HRP20110830T1 - Derivati 1-[2', 3'-dideoksi-3'-c-(hidroksimetil) - beta-d-eritro-pentofuranosil] citozina kao hiv inhibitori - Google Patents
Derivati 1-[2', 3'-dideoksi-3'-c-(hidroksimetil) - beta-d-eritro-pentofuranosil] citozina kao hiv inhibitori Download PDFInfo
- Publication number
- HRP20110830T1 HRP20110830T1 HR20110830T HRP20110830T HRP20110830T1 HR P20110830 T1 HRP20110830 T1 HR P20110830T1 HR 20110830 T HR20110830 T HR 20110830T HR P20110830 T HRP20110830 T HR P20110830T HR P20110830 T1 HRP20110830 T1 HR P20110830T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound according
- compound
- hiv
- pharmaceutically acceptable
- multidrug
- Prior art date
Links
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical class NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 title 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- 239000003814 drug Substances 0.000 claims abstract 3
- 230000035772 mutation Effects 0.000 claims abstract 3
- 229940079593 drug Drugs 0.000 claims abstract 2
- 150000002148 esters Chemical class 0.000 claims 4
- 102100034343 Integrase Human genes 0.000 claims 3
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- YCXAJSYDEWTBPT-UHFFFAOYSA-N 13-(4-amino-2-oxopyrimidin-1-yl)-3,9,12-trioxabicyclo[9.3.0]tetradecane-4,8-dione Chemical compound O=C1N=C(N)C=CN1C1OC2COC(=O)CCCC(=O)OCC2C1 YCXAJSYDEWTBPT-UHFFFAOYSA-N 0.000 claims 1
- QSCFYTREZLHBBB-UHFFFAOYSA-N 2-(4-amino-2-oxopyrimidin-1-yl)-2,3,3a,4,7,8,11,11a-octahydrofuro[2,3-c][1,6]dioxecine-6,9-dione Chemical compound O=C1N=C(N)C=CN1C1OC2COC(=O)CCC(=O)OCC2C1 QSCFYTREZLHBBB-UHFFFAOYSA-N 0.000 claims 1
- 108020004414 DNA Proteins 0.000 claims 1
- 102000053602 DNA Human genes 0.000 claims 1
- 230000037430 deletion Effects 0.000 claims 1
- 238000012217 deletion Methods 0.000 claims 1
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 claims 1
- 235000011180 diphosphates Nutrition 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 241001430294 unidentified retrovirus Species 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Spoj formule Igdje: R1 je nezavisno H, -OR3, -NHR4, C1-C4 alkil; ili, kada je n jednako 2, susjedni R1 zajedno definiraju olefinsku vezu; R2 je H; ili kada je susjedni R1 jednak C1-C4 alkil, tada R2 također može biti C1-C4 alkil; ili kada je susjedni R1 jednak -OR3, tada R2 također može biti -C(=O)OH ili farmaceutski prihvatljivi ester spoja; R3 je nezavisno H, ili farmaceutski prihvatljivi ester spoja; R4 je nezavisno H ili farmaceutski prihvatljivi amid spoja; R5 je H; R6 je H; n je 1, 2 ili 3; i njegove farmaceutski prihvatljive soli. Patent sadrži još 19 patentnih zahtjeva.
Claims (20)
1. Spoj formule I
[image]
gdje:
R1 je nezavisno H, -OR3, -NHR4, C1-C4 alkil;
ili, kada je n jednako 2, susjedni R1 zajedno definiraju olefinsku vezu;
R2 je H;
ili kada je susjedni R1 jednak C1-C4 alkil, tada R2 također može biti C1-C4 alkil;
ili kada je susjedni R1 jednak -OR3, tada R2 također može biti -C(=O)OH ili farmaceutski prihvatljivi ester spoja;
R3 je nezavisno H, ili farmaceutski prihvatljivi ester spoja;
R4 je nezavisno H ili farmaceutski prihvatljivi amid spoja;
R5 je H;
R6 je H;
n je 1, 2 ili 3;
i njegove farmaceutski prihvatljive soli.
2. Spoj prema zahtjevu 1, gdje n je 1.
3. Spoj prema zahtjevu 2, gdje R1 je H, OH ili njegov farmaceutski prihvatljivi ester.
4. Spoj prema zahtjevu 1, gdje n je 2.
5. Spoj prema zahtjevu 4, gdje prvi R1 je H; i drugi R1 je -OH ili -NH2, ili njegov farmaceutski prihvatljivi ester ili amid.
6. Spoj prema zahtjevu 5, s formulom:
[image]
gdje su R5 i R6 kako je definirano u zahtjevu 1 i R1* je spomenuti drugi R1.
7. Spoj prema zahtjevu 4, označen kao 2-(4-amino-2-okso-2H-pirimidin-1-il)-oktahidro-1,5,10-trioksaciklopentaciklodecen-6,9-dion; ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema zahtjevu 1, gdje n je 3.
9. Spoj prema zahtjevu 8, označen kao 2-(4-amino-2-okso-2H-pirimidin-1-il)-oktahidro-1,5,11-trioksa-ciklopentacikloundecen-6,10-dion, ili njegova farmaceutski prihvatljiva sol.
10. Farmaceutski oblik koji sadrži spoj prema bilo kojem od zahtjeva 1 do 9 zajedno s farmaceutski prihvatljivim nosačem ili pomoćnom tvari.
11. Spoj prema bilo kojem od zahtjeva 1 do 9 za uporabu kao lijek.
12. Spoj prema zahtjevu 11, za uporabu u liječenju ili prevenciji HIV-a.
13. Spoj za uporabu prema zahtjevu 12, gdje je HIV multirezistentni HIV.
14. Spoj prema zahtjevu 13, gdje reverzna transkriptaza multirezistentnog HIV-a nosi barem jednu mutaciju koja omogućuje da obvezni krajevi lanca nukleozid- ili nukleotid- fosfati budu izrezani iz nascentnog (rastućeg) DNA lanca pomoću ATP- ili pirofosfat- posredovanog izrezivanja.
15. Spoj prema zahtjevu 14, gdje reverzna transkriptaza nosi barem jedan od sljedećih genotipskih obrazaca:
(a) M41, ±D67, L210 i T215;
(b) D67, K70 i K219;
(c) T69S-XX; ili
(d) ▲67 (delecija na 67).
16. Spoj prema zahtjevu 15 gdje reverzna transkriptaza nosi barem 3 mutacije.
17. Uporaba prema bilo kojem od zahtjeva 1 do 9 za proizvodnju lijeka za liječenje ili prevenciju zaraze HIV-om.
18. Uporaba prema zahtjevu 17, gdje je HIV multirezistentni HIV.
19. Spoj prema zahtjevu 11 za uporabu u liječenju ili prevenciji zaraze HIV-om.
20. Spoj za uporabu prema zahtjevu 19, gdje je HIV multirezistentni HIV.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0513835.9A GB0513835D0 (en) | 2005-07-07 | 2005-07-07 | HIV inhibitors |
| PCT/EP2006/063919 WO2007006707A1 (en) | 2005-07-07 | 2006-07-05 | 1- [2' , 3' -dideoxy-3' c- (hydroxymethyl) - beta-d-erythro-pentofuranosyl] cytosine derivatives as hiv inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20110830T1 true HRP20110830T1 (hr) | 2011-12-31 |
Family
ID=34856749
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20110830T HRP20110830T1 (hr) | 2005-07-07 | 2011-11-11 | Derivati 1-[2', 3'-dideoksi-3'-c-(hidroksimetil) - beta-d-eritro-pentofuranosil] citozina kao hiv inhibitori |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US7888367B2 (hr) |
| EP (2) | EP2336135A3 (hr) |
| JP (1) | JP5174660B2 (hr) |
| CN (1) | CN101213198B (hr) |
| AT (1) | ATE527267T1 (hr) |
| AU (1) | AU2006268743C1 (hr) |
| BR (1) | BRPI0612678A2 (hr) |
| CA (1) | CA2610210A1 (hr) |
| CY (1) | CY1112164T1 (hr) |
| DK (1) | DK1899352T3 (hr) |
| ES (1) | ES2373743T3 (hr) |
| GB (1) | GB0513835D0 (hr) |
| HK (1) | HK1122798A1 (hr) |
| HR (1) | HRP20110830T1 (hr) |
| MX (1) | MX2008000221A (hr) |
| PL (1) | PL1899352T3 (hr) |
| PT (1) | PT1899352E (hr) |
| WO (1) | WO2007006707A1 (hr) |
| ZA (1) | ZA200710662B (hr) |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8810907D0 (en) | 1988-05-09 | 1988-06-15 | British Telecomm | Fluoride glass optical coupler & method of manufacture |
| ZA902631B (en) * | 1989-04-06 | 1990-12-28 | Bristol Myers Squibb Co | 3'-substituted methyl nucleosides as antiviral agents |
| US5866775A (en) | 1990-09-28 | 1999-02-02 | Monsanto Company | Glyphosate-tolerant 5-enolpyruvyl-3-phosphoshikimate synthases |
| US5627160A (en) * | 1993-05-25 | 1997-05-06 | Yale University | L-2',3'-dideoxy nucleoside analogs as anti-hepatitis B (HBV) and anti-HIV agents |
| AU697612B2 (en) * | 1994-05-31 | 1998-10-15 | Medivir Ab | Post exposure prevention of HIV |
| US5612319A (en) | 1994-05-31 | 1997-03-18 | Medivir Ab | Postexposure prevention of HIV infection or seroconversion |
| ATE200900T1 (de) | 1997-08-15 | 2001-05-15 | Medivir Ab | Analoge nukleoside, wie antivirale einschliesslich inhibitoren der retroviralen reverstranskriptase und der dna polymerase des hepatitis b virus |
| BR0110023A (pt) * | 2000-04-13 | 2003-12-30 | Pharmasset Ltd | Derivados de nucleosìdeo 3'-ou-2' substituìdos para tratamento de infecções por vìrus da hepatite |
| US7109931B2 (en) | 2004-06-18 | 2006-09-19 | Centurion Wireless Technologies, Inc. | Method and apparatus to control an antenna efficiency test device |
| WO2006070004A1 (en) * | 2004-12-30 | 2006-07-06 | Medivir Ab | Compounds useful in the treatment of hiv |
-
2005
- 2005-07-07 GB GBGB0513835.9A patent/GB0513835D0/en not_active Ceased
-
2006
- 2006-07-05 US US11/994,633 patent/US7888367B2/en not_active Expired - Fee Related
- 2006-07-05 CN CN2006800244086A patent/CN101213198B/zh not_active Expired - Fee Related
- 2006-07-05 CA CA002610210A patent/CA2610210A1/en not_active Abandoned
- 2006-07-05 PL PL06777595T patent/PL1899352T3/pl unknown
- 2006-07-05 BR BRPI0612678-2A patent/BRPI0612678A2/pt not_active IP Right Cessation
- 2006-07-05 ES ES06777595T patent/ES2373743T3/es active Active
- 2006-07-05 JP JP2008519938A patent/JP5174660B2/ja not_active Expired - Fee Related
- 2006-07-05 MX MX2008000221A patent/MX2008000221A/es active IP Right Grant
- 2006-07-05 WO PCT/EP2006/063919 patent/WO2007006707A1/en active Application Filing
- 2006-07-05 EP EP11161299A patent/EP2336135A3/en not_active Withdrawn
- 2006-07-05 EP EP06777595A patent/EP1899352B1/en active Active
- 2006-07-05 AU AU2006268743A patent/AU2006268743C1/en not_active Ceased
- 2006-07-05 AT AT06777595T patent/ATE527267T1/de not_active IP Right Cessation
- 2006-07-05 PT PT06777595T patent/PT1899352E/pt unknown
- 2006-07-05 DK DK06777595.7T patent/DK1899352T3/da active
-
2007
- 2007-12-06 ZA ZA200710662A patent/ZA200710662B/xx unknown
-
2008
- 2008-12-19 HK HK08113816.7A patent/HK1122798A1/xx not_active IP Right Cessation
-
2010
- 2010-12-30 US US12/982,667 patent/US8143396B2/en not_active Expired - Fee Related
-
2011
- 2011-11-11 HR HR20110830T patent/HRP20110830T1/hr unknown
- 2011-12-22 CY CY20111101278T patent/CY1112164T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CY1112164T1 (el) | 2015-12-09 |
| CA2610210A1 (en) | 2007-01-18 |
| CN101213198B (zh) | 2011-08-03 |
| GB0513835D0 (en) | 2005-08-10 |
| EP1899352B1 (en) | 2011-10-05 |
| HK1122798A1 (en) | 2009-05-29 |
| US20110112294A1 (en) | 2011-05-12 |
| WO2007006707A1 (en) | 2007-01-18 |
| PL1899352T3 (pl) | 2012-03-30 |
| AU2006268743B2 (en) | 2010-07-29 |
| JP5174660B2 (ja) | 2013-04-03 |
| JP2008545002A (ja) | 2008-12-11 |
| ZA200710662B (en) | 2008-11-26 |
| US8143396B2 (en) | 2012-03-27 |
| EP2336135A2 (en) | 2011-06-22 |
| US7888367B2 (en) | 2011-02-15 |
| AU2006268743A1 (en) | 2007-01-18 |
| CN101213198A (zh) | 2008-07-02 |
| EP2336135A3 (en) | 2011-07-27 |
| BRPI0612678A2 (pt) | 2010-11-30 |
| EP1899352A1 (en) | 2008-03-19 |
| PT1899352E (pt) | 2012-01-05 |
| ES2373743T3 (es) | 2012-02-08 |
| AU2006268743C1 (en) | 2010-12-16 |
| US20080221140A1 (en) | 2008-09-11 |
| ATE527267T1 (de) | 2011-10-15 |
| MX2008000221A (es) | 2008-03-18 |
| DK1899352T3 (da) | 2012-01-30 |
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