571 results about "Thiazine" patented technology

The present invention relates to novel heterocyclic pro-fragrances, preferably oxazolidines, tertahydro-1,3-oxazines, thiazolidines, or tetrahydro-1,3-thiazines, more preferably oxazolidines, or tertahydro-1,3-oxazines, most preferably oxazolidines, which are capable of sustained release of fragrance raw material ketones and aldehydes and to fragrance delivery systems which comprise said pro-fragrances.

Q is —N=or CR2 X is S, O or NOR3 Y is —O—, —S—, —SO— or —SO2—R and R1 are each, independently, H, a substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl groupR2 is H or a substituentR3 is H, or —C(O)R4 R4 is a substituted or unsubstituted aliphatic or aromatic groupn is an integer from 0 to 1Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine / threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001" / >(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

The present invention relates to heterocyclic compounds represented by the formula I or pharmaceutically acceptable salts thereof and antitumor agents containing the heterocyclic compounds as effective components:wherein X represents nitrogen atom or CH; R1 represents CHnF3-n (wherein n is 1 or 2), hydroxy C1–C6 alkyl, NHR6 [wherein R6 represents hydrogen atom or COR (wherein R represents hydrogen atom, C1–C6 alkyl or C1–C6 alkoxy)]; R2 represents morpholino (which may be substituted with one to four C1–C6 alkyl), thiomorpholino, piperidino, pyrrolidinyl (which may be substituted with hydroxy C1–C6 alkyl), oxazolidinyl (which may be substituted with one or two C1–C6 alkyl) or tetrahydro-1,4-thiazin-1-oxo-4-yl; R3 and R4 each represent hydrogen atom or C1–C6 alkyl; and R5 represents hydrogen atom, amino or hydroxyl.

The present invention relates to a phenothiazinium compound of Formula (I): wherein: A and B each independently is in which R' and R'' each independently is a linear, branched or cyclic hydrocarbon group, or R' and R'' together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where X<p-> is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either -N(CH3)2 or -N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells. The invention also relates to compositions comprising the compounds of Formula I, to selected compounds of Formula I, use of the compounds of Formula I as medicaments and as a PDT agent or a photodiagnostic agent, a conjugate or composite formed between a compound of Formula I and a polymer; and to a method for sterilising fluids in which the fluid is passed over the conjugate or composite whilst it is illuminated. The compounds are biologically active photosensitisers which are strongly photocytotoxic and have application in the areas of photodynamic therapy (PDT), as well as for the diagnosis and detection of medical conditions and related uses in photochemical internalisation, in the production of cancer vaccines, in the treatment and prevention of microbial infections and in photodisinfection or photosterilisation.

The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′-and / or 6′ halo and / or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.

The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and / or caused by the formation and / or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.

A method for using thiazine dyes, especially methylene blue or methylene blue derivatives, in an immediate or controlled release formulation, alone or in combination with low levels of light or other drugs, to selectively inactivate or inhibit hepatitis infection, has been developed. Clinical trial results demonstrate efficacy in a human clinical trial for treatment of hepatitis C by oral administration of methylene blue immediate release formulation, in a dosage of 65 mg twice daily, over a period of at least 100 days. A method for using thiazine dyes, especially methylene blue or methylene blue derivatives, in an immediate or controlled release formulation, along or in combination with low levels of light or other drugs, to prevent or decrease reactivation of viruses, is also described. The preferred class of patient is infected with, or has been exposed to, viruses such as Herpes simplex virus type 1 & 2, Varicella zoster virus, Epstein-Barr virus, Cytomegalovirus, and Herpes virus type 6 & 7, Adenovirus, and Human polyoma viruses, e.g. JC virus and BK virus. In one embodiment the thiazine dye is administered to a patient experiencing symptoms or disease caused by reactivation of a virus. In a preferred embodiment the thiazine dye is administered to a patient at risk for or experiencing symptoms or disease caused by reactivation of a virus, prior to or during immunosuppression or chemotherapy.

The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be useful as BACE inhibitors and / or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and uses, including Alzheimer's disease, are also disclosed.

The invention relates to a pesticide composition, in particular to an insecticide composition. The composition comprises chlorantraniliprole with synergistic effective dose, abamectin or emamectin benzoate, and one of cyhalothrin, dursban, diazinon, acetamiprid, cypermethrin, alpha cypermethrin, thiamethoxam, thiacloprid, fenvalerate, propargite, diafenthiuron, benfuracarb, azocyclotin, buprofezin, ethofenprox, phonamiphos, fipronil, flufenoxuron, monosultap, dimehypo, imidacloprid, flufenoxuron, chlorfluazuron, pleocidin and tebufenozide, wherein the mass percentage of the three compositions is that: the chlorantraniliprole is 1 to 35 percent, the abamectin or the emamectin benzoate is 1 to 10 percent, and any one of the insecticides is 1 to 50 percent. The invention discloses a process for processing the compositions and application of the compositions in preparing insecticides for controlling agricultural, forestry and gardening insect pests.

The invention relates to a method for production of an aqueous dispersion of polymer-encapsulated pigments, characterised in that (a) an aqueous pigment dispersion, containing at least one organic pigment (P), selected from the group of azo, isoindolinone, isoindoline, anthanthrone, thioindigo, thiazinindigo, triarylcarbonium, quinophthalone, anthraquinone, dioxazine, phthalocyanine, quinacridone, quinacridonquinone, indanthrone, perylene, perinone, pyranthrone, diketopyrrolopyrrole, isoviolanthrone and azomethine pigments, at least one detergent (T), and water is prepared, (b) a monomer miniemulsion, stabilised by a hydrophobic organic compound with a water solubility at 20 DEG C of at most 5x10<-5> g / l, is prepared from a polymerisable monomer (M) and at least one detergent (T) in water, (c) a monomer pigment emulsion is prepared, whereby the aqueous dispersion from (a) and the monomer miniemulsion from (b) are mixed and homogenised and (d) the pigment-containing monomer from (c) is polymerised in the presence of a polymerisation initiator and / or by heat, whereupon an encapsulation of the pigment with the polymer thus formed occurs.

The present invention provides the compounds inhibiting PDE 7 selectively, and therefore, enhances cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is imidazotirazinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl group, R2 is methyl group; R3 is a hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; substituted or unsubstituted C1-C6 alkyl group; substituted or unsubstituted C2-C6 alkenyl group; saturated or unsaturated heterocycloalkyl group which is substituted or unsubstituted; a group: —NR5R6, —C(O)R7, —SO2R7, —OR8, —NR8COR7, —NR8S02R7; A is CR4; and B is CH.

An object of the present invention is to provide a material for more easily and accurately detecting treatment status using gas exposure. The present invention relates to an ink composition for detecting an oxidizing gas, or the like, comprising at least one type of azo dye, methine dye, triarylmethane dye and thiazine dye.

The present invention relates to compounds according to Formula I:and salts thereof, wherein R1, R2, R3, R4, Ar, and n are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.

Disclosed herein are phenazine-3-one and phenothiazine-3-one derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging.

The present invention relates to methods and reagents for modifying the emission of light from labeled nucleic acids for the purpose of real time detection, analysis, and quantitation of nucleic acid sequences, e.g., using singly labeled probes. These methods and reagents exploit advantageous properties of thiazine dyes and diazine dyes. Furthermore, the use of these light emission modifiers in background reduction, nucleic acid duplex stabilization and other uses is also described. Related kits, reaction mixtures and integrated systems are described.

This invention relates to lubricating oil additives, and to lubricating oil compositions, their method of preparation, and use. More specifically, this invention relates to several novel lubricating oil additives and compositions which contain a tungsten compound and an antioxidant, namely aminic antioxidants such as a secondary diarylamine or an alkylated phenothiazine. The use of the tungsten compound with the secondary diarylamine and / or the alkylated phenothiazine provides improved oxidation and deposit control to lubricating oil compositions. The lubricating oil compositions of this invention are particularly useful as crankcase and transmission lubricants, gear oils and other high performance lubricant applications.

The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, and / or various fused ring systems with the benzene ring at the 4′,5′ or 5′,6′ positions.

An oxidative dye solution comprises an indicating dye that has been reacted with a reducing agent. The pre-reacted dye when subjected to an oxidizing disinfection or sterilization agent such as peracetic acid or hydrogen peroxide under goes a visible color change and thus can serve as a chemical, process, or chemical integrator, indicator. The dyes include various azines, thiazines, and oxazines compounds and the reducing agents include alkali metal alkyloxides and alkaline earth metal alkyloxide compounds.

The invention relates to a medicinal oral preparation containing Valsartan and Hydrochlorothiazide, more specifically the dispersible tablets for enhancing the beneficial effects of Valsartan and Hydrochlorothiazide.

An active insecticide for preventing and eliminating the agricultural pests, such as thrips, aphis, aleyrodid, leafhopper, plant hopper, rice borer, etc, is proportionally prepared from pymetrozine and other active components chosen from pyriproxyfen, methylamino abamectin benzoate and buprofezin.

The invention discloses a thermal activation delayed fluorescence material based on a dibenzophenazine derivative as well as a preparation method and application of the thermal activation delayed fluorescence material, and belongs to the technical field of organic photoelectric materials and devices. The structural formula of the material is shown as a formula (I), in the formula (I), R1 is phenoxazinyl, phenothiazinyl or dimethyl acridinyl, R1' is phenoxazinyl, phenothiazinyl or dimethyl acridinyl, R1 '' is phenoxazinyl, phenothiazinyl or dimethyl acridinyl, and R2 is H, phenoxazinyl, phenothiazinyl or dimethyl acridinyl. The material provided by the invention has the advantages that the electron acceptor and the electron donor unit show a highly distorted rigid structure, 100% theoretical internal quantum efficiency can be realized, the fluorescence quantum yield is high, a guarantee is provided for a high-efficiency long-waveband OLED device, and the like. And a polysubstitution mode is adopted, so that red shift of molecular emission wavelength is facilitated, long-waveband luminescence is realized, and a guarantee is provided for an efficient long-waveband OLED device.

Inhibition of RNA function, and treatment or control of diseases or conditions, e.g. infectious diseases such as viruses and viral infections (including HIV) and microbial infections, by the contacting of the RNA with a compound having a central or core structure comprising three fused rings containing from 12 to 15 ring atoms, the central ring including at least one heteroatom selected from nitrogen, oxygen and sulfur, the atoms of the three-ring core structure being optionally substituted with substituents such as halogens, cyano, and / or various substituted or unsubstituted aliphatic and / or heteroaliphatic moieties, or contacting the RNA with yohimbine, usnic acid or N-{4-[2,5-Dioxo-1-(4-trifluoromethoxy-phenyl)-pyrrolidin-3-yl]-phenyl}-2,2,2-trifluoro-acetamide. Preferred compounds are various phenothiazines, including both known and novel compounds.

This invention relates to an anti-infective compound, more specifically, 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1, 3] thiazine [3, 2-a] quinoline-3-carboxylic mesylate (compound I), its preparation method and its application. Compound I is prepared by reaction of 6-fluoro-1-methyl-4-oxo-7-(1-piperazine)-4H-[1,3]thiazine[3,2-a]quinoline-3-carboxylic acid and methyl sulfonic acid. Compound I can be used as effective component and mixed with normal pharmaceutical carrier to manufacture anti-infective drug composition, which can be tablets, capsules, granules, injection, eye preparations, ear preparations, gynecological preparations, and external use preparations. Compound I has stable properties, and can be easily dissolved in water, thus can be easily manufactured into various preparations used in clinical treatment. The method has such advantages as simple and reasonable process.

A conjugated polymer having a phenoxazine structure and a phenothiazine structure as subsituents.

Disclosed are 4H-1,4-Benzothiazine-2-carboxamides. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, depression, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

A scorch inhibitor composition for polyurethane foams is composed of(a) one or more derivatized phenolic compounds in an amount of about 60-80% by weight;(b) one or more aromatic amines in the form of a liquid in an amount of about 15-35% by weight;(c) an alkyl-substituted hydroquinone in an amount of about 4-8% by weight, and(d) phenothiazine at 0 to about 1.0% by weight.