C07F9/60

NITROXOLINE PRODRUG AND USE THEREOF
20210363165 · 2021-11-25 ·

Provided are a nitroxoline prodrug and a use thereof. Specifically, provided are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a composition containing the compound, and a use thereof in the preparation of anti-infective and antitumor drugs, and definitions of groups in formula (I) are as stated in the specification. The compound represented by formula (I) has better pharmacokinetic parameters such as solubility, blood medicine concentration, or half-life period than nitroxoline. The compound represented by formula (I) can reduce the frequency of drug administration, and has potential for application in other fields other than the field of urinary tracts.

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NITROXOLINE PRODRUG AND USE THEREOF
20210363165 · 2021-11-25 ·

Provided are a nitroxoline prodrug and a use thereof. Specifically, provided are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, a composition containing the compound, and a use thereof in the preparation of anti-infective and antitumor drugs, and definitions of groups in formula (I) are as stated in the specification. The compound represented by formula (I) has better pharmacokinetic parameters such as solubility, blood medicine concentration, or half-life period than nitroxoline. The compound represented by formula (I) can reduce the frequency of drug administration, and has potential for application in other fields other than the field of urinary tracts.

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INHIBITORS OF PSEUDOMONAS AERUGINOSA VIRULENCE FACTOR LasB

The present invention relates to compounds of formula (Ia) and the use thereof as inhibitors of P. aeruginosa virulence factor LasB. Formula (Ia). These compounds are useful in the treatment of bacterial infections, especially caused by P. aeruginosa.

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ENPP1 Inhibitors and Methods of Modulating Immune Response

Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with an ENPP1 inhibitor compound to inhibit the cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor compound is cell impermeable. ENPP1 inhibitor compounds can act extracellularly to block the degradation of cGAMP. Also provided are pharmaceutical compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of an ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject in conjunction with administering an ENPP1 inhibitor to the subject. The radiation therapy can be administered in the subject methods at a dosage and/or frequency effective to reduce radiation damage to the subject, but still instigate an immune response.

ENPP1 Inhibitors and Methods of Modulating Immune Response

Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with an ENPP1 inhibitor compound to inhibit the cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor compound is cell impermeable. ENPP1 inhibitor compounds can act extracellularly to block the degradation of cGAMP. Also provided are pharmaceutical compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of an ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject in conjunction with administering an ENPP1 inhibitor to the subject. The radiation therapy can be administered in the subject methods at a dosage and/or frequency effective to reduce radiation damage to the subject, but still instigate an immune response.

Drug targets of delayed aging and human brain diseases

The present invention includes a molecule, a method of identifying said molecule, and a method of using said molecule to inhibit the interaction of Aβ and Drp1 proteins. The molecules including diethyl (3,4-dihydroxyphenethylamine)(quinolin-4-yl)methylphosphonate (DDQ); [10-(4,5-dimethoxy2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)decyl]triphenylphosphonium methanesulfonate (MitoQ); 3-Hydroxynaphthalene-2-carboxylic acid (3,4-dihydroxy-benzylidene)-hydrazide (Dynasore); and/or 3-(2,4Dichloro-5-methoxyphenyl)-2,3-dihydro-2-thioxo-4(1H)-quinazolinone/3-(2,4-Dichloro-5-methoxyphenyl)-2-sulfanyl-4(3H)-quinazolinone (Mdivi-1).

Organic electron transport material and organic electroluminescent element using same

An organic electron transport material, which includes a phosphine oxide derivative represented by the following Formula (1): ##STR00001## R.sup.1 represents an atomic group which has one or more of either or both of aryl and heteroaryl groups and may have one or more phosphine oxide groups, R.sup.2 to R.sup.11 each independently represent an atom or an atomic group selected from the group consisting of a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a carbonyl group, an alkoxycarbonyl group, and a trifluoromethyl group.

Organic electron transport material and organic electroluminescent element using same

An organic electron transport material, which includes a phosphine oxide derivative represented by the following Formula (1): ##STR00001## R.sup.1 represents an atomic group which has one or more of either or both of aryl and heteroaryl groups and may have one or more phosphine oxide groups, R.sup.2 to R.sup.11 each independently represent an atom or an atomic group selected from the group consisting of a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a carbonyl group, an alkoxycarbonyl group, and a trifluoromethyl group.

INHIBITORS OF CREB-CBP INTERACTION FOR TREATMENT OF LEUKEMIA

Compounds and methods are provided for inhibiting a CREB-CBP protein-protein interaction in a sample. In some cases, the method includes modulating transcription of CREB in a cell that overexpresses CREB. Also provided are methods of inhibiting the proliferation of a cancer cell. The subject CREB transcription inhibitor compounds include a substituted salicylamide or a prodrug thereof. Methods of alleviating symptoms associated with cancer (e.g., Acute Myeloid Leukemia (AML) or Acute Lymphomblastic Leukemia (ALL)) in a subject in need thereof are also provided. Pharmaceutical compositions including the subject compounds find use in treating cancer. The subject compounds may be formulated or provided to a subject in combination with a second agent, e.g. an anticancer agent.

Organic electronic device

The present invention relates to organic electronic devices. The devices can include a first electrode, a second electrode, and a substantially organic layer. The substantially organic layer may include a lithium-containing compound, and may be arranged between the first and the second electrode. Also provided herein are organic light emitting diodes, organic solar cells, and organic field effect transistors that include the lithium-containing compound.