213 results about "Aza Compounds" patented technology

This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and / or pestivirus, comprising administering to that host an effective amount of an anti-flavivirus or anti-pestivirus, biologically active compound has a 5-aza-7-deazapurine moiety. The 5-aza-7-deazapurine moiety may be substituted or unsubstituted, and may comprise a nucleoside analogue, or a salt or prodrug thereof. The compound of the present invention may be administered alone or in combination with another anti-hepatitis C, anti-flavivirus and / or anti-pestivirus agent.

The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

The present invention provides pharmaceutical formulations of cytidine analogs and derivatives, such as 5-azacytidine, 5-aza-2′-deoxy-2′,2′-difluorocytidine, 5-aza-2′-deoxy-2′-fluorocytidine, 2′-deoxy-2′,2′-difluorocytidine, and cytosine 1-β-D-arabinofuranoside, as well as methods of manufacturing the formulations. In particular, the cytidine analog or derivative is formulated with a cyclodextrin compound to stabilize and / or enhance solubility of the drug. Kits and methods for using the pharmaceutical formulations are also provided, including methods of administering the cytidine analog or derivative to treat conditions or diseases, such as cancer and hematological disorders.

A method of treating a patient suffering from pancreatitis comprising treating said patient with a therapeutically effective amount of a cholinergic agonist selective for an α7 nicotinic receptor in an amount sufficient to decrease the amount of the proinflammatory cytokine that is released from a macrophage wherein said condition is acute pancreatitis. The compounds of the present invention include a quaternary analog of cocaine; (1-aza-bicyclo[2.2.2]oct-3-yl)-carbamic acid 1-(2-fluorophenyl)-ethyl ester; a compound of formula (I), a compound of formula (II), a compound of formula (III), a compound of formula (IV), and an oligonucleotide or mimetic capable of attenuating the symptoms of acute pancreatitis wherein the oligonucleotide or mimetic consists essentially of a sequence greater than 5 nucleotides long that is complementary to an mRNA of an α7 cholinergic receptor. The variables of formulae (I), (II), (III) and (IV) are described herein

Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2′-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.

The invention provides a compound of the formula:wherein A is selected from N, CH and CR; R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH2, NHR1, NR1R2 and SR3; R1, R2 and R3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from NH2 and NHR4; R4 is an optionally substituted alkyl, aralkyl or aryl group; X is selected from H, OH and halogen; Z is selected from H, Q, SQ and OQ; Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer, a pharmaceutically acceptable salt, an ester, or a prodrug thereof; with the proviso that the stereochemistry of the aza-sugar moiety is D-ribo or 2′-deoxy-D-erythro-; pharmaceutical compositions comprising said compound; and methods of treatment using said compound.

Aza-quinolinol phosphonate compounds and methods for inhibition of HIV-integrase are disclosed. Formula (I). Ar is aryl or heteroaryl connecting R6 to L. L is a bond or a linker connecting a ring atom of Ar to N. The ring atoms, X1-X5 may be N, substituted nitrogen, or substituted carbon, and form rings. The compounds include at least one phosphonate group covalently attached at any site.

The present invention relates to a process for the preparation of Dutasteride, which is chemically known as 17β-N-[2,5-bis (trifluoromethyl) phenyl] carbamoyl-4-aza-5-α-androst-1-en-3-one and can be represented by Formula (I).

The instant invention provides for compounds which comprise benzoisoquinolinones and aza derivatives that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.

The present invention provides substituted aza compounds of formula (I) or (II) and pharmaceutically acceptable salts thereof, and their use to inhibit IRAK-4 and / or for the treatment of diseases or disorders induced by IRAK-4.

A stable composition of a 2-aza-bicyclo[3.3.0]-octane-3-carboxylic acid derivative and a method for its preparation are described. The stable composition includes an intimate admixture of the derivative and a stabilizing effective amount of a lubricant. The stable composition further includes an external excipient. A method of preparing the stable composition includes forming an intimate admixture of the derivative and a lubricant and then blending the intimate admixture with at least one excipient. Preferably the final blend is transformed into solid unit dosage form.

The invention relates to a method for preparing aza graphene and nanometer metal graphene by using a solid phase cracking technology, wherein a phthalocyanine compound, a phthalocyanine polymer and a derivative thereof are adopted as starting raw materials, and cracking is performed at a temperature of more than 700 DEG C under an atmosphere of high purity nitrogen gas, argon gas or argon / hydrogen mixed gas to obtain the nitrogen-containing graphene and nanometer metal graphene materials. The method is characterized in that 1, the method is simple, and the aza graphene and nanometer metal graphene materials can be obtained through one-time solid phase cracking; 2, the graphene materials can be obtained through cracking in a non-hydrogen environment; 3, with adjustment on the cracking temperature, the gas flow rate and other experiment parameters, the size, the thickness and the quality of the graphene materials can be effectively controlled; and 4, the graphene materials with the coil behavior can be obtained under the catalyst effect. The prepared graphene materials can be applied in the fields of single molecule detection technologies, field-effect transistors and integrated circuits thereof, transparent conductive electrodes, conductive inks, field emission sources and vacuum electron devices thereof, supercapacitors, biological devices and the like.

The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.

The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1)or a salt thereof,wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl;R2 and R3 may be linked to form lower alkylene;A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo;Y1 and Y2 are each independently —N═ or —CH═;andR5 is group represented bywherein R6 and R7 are each independently hydrogen or organic group;R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—;XA and XB are each independently a bond, lower alkylene, etc.

The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula Ihaving BACE1 and / or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and / or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

The invention belongs to the technical field of organic photoelectric material application, and particularly relates to di-aza-carbazole derivatives and application thereof. The derivatives are obtained by bonding di-aza-carbazole serving as a core to different aromatic cyclic compounds. Efficient compounding of current carriers in an organic electroluminescence device can be realized radically by adjusting the bonding amount and the bonding positions of di-aza-carbazole, and adjusting the energy level structure and the current carrier transmission capability of the derivatives, so as to obtain an efficient and energy-saving OLED device.

The invention relates to azabenzofuranyl compounds of Formula I with anti-cancer and / or anti-inflammatory activity and more specifically to azabenzofuranyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

The invention discloses a near-infrared chlorinated aza-boron fluoride dye. In a preparation process of the dye, a chlorine substituted basic aza-boron fluoride framework is finally prepared by a multi-step reaction such as a synthesis-addition reaction-cyclic reaction-coordination substitution reaction of ketene. The dye has stronger absorption and emission in a near-infrared wavelength area; a photo-thermal property and chemical stability are improved; and the dye can be used for the fields of photodynamic treatment and photo-thermal treatment under guidance of photo-thermal imaging and photoacoustic imaging, bio-labeling and detection, a time gate imaging technology and the like.

The invention discloses a preparing method of two aza naphthalene biphenyl type sulfonated polyarylether nitrile ion conductive film material, which comprises the following steps: incorporating structural element of formula 1; passing two aza naphthalene ketone biphenyl bis-phenol, dihalogen (or two nitro group) cyanobenzene, 3, 3'-two petroleum sulfonate-4, 4'- aromatic dihalogen (or two nitro group) and aromatic dihalogen (or two nitro group) as monomer; choosing alkali or salt of alkali metal or alkali earth metal; getting the product in non-proton polar solvent through high-heat copolymerization reaction; wherein R1, R2, R3, R4 maybe alkyl group, alkoxy, phenyl group, halogen atom or hydrogen atom. This invention possesses good tenacity, dig intensity, low swelling ratio, which can be used to fuel battery or energy-storage battery or film separating technology domain.

The invention relates to a method for generating beta-aminoketone, ester, nitrile and amide derivatives by performing aza-Michael addition on amine substances and electron-deficient alkenes through an efficient environment-friendly catalyst under solvent-free mild (room temperature) reaction conditions. The method comprises the steps of taking ionic liquid as the catalyst, subjecting amine substances and electron-deficient alkenes to aza-Michael addition at room temperature under normal pressure and obtaining corresponding beta-aminoketone, ester, nitrile and amide derivatives. The ionic liquid is repeatedly used five times, and reaction yield does not obviously drop. The method has the advantages of simple operation, high yield, good using repeatability of the catalytic reaction system, mild reaction conditions and good prospects for industrialization.

The invention relates to a bis-nitrogen heterocyclic carbene bis-palladium complex and a preparation method thereof, which belong to the bis-palladium complex and a preparation method thereof. The preparation method is as follows: according to the molar ratio of 1:2.05:20, bis-imidazolium chloride salt, palladium chloride, and potassium carbonate are added into a round-bottomed flask, a condenser is added to the mouth of the flask, and an inversion plug is added to the condenser. Connect it to a double-row tube vacuum line connected with argon; react at 85°C for 18h; Wash the diatomaceous earth until no yellow liquid flows down, and collect the filtrate; use a rotary evaporator to remove dichloromethane in the collected filtrate, and remove pyridine in the collected filtrate to obtain a yellow crude product; recrystallize with dichloromethane / ether to obtain a light yellow solid , that is, the bis-palladium complex of the diazoheterocyclic carbene is obtained. The synthesis step of the invention is simple, the yield is high, and it is convenient to realize industrialization.

The invention describes crown ether chelators, including crown ethers having the formulaand aza-substituted and thia-substituted analogs thereof. These crown ethers may be substituted by a dye moiety, a chemically reactive group, a conjugated substance, or a combination thereof. Chelators that are substituted by fluorescent dyes are particularly useful as indicators for metal cations, particularly Na+ and K+ ions, and particularly where binding of the target ion results in a change in the fluorescence properties of the indicator that can be correlated with the ion concentration. Methods are provided for utilizing reactive groups on the chelators for conjugation to dyes, lipids and polymers and methods for enhancing entry of the indicators into living cells.

The invention relates to a synthetic method of a dicyclic azacyclo fluorescence or phosphorescent compounds: a metal carbene compound with a dicyclic azacyclo structure skeleton is produced from a carbene compound and 2-pyrazoline-5-ketone through a cycloaddition reaction in an organic solvent, and cis- and trans- dicyclic azacyclo organic compounds are respectively prepared after oxidation and demetalization; wherein, the cis-dicyclic azacyclo compounds have strong fluorescence performance, which can be uses as a small molecule probe compound for the analysis and checking of protein and cell; trans-dicyclic azacyclo compound is a non-fluorescent compound and may has phosphorescence; the oxidant used is inorganic or organic oxidant, and the reaction solvent is polar or non-polar organic solvent. The invention is of simple operation, with material easy to be acquired, a few reaction steps, better efficiency and selectiveness than traditional method; in particularly, compared with traditional synthesis method, the invention can more easily synthesize asymmetrical dicyclic azocyclo bimane compound.

Heteroaryl pyridone and aza-pyridone amide compounds of Formula I are provided, and various substituents including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

A storage stable, efficacious pesticide formulation is provided that is dilutable by the user and contains azadirachtin (AZA) and a pyrethrin or pyrethroid (PYR), and optionally an aprotic solvent and non-ionic, substantially water-free emulsifier. A sufficient amount of the PYR is provided to complex with the AZA A on opposite sides of the molecular structure thereof, thereby preventing rearrangement of the AZA A molecule in the presence of moisture that would result in hydrolysis and decomposition of AZA A. The AZA-PYR combination is sufficiently chemically stable such that less than 10% of the AZA A is decomposed when the formulation is subjected to an accelerated aging test for 30 days at 40° C. in a sealed container. The molar ratio of PYR to AZA A is preferably within the range of 0.5 / 1-10.5 / 1, more preferably within the range of 1.5 / 1-7 / 1, and most preferably with the range of 3 / 1-6 / 1. A solvent, when provided, should be in the range of about 70% to about 90% by weight based on the weight of the formulation, and the emulsifier should be within the range of about 0% to about 20%.

The invention relates to an aza-fluorine organic semiconductor material and preparation and application methods thereof, belonging to the organic photoelectric material scientific field, in particular to the aza-fluorine organic semiconductor material and the preparation method. And the material is applied to organic electronic fields of organic light emitting display, fluorescence sensing, flash memory devices, solar cells, and etc. With the structure shown above, the material has the advantages that: (1) the aza-fluorine has special electron acceptor electronic structure and opto-electrical properties; (2) the material can interact or react with metal mutually and can be applied to the sensing field; (3) synthetic route is simple, etc.

The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.

The invention discloses a trifluoromethylselenolation method of electron-rich arene or aza-arene. The method comprises the following steps: adding trifluoromethylseleno ammonium salt or metal salt andan oxidizing agent into a solvent; adding electron-rich arene or aza-arene at -80 to 100 DEG C; stirring and reacting for 0.1-48h; adding water for quenching; performing column chromatography to obtain a trifluoromethylselenolation product. By adopting trifluoromethylseleno ammonium salt or metal salt as a trifluoromethylseleno source, the invention proposes a new trifluoromethylselenolation method of electron-rich arene or aza-arene, wherein oxidation trifluoromethylselenolation of electron-rich arene or aza-arene is realized in quite mild conditions, and a C-SeCF3 bond is directly constructed from aC-H bond; the method has the advantages of easiness in operation, mild conditions, relatively high yield, perfect tolerance of functional group and cheap and easily available raw materials.

The invention belongs to the technical field of organic photoelectric materials and in particular relates to an aza aromatic compound used as a blue fluorescent material and application. The inventionprovides a series of the aza aromatic compound, which is used as a novel core structure of a fluorescent material, to prepare the sky-blue fluorescent material; the organic compound provided by the invention not only has high luminous efficiency, but also can finely adjust the wavelength of emitted light through positions of a substituent group and a heteroatom; the material can be applied to organic electroluminescence devices.