PT2376453T - Processos e intermediários para inibidores carbamoilpiridona da integrase de vih - Google Patents
Processos e intermediários para inibidores carbamoilpiridona da integrase de vihInfo
- Publication number
- PT2376453T PT2376453T PT98322324T PT09832232T PT2376453T PT 2376453 T PT2376453 T PT 2376453T PT 98322324 T PT98322324 T PT 98322324T PT 09832232 T PT09832232 T PT 09832232T PT 2376453 T PT2376453 T PT 2376453T
- Authority
- PT
- Portugal
- Prior art keywords
- intermediates
- processes
- hiv integrase
- integrase inhibitors
- carbamoylpyridone
- Prior art date
Links
- OHEKQGOBJIKKIF-AWEZNQCLSA-N (12as)-n-[(4-fluorophenyl)methyl]-7-hydroxy-6,8-dioxo-3,4,12,12a-tetrahydro-2h-pyrido[5,6]pyrazino[2,6-b][1,3]oxazine-9-carboxamide Chemical compound C([C@@H]1OCCCN1C(=O)C1=C(C2=O)O)N1C=C2C(=O)NCC1=CC=C(F)C=C1 OHEKQGOBJIKKIF-AWEZNQCLSA-N 0.000 title 1
- 229940099797 HIV integrase inhibitor Drugs 0.000 title 1
- 239000003084 hiv integrase inhibitor Substances 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
- C07D213/803—Processes of preparation
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
- C07D213/803—Processes of preparation
- C07D213/807—Processes of preparation by oxidation of pyridines or condensed pyridines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US19363608P | 2008-12-11 | 2008-12-11 |
Publications (1)
Publication Number | Publication Date |
---|---|
PT2376453T true PT2376453T (pt) | 2020-01-14 |
Family
ID=42242995
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PT98322324T PT2376453T (pt) | 2008-12-11 | 2009-12-09 | Processos e intermediários para inibidores carbamoilpiridona da integrase de vih |
PT192041473T PT3617194T (pt) | 2008-12-11 | 2009-12-09 | Processos e intermediários para inibidores carbamoilpiridona da integrase do vih |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PT192041473T PT3617194T (pt) | 2008-12-11 | 2009-12-09 | Processos e intermediários para inibidores carbamoilpiridona da integrase do vih |
Country Status (10)
Country | Link |
---|---|
US (2) | US8552187B2 (pt) |
EP (2) | EP2376453B1 (pt) |
JP (1) | JP5572168B2 (pt) |
KR (2) | KR101682058B1 (pt) |
CN (4) | CN107011260A (pt) |
ES (2) | ES2964383T3 (pt) |
PT (2) | PT2376453T (pt) |
SG (1) | SG171731A1 (pt) |
TW (1) | TWI450890B (pt) |
WO (1) | WO2010068262A1 (pt) |
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CA2955957A1 (en) | 2008-12-11 | 2010-06-17 | Shionogi & Co., Ltd. | Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates |
TWI518084B (zh) | 2009-03-26 | 2016-01-21 | 鹽野義製藥股份有限公司 | 哌喃酮與吡啶酮衍生物之製造方法 |
PT2531027E (pt) | 2010-01-27 | 2015-09-16 | Viiv Healthcare Co | Combinação terapêutica compreendendo dolutegravir, abacavir e lamivudina |
TWI582097B (zh) | 2010-03-23 | 2017-05-11 | Viiv醫療保健公司 | 製備胺甲醯吡啶酮衍生物及中間體之方法 |
EP3456721B1 (en) | 2010-08-05 | 2021-02-24 | Shionogi & Co., Ltd | Method of producing compounds having hiv integrase inhivitory activity |
TWI577377B (zh) | 2010-09-16 | 2017-04-11 | Viiv醫療保健公司 | 醫藥組合物 |
AU2012321762A1 (en) | 2011-10-12 | 2014-04-17 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative having integrase-inhibiting activity |
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CN106565747A (zh) * | 2016-11-10 | 2017-04-19 | 顾世海 | 一种制备度鲁特韦的新方法 |
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KR20200066644A (ko) | 2017-10-06 | 2020-06-10 | 시오노기세야쿠 가부시키가이샤 | 치환된 다환성 피리돈 유도체의 입체 선택적인 제조 방법 |
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KR100981063B1 (ko) * | 2008-12-04 | 2010-09-08 | 한일이화주식회사 | 마이크로 파이버 코팅 공법을 이용한 자동차용 내장재의 제조방법 및 그를 이용한 내장재 |
SG171731A1 (en) | 2008-12-11 | 2011-07-28 | Glaxosmithkline Llc | Processes and intermediates for carbamoylpyridone hiv integrase inhibitors |
CA2955957A1 (en) | 2008-12-11 | 2010-06-17 | Shionogi & Co., Ltd. | Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates |
TWI518084B (zh) | 2009-03-26 | 2016-01-21 | 鹽野義製藥股份有限公司 | 哌喃酮與吡啶酮衍生物之製造方法 |
TWI582097B (zh) | 2010-03-23 | 2017-05-11 | Viiv醫療保健公司 | 製備胺甲醯吡啶酮衍生物及中間體之方法 |
EP3456721B1 (en) | 2010-08-05 | 2021-02-24 | Shionogi & Co., Ltd | Method of producing compounds having hiv integrase inhivitory activity |
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2009
- 2009-12-09 SG SG2011035078A patent/SG171731A1/en unknown
- 2009-12-09 CN CN201710119972.6A patent/CN107011260A/zh active Pending
- 2009-12-09 CN CN201710119973.0A patent/CN106986823A/zh active Pending
- 2009-12-09 WO PCT/US2009/006461 patent/WO2010068262A1/en active Application Filing
- 2009-12-09 PT PT98322324T patent/PT2376453T/pt unknown
- 2009-12-09 KR KR1020167030006A patent/KR101682058B1/ko active IP Right Grant
- 2009-12-09 CN CN201510071074.9A patent/CN104788367A/zh active Pending
- 2009-12-09 JP JP2011540693A patent/JP5572168B2/ja active Active
- 2009-12-09 CN CN200980149670.7A patent/CN102245572B/zh active Active
- 2009-12-09 KR KR1020117016063A patent/KR101678563B1/ko active IP Right Grant
- 2009-12-09 EP EP09832232.4A patent/EP2376453B1/en active Active
- 2009-12-09 PT PT192041473T patent/PT3617194T/pt unknown
- 2009-12-09 EP EP19204147.3A patent/EP3617194B1/en active Active
- 2009-12-09 ES ES19204147T patent/ES2964383T3/es active Active
- 2009-12-09 US US13/128,457 patent/US8552187B2/en active Active
- 2009-12-09 ES ES09832232T patent/ES2763540T3/es active Active
- 2009-12-11 TW TW098142599A patent/TWI450890B/zh active
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2013
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Also Published As
Publication number | Publication date |
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KR20110096574A (ko) | 2011-08-30 |
ES2964383T3 (es) | 2024-04-05 |
ES2763540T3 (es) | 2020-05-29 |
EP2376453B1 (en) | 2019-11-20 |
US20140005405A1 (en) | 2014-01-02 |
EP2376453A4 (en) | 2012-06-27 |
EP3617194B1 (en) | 2023-11-08 |
TW201029973A (en) | 2010-08-16 |
SG171731A1 (en) | 2011-07-28 |
JP5572168B2 (ja) | 2014-08-13 |
EP2376453A1 (en) | 2011-10-19 |
CN102245572A (zh) | 2011-11-16 |
US8669362B2 (en) | 2014-03-11 |
KR101682058B1 (ko) | 2016-12-02 |
EP3617194A1 (en) | 2020-03-04 |
KR101678563B1 (ko) | 2016-11-22 |
CN102245572B (zh) | 2015-03-25 |
US20110263855A1 (en) | 2011-10-27 |
CN104788367A (zh) | 2015-07-22 |
US8552187B2 (en) | 2013-10-08 |
CN107011260A (zh) | 2017-08-04 |
CN106986823A (zh) | 2017-07-28 |
KR20160127179A (ko) | 2016-11-02 |
WO2010068262A1 (en) | 2010-06-17 |
JP2012511574A (ja) | 2012-05-24 |
TWI450890B (zh) | 2014-09-01 |
PT3617194T (pt) | 2023-11-27 |
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