43 results about "Ditazole" patented technology

The invention discloses a precise construction strategy of a dibenzothiophene sulfuryl covalent organic framework material and systematically explains efficient application of the dibenzothiophene sulfuryl covalent organic framework material in photocatalytic synthesis of thiadiazole and derivatives thereof. The achievement relates to a plurality of leading subjects such as catalytic chemistry, organic synthesis, material science, environmental engineering and green chemistry. According to the method, 2, 4, 6-triformyl phloroglucinol and 3, 7-diaminodibenzo [b, d] thiophene-5, 5-dioxide are taken as construction units, and the crystalline S-COF rich in sulfuryl active sites can be quantitatively obtained through topology-oriented Schiff base condensation under the conditions of protonic acid catalysis, no water and no oxygen. Under the radiation condition of visible blue light, S-COF is used as a heterogeneous photocatalyst to drive green synthesis of 3, 5-di-p-tolyl-1, 2, 4-thiadiazole and series of derivatives thereof; the invention provides a new catalyst design normal form for light-induced organic conversion, and lays a solid foundation for sustainable development-oriented efficient synthesis chemistry.

The present invention relates to fungicidal compositions comprising as component 1) the compound (I) methyl (2Z)-3-methoxy-2-[(4-methylbiphenyl-3-yl)oxy]prop-2-enoate) and as active component 2) the compound (II) N-(2-fluorophenyl)-4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3- yl]benzamide wherein the weight ratio of compound (I) to compound (II) is from 10:1 to 1:10.

One aspect of the present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is a phenyl group or a 5- or 6-membered heteroaryl group; Ring B is absent or is phenyl, pyridinyl, pyrazidinyl, pyrazinyl, pyrimidinyl, oxazolyl, isoxazolyl, thiadiazolyl, pyrazolyl, isothiazolyl or thiazolyl; Ring C is a fused bicyclic group of formula: (AA), wherein X1 to X9 form a substituted heteroaryl group containing at least one N and at least one NH; X-Y is -(CH2) m NR 21 CO; L is a direct bond or a linker group; Z is selected from alkyl, cycloalkyl, aryl, heteroaryl and heterocycloalkyl, each of which may be substituted; each R a and each R b is independently selected from alkyl, halo, haloalkyl, alkoxy, cycloalkoxy, haloalkoxy, cyano, NR 23 COR 25 、NR 24 -SO2R 26 、(CH2) q SR 27 、(CH2) q SOR 28 、(CH2) q SO2R 29 、SO2NR 30 R 31 、(CH2) q OH、(CH2) q OR 32 、NR 33 R 34 、CONR 35 R 36 、cycloalkyl and (CH q 2)-heterocycloalkyl; R 10 、R 11 、R 21 、R 22 、R 23 and R 24 are each independently selected from H and alkyl; R 12 ~R 20 、and R 25 ~R36 Each of the following is independently selected from H, alkyl, aralkyl, alkoxy, alkoxyalkyl, hydroxyalkyl, and cycloalkyl; each of m, n, and p is independently an integer from 0 to 4; and each of q is independently an integer from 0 to 4. Further aspects of the present invention relate to pharmaceutical compositions comprising the compounds according to the present invention and the use of the compounds in the treatment of various GPR35-related disorders. [Formula 1] TIFF2026510355000540.tif56170

Embodiments of the present disclosure are directed towards spray-dried compositions including a Zr phenol-oxadiazole complex and methods utilizing these spray-dried compositions.

The present invention relates to a process for the preparation of a P2X3 inhibitor, i.e., (R)-6-(5-fluoropyridin-2-yl)-8-methoxy-N-(1-(5-methyl-1, 2, 4-diazol-3-yl) ethyl) quinazoline-4-amine, or a pharmaceutically acceptable salt thereof, in particular to a process for the preparation of a P2X3 inhibitor. It also relates to intermediate compounds suitable for use in this process and the preparation thereof. The synthesized P2X3 inhibitor is suitable for medical application in pharmaceutical application.

The disclosure provide compounds of Formula I and the pharmaceutically acceptable salts thereof. The variables, R1, R2, R3, X1, X2, and Z are defined herein. Certain compounds of Formula I act as selective mitochondrial protonophore uncouplers that do not affect the plasma membrane potential. Compounds and salts of Formula I are useful for treating or decreasing the risk of conditions responsive to mitochondrial uncoupling, such as cancer, obesity, type II diabetes, fatty liver disease, insulin resistance, Parkinson's disease, ischemia reperfusion injury, heart failure, non-alcoholic fatty liver disease (NALFD), and non-alcoholic steatohepatitis (NASH). Because mitochondrial uncouplers decrease the production of reactive oxygen species (ROS), which are known to contribute to age-related cell damage, compounds of Formula I are useful for increasing lifespan. Compounds and salts of Formula I are also useful for regulating glucose homeostasis or insulin action in a patient.

The application discloses a thiazole-containing flavonol derivative and a preparation method and application thereof, and belongs to the technical field of pesticide synthesis. A thiazole-containing flavonol derivative is generated by substitution reaction of 3-(bromoalkyloxy)-7-substituent-2-(4-substituent phenyl)-4H-chromone-4-ketone and 5-substituent-2-thiol-1,3,4-thiadiazole, and a structural formula is shown as formula Y: wherein n is 3 or 4; R1 is hydrogen or an amino group; R2 is hydrogen, an alkyl group or an alkoxy group; and R3 is hydrogen, a halogen, an alkyl group or an alkoxy group. The thiazole-containing flavonol derivative has good bacteriostatic activity and can be applied to the preparation of bacteriostatic medicaments.

The application discloses a method for synthesizing 1,3,4-oxadiazole compounds from 1,2-dihydrazide compounds, and the specific implementation process is as follows: taking 1,2-dihydrazide compounds as shown in formula (I) as raw materials, adding alkali and a solvent into a reactor in sequence, and reacting in the atmosphere of a cyclization agent gas SO2F2, and after the reaction is completed, post-treatment is carried out to obtain 1,3,4-oxadiazole compounds as shown in formula (II), and the reaction process is as follows: in the formula, the substituent R1 on the benzene ring is substituted or not substituted, when the substituent R1 is substituted, the substituent R1 is fluorine, chlorine, bromine, a methyl group or a methoxy group, and the substituent R2 is a methyl group, an isopropyl group, a tert-butyl group or a phenyl group. The application has mild reaction conditions, uses a cheap and easily obtained cyclization agent, and efficiently promotes the preparation of 1,3,4-oxadiazole compounds.

Oxadiazole antibiotics that exhibit bactericidal activity against C. difficile vegetative cells. We screened a library of 75 oxadiazoles against C. difficile ATCC 43255. The findings from this collection served as the basis for the syntheses of an additional 58 analogs, which were tested against the same strain. We discovered a potent (MIC50=0.5 μg / mL, MIC90=1 μg / mL for 101 C. difficile strains) and narrow-spectrum oxadiazole (3-(4-(cyclopentyloxy)phenyl)-5-(4-nitro-1H-imidazol-2-yl)-1,2,4-oxadiazole; compound 57) that is not active against common gut bacteria or other tested organisms, but is selectively bactericidal against C. difficile and targets cell-wall synthesis. Other similarly effective oxadiazole antibiotics of formula I and II are described herein, several of which inhibit or prevent C. difficile spore germination.

The application belongs to the field of organic photoelectric functional materials, and discloses an organic up-conversion red light photosensitizer material, a preparation method and application. The material has the structure shown in the following formula (I). The molecule has a D-pi-A-pi-D structure, wherein 4,7-dibromo benzo[1,2-c:4,5-c'] bis([1,2,5]thiadiazole), 4,7-dibromo benzo[c]-1,2,5-thiadiazole, 4,7-dibromo benzo[d]thiazole and 4,7-dibromo-2,1,3-benzoselenadiazole are used as strong electron acceptors, can reduce the energy gap of the molecule, and make the absorption peak / emission peak red shift; triphenylamine is used as a strong electron donor and a pi-bridge, a spiral structure is formed, steric hindrance is increased, and the aggregation-induced emission characteristics are ensured; the carboxyl group on the triphenylamine provides good amphiphilicity for the overall structure. The synthetic route of the application is simple, is a potential red light TADF material, and has good fluorescence quantum yield and up-conversion efficiency.

The present invention discloses two novel synthetic methods for preparing monothiol-labeled mesylphenyl oxadiazole active esters. These methods use inexpensive commercial raw materials to prepare two kinds of mesylphenyl oxadiazole active esters for thiol labeling of antibodies, polypeptides, hydrogels, etc. through conventional transformations such as condensation and coupling. The preparation method of the present invention has a simple process, easily available raw materials, high product added value, and has good economic benefits and market prospects.

One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is phenyl or a 5-or 6-membered heteroaryl group; ring B does not exist, or is phenyl, pyridyl, pyridazinyl, pyrazinyl, pyrimidinyl, oxazolyl, isoxazolyl, thiadiazolyl, pyrazolyl, isothiazolyl or thiazolyl; ring C is a fused bicyclic group of the formula: (AA) wherein X1-X9 form an optionally substituted heteroaryl group containing at least one N and at least one NH; x-Y is-(CH2) mNR < 21 > CO; l is a direct bond or a linking group; z is selected from alkyl, cycloalkyl, aryl, heteroaryl and heterocycloalkyl, each optionally substituted; each Ra and each Rb are independently selected from the group consisting of an alkyl group, a halogen group, a haloalkyl group, an alkoxy group, a cycloalkyloxy group, a haloalkoxy group, a cyano group, NR23COR25, NR24-SO2R26, (CH2) qSR27, (CH2) qSOR28, (CH2) qSO2R29, SO2NR30R31, (CH2) qOH, (CH2) qOR32, NR33R34, CONR35R36, a cycloalkyl group, and (CH2) q-heterocycloalkyl group; r < 10 >, R < 11 >, R < 21 >, R < 22 >, R < 23 > and R < 24 > are each independently selected from H and alkyl; r12-R20 and R25-R36 are each independently selected from the group consisting of H, an alkyl group, an aralkyl group, an alkoxy group, an alkoxy alkyl group, a hydroxyalkyl group, and a cycloalkyl group; m, n, and p are each independently an integer from 0 to 4; and each q is independently an integer of 0 to 4. Other aspects of the invention relate to pharmaceutical compositions comprising compounds according to the invention, and the use of said compounds in the treatment of various GPR35-related conditions.

A solid formulation including at least one 1,2,4-oxadiazole derivative of formula (I):wherein R1, R2, R3, R4 and R5 are each independently selected from hydrogen, C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy and C1-C3 thioalkyl; and citric acid and / or saccharin, wherein the molar ratio in the solid formulation between the total amount of citric acid and / or saccharin and the amount of the 1,2,4-oxadiazole derivative(s) ranges from about 2 to about 20. Also a process for manufacturing the solid composition and a method for increasing the physical stability of a 1,2,4-oxadiazole derivative of formula (I).

This invention relates to a photosensitizer with a D1-π-A-π-D2 type structure based on asymmetric end-capped donor units. This material is characterized by using 4-(5-(4-(9H-carbazole-9-yl)phenyl)) as donor units (D1) and 5-(4-(diphenylamino)phenyl) as donor units (D2), with isooctylthiophene as the connecting π-bridge, and phenazine as the central acceptor unit (A), specifically naphthiazo[1,2-b][1,2,5]thiadiazo[3,4-g]quinoxaline and [1,2,5]thiadiazo[3,4-i]dithienozo[2,3-a:3',2'-c]phenazine. The photophysical properties of this D1-π-A-π-D2 type photosensitizer were tested, and a novel photosensitizer with high photothermal conversion efficiency and high reactive oxygen species (ROS) yield was developed. The material involved in this invention has near-infrared II region imaging and photothermal in-situ imaging diagnostic functions, and is expected to be used as an organic photosensitizer material for integrated photothermal and photodynamic diagnosis and treatment.

The present invention relates to a compound of formula (1) wherein Q1 is halogen atom, Q2 is hydrogen atom, etc., X, Y, and Z are nitrogen atom or oxygen atom, and R1 has a given structure, or a pharmaceutically acceptable salt thereof, and a medicament comprising the compound for treating and / or preventing a disease such as epilepsy.

To provide a compound which is an agonist of muscarinic M1 and / or M4 receptors and is useful for treating diseases mediated by muscarinic M1 and M4 receptors.SOLUTION: Also provided are pharmaceutical compositions containing the compounds, and therapeutic uses of the compounds. The compounds provided are of formula (I) wherein X1; X2; X3; X4; R1, R2 and R4 are as defined herein.SELECTED DRAWING: None

The present invention relates to crystalline forms of 2-(3-{5-[(R)-(1,3-dimethyl-azetidin-3-yl)-hydroxy-(4-isopropyl-phenyl)-methyl]-pyridin-3-yl}-[1,2,4]oxadiazol-5-yl)-propan-2-ol adipate and its use in the treatment or prevention of various diseases or disorders, such as cancer or inflammatory / autoimmune diseases or disorders.

The invention relates to an hnRNP A2B1 inhibitor based on a 1, 2, 4-oxadiazole structure and application of the hnRNP A2B1 inhibitor, and belongs to the field of chemical medicines. The structure of the hnRNP A2B1 inhibitor is as shown in a general formula I in the specification; wherein R represents benzyl and derivative groups thereof, benzoyl and derivative groups thereof, and cinnamoyl and derivative groups thereof. 1, 2, 4-oxadiazole is taken as a core structure and directly acts on an hnRNP A2B1 target spot, so that the problems of wide action target spots and high off-target toxicity risk of nonspecific inhibitors such as TAK-981 in the prior art are solved, and the specificity is remarkably improved. The compound is clear in structure, can be prepared on a large scale through chemical synthesis, is rich in pharmaceutically acceptable salt forms (hydrochloride, sulfate and the like), meets various preparation process requirements, and lays a good foundation for subsequent drug development.

The invention relates to compounds of Formula (I) as described herein, useful as histone deacetylase 6 (HDAC6) inhibitors. The invention also relates to pharmaceutical compositions comprising these compounds and to their use in therapy.

The present application relates to a kind of substituted benzyl sulfide oxadiazole compound, it has the regulation effect to PIEZO1 ion channel, can specifically agonize or inhibit PIEZO1 ion channel function, potential cardiotoxicity is lower, side effect is smaller, further perfects the structure-effect relationship of this kind of general formula applied to PIEZO1 agonist or antagonist and provides part pharmacological activity.

The invention discloses a preparation method of 3, 3 '-(1, 3, 4-oxadiazole-2, 5-methylene) bipyridine, which comprises the following steps: 1, dissolving 3, 6-bis (3-pyridyl)-1, 2, 4, 5-tetraazabenzene in an alcohol solvent to obtain a purple clear solution, adding hydrazine hydrate with the mass fraction of 50%, stirring at normal temperature, and separating out a solid, the alcohol solvent being methanol or ethanol; 2, filtering and washing with water to obtain a faint yellow solid; adding a first organic solvent for dissolving, slowly dropwise adding a second organic solvent to precipitate white solid, filtering, washing with a washing solvent, and carrying out rotary evaporation drying on the filtered solid to obtain a white solid pure product. The method has the advantages of simple preparation process route, mild reaction, easiness in control, low purification difficulty, few byproducts, high yield and high purity.

The present invention provides a synthesis method for fezolinetant, comprising: using (R)-3-methylpiperazin-2-one compound 1 as a starting material, first using p-toluenesulfonyl chloride to protect amino groups, to obtain (R)-3-methyl-4-p-toluenesulfonylpiperazin-2-one compound 2, then performing an alkylation reaction to activate amides, to obtain compound 3; compound 3 producing (R)-3-methyl-5-(8-methyl-7-p-toluenesulfonyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]piperazin-3-yl)-1,2,4-thiadiazole compound 7 by means of two pathways; finally, deprotecting and salifying compound 7 to obtain compound 8, and compound 8 undergoing a condensation reaction with compound 9, to yield a final product of fezolinetant, compound 10. This route is simple in operation, provides a relatively high overall yield, obtains a product having high purity, and is suitable for scaled-up production.

The invention discloses a method for preparing an On-DNA (deoxyribonucleic acid) 3-amino substituted-1, 2, 4-oxadiazole compound. The method comprises the following steps: by taking an On-DNA secondary amine compound as a substrate, carrying out nucleophilic substitution reaction on the On-DNA secondary amine compound and cyanogen bromide under an alkali condition to obtain an On-DNA cyano compound; the method comprises the following steps: carrying out an addition reaction on an On-DNA cyano compound and hydroxylamine hydrochloride under an alkaline condition to obtain an On-DNA amidoxime compound; carrying out condensation on the On-DNA amide oxime compound and small molecular acid to obtain an On-DNA-O-acetamido oxime intermediate compound; and finally, carrying out ring closing to obtain the On-DNA-3-amino substituted-1, 2, 4-oxadiazole compound. The reaction method provided by the invention can be carried out in a mixed water phase of an organic solvent / water phase, post-treatment is simple, conditions are mild, a high-diversity DNA coding compound library can be obtained at high yield within a short time, and the method is suitable for synthesis of DNA coding compounds by a porous plate.

This invention discloses two novel methods for synthesizing dithiol-bridged labeled bis(methylsulfonyl)phenyloxadiazole. These methods utilize inexpensive, commercially available raw materials and conventional transformations such as condensation and coupling to prepare two bis(methylsulfonyl)phenyloxadiazoles suitable for dithiol-bridged labeling of antibodies, peptides, and hydrogels. The preparation methods of this invention are simple, use readily available raw materials, and produce high-value-added products, demonstrating significant economic benefits and market potential.

Described herein are crystalline forms of (R)-5-(2,5-dichloro-4-(5-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)-1,2,4-oxadiazol-3-yl)phenoxy)piperidin-2-one, or a salt or solvate thereof.