80 results about "Isothiazole" patented technology

A wood preservative composition comprising 4,5-dichloro-2-octylisothiazol-3(2H)-one, a method of treating a wood substrate therewith, and a wood product produced therefrom are provided. The wood preservative composition comprises at least 0.5% by weight of DCOI based on the total weight of the composition and a retaining additive comprising a solvent-borne polymeric resin, N a wax, or a combination thereof. A weight ratio of the DCOI to the retaining additive in the composition is in a range of 1:5 to 5:1.

The invention discloses a quaternized chitosan benzisothiazolinone derivative as well as a preparation method and application of the quaternized chitosan benzisothiazolinone derivative in efficient antibacterial performance. The derivative has a structure as shown in a formula 1. The preparation method comprises the following steps: reacting chitosan with glycidyl trimethyl ammonium chloride at 60-100 DEG C for 6-48 hours to obtain a product 1, namely hydroxypropyl trimethyl ammonium chloride chitosan (HACC); the preparation method comprises the following steps: reacting 1, 2-benzisothiazolin-3-one with sodium chloroacetate at the temperature of 110-140 DEG C for 12-36 hours to obtain a product 2: 2-(3-carbonyl benzo [d] isothiazole-2-(3H)-yl) acetic acid (BITCOOH); and reacting the product 1 with the product 2 under a neutral condition for 12-48 hours to obtain the quaternized chitosan benzisothiazolinone derivative (HACCBIT). The derivative has a broad-spectrum antibacterial property, and has a killing effect on a plurality of bacteria, such as staphylococcus aureus, escherichia coli, salmonella salmonella salmonella, lactobacillus paracasei, lysinibacillus sphaericus, acinetobacter lwoffii and the like, and the derivative can be used for killing a plurality of bacteria, such as the staphylococcus aureus, the escherichia coli, the salmonella salmonella salmonella, the lactobacillus paracasei, the lysinibacillus sphaericus, the acinetobacter lwoffii and the like.

A wood preservative composition comprising 4,5-dichloro-2-octylisothiazol-3(2H)-one, a method of treating a wood substrate therewith, and a wood product produced therefrom are provided. The wood preservative composition comprises at least 0.5% by weight of DCOI based on the total weight of the composition and a retaining additive comprising a solvent-borne polymeric resin, a wax, or a combination thereof. A weight ratio of the DCOI to the retaining additive in the composition is in a range of 1:5 to 5:1.

The invention discloses an application of a benzotriazolyl piperazine compound or a salt thereof in preparation of a medicine for treating pulmonary arterial hypertension, and belongs to a new application of the benzotriazolyl piperazine compound. 3-[4-[4-(1H-benzotriazole-1-yl) butyl] piperazine-1-yl] benzisothiazole hydrochloride (PH-001) is subjected to an in-vivo animal experiment; mainly based on pharmacological experiments in a rat pulmonary arterial hypertension model induced by monocrotaline, it is found that the right ventricular systolic pressure (RVSP), the right ventricular hypertrophy index (RVHI) and the pulmonary arterial wall thickness (PAWT) of a rat are all remarkably reduced after intervention of a test sample PH-001, and the technical scheme opens up a new way for clinical application in the field of pulmonary arterial hypertension treatment. Therefore, PH symptoms and disease course development are effectively relieved, a theoretical basis is provided for clinical development, and the traditional Chinese medicine composition is expected to become a new effective treatment strategy.

The invention belongs to the technical field of fine chemical engineering, and particularly discloses a method for preparing a broad-spectrum bactericide 2-n-butylbenzo [d] isothiazole-3 (2H)-ketone by a molecular editing method. The preparation method comprises the following specific steps: taking 3H-1, 2-benzodisulfophenol-3-ketone and n-butylamine as raw materials, taking Selectfluor as an additive, adding the raw materials and the additive into a mixed solvent, and carrying out heating and stirring reaction, so as to obtain the target product 2-n-butylbenzo [d] isothiazole-3 (2H)-ketone (BBIT). The method is simple and convenient to operate, the raw materials are easy to obtain, the yield is high, thiophenol raw materials or excessive alkali are prevented from being used, and potential application value is achieved.

The invention discloses a gastric retention double-layer sustained-release tablet and a preparation method and application thereof, and belongs to the field of pharmaceutical preparations, the active ingredient of the gastric retention double-layer sustained-release tablet is 3-[4-[4-(lH-benzotriazole-1-yl) butyl] piperazine-1-yl] benzisothiazole hydrochloride, and the gastric retention double-layer sustained-release tablet is composed of a quick-release drug release layer and a sustained-release drug release layer, the quick release layer contains an active component, a filler I and a disintegrating agent; and the sustained-release layer contains an active component, a filler II, an expansion material, a release retardant, an expansion accelerator and a stabilizer. According to the gastro-retention double-layer sustained-release tablet, the quick-release layer can quickly release the medicine to reach the effective blood concentration, and the retention time of the tablet in the stomach is prolonged after the sustained-release layer expands, so that the in-vivo absorption window of the medicine is prolonged, the maintenance of the blood concentration is realized, the in-vivo half-life period of active ingredients is remarkably prolonged, the administration frequency can be reduced, and the compliance of a patient is improved. The product is simple in preparation process, suitable for industrial production and wide in development prospect.

The present invention relates to an aqueous coating compound, in particular a paint or plaster, containing at least one organic and / or inorganic pigment and / or at least one filler, at least one polymeric organic binder, 2-octyl-2H-isothiazol-3-one (OIT), 4,5-dichloro-2-octyl-2H-isothiazol-3-one (DCOIT), at least one additive, and water, and in particular also zinc sulfide and / or zinc oxide. The pH value of the aqueous coating compound according to the invention is preferably less than 11.0 and is particularly in the range of 7.5 to 10.0. Furthermore, the invention relates to a coating obtained from the coating compound according to the invention, and to a substrate comprising a coatable surface and the coating according to the invention on this coatable surface.Finally, the invention relates to the use of the aqueous coating mass according to the invention for the production of coatings protected against microbial damage.

A wood preservative composition comprising 4,5-dichloro-2-octylisothiazol-3(2H)-one, a method of treating a wood substrate therewith, and a wood product produced therefrom are provided. The wood preservative composition comprises at least 0.5% by weight of DCOI based on the total weight of the composition and a retaining additive comprising a solvent-borne polymeric resin, a wax, or a combination thereof. A weight ratio of the DCOI to the retaining additive in the composition is in a range of 1:5 to 5:1.

The present invention provides a method for preparing an isothiazole-5(2H)-imine compound and its application. The method uses a thioacrylamide compound shown in formula I as a raw material, and a polysubstituted isothiazole-5(2H)-imine compound shown in formula II undergoes a ring-forming reaction under the action of an organic high-valent iodine compound. Compared with the preparation method of polysubstituted isothiazole-5(2H)-imine compounds in the prior art, the present invention utilizes an organic high-valent iodine compound to participate in the ring-forming reaction of the thioacrylamide compound, thereby realizing the preparation of polysubstituted isothiazole-5(2H)-imine compounds. The synthesis method has the advantages of easy availability of raw materials, mild reaction conditions, no safety risks, and no need to use a metal catalyst.

The present disclosure relates, in part, to solid forms of (S)-N-(8-(2-chloro-5-fluorophenyl)-3-(methylcarbamoyl)-6-oxo-5, 6, 7, 8-tetrahydroimidazo [1, 5-a] pyrazin-1-yl) benzo [d] isothiazol-3-carboxamide, salts thereof, crystalline forms thereof, and variants thereof.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

Telomerase inhibitor compounds are provided. Some compounds contain a lactone or lactam group covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In other examples, a sulfonamide-containing moiety is covalently bonded to a phenyl ring, which is itself bonded to a pyrazole group. In some embodiments, the telomerase inhibitor compounds have an amide moiety and a vinyl sulfonamide group bonded to an aromatic group. In other examples, the inhibitor compounds have an isothiazolidine 1,1-dioxide core bonded to a phenyl group. Aspects of the present invention also include pharmaceutical compositions containing the telomerase inhibitor compounds of the present invention, as well as methods for treating telomerase-related diseases or conditions.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

The present invention relates to compounds of Formula (I) wherein Ar1, R1 and R2 are as described in the description, and A is 4,5-dihydroisoxazole-3,5-diyl, imidazolidin-4-one-1,3-diyl, oxazol-2-one-3,5-diyl and oxazolidine-2-one-3,5-diyl, 1,2,3-triazole-1,4-diyl, isoxazole-3,5-diyl, imidazole-1, 4-diyl, and isothiazole-3,5-diyl; and their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.

The present invention relates to a method for preparing substituted isothiazole derivatives. The present invention belongs to the field of chemical synthesis, and specifically relates to a method for preparing substituted isothiazole derivatives represented by a compound of formula I, wherein each group is as defined in the specification.

This invention relates to a novel heterocyclic azo disperse dye and its preparation method. The dye has the following structural formula: R1, R2, R3, H, CH3, NHCOCH3; D1 is a substituted benzothiazole or benzoisothiazole. The compound provided by this invention can be used as a dye for dyeing polylactic acid fibers, and has the characteristics of high dyeing rate, bright color, excellent color fastness and strong industrial feasibility.

Telomerase reverse transcriptase (TERT) expression enhancing compounds, and methods for using the same, are provided. In some embodiments, the compounds are azoles, such as such as pyrazoles, imidazoles, triazoles, tetrazoles, thiazoles, isothiazoles, oxazoles, and isoxazoles. In certain embodiments, the azole compound includes an acyl substituent which includes an amide, for example, an alkyl amide. Methods of interest include contacting cells with a TERT expression enhancing effective amount of compound to increase TERT expression in the cells. These compounds and methods find use in a variety of applications in which increased expression of telomerase reverse transcriptase is desired.

Provided are a benzisothiazole compound and application thereof, and a pharmaceutical composition and application thereof, which relate to the technical field of medications, and specifically relate to a 2H-benzotriazole-substituted benzisothiazole compound having a novel structure shown in a formula (I), as well as a pharmaceutical composition including the compound, and use of the pharmaceutical composition for the manufacture of a medicament for treatment and / or prevention of premature ejaculation. The anti-premature ejaculation activity of the compound is significantly higher than that of a marketed drug, namely dapoxetine, as studied by in vivo activity tests.

The invention provides an isothiazole bixadiazole compound (formula I) and application thereof, the structural formula of the formula I is shown in the specification, and the definitions of R1-R7 are as defined in the specification. The isothiazole dioxadiazole compound disclosed by the invention has the advantages of high activity, low toxicity, small dosage and the like, particularly has better persistence and has better application prospects.

The present disclosure belongs to the technical field of medicines, and relates to the use of an isothiazolo[5,4-d]pyrimidine compound in treating inflammatory diseases, in particular to the use of a compound shown as formula (I) or pharmaceutically acceptable salts thereof in treating rheumatoid arthritis. The compound of formula (I) or the pharmaceutically acceptable salts or pharmaceutical compositions thereof of the present disclosure can achieve good safety while achieving good therapeutic effects, including but not limited to a relatively low incidence of adverse reactions.

The invention discloses a nanoparticle modified antibacterial packaging film and a preparation method thereof, and relates to the technical field of packaging materials. When the nano particle modified antibacterial packaging film is prepared, nano graphene sequentially reacts with 2-(2-chloroethyl) furan and 1, 2-benzisothiazole-3-ketone, and modified nano graphene is prepared; the preparation method comprises the following steps: reacting barbaloin with 2-chloro-4, 6-bis (oxyalkan-2-yl methoxy)-1, 3, 5-triazine to obtain functionalized barbaloin; the preparation method comprises the following steps: sequentially reacting linear low-density polyethylene with dimethyl allyl phosphate and 3-mercapto-1-propanol to prepare modified polyethylene; uniformly mixing the modified polyethylene, the functionalized barbaloin and the modified nano graphene, and carrying out tape casting to obtain a polyethylene film material; and coating the fluorine-containing coating liquid on the surface of a polyethylene film material to prepare the nano particle modified antibacterial packaging film. The nano particle modified antibacterial packaging film prepared by the invention has excellent antibacterial, flame-retardant, water vapor barrier and mechanical properties.

The present invention relates to substituted heterocyclic compounds represented by the general formula (I), or their isotopic forms, stereoisomers, or pharmaceutically acceptable salts thereof. The present invention also describes the method of making such compounds, pharmaceutical compositions comprising such compounds and their use in the treatment of central nervous system disorders.

The invention relates to A61M37 / 00, in particular to a hydrogel microneedle capable of controllably releasing an antibacterial agent to a diabetic wound and a preparation method of the hydrogel microneedle. The hydrogel microneedle is prepared from the following components: a composite antibacterial agent, a gel matrix, metal ions and water, the composite antibacterial agent comprises at least one of polysaccharide antibacterial agents, imidazole antibacterial agents, thiazole antibacterial agents, isothiazolone derivative antibacterial agents, quaternary ammonium salt antibacterial agents, quaternary phosphonium salt antibacterial agents, pyridinium salt antibacterial agents, organic tin antibacterial agents, guanidine salt antibacterial agents, phenol antibacterial agents and vanillin antibacterial agents; the gel matrix comprises at least one of hyaluronic acid or a derivative thereof, polyvinyl alcohol or a derivative thereof, polyvinylpyrrolidone or a derivative thereof, gelatin or a derivative thereof, and chitosan or a derivative thereof. The microneedle prepared from the composite antibacterial agent, the gel matrix, metal ions and water has excellent anti-inflammatory, anti-oxidation, mechanical strength and drug sustained-release effects, and can be used for continuously and effectively improving the pathological environment on diabetic wounds.

A wood preservative composition comprising 4,5-dichloro-2-octylisothiazol-3(2H)-one, a method of treating a wood substrate therewith, and a wood product produced therefrom are provided. The wood preservative composition comprises at least 0.5% by weight of DCOI based on the total weight of the composition and a retaining additive comprising a solvent-borne polymeric resin, a wax, or a combination thereof. A weight ratio of the DCOI to the retaining additive in the composition is in a range of 1:5 to 5:1.

The present application relates to the technical field of medicine, and particularly relates to a method for preparing a key intermediate 2-methylthio-N-methyl benzamide of axitinib medicine. The existing method for synthesizing 2-methylthio-N-methyl benzamide generally uses dangerous chemicals, has low process safety, and has poor stability of raw materials, and thus cannot meet the requirements of green chemistry and safe production. In view of the above problems, the present application provides a method for preparing a key intermediate 2-methylthio-N-methyl benzamide of axitinib medicine, which directly synthesizes 2-methylthio-N-methyl benzamide through one-step reaction by taking 2-methylbenzo[d] isothiazole-3(2H)-ketone as raw material and taking sodium sulfide nonahydrate as a key additive. The synthesis route is short, and the operation steps are few, and high-risk reagents such as sodium borohydride, trimethylaluminum and dimethylaminothiocarbonyl chloride used in the existing method are completely avoided.

The present invention relates to the technical field of fine chemical engineering, and specifically provides a method for preparing 3-halo-1,2-benzisothiazole, aiming to solve the problems of corrosion of reaction equipment and harsh production conditions existing in the purification of 3-chloro-1,2-benzisothiazole by direct concentration and distillation in the prior art. For this purpose, the preparation method of the present invention includes: S1: reacting 1,2-benzisothiazol-3-one, thionyl halide, a polar aprotic solvent, and a non-polar solvent under preset conditions to obtain a mixture containing 3-halo-1,2-benzisothiazole; S2: cooling the mixture containing 3-halo-1,2-benzisothiazole to -10 to 40 °C and then standing for layering to obtain a non-oil phase and an oil phase; S3: washing and distilling the oil phase in S2 to obtain 3-halo-1,2-benzisothiazole and a non-polar solvent. The present invention controls the proportion of raw materials, cools and layers after the reaction, and the oil phase is purified by first washing with water and then distilling to obtain the target product, thereby effectively improving the production conditions.

The invention provides isothiazolylcarboxamide compounds, pharmaceutical compositions, their use for inhibiting mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT 1), and their use in the treatment of a disease or condition, such as a proliferative disorder, inflammatory disorder, or autoimmune disorder.

This invention discloses a silver-catalyzed method for synthesizing benzo[d]isothiazol-3(2H)-one via sulfur-nitrogen atom exchange, belonging to the field of organic synthesis technology. The method uses benzodisulfonic acid ketone compounds and azide compounds as raw materials, and, under the action of a silver catalyst, inorganic base, and organophosphorus compounds, with acetonitrile as the solvent, undergoes a heated reaction followed by separation and purification to obtain the target product. This invention achieves molecular skeleton editing of benzodisulfonic acid ketone through S-N atom exchange. The reaction conditions are mild, require no inert gas protection, are simple to operate, exhibit good functional group tolerance, and achieve high yields. It can be applied to the later-stage transformation of active molecules and drug molecules, providing a new route for the efficient synthesis of benzo[d]isothiazol-3(2H)-one compounds.

A wood preservative composition comprising 4,5-dichloro-2-octylisothiazol-3(2H)-one, a method of treating a wood substrate therewith, and a wood product produced therefrom are provided. The wood preservative composition comprises at least 0.5% by weight of DCOI based on the total weight of the composition and a retaining additive comprising a solvent-borne polymeric resin, a wax, or a combination thereof. A weight ratio of the DCOI to the retaining additive in the composition is in a range of 1:5 to 5:1.

The invention relates to the technical field of TLR2 antagonists, in particular to a compound with a ketoxime ether structure and application thereof. The compound has a structure as shown in a formula I: # imgabs0 # or a pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R5 are independently selected from any one of hydrogen atoms, phenolic hydroxyl groups, amino groups, halogen, C1-C4 alkyl groups, C1-C4 alkoxy groups, C3-C5 cycloalkyl groups, C2-C4 alkenyl groups, C2-C4 alkynyl groups, amide groups, sulfanilamide groups, ester groups, cyano groups, OCH2F, OCHF2, OCF3, SCF3 and N (CH3) 2; the ring A is one of a 6-14-membered aryl group and a 5-14-membered heteroaryl group; and R6 is any one of an ester group with 1-15 carbon atoms, an amide group, a sulfanilamide group, an alkyl group, an alkoxy group, oxazole, isoxazole, thiazole, isothiazole, oxadiazole, thiadiazole, substituted oxazole, substituted isoxazole, substituted thiazole, substituted isothiazole, substituted oxadiazole and substituted thiadiazole. The compound can be used as a TLR2 antagonist.