Patent classifications
Y02P20/55
METAL OXIDE FILM-FORMING COMPOSITION AND METHOD OF PRODUCING METAL OXIDE FILM USING THE COMPOSITION
A metal oxide film-forming composition including a tertiary alkyloxycarbonyloxy group-containing aromatic hydrocarbon ring-modified fluorene compound represented by Formula (1) below; metal oxide nanoparticles surface-treated with a capping agent; and a solvent. In the formula, ring Z.sup.1 represents an aromatic hydrocarbon ring, R.sup.1a and R.sup.1b each independently represents a halogen atom, a cyano group, or an alkyl group, R.sup.2a and R.sup.2b each independently represents an alkyl group, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5a, and R.sup.5b each independently represents an alkyl group having 1 to 8 carbon atoms, k1 and k2 each independently represents an integer of 0 or more and 4 or less, and m1 and m2 each independently represents an integer of 0 or more and 6 or less
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NOVEL PHENOL COMPOUND OR SALT THEREOF
The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof:
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wherein R.sub.1, R.sub.2, R.sub.5, L.sub.1, L.sub.2, L.sub.3, A, X, and m are as described in the specification.
Nitrogenous heterocyclic compound, preparation method, intermediate, composition, and application
A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target. ##STR00001##
SYNTHESIS OF AMANIN AND ITS DERIVATIVES
The present invention relates to the chemical synthesis of amanin and its derivatives. The present invention also relates to intermediate products of the amanin synthesis.
HETEROAROMATIC DERIVATIVES FOR USE AS REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
The present invention relates to heteroaromatic derivatives for use as a regulator, a preparation method therefor and a use thereof. In particular, disclosed are compounds represented by general formula (I), preparation methods therefor, pharmaceutical compositions comprising said compounds, and a use thereof as Janus kinase inhibitors in treating inflammatory diseases and tumor-related diseases.
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A Process For Preparing Isoindolinone Derivative, Novel Intermediates Used For The Process, And A Process For Preparing The Intermediates
The present invention relates to a process for preparing an isoindolinone derivative represented by Formula 1, novel intermediates used for the process and a process for preparing the intermediates.
Mitochondria-Targeted Polypeptide, Preparation Method thereof, and Use thereof
Disclosed are a type of mitochondria-targeted polypeptides, the preparation method and the uses thereof. The polypeptide is abbreviated as MTP. The synthesis method of the present disclosure is simple, and the mitochondria-targeted polypeptide prepared by the method can specifically target the mitochondria of cells and are basically non-toxic to cells. In addition, these synthesized polypeptides demonstrate good cell-membrane-penetrating properties, and can conveniently undergo further multi-functional derivation and modification, thereby providing a potential delivery tool for the preparation of a mitochondria-targeted medicament.
METHOD FOR PREPARING ETELCALCETIDE HYDROCHLORIDE
The present invention relates to a method for preparing etelcalcetide hydrochloride (etelcalcetide HCL). A first peptide is de-protected and cleaved from a solid support by a first solution system, for obtaining a second peptide, followed by coupling an activated L-Cys-OH to the second peptide in the second solution system for forming a TFA salt of etelcalcetide that is not or hardly dissolved in the second solution system. After purification by column chromatography, the TFA salt of etelcalcetide can be converted to etelcalcetide HCL using a third solution system that excludes hydrogen chloride during a real-time monitoring salt exchange step. The present method provides a simplified process and the etelcalcetide HCL with high purity and yield, for being advantageously applied in mass production of etelcalcetide HCL.
FGFR4 inhibitor, preparation method therefor and pharmaceutical use thereof
Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs. ##STR00001##
NUCLEOSIDE DERIVATIVE AND USE THEREOF
Provided is a nucleoside derivative represented by the following formula (1):
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or a salt thereof, wherein R.sup.1 represents an alkoxy group, a hydrogen atom or a halogen atom; R.sup.2 and R.sup.4, which may be the same as or different from each other, each represents a hydrogen atom, a protective group for a hydroxyl group, a phosphate group, a protected phosphate group, or —P(═O).sub.nR.sup.5R.sup.6 in which n represents 0 or 1, R.sup.5 and R.sup.6, which may be the same as or different from each other, each represents a hydrogen atom, a hydroxyl group, a protected hydroxyl group, a mercapto group, a protected mercapto group, an alkoxy group, a cyanoalkoxy group, an amino group, or a substituted amino group, provided that when n is 1, both R.sup.5 and R.sup.6 cannot be the hydrogen atom at the same time; R.sup.3 represents —(CH.sub.2).sub.mNHR.sup.7 in which m represents an integer of 1 to 6, R.sup.7 represents a hydrogen atom, an alkyl group, an alkenyl group or a protective group for an amino group; and B represents a purin-9-yl group, a 2-oxo-pyrimidin-1-yl group, a substituted purin-9-yl group, or a substituted 2-oxo-pyrimidin-1-yl group.