54 results about "Entry inhibitor" patented technology

This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

The invention discloses low molecular weight carboxyl-reduced derivatives of fucosylated glycosaminoglycans (LCRG). The extent of carboxyl reduction is not less than 20%. Weight-average molecular weight of the LCRG is about 3000-20000Da, and monosaccharides comprise acetyl galactosamine (GalNAc), glucose (Glc) or glucuronic acid (GlcUA) and fucose (Fuc) or sulfates of fucose (shown as -OSO3-). The mole ratio of GalNAc, Glc (containing GlcUA), Fuc and -OSO3- is about 1: (1+-0.3): (1+-0.3): (3.0+-1.0). The LCRG is a potent human immunodeficiency virus (HIV) Type 1 entry inhibitor which acts on conserved regions and has the advantages of high activity against HIV Type 1, high therapeutic index and no-drug-resistance, and the LCRG can be used for preventing or curing HIV. The invention further provides a preparation method of the LCRG. The carboxyl-reduced derivatives of fucosylated glycosaminoglycans and medicinal compositions of the carboxyl-reduced derivatives can be prepared into injection agents, lyophilized powder or suppository and the like.

This invention provides compounds of Formula I, including pharmaceutically accceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I have the formula wherein: Z is Q is selected from the group consisting of m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and —W— is

The invention discloses a low molecular weight glycosylated chondroitin sulfate, whose weight average molecular weight is 3000-15000Da. The monosaccharide composition comprises acetyl galactosamine (D-GalNAc), glucuronic acid (D-GlcUA), fucose (L-Fuc), or its sulfuric ester (expressed in -OS03<->), wherein the mole ratio of D-GalNAc to D-GlcUA to L-Fuc to -OS03<-> is 1: (1+ / -0.3): (1+ / -0.3): (3.5+ / -0.5). The low molecular weight glycosylated chondroitin sulfate has a strong anti-HIV-1 virus activity, is a gp120 entry inhibitor, and can be used for preventing and / or treating AIDS. The invention also provides a method for preparing the low molecular weight glycosylated chondroitin sulfate and its composition preparation. Glycosylated chondroitin sulfate is depolymerized by the peroxide method to obtain a low molecular weight product, and then low molecular and / or high-molecular impurities of the product are removed by gel separation or ultrafiltration method. The low molecular weight glycosylated chondroitin sulfate and its medicinal composition can be prepared in the form of an injection, a lyophilized powder or a suppository.

Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally 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 present invention is based upon the surprising discovery that exposure of a non-resistant HIV to a first entry inhibitor, such as an anti-CD4 antibody or a co-receptor inhibitor, which like all current HIV drugs selects for mutations that result in a resistant HIV, surprisingly results in HIV viruses much more susceptible to neutralization by a second entry inhibitor, such as soluble CD4 (sCD4) or an HIV gp41 inhibitor. Therefore, the present invention provides methods and compositions for inhibiting HIV-1 infection in a subject that overcomes the problem of drug resistance.

Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally 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.

Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.

The present invention relates to hydrophobic modified preS-derived peptides of hepatitis B virus (HBV) which are derived from a HBV preS consensus sequence and are N-terminal preferably acylated and optional C-terminal modified. These hydrophobic modified preS-derived peptides of HBV are very effective HBV entry inhibitors as well as HDV entry inhibitors and are, thus, suitable for the inhibition of HBV and / or HDV infection, prevention of primary HBV and / or HDV infection as well as treatment of (chronic) hepatitis B and / or D. The present invention further relates to pharmaceutical and vaccine compositions comprising these hydrophobic modified preS-derived peptides of HBV.

The invention provides a novel infection model based on EBOV (Ebola Virus) virus-like particles (VLP) and taking firefly luciferase (Fluc) as a reporter protein. The model enters cells with the help of an EBOV envelope protein (GP); the Fluc can be introduced into the cells after the model enters the cells, so that cell infection can be quantified according to signal intensity of the Fluc in the cells; mouse infection can be quantified through biological imaging according to signal intensity of bioluminescence in a mouse body. Therefore, the inventor can utilize the model to carry out in-vitro and in-vivo pre-screening experiments on a neutralizing antibody and an entered inhibitor of the GP outside a BSL-4 (Biosafety Level-4) laboratory.

This invention provides compounds, methods, immunoassays, and kits relating to active, metabolically sensitive (“met-sensitive”) moieties of anti-HIV therapeutics, such as HIV protease inhibitors (PI), HIV nucleoside reverse transcriptase inhibitors (NRTI) and HIV entry inhibitors (EII).

A rocaglamide or a rocaglate derivative, particularly aglaroxin C, blocks hepatitis C virus (HCV) entry with improved potency and therapeutic index.

Abstract The invention relates peptide entry inhibitors and methods of determining such inhibitors that are bindable to regions of viruses having class II E proteins, such as the dengue virus E protein, as candidates for in vivo anti-viral compounds.

This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with ureido and thioureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I are wherein: Y is O or S; Q is selected from the group consisting of m is 2; A is NR13R14; and —W— is

The invention provides a peptide triazole conjugate and derivatives thereof, and methods of its use. Further provided are an antibody to the peptide triazole conjugate, and a method of identifying an HIV-I entry inhibitor candidate.

Compounds, compositions, and methods of treatment and prevention of HIV, including HIV-1 and HIV-2, Dengue, and Chikungunya infection are disclosed. The compounds are TREM-1 inhibitors. Combinations of these TREM-1 inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, JAK inhibitors, macrophage depleting agents, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally 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, Dengue, or Chikungunya virus in an infected patient.

The present invention features methods of screening for compounds that inhibit HCV binding to a cell, methods of inhibiting IICV entry into a cell, and methods of actively or prophylactically treating against an IICV infection. The different methods are based on the identification of the scavenger receptor class B type I as a target site for HCV E2 binding to a cell.

The invention relates chemical compound entry inhibitors and methods of determining such inhibitors that interact with regions of viruses, such as the dengue virus, as candidates for in vivo anti-viral compounds.

The invention relates to the field of compound synthesis, and mainly relates to a difluoro methylene piperidine carboxamide derivative (I), a medicament composition containing the difluoro methylene piperidine carboxamide derivative (I), and a preparation method and application thereof. The definition of R<1> is shown in the specification. Proved by pharmacodynamic tests, a compound disclosed by the invention has a CCR5 antagonistic action, can be used as an entry inhibitor of HIV virus, and can also be developed to be anti-AIDS medicines.

Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

The present invention relates to cyclic NTCP targeting peptides which are preS-derived peptides of hepatitis B virus (HBV). The present invention further relates to pharmaceutical compositions comprising at least one cyclic peptide. The present invention further relates to medical uses of said cyclic peptides and the pharmaceutical compositions, such as in the diagnosis, prevention and / or treatment of a liver disease or condition, and / or in the inhibition of HBV and / or HDV infection. The present invention further relates to methods of diagnosis, prevention and / or treatment of a liver disease or condition and / or the inhibition of HBV and / or HDV infection.

The present invention features interferon-free therapies for the treatment of HCV. The therapies comprise administering 2R,6S,13aS,14aR,16aS,Z)-N-(cyclopropylsulfonyl)-6-(5-methylpyrazine-2-carboxamido)-5,16-dioxo-2-(phenanthridin-6-yloxy)-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-exadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a-carboxamide (Compound I), or a pharmaceutically acceptable salt thereof, and another anti-HCV agent. Preferably, the therapies are both interferon- and ribavirin-free. The other anti-HCV agent can be a HCV polymerase inhibitor, an HCV NS5A inhibitor, an HCV entry inhibitor, a cyclophilin inhibitor, or an internal ribosome entry site inhibitor. Preferably, the other anti-HCV agent is an HCV polymerase inhibitor. Also preferably, the other anti-HCV agent is an HCV NS5A inhibitor. Also preferably, the other anti-HCV agent is administered concurrently with Compound I or a pharmaceutically acceptable salt thereof. In another example, the other anti-HCV agent is administered sequentially with Compound I or a pharmaceutically acceptable salt thereof. In still another embodiment, Compound I (or a pharmaceutically acceptable salt thereof) is co-administered with two or more other anti-HCV agents. For instance, Compound I (or a pharmaceutically acceptable salt thereof) can be co-administered with an HCV polymerase inhibitor and an HCV NS5A inhibitor. For another instance, Compound I (or a pharmaceutically acceptable salt thereof) can be co-administered with two different HCV polymerase inhibitors (e.g., one is a nucleoside polymerase inhibitor and the other is a non-nucleoside polymerase inhibitor; or both are nucleoside polymerase inhibitors; or both are non-nucleoside polymerase inhibitor). In yet another example, Compound I (or a pharmaceutically acceptable salt thereof) is co-administered with another HCV protease inhibitor and an HCV polymerase inhibitor. In still another example, Compound I (or a pharmaceutically acceptable salt thereof) is administered with two different HCV NS5A inhibitors.

Methods for treating HIV positive patients, and purging and eradicating latent HIV virus from a patient's system, are disclosed. The bulk of viral load is eradicated using conventional antiretroviral (ARV) therapy. Compounds that encourage viral production in the latent cells are then administered, preferably without activating those cells, while maintaining the ARV therapy. The administration of compounds that encourage viral production in latent cells is cycled, and after around 7-10 cycles, the methods can virtually eliminate latent HIV in the patient. Ideally, the ARV regimen includes at least one integrase inhibitor, at least one entry inhibitor, such as a CCR5 antagonist, and at least one, and preferably two, reverse transcriptase inhibitors. The compounds that encourage viral production in latent cells ideally include a combination of prostratin or a prostratin analog and an HDAC inhibitor, such as butyrate, valproate, or SAHA.

The invention provides a peptide triazole conjugate and derivatives thereof, and methods of its use. The invention also provides an antibody to the peptide triazole conjugate. The invention further provides a method of identifying an HIV-1 entry inhibitor candidate.

The present invention relates generally to the use of recombinant adeno-associated viruses (rAAV) for gene delivery and more specifically to the use of rAAV to deliver genes encoding human immunodeficiency virus entry inhibitors to target cells in mammals.

The disclosure provides compositions and methods for sensitizing primary HIV-1, including transmitted / founder viruses, to neutralization by monoclonal antibodies, e.g., those directed against CD4-induced (CD4i) epitopes and the V3 region. In certain embodiments, the disclosure relates to the use of small molecules as microbicides to inhibit HIV-1 infection directly and to sensitize primary HIV-1 to neutralization by readily elicited antibodies.