83 results about "Thiopyran" patented technology

A member including for example, a supporting layer and a single photogenerating layer, the photogenerating layer comprising particles including hydroxygallium phthalocyanine phthalocyanine Type V, x polymorph metal free phthalocyanine, or chlorogallium phthalocyanine dispersed in a matrix comprising an arylamine hole transporter and an electron transporter selected from the group consisting of N,N'bis(1,2-dimethylpropyl)-1,4,5,8-naphthalenetetracarboxylic diimide, 1,1'-dioxo-2-(4-methylphenyl)-6-phenyl-4-(dicyanomethylidene)thiopyran, and a quinone selected from the group consisting of carboxybenzylhaphthaquinone, and tetra (t-butyl) diphenoquinone, and mixtures thereof, and a film forming binder.

A member including, for example, a supporting layer and a single photogenerating layer, the photogenerating layer comprising particles including hydroxygallium phthalocyanine phthalocyanine Type V, x polymorph metal free phthalocyanine, or chlorogallium phthalocyanine dispersed in a matrix comprising an arylamine hole transporter and an electron transporter selected from the group consisting of N,N'bis(1,2-dimethylpropyl)-1,4,5,8-naphthalenetetracarboxylic diimide, 1,1'-dioxo-2-(4-methylphenyl)-6-phenyl-4-(dicyanomethylidene)thiopyran, and a quinone selected from the group consisting of carboxybenzylhaphthaquinone, and tetra (t-butyl) diphenoquinone, and mixtures thereof, and submicrometer size polytetrafluroethylene particles, and a film forming binder.

The present invention relates to an improved process for the preparation of 5,6-dihydro-4-(S)-(ethylamino)-6-(S)methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide hydrochloride of formula (I) commonly known as Dorzolamide Hydrochloride useful as an agent to reduce intraoccular pressure by inhibiting carbonic anhydrase enzyme

The process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-sulfonamide-7,7-dioxides (I) wherein R₁ is H or C_1-5 alkyl, and R₂ is C_1-5 alkyl, starts from the corresponding 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-7,7-dioxides, and comprises protecting the alkylamine group, introducing a sulfonamide group and eliminating protecting group. Some compounds of formula (I) are inhibitors of the carbonic anhydrase and can be used in the treatment of elevated intraocular pressure

This invention includes an organophotoreceptor having an electrically conductive substrate and photoconductive element on the electrically conductive substrate, the photoconductive element having

a) a polymeric charge transport composition with the formula

• • where Y₁ and Y₂ are, each independently, a bond, a —CR₁═N—NR₂— group, or a —CR₃═N—N═CR₄— group;
  • R, R′, R″, R₁, R₂, R₃, and R₄ comprise, each independently, H, an alkyl group, an alkenyl group, a heterocyclic group, an aromatic group, or a part of a ring group;
  • X₁ and X₂ are, each independently, a linking group;
  • T₂ comprises a thiiranyl group, H, an alkyl group, an alkenyl group, or an aromatic group; Ar comprises an aromatic group; Z is a bridging group; and n is a distribution of integers between 1 and 100,000 with an average value at least 2; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging processes are also described.

The present invention is related to compounds comprising six-membered rings capable of being incorporated into nucleic acids. Particularly, the six-membered ring is a derivative of cyclohexane, cyclohexene, tetrahydropyran, tetrahydrothiopyran or piperidine. These compounds may be used to build up oligomeric compounds. The invention is further related to uses of these oligomeric compounds for hybridization and as probes. In addition, methods for the detection of nucleic acids are provided wherein the oligomeric compounds are used.

The invention discloses a chromogenic medium used for detecting escherichia coli O157:H7. The medium contains agar, peptone, a yeast extract, sodium chloride, sorbitol, inositol, neutral red, a beta-galactosidase chromogenic substrate I 5-bromo-4-chloro-3-indolyl-beta-galactose, a beta-galactosidase chromogenic substrate II o-nitrophenyl-beta-D-galactoside, isopropyl-beta-D-thiopyran galactoside, bile salt, potassium tellurite and cefixime. The chromogenic medium is used for detecting escherichia coli O157:H7, has high detection sensitivity and good specificity and can be used for directly identifying strains according to colors of bacterial colonies. The color of the target bacterial colony escherichia coli O157:H7 is different from that of the prior art, thus providing more choices for researchers.

There is provided a pharmaceutical drug, particularly a novel compound useful for prophylaxis or a therapeutic treatment of various diseases involving infections with viruses of the herpesvirus family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. An N-{2-[(4-substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative, of which phenyl group is substituted at position 4 with a specific 5- or 6-membered heteroaryl group, and a salt thereof have an effective anti-virus activity, and the oral administration thereof at a low dose enabled the therapeutic treatment of the above diseases.

The invention relates to a new synthetic method of a dorzolamide intermediate (S)-6-methyl-2-chlorosulfuryl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-4-carboxide, comprising the steps of synthesizing raceme 3-(thien-2-ylthio)butyric acid, performing chiral resolution to obtain stereoisomer thereof (S)-3-(thien-2-ylthio)butyric acid, and performing addition and ring-closing reactions to obtain (S)-6-methyl-2-chlorosulfuryl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-4-carboxide. The inventive method shortens conventional synthesis route, and performs chiral resolution of the intermediate raceme at the beginning of the synthesis route with a chiral resolution agent, so as to save a large amount of subsequent raw materials consumption. In addition, the synthetic method adopts 'one-pot' method, so as to reduce loss and the steps and cost of the subsequent operations, resulting in a more convenient, economical and effective synthesis route, compared with the known synthesis routes.

The present invention is directed to a functionalized elastomer comprising the reaction product of a living anionic elastomeric polymer and a polymerization terminator of formula I

where X is Cl, Br, or I;

m is an integer from 0 to 2, n is an integer from 1 to 3, with the proviso that n+m=3;

R¹, R² are independently C1 to C18 alkyl, aryl, or a combination thereof, or R¹, R² are independently —SiR₃ where R is independently alkyl, aryl, alkoxy, or disubstituted amino, or R¹ and R² taken together with their common nitrogen atom and optionally a sulfur or oxygen heteroatom to form a five to eight membered ring;

R³ is hydrogen, or C1 to C18 alkyl, aryl, or a combination thereof, or R³ is —SiR₃ where R is independently alkyl, aryl, alkoxy, or disubstituted amino, or R³ is —R⁶—R⁷, where R⁶ is C1 to C3 alkanediyl and R⁷ is selected from the following structures

—S—Z, —N(R⁸)(R⁹), —O(Y), or Si(OR¹⁰)₃, where R⁸ and R⁹ are independently C1 to C18 alkyl, aryl, or a combination thereof,

Y and Z are independently selected from the group consisting of methoxymethyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrofuranyl, tert-butyl, allyl, 1-ethoxyethyl, benzyl, triphenylmethyl, triethylsilyl, triisopropylsilyl, trimethylsilyl, tert-butyl dimethyl silyl, tert-butyl diphenyl silyl, and isopropyldimethylsilyl, and

R¹⁰ are independently C1 to C4 alkyl;

or when m=1, the polymerization terminator may have the formula II

where R⁴, R⁵ are independently C1 to C18 alkyl, aryl, or a combination thereof, or R⁴, R⁵ are independently —SiR₃ where R is independently alkyl, aryl, alkoxy, or disubstituted amino, X and R³ are as defined previously, and k is an integer from 0 to 10.

The invention relates to 2,3,4,5-tetrahydro-4H-benzo[b]thiopyrano[4,3,c]pyrazole-2-formamide derivatives and a preparation method thereof. The structural formula of the compounds is shown in the specifications. The invention also relates to pharmaceutically acceptable salts of the derivatives and medicines taking the derivatives and the salts thereof as active ingredients. The structure of the derivates is obtained according to an association principle in pharmaceutical chemistry; and the inventor has systematically and comprehensively studied the compounds, modified and transformed a plurality of sites in the structure, and tested the in-vitro antifungal activity of the compounds by a double dilution method. Serving as novel antifungal agents, the compounds have higher killing effect on clinically common pathogenic fungi, and can overcome the defects of large toxic and side effect, high possibility of generating tolerance and the like of the clinically widely used azole antifungal medicines at present.

The invention discloses a near-infrared II thiapyran salt fluorescent compound capable of targeting mitochondria, a preparation method and application thereof. According to the invention, a thiapyransalt heterocyclic structure is modified, different modification groups are introduced, and the emission wavelength of the thiapyran salt heterocyclic structure can be redshifted to a near-infrared IIregion (1000-1200 nm); the compound has good light stability, is easy for post-modification, can be connected with different biomarkers (polypeptide, antibody, PEG, folic acid and the like) through chemical bonding, improves the water solubility and targeting property, reduces the biotoxicity, and improves the bioavailability; and the compound can be used for mitochondrial imaging, drug efficacy evaluation, solid tumor imaging for breast cancer, osteosarcoma, glioma and other solid tumors, and vascular imaging, can also be used for surgical navigation, early diagnosis of diseases, intraoperative real-time monitoring, photothermal therapy, photodynamic therapy and other biological applications, and has good industrial production values and biomedical application prospects.

The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I)

wherein X=CH₂, N—R⁷, S or O, R¹, R² and R³ are certain specific substituents, with the proviso that at least one of R¹ and R² is an amino radical of formula N—R¹⁰R¹¹ wherein R¹⁰ and R¹¹ are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R³ represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonin (5-HT) reuptake inhibitor activity in combination with additional α₂-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention are also suitable for treating depression, anxiety and body weight disorders. The invention also relates to novel combination of substituted amino isoxazoline derivatives according to the invention with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action.

The invention belongs to the field of the pharmaceutical chemistry and pharmacology, and concretely relates to an application of a compound of [(1Z,1'Z)-(4-Oxo-2H-1-thiopyran-3,5(4H,6H)-diylidene)bis(methanylylidene)]bis(2-methoxy-4,1-phenylene)bis(2-methylpropanoate) (S5) in the preparation of anti-inflammation or/and anti-oxidation drugs. The above thiapyrone type curcumin analog S5 can dose-dependently inhibit the expression and release of inflammation factors comprising TNF-alpha, IL-6 and the like, and can also obviously improve the survival rate of mice death-induced by LPS. The compound has a good safety and stability, and can be exploited to inflammation or/and oxidation stress related disease treatment drugs.

The invention discloses a chiral benzodihydrothiapyran-4-one compound and a preparation method and application thereof. The preparation method comprises the following steps of: dispersing 4H-benzothiapyran-4-one with different substituent groups, 2-vinylpyridine, a photosensitizer DPZ, a reducing agent Hanus ester HE and a chiral phosphoric acid catalyst BA in an organic solvent, degassing the solution at the temperature not higher than -78 DEG C, placing the solution at the temperature of (-15)-(-35) DEG C, irradiating by using a 3-10W blue lamp, reacting for 60-80 hours, and after the reaction is finished, separating and purifying to obtain the (R)-2-(2-(2'-pyridine) ethyl) benzodihydrothiapyran-4-one and derivatives thereof. The yield of the obtained target product is medium or above, the reaction does not need heavy metals, and the product is green and pollution-free.

The invention belongs to the technical field of medicines, and relates to a 4H-thieno[2,3-b]thiapyran-4-ketone compound, a preparation method thereof and application thereof as an epidermal growth factor receptor tyrosine kinase inhibitor. The compound, a prodrug thereof, a pharmaceutically active metabolite thereof and a pharmaceutically acceptable salt thereof have structural formula as shown inthe specification, wherein R is independently selected from hydrogen, halogen, hydroxy, nitro, cyan, C1-C4 alkyl, C1-C4 alkoxy, halogen atoms substituted C1-C4 alkyl, and halogen atoms substituted C1-C4 alkoxy. The formula is shown in the description.

The present invention is directed to a functionalized elastomer comprising the reaction product of a living anionic elastomeric polymer and a polymerization terminator of formula I

where X is Cl, Br, or I;

m is an integer from 0 to 2, n is an integer from 1 to 3, with the proviso that n+m=3;

R¹, R² are independently C1 to C18 alkyl, aryl, or a combination thereof, or R¹, R² are independently —SiR₃ where R is independently alkyl, aryl, alkoxy, or disubstituted amino, or R¹ and R² taken together with their common nitrogen atom and optionally a sulfur or oxygen heteroatom to form a five to eight membered ring;

R³ is hydrogen, or C1 to C18 alkyl, aryl, or a combination thereof, or R³ is —SiR₃ where R is independently alkyl, aryl, alkoxy, or disubstituted amino, or R³ is —R⁶—R⁷, where R⁶ is C1 to C3 alkanediyl and R⁷ is selected from the following structures

—S—Z, —N(R⁸)(R⁹), —O(Y), or Si(OR¹⁰)₃, where R⁸ and R⁹ are independently C1 to C18 alkyl, aryl, or a combination thereof,

Y and Z are independently selected from the group consisting of methoxymethyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrofuranyl, tert-butyl, allyl, 1-ethoxyethyl, benzyl, triphenylmethyl, triethylsilyl, triisopropylsilyl, trimethylsilyl, tert-butyl dimethyl silyl, tert-butyl diphenyl silyl, and isopropyldimethylsilyl, and

R¹⁰ are independently C1 to C4 alkyl;

or when m=1, the polymerization terminator may have the formula II

where R⁴, R⁵ are independently C1 to C18 alkyl, aryl, or a combination thereof, or R⁴, R⁵ are independently —SiR₃ where R is independently alkyl, aryl, alkoxy, or disubstituted amino, X and R³ are as defined previously, and k is an integer from 0 to 10.

The invention relates to a novel benzothiapyran diketone compound as well as a preparation method and application thereof. The compound is 8-methyl benzothiapyran diketone, 8-ethyl benzothiapyran diketone, 10-methyl benzothiapyran diketone and 7,9-dimethyl benzothiapyran diketone. The invention discloses a method for synthesizing a series of benzothiapyran diketone compounds by taking thiophenol as an initial raw material for the first time, in-vitro anti-tumor activity experiments are carried out on the benzothiapyran diketone compounds, and results show that the compounds have an obvious inhibition effect on human cervical cancer cells (Hela), human liver cancer cells (SMMC-7721), human lung cancer cells (A549) and human breast cancer cells (MCF77); and the potential value is realized inthe aspects of anti-tumor medicine development and application.

The invention discloses a thiapyran[4,3-b] indole compound and a preparing method and application thereof. The structure of the compound is shown in the formula 1, wherein the formula 1 is shown in the description, and R1-R5 are not all hydrogen. The compound has excellent activities of inhibiting mycelial growth, protecting detached leaves, protecting living bodies and treating the living bodiesfor rhizoctonia solani, the effects of the compound are even superior to those of positive control drugs, and the compound has an important application value in preventing and/or treating rice sheathblight.

The invention discloses a chromogenic medium used for detecting escherichia coli O157:H7 and other intestinal floras. The medium contains agar, peptone, a yeast extract, sodium chloride, sorbitol, inositol, neutral red, a beta-galactosidase chromogenic substrate, 4-methyl sector ketone-beta-D-glucuronide, isopropyl-beta-D-thiopyran galactoside, bile salt, potassium tellurite and cefixime. The chromogenic medium disclosed by the invention can be used for identifying escherichia coli O157:H7 in coliforms rapidly, simply and conveniently.