287 results about "Pyrazolylchalcone" patented technology

Pyrazolyl compounds of Formulas Ia and Ib are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using pyrazolyl compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

The compound 4-{4-[({3-tert-Butyl-1-[3-(hydroxymethyl)phenyl]-1H-pyrazol-5-yl}carbamoyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide and alternative forms thereof (e.g., salts, solvates, hydrates, prodrugs, polymorphs and metabolites); pharmaceutical compositions which contain them; and methods for treating cancer using them.

A proton pump inhibitor containing a compound represented by the formula (I)wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.

Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I), and pharmaceutically acceptable salts thereof; wherein-, R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful NI for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and / or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and / or withdrawal syndromes, and tinnitus.

Pyrazolyl compounds of Formulas Ia and Ib are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using pyrazolyl compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

The present invention relates to pyrazolylmethylamine-piperazine derivatives and their pharmaceutically acceptable salts effective as calcium channel modulators and a method of manufacturing the same. The present invention also relates to the medicinal use of the above compounds as therapeutic treatment of diseases due to their effect as calcium channel modulators.

Provided herein are methods for treating sickle cell disease, comprising administering to a subject 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)-methoxy)benzaldehyde (Compound 1), or a polymorph thereof, in certain dosing regimens.

The present invention relates to pyrazole compounds of formulae I or II and the salts and N-oxides thereof,wherein A is a pyrazole radical of formulae A1, A2 or A3, wherein# denotes the binding site; R41, R42, R43, R51 are H, halogen, CN, NO2, C1-C10-alkyl and the like; R52, R53 are H, halogen, CN, NO2, C1-C10-alkyl, and the like; R61, R62, R63 are H, CN, NO2, C1-C10-alkyl, and the like; T is C(Rt) or N; U is C(Ru) or N; V is C(Rv) or N; W is C(Rw) or N; with the proviso that at least one of the groups T, U, V and W is N; Rt, Ru, Rv, Rw are H, halogen, C1-C4-alkyl and the like; X1 is S, O or NR1a, wherein R1a is selected H, C1-C10-alkyl and the like; X2 is OR2a, NR2bR2c, S(O)mR2d, wherein m is 0, 1 or 2, R2a is C1-C4-alkyl, C1-C4-haloalkyl and the like, R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl and the like, or R2b and R2c together with the nitrogen atom to which they are bound form a heterocycle, and R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl and the like; and R1 is H, CN, C1-C10-alkyl and the like.The present invention further relates to a method for controlling invertebrate pests, to a method for protecting plant propagation material and / or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.

An ink set for ink-jet recording is formed from a yellow ink in which C. I. Direct Yellow 132 and C. I. Direct Yellow 86 are employed, a magenta ink in which a specific pyrazolylazopyridine-based (or pyrazolylazopyrazine-based) dye and another specific dye are employed, and a cyan ink in which two specific types of copper phthalocyanine-based dyes are employed.

Disclosed herein are novel antioxidant inflammation modulators, including those of the formula:wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.

A proton pump inhibitor containing a compound represented by the formula (I)wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof. or a prodrug thereof is provided.

6-Methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form.

The invention discloses a 4-aminopyrimidine derivative used as an adenosine A2A receptor antagonist. The 4-aminopyrimidine derivative has a general structural formula as shown in the description, wherein R1 is selected from halogen, cyano group or trifluoromethyl; R2 is selected from pyrazolyl, pyrrolidyl, or pyrazolyl or pyrrolidyl substituted by one or more halogens or C1-3 alkyl groups; and R3 is selected from oxazolyl, oxadiazolyl, triazolyl, or oxazolyl substituted by one or more halogens or C1-3 alkyl groups. The 4-aminopyrimidine derivative provided by the invention has an obvious antagonistic action on a human-derived adenosine A2A receptor, and can be applied to compositions or combination products for treating diseases or pathological symptoms having responses to the A2A antagonistic action, especially for treating neurodegenerative disease, extrapyramidal syndrome, depression, hyperkinetic syndrome, sleep disorders, anxiety disorder, diabetes, or tumor and other diseases.

The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

The invention discloses a porous metal-organic framework material, a preparation method and an adsorption and separation application of the porous metal-organic framework material, and belongs to thetechnical field of crystalline materials. The chemical formula is [M (BDP)], wherein M is Zn or Co and the organic ligand is 1, 4-bis (lH-pyrazol-4-yl) benzene (H2BDP). Under the sealing condition, the organic ligand H2BDP, isophthalic acid and cobalt nitrate hexahydrate or zinc nitrate hexahydrate are subjected to thermal reaction in a mixed solution of N, N-dimethylformamide, ethanol and water to obtain crystals of the metal-organic framework. In the structure of the metal-organic framework, benzene rings of the ligand have 'face-to-face' pi-pi action, and the ligand is arched. The materialhas a large specific surface area and a permanent pore structure, and can be used as a material for separating ethane-ethylene mixed gas from propane-propylene mixed gas.

This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.

The present application relates to: (a) compounds of Formula (I):and salts thereof, wherein R1, R2, R3, R4, R5, R6, m, n, X and Y are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use for the treatment and prevention of diseases such as those associated with oxidative stress and inflammation.

The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and / or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.

The invention discloses a tri pyrazole ligand based nickel metal organic framework material, and a preparation method and applications thereof, and belongs to the technical field of crystalline statematerial. The chemical molecular formula is [Ni8(OH)4(OH2)2(BTPP)4], H3BTPP is used for presenting organic ligand 4, 4'-(5'-(4-(1H-pyrazole-4-yl)phenyl)-[1, 1':3'-1''-tetraphenyl]4, 4''-di yl)bi(1H-pyrazole). The tri pyrazole ligand based nickel metal organic framework material is synthesized under sealing conditions, organic ligand tri pyrazole ligand based nickel metal organic framework material(H3BTPP) and nickel nitrate are subjected to solvothermal reaction in a mixed solution of N, N-dimethyl formamide and water so as to obtain the tri pyrazole ligand based nickel metal organic framework material. The tri pyrazole ligand based nickel metal organic framework material is low in absorption capacity on low carbon hydrocarbons.

The invention relates to a 3-pyrazolyl tyrosine translation system and an application thereof. The invention relates to an aminoacyl-tRNA synthetase mutant, and an amino acid sequence contained in the aminoacyl-tRNA synthetase mutant is selected from a group consisting of amino acids as shown in SEQ (sequence) ID (identity) NO: 3 and conservative variants thereof. The invention provides a 3-pyrazolyl tyrosine translation system inserting 3-pyrazolyl tyrosine (pyTyr) into target proteins in a fixed-point specific manner by utilizing the pairing of orthogonal tRNA (transfer ribonucleic acid) and orthogonal aminoacyl-tRNA synthetase and a method for inserting the 3-pyrazolyl tyrosine into the target proteins in a fixed-point specific manner by utilizing the translation system. The 3-pyrazolyl tyrosine translation system contains (i) the 3-pyrazolyl tyrosine; (ii) the orthogonal aminoacyl-tRNA synthetase; (iii) the orthogonal tRNA, wherein the orthogonal aminoacyl-tRNA synthetase uses the 3-pyrazolyl tyrosine to perform priority aminoacylation on the orthogonal tRNA; and (iv) nucleic acid encoding the target proteins, wherein the nucleic acid contains at least one selector codon which is specifically identified by the orthogonal tRNA.

This charge-transporting varnish, which contains a solvent, an electron-accepting dopant substance, and an aryldiamine compound represented by formula (1), imparts a charge-transporting thin film that has high transparency and can evince favorable element characteristics when applied to an organic EL element.(In the formula: R1-R4 each independently represent a hydrogen atom, a halogen atom, a nitro group, a cyano group, a hydroxyl group, a thiol group, a phosphate group, a sulfone group, a carboxyl group, an alkoxy group having 1-20 carbon atoms, or the like; R5-R8 each independently represent a hydrogen atom, a phenyl group, a naphthyl group, a pyridyl group, a pyrimidinyl group, a pyridazinyl group, a pyrazinyl group, a furanyl group, a pyrrolyl group, a pyrazolyl group, an imidazolyl group, a thienyl group, or the like; and n represents an integer from 2 to 5.)

The invention discloses a metal-organic framework based on a tripyrazole ligand, a preparation method and application of the metal-organic framework in organic dye degradation, and belongs to the technical field of crystalline materials. The chemical formula of the metal-organic framework is [Zn7 (OH) 2 (TPA) 4 (H2O)], and the organic ligand is 4, 4 ', 4'-tri (1H-pyrazole-4-yl) triphenylamine (H3TPA). The preparation method comprises the following steps: under a sealed condition, carrying out thermal reaction on an organic ligand H3TPA, zinc nitrate hexahydrate and 4, 4 '-dipyridyl in a mixed solution of N, N-dimethylformamide and water to obtain a crystal of the metal-organic framework. The metal-organic framework material has a relatively large specific surface area and a permanent porous structure, and the integrity of the framework structure can be kept in an aqueous solution environment with the pH value of 2-13. The material has visible light absorption performance and can be used as a catalyst for photocatalytic degradation of organic dye in a water body.

Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R1, R2 and R3 at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R4 is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl.

The invention discloses pyrazolyl steroid derivatives having a structure shown in the formula (I) in the specification, wherein substituent R1 can be H, nitryl or halogen, substituent R2 can be C1-C6 alkyl, hydroxy-substituted C1-C6 alkyl or monosubstituted or polysubstituted aryl. The synthesis route of the pyrazolyl steroid derivatives takes pregnenolone as a raw material; the method is used for synthesizing the pyrazolyl steroid derivatives for the first time and has the advantages of high yield, easy separation and the like. The pyrazolyl steroid derivatives show inhibitory activity for human lung adenocarcinoma cell, cervical carcinoma cell line and hepatoma carcinoma cell and have a prospect of being developed into anti-cancer drug or medicine compositions.

The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formulawhereinAr is a 6-membered heteroaryl group, containing one or two N-atoms, which are the groups, pyridinyl, pyrimidinyl, pyridazinyl, or a 5-membered heteroaryl group containing from 1 to 3 heteroatoms, selected from N, S or O, which groups are imidazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadazolyl, isoxazolyl, oxazolyl, 1,3,4-thiadiazolyl or pyrazolyl;R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl;R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o—O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o—S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH2)o—S(O)2-lower alkyl, lower alkyl substituted by halogen or CH2CH(OH)CF3;R3 is halogen or lower alkyl;X is CH or N;X1 is CH or N;n is 1 or 2;is 0, 1, 2 or 3;m is 0, 1 or 2;and the dotted line indicates a bond may or may not be present; or,a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and / or optical isomer and / or stereoisomer thereofThe compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

The invention discloses a silicon-nitrogen compound as well as a preparation method and application thereof. The structural formula of the silicon-nitrogen compound is as shown in a formula I, wherein X radical is one radical or a combination of radicals selected from pyrazolyl, substituted pyrazolyl, imidazolyl, substituted imidazolyl or amino. The silicon-nitrogen compound disclosed by the invention has a higher vulcanization rate for RTV (Room Temperature Vulcanization) silicon rubber under the room temperature and can be used for providing better heat resistance to the silicon rubber, better bonding strength to the steel and bigger application value.

There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of kallikrein, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing certain diseases or disorders, which disease or disorder is amenable to treatment or prevention by the inhibition of kallikrein.

The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.