536 results about "Pyrimidinones" patented technology

The present invention provides compounds of Formula I,

including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R_a, R₂, and R₃ are defined as described herein.

The invention provides a fungicide composition containing an active component A and an active component B, and application thereof in preventing and controlling various agricultural fungal diseases. The active component A in the composition is one of two methoxyl acrylic ester compounds; and as shown above, the active component B of the compound A1 and the compound A2 is one of the following fungicide varieties: thiocarbamate compounds or salt thereof, aliphatic compounds or salt thereof, carbamate compounds or salt thereof, oxazole compounds or salt thereof, thiazole compounds or salt thereof, amide compounds or salt thereof, organophosphorus compounds or salt thereof, imidazole compounds or salt thereof, antibiotic compounds or salt thereof, pyridine compounds or salt thereof and triazole compounds or salt thereof.

The invention discloses a thieno 2,4-substituted pyrimidine compound of which the general formulas are (I), (II), (III) and (IV), or pharmaceutically acceptable salt or stereisomer or a prodrug molecule, and a pharmaceutical composition and application thereof. The thieno 2,4-substituted pyrimidine compound can effectively restrain abnormal expression of Aurora kinase, has specific inhibited effect on Aurora-A and Aurora-B, can be applied to a novel field of molecular targeting treatment, and has strong inhibitory activity on an excessive hyperplasia disease, especially cervical tumor cells, human macrophage line leukemia cell, and human t-lymphocyte line cancer cell.

The invention relates to novel pyrazolo[3,4-d]pyrimidines of the formula

in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

The invention relates to five-membered heterocycle pyrimidine compounds, their pharmaceutical acceptable salt or pharmaceutical acceptable solvate and a preparation method thereof. The five-membered heterocycle pyrimidine compounds possess a c-Met inhibitory activity and have a structure as shown in the general formula 1. The invention also relates to a drug combination which contains the compounds and applications of the compounds in preparation of drugs used for prevention and treatment of in vivo Hepatocyte Growth Factor Receptor (HGFR) related abnormal cell proliferation, morphologic change and hyperkinesis associated diseases, angiogenesis or cancer metastasis associated diseases, and especially for prevention and treatment of tumor growth and metastasis.

The invention searches the novel micromolecule inhibitor pyrazolo (1, 5-a) miazines compounds of cyclin-dependent kinase CDK9 (cyclin-dependent kinase) through the virtual screening of a computer, biometrically measures activity thereof, and validates interaction mechanism. The invention specifically comprises the following steps: the three-dimensional crystal conformation of the cyclin-dependent kinase family member CDK9 is obtained in a way of homology modeling; and micromolecule three-dimensional database is screened with DOCK (molecular docking). The invention uses a MTT tumor cell growth inhibition test to biometrically measures the activity of the selected compounds, researches the selected compounds pyrazolo (1, 5-a) miazines with high activety in a way of molecular mechanism, validates the inhibiting effect of the compounds to the activity of CDK9 kinase, and clarifies the interaction mechanism of the compounds for inhibiting the external activity and the molecule of various malignancies such as lung cancer, osteosarcoma, oophoroma, cervical carcinoma, breast cancer, etc.

The invention provides a pyrazolopyrimidine compound shown as a structural formula (I), a pharmaceutical composition taking the pyrazolopyrimidine compound as an active component, a preparation method of the pyrazolopyrimidine compound and the pharmaceutical composition as well as an application of the pyrazolopyrimidine compound and the pharmaceutical composition in preparation of a TRPC6 (Transient Receptor Potential Channel 6) adjustor probe medicine and related medicines for preventing and treating glomerulopathy and myocardial hypertrophy. The pyrazolopyrimidine compound and derivatives provided by the invention can be used to prepare medical preparations in various forms which comprise oral liquids, injections, pulmonary inhalation preparations and transdermal preparations, specifically injections, oral liquids, troches, capsules, granules, aerosols, dry powder inhalation, patches and the like.

The invention belongs to the medicine field, and concretely relates to a miazines compound having a structure of a formula (1), its pharmaceutically acceptable salt, a preparation method and an application of the compound for preparing an antitumor drug. The pharmacological experiment result shows that the compound has good inhibition effect to an epidermal growth factor acceptor (EGFR) and its mutant, can inhibit propagation of a plurality of tumor cells, and can be taken as an EGFR inhibitor used for preparing the antitumor drug.

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.

The invention belongs to the technical field of medicine, particularly relates to a substituted miazines compound disclosed in a general formula (I) and clinically-acceptable salt thereof, wherein R1, R2, R3, R4, R5, Z or W is defined as in a specification. The invention also relates to a preparation method of the compounds and the application of the compounds in preparing medicines capable of treating and/ or preventing sexual dysfunctions.

The present invention provides non-aqueous electrolyte solution for a lithium secondary battery, comprising a pyrimidine-based compound, a non-fluorinated solvent and a fluorinated solvent; and a lithium secondary battery using the same.

The invention relates to a triazolopyrimidine derivative, a preparation method thereof, and an application thereof in medicines. In particular, the invention relates to the triazolopyrimidine derivative represented as the general formula (I), a preparation method thereof, a medicine composition containing the derivative, and an application of the derivative as a treatment agent, especially an application as an A2a receptor antagonist, and an application in preparation of a medicine for relieving symptoms and diseases by inhibiting the A2a receptor; wherein the substituent groups in the generalformula (I) are defined as the specification.

The invention discloses thieno miazines derivatives and a preparation method and application thereof. The thieno miazines derivatives are compounds of which the structures are shown in the general formula I or pharmaceutically acceptable salts, esters or prodrugs of the compounds. The invention further provides the preparation method of the compounds as well as application of composition of one or more of the compounds to preparation of medicines for treating and preventing human immunodeficiency virus (HIV) infection.

The invention provides a pesticide composition and application thereof. The active components in the composition comprise methoxyl acrylic ester bactericide and pyrimidine bactericide (ethirimol or ethirimol sulphonate or dimethirimol); and the composition is suitable for controlling diseases in the agriculture. The pesticide composition has the following advantages: (1) the composition shows perfect synergy in a certain matching range, remarkably improves the bactericidal effect compared with a single dosage, simultaneously reduces the using dosage of the pesticide, application labor and cost, and also reduces adverse effect on the environment and pesticide residue; (2) two effective components in the composition have different action mechanisms, so the application of the composition can delay or overcome the pesticide resistance of pathogenic bacteria and prolong the service life of the single dosage; and (3) the composition has broad prevention and control spectrum, and can control various diseases of crops.

The present invention provides aminopyrimidine compounds of formula (I) and their salts, wherein R1, R2, R3, R4, R5, R6, Q, Z, L, m, n are defined as the description, the methods for preparation thereof, the uses thereof and the pharmaceutical compositions comprising the effective amount of compounds of formula (I). The compounds of formula (I) and their salts can be used as protein kinase inhibitors.

The invention provides substituted diaminopyrimidine compound, a composition comprising the compound and application of the compound. The substituted diaminopyrimidine compound is diaminopyrimidine compound shown as in formula (I) or its crystal-form pharmaceutically acceptable salts and prodrugs, and stereoisomer, hydrate or solvent compound. The substituted diaminopyrimidine compound disclosed herein and the composition comprising the compound have excellent inhibitory action on EGFR (epidermal growth factor receptor) kinase, have better pharmacokinetics parameter characteristics, and can increase the drug concentration of the compound in an animal body to provide improved drug therapeutic effect and safety.

The invention provides a substituted diaminopyrimidine compound and medicinal salt thereof. The structure of the substituted diaminopyrimidine compound is as shown in a general formula (I). A pharmacodynamic test proves that the compound is capable of effectively inhibiting growth of multiple tumor cells and can be used for preparing anti-tumor drugs, and meanwhile, the drug resistance of EGFR T790M can be overcome.

A beta-elemene pyrimidine derivative series is disclosd, which is prepared through reaction of beta-elemene on hypochlorite or NBS to obtain intermediate, and reacting on the pyrimidine's cyclic derivative in DMF or DMSO solvent.

The present invention relates to novel compounds, their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.