190 results about "Pyrazole derivative" patented technology

The invention provides a tetrahydropyridinopyrazole derivative and application thereof in medicine, and particularly relates to 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 eutectic of the compound, and an intermediate and a preparation method of the tetrahydropyridinopyrazole derivative. The invention also relates to application in preparation of related medicines for treating diabetes mellitus. # imgabs0 #

Provided in the present invention are a tetrahydropyridopyrazole derivative and use thereof in medicine. Specifically provided is a compound as shown in general formula (I) or a racemate, stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or eutectic crystal thereof, an intermediate thereof, a preparation method therefor, and use thereof in the preparation of a related drug for treating diabetes or obesity.

Disclosed is a dual functional urease and nitrification inhibitor composition and method for inhibiting the hydrolysis of urea and nitrification of ammonia in soil. Methods of making the dual functional urease and nitrification inhibitor and / or a composition containing the dual functional urease and nitrification inhibitor are also disclosed.

Provided in the present invention are a pyridinopyrazole derivative pharmaceutical composition as shown in formula (I), and the use thereof in the preparation of an anti-tumor drug. The pharmaceutical composition comprises a compound of formula (I) and a PARP inhibitor.

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 invention provides a crystal form of a salt or eutectic of a pyridinopyrazole derivative (a compound as shown in a formula (I)), a preparation method of the crystal form, and application of the crystal form and the preparation method in preparation of related medicines. # imgabs0 #

A tetrahydropyridinopyrazole derivative and the use thereof in medicine. Specifically disclosed are a compound as shown in general formula (I) or a stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or eutectic crystal thereof, an intermediate thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating diabetes or obesity.

The invention relates to a pyrazole derivative as well as a preparation method and application thereof, and belongs to the technical field of medicines. Specifically, the invention discloses a pyrazole derivative as shown in a general formula (I), a pharmaceutical composition containing the pyrazole derivative and application of the pyrazole derivative in preparation of anti-parasitic drugs. The structural general formula (I) of the pyrazole derivative is # imgabs0. The pyrazole derivative disclosed by the invention has a remarkable effect in the aspects of resisting parasites, agricultural and forestry pests or environmental pests and the like, and has a wide application prospect.

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.

A method for preparing a pyrazole derivative 3-bromo-5-methyl-1-H-pyrazole-N-2-chloropyridine (compound of formula I) is disclosed, wherein the method is by reacting a compound of formula II with a halogen-substituted pyridine, or by decarboxylating a pyrazole carboxylic acid of formula XI in the presence of an acid, optionally in the presence of a base and an organic solvent. In addition, a method for preparing a synthetic precursor of formula II, formula IV, formula V, formula VI, formula XI, and a method for preparing a compound of formula VII are provided, including reacting a compound of formula I with an oxidant, optionally in the presence of a catalyst. A compound of formula I as a useful synthetic precursor for preparing an o-aminobenzamide of formula VIII is also disclosed.

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 invention belongs to the technical field of pharmaceutical synthesis, and particularly relates to epiandrosterone pyrazole derivatives, their synthesis methods and applications. The epiandrosterone pyrazole derivatives have a chemical structure represented by the general formula (1), wherein R is an alkyl group or an aromatic ring-containing group. The alkyl group is an aliphatic chain or a cycloalkane, and the aromatic ring-containing group is a phenyl group or a substituted phenyl group. The synthesis method of the epiandrosterone pyrazole derivatives uses epiandrosterone as a basic raw material and obtains the epiandrosterone pyrazole derivatives of the present invention through a series of different reactions. The epiandrosterone pyrazole derivatives disclosed in the present invention are a series of brand-new compounds, which are proposed for the first time. The synthesis method has a high preparation yield, and the obtained product is easy to separate. It is confirmed by biological assays that the epiandrosterone pyrazole derivatives exhibit good insecticidal activity against pests such as aphids, oriental armyworms, diamondback moths and whiteflies, and can be applied to the control of plant pests.

The invention relates to the technical field of biological medicines, in particular to application of pyrimido pyrazole derivatives in treatment of postmenopausal osteoporosis. The pyrimido pyrazole derivative is a derivative as shown in a formula I or a pharmaceutically acceptable salt thereof. Wherein R1 is as described in the claims and the specification. The pyridinopyrazole derivative is a derivative shown in a formula I or a pharmaceutically acceptable salt thereof, and can be used for preparing a medicine for treating and / or preventing osteoporosis, especially postmenopausal osteoporosis. # imgabs0 #

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.

The invention relates to the technical field of biological medicines, in particular to a pyrazole derivative with antitumor activity and a preparation method and application thereof. In the invention, a novel pyrazole derivative is prepared, and the pyrazole derivative has the property of efficiently inhibiting the activity of HIF-2alpha and shows a good effect of resisting the proliferation of colorectal cancer cells at an animal level, so that a safe and efficient candidate drug molecule is provided for targeted therapy of colorectal cancer; the pyrazole derivative is simple and feasible in preparation process, low in raw material cost and good in functional group compatibility.

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.