41 results about "Diarylpyrimidines" patented technology

The present invention relates to diaryl pyrimidine-2,4-diamines, pharmaceutical compositions thereof, and the use of the compounds and compositions for the inhibition of kinases. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.

The invention relates to a diarylpyrimidines HIV-1 reverse transcriptase inhibitor as well as a preparation method and application thereof. The diarylpyrimidines HIV-1 reverse transcriptase inhibitorhas a structure shown as a formula I. The invention further relates to a pharmaceutical composition containing the compound with the structure formula I. The invention further provides application ofthe compound and the composition containing one or more compounds to preparation of medicines for treating and preventing human immunodeficiency virus (HIV).

The invention relates to a diarylpyrimidine compound, a composition and application. The diarylpyrimidine compound is particularly a compound as shown in a general formula (I), and all substituent groups of the general formula (I) are as defined in the description. The invention further relates to application of the compound as shown in the general formula (I) or a pharmaceutically acceptable salt or the pharmaceutical composition in treating tumor diseases, particularly treating a non-small cell lung cancer, a small cell lung cancer, squamous-cell carcinoma, a breast cancer and lymphocytic leukemia by inhibiting epidermal growth factor receptor (EGFR) protein tyrosine kinase (PTK). Please see the formula in the description.

The invention discloses a substituted diarylpyrimidine derivative as well as a preparation method and application thereof. The substituted diarylpyrimidine derivative or a pharmaceutically acceptable salt or predrug of the substituted diarylpyrimidine derivative has a structure represented by the following general formula I or II (shown in the description). The invention further discloses a preparation method of the substituted diarylpyrimidine derivative and application of a composition containing one or more compounds in preparation of drugs for treating and preventing human immunodeficiency virus (HIV). The formulae I and II are as shown in the specification.

The invention belongs to the technical field of medicament, and specifically discloses diaryl pyridine derivatives (DAPYs), a preparation method thereof and an application thereof. A structural formula of the compound is expressed as formula I. The invention also relates to medicinal salts thereof such as hydrochloride, sulfate, tartrate, citrate, fumarate and malate, pharmaceutically acceptable prodrug and derivatives, and the application of a composition containing one or more the compounds in related medicaments for treating AIDS.

The invention belongs to the technical field of medicines, particularly relates to diaryl pyrimidone hydrazone derivatives and a preparation method and application of the diaryl pyrimidone hydrazone derivatives. The diaryl pyrimidone hydrazone derivatives also contain medicine salt, a stereochemical isomer, hydrate, solvate, polycrystals or eutectic crystals and a precursor and derivatives with the same biological functions. The preparation method comprises a step that hydrazonium salt and substituted hydrazonium salt react with diaryl pyrimidine in an organic solvent under the action of alkali to prepare target products, or hydrazine, a complex compound of hydrazine and a complex compound of substituted hydrazine directly react with diaryl pyrimidine to prepare the target products. A pharmacological test result shows that most of the compounds have strong inhibitory activity for replication of a wild-type HIV-1 strains and various drug resistant HIV-1 virus strains; part of the compounds have strong inhibitory activity for HIV-2; and the compounds are expected to become HIV-resistant candidate drugs.

The invention belongs to the technical field of medicines, and particularly relates to a diarylpyrimidine derivative containing a biphenyl structure and a preparation method and application thereof. The compound structure disclosed by the invention relates to the diarylpyrimidine derivative containing the biphenyl structure shown as general formula I, and the invention further relates to a medicinal salt, a hydrate and a solvate thereof, a polycrystal or a co-crystal thereof, a precursor and a derivative with the same biological function thereof, a preparation method thereof and application ofa composition containing one or more of such compounds in related drugs for treating AIDS and the like. An in-vitro cell-level anti-HIV-1 activity experiment result shows that such small molecules have high anti-HIV-1 bioactivity, the replication of viruses in MT-4 cells infected by HIV-1 viruses can be notably inhibited, and moreover, cytotoxicity is low. (The general formula I is shown in the description.).

The invention discloses a diarylpyrimidine compound containing a six-membered nitrogen heterocyclic ring as well as a preparation method and application of the diarylpyrimidine compound. The compoundhas a structure as shown in a general formula I in the specification. The invention also relates to a pharmaceutical composition containing the compound with the structure shown in the formula I. Activity screening experiments show that the compound provided by the invention has good anti-HIV1 activity, so that the invention also provides application of the compound in preparation of anti-AIDS drugs.

Disclosed is a 2-amido-4, 5-diaryl pyridine compound as well as a preparation method and drug purposes thereof, belonging to the heterocyclic compound technique field, and relating to a heterocyclic compound which is heterocyclic and not hydrogenated, contains six rings and takes two nitrogen atoms as exclusive heterocyclic atoms, and does not condense with other rings. An isoflavone is added into a reaction kettle, a solvent and carbamidine are added thereto under agitation, the isoflavone and the carbamidine are present in a molar ratio of 1:1-1:10, with a reaction solution temperature of between 50 and 100 DEG C, an alkaline solution is dripped continuously to make a reaction system have a pH value of 8 to 10, a mixture of 2-substituted-4, 5-diaryl pyridine and matters which do not undergo reaction is obtained after the reaction for 5 to 50 hours, the reaction mixture is distillated to be dry and is added with a 1 to 5 percent HCl aqueous solution with the weight 50 to 130 times that of the mixture, and the crude product of 2-amido-4, 5-diaryl pyridine is obtained through heating, dissolving, filtration, neutrality adjustment, standing, generation of precipitation and filtration, and the crude product is recrystallized with a 50 to 80 percent ethanol solution with the weight 40 to 120 times that of the crude product, so the pure product is acquired.

The invention provides a diarylpyrimidine derivative substituted by a 5-site aromatic ring. The diarylpyrimidine derivative has a structure as shown in a general formula I which is described in the specification. The invention also relates to a preparation method of the derivative and application of the derivative as an HIV inhibitor in preparation of anti-AIDS drugs.

The invention relates to a triazole-ring-containing diaryl pyrimidine HIV-1 inhibitor as well as a preparation method and application of the triazole-ring-containing diaryl pyrimidine HIV-1 inhibitor.The compound has a structure as shown in a formula I. The invention further relates to a pharmaceutical composition containing the compound with the structure as shown in the formula I. The inventionfurther provides an application of the compound and a composition containing one or more of the compound to preparation of a drug for treating and preventing a human immunodeficiency virus (HIV).

The invention relates to a diarylpyrimidine HIV-1 reverse transcriptase inhibitor containing trans-double bonds, and a preparation method and application thereof. The compound has a structure represented by formula I in the specification. The invention also relates to a pharmaceutical composition containing the compound with the structure represented by the formula I. The invention also provides application of the compound and the composition containing one or more compounds in preparation of drugs for treating and preventing human immunodeficiency virus (HIV).

The invention discloses a substituted 1,2,3 triazole diarylpyrimidine derivative as well as a preparation method and application thereof. The substituted 1,2,3 triazole diarylpyrimidine derivative orpharmaceutically acceptable salts or prodrugs thereof have the following structure shown as a formula I. The invention further provides a preparation method of the substituted 1,2,3 triazole diarylpyrimidine derivative and application of a composition containing one or more compounds in preparing drugs for treating and preventing human immunodeficiency virus (HIV). (The formula I is shown in the description).

The invention belongs to the technical field of medicines, in particular to a piperidine-4-amido diaryl pyrimidine derivative shown as the general formula I, and pharmaceutical salt, hydrates and solvate, polycrystal or an eutectic crystals, precursors and derivatives, having the same biological functions with the piperidine-4-amido diaryl pyrimidine derivative, of the piperidine-4-amido diaryl pyrimidine derivative, as well as a preparation method and application of a composition containing one or more chemical compounds of this kind in related drugs for treating aids and the like. Pharmacological experimental results prove that the compounds have remarkable anti-HIV-1 virus activity, can effectively inhibit replication of HIV-1 virus infected MT-4 cells, and have relatively low cytotoxicity.

The invention belongs to the technical field of medicines, and particularly relates to a biphenyl diaryl methyl pyrimidine derivative containing an aromatic heterocyclic structure, and a preparation method thereof. According to the present invention, the structure optimization and the salt formation optimization are performed on a diaryl pyrimidine non-nucleoside reverse transcriptase inhibitor, and the pharmacological toxicology of the diaryl pyrimidine non-nucleoside reverse transcriptase inhibitor is investigated to obtain the novel efficient non-nucleoside reverse transcriptase inhibitor with excellent antiviral activity and pharmacokinetic characteristics, comprising pharmaceutically acceptable salts, stereochemical isomers, hydrates or solvates. An in-vitro cellular level anti-HIV-1 activity experiment result shows that the compound has relatively high anti-HIV-1 biological activity, can be used for remarkably inhibiting virus replication in MT-4 cells infected by an HIV-1 virus, and has relatively low cytotoxicity. The invention also comprises a pharmaceutical composition which is used for preventing and treating AIDS and contains the compound.

The invention discloses a diaryl pyrimidine HIV-1 reverse transcriptase inhibitor containing a six-membered non-aromatic ring as well as a preparation method and application of the diaryl pyrimidine HIV-1 reverse transcriptase inhibitor. The compound has a structure as shown in a general formula I. The invention also relates to a pharmaceutical composition containing the compound with the structure as shown in the formula I. An activity screening experiment shows that the compound disclosed by the invention has good anti-HIV-1 activity, so that the invention also provides application of the compound in preparation of an anti-AIDS medicine.

The invention belongs to the technical field of green organic chemistry, and particularly relates to a method for catalytically synthesizing a pyrimidones derivative by using natural polymer modified sulfonic acid functional chitosan. The method comprises the following steps: adding aromatic aldehyde, aromatic ketone, urea and a sulfonic acid functional chitosan catalyst in a flask; carrying out heating reaction at the temperature of 90 DEG C under the condition that a solvent does not exist to obtain a coarse product; and carrying out recrystallization on the coarse product to obtain a pure 4,6-diaryl pyrimidine-2(1H)-one derivative. The catalyst has the advantages of good catalyst biocompatibility, high catalytic activity, easiness in separation and recycling, environmental friendliness and the like, and has wide development prospect in the field of organic synthesis and catalysis.

The invention belongs to the technical field of medicines, and particularly relates to a cyano-vinyl substituted benzodiaryl pyrimidine compound and a preparation method and application thereof. The compound disclosed by the invention is the cyano-vinyl substituted benzodiaryl pyrimidine compound, and further comprises pharmaceutically acceptable salts, hydrates and solvates, polycrystals or cocrystals thereof as well as precursors and derivatives with the same biological function. The invention further discloses a preparation method of the cyano-vinyl substituted benzodiaryl pyrimidine compound and application of a composition containing one or more compounds in related drugs for treating acquired immune deficiency syndrome and the like. In-vitro cell-level anti-HIV-1 activity experimentsshow that the small molecules have high anti-HIV-1 biological activity, can remarkably inhibit virus replication in MT-4 cells infected by HIV-1 virus, and have low cytotoxicity.

The invention belongs to the technical field of heterocyclic compounds, and specifically relates to a heterocyclic compound containing six-membered rings without hydrogenation, with two nitrogen atoms as the only ring heteroatoms and not fused with other rings. The present invention provides a class of 4,5-diarylpyrimidinethiourea compounds conforming to the general formula 1. The process includes: adding reactant isoflavones to a solvent, and then adding a basic catalyst, amidinothiourea, and isoflavones The compound reacts chemically with amidinothiourea to obtain a mixture of the compound of the present invention and unreacted matter, which is purified by suction filtration under reduced pressure and recrystallization or column chromatography to obtain the pure product of the compound of the present invention. Also provided are a class of bactericidal drugs and compositions. Formula 1

The invention discloses an oxime group-containing diarylpyrimidine HIV-1 reverse transcriptase inhibitor, and a preparation method and application thereof. The oxime group-containing diaryl pyrimidineHIV-1 reverse transcriptase inhibitor or pharmaceutically acceptable salt or prodrug thereof has a structure represented by general formula I. The invention also discloses the preparation method of the oxime group-containing diarylpyrimidine HIV-1 reverse transcriptase inhibitor and application of a composition containing one or more compounds in preparation of medicines for treating and preventing human immunodeficiency virus (HIV). The structure of the diarylpyrimidine HIV-1 reverse transcriptase inhibitor is represented by general formula I in the specification.

A method for synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitor such as etravirine is provided Typically, etravirine is synthesized by the steps of a Condensing 2,4,6-trichlorpyrimidine with 3,5-dimethyl-4-hydroxybenzonitrile to obtain compound (V), b Condensing compound (V) with 4-aminobenzonitrile to obtain compound (VI), c Ammonolysis of compound (VI) to get compound (IV), d Halogenation of compound (IV) to get etravirine.