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41 results about "Diarylpyrimidines" patented technology

Diarylpyrimidines (DAPY) and diaryltriazines (DATA) are two closely related classes of molecules resembling the pyrimidine nucleotides found in DNA. They show great potency in inhibiting the activity of HIV reverse transcriptase. Several compounds in this class are non-nucleoside reverse transcriptase inhibitors used clinically in the treatment of HIV/AIDS, notably etravirine and rilpivirine.

Pyrimidine-2,4-diamines and their uses

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.
Owner:RIGEL PHARMA

Pyrimidine-2,4-diamines and Their Uses

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.
Owner:PHAMIDIPATI SOMASEKHAR +1

Pyrimidine-2,4-diamines and their uses

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.
Owner:RIGEL PHARMA

Pyrimidine derivative, preparation method and use thereof

A pyrimidine derivative and the preparation method and usethereof. The said pyrimidine derivative is a diaryl pyrimidine derivative or a diaryl benzo pyrimidine derivative which has the structure shown as the Formula I and IV.Present pyrimidine derivative can be used for the prevention or the treatment of HIV.
Owner:FUDAN UNIV

Diarylpyrimidines HIV-1 reverse transcriptase inhibitor as well as preparation method and application thereof

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).
Owner:SHANDONG UNIV

Diarylpyrimidine compound, composition and application

InactiveCN105968056AMost of these compounds have strong application valueStrongly inhibit the proliferation of non-small cell lung cancer (NSCLC) cellsOrganic active ingredientsOrganic chemistryDiseaseProtein-Tyrosine Kinases
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.
Owner:DALIAN MEDICAL UNIVERSITY

Diaryl pyridine derivatives, preparation method thereof and application thereof

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.
Owner:FUDAN UNIV

Chemical Compounds

Novel diarylpyrimidine derivatives and pharmaceutically acceptable salts, solvates or hydrates thereof, designed to inhibit HIV reverse transcriptase, are provided, and a pharmaceutical composition containing the same, especially an anti-HIV agent. More specifically, novel diarylpyrimidine derivatives that are derivatives of the HIV reverse transcriptase inhibitor TMC278 of formula (1a) are provided, and pharmaceutically acceptable salts, solvates or hydrates thereof.
Owner:GLAXO SMITHKLINE LLC

2,3-diaryl pyrimidine [1,2-a]benzimidazole heterocyclic compound, preparation and use thereof

InactiveCN101486711APhotoluminescenceStrong photochromic performanceOrganic chemistryTenebresent compositionsChemical reactionPhotoluminescence
The invention pertains to the technical field of a heterocyclic compound, in particular relates to an un-hydrogenated heterocyclic compound which contains five / six-membered ring, three nitrogen atoms as heterocycle atoms and other condensed benzene rings. The invention provides 2, 3-diaryl pyrimidine [1, 2-a] benzimidazole compounds which conform to general formula 1; the technology comprises the following steps: a reactant, i.e., isoflavone is added into a solvent; then, a basic catalyst and benzo 2-aminooimidazole are also added into the solvent; the reactant reacts with the 2-aminooimidazole to obtain a mixture of the un-hydrogenated heterocyclic compound and un-reacted materials; and the mixture is re-crystallized for purification so that the pure heterocyclic compound is obtained. The invention also provides a photoluminescence material which can be applied to the preparation of anti-fake labels and modification labels and also can be used as indicators of night road-signs.
Owner:SHAANXI NORMAL UNIV

Diaryl pyrimidine derivative, preparation method and use thereof

The invention belongs to the technical field of medicines and relates to a diaryl pyrimidine derivative of the general formula I, medicinal salts thereof, hydrates and solvolytes thereof, polycrystal and eutectic thereof, and precursors and derivatives thereof with the same biological functions, a preparation method thereof, application of combination containing one or more compounds in relative medicines for treating acquired immune deficiency syndrome and the like, a preparation method and use of the combination. Experimental results show that the compound of the invention not only has excellent biological activity of resisting HIV-1 virus and relatively small cytotoxicity, but also shows relatively good inhibitory action to a drug-resistant virus strain L103N+Y181C, can be used as medical candidate resisting the HIV and can be further developed as a medicine resisting AIDS.
Owner:FUDAN UNIV

Diaryl pyrimidone hydrazone derivatives and preparation method and application of diaryl pyrimidone hydrazone derivatives

InactiveCN102153517ANovel structureGood anti-HIV biological activityOrganic active ingredientsAntiviralsHydrazoneOrganic solvent
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.
Owner:FUDAN UNIV

Diarylpyrimidine derivative containing biphenyl structure and preparation method and application thereof

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.).
Owner:FUDAN UNIV

Diarylpyrimidine derivative containing six-membered nitrogen heterocyclic ring as well as preparation method and application of diarylpyrimidine derivative

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.
Owner:SHANDONG UNIV

2-amido-4, 5-diaryl miazines compound, preparation and pharmaceutical use thereof

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.
Owner:SHAANXI NORMAL UNIV

Triazole-ring-containing diaryl pyrimidine HIV-1 inhibitor as well as preparation method and application of triazole-ring-containing diaryl pyrimidine HIV-1 inhibitor

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).
Owner:SHANDONG UNIV

Diarylpyrimidine HIV-1 reverse transcriptase inhibitor containing trans-double bonds, and preparation method and application thereof

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).
Owner:SHANDONG UNIV

Substituted 1,2,3 triazole diarylpyrimidine derivative as well as preparation method and application thereof

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).
Owner:SHANDONG UNIV

Piperidine-4-amido diaryl pyrimidine derivative as well as preparation method and application thereof

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.
Owner:FUDAN UNIV

Biphenyl diaryl methyl pyrimidine derivative containing aromatic heterocyclic structure, and preparation method thereof

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.
Owner:FUDAN UNIV

Diaryl pyrimidine HIV-1 reverse transcriptase inhibitor containing six-membered non-aromatic ring as well as preparation method and application of diaryl pyrimidine HIV-1 reverse transcriptase inhibitor

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.
Owner:SHANDONG UNIV

Method for catalytically synthesizing 4,6-diaryl pyrimidine-2(1H)-one derivative by using sulfonic acid functional chitosan

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.
Owner:NANYANG INST OF TECH

Cyano-vinyl substituted benzodiaryl pyrimidine compound and preparation method and application thereof

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.
Owner:FUDAN UNIV

4,5-diarylpyrimidinethiourea compounds and pharmaceutical uses

InactiveCN101759651BAntibacterialDifferent degrees of antibacterial effectAntibacterial agentsOrganic active ingredientsChemical reactionFiltration
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
Owner:SHAANXI NORMAL UNIV

Oxime group-containing diarylpyrimidine HIV-1 reverse transcriptase inhibitor, and preparation method and application thereof

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.
Owner:SHANDONG UNIV

Process for synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitor

InactiveUS20110196156A1Simple and cost-effective and efficientSimple ,Organic chemistryAntiviralsNucleoside Reverse Transcriptase InhibitorStereochemistry
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.
Owner:GURJAR MUKUND KESHAV +5
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