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Specializes in:
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Rates per language pair: English to Romanian - Rates: 0.04 - 0.07 EUR per word / 27 - 30 EUR per hour French to Romanian - Rates: 0.04 - 0.07 EUR per word / 27 - 30 EUR per hour English to French - Rates: 0.04 - 0.07 EUR per word / 27 - 30 EUR per hour
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Sample translations submitted: 1
English to Romanian: 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors General field: Law/Patents Detailed field: Chemistry; Chem Sci/Eng
Source text - English EP 2 035 432 B1 Patent
The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broad- spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)- benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
The virus causing the acquired immunodeficiency syndrome (AIDS) is known by different names, including T-lymphocyte virus III (HTLV-III) or lymphadenopathy- associated virus (LAV) or AIDS-related virus (ARV) or human immunodeficiency virus (HIV). Up until now, two distinct families have been identified, i.e. HIV-I and HIV-2. Hereinafter, HIV will be used to generically denote these viruses.
One of the critical pathways in a retroviral life cycle is the processing of polyprotein precursors by aspartic protease. For instance the HIV viral gag-pol protein is processed by HIV protease. The correct processing of the precursor polyproteins by the aspartic protease is required for the assembly of infectious virions, thus making the aspartic protease an attractive target for antiviral therapy. In particular for HIV treatment, the HIV protease is an attractive target.
HIV protease inhibitors (PIs) are commonly administered to AIDS patients in combination with other anti-HIV compounds such as, for instance nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), fusion inhibitors such as T-20 or other protease inhibitors. Despite the fact that these antiretrovirals are very useful, they have a common limitation, namely, the targeted enzymes in HIV are able to mutate in such a way that the known drugs become less effective, or even ineffective against these mutant HIV viruses. Or, in other words HIV creates an ever-increasing resistance against the available drugs.
Resistance of retroviruses, and in particular HIV, against inhibitors is a major cause of therapy failure. For instance, half of the patients receiving anti-HIV combination therapy do not respond fully to the treatment, mainly because of resistance of the virus to one or more drugs used. Moreover, it has been shown that resistant virus is carried over to newly infected individuals, resulting in severely limited therapy options for these drug-naive patients. Therefore, there is a need in the art for new compounds for retrovirus therapy, more particularly for AIDS therapy. The need in the art is particularly acute for compounds that are active not only on wild type HIV, but also on the increasingly more common resistant HIV.
Translation - Romanian Brevet EP 2 035 432 B1
[0001] Prezenta invenţie se referă la compuşi ai 2-(amino)-benzotiazol sulfonamidei substituiţi şi la derivaţii lor, utilizarea lor ca inhibitori de protează, în special ca inhibitori de protează HIV cu spectru larg, procedee de preparare a acestora, precum şi compoziţii farmaceutice şi truse de diagnostic care îi cuprind. Prezenta invenţie se referă, de asemenea, la combinaţii ale prezenţilor compuşi ai sulfonamidei 2 - (amino-)-benzotiazol substituiţi şi derivaţi cu un alt agent anti-retroviral. În continuare, se referă la utilizarea lor în cadrul testelor ca şi compuşi de referinţă sau ca reactivi.
[0002] Virusul care provoacă sindromul imunodeficienţei dobândite (SIDA), este cunoscut sub diferite nume, care includ virus III al limfocitelor T (HTLV-III) sau virus asociat limfadenopatiei (LAV), sau virusul legat de SIDA (ARV) sau virusul imunodeficienţei umane (HIV). Până acum, au fost identificate două familii distincte, de exemplu HIV-1 şi HIV-2. În continuare, HIV, va fi folosit pentru a desemna generic aceste virusuri.
[0003] Una dintre căile critice într-un ciclu de viaţă retrovirală este de prelucrare a precursorilor poliproteinei cu protează aspartică. De exemplu proteina virală gag-pol de HIV este prelucrată de proteaza HIV. Prelucrarea corectă a poliproteinelor precursoare de proteaze aspartice este necesară pentru asamblarea virionilor infecţioşi, făcând astfel proteaza aspartică o ţintă atractivă pentru tratamentul antiviral. În special pentru tratamentul HIV, proteaza HIV este o ţintă atractivă.
[0004] Inhibitorii de protează HIV (IP) sunt de obicei administraţi la pacientii cu SIDA, în asociere cu alte medicamente anti-HIV, compuşi, cum ar fi, de exemplu, inhibitori nucleozidici de revers transcriptază (INRT), inhibitori ne-nucleozidici de revers transcriptază (INNRT), inhibitori de fuziune cum ar fi inhibitorii proteazei T-20 sau de altă natură. În ciuda faptului că aceste medicamente antiretrovirale sunt foarte utile, ele au o limitare comună, şi anume, enzimele specifice din HIV sunt capabile de a evolua în aşa fel că medicamentele cunoscute devin mai putin eficiente, sau chiar ineficiente împotriva acestor virusuri mutante de HIV. Sau, cu alte cuvinte, HIV creează o rezistenţă tot mai mare în raport cu medicamentele disponibile.
[0005] Rezistenţa retrovirusurilor, şi în special a HIV la inhibitori este o cauză majoră de eşec a tratamentului. De exemplu, jumătate din pacienţii care au primit terapie de combinaţie anti-HIV nu răspund pe deplin la tratament, în principal din cauza rezistenţei virusului la unul sau mai multe medicamente utilizate. În plus, s-a demonstrat că virusul rezistent este purtat la indivizii nou infectaţi, rezultând opţiuni severe de tratament limitat cu medicamente la aceşti pacienţi noi. Prin urmare, în domeniu sunt necesari noi compuşi pentru tratamentul retrovirusului, mai ales pentru tratamentul SIDA. Necesitatea în domeniu este deosebit de acută pentru compuşi care sunt activi, nu numai pe tipul sălbatic de HIV, dar, de asemenea, pe HIV-ul rezistent din ce în ce mai frecvent.
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Years of experience: 26. Registered at ProZ.com: Mar 2012.
English to French (Ministry of Culture) English to Romanian (Ministry of Culture) French to Romanian (Ministry of Culture) English to Romanian (Romanian Ministry of Culture - Central Commission for Granting Translator Certificates) French to Romanian (Romanian Ministry of Culture - Central Commission for Granting Translator Certificates)
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