57 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.

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 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.

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.

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; .

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 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.

A pyrazole derivative having a structure as shown in formula (I), and a pharmaceutically acceptable salt, stereoisomer, pharmaceutical composition and the use thereof. The compound has a good inhibitory activity and selectivity on CDK2.

This invention provides a 3-amino-5-phenyl-pyrazole derivative microtubule inhibitor, its preparation, and its pharmaceutical uses. The structure of the 3-amino-5-phenyl-pyrazole derivative is shown in formula (I): In formula (I), R1 is independently selected from 3,4,5-trimethoxyphenyl, 3,4-dimethoxyphenyl, or dioxolane[1,3-d]phenyl; R2 and R3 are independently selected from methyl, methoxy, fluorine, chlorine, or bromine. This type of compound not only possesses strong antitumor activity but also anti-angiogenic effects, effectively inhibiting the proliferation of tumor cells and can be used to prepare tumor proliferation inhibitors. Furthermore, it has a strong ability to inhibit microtubule aggregation, providing a novel microtubule inhibitor for inhibiting tumor cell proliferation.

The present application relates to pyrazole derivatives as inhibitors of the PD-1 / PD-L1 interaction. The applicants have designed compounds of general formula (I) wherein R ', R2, y3, R3, R4, R5, R6 and R7 are as defined herein, which are effective in blocking PD-1 / PD-L1 interactions to restore an anti-tumor immune response in a subject and eradicate any tumors in which dormant tumor cells and PD-L1 participate in immune escape. The inventor verifies that these compounds block the PD-1 / PD-L1 interaction by performing physical and chemical tests (MST, NanoDSF) and in vitro biological tests (FRET assay, Pralomig block assay, T cell assay). These compounds have affinity (Kd) in the order of pM, which Kd is higher than the Kd of the antibody Atezumab used in clinical use, and have IC50 comparable to or higher than that observed using Atezumab. Therefore, the invention also relates to a pharmaceutical composition containing the compound and application of the pharmaceutical composition in treatment of PD-1-PD-L1 interaction related diseases (cancers, chronic inflammatory diseases, neurological diseases and chronic infections).

The application discloses a kind of pyrimidopyrazole derivatives and its medical purposes.The pyrimidopyrazole derivatives are the compounds shown in general formula I, its pharmaceutically acceptable salt or solvate, the compound of the application can be used as ALKBH5 protein small molecule inhibitor, inhibits RNA demethylase at the level of protease, and can be used for treating acute leukemia, lung cancer, breast cancer, colon cancer, prostate cancer, pancreatic cancer, gastric cancer, liver cancer, ovarian cancer, kidney cancer, neuroglioma, melanoma, myeloma, lymphoma, bladder cancer or cervical cancer.

The application discloses a synthetic method for constructing N-B bond-containing pyrazole derivatives, and the method is characterized in that, under light conditions, an iridium metal complex is used as a photosensitizer, and an alkenyl diazo compound 1 is reacted with an azaheterocyclic carbene borane compound 2 in a solvent. In the reaction process, the azaheterocyclic carbene borane compound 2 generates an azaheterocyclic carbene boron radical cation through a single electron transfer process under the action of visible light and the photosensitizer, and the azaheterocyclic carbene boron radical cation then completes an addition-cyclization reaction on the alkenyl diazo compound 1. The method is driven by visible light as a green energy source, and the reaction is carried out in an air atmosphere, has a short reaction time and high efficiency, and is easy to operate.

The invention provides a preparation method of a sulfonylated dihydropyrazole derivative, and belongs to the field of organic synthesis. According to the invention, a (E)-N-allyl-N '-benzyl acethydrazide compound (compound 1), an aryl diazonium salt compound (compound 2) and DABSO (1, 4-diazabicyclo [2.2. 2] octane-1, 4-dionium-1, 4-disulfinic acid) are used as raw materials, and the sulfonylated dihydropyrazole derivative is prepared by a method of catalyzing insertion of sulfur dioxide. According to the preparation method, the problems of corrosion of reagents, expensive metals and excessive oxidizing agents during insertion of SO2 in the prior art are avoided.

The invention provides novel anilino-pyrazole derivatives as a cyclin-dependent kinase 2 (CDK2) inhibitors. The invention also provides pharmaceutical compositions comprising the compounds and methods thereof for treating various conditions, diseases and disorders associated with or related to CDK2 activities, or associated with abnormal cell growth, such as tumor growth and cancer.

The present disclosure relates to a crystal form of substituted 2-hydro-pyrazole derivative (I) and a preparation method thereof, and also includes the use of the crystal form in the preparation of drugs for treating breast cancer and other cancers.

Dual function urease and nitrification inhibitor compositions and methods for inhibiting hydrolysis of urea and nitrification of ammonia in soil are disclosed. Also disclosed are methods of preparing the dual-function urease and nitrification inhibitor and / or compositions containing the dual-function urease and nitrification inhibitor.

The invention discloses a dihydropyrazole EFTUD2 degradation agent as well as a preparation method and application thereof, the dihydropyrazole EFTUD2 degradation agent provided by the invention is designed by adopting a proteolysis targeting chimera, and a dihydropyrazole derivative is used as an EFTUD2 protein binding ligand and is connected with an E3 ubiquitin ligase ligand through connecting chains with different lengths and types. The compound has a remarkable EFTUD2 protein degradation effect, can effectively inhibit proliferation of tumor cells such as non-small cell lung cancer and the like, and also has potential treatment value on other types of solid tumors such as breast cancer, ovarian cancer, prostatic cancer and the like and blood system tumors. The synthesis route of the compound is simple and efficient, raw materials are easy to obtain, the yield is high, and the compound has a good industrialization prospect.