AR063484A1 - Sal de acido p-toluensulfonico de 5-amino-3-(2'-o-acetil-3'-desoxi-beta-d-ribofuranosil)-3h-tiazol[4, 5-d]pirimidin-2-ona, metodos para la preparacion de la misma y de sus intermediarios de sintesis, una composicion farmaceutica que la comprende y su uso en el tratamiento de infecciones virales y ca - Google Patents
Sal de acido p-toluensulfonico de 5-amino-3-(2'-o-acetil-3'-desoxi-beta-d-ribofuranosil)-3h-tiazol[4, 5-d]pirimidin-2-ona, metodos para la preparacion de la misma y de sus intermediarios de sintesis, una composicion farmaceutica que la comprende y su uso en el tratamiento de infecciones virales y caInfo
- Publication number
- AR063484A1 AR063484A1 ARP070104611A ARP070104611A AR063484A1 AR 063484 A1 AR063484 A1 AR 063484A1 AR P070104611 A ARP070104611 A AR P070104611A AR P070104611 A ARP070104611 A AR P070104611A AR 063484 A1 AR063484 A1 AR 063484A1
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- compound
- amino
- acetyl
- beta
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
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- 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
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- 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
-
- 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
-
- 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
- A61P31/20—Antivirals for DNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D307/20—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
La presente descripcion se refiere a sal de ácido p-toluensulfonico de 5-amino-3-(2'-O-acetil-3'-desoxi-beta-D-ribofuranosil)-3H-tiazolo[4,5-d]pirimidin-2-ona y a su uso para tratar condiciones patologicas tales como infecciones virales, tumores y cáncer. También se describe un método para preparar la sal de ácido p-toluensulfonico de 5-amino-3-(2-O-acetil-3'-desoxi-beta-D-ribofuranosil)-3H-tiazolo[4,5-d]pirimidin-2-ona y métodos para producir compuestos de furanosa que son intermediarios utiles en la preparacion de compuestos farmacéuticos tales como sal de ácido p-toluensulfonico de 5-amino-3-(2'-O-acetil-3'-desoxi-beta-D-ribofuranosil)-3H-tizaolo4,5-d]pirimidin-2-ona y similares. Reivindicacion 11: Un método para sinterizar la sal de ácido p-toluensulfonico de 5-amino-3-(2'-O-acetil-3'-desoxi-beta-D-ribofuranosil) -3H-tiazolo[4,5-d] pirimidin-2-ona (1) que comprende las etapas de: (i) acoplamiento de 5-amino-3H-tiazolo[4,5-d]pirimidin-2-ona (2) con una desoxirribofuranosa (3) para formar un compuesto de la formula (4) (ii) clivaje selectivo de 5'-acetato en el compuesto de la formula (4) para formar 5-amino-3-(2'-O-acetil-3'-desoxi-beta-D-ribofuranosil)-3H-tiazolo[4,5-d] pirimidin-2-ona (5) (iii) reaccion de 5-amino- 3-(2'-O-acetil-3'-desoxi-beta-D-ribofuranosil)-3H-tiazolo[4,5-d]pirimidin-2-ona (5) con ácido p-toluensulfonico para formar sal de ácido p-toluensulfonico de 5-amino-3(2'-O-acetil-3'-desoxi-beta-D-ribofuranosil)-3H-tiazolo [4,5-d]pirimidin-2-ona (1). Reivindicacion 29: Un método para la preparacion de un compuesto de la formula (3) que comprende: (i) sulfonatar un compuesto de la formula (6) con un agente de sulfonatacion y una base para formar un compuesto sustituido con sulfonilo de la formula (7) en donde R es un alquilo o arilo opcionalmente sustituido; (ii) reducir el compuesto sustituido con sulfonilo de la formula (7) con un agente de reduccion para formar un compuesto de la formula (8) (iii) hidrolizar el compuesto de la formula (8) con un ácido para formar un compuesto de la formula (9), (iv) oxidar el compuesto de la formula (9) con agente oxidante, seguido de la reduccion con un agente de reduccion para formar el compuesto de la formula (10) (v) acetilar el compuesto de la formula (10) con un agente de acetilacion en presencia de un catalizador ácido para formar el compuesto de la formula (3). Reivindicacion 45: Un método de reduccion de un compuesto sustituido con sulfonilo de la formula (7) que comprende reducir el compuesto sustituido con sulfonilo con un agente de reduccion de borhidruro para formar un compuesto de la formula (8).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85200206P | 2006-10-17 | 2006-10-17 | |
| US89940507P | 2007-02-05 | 2007-02-05 | |
| US95359707P | 2007-08-02 | 2007-08-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR063484A1 true AR063484A1 (es) | 2009-01-28 |
Family
ID=39472747
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070104611A AR063484A1 (es) | 2006-10-17 | 2007-10-17 | Sal de acido p-toluensulfonico de 5-amino-3-(2'-o-acetil-3'-desoxi-beta-d-ribofuranosil)-3h-tiazol[4, 5-d]pirimidin-2-ona, metodos para la preparacion de la misma y de sus intermediarios de sintesis, una composicion farmaceutica que la comprende y su uso en el tratamiento de infecciones virales y ca |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US7928085B2 (es) |
| EP (1) | EP2076132B1 (es) |
| JP (2) | JP5279715B2 (es) |
| KR (2) | KR101486444B1 (es) |
| AR (1) | AR063484A1 (es) |
| AU (1) | AU2007353381B2 (es) |
| BR (1) | BRPI0717741A2 (es) |
| CA (2) | CA2898225A1 (es) |
| CY (1) | CY1113368T1 (es) |
| DK (1) | DK2076132T3 (es) |
| DO (1) | DOP2007000131A (es) |
| EA (1) | EA017005B1 (es) |
| ES (1) | ES2390930T3 (es) |
| HK (1) | HK1132429A1 (es) |
| IL (2) | IL198180A (es) |
| MX (1) | MX2009004028A (es) |
| MY (1) | MY150408A (es) |
| NO (1) | NO20091598L (es) |
| NZ (1) | NZ576408A (es) |
| PE (1) | PE20081105A1 (es) |
| PL (1) | PL2076132T3 (es) |
| PT (1) | PT2076132E (es) |
| TW (1) | TWI415854B (es) |
| UY (1) | UY30650A1 (es) |
| WO (1) | WO2008140549A1 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE496924T1 (de) | 2006-06-22 | 2011-02-15 | Anadys Pharmaceuticals Inc | Prodrugs von 5-amino-3-(3'-deoxy-beta-d- ribofuranosyl)-thiazolä4,5-düpyrimidin-2,7-dion |
| WO2009026292A1 (en) * | 2007-08-20 | 2009-02-26 | Anadys Pharmaceuticals, Inc. | Dosing methods for treating disease |
| PL3230298T3 (pl) | 2014-12-08 | 2021-06-14 | F.Hoffmann-La Roche Ag | 3-podstawione związki 5-amino-6h-tiazolo[4,5-d]pirymidyno-2,7-dionowe do leczenia i profilaktyki zakażenia wirusowego |
| US9676793B2 (en) | 2014-12-23 | 2017-06-13 | Hoffmann-Laroche Inc. | Co-crystals of 5-amino-2-oxothiazolo[4,5-d]pyrimidin-3(2H)-yl-5-hydroxymethyl tetrahydrofuran-3-yl acetate and methods for preparing and using the same |
| SG10201912847QA (en) | 2015-03-16 | 2020-02-27 | Hoffmann La Roche | Combined treatment with a tlr7 agonist and an hbv capsid assembly inhibitor |
| CN107743491B (zh) | 2015-05-08 | 2020-08-21 | 豪夫迈·罗氏有限公司 | 用于治疗和预防病毒感染的新的氧硫杂环戊烷甲酸及其衍生物 |
| EP4001283A1 (en) | 2015-05-12 | 2022-05-25 | F. Hoffmann-La Roche AG | Substituted aminothiazolopyrimidinedione derivatives for the treatment and prophylaxis of virus infection |
| WO2017001307A1 (en) | 2015-06-30 | 2017-01-05 | F. Hoffmann-La Roche Ag | Novel substituted aminothiazolopyrimidinedione for the treatment and prophylaxis of virus infection |
| CN110139868B (zh) | 2017-01-06 | 2021-07-09 | 豪夫迈·罗氏有限公司 | 制备3-取代的5-氨基-6H-噻唑并[4,5-d]嘧啶-2,7-二酮化合物的方法 |
| CN110007010A (zh) * | 2018-01-05 | 2019-07-12 | 大鹏药品工业株式会社 | 源自曲氟尿苷的类似物质的检测方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH07224081A (ja) * | 1994-02-10 | 1995-08-22 | Kobayashi Koryo Kk | デオキシリボフラノシルハライド誘導体の製造方法 |
| US5532374A (en) * | 1995-06-06 | 1996-07-02 | Hitachi Chemical Company, Ltd. | Method of preparation of bis-quinolines |
| JP4067226B2 (ja) * | 1999-04-01 | 2008-03-26 | 三井化学株式会社 | １―ハロゲノ−２−デオキシリボフラノース誘導体の製造方法 |
| JP2000327693A (ja) * | 1999-05-21 | 2000-11-28 | Mitsui Chemicals Inc | ２’−デオキシ−β−シチジン誘導体の製造方法 |
| US6649761B2 (en) * | 2001-05-30 | 2003-11-18 | Merck & Co., Inc. | Process for preparing piperazinepentaneamide HIV protease inhibitors |
| DE60234376D1 (de) * | 2001-11-27 | 2009-12-24 | Anadys Pharmaceuticals Inc | 3-beta-d-ribofuranosylthiazolo(4,5-delta)pyridimin-nucleoside und ihre verwendung |
| AU2003289995A1 (en) * | 2002-12-09 | 2004-06-30 | Texcontor Etablissement | Anhydrous crystalline form of valacyclovir hydrochloride |
| CA2537450C (en) * | 2003-09-05 | 2012-04-17 | Anadys Pharmaceuticals, Inc. | Administration of tlr7 ligands and prodrugs thereof for treatment of infection by hepatitis c virus |
| CA2566541C (en) * | 2004-06-07 | 2012-10-09 | Anadys Pharmaceuticals, Inc. | 3-.beta.-d-ribofuranosylthiazolo[4,5-d]pyrimidine nucleosides and uses thereof |
| TWI407956B (zh) * | 2004-12-17 | 2013-09-11 | Anadys Pharmaceuticals Inc | ３，５-二取代和３，５，７-三取代-３Ｈ-唑并及３Ｈ-噻唑并〔４，５-ｄ〕嘧啶-２-酮化合物及其前藥 |
| US7501526B2 (en) * | 2005-01-20 | 2009-03-10 | Taigen Biotechnology | Synthesis of polyamine compounds |
| ATE496924T1 (de) | 2006-06-22 | 2011-02-15 | Anadys Pharmaceuticals Inc | Prodrugs von 5-amino-3-(3'-deoxy-beta-d- ribofuranosyl)-thiazolä4,5-düpyrimidin-2,7-dion |
| US8394935B2 (en) * | 2006-12-08 | 2013-03-12 | Api Corporation | Method for producing furanose derivative |
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2007
- 2007-10-06 BR BRPI0717741-0A2A patent/BRPI0717741A2/pt not_active Application Discontinuation
- 2007-10-16 KR KR1020097010038A patent/KR101486444B1/ko active IP Right Grant
- 2007-10-16 ES ES07873546T patent/ES2390930T3/es active Active
- 2007-10-16 MX MX2009004028A patent/MX2009004028A/es active IP Right Grant
- 2007-10-16 PT PT07873546T patent/PT2076132E/pt unknown
- 2007-10-16 CA CA2898225A patent/CA2898225A1/en not_active Abandoned
- 2007-10-16 NZ NZ576408A patent/NZ576408A/en not_active IP Right Cessation
- 2007-10-16 TW TW096138583A patent/TWI415854B/zh not_active IP Right Cessation
- 2007-10-16 DK DK07873546.1T patent/DK2076132T3/da active
- 2007-10-16 EP EP07873546A patent/EP2076132B1/en not_active Not-in-force
- 2007-10-16 KR KR1020147026217A patent/KR101515077B1/ko active IP Right Grant
- 2007-10-16 EA EA200970387A patent/EA017005B1/ru not_active IP Right Cessation
- 2007-10-16 WO PCT/US2007/081526 patent/WO2008140549A1/en active Application Filing
- 2007-10-16 MY MYPI20091559 patent/MY150408A/en unknown
- 2007-10-16 PE PE2007001399A patent/PE20081105A1/es not_active Application Discontinuation
- 2007-10-16 JP JP2009533481A patent/JP5279715B2/ja not_active Expired - Fee Related
- 2007-10-16 PL PL07873546T patent/PL2076132T3/pl unknown
- 2007-10-16 AU AU2007353381A patent/AU2007353381B2/en not_active Ceased
- 2007-10-16 US US11/873,202 patent/US7928085B2/en not_active Expired - Fee Related
- 2007-10-16 CA CA2666537A patent/CA2666537C/en not_active Expired - Fee Related
- 2007-10-17 UY UY30650A patent/UY30650A1/es not_active Application Discontinuation
- 2007-10-17 DO DO2007000131A patent/DOP2007000131A/es unknown
- 2007-10-17 AR ARP070104611A patent/AR063484A1/es unknown
-
2009
- 2009-04-16 IL IL198180A patent/IL198180A/en active IP Right Grant
- 2009-04-22 NO NO20091598A patent/NO20091598L/no not_active Application Discontinuation
-
2010
- 2010-01-05 HK HK10100028.4A patent/HK1132429A1/xx not_active IP Right Cessation
-
2011
- 2011-03-23 US US13/069,426 patent/US8193342B2/en active Active
-
2012
- 2012-09-28 CY CY20121100897T patent/CY1113368T1/el unknown
- 2012-11-19 IL IL223126A patent/IL223126A/en active IP Right Grant
-
2013
- 2013-05-21 JP JP2013107302A patent/JP5703334B2/ja not_active Expired - Fee Related
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