DK1663240T3 - Kombinationer af en pyrimidin-holdig nnrti med rt-inhibitorer - Google Patents
Kombinationer af en pyrimidin-holdig nnrti med rt-inhibitorer Download PDFInfo
- Publication number
- DK1663240T3 DK1663240T3 DK04787096.9T DK04787096T DK1663240T3 DK 1663240 T3 DK1663240 T3 DK 1663240T3 DK 04787096 T DK04787096 T DK 04787096T DK 1663240 T3 DK1663240 T3 DK 1663240T3
- Authority
- DK
- Denmark
- Prior art keywords
- combination
- tmc278
- reverse transcriptase
- pharmaceutically acceptable
- acceptable salt
- Prior art date
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (35)
1. Kombination, der omfatter (i) 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amino]-benzonitril, også kaldet TMC278, eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) en nukleosid-revers transkriptase-inhibitor og/eller en nukleotid-revers transkriptase-inhibitor; hvor TMC278 og nukleotid-revers transkriptase-inhibitoren og nukleosid-revers transkriptase-inhibitoren er terapeutisk effektive HIV-inhibitorer ved en dosis, der kan administreres en gang dagligt; til anvendelse til behandling af HIV-infektion, hvor kombinationen administreres en gang dagligt.
2. Kombination til anvendelse ifølge krav 1, der omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) en nukleosid-revers transkriptase-inhibitor; hvor TMC278 og nukleosid-revers transkriptase-inhibitoren er terapeutisk effektive HIV-inhibitorer ved en dosis, der kan administreres en gang dagligt.
3. Kombination til anvendelse ifølge krav 1, der omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) en nukleotid-revers transkriptase-inhibitor; hvor TMC278 og nukleotid-revers transkriptase-inhibitoren er terapeutisk effektive HIV-inhibitorer ved en dosis, der kan administreres en gang dagligt.
4. Kombination til anvendelse ifølge krav 1, der omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) en nukleosid-revers transkriptase-inhibitor; og (iii) en nukleotid-revers transkriptase-inhibitor; hvor TMC278 og nukleotid-revers transkriptase-inhibitoren og nukleosid- revers transkriptase-inhibitoren er terapeutisk effektive HIV-inhibitorer ved en dosis, der kan administreres en gang dagligt.
5. Kombination til anvendelse ifølge krav 1, der omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) en nukleosid-revers transkriptase-inhibitor; og (iii) en anden nukleosid-revers transkriptase-inhibitor, der er forskellig fra nukleosid-revers transkriptase-inhibitoren i (ii) ; hvor TMC278 og nukleosid-revers transkriptase-inhibitorerne er terapeutisk effektive HIV-inhibitorer ved en dosis, der kan administreres en gang dagligt.
6. Kombination til anvendelse ifølge et hvilket som helst af kravene 1-5, hvor nukleotid-revers transkriptase-inhibitoren og/eller nukleosid-revers transkriptase-inhibitoren eller inhibitorerne vælger mutationer i revers transkriptasen, der ikke forårsager resistens over for TMC278.
7. Kombination til anvendelse ifølge et hvilket som helst af kravene 1, 3, 4 eller 6, hvor nukleotid-revers transkriptase- inhibitoren er tenofovir eller dets prodrug tenofovirdisoproxilfumarat.
8. Kombination til anvendelse ifølge et hvilket som helst af kravene 1, 2, 4 til 6, hvor nukleosid-revers transkriptase- inhibitoren er emtricitabin, racemisk FTC, lamivudin (også kaldet 3TC), abacavir eller et farmaceutisk acceptabelt salt deraf.
9. Kombination til anvendelse ifølge krav 8, hvor nukleosid-revers transkriptase-inhibitoren er emtricitabin.
10. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller et farmaceutisk acceptabelt salt og (ii) tenofovir eller dets prodrug tenofovirdisoproxilfumarat og (iii) emtricitabin.
11. Kombination til anvendelse ifølge krav 8, hvor nukleosid-revers transkriptase-inhibitoren er lamivudin.
12. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller et farmaceutisk acceptabelt salt og (ii) tenofovir eller dets prodrug tenofovirdisoproxilfumarat og (iii) lamivudin.
13. Kombination til anvendelse ifølge krav 8, hvor nukleosid-revers transkriptase-inhibitoren er abacavir eller et farmaceutisk acceptabelt salt deraf.
14. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller et farmaceutisk acceptabelt salt og (ii) tenofovir eller dets prodrug tenofovirdisoproxilfumarat og (iii) abacavir eller et farmaceutisk acceptabelt salt deraf.
15. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller et farmaceutisk acceptabelt salt og (ii) lamivudin og (iii) emtricitabin.
16. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller et farmaceutisk acceptabelt salt og (ii) abacavir eller et farmaceutisk acceptabelt salt deraf; og (iii) emtricitabin.
17. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller et farmaceutisk acceptabelt salt og (ii) lamivudin og (iii) abacavir eller et farmaceutisk acceptabelt salt deraf.
18. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) tenofovir eller dets prodrug tenofovirdisoproxilfumarat.
19. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; (ii) en nukleosid-revers transkriptase-inhibitor og (iii) tenofovirdisoproxilfumarat.
20. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; (ii) emtricitabin og (iii) tenofovir eller dets prodrug tenofovirdisoproxilfumarat.
21. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) emtricitabin.
22. Kombination til anvendelse ifølge et hvilket som helst af kravene 1, 4, 5 til 21, hvor vægtforholdet mellem hvert par af bestanddele i tripelkombinationen, der tages på daglig basis, kan variere inden for et interval fra 1/4 til 4/1.
23. Kombination til anvendelse ifølge et hvilket som helst af kravene 1, 4, 5 til 21, hvor vægtforholdet mellem hvert par af bestanddele i tripelkombinationen, der tages på daglig basis, kan variere inden for et interval fra 1/10 til 10/1.
24. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) lamivudin.
25. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) abacavir eller et farmaceutisk acceptabelt salt deraf.
26. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter (i) TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; og (ii) emtricitabin og (iii) en nukleotid-revers transkriptase-inhibitor.
27. Kombination til anvendelse ifølge krav 1, hvor kombinationen omfatter TMC278 eller en stereoisomer form deraf; eller et farmaceutisk acceptabelt salt deraf; med emtricitabin og tenofovirdisoproxilfumarat.
28. Kombination til anvendelse ifølge et hvilket som helst af kravene 1 til 27, hvor TMC278 forekommer i dets E-isomere form.
29. Kombination til anvendelse ifølge et hvilket som helst af kravene 1 til 28, hvor TMC278 er til stede som E-TMC278- hydrochlorid.
30. Produkt, der indeholder en kombination ifølge et hvilket som helst af kravene 1 til 29, til anvendelse til behandling af HIV-infektion, hvor kombinationen administreres en gang dagligt som et kombineret præparation til samtidig, separat eller sekventiel anvendelse.
31. Farmaceutisk formulering, der omfatter et farmaceutisk acceptabelt bæremateriale og en kombination ifølge et hvilket som helst af kravene 1 til 29, til anvendelse til behandling af HIV-infektion, hvor formuleringen administreres en gang dagligt.
32. Formulering til anvendelse ifølge krav 31, der omfatter en kombination ifølge krav 27.
33. Anvendelse af en kombination ifølge et hvilket som helst af kravene 1 til 29 til fremstilling af et medikament til forebyggelse af HIV-infektion eller overførsel ved kønslig omgang eller relateret intim kontakt mellem partnere, hvor kombinationen administreres en gang dagligt.
34. Anvendelse af en kombination ifølge et hvilket som helst af kravene 1 til 29 til fremstilling af et medikament til behandling af HIV-infektion, hvor kombinationen administreres en gang dagligt.
35. Anvendelse af en farmaceutisk formulering ifølge krav 31 eller 32 til fremstilling af et medikament til behandling af HIV-infektion, hvor formuleringen administreres en gang dagligt.
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US49977103P | 2003-09-03 | 2003-09-03 | |
| EP03103275 | 2003-09-03 | ||
| EP03103319 | 2003-09-08 | ||
| EP03103335 | 2003-09-10 | ||
| EP03103668 | 2003-10-02 | ||
| US50848603P | 2003-10-03 | 2003-10-03 | |
| PCT/EP2004/052028 WO2005021001A1 (en) | 2003-09-03 | 2004-09-03 | Combinations of a pyrimidine containing nnrti with rt inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DK1663240T3 true DK1663240T3 (da) | 2015-07-20 |
| DK1663240T4 DK1663240T4 (da) | 2023-04-17 |
Family
ID=43778148
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK04787096.9T DK1663240T4 (da) | 2003-09-03 | 2004-09-03 | Kombinationer af en pyrimidin-holdig nnrti med rt-inhibitorer |
Country Status (9)
| Country | Link |
|---|---|
| KR (2) | KR101539245B1 (da) |
| CN (1) | CN102319433A (da) |
| DK (1) | DK1663240T4 (da) |
| EA (1) | EA014840B1 (da) |
| ES (1) | ES2542017T5 (da) |
| HU (1) | HUE025576T2 (da) |
| PT (1) | PT1663240E (da) |
| SI (1) | SI1663240T2 (da) |
| TW (1) | TWI365744B (da) |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3429B1 (ar) * | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
-
2004
- 2004-09-02 TW TW093126446A patent/TWI365744B/zh active
- 2004-09-03 SI SI200432257T patent/SI1663240T2/sl unknown
- 2004-09-03 CN CN2011102800883A patent/CN102319433A/zh active Pending
- 2004-09-03 ES ES04787096T patent/ES2542017T5/es not_active Expired - Lifetime
- 2004-09-03 KR KR1020117025799A patent/KR101539245B1/ko not_active Expired - Lifetime
- 2004-09-03 DK DK04787096.9T patent/DK1663240T4/da active
- 2004-09-03 HU HUE04787096A patent/HUE025576T2/en unknown
- 2004-09-03 PT PT47870969T patent/PT1663240E/pt unknown
- 2004-09-03 KR KR1020137024817A patent/KR101638999B1/ko not_active Expired - Lifetime
- 2004-09-03 EA EA200600522A patent/EA014840B1/ru active Protection Beyond IP Right Term
Also Published As
| Publication number | Publication date |
|---|---|
| ES2542017T5 (es) | 2023-06-15 |
| PT1663240E (pt) | 2015-09-01 |
| HUE025576T2 (en) | 2016-04-28 |
| CN102319433A (zh) | 2012-01-18 |
| EA014840B1 (ru) | 2011-02-28 |
| KR20130127515A (ko) | 2013-11-22 |
| KR101539245B1 (ko) | 2015-07-27 |
| KR20110132475A (ko) | 2011-12-07 |
| TWI365744B (en) | 2012-06-11 |
| SI1663240T1 (sl) | 2015-10-30 |
| KR101638999B1 (ko) | 2016-07-12 |
| SI1663240T2 (sl) | 2023-05-31 |
| ES2542017T3 (es) | 2015-07-29 |
| DK1663240T4 (da) | 2023-04-17 |
| TW200524612A (en) | 2005-08-01 |
| EA200600522A1 (ru) | 2006-08-25 |
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