AU2012255029B2 - Processes and intermediates for preparing anti-HIV agents - Google Patents
Processes and intermediates for preparing anti-HIV agents Download PDFInfo
- Publication number
- AU2012255029B2 AU2012255029B2 AU2012255029A AU2012255029A AU2012255029B2 AU 2012255029 B2 AU2012255029 B2 AU 2012255029B2 AU 2012255029 A AU2012255029 A AU 2012255029A AU 2012255029 A AU2012255029 A AU 2012255029A AU 2012255029 B2 AU2012255029 B2 AU 2012255029B2
- Authority
- AU
- Australia
- Prior art keywords
- compound
- formula
- salt
- alkyl
- pho
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
- C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4075—Esters with hydroxyalkyl compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/44—Amides thereof
- C07F9/4434—Amides thereof the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4449—Esters with hydroxyaryl compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
- C07H19/173—Purine radicals with 2-deoxyribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
-
- 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
- A61K31/66—Phosphorus compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Saccharide Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2016208292A AU2016208292B2 (en) | 2011-05-19 | 2016-07-26 | Processes and intermediates for preparing anti-HIV agents |
| AU2018200776A AU2018200776B2 (en) | 2011-05-19 | 2018-02-01 | Processes and intermediates for preparing anti-HIV agents |
| AU2019226278A AU2019226278A1 (en) | 2011-05-19 | 2019-09-09 | Processes and intermediates for preparing anti-hiv agents |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161488133P | 2011-05-19 | 2011-05-19 | |
| US61/488,133 | 2011-05-19 | ||
| PCT/US2012/038615 WO2012159047A1 (en) | 2011-05-19 | 2012-05-18 | Processes and intermediates for preparing anti-hiv agents |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2016208292A Division AU2016208292B2 (en) | 2011-05-19 | 2016-07-26 | Processes and intermediates for preparing anti-HIV agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2012255029A1 AU2012255029A1 (en) | 2013-05-02 |
| AU2012255029B2 true AU2012255029B2 (en) | 2016-04-28 |
Family
ID=46208163
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2012255029A Active AU2012255029B2 (en) | 2011-05-19 | 2012-05-18 | Processes and intermediates for preparing anti-HIV agents |
| AU2016208292A Active AU2016208292B2 (en) | 2011-05-19 | 2016-07-26 | Processes and intermediates for preparing anti-HIV agents |
| AU2018200776A Active AU2018200776B2 (en) | 2011-05-19 | 2018-02-01 | Processes and intermediates for preparing anti-HIV agents |
| AU2019226278A Abandoned AU2019226278A1 (en) | 2011-05-19 | 2019-09-09 | Processes and intermediates for preparing anti-hiv agents |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2016208292A Active AU2016208292B2 (en) | 2011-05-19 | 2016-07-26 | Processes and intermediates for preparing anti-HIV agents |
| AU2018200776A Active AU2018200776B2 (en) | 2011-05-19 | 2018-02-01 | Processes and intermediates for preparing anti-HIV agents |
| AU2019226278A Abandoned AU2019226278A1 (en) | 2011-05-19 | 2019-09-09 | Processes and intermediates for preparing anti-hiv agents |
Country Status (10)
| Country | Link |
|---|---|
| US (5) | US8987437B2 (OSRAM) |
| EP (3) | EP3450438A1 (OSRAM) |
| JP (4) | JP5951757B2 (OSRAM) |
| AR (1) | AR086492A1 (OSRAM) |
| AU (4) | AU2012255029B2 (OSRAM) |
| CA (1) | CA2835932C (OSRAM) |
| ES (2) | ES2629913T3 (OSRAM) |
| PT (2) | PT2710019T (OSRAM) |
| TW (1) | TWI635093B (OSRAM) |
| WO (1) | WO2012159047A1 (OSRAM) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3450438A1 (en) | 2011-05-19 | 2019-03-06 | Gilead Sciences, Inc. | Processes and intermediates for preparing anti-hiv agents |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| US20180085387A1 (en) | 2016-09-27 | 2018-03-29 | Gilead Sciences, Inc. | Therapeutic compositions for treatment of human immunodeficiency virus |
| ES2892402T3 (es) | 2017-08-01 | 2022-02-04 | Gilead Sciences Inc | Formas cristalinas de ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il)oxi)metil)(fenoxi)fosforil)-L-alaninato de etilo para tratar infecciones virales |
| WO2019165374A1 (en) | 2018-02-26 | 2019-08-29 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds as hbv replication inhibitors |
| CN114409706B (zh) * | 2019-07-01 | 2023-11-28 | 上海医药工业研究院 | 一种苯基氢膦酸酯及其中间体的制备方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050009043A1 (en) * | 2000-07-21 | 2005-01-13 | Gilead Sciences, Inc. | Prodrugs of phosphonate nucleotide analogues |
| WO2007014352A2 (en) * | 2005-07-27 | 2007-02-01 | Gilead Sciences, Inc. | Antiviral phosphonate conjugates for inhibition of hiv |
| WO2010005986A1 (en) * | 2008-07-08 | 2010-01-14 | Gilead Sciences, Inc. | Salts of hiv inhibitor compounds |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US599431A (en) | 1898-02-22 | Clothes-wringer | ||
| GB835785A (en) * | 1956-04-30 | 1960-05-25 | Victor Chemical Works | Method of making diaryl phosphites |
| MX3898E (es) * | 1975-12-29 | 1981-09-10 | Monsanto Co | Procedimiento mejorado para la preparacion de triesteres de n-fosfonometilglicina |
| US4198355A (en) | 1977-03-28 | 1980-04-15 | Mobil Oil Corporation | Preparation of tertiary alkylphosphorodichloridite derivatives |
| US5459256A (en) * | 1987-04-17 | 1995-10-17 | The Government Of The United States Of America As Represented By The Department Of Health And Human Services | Lipophilic, aminohydrolase-activated prodrugs |
| HU906976D0 (en) | 1989-11-13 | 1991-05-28 | Bristol Myers Squibb Co | Process for producing 2', 3'-didesoxy-2'-fluoarabinonucleoside analogues |
| US5672697A (en) * | 1991-02-08 | 1997-09-30 | Gilead Sciences, Inc. | Nucleoside 5'-methylene phosphonates |
| JP4942915B2 (ja) * | 2002-04-26 | 2012-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖプロテアーゼ阻害剤化合物のホスホネートアナログの細胞蓄積 |
| EP1628685B1 (en) * | 2003-04-25 | 2010-12-08 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
| JP2010535701A (ja) * | 2003-04-25 | 2010-11-25 | ギリアード サイエンシーズ， インコーポレイテッド | 抗癌ホスホネートアナログ |
| HRP20070043A2 (hr) * | 2004-07-16 | 2007-07-31 | Gilead Sciences | Antivirusna sredstva |
| WO2006110157A2 (en) | 2004-07-27 | 2006-10-19 | Gilead Sciences, Inc. | Nucleoside phosphonate conjugates as anti hiv agents |
| CZ2008547A3 (cs) * | 2006-03-17 | 2009-06-10 | Invista Technologies S. A. R. L. | Zpusob purifikace triorganofosfitu ošetrením bazickým aditivem |
| US8324179B2 (en) * | 2007-02-09 | 2012-12-04 | Gilead Sciences, Inc. | Nucleoside analogs for antiviral treatment |
| WO2011003018A2 (en) * | 2009-07-01 | 2011-01-06 | Cornell University | Halogenated 2-deoxy-lactones, 2'-deoxy--nucleosides, and derivatives thereof |
| EP3450438A1 (en) | 2011-05-19 | 2019-03-06 | Gilead Sciences, Inc. | Processes and intermediates for preparing anti-hiv agents |
-
2012
- 2012-05-18 EP EP18200819.3A patent/EP3450438A1/en not_active Withdrawn
- 2012-05-18 AR ARP120101777A patent/AR086492A1/es unknown
- 2012-05-18 PT PT127255701T patent/PT2710019T/pt unknown
- 2012-05-18 TW TW101117811A patent/TWI635093B/zh active
- 2012-05-18 AU AU2012255029A patent/AU2012255029B2/en active Active
- 2012-05-18 EP EP16204289.9A patent/EP3199537B1/en active Active
- 2012-05-18 JP JP2014511589A patent/JP5951757B2/ja active Active
- 2012-05-18 PT PT16204289T patent/PT3199537T/pt unknown
- 2012-05-18 CA CA2835932A patent/CA2835932C/en active Active
- 2012-05-18 US US13/475,569 patent/US8987437B2/en active Active
- 2012-05-18 ES ES12725570.1T patent/ES2629913T3/es active Active
- 2012-05-18 EP EP12725570.1A patent/EP2710019B1/en active Active
- 2012-05-18 ES ES16204289T patent/ES2700470T3/es active Active
- 2012-05-18 WO PCT/US2012/038615 patent/WO2012159047A1/en not_active Ceased
-
2015
- 2015-02-05 US US14/615,357 patent/US9296779B2/en active Active
-
2016
- 2016-01-15 JP JP2016005955A patent/JP6282295B2/ja active Active
- 2016-02-17 US US15/046,399 patent/US9783567B2/en active Active
- 2016-07-26 AU AU2016208292A patent/AU2016208292B2/en active Active
-
2017
- 2017-02-06 JP JP2017019959A patent/JP6621772B2/ja active Active
- 2017-09-06 US US15/697,136 patent/US10196419B2/en active Active
-
2018
- 2018-02-01 AU AU2018200776A patent/AU2018200776B2/en active Active
- 2018-12-20 US US16/226,811 patent/US20190359644A1/en not_active Abandoned
-
2019
- 2019-02-01 JP JP2019017324A patent/JP2019089808A/ja active Pending
- 2019-09-09 AU AU2019226278A patent/AU2019226278A1/en not_active Abandoned
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050009043A1 (en) * | 2000-07-21 | 2005-01-13 | Gilead Sciences, Inc. | Prodrugs of phosphonate nucleotide analogues |
| WO2007014352A2 (en) * | 2005-07-27 | 2007-02-01 | Gilead Sciences, Inc. | Antiviral phosphonate conjugates for inhibition of hiv |
| WO2010005986A1 (en) * | 2008-07-08 | 2010-01-14 | Gilead Sciences, Inc. | Salts of hiv inhibitor compounds |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2018200776B2 (en) | Processes and intermediates for preparing anti-HIV agents | |
| AU2016228317B2 (en) | Methods for preparing anti-viral nucleotide analogs | |
| JPWO2019208571A1 (ja) | アミダイト化合物及び該化合物を用いたポリヌクレオチドの製造方法 | |
| MX2014009344A (es) | Metodos e intermediarios para preparar agentes farmaceuticos. | |
| CN112175003A (zh) | 一种苯基氢膦酸酯及其中间体的制备方法 | |
| KR101832238B1 (ko) | 신규한 설포닐옥시메틸포스포네이트 유도체 및 이를 이용한 다이아이소프로필 ((1-(트리틸옥시메틸)-사이클로프로필)옥시)메틸 포스포네이트의 제조방법 | |
| NZ618939B2 (en) | Processes and intermediates for preparing anti-hiv agents | |
| HK1239695B (en) | Processes and intermediates for preparing anti-hiv agents | |
| HK1196133A (en) | Processes and intermediates for preparing anti-hiv agents | |
| HK1196133B (en) | Processes and intermediates for preparing anti-hiv agents | |
| HK1239695A1 (en) | Processes and intermediates for preparing anti-hiv agents | |
| HK40004474A (en) | Processes and intermediates for preparing anti-hiv agents | |
| JPH0931075A (ja) | カルバペネム中間体の製造方法 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| DA2 | Applications for amendment section 104 |
Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE APPLICANT TO READ GILEAD SCIENCES, INC. . |
|
| FGA | Letters patent sealed or granted (standard patent) | ||
| HB | Alteration of name in register |
Owner name: GILEAD SCIENCES, INC. Free format text: FORMER NAME(S): KENNETH M. KENT; ALAN SCOTT TRIMAN; DUONG DUC-PHI TRAN; BENJAMIN R. GRAETZ; STEVEN PFEIFFER; BRANDON HEATH BROWN; RICHARD P. POLNIASZEK; RICHARD HUNG CHIU YU; GILEAD SCIENCES, INC.; KEIKO SUJINO |