JP2011246469A5 - - Google Patents
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- Publication number
- JP2011246469A5 JP2011246469A5 JP2011138647A JP2011138647A JP2011246469A5 JP 2011246469 A5 JP2011246469 A5 JP 2011246469A5 JP 2011138647 A JP2011138647 A JP 2011138647A JP 2011138647 A JP2011138647 A JP 2011138647A JP 2011246469 A5 JP2011246469 A5 JP 2011246469A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pivaloyl
- mesylate
- benzoyl
- hydrogen succinate
- 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.)
- Pending
Links
- LULAYUGMBFYYEX-UHFFFAOYSA-N 3-chlorobenzoic acid Chemical compound OC(=O)C1=CC=CC(Cl)=C1 LULAYUGMBFYYEX-UHFFFAOYSA-N 0.000 claims 78
- 125000000217 alkyl group Chemical group 0.000 claims 62
- YQTCQNIPQMJNTI-UHFFFAOYSA-N 2,2-dimethylpropan-1-one Chemical group CC(C)(C)[C]=O YQTCQNIPQMJNTI-UHFFFAOYSA-N 0.000 claims 41
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 41
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 41
- KDYFGRWQOYBRFD-UHFFFAOYSA-M succinate(1-) Chemical compound OC(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-M 0.000 claims 41
- 150000001875 compounds Chemical class 0.000 claims 25
- 239000000203 mixture Substances 0.000 claims 25
- 239000001177 diphosphate Substances 0.000 claims 20
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 claims 20
- 235000011180 diphosphates Nutrition 0.000 claims 20
- 150000004712 monophosphates Chemical class 0.000 claims 20
- 239000001226 triphosphate Substances 0.000 claims 20
- 235000011178 triphosphate Nutrition 0.000 claims 20
- 125000002264 triphosphate group Chemical group [H]OP(=O)(O[H])OP(=O)(O[H])OP(=O)(O[H])O* 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 229960004413 flucytosine Drugs 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 claims 6
- 208000002672 hepatitis B Diseases 0.000 claims 4
- 241001465754 Metazoa Species 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- IKCLCGXPQILATA-UHFFFAOYSA-N 2-chlorobenzoic acid Chemical compound OC(=O)C1=CC=CC=C1Cl IKCLCGXPQILATA-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10711698P | 1998-11-05 | 1998-11-05 | |
| US60/107,116 | 1998-11-05 | ||
| US11565399P | 1999-01-13 | 1999-01-13 | |
| US60/115,653 | 1999-01-13 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000579613A Division JP2002528554A (ja) | 1998-11-05 | 1999-11-05 | Ｂ型肝炎ウイルス活性を持ったヌクレオシド |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011246469A JP2011246469A (ja) | 2011-12-08 |
| JP2011246469A5 true JP2011246469A5 (enExample) | 2012-09-06 |
Family
ID=26804401
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000579613A Withdrawn JP2002528554A (ja) | 1998-11-05 | 1999-11-05 | Ｂ型肝炎ウイルス活性を持ったヌクレオシド |
| JP2011138647A Pending JP2011246469A (ja) | 1998-11-05 | 2011-06-22 | Ｂ型肝炎ウイルス活性を持ったヌクレオシド |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000579613A Withdrawn JP2002528554A (ja) | 1998-11-05 | 1999-11-05 | Ｂ型肝炎ウイルス活性を持ったヌクレオシド |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US6458773B1 (enExample) |
| EP (1) | EP1124839B1 (enExample) |
| JP (2) | JP2002528554A (enExample) |
| KR (1) | KR100618028B1 (enExample) |
| CN (1) | CN1216893C (enExample) |
| AT (1) | ATE315574T1 (enExample) |
| AU (1) | AU774720B2 (enExample) |
| BR (1) | BR9915555A (enExample) |
| CA (1) | CA2348470C (enExample) |
| DE (1) | DE69929460D1 (enExample) |
| IL (2) | IL142983A0 (enExample) |
| MX (1) | MXPA01004504A (enExample) |
| WO (1) | WO2000026225A2 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2787199A (en) * | 1998-02-25 | 1999-09-15 | Emory University | 2'-fluoronucleosides |
| MY164523A (en) | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
| JP5230052B2 (ja) * | 2000-05-26 | 2013-07-10 | イデニクス（ケイマン）リミテツド | フラビウイルスおよびペスチウイルス治療のための方法および組成物 |
| EP1387850A2 (en) | 2001-05-18 | 2004-02-11 | Rakesh Kumar | Antiviral nucleosides |
| US7608600B2 (en) * | 2002-06-28 | 2009-10-27 | Idenix Pharmaceuticals, Inc. | Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections |
| NZ537662A (en) | 2002-06-28 | 2007-10-26 | Idenix Cayman Ltd | 2'-C-methyl-3'-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections |
| AP2005003213A0 (en) | 2002-06-28 | 2005-03-31 | Univ Cagliari | 2'-C-methyl-3'-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections. |
| US20040067877A1 (en) | 2002-08-01 | 2004-04-08 | Schinazi Raymond F. | 2', 3'-Dideoxynucleoside analogues for the treatment or prevention of Flaviviridae infections |
| BR0315795A (pt) * | 2002-10-31 | 2005-09-13 | Metabasis Therapeutics Inc | Pró-medicamentos de monofosfato de citarabina |
| US7824851B2 (en) | 2002-11-15 | 2010-11-02 | Idenix Pharmaceuticals, Inc. | 2′-branched nucleosides and Flaviviridae mutation |
| MXPA05006230A (es) | 2002-12-12 | 2005-09-20 | Idenix Cayman Ltd | Proceso para la produccion de nucleosidos ramificados-2'. |
| ES2422290T3 (es) | 2005-12-23 | 2013-09-10 | Idenix Pharmaceuticals Inc | Procedimiento para preparar un producto intermedio sintético para la preparación de nucleósidos ramificados |
| AU2015217221A1 (en) | 2014-02-13 | 2016-08-11 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and their uses |
| JP2017520545A (ja) | 2014-07-02 | 2017-07-27 | リガンド・ファーマシューティカルズ・インコーポレイテッド | プロドラッグ化合物およびそれらの使用 |
| CA3087932A1 (en) | 2018-01-09 | 2019-07-18 | Ligand Pharmaceuticals, Inc. | Acetal compounds and therapeutic uses thereof |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4681933A (en) | 1986-05-01 | 1987-07-21 | University Of Georgia Research Foundation, Inc. | 2',3'-dideoxy-5-substituted uridines and related compounds as antiviral agents |
| US5084445A (en) | 1986-05-01 | 1992-01-28 | University Of Georgia Research Foundation, Inc. | 3'-azido-2',3'-dideoxy-5-methylcytidine |
| US4916122A (en) | 1987-01-28 | 1990-04-10 | University Of Georgia Research Foundation, Inc. | 3'-Azido-2',3'-dideoxyuridine anti-retroviral composition |
| US5077279A (en) | 1986-05-01 | 1991-12-31 | University Of Georgia Research Foundation, Inc. | 3'-azido-2',3'-dideoxy-5-methylcytidine anti-viral composition |
| US4841039A (en) | 1986-05-01 | 1989-06-20 | Emory University | 2',3'-dideoxy-5-substituted uridines and related compounds as antiviral agents |
| US5190926A (en) | 1987-01-28 | 1993-03-02 | University Of Georgia Research Foundation, Inc. | 3'-azido-2',3'-dideoxypyrimidines and related compounds as antiviral agents |
| NZ228645A (en) | 1988-04-11 | 1991-09-25 | Iaf Biochem Int | 1,3-dioxolane derivatives substituted in the 5th position by a purine or pyrimidine radical; treatment of viral infections |
| US5041449A (en) | 1988-04-11 | 1991-08-20 | Iaf Biochem International, Inc. | 4-(nucleoside base)-substituted-1,3-dioxolanes useful for treatment of retroviral infections |
| US5047407A (en) | 1989-02-08 | 1991-09-10 | Iaf Biochem International, Inc. | 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties |
| DD293498A5 (de) * | 1989-07-20 | 1991-09-05 | Zi Fuer Molekularbiologie Der Adw,De | Verfahren zur herstellung eines mittels fuer die behandlung oder prophylaxe von hepatits-infektionen bei mensch und tier |
| US5204466A (en) | 1990-02-01 | 1993-04-20 | Emory University | Method and compositions for the synthesis of bch-189 and related compounds |
| DE4224737A1 (de) | 1992-07-27 | 1994-02-03 | Herbert Prof Dr Schott | Neue Cytosinnucleosidanaloga, Verfahren zu ihrer Herstellung und ihre Verwendung |
| FR2709754B1 (fr) | 1993-09-10 | 1995-12-01 | Centre Nat Rech Scient | Composés 2' ou 3'-déoxy- et 2', 3'-didéoxy-beta-L-pentofuranonucléosides, procédé de préparation et application thérapeutique, notamment anti-virale. |
| WO1995007086A1 (en) | 1993-09-10 | 1995-03-16 | Emory University | Nucleosides with anti-hepatitis b virus activity |
| DE4418690A1 (de) | 1994-05-28 | 1996-01-11 | Boehringer Mannheim Gmbh | Neue Lipidester von Nucleosid-Monophosphaten und deren Verwendung als immunsuppressive Arzneimittel |
| US5559101A (en) | 1994-10-24 | 1996-09-24 | Genencor International, Inc. | L-ribofuranosyl nucleosides |
| US5703058A (en) | 1995-01-27 | 1997-12-30 | Emory University | Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent |
| DK0831852T3 (da) | 1995-06-07 | 2007-03-19 | Univ Emory | Nukleosider med anti-hepatitis B-virusaktivitet |
| BR9610120A (pt) | 1995-09-07 | 1999-12-21 | Univ Georgia Res Found | Composição farmacêutica e processo para aumentar a meia vida de um medicamento em um indivìduo e para melhorar uma condição patológica em um paciente. |
| CN1268140A (zh) | 1996-10-16 | 2000-09-27 | Icn药品公司 | 单环l－核苷、类似物及其应用 |
-
1999
- 1999-11-05 EP EP99958793A patent/EP1124839B1/en not_active Expired - Lifetime
- 1999-11-05 AT AT99958793T patent/ATE315574T1/de not_active IP Right Cessation
- 1999-11-05 US US09/435,261 patent/US6458773B1/en not_active Expired - Lifetime
- 1999-11-05 CA CA002348470A patent/CA2348470C/en not_active Expired - Fee Related
- 1999-11-05 BR BR9915555-9A patent/BR9915555A/pt not_active IP Right Cessation
- 1999-11-05 JP JP2000579613A patent/JP2002528554A/ja not_active Withdrawn
- 1999-11-05 IL IL14298399A patent/IL142983A0/xx active IP Right Grant
- 1999-11-05 CN CN998141895A patent/CN1216893C/zh not_active Expired - Fee Related
- 1999-11-05 WO PCT/US1999/026157 patent/WO2000026225A2/en not_active Ceased
- 1999-11-05 KR KR1020017005679A patent/KR100618028B1/ko not_active Expired - Fee Related
- 1999-11-05 DE DE69929460T patent/DE69929460D1/de not_active Expired - Lifetime
- 1999-11-05 MX MXPA01004504A patent/MXPA01004504A/es not_active IP Right Cessation
- 1999-11-05 AU AU16085/00A patent/AU774720B2/en not_active Ceased
-
2001
- 2001-05-04 IL IL142983A patent/IL142983A/en not_active IP Right Cessation
-
2011
- 2011-06-22 JP JP2011138647A patent/JP2011246469A/ja active Pending