54 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 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 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.

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 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 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.

A lurasidone hydrochloride oral soluble film composition, a preparation method therefor and a use thereof are provided. The lurasidone hydrochloride oral soluble film composition contains an active drug, a film-forming material, a plasticizer and a flavoring agent. The active drug is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazole 3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylene-2H-isoindole-1,3-dione hydrochloride, as shown in Formula I.

The invention belongs to the technical field of medicine synthesis, and discloses a synthesis method of ceftazidime, which comprises the following steps: (1) under the action of an acid-binding agent, carrying out condensation reaction on 7-APCA and alpha-(2-aminothiazole-4-yl)-alpha-[(tert-butyloxycarboryl) isopropoxyimino] acetic acid mercaptobenzene isothiazole ester in a solvent to obtain 7-APCA-alpha (2-aminothiazole-4-yl)-alpha-[(tert-butyloxycarboryl) isopropoxyimino] acetic acid mercaptobenzene isothiazole ester; after the reaction is finished, carrying out post-treatment to obtain ceftazidime tert-butyl ester; in the step (1), the acid-binding agent is isooctylamine and an aniline compound in a mass ratio of (1-5): 1; (2) hydrolyzing and crystallizing the ceftazidime tert-butyl ester obtained in the step (1) under an acidic condition to obtain ceftazidime hydrochloride; and (3) further neutralizing and crystallizing the ceftazidime hydrochloride in the step (2) to obtain the ceftazidime. According to the synthesis method, by adopting the composite acid-binding agent, side reactions are reduced, the content of by-products is reduced, and the purity of the product is improved.

The application discloses a benzisothiazole carboxamide compound and application thereof. The benzisothiazole carboxamide compound has the characteristics of high specificity and high activity as an inhibitor of myosin motor domain, and can significantly inhibit the growth and development process and pathogenicity of pathogenic fungi, especially Pyricularia oryzae.

The invention relates to the technical field of organic synthesis, in particular to a method for preparing 3H-1, 2-benzodisulfonyl-3-ketone. The invention relates to a conventional synthesis method of 3, 3, 3-H-1, 2-benzodisulfonyl-3-ketone, which needs to use a thiophenol raw material with an unpleasant smell or a transition metal catalyst or a large amount of organic acid. In order to solve the technical problem, the invention provides the method for preparing the 3H-1, 2-benzobenzene-3-ketone, which comprises the following steps: by taking hydriodic acid as an additive and taking 2-methylbenzo [d] isothiazole-3 (2H)-ketone and a sodium sulfide hydrate as reaction raw materials, stirring and reacting in an organic solvent to generate the 3H-1, 2-benzene-3-ketone. In the reaction process, any thiophenol raw material or transition metal catalyst or a large amount of organic acid does not need to be added, the method is simple, raw materials are easy to obtain, and the method is green, environmentally friendly and high in yield and has good application prospects.

The application discloses a preparation method of lurasidone hydrochloride and belongs to the technical field of chemical synthesis. The method comprises the following steps: A: reacting (3aR,7aR)-4'-(benzo[d]isothiazol-3-yl) octahydrospiro[isoindol-2,1'-piperazine]-2-X ammonium with ronexiamine, toluene and potassium carbonate to generate an intermediate product shown in formula III (3aR,4R,7S,7aS)-2-((1R,2R)-2-(4-(benzo[d]isothiazol-3-yl)piperazine-1-methyl)cyclohexyl)methyl)-3a,4,7,7a-tetrahydro-1H-4,7-methylisoindol-1,3(2H)-dione; B: reacting the intermediate product shown in formula III with hydrogen and a catalyst Y to generate lurasidone, and reacting lurasidone with hydrochloric acid to generate lurasidone hydrochloride. The application avoids the use of a phase transfer catalyst, overcomes the defects of low separation yield, poor selectivity, low yield and high cost, and has great implementation value and social and economic benefits due to the following advantages: raw materials are easy to obtain, operation is simple, reaction conditions are mild, and waste is less.

The invention discloses a benzisothiazole compound as well as a pharmaceutical composition and application thereof, belongs to the technical field of medicines, and particularly relates to a 2H-benzotriazole substituted benzisothiazole compound with a novel structure as shown in a formula (I), a pharmaceutical composition containing the compound and application of the compound in preparation of medicines for treating and / or preventing premature ejaculation. Through in-vivo activity test research, the compound has obviously higher anti-premature ejaculation activity than the on-sale drug dapoxetine.

Provided are a lurasidone hydrochloride orally dissolving film composition, a preparation method and application thereof. The lurasidone hydrochloride orally dissolving film composition comprises an active drug, a film forming material, a plasticizer and a flavoring agent, and the active drug is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazole 3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylen-2H-isoindole-1,3-dione hydrochloride salt as shown in formula I. The obtained lurasidone hydrochloride orally dissolving film composition has a good dissolution rate, does not have a sand feeling after dissolving in the oral cavity, has a uniform appearance, good flexibility, and does not have sedimentation during the preparation of the film liquid, and the content uniformity meets the requirements.

The invention belongs to the technical field of medicines, and relates to application of an isothiazolo [5, 4-d] pyrimidine compound to treatment of inflammatory diseases, in particular to application of a compound shown as a formula (I) or pharmaceutically acceptable salt thereof to treatment of rheumatoid arthritis. The compound as shown in the formula (I) or the pharmaceutically acceptable salt or the pharmaceutical composition of the compound has a good treatment effect and also has good safety including but not limited to a low adverse reaction incidence rate.

The invention belongs to the technical field of pesticides, and particularly relates to an isothiazolone compound, a preparation method thereof, a bactericidal composition and application. The compound is shown as a general formula I, wherein R represents alkyl, alkenyl, alkynyl, naphthenic base, or alkyl, alkenyl or alkynyl substituted by at least one group selected from halogen, cyano, nitro, naphthenic base and other groups. The compound has good prevention and treatment activity on fungi, bacteria and the like.

The present application relates to the technical field of TLR2 antagonists, and particularly relates to a compound with a ketoxime ether structure and application thereof.The compound has a structure shown in formula I: or a pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R5 are independently selected from any one of a hydrogen atom, a phenolic hydroxyl group, an amino group, a halogen, a C1-C4 alkyl group, a C1-C4 alkoxy group, a C3-C5 cycloalkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group, an amide group, a sulfonamide group, an ester group, a cyano group, OCH2F, OCHF2, OCF3, SCF3 and N(CH3)2; 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 sulfonamide group, an alkyl group, an alkoxy group, an oxazole, an isoxazole, a thiazole, an isothiazole, an oxadiazole, a thiadiazole, a substituted oxazole, a substituted isoxazole, a substituted thiazole, a substituted isothiazole, a substituted oxadiazole and a substituted thiadiazole.The compound can be used as a TLR2 antagonist.