86 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

A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.

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 C1-5 alkyl, and R2 is C1-5 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

The invention relates to a preparation method of 5,6-dihydro-6-methylthieno(2,3-b) thiopyran-2-sulfamide-4-ketone, which is characterized by comprising the following processing steps of: adding 0.125 mol of thiophene and 150 milliliter of tetrahydrofuran in a four-hole flask, and cooling down to -20 DEG C; dropwise adding 63 milliliter of 2 mol / liter butyl lithium pentane solution, and adding 0.125 mol of sulfur and 0.125 mol of (R)-beta-butyrolactone; when heating to room temperature, adding 0.125 mol of trifluoro acetic anhydride, and carrying out mechanical intense stirring; after the completion of reaction, slowly adding the mixture in a flask containing 0.166 mol of chlorosulfonic acid at the temperature of 0 DEG C; and heating the obtained dark solution to 50 DEG C, keeping for 12 hours, then cooling to 20 DEG C, adding thionyl chloride and strong ammonia, stirring and diluting at the temperature of 0 DEG C, and drying to obtain target products. The preparation method has the advantages of stable reaction, stronger antimicrobial bactericidal effects of the target products than those of common antimicrobial drugs, easy enlarging production and no pollution in the production process.

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 invention belongs to the technical field of medicines and relates to a thienothio compound and an application thereof. A thienothiapyran compound comprises derivatives and pharmaceutically applicable salt of the thienothiapyran compound, and has a structural formula; the thienothiapyran compound and the pharmaceutically applicable acid addition salt of the thienothiapyran compound can be combined with conventional drugs or are individually used as epidermal growth factor tyrosine kinase inhibitors for treating related diseases of epidermal growth factor receptor signaling dysregulation, such as small cell lung cancers, squama cancers, glandular cancers, large cell cancers, colorectal cancers, breast cancers, ovarian cancers, renal cell cancers and bronchial asthma.

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 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

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 Iwhere 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, andR10 are independently C1 to C4 alkyl;or when m=1, the polymerization terminator may have the formula IIwhere 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 belongs to the technical field of medicine and relates to a 1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and application thereof used as an estrogen receptor, in particular to a 1,4-dihydrobithiophene [3', 2': 5, 6] bithiapyran [4, 3-c] pyrazol-3-carboxylic acid derivative and a pharmaceutically acceptable salt, or a stereoisomer thereof and a prodrug as well as a pharmaceutically acceptable vector in compatibility or a diluent used as an estrogen receptor. The structural general formula of the derivative is disclosed in the specification, and in the structural formula, n R1 can be independently selected from a substituted or unsubstituted amido group, and R2 can be independently selected from H or an acetyl group. The derivative can be used for treating and preventing various diseases related to estrogen functions, such as diseases related to estrogen deficiency, estrogen sensitive cancer and hyperplasia, endometriosis, uterus myoma and osteoarthritis. Compounds or compositions of the derivative can also be independently used or combined with progestogen or a hormoneantagonist as a contraceptive.

The invention discloses a liquid crystal compound containing a tetrahydro-thiopyran group and a preparation method thereof and a liquid crystal composition. The liquid crystal compound is represented by a general formula I. The liquid crystal composition comprises no more than 40% but more than 0 of the compound as represented by the general formula I, 4 to 50% of a compound as represented by a general formula II, 5 to 50% of a compound as represented by a general formula III and 3 to 45% of a compound as represented by a general formula IV. The liquid crystal compound provided by the invention has low rotary viscosity gamma 1, great dielectric anisotropy, a wide nematic phase temperature range, good intermiscibility, light stability and thermal stability and is fairly applicable as a liquid crystal monomer; the liquid crystal composition containing the liquid crystal compound has a great liquid crystalline phase temperature range, appropriate optical anisotropy, small rotary viscosity and low starting voltage and is especially applicable to liquid crystal display elements of a TN mode, a VA mode, an IPS mode and a PDLC mode.

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 Iwhere 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, andR10 are independently C1 to C4 alkyl;or when m=1, the polymerization terminator may have the formula IIwhere 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 provides a nAChR-alpha1-ECD protein which is characterized in that the amino acid series is SEQ ID 1, wherein the molecular weight of the protein is 28.7kDa and the isoelectric point is 6.0. Moreover, the invention also provides a preparation method of the protein. The method comprises the following steps: S1, performing in vitro synthesis of a cDNA sequence SEQ ID2 corresponding to a SEQ ID 1 amino acid sequence; S2, inserting the SEQ ID 2 sequence into an expression vector pCold II, wherein the insertion site is Nde I / Hind III; S3, converting pCold II-AChR-alpha1-ECD plasmids obtained in the S2 into BL21(DE3) competent cells, performing overnight culture with a panel with penbritin, selecting a monoclonal colony and performing an expression lab-scale test by inductive amplification of isopropyl-beta-D-thiopyran galactoside (IPTG) to obtain an escherichia coli strain expressed by AChR-alpha1-ECD BL21(DE3); S4, performing amplified fermentation on the escherichia coli strain expressed by AChR-alpha1-ECD BL21(DE3); and S5, splitting the Escherichia coli thalli to obtain an inclusion body solution, and performing follow-up separating, purifying and renaturating steps.

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.