102 results about "Pyrazole derivative" patented technology

Disclosed are an optically pure oxaspiro-substituted pyrrolopyrazole derivative, a preparation method therefor and the pharmaceutical use thereof. The compounds are compounds as shown in formula (I) and formula (II) or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a prodrug thereof. Also disclosed are a preparation method therefor and the use thereof.

The present invention relates to pyrazole derivatives of formula (X)wherein ring A is a pyrazole and substituents RB1, RB2, n, RQ1, RQ2, RQ3, and RQ4 are as defined in claim 1, their manufacture, and their use in the manufacture of agrochemicals and pharmaceuticals.

Provided herein are compounds of formula (A): or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4, Ry, and Rz are as defined herein. Also provided herein is a pharmaceutically acceptable composition comprising a compound of formula (A), or a pharmaceutically acceptable salt thereof, as well as methods of using a compound of formula (A), or a pharmaceutically acceptable salt thereof, to treat various diseases and conditions mediated by nicotinamide phosphoribosyltransferase (NAMPT).

The present invention provides: a pharmaceutical composition for preventing, alleviating or treating cancer, comprising a compound of chemical formula 1 or 2, which is a pyrazole derivative, or a pharmaceutically acceptable salt, solvate, stereoisomer or combination thereof; and a pharmaceutical composition for preventing, alleviating or treating cancer, comprising a compound of chemical formula 1 or 2, or a pharmaceutically acceptable salt, solvate, stereoisomer or combination thereof, and an immune checkpoint inhibitor or an immune checkpoint pathway inhibitor.

The invention discloses a non-heme nitrogen tetradentate metal complex containing a pyrazole derivative and application of the non-heme nitrogen tetradentate metal complex, the pyrazole derivative is introduced into 2, 2 ', 2' '-(ethane-1, 1, 1-triyl) tripyridine to obtain a ligand, and the ligand is coordinated with metal to obtain the metal complex. The preparation method comprises the following steps: introducing pyrazole into 2, 2 ', 2' '-(ethane-1, 1, 1-triyl) tripyridine, introducing a substituent group on a pyrazole ring, and regulating central metal, so as to obtain the metal complex. The metal complex is used as a catalyst, can catalyze oxidation of an aromatic hydrocarbon substrate C (sp3)-H, and can improve the catalytic efficiency and stability of the catalyst; the method can be applied to the field of catalyzing oxidation of aromatic hydrocarbon substrate C (sp3)-H.

The application discloses cis-olefin amide-pyrazole derivatives and application thereof in anti-inflammatory drugs. The compounds have the effects of anti-inflammation, treatment of lung injury, chronic obstructive pulmonary disease and the like.

The present invention relates to a pyrazole derivative and a use thereof in medicine, and specifically relates to a compound as shown in general formula (I) or a stereoisomer, racemate, tautomer, and pharmaceutically acceptable salt thereof, an intermediate thereof, and a use thereof in inhibition or degradation of EGFR for treatment of EGFR-associated diseases such as cancer. B-L-K(I).

The invention relates to the technical field of compound synthesis and pesticides, in particular to benzothiazinone pyrazole derivatives as well as a preparation method and application thereof, and the general formula of the benzothiazinone pyrazole derivatives is as shown in formula I; the derivative has effective pre-emergence and post-emergence herbicidal activity, is high in safety to crops and can be applied to preparation of herbicides; the derivative is simple in structure and preparation process, low in production cost and wide in application prospect.

Disclosed is a fungicidal composition comprising (a) at least one compound selected from the group consisting of compounds having Formula 1, including all geometric and stereoisomers, tautomers, iV-oxides and salts thereof, (I) wherein R1, R2, R3, R4, R5, R6, m and n are as defined in the disclosure, and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant disease caused by a fungal plant pathogen, the method comprising applying to a plant or part thereof, or a plant seed, a fungicidally effective amount of a compound of Formula 1, an A-oxide or salt thereof (e.g., as a component in the above composition). Also disclosed is a composition comprising: (a) at least one compound selected from the above compounds of Formula 1, A-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.

The present invention relates to novel compounds of Formula (I'), wherein P, Q, A, B, m, n, R1, R2, R9, R10, R11 and R12 are defined as in Formula (I'). These compounds may be useful as muscarinic M4 receptor subtype ("M4-mAChR") positive allosteric modulators which are useful for the treatment or prevention of neurological and psychiatric disorders associated with muscarinic M4 receptor dysfunction and diseases in which the M4 receptor is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes of preparing such compounds and such compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases such as for example, cognitive decline, both positive and negative symptoms in schizophrenia as well as other disorders modulated by M4 muscarinic receptors.

The present application relates to pyrazole derivatives and their use in pesticides, in particular their use in the prevention and treatment of plant diseases caused by fungi. The structure of the pyrazole derivatives is shown in (I): wherein R1 is at least one of fluorine atom, chlorine atom, bromine atom, methyl, methoxy, difluoromethyl, trifluoromethyl, trifluoromethoxy; R2 is difluoromethyl or trifluoromethyl; X is nitrogen atom or oxygen atom. The pyrazole derivatives disclosed in the present application have good inhibitory effect on plant pathogenic fungi and can be applied to the prevention and treatment of plant diseases caused by fungi.

Relates to a pharmaceutical composition of pyridinopyrazole derivatives and application thereof in medicine, the pharmaceutical composition comprises an active component A and a pharmaceutical excipient, the active component A is selected from a compound shown in a general formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a co-crystal thereof, the pharmaceutical composition comprises 1-1200 mg of an active component A, and the content of the active component A is selected from 0.5%-99.0%. The invention also relates to application of the pharmaceutical composition in preparation of related medicines for treating cancers.

The present invention provides novel anilino-pyrazole derivatives that are inhibitors of cyclin dependent kinase 2 (CDK2). The invention also provides pharmaceutical compositions comprising the compounds, and methods for their use in the treatment of various conditions, diseases, and conditions associated with or associated with CDK2 activity or associated with abnormal cell growth, such as tumor growth and cancer.

A pharmaceutical composition or an antiviral agent for the treatment of pulmonary fibrosis is disclosed. The composition or the antiviral agent contains a compound of Formula 1, which is a pyrazole derivative, or a pharmaceutically acceptable salt thereof.

The present application relates to 1, 3-dimethyl-5-pyrazole carboxylic acid esters and related compounds, methods for their preparation and methods of their use as perfume and flavor ingredients in food, cosmetic, pharmaceutical, consumer and other compositions and products.

There is provided a method of treating an immune cytopenia in a subject in need thereof, the method comprising administering a therapeutically effective amount of a compound of formula (I) wherein R1, R2, R3 and R4 are as defined herein.

The present application relates to the technical field of pyrazole derivative compound synthesis, and particularly relates to a preparation method of an amino-formamido pyrazole derivative compound, which comprises the following steps: S1, synthesizing an intermediate 1 by using pyrazole amine and triphenyl chloromethane as raw materials; S2, synthesizing an intermediate 2 by means of a hydrazinolysis reaction of the intermediate 1; S3, oxidizing the intermediate 2 into an intermediate 3 by means of sodium nitrite; and S4, preparing a target product by condensing the intermediate 3 with Boc-ethylenediamine. The raw material in the present application is easy to obtain, and the reaction process is mild. The key intermediate acylhydrazine is synthesized by means of a hydrazinolysis reaction, and then the acylhydrazine is oxidized into the intermediate acyl azide by means of sodium nitrite, so that the use of an expensive reagent DPPA is avoided, and the material cost is greatly saved.

The invention discloses a functionalized pyrazole derivative with a structural formula as shown in a formula I or a formula II, which is prepared by the following steps: by taking N (1)-(o-acetyl aryl)-1, 2, 3-triazole as a raw material, adding a proper amount of solvent in an argon atmosphere under the action of alkali, and reacting at specific time and temperature to generate the functionalized pyrazole derivative; the method has wide substrate adaptability, the reaction process is simple and convenient to operate, the method is suitable for large-scale synthesis, and a new method and a new target can be provided for synthesis and modification of drugs; .

A compound, which can act as inhibitors of protein kinases, especially Class III RTKs such as FLT3, PDGFRα, c-KIT and / or CSF-1R kinases, for the treatments of diseases or disorders mediated by such kinases, has a structure of formula (I):or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a binder of a Proteolysis-Targeting Chimera (PROTAC) thereof. The compound can be used in the treatments of diseases or conditions mediated by FLT3, PDGFR, c-KIT, and / or CSF-1R kinases, or mediated by a mutant kinase of FLT3, PDGFR, c-KIT, and / or CSF-1R kinases. Such diseases or conditions may include cancers, autoimmune diseases, and bone resorptive diseases.

The present disclosure relates to a pyridinylpyrazole derivative or a pharmaceutically acceptable salt thereof and a composition for preventing or treating a protein kinase-related disease, which contains the derivative or salt as an active ingredient. Since the pyridinylpyrazole derivative of the present disclosure exhibits cytotoxicity by inhibiting polo-like kinase 1 (PLK1), which induces cell proliferation, when administered to an individual, it can be used for prevention or treatment of a protein kinase-related disease, specifically for prevention or treatment of cancer.

The present invention discloses a method for synthesizing a chiral 1,4-dienylpyrazole derivative compound with high chemical, regio- and enantioselectivity. Specifically, it is a method for preparing a chiral 1,4-dienylpyrazole derivative compound by combining an iridium catalyst and a chiral ligand to catalyze a substitution reaction between racemic 1,4-dienyl allyl alcohol and a pyrazole derivative compound, and the method belongs to the field of organic synthesis. The specific operation steps are: under argon protection, an iridium catalyst and a chiral ligand are added to a reaction tube, followed by adding 1,4-dienyl allyl alcohol, a pyrazole derivative compound and an additive, and then reacting at 0°C. After the reaction is complete, the reaction is quenched and purified to obtain a chiral 1,4-dienylpyrazole derivative compound. The method has good substrate applicability and mild reaction conditions. It has the advantages of high chemical selectivity, regioselectivity and enantioselectivity.

To provide crystalline polymorphs of a thiazolylpyrazole derivative, pharmaceutical compositions comprising them, and methods of using the crystalline polymorphs and their compositions.SOLUTION: Provided are crystalline polymorphs of 4-(3-fluorophenyl)-1-(5-(isopropylthio)-4-(4-(trifluoromethyl)cyclohex-1-en-1-yl)thiazol-2-yl)-3-methyl-1H-pyrazole-5-carboxylic acid, optionally in the form of its salt and / or hydrate or solvate.SELECTED DRAWING: None

The application belongs to the technical field of organic compounds and agricultural fungicides, and particularly relates to the antifungal application of a novel pyrazole compound. The application provides a novel pyrazole compound, which has a structure shown in formula (a). The pyrazole derivative has good antibacterial activity on various fungi and can be used for preparing an agricultural fungicide. Moreover, the pyrazole compound in the application has the advantages of simple synthesis and high yield, and overcomes the problems of complex synthesis and low yield of current pyrazole fungicides. The application has important significance for promoting the application of pyrazole fungicides in the disease control of crops, fruits and vegetables. The application not only provides a new control drug for crop fungi and fungal diseases caused by the fungi, but also enriches the resource library of pyrazole fungicides, and provides more choices for the application of pyrazole derivatives in the fields of medicine and agricultural research.

This invention relates to novel compounds and pharmaceutical compositions comprising novel isoquinolone compounds. More specifically, the invention relates to compounds useful as inhibitors of discoidin domain receptor 1 (DDR1) and discoidin domain receptor 2 (DDR2). The compounds are particularly useful in the treatment of cancer and fibrotic diseases.

The invention relates to the technical field of compound synthesis and pesticides, in particular to an N-phenylpyrazole derivative and a preparation method and application thereof.The N-phenylpyrazole derivative has the 100% control effect on broadleaf weeds under the dosage of 37.5-150 g a.i. / ha, and part of compounds have the good control effect on grassy weeds; the compound can obtain a better weeding effect at a low dosage, can be used as a potential PPO inhibitor and broadleaf weed post-emergence herbicide for development and use, and has the advantages of novel structure, simple preparation process, low production cost and wide application prospect.