38 results about "Isothiazole" patented technology

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.

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 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.

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 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 invention relates to a fungicidal composition comprising: (a) pydiflumetofen; and (b) a combination of biocides comprising: i. 2-bromo-2-nitro-1,3-propanediol; ii. 1,2-benzisothiazol-3(2H)-one; and iii. a mixture of 5-chloro-2-methyl-1,2-thiazol-3-one and 2-methyl-1,2-thiazol-3- one. The present invention further relates to the use of the fungicidal composition for the control of phytopathogenic diseases on useful plants.

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.

This disclosure discloses a method for preparing 2,5-furandicarboxylic acid (FDCA) compounds. The method includes providing a hexose diacid compound, an acid catalyst, and an ionic liquid; and dehydrating the hexose diacid compound in the ionic liquid under the catalysis of the acid catalyst to form a 2,5-furandicarboxylic acid compound; wherein the ionic liquid comprises a cationic moiety selected from pyridinium, pyridazinium, pyrimidinium, pyrazinium, oxazinium, thiazinium, imidazoline, pyrazolium, thiazoline, isothiazinium, oxazolium, isoxazolium, or triazolium and an anionic moiety selected from halide anions.

This invention relates to a method for preparing 2,5-furandicarboxylic acid compounds. The method includes: providing a hexose diacid compound, an acid catalyst, and an ionic liquid; and dehydrating the hexose diacid compound in the ionic liquid under the catalysis of the acid catalyst to form the 2,5-furandicarboxylic acid compound. The ionic liquid comprises a cationic moiety selected from pyridinium, pyridazinium, pyrimidinium, pyrazinium, oxazinium, thiazinium, imidazoline, pyrazolium, thiazoline, isothiazinium, oxazolium, isoxazolium, or triazolium, and an anionic moiety selected from halide anions. The acid catalyst comprises trifluoromethanesulfonic acid. The general structural formula of the hexose diacid compound is R1OOC(CHOH)4COOR2, and the structure of the 2,5-furandicarboxylic acid compound is shown in formula (I). This method offers mild reaction conditions; good FDCA selectivity and high yield; high product purity; simple operation; and low pollution.

A water-based rolling liquid suitable for a thread rolling machine and a preparation method thereof, the water-based rolling liquid is composed of water, diethyleneglycol amine, triethanolamine, triethanolamine borate, 2-amino-2-methyl-1-propanol, 2-methyl-2-methylamino-1-propanol, ethylenediaminetetraacetic acid disodium, 2,4,6-tris(aminohexanoic acid)-1,3,5-triazine, 2-methyl-3(2H)-isothiazolinone, 1,2-benzisothiazolyl-3(2H)-ketone, polydichloroethyl ether tetramethyl ethylenediamine, polyoxyethylene polyoxypropylene, and polyalkylene glycol monobutyl ether, the water-based rolling liquid is a water-based lubricating coolant, can be used by diluting two to ten times, saves transportation cost, can better complete heat dissipation work due to the specific heat of water being greater than that of oil, and does not volatilize aromatic organic gas during use, does not generate oil mist, reduces safety hazards, and additionally adds various amines to increase biological stability. The application also provides a preparation method of the water-based rolling liquid.

The invention relates to the technical field of fine chemical engineering, and discloses a method for synthesizing 2-butylbenzo [d] isothiazole-3 (2H)-ketone through ring shrinkage reaction. The preparation method comprises the following specific steps: by taking 4H-benzo [d] [1, 3] oxathiacyclohexadiene-4-ketone and n-butylamine as raw materials and sodium phosphate and sodium dihydrogen phosphate as key additives, carrying out one-step reaction in a mixed solvent of tetrahydrofuran and water, and purifying to obtain the target product 2-butylbenzo [d] isothiazole-3 (2H)-ketone. The method is simple and convenient to operate and high in yield, 4H-benzo [d] [1, 3] oxathiacyclohexadiene-4-ketone is converted into the 2-butylbenzo [d] isothiazole-3 (2H)-ketone compound in one step, and potential application value is achieved.

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.

Disclosed are a gastroretentive double-layer sustained-release tablet, a preparation method therefor, and use thereof. An active ingredient of the gastroretentive double-layer sustained-release tablet is 3-[4-[4-(lH-benzotriazol-1-yl)butyl]piperazin-1-yl]benzisothiazole hydrochloride. Said tablet consists of two drug release layers comprising an immediate-release layer and a sustained-release layer. The immediate-release layer comprises the active ingredient, a filler I, and a disintegrant, and the sustained-release layer comprises the active ingredient, a filler II, a swelling material, a release blocker, a swelling enhancer, and a stabilizer. Said tablet can prolong the in vivo absorption window of the drug, maintain the plasma concentration, and prolong the in vivo half-life of the active ingredient.

The present disclosure relates to a perovskite solar cell, a preparation method thereof and a laminated battery, the perovskite solar cell comprising, in sequence, a bottom electrode, a hole transport layer, a perovskite absorption layer, an optional first passivation layer, a second passivation layer, an electron transport layer and a counter electrode; wherein the first passivation layer contains an organic amine passivation agent, and the second passivation layer contains a benzothiazole derivative and / or a benzoisothiazole derivative. The perovskite solar cell of the present disclosure has a higher short-circuit current and fill factor, and a higher photoelectric conversion efficiency.

The present invention relates to a method of laundering fabrics in a washing machine, the method comprising adding a laundry detergent composition and a laundry additive composition to a wash tank. In the method, the temperature of the wash liquor is above 15°C and below 40°C; 0.5g to 20g of the laundry additive composition is added to the wash tank per litre of wash liquor; and the total wash time is 60 minutes or less. The laundry additive composition comprises, based on the total weight of the additive composition: 20wt% to 60wt% of at least one bleach, 0.1wt% to 20wt% of at least one bleach activator, and 0.001wt% to 2wt% of 3-methyl-1,2-benzisothiazol-1,1-dioxide.