39 results about "Adenine derivatives" patented technology

The invention relates to a phosphonate prodrug of an adenine derivative and medical application of the phosphonate prodrug. Specifically, the invention relates to a compound shown in a general formula (I) or an optical isomer, or a pharmaceutical salt, or a hydrate or a solvate of the compound, and application of the compound or the optical isomer, or the pharmaceutical salt, or the hydrate or the solvate of the compound to preparation of medicines for curing virus infective diseases, especially hepatitis B (HBV) and acquired immune deficiency syndrome (HIV), wherein the definitions of all substituents in the general formula (I) are the same as the definitions in the specification.

The present invention provides N⁶-substituted adenosine derivatives and N⁶-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.

Compounds of formula (I):

wherein R¹ is C_1-6alkylamino, or C_1-6alkoxy; R² is a group having the structure:

n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the —(CH₂)_n— moiety at any carbon atom of the heterocycle; R³ is hydrogen, C_1-8alkyl, or C_3-7cycloalkylC_0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.

The invention discloses the technical field of medicines and particularly discloses a new prodrug, namely (R)-9-(2-(phosphonyl methoxyl)propenyl) adenine, a cyclodextrin inclusion compound of the prodrug and a non-toxic and pharmaceutically acceptable salt of the prodrug. The prodrug disclosed by the invention can be metabolized into PMPA in vivo, and has the bioavailability of about 39%, and the bioavailability of the prodrug is better than that of tenofovir disoproxil fumarate (Bis-(POC)-PMPA); and the prodrug has more excellent antiviral activity and better safety compared with the tenofovir disoproxil fumarate.

An adenine derivative series is prepared from bromobenze with borate radical through Dimroth rearranging reaction. Its advantage is high activity to suppress proinflammatory factor (tumor necrosis factor alpha) and splitting cell.

The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R¹, R², L¹, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.

Adenine derivatives substituted at the C2, N6, and N9 purine positions having antisenescent and combined photoprotective UVA/UVB effects. These substances are particularly suitable as anti-senescent and UV-photoprotective component in cosmetic preparations, plant protection preparations and in preparations for the treatment/application of tissue cultures

Disclosed are novel methyltransferase assay methods, comprising: including, in a reaction mixture for a methyltransferase activity, a purified or recombinant adenosine nucleosidase activity that catalyses release of an adenine or adenine derivative moiety from a transmethylation product, and a purified or recombinant adenine deaminase activity that catalyses deamination of the released moiety to hypoxanthine or respective derivative and ammonia, wherein the methyltransferase activity is rate-limiting; and determining the methyltransferase activity by spectrophotometric or chromatographic monitoring of the coupled deamination reaction products, or of subsequent enzymatic or chemical reactions coupled thereto. Coupled oxidation of the hypoxanthine to uric acid and hydrogen peroxide is optionally affected using purified or recombinant xanthine oxidase, wherein the methyltransferase activity is rate-limiting, and wherein determining the methyltransferase activity comprises monitoring of the coupled oxidation reaction. Variations are disclosed comprises monitoring of reaction products (e.g., to detect NH3, Hypoxanthine, H2O2, and Uric Acid).

A novel nucleotide derivative, in case of existing as a member of a single-stranded sequence, undergoing a change in the fluorescent signal intensity depending on the corresponding base type in the partner strand with which the single-stranded sequence is hybridized, and which is a thymine/uracil derivative (1) emitting light most intensely when a confronting base in the partner strand with which the single-stranded nucleotide sequence is hybridized is adenine; a cytosine derivative (2) emitting light most intensely when the confronting base is guanine; an adenine derivative (3) emitting light most intensely when the confronting base is cytosine; a guanine derivative (4) emitting light most intensely when the confronting base is cytosine or thymine/uracil; and an adenine derivative (5) emitting light most intensely when the confronting base is thymine/uracil.

A novel nucleotide derivative showing a change in the fluorescent signal intensity depending on the corresponding base species of the counterpart chain of hybridization. And occurring as a member of a single-strand nucleotide sequence, where the corresponding base of the counterpart chain of the hybridization of the single-strand sequence is as followed:(1) which is a thymine/uracil derivative showing the most intense light emission in the case where the corresponding base is adenine; (2) which is a cytosine derivative showing the most intense light emission in the case where the corresponding base is guanine; (3) which is an adenine derivative showing the most intense light emission in the case where the corresponding base is cytosine; or (4) which is a guanine derivative showing the most intense light emission in the case where the corresponding base is cytosine or thymine/uracil.

The present invention relates to a preparation method of adenine derivative. Said method includes the following steps: in non-protonic polar solvent, under the action of catalyst making adenine and phosphonate ester react at 50-150deg.C, then making after-treatment so as to obtain the invented product. The described catalyst at least contains one inorganic alkali and one organic alkali, the described inorganic alkali is selected from carbonate of alkali metal or sodium hydride, and the described organic alkali is selected from alcohol sodium or alcohol potassium of C1-C5.

The invention relates to the development of drugs intended for the prophylaxis and/or treatment of viral diseases caused, in particular, by herpes viruses. What are proposed are complex compounds of germanium having the general structural formula:

Ge_x[AD][CA]_y[AA]_z  (I),

• • where AD is a derivative of a nitrogenous base of the purine series that has antiviral activity and can be selected from guanine derivatives, such as acyclovir, valacyclovir, gancyclovir and pencyclovir, or from adenine derivatives, such as vidarabine; CA is a hydroxycarboxylic acid which can be selected from acids such as (but not limited to) citric acid, lactic acid and malic acid; AA is an amino acid which can be selected from various a-amino acids, such as arginine, glycine, lysine and threonine, and where x=1-2, y=2-4 and z=0-2. Complex compounds of germanium have a high level of antiviral and immune-stimulating activity and are readily soluble in water. The above-mentioned compounds are produced by producing an aqueous suspension of germanium dioxide, adding a hydroxycarboxylic acid, a derivative of a nitrogenous base of the purine series and, optionally, but preferably, an amino acid thereto, heating the mixture produced at a temperature of 40-100° C. for 3-14 hours while stirring and removing the water from the solution, thus producing a complex compound of germanium.