77 results about "HIV integration" patented technology

The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I]

wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

A compound of the formula (I):wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is -COORA wherein RA is hydrogen or ester residue, -CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.

A process for preparing a compound represented by formula (Y1) or (Y2) [wherein R^x is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R^1d is hydrogen, halogen, or the like; R^2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R^4d is a lower alkyl optionally substituted with substituent E, or the like; and R^6d is a lower alkyl group optionally substituted with substituent group E, or the like].

The present invention relates to a compound represented by the following formula [I]

wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.

The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds.

Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.

A¹ and A² are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, ⁺NR, or CR⁴. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.

The invention belongs to the fields of genetic engineering and cell engineering, pertaining to a human T-lymphocytic series model for screening and reactivating latent infection HIV-1 compound and a preparation method thereof. The invention discloses a T lymphocyte used for screening and activating latent infection HIV-1 drug, and the T lymphocyte is a Jurkat stable strain that is infected by but not expresses HIV slow virus carrying reporter gene. The preservation number of the T lymphocyte is CCTCC NO.C200821. The invention also provides a preparation method for the T lymphocyte, including infecting human T-lymphocytic series Jurkat with the HIV-1 slow virus carrying EGFO reporter gene, and carrying out cell sorting and HIV integration test so as to obtain the clone with HIV integration while not expressing EGFP. The invention is the cell model for the virus preservation library to control drug screening.

The present invention relates to a series of pyrimidine compounds of Formula I which inhibit HIV integrase and to pharmaceutical compositions and methods of treatment for AIDS or ARC using these compounds.

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula, wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

A compound of the formula (I) wherein Z<4>, Z<5> and Z<9> each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; R is a group of the formula (II) (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.

An embodiment of a method for detecting low frequency occurrence of one or more HIV sequence variants associated with integrase is described that comprises the steps of: (a) generating a cDNA species from a plurality of RNA molecules in an HIV sample population; (b) amplifying a plurality of first amplicons from the cDNA species, wherein each first amplicon is amplified with a pair of nucleic acid primers; (c) clonally amplifying the amplified copies of the first amplicons to produce a plurality of second amplicons; (d) determining a nucleic acid sequence composition of the second amplicons; (e) detecting one or more sequence variants that occur at a frequency of 5% or less in the nucleic acid sequence composition of the second amplicons; and (f) correlating the detected sequence variants with variation associated with HIV integrase.

The present invention relates to compounds of formula (I) wherein c, X, Y, R², R³, R⁴ and R⁶ are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of HIV integrase, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection

The invention relates to a nitrogen-containing polyhydroxy arometic compound having a structure as shown in a general formula 1, wherein R1 is hydrogen, methyl or fluorine; R2 is hydrogen, methyl, acetyl, fluorine, chlorine or bromine; R3 is hydrogen, methyl, butyl, methoxyl, ethoxyl, fluorine, chlorine, bromine or nitro; R4 is hydrogen, methyl, acetyl, fluorine, chlorine or bromine; and n is 0 or 1. The invention also relates to a method for preparing the nitrogen-containing polyhydroxy arometic compound in the general formula 1. The compound has obvious inhibitory activity to HIV integrase, and is used for preparing anti-AIDS medicine. The n is equal to 0 or 1.

1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.

Orally administered, taste-masked tablets and granules contain (a) a hydroxypyrimidinone carboxamide, a hydroxy-tetrahydropyridopyrimidinone carboxamide, or a related carboxamide compound, or a pharmaceutically acceptable salt thereof, (b) a taste-masking polymer, (c) a superdisintegrant, and optionally other excipients. The carboxamide compound is an HIV integrase inhibitor, and the tablets and granules are suitable for use in the inhibition of HIV integrase, the treatment or prophylaxis of HIV infection, and the treatment or prophylaxis or delay in the onset of AIDS.