A Multicenter, Randomized, Double-Blinded, Dose-Escalation Study Evaluating the Safety and Antiretroviral Activity of HBY 097 Versus HBY 097 Plus AZT in Patients With Asymptomatic or Mildly Symptomatic HIV Infection

To obtain preliminary information on the safety, tolerability, and antiretroviral activity of HBY 097 alone or in combination with zidovudine ( AZT ) versus AZT alone.
PER 1/19/96 AMENDMENT: AZT monotherapy arm was eliminated.

Start Date-

Sponsor / Collaborator

Hoechst Marion Roussel

100 Clinical Results associated with Talviraline

100 Translational Medicine associated with Talviraline

100 Patents (Medical) associated with Talviraline

Literatures (Medical) associated with Talviraline

01 Jan 2013·Organic & Biomolecular ChemistryQ3 · CHEMISTRY

Diverse reactivity in microwave-promoted catalyst-free coupling of substituted anilines with ethyl trifluoropyruvate and biological evaluation

Q3 · CHEMISTRY

Article

Author: Jing-Yun Li ; Jian-Yong Wang ; Dao-Min Zhuang ; Biao Jiang ; Xiao-Long Du ; Si-Yuan Chen ; Jia Li ; Chen Zhang ; Jian-Hua Yao

Diverse reactivity by coupling of substituted anilines with ethyl trifluoropyruvate was developed under microwave irradiation without catalysts to generate 3-trifluoromethyl-3-hydroxy oxindoles, aromatic hydroxy trifluoromethyl esters, and 1,2-dicarbonyl compounds in a fast and efficient manner. The plausible mechanism for obtaining different products was proposed. Furthermore, the anti-HIV activity of aromatic hydroxy trifluoromethyl esters was first reported. The best inhibitory activity against wild-type HIV-1 IIIB was exemplified by trifluoromethyloxindole 3q with an IC50 = 5.8 μM, which also displayed potential activity against Y181C mutant virus with an IC50 = 7.5 μM. More significantly, the activities of oxindoles 3q and 3r to inhibit K103N/Y181C double mutant HIV-1 reverse transcriptase (RT) are probably similar to that of the second-generation nonnucleoside inhibitor HBY 097 by docking calculation.

01 Aug 2010·Antiviral Chemistry and Chemotherapy

Looking for an Active Conformation of the Future HIV Type-1 Non-Nucleoside Reverse Transcriptase Inhibitors

Review

Author: Silvestri, Romano ; Regina, Giuseppe La ; Coluccia, Antonio

HIV type-1 (HIV-1) non-nucleoside reverse transcriptase inhibitors (NNRTIs) are key drugs of highly active antiretroviral therapy (HAART) in the clinical management of AIDS/HIV infection. NNRTI-based HAART regimes effectively suppress viral reproduction, are not cytotoxic and show favourable pharmacokinetic properties. First-generation NNRTIs suffer the rapid selection of viral variants, hampering the binding of inhibitors into the reverse transcriptase (RT) non-nucleoside binding site (NNBS). Efforts to improve these first inhibitors led to the discovery of second-generation NNRTIs that proved to be effective against the drug-resistant mutant HIV-1 strains. The success of such agents launched a new season of NNRTI design and synthesis. This paper reviews the characteristics of second-generation NNRTIs, including etravirine, rilpivirine, RDEA-806, UK-453061, BIRL 355 BS, IDX 899, MK-4965 and HBY 097. In particular, the binding modes of these inhibitors into the NNBS of the HIV-1 RT and the most clinically relevant mutant RTs are analysed and discussed.

01 Sep 2008·Journal of Molecular ModelingQ4 · CHEMISTRY

The use of local surface properties for molecular superimposition

Q4 · CHEMISTRY

Article

Author: Manallack, David T

This study employed surface-based properties for use in the superimposition of three series of molecules. The properties used were derived from semiempirical molecular orbital calculations and can be related to the physics of intermolecular interactions. In each case, the superimposition of the compounds was within 0.6 A of the experimental overlay. The superimposition cases presented differing levels of involvement of electrostatic interactions, and in only one case did shape similarity provide the best overlay. Two test compounds were applied to an example exploring non-nucleoside HIV-1 reverse transcriptase inhibitors and only one of these compounds overlaid in the same manner as their crystal structure complexes. This served to highlight the need for molecules to occupy the same region of space when employing this technique. Nevertheless, the method can be used to generate pharmacophores and ultimately could be used to interrogate databases for molecules that match the key surface properties, thus allowing scaffold hopping.

100 Deals associated with Talviraline

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Infections	Phase 2	-	GSK Plc	-
HIV Infections	Phase 2	Germany	Bayer AG	-
HIV Infections	Phase 2	Germany	Bayer AG	-
HIV Infections	Phase 2	-	GSK Plc	-

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