HRP20100504T1 - 2-(4-cijanofenil)-6-hidroksilaminopirimidini koji inhibiraju hiv - Google Patents
2-(4-cijanofenil)-6-hidroksilaminopirimidini koji inhibiraju hiv Download PDFInfo
- Publication number
- HRP20100504T1 HRP20100504T1 HR20100504T HRP20100504T HRP20100504T1 HR P20100504 T1 HRP20100504 T1 HR P20100504T1 HR 20100504 T HR20100504 T HR 20100504T HR P20100504 T HRP20100504 T HR P20100504T HR P20100504 T1 HRP20100504 T1 HR P20100504T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound according
- pharmaceutically acceptable
- compounds
- formula
- bromo
- Prior art date
Links
- MMXJEHSOCRNQTF-UHFFFAOYSA-N 4-[4-(hydroxyamino)pyrimidin-2-yl]benzonitrile Chemical class ONC1=CC=NC(C=2C=CC(=CC=2)C#N)=N1 MMXJEHSOCRNQTF-UHFFFAOYSA-N 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 10
- 238000000034 method Methods 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 239000002253 acid Substances 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical compound ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000010076 replication Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Spoj formulefarmaceutski prihvatljiva adicijska sol; ili njegov stereokemijski izomerni oblik, naznačen time daR1 je halo; R2 i R3 svaki nezavisno su C1-6alkil. Patent sadrži još 7 patentnih zahtjeva.
Claims (8)
1. Spoj formule
[image]
farmaceutski prihvatljiva adicijska sol; ili njegov stereokemijski izomerni oblik, naznačen time da
R1 je halo;
R2 i R3 svaki nezavisno su C1-6alkil.
2. Spoj prema zahtjevu 1 naznačen time da R1 je kloro ili bromo.
3. Spoj prema zahtjevu 1 naznačen time da R1 je bromo.
4. Spoj prema bilo kojem zahtjevu 1 - 3 naznačen time da R2 i R3 su metil.
5. Farmaceutski pripravak naznačen time da sadrži farmaceutski prihvatljiv nosač i kao aktivnu tvar terapeutski učinkovitu količinu spoja prema bilo kojem od zahtjeva 1-4.
6. Spoj prema bilo kojem zahtjevu 1 - 4 za upotrebu kao lijek.
7. Postupak za dobivanje pripravka prema zahtjevu 5, naznačen time da se postupak sastoji od bliskog miješanja aktivne tvari i nosača.
8. Postupak za dobivanje spoja prema bilo kojem zahtjevu 1 - 4, naznačen time da se sastoji od reakcije intermedijera (III) sa zaštićenim hidroksilaminom, gdje W predstavlja pogodnu odlaznu skupinu, te se tako dobije intermedijer (II); te se naknadno uklanja zaštita sa intermedijera (II), te se dobivaju krajnji produkti (I):
[image]
te se po želji priprema farmaceutski prihvatljiv oblik kisele adicijske soli od spojeva formule (I) njihovim tretiranjem sa farmaceutski prihvatljivom kiselinom.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP05101707 | 2005-03-04 | ||
PCT/EP2006/060407 WO2006094930A1 (en) | 2005-03-04 | 2006-03-02 | Hiv inhibiting 2-(4-cyanophenyl)-6-hydroxylaminopyrimidines |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20100504T1 true HRP20100504T1 (hr) | 2010-10-31 |
Family
ID=34938904
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20100504T HRP20100504T1 (hr) | 2005-03-04 | 2010-09-13 | 2-(4-cijanofenil)-6-hidroksilaminopirimidini koji inhibiraju hiv |
Country Status (20)
Country | Link |
---|---|
US (2) | US20080214588A1 (hr) |
EP (1) | EP1858861B1 (hr) |
JP (1) | JP5118978B2 (hr) |
CN (1) | CN101133038B (hr) |
AT (1) | ATE473212T1 (hr) |
AU (1) | AU2006222057B2 (hr) |
BR (1) | BRPI0609291B1 (hr) |
CY (1) | CY1111102T1 (hr) |
DE (1) | DE602006015291D1 (hr) |
DK (1) | DK1858861T3 (hr) |
ES (1) | ES2347815T3 (hr) |
HR (1) | HRP20100504T1 (hr) |
ME (1) | ME01229B (hr) |
MX (1) | MX2007010744A (hr) |
PL (1) | PL1858861T3 (hr) |
PT (1) | PT1858861E (hr) |
RS (1) | RS51435B (hr) |
RU (1) | RU2401261C2 (hr) |
SI (1) | SI1858861T1 (hr) |
WO (1) | WO2006094930A1 (hr) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101119976B (zh) * | 2005-02-18 | 2010-12-22 | 泰博特克药品有限公司 | 抑制hiv的2-(4-氰基苯氨基)嘧啶氧化物衍生物 |
RU2469032C2 (ru) | 2006-12-13 | 2012-12-10 | Ф.Хоффманн-Ля Рош Аг | Производные 2-(пиперидин-4-ил)-4-фенокси- или фениламинопиримидина в качестве ненуклеозидных ингибиторов обратной транскриптазы |
EP2342186B1 (en) * | 2009-06-22 | 2014-09-17 | Emcure Pharmaceuticals Limited | Process for synthesis of etravirine |
US8153790B2 (en) | 2009-07-27 | 2012-04-10 | Krizmanic Irena | Process for the preparation and purification of etravirine and intermediates thereof |
CN101993419B (zh) * | 2009-08-20 | 2013-01-16 | 浙江九洲药业股份有限公司 | 一种4-[(5-溴-4,6-二氯-2-嘧啶基)氨基]苯甲腈的制备方法 |
GR1007010B (el) | 2009-10-08 | 2010-10-07 | Χημικα Και Βιοφαρμακευτικα Εργαστηρια Πατρων Αε (Cbl-Patras), | Ινσουλινοειδη πεπτιδια |
WO2011135578A1 (en) | 2010-04-28 | 2011-11-03 | Chetan Balar | Composition comprising chitin and tinosporin for use in the treatment of viral diseases |
US20130123498A1 (en) | 2011-10-19 | 2013-05-16 | Maja Sepelj MAJER | Process for the preparation of etravirine and intermediates in the synthesis thereof |
WO2021167495A1 (en) | 2020-02-19 | 2021-08-26 | Pharmasyntez, Joint Stock Company | Pyrimidine-based bicycles as antiviral agents for the treatment and prevention of hiv infection |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3459731A (en) * | 1966-12-16 | 1969-08-05 | Corn Products Co | Cyclodextrin polyethers and their production |
NZ322907A (en) | 1995-11-23 | 1998-12-23 | Janssen Pharmaceutica Nv | Solid mixtures of cyclodextrins prepared via melt-extrusion |
HU230394B1 (hu) * | 1998-11-10 | 2016-04-28 | Janssen Pharmaceutica N.V. | HIV-vírus szaporodását gátló pirimidin-származékok |
AU775360B2 (en) * | 1999-09-24 | 2004-07-29 | Janssen Pharmaceutica N.V. | Antiviral compositions |
AU782948B2 (en) * | 2000-05-08 | 2005-09-15 | Janssen Pharmaceutica N.V. | Prodrugs of HIV replication inhibiting pyrimidines |
-
2006
- 2006-03-02 AU AU2006222057A patent/AU2006222057B2/en not_active Ceased
- 2006-03-02 AT AT06708609T patent/ATE473212T1/de active
- 2006-03-02 RS RSP-2010/0412A patent/RS51435B/en unknown
- 2006-03-02 SI SI200630779T patent/SI1858861T1/sl unknown
- 2006-03-02 WO PCT/EP2006/060407 patent/WO2006094930A1/en active Application Filing
- 2006-03-02 BR BRPI0609291-8A patent/BRPI0609291B1/pt not_active IP Right Cessation
- 2006-03-02 DE DE602006015291T patent/DE602006015291D1/de active Active
- 2006-03-02 US US11/814,982 patent/US20080214588A1/en not_active Abandoned
- 2006-03-02 ME MEP-2010-147A patent/ME01229B/me unknown
- 2006-03-02 PL PL06708609T patent/PL1858861T3/pl unknown
- 2006-03-02 PT PT06708609T patent/PT1858861E/pt unknown
- 2006-03-02 JP JP2007557513A patent/JP5118978B2/ja active Active
- 2006-03-02 CN CN2006800069458A patent/CN101133038B/zh active Active
- 2006-03-02 RU RU2007136782/04A patent/RU2401261C2/ru active
- 2006-03-02 EP EP06708609A patent/EP1858861B1/en active Active
- 2006-03-02 DK DK06708609.0T patent/DK1858861T3/da active
- 2006-03-02 ES ES06708609T patent/ES2347815T3/es active Active
- 2006-03-02 MX MX2007010744A patent/MX2007010744A/es active IP Right Grant
-
2010
- 2010-01-20 US US12/690,673 patent/US8119801B2/en active Active
- 2010-09-13 HR HR20100504T patent/HRP20100504T1/hr unknown
- 2010-10-06 CY CY20101100890T patent/CY1111102T1/el unknown
Also Published As
Publication number | Publication date |
---|---|
US20080214588A1 (en) | 2008-09-04 |
RU2401261C2 (ru) | 2010-10-10 |
WO2006094930A1 (en) | 2006-09-14 |
MX2007010744A (es) | 2007-09-12 |
ATE473212T1 (de) | 2010-07-15 |
PT1858861E (pt) | 2010-09-16 |
CN101133038A (zh) | 2008-02-27 |
AU2006222057A1 (en) | 2006-09-14 |
SI1858861T1 (sl) | 2010-10-29 |
JP2008531658A (ja) | 2008-08-14 |
PL1858861T3 (pl) | 2010-12-31 |
DE602006015291D1 (de) | 2010-08-19 |
ES2347815T3 (es) | 2010-11-04 |
BRPI0609291B1 (pt) | 2022-02-08 |
ME01229B (me) | 2013-06-20 |
US8119801B2 (en) | 2012-02-21 |
BRPI0609291A2 (pt) | 2010-03-09 |
DK1858861T3 (da) | 2010-11-08 |
AU2006222057B2 (en) | 2012-10-04 |
EP1858861B1 (en) | 2010-07-07 |
EP1858861A1 (en) | 2007-11-28 |
US20100121060A1 (en) | 2010-05-13 |
RS51435B (en) | 2011-04-30 |
CN101133038B (zh) | 2012-06-27 |
RU2007136782A (ru) | 2009-04-10 |
CY1111102T1 (el) | 2015-06-11 |
JP5118978B2 (ja) | 2013-01-16 |
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