568 results about "Pyrimidinones" patented technology

The present invention provides a novel pyrimidine compound having an excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them. In the formula, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a cycloalkenyl group having three to eight carbon atoms which may be substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, a nitrogen atom which may be substituted, an oxygen atom which may be substituted or a sulfur atom which may be substituted; R4 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one or more unsaturated bonds which may be substituted; and R5 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted.

A compound having excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action, of the following formula, a salt thereof or a solvate of them:wherein, R1 and R2, same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an aromatic hydrocarbon cyclic group, an acyl group or an alkylsulfonyl group, which groups may be substituted (except the hydrogen atom); R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, a nitrogen atom, an oxygen atom or a sulfur atom, which groups may be substituted (except the hydrogen atom, the halogen atom and the cyano group); R4 represents an aromatic hydrocarbon cyclic group which may be substituted, and R5 represents an aromatic hydrocarbon cyclic group which may be substituted.

Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation wherein R1 is cyclopropyl optionally substituted with 1-5 R5, isopropyl optionally substituted with 1-5 R6, or phenyl optionally substituted with 1-3 R7; R2 is ((O)jC(R15)(R16))kR; R is CO2H or a herbicidally effective derivative of CO2H; R3 is halogen, cyano, nitro, OR20, SR21 or N(R22)R23; R4 is —N(R24)R25 or —NO2; j is 0 or 1; and k is 0 or 1; provided that when k is 0, then j is 0; and R5, R6, R7, R15, R16, R20, R21, R22, R23, R24 and R25 are as defined in the disclosure. Also disclosed are compositions comprising the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I. Also disclosed are compositions comprising a compound of Formula I and at least one additional active ingredient selected from the group consisting of an other herbicide and a herbicide safener.

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.

Disclosed are a 2,4,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient.Since the novel 2,4,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.

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

Disclosed herein is a regioselective synthesis of compounds represented by formula (I):or a salt, solvate, clathrate, or prodrug thereof, wherein X, Y, R2, R3, R4, R7, R8, R9, R10, m and n are defined as within.

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 present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

A compound of the formula:wherein R1 and R2 each is hydrogen, hydroxy, C1-4 alkoxy, C1-4 alkoxy-carbonyl or C1-4 alkyl which may be substituted; R3 is hydrogen, halogen, hydroxy or C1-4 alkoxy which may be substituted; or adjacent two R3 may form C1-4 alkylenedioxy; R4 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl which may be substituted or a group of the formula:wherein R5 is hydrogen or R4 and R5 may form heterocycle; and n is 0-5, or a salt thereof, has an excellent GnRH-antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases.

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 disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

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 present invention relates to herbicidally active compositions, which comprise 3-[5-(difluoromethoxy)-1-methyl-3-(trifluoromethyl)pyrazol-4-ylmethylsulfonyl]-4,5-dihydro-5,5-dimethyl-1,2-oxazole [common name pyroxasulfone] and at least one herbicide B which is selected from the groups ofb.1 imidazolinone herbicides;b.2 sulfonylurea herbicides;b.3 triazolopyrimidine herbicides;b.4 pyrimidinylbenzoate herbicides; andb.5 sulfonylaminocarbonyltriazolinone herbicides.The invention furthermore relates to the use of a composition as defined herein for controlling undesirable vegetation in crops.

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 present invention provides a pyrrolopyrimidine compound and a use thereof. Specifically that the present invention provides a class of pyrrolopyrimidine compounds with the inhibitory activity of JAK kinase. The present invention further provides a drug composition containing the pyrrolopyrimidine compound, and an application of the drug composition in treatments of inflammatory diseases, cancer and other diseases.

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.