40 results about "Abacavir" patented technology

Combinations of antiretroviral nucleoside reverse transcriptase inhibitors, and methods for their use in treating retroviral infections, are provided. In one embodiment, the combinations include non-thymidine nucleoside antiretroviral agents, such as tenofovir-DF, abacavir, APD and DAPD, that select for the K65R mutation and relatively low doses of zidovudine (AZT) or other thymidine nucleoside antiretroviral agents. The thymidine nucleoside antiretroviral agents retard development of the K65R mutation, and at the low doses, are less likely to produce side effects. In another embodiment, the combinations include DAPD and AZT. DAPD retards the development of TAMs, and AZT retards the development of the K65R mutation. In a third embodiment, the combinations include adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.

The invention discloses a method for synthesizing a chiral carbon ring intermediate of Abacavir. The steps are as follows: firstly, an intermediate 1 is prepared by 2-azabicyclo[2.2.1]hept-5- en-3-one, 1 mol of intermediate 1 is dissolved into 500 to 2000ml of organic solvent, the organic solvent is added into phosphate buffer solution of bacillus subtilis proteinase cross-linked enzyme crystals;the system is maintained between 15 and 35 DEG C and is mechanically stirred for 5 to 10 hours, the stirring speed is between 100 and 500r / m; the reaction is stopped, and the bacillus subtilis proteinase cross-linked enzyme crystals are reclaimed after the filtration; another 1000 to 2000ml of organic solvent is used to extract the filtrate for 3 to 6 times; organic phases are merged and dried bydrying agent; and the target compound is obtained through reduced pressure distillation or column chromatography. The method has the advantages that: the method has short reaction time and high yield,the obtained product has high optical purity, and the catalyst can be reclaimed and reused.

Nucleosides and nucleotides (nucleos(t)ides) have been in clinical use for almost 50 years and have become cornerstones of treatment for patients with viral infections or cancer. The approval of several additional drugs over the past decade demonstrates that this family still possesses strong potential. Therefore nucleos(t)ide are of great interest as promising chemotherapeutic agents, including: 2′-deoxy-L-uridine (CAS 31501-19-6), 2′-deoxy-D-uridine (CAS 951-78-0), telbivudine (CAS 3424-98-4), zidovudine (AZT, CAS 30516-87-1), trifluridine (CAS 70-00-8), clevudine (CAS 163252-36-6), PSI-6206 (CAS 863329-66-2), 2′-(S)-2′-chloro-2′-deoxy-2′-fluorouridine (CAS 1673560-41-2), ND06954 (CAS 114248-23-6), stavudine (CAS 3056-17-5), 5-ethynyltavudine (Festinavir, CAS 634907-30-5), torcitabine (CAS 40093-94-5), (−)-beta-D-(2R,4R)-dioxolane-thymine (DOT, 1-((2R,4R)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl-2,4(1H,3H)-pyrimidinedione, CAS No. 127658-07-5), 2-(6-amino-purin-9-yl)-ethanol (CAS 707-99-3), 2′-C-methylcytidine (CAS 20724-73-6), PSI-6130 (CAS 817204-33-4), gemcitabine (CAS 95058-81-4), 2′-chloro-2′-deoxy-2′-fluorocytidine (CAS 1786426-19-4), 2′,2′-dichloro-2′-deoxycytidine (CAS 1703785-65-2), 2′-C-methylcytidine (CAS 20724-73-6), PSI-6130 (CAS 817204-33-4), lamivudine (3TC, CAS 134678-17-4), emtricitabine (CAS 143491-57-0), 2′-deoxyadenosine (CAS 958-09-8), 2′-deoxy-β-L-adenosine (CAS 14365-45-8), 2′-deoxy-4′-C-ethynyl-2-fluoroadenosine (CAS 865363-93-5), didanosine (CAS 69655-05-6), entecavir (CAS 209216-23-9), FMCA (CAS 1307273-70-6), dioxolane-G (DOG, CAS 145514-01-8), β-D-2′-deoxy-2′-(R)-fluoro-2′-β-C-methylguanosine (CAS No 817204-45-8), abacavir (ABC, CAS 136470-78-5), dioxolane-A (DOA, CAS #145514-02-9), [(2R,4R)-4-(6-cyclopropylamino-purin-9-yl)-[1,3]dioxolan-2-yl]-methanol (CAS 1446751-04-7), amdoxovir (AMDX, CAS 145514-04-1), (R)-1-(6-amino-purin-9-yl)-propan-2-ol (CAS 14047-28-0), and [(2S,5R)-5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yl]-methanol.Macroheterocyclic nucleoside derivative and its analog of the general formula 1 or general formula 2, a stereoisomer, isotope-enriched analog, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof,wherein:Ar is aryl or hetaryl;R1 and R2 are not necessarily the same substituents selected from H, F, Cl, CH3, OH;R3 is H or CH3;X is oxygen or ethanediyl-1,1 (C═CH2);Y is CH(R4)(CH2)k, CH(R4)(CH2)mC(O)O(CH2)n;R4 is H or CH3;k has a value from zero to six;m has a value from zero to two;n has a value of one to four;Q is a radical selected from Q1-Q4;wherein: R5 is the substituent selected from H, F, Cl, CH3, OH;the arrow (→) indicates the location, joined by Q1-Q4.

Methods of assessing the risk of clinical signs of hypersensitivity reaction to nucleoside antiviral compounds, including abacavir, are described. The methods include genotyping subjects for polymorphisms in the TNFα gene, the class 1 HLA genes, or a combination of both the TNFα and HLA genes.

Process for removal of the amino protective group of a N-acylated {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl}methanol of formula (II) where R═H or a (C1-C4)-alkyl, using an inorganic base in a mixture of water and alcohol, to yield abacavir or its salts. The process proceeds very fast and the product can be obtained in high yield and purity.

The invention provides an abacavir individualized medication detection kit and method and belongs to the technical field of abacavir medication detection. The Allele-Specific LAMP (loop-mediated isothermal amplification) technology is adopted, specific primers are designed aiming at a G allele of rs2395029, and whether a patient carries HLA (human leukocyte antigen)-B*5701 allele is judged according to the relevance of the G allele of rs2395029 and HLA-B*5701. After detection, whether a positive reaction is performed can be judged through observation of the state change, namely, whether precipitation or color change exists or not, of a reaction system, judgment can be performed with naked eyes, additional device equipment is not needed, and easiness and feasibility are realized.

The invention provides a method for detecting the concentration of metacavir and metabolites thereof in a biological sample. According to the method, the metacavir, the metabolites and tinidazole (internal standard) are extracted with ethyl acetate, and a UPLC-MS / MS (ultra-performance liquid chromatography-tandem mass spectrometry) method is adopted for performing separation and determination. The method provided by the invention is proved to be accurate and reliable by methodology and can be used for analyzing the content of the metacavir and the metabolites thereof in the biological sample.

A process for preparing the optical-purity (99.9% ee) Abakawei features that its initial raw materials are (1S,4R)-4-amino-2-cyclopentyl-1-methanol and 2,5-diamino- 4,6-dichloropyrimidine.

The invention discloses an abacavir intermediate and a method for purifying the same. The method includes heating mixtures with abacavir intermediate crude products, purified water and water-soluble organic solvents until the abacavir intermediate crude products are completely dissolved so as to obtain mixed liquid; carrying out cooling and crystallization treatment on the mixed liquid; carrying out filtering and drying treatment after crystallization treatment is carried out so as to obtain abacavir intermediate pure products. A structural formula of the abacavir intermediate is shown as a formula IV. The abacavir intermediate and the method have the advantage that the method is easy and convenient to implement and is suitable for industrial production.

The invention discloses an abacavir crystal and a preparation method thereof. Under powder X-ray diffraction, the crystal has main characteristic peaks at the diffraction angle 2[theta] of 9.0 degrees, 10.1 degrees, 12.7 degrees, 13.2 degrees, 17.8 degrees, 20.2 degrees, 23.8 degrees and 25.5 degrees, wherein test error is + / - 0.2 degrees. The preparation method comprises the following steps: adding an abacavir raw material to an organic solvent, increasing the temperature until the solution is clear, dropwisely adding an anti-solvent at 50-60 DEG C, and then performing temperature-maintained stirring for 1-2 h, finally reducing the temperature to room temperature, collecting the separated-out crystal and drying the crystal. The abacavir crystal has stable form, is easy to separate, is high in purity and is stable in quality. The preparation method is simple in process, is easy to operate and achieve in large scale, and is beneficial to development and large-scale production of a follow-up preparation.

The application discloses a high performance liquid phase detection method for impurities of abacavir. The structural formula of the impurities is wherein, R is an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a hydroxyl group, a halogen, a hydroxyalkyl group, a carboxyl group or an ester The method includes: providing a sample analysis solution; injecting the sample analysis solution into a high-performance liquid chromatograph for chromatographic analysis, and recording the chromatogram; wherein the chromatographic column used is a reversed-phase chromatographic column, and the mobile phase used is acid solution and A mixture of solvent phases. Through the above method, the present application can improve the separation and accuracy of detection.

Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C1-C4)-alcohol, dichloromethane, acetonitrile / water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and / or prophylaxis of HIV infections.