11results about How to "Reduced inhibitory activity" patented technology

The invention discloses a pyrimidine compound as well as a preparation method, a pharmaceutical composition and application thereof. The structure of the compound is shown in a formula I, and the compound further comprises enantiomers, diastereoisomers, racemes, cis-trans-isomers, deuterated compounds, metabolites, prodrugs, solvates, hydrates, pharmaceutically acceptable salts or co-crystals of the compound. The compound has high-efficiency and high-selectivity inhibitory activity on various mutants of EGFR single mutation, double mutation and triple mutation, has low activity and low toxicity on wild type EGFR, and has a good treatment effect on cancers; the problems that an existing EGFR inhibitor is poor in effect, low in selectivity, resistant to drugs and the like are solved. # imgabs0 #

This application provides a compound. The compound is a compound as shown in Formula (I) or a stereoisomer, tautomer, deuterated compound, oxynitride, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compound having a structure as shown in Formula (I).

The present invention provides an anti-tumor agent for treating a patient with a malignant tumor expressing EGFR, wherein the EGFR has at least one mutation selected from the group consisting of an L718X mutation in exon 18 and an L792X mutation in exon 20, wherein X represents any amino acid residue, and the anti-tumor agent comprises (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizine-8-yl)acrylamide (compound (A)) or a salt thereof.

The invention relates to a tetrahydro-beta-carboline bacteriostatic agent as well as a synthesis method and application thereof. The method comprises the following steps: by taking a nicotinic acid analogue as a raw material, adding a solvent anhydrous dichloromethane for dissolving, reacting with thionyl chloride under the condition of oil bath heating to prepare a corresponding acyl chloride substrate, then carrying out amidation reaction with a tetrahydro-beta-carboline compound, adding a quenching agent for quenching reaction, and carrying out vacuum concentration to remove dichloromethane to obtain the heterocyclic compound. The compound has the application of inhibiting phytopathogen. The phytopathogens are Dioscorea nipponica, Phytophthora parasitica var nicotianae, rhizoctonia solani, Colletotrichum gloeosporioides, Colletotrichum frutescens and Coriolus versicolor. The synthesis process is simple, and the product purity is high.

A phosphate compound of a trifluoromethyl-substituted sulfonamide compound for selectively inhibiting anti-apoptotic protein BCL-2, a preparation method therefor, a pharmaceutical composition containing the compound, and the use thereof in the treatment of anti-apoptotic protein BCL-2-related diseases, such as cancer.

This invention discloses a benzamide / benzenesulfonamide compound containing an aryl butanone structure, its preparation method, and its application, belonging to the field of medicinal chemistry. The structure of the benzamide compound containing the aryl butanone structure is as follows: R1 is hydrogen, halogen, alkyl, or alkoxy; R2 is tert-butyl, tert-pentyl, tert-octyl, adamantyl, or α,α-dimethylbenzyl; R3 is hydrogen, halogen, alkyl, alkoxy, fused ring, or aryl; R4 is hydrogen, alkyl, or aryl. The structure of the benzenesulfonamide compound containing the aryl butanone structure is as follows: R1 is hydrogen, halogen, or alkyl; R2 is tert-butyl, tert-pentyl, or tert-octyl; R3 is hydrogen, halogen, alkyl, or fused ring. The advantages of this invention are that some of the prepared compounds exhibit strong inhibitory effects on MCF-7 and HCT-116, and can be used as lead compounds for the subsequent preparation and development of antitumor drugs.

The present invention discloses a pyridone compound, a preparation method and an application thereof. Specifically, the present invention relates to a compound of formula I, which can be used to treat diseases related to irritable bowel syndrome (IBS) and other gastrointestinal disorders, as well as to treat RET and / or TRK functional disorders or cancers that regulate RET and / or TRK activity, inflammatory bowel disease, neurodegenerative diseases, chronic pain, acute pain, inflammatory diseases, Trypanosoma cruzi infection, and diseases related to imbalanced bone remodeling regulation. #imgabs0#

A substituted triazinylmethylcycloalkylcarboxylic acid derivative having a structure as shown in formula (I). In addition, further disclosed are a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical composition and the use of the derivative. The compound has significant P2X3 inhibitory activity and selectivity, and is high in application value.

The present application relates to a kind of pyrazolo [1, 5-a] pyridine compound and its preparation method and application, including the pharmaceutical composition of active ingredient or its pharmaceutically acceptable salt of the compound described herein.The present application further relates to the compound of formula (I) in for treating and preventing the disease that can be treated with wild type, gene fusion type and mutant (including but not limited to G804 and G810) RET kinase inhibitor, including the disease or condition mediated by RET kinase.