AR059114A1 - Metodos para la preparacion de inhibidores de polimerasa del vhc - Google Patents
Metodos para la preparacion de inhibidores de polimerasa del vhcInfo
- Publication number
- AR059114A1 AR059114A1 ARP060103695A ARP060103695A AR059114A1 AR 059114 A1 AR059114 A1 AR 059114A1 AR P060103695 A ARP060103695 A AR P060103695A AR P060103695 A ARP060103695 A AR P060103695A AR 059114 A1 AR059114 A1 AR 059114A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- compound
- formula
- hydrogen
- halogen
- Prior art date
Links
- 229940124683 HCV polymerase inhibitor Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 16
- 150000001875 compounds Chemical class 0.000 abstract 13
- 229910052739 hydrogen Inorganic materials 0.000 abstract 11
- 239000001257 hydrogen Substances 0.000 abstract 11
- 229910052736 halogen Inorganic materials 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 8
- 150000002431 hydrogen Chemical class 0.000 abstract 7
- -1 - (CR6R10) nR11 Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 150000001450 anions Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
-
- 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
-
- 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
-
- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/55—Acids; Esters
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
Abstract
Reivindicacion 1: Un método para preparar un compuestos de la formula (1) caracterizado porque R1 es alquilo C1-6 o cicloalquilo C3-6; cada R2a, R2b y R2c se selecciona independientemente de: hidrogeno, halogeno, alquilo C1-C6, cicloalquilo C3-C6, - OR12a, -CF3, -CN y -NR1aR12b, R4 se selecciona de: hidrogeno, alquilo C1-6, -(CR9R10)nR11, -CF3, halogeno OR12a, -CN y -NR12aR12b: R5 se selecciona de hidrogeno, alquilo C1-6, -(CR6R10)nR11, -CF3, halogeno OR12a, -CN y NR12aR12b; R6 se selecciona de: hidrogeno, alquilo C1-6, -(CR9R10)nR11, -CF3, halogeno, -OR12a, -CN y NR12aR12; R7 se selecciona de hidrogeno, alquilo C1-C6, - (CR9R10)nR11, -CF3, halogeno, OR12a, - CN y NR12aR12b; Cada R9 y R10 se selecciona independientemente de hidrogeno y alquilo C1-6 o R9 y R10, junto con el átomo de carbono al que están unidos, forman un grupo cicloalquilo C3-C6; Cada R11 se selecciona independientemente de: hidrogeno, alquilo C1-6, halogeno, -OR12a, -CN, -CF3 y NR9R10, cada R12a y R12b se selecciona independientemente de hidrogeno y alquilo C1-C6 y cada n se elige independientemente y es un numero entero de 0 a 5; comprendiendo dicho método: a) tratar un compuesto de la formula (V), en la que R1 se definio anteriormente, con un anion de un compuesto de la formula (X), en la que R13 es: hidrogeno, alquilo C1-6, -Si(alquilo C1-6)3 o CH2(arilo C6-10 en los que dicho grupo arilo C6-10 está opcionalmente sustituido con al menos un sustituyente seleccionado de: halogeno, alquilo C1-6, -OH, -OCH3 y N(alquilo C1-6)2, para proporcionar un compuesto de la formula (IV); b) hidrolizar el compuesto de formula (IV) para proporcionar un compuesto de formula (IV) en el que R13 es hidrogeno; c) tratar el compuesto de la formula (IV) con una combinacion de reactivos para proporcionar un compuesto de la formula (III) en los que P1 es hidrogeno o un grupo protector adecuado y R14 es: alquilo C1-6 o CH2(arilo C6-10) en los que dicho grupo arilo C6-10 está opcionalmente sustituido con al menos un sustituyente seleccionado de: halogeno, alquilo C1-6, -OH, -OCH3 y -N(alquilo C1-6)2; d) tratar el compuesto de formula (III) con un ácido o una base para proporcionar un compuesto de formula (II) y e) tratar el compuesto de la formula (II) con un compuesto de la formula (IXa), para proporcionar el compuesto de la formula (Ia).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71104205P | 2005-08-24 | 2005-08-24 | |
| US74427306P | 2006-04-04 | 2006-04-04 | |
| US80464406P | 2006-06-13 | 2006-06-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR059114A1 true AR059114A1 (es) | 2008-03-12 |
Family
ID=37198917
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060103695A AR059114A1 (es) | 2005-08-24 | 2006-08-24 | Metodos para la preparacion de inhibidores de polimerasa del vhc |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US7807838B2 (es) |
| EP (1) | EP1928878A1 (es) |
| JP (1) | JP2007056022A (es) |
| KR (1) | KR101064459B1 (es) |
| CN (1) | CN102336758A (es) |
| AR (1) | AR059114A1 (es) |
| AU (1) | AU2006283297B2 (es) |
| BR (1) | BRPI0615016A2 (es) |
| CA (1) | CA2619077C (es) |
| IL (1) | IL189210A0 (es) |
| MX (1) | MX2008001541A (es) |
| NZ (1) | NZ565496A (es) |
| TW (2) | TWI320412B (es) |
| WO (1) | WO2007023381A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2008248116A1 (en) | 2007-05-04 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Combination therapy for the treatment of HCV infection |
| BRPI0814939A2 (pt) * | 2007-08-10 | 2015-01-27 | Glaxosmithkline Llc | Entidade química, composição farmacêutica, e, método para tratar uma infecção viral em um mamífero. |
| US8717565B2 (en) * | 2008-12-17 | 2014-05-06 | The Lubrizol Corporation | Optically active functional fluid markers |
| EP2558577B1 (en) | 2010-04-16 | 2018-12-12 | Nuevolution A/S | Bi-functional complexes and methods for making and using such complexes |
| US10392598B2 (en) * | 2015-06-19 | 2019-08-27 | Emory University | Methods of measuring cell purity for making quality control determinations and related compositions |
| WO2017207599A1 (en) * | 2016-05-31 | 2017-12-07 | Roche Diagnostics Gmbh | Method for serological detection of viral antigens |
| CN107744831B (zh) * | 2017-08-31 | 2020-04-21 | 博事利达（苏州）生物科技有限公司 | 一类奎尼定衍生物催化剂、制备方法及应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US176701A (en) * | 1876-04-25 | Improvement in school-furniture | ||
| RU2223958C2 (ru) * | 1997-09-11 | 2004-02-20 | Фармация Энд Апджон Компани | Новый способ получения ингибитора протеазы |
| EP2335700A1 (en) * | 2001-07-25 | 2011-06-22 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis C virus polymerase inhibitors with a heterobicylic structure |
| DOP2003000641A (es) * | 2002-05-10 | 2003-11-15 | Pfizer | Inhibidores de las arn polimerasa dependiente de arn del virus de las hepatitis c y composiciones y tratamiento que los usan |
| US7148226B2 (en) * | 2003-02-21 | 2006-12-12 | Agouron Pharmaceuticals, Inc. | Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same |
| GEP20094751B (en) * | 2004-08-18 | 2009-08-10 | Pfizer | Inhibitors of hepatitis c virus rna-dependent rna polymerase, and compositions and treatments using the same |
-
2006
- 2006-08-16 CA CA2619077A patent/CA2619077C/en not_active Expired - Fee Related
- 2006-08-16 WO PCT/IB2006/002342 patent/WO2007023381A1/en not_active Ceased
- 2006-08-16 MX MX2008001541A patent/MX2008001541A/es active IP Right Grant
- 2006-08-16 EP EP06795351A patent/EP1928878A1/en not_active Withdrawn
- 2006-08-16 BR BRPI0615016-0A patent/BRPI0615016A2/pt not_active IP Right Cessation
- 2006-08-16 CN CN2011101890312A patent/CN102336758A/zh active Pending
- 2006-08-16 AU AU2006283297A patent/AU2006283297B2/en not_active Ceased
- 2006-08-16 NZ NZ565496A patent/NZ565496A/en not_active IP Right Cessation
- 2006-08-16 US US12/064,747 patent/US7807838B2/en not_active Expired - Fee Related
- 2006-08-16 KR KR1020087004390A patent/KR101064459B1/ko not_active Expired - Fee Related
- 2006-08-23 TW TW098115301A patent/TWI320412B/zh not_active IP Right Cessation
- 2006-08-23 JP JP2006226037A patent/JP2007056022A/ja active Pending
- 2006-08-23 TW TW095130984A patent/TWI316516B/zh not_active IP Right Cessation
- 2006-08-24 AR ARP060103695A patent/AR059114A1/es not_active Application Discontinuation
-
2008
- 2008-02-03 IL IL189210A patent/IL189210A0/en unknown
-
2010
- 2010-08-17 US US12/857,644 patent/US20110070187A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| KR101064459B1 (ko) | 2011-09-16 |
| EP1928878A1 (en) | 2008-06-11 |
| IL189210A0 (en) | 2008-06-05 |
| US7807838B2 (en) | 2010-10-05 |
| TW200740817A (en) | 2007-11-01 |
| TWI320412B (en) | 2010-02-11 |
| BRPI0615016A2 (pt) | 2011-05-03 |
| TWI316516B (en) | 2009-11-01 |
| CA2619077C (en) | 2011-09-13 |
| JP2007056022A (ja) | 2007-03-08 |
| NZ565496A (en) | 2010-10-29 |
| AU2006283297A1 (en) | 2007-03-01 |
| MX2008001541A (es) | 2008-02-15 |
| AU2006283297B2 (en) | 2012-07-26 |
| US20090023921A1 (en) | 2009-01-22 |
| US20110070187A1 (en) | 2011-03-24 |
| KR20080038354A (ko) | 2008-05-06 |
| WO2007023381A1 (en) | 2007-03-01 |
| CN102336758A (zh) | 2012-02-01 |
| CA2619077A1 (en) | 2007-03-01 |
| TW200942546A (en) | 2009-10-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |