EA200501682A1 - HIV INTEGRASE INHIBITORS - Google Patents
HIV INTEGRASE INHIBITORSInfo
- Publication number
- EA200501682A1 EA200501682A1 EA200501682A EA200501682A EA200501682A1 EA 200501682 A1 EA200501682 A1 EA 200501682A1 EA 200501682 A EA200501682 A EA 200501682A EA 200501682 A EA200501682 A EA 200501682A EA 200501682 A1 EA200501682 A1 EA 200501682A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- optionally polysubstituted
- alkyl
- het
- relates
- polysubstituted
- Prior art date
Links
Abstract
Настоящее изобретение относится к соединениям, имеющим формулу (I), их N-оксидам, солям, стереоизомерным формам, рацемическим смесям, пролекарствам, сложным эфирам и метаболитам, в которых (a) или (b); A вместе с двумя атомами углерода фенильного кольца, к которому оно присоединено, образует моноциклический арил или моноциклический Het; Rпредставляет собой водород, галоген, нитро, циано, сультам, сультим, Cциклоалкил, C(=O)-R, S(=O)-R, OR, NRR, C(=NR)-R, необязательно полизамещенный Cалкил, необязательно полизамещенный Cалкенил, необязательно полизамещенный Cалкинил; Rпредставляет собой водород, Cциклоалкил, арил, Het, Het, C(=O)-R, S(=O)-R, OR, NRR, C(=NR)-Rили необязательно полизамещенный Cалкил, необязательно полизамещенный Cалкенил или необязательно полизамещенный Cалкинил. Кроме того, оно относится к их применению в качестве ингибиторов ВИЧ-интегразы, способам их получения, а также фармацевтическим композициям и диагностическим наборам, содержащим их. Оно также относится к сочетаниям их с другими антиретровирусными агентами и к их применению при анализе эталонных соединений или в качестве реагентов.The present invention relates to compounds having formula (I), their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, in which (a) or (b); A, together with the two carbon atoms of the phenyl ring to which it is attached, forms monocyclic aryl or monocyclic Het; R 2 is hydrogen, halogen, nitro, cyano, sultam, sultim, Ccycloalkyl, C (= O) -R, S (= O) -R, OR, NRR, C (= NR) -R, optionally polysubstituted C1-6 alkyl, optionally polysubstituted Calkenyl, optionally polysubstituted Calkynyl; R1 is hydrogen, Ccycloalkyl, aryl, Het, Het, C (= O) -R, S (= O) -R, OR, NRR, C (= NR) -R or optionally polysubstituted C1-6 alkyl, optionally polysubstituted C1-6 alkenyl or optionally polysubstituted C1-6 alkyl, . In addition, it relates to their use as HIV integrase inhibitors, methods for their preparation, as well as pharmaceutical compositions and diagnostic kits containing them. It also relates to their combination with other antiretroviral agents and to their use in the analysis of reference compounds or as reagents.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US46598703P | 2003-04-28 | 2003-04-28 | |
| EP03101164 | 2003-04-28 | ||
| PCT/EP2004/050621 WO2004096807A2 (en) | 2003-04-28 | 2004-04-27 | Hiv integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA200501682A1 true EA200501682A1 (en) | 2006-04-28 |
Family
ID=34924058
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200501682A EA200501682A1 (en) | 2003-04-28 | 2004-04-27 | HIV INTEGRASE INHIBITORS |
Country Status (1)
| Country | Link |
|---|---|
| EA (1) | EA200501682A1 (en) |
-
2004
- 2004-04-27 EA EA200501682A patent/EA200501682A1/en unknown
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