a (C1-C6)cycloalkyl group, said alkyl and cycloalkyl group being substituted with one, two or three —OCORa group(s).

This invention relates to crystalline forms of substituted purine derivatives and pharmaceutical compositions thereof, methods of preparation thereof, and use in the preparation of DNA-PK inhibitors. Specifically, it relates to crystalline forms of compounds of formula (A) and pharmaceutical compositions thereof, methods of preparation thereof, and use in the preparation of DNA-PK inhibitors.

The present invention relates to compounds of formula (I) and to the addition salts thereof with a pharmaceutically acceptable acid, for the treatment of non-traumatic acquired brain injury, wherein M represents NR 1 R 2 group, OR 1 group or SR 1 group, A represents NR 4 R 5 group, OR 10 group or a hydrogen atom, R 3 is (C1-C6)alkyl, (C1-C6)cycloalkyl, aryl, -CH2-aryl, CH2-(C1-C6)cycloalkyl or -CH2-heteroaryl. The present invention further relates to compounds of formula (I) wherein R 5 is (C1-C8)alkyl or (C1-C6)cycloalkyl, said alkyl and cycloalkyl being substituted by one, two or three -OCOR a groups.

Toll-like receptors (TLRs) are integral components of the innate immune system, serving as key players in the recognition and response to microbial pathogens. TLR7, TLR8 and TLR9 are located inside the cell within the endosomal-lysosomal compartments, subsequently specialized for detecting microbial nucleic acids after microbes get phagocytosed and reach the endosomal compartments. The biological importance of TLR agonists lies in their ability to serve as powerful tools for studying innate immune responses, developing vaccines, and potential therapeutic applications. Additionally, TLR agonists have been explored as immunotherapies, whereas antagonists of these TLRs could serve as novel pathogenic node in different autoimmune disease contexts. Thus, both agonists and antagonists of these endosomal TLRs have therapeutic significance in different clinical context. The previous studies in 8-oxoadenine class depicted that the C-6 position -NH2 group is extremely important for recognition of the agonistic active site and subsequent interferon (IFN) induction. The present invention explores ability of 8-oxopurine derivatives, which does not contain the essential C-6 amine group and was replaced with hydrogen. The replacement of C-6 amino with a hydrogen (H) in 8-oxopurine derivatives provided exciting insight into these endosomal TLR modulation. The ability to modulate the endosomal TLRs by 8- oxopurine derivatives in correlation / interrelation with various substitution at N-7, N-9 and C-2 with all the derivatives containing hydrogen at C-6 were reported.

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 invention discloses a synthesis method of a [1, 2, 4]-triazolone fused purine nucleoside compound, and belongs to the field of organic chemistry. The [1, 2, 4]-triazolone purine nucleoside compound is obtained by taking a 6-hydrazino purine derivative as a raw material and reacting in an undivided electrolytic tank in the presence of a catalyst and an organic solvent. According to the triazolone fused N-heteroaromatic compound and the preparation method of the triazolone fused N-heteroaromatic compound, electrochemical anodic oxidation is combined with aminooxy catalysis, and the conversion can convert a hydrazino heterocycle into various triazolone fused N-heteroaromatic compounds through tandem NH-NH oxidative dehydrogenation, intramolecular cyclization and 1, 2-carbon migration reaction, so that a huge potential is provided for developing a new tricyclic purine core lead compound.