AR040411A1 - Inhibidores de la arn polimerasa dependiente de arn del virus de la hepatitis c y composiciones y tratamientos que los usan - Google Patents
Inhibidores de la arn polimerasa dependiente de arn del virus de la hepatitis c y composiciones y tratamientos que los usanInfo
- Publication number
- AR040411A1 AR040411A1 AR20030101630A ARP030101630A AR040411A1 AR 040411 A1 AR040411 A1 AR 040411A1 AR 20030101630 A AR20030101630 A AR 20030101630A AR P030101630 A ARP030101630 A AR P030101630A AR 040411 A1 AR040411 A1 AR 040411A1
- Authority
- AR
- Argentina
- Prior art keywords
- nhc
- integer
- aryl
- group
- cycloalkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/32—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
Abstract
Reivindicación 1: Un método para inhibir la actividad de la polimerasa de VHC caracterizado porque comprende poner en contacto una polimerasa VHC con una cantidad eficaz de un compuesto representado por la fórmula (1) o una sal, solvato, profármaco, o metabolito del mismo; en la que r es 0, 1, 2, 3, 4 o 5; R1 es hidrógeno, o un grupo arilo, heteroarilo, cicloalquilo, o heterocicloalquilo, sin substituir o substituido con uno o más substituyentes seleccionados entre el grupo substituir o substituido con uno o más substituyentes seleccionados entre el grupo compuesto por grupos halógenos; =O; =S; -CN; -NO2; alcano ramificado o no ramificado; alquilo; heteroalquilo; alquenilo; alquinilo; arilo; cicloalquilo; heterocicloalquilo; heteroarilo; compuesto por halógeno; =O; =S; -CN; -NO2; alquilo; heteroalquilo; alquenilo; alquinilo; arilo; cicloalquilo; heterocicloalquilo; heteroarilo; alcoxi; isopropilo; t-butilo; -(CH2)zCN donde z es un entero de 1 a 4; =NH; -NHOH; -OH; -OCH3; -OCH2-; -OCH2CH3; -C(O)H; -OC(O)H; -C(O)OH; -CH2CH(O)OCH3; -OC(O)OH; -OC(O)OC(O)H; -OOH; -C(NH)NH2; -NHC(NH)NH2; -C(S)NH2; -NHC(S)NH2; -NHC(O)NH2; -S(O2)H; -S(O)H; -NH2; -C(O)NH2; -OC(O)NH2; -NHC(O)H; -NHC(O)OH; -C(O)NHC(O)H; -OS(O2)H; -OS(O)H; -OSH; -SC(O)H; -S(O)C(O)OH; -SO2C(O)OH; -SO2CH3; -NHSH; -NHS(O)H; -NHSO2H; -C(O)SH; -C(O)S(O)H; -C(O)S(O2)H; -C(S)OH; -C(SO)OH; -C(SO2)OH; -NHC(S) H; -OC(S)H; -OC(S)OH; -OC(SO2)H; -S(O2)NH2; -S(O)NH2; -SNH2; -NHCS(O2)H; -NHC(SO)H; -NHC(S)H; y -SH, sin alcoxi; -(CH2)zCN donde z es un entero de 1 a 4; =NH; -NHOH; -OH; -C(O)H; -OC(O)H; -C(O)OH; -C(O)OC(CH3)n, donde n es un entero de 1 a 3; -OC(O)OH; -OC(O)OC(O)H; -OOH; -C(NH)NH2; -NHC(NH)NH2; -C(S)NH2; -NHC(S)NH2; -NHC(O)NH2; -S(O2)H; -S(O)H; -NH2; -C(O)NH2; -OC(O)NH2; -NHC(O)H; -NHC(O)OH; -C(O)NHC(O)H; -OS(O2)H; -OS(O)H; -OSH; -SC(O)H; -SCH2CH3; -S(O)C(O)OH; -SO2C(O)OH; -NHSH; -NHS(O)H; -NHSO2H; -C(O)SH; -C(O)S(O)H; -C(O)S (O2)H; -C(S)H; -C(SO)OH; -C(SO2)OH; -NHC(S)H; -OC(S)H; -OC(S)OH; -OC(SO2)H; -S(O2)NH2; -S(O)NH2; -SNH2; -NHCS(O2)H; -NHC(SO)H; -NHC(S)H; y -SH sin substituir o substituidos con uno o más substituyentes seleccionados entre el grupo compuesto por halógenos; fenilo; cicloalcano; -O-; -OH; y CH3; R2 es un grupo isopropilo, ciclopentilo, o ciclohexilo, sin substituir o substituido con uno o más substituyentes seleccionados entre el grupo compuesto por halógenos; =O; =S; -CN; -NO2; alquilo; alquenilo; alquinilo; arilo; cicloalquilo; heterocicloalquilo; heteroarilo; -(CH2)zCN donde z es un entero de 1 a 4; =NH; -NHOH; -OH; -C(O)H; -OC(O)H; -C(O)OH; -OC(O)OH; -OC(O)OC(O)H; -OOH; -C(NH)NH2; -NHC(NH)NH2; -C(S)NH2; -NHC(S)NH2; -NHC(O)NH2; -S(O2)H; -S(O)H; -NH2; -C(O)NH2; -OC(O)NH2; -NHC(O)H; -NHC(O)OH; -C(O)NHC(O)H; OS(O2)H; -OS(O)H; -OSH; -SC(O)H; -S(O)C(O)OH; -SO2C(O)OH; -NHSH; -NHS(O)H; -NHSO2H; -C(O)SH; -C(O)S(O)H; -C(O)S(O2)H; -C(S)OH; -C(SO)OH; -C(SO2)OH; -NHC(S)H; -OC(S)H; -OC(S)OH; -OC(SO2)H; -S(O2)NH2; -S(O)NH2; -SNH2; -NHCS (O2) H; -NHC(SO)H; -NHC(S)H; y -SH; R3 es hidrógeno; halógeno; =S; -SH; -S-(CH2)z-heteroarilo donde z es un entero de 0 a 4; -S-(CH2)z-heterocicloalquilo donde z es un entero de 0 a 4; -S-(CH2)z-arilo donde z es un entero de 0 a 4; -(CH2)z-arilo donde z es un entero de 0 a 4; -O-arilo; -C(O)H; -C(O)-alquilo; amino; o un halógeno, sin substituir o substituido con un grupo arilo, halógenos; =O; =S; -CN; -NO2; alquilo; heteroalquilo; alquenilo; alquinilo; arilo; cicloalquilo; heterocicloalquilo; heteroarilo; alcoxi; isopropilo; t-butilo; - (CH2)zCN donde z es un entero de 1 a 4; =NH; -NHOH; -OH; -OCH3, -OCH2-; -OCH2CH3; -C(O)H; -OC(O)H; -C(O)OH; -OS(O2)H; -OS(O)H; -OSH; -SC(O)H; -S(O)C(O)OH; -SO2C(O)OH; -SO2CH3; -NHSH; -NHS(O)H; -NHSO2H; -C(O)SH; -C(O)S(O)H; -C(O)S(O2)H; -C(S)OH; -C(SO)OH; -C(SO2)OH; -NHC(S)H; -OC(S)H; -OC(S)OH; -OC(SO2)H; -S(O2)NH2; -S(O)NH2; -SNH2; -NHCS(O2)H; -NHC(SO)H; -NHC(S)H; y -SH, sin substituir o substituido con uno o más substituyentes seleccionados entre el grupo compuesto por halógenos; =O; =S; -CN; -NO2; alcano, ramificado o no ramificado; alquilo; heteroalquilo; alquenilo; alquinilo; arilo; cicloalquilo; heterocicloalquilo; heteroarilo; alcoxi; -(CH2)zCN donde z es un entero de 1 a 4; =NH; -NHOH; -OH; -C(O)H; -OC(O)H; -C(O)OH; -C(O)OC(CH3)n, donde n es un entero de 1 a 3; -OC(O)OH; -OC(O)OC(O)H; -OOH; -C(NH)NH2; -NHC(NH)NH2; -C(S)NH2; -NHC(S)NH2; -NHC(O)NH2; -S(O2)H; -S(O)H; -NH2; -C(O)NH2; -OC(O)NH2; -NHC(O)H; -NHC(O)OH; -C(O)NHC(O)H; -OS(O2)H; -OS(O)H; -OSH; -SC(O)H; -SCH2CH3; -S(O)C(O)OH; -SO2C(O)OH; -NHSH; -NHS(O)H; -NHSO2H; -C(O)SH; -C(O)S(O)H; -C(O)S(O2)H; -C(S)H; -C(SO)OH; -C(SO2)OH; -NHC(S)H; -OC(S)H; -OC(S)OH; -OC(SO2)H; -S(O2)NH2; -S(O)NH2; -SNH2; -NHCS(O2)H; -NHC(SO)H; -NHC(S)H; y -SH, sin substituir o substituido con uno o más substituyentes seleccionados entre el grupo compuesto por halógenos; fenilo; cicloalcano; -O-; -OH; y CH3; R4 es =O ó -OR5; X-W es C-CH cuando R4 es =O, y X-W es C=C cuando R4 es -OR5; o R3 y R4 junto con X y W forman un grupo cicloalquilo, heteroarilo, cicloalquilo, o heterocicloalquilo sin substituir o substituidos con uno o más substituyentes seleccionados entre el grupo compuesto por halógenos; =O; =S; -CN; -NO2; alquilo; heteroalquilo; alquenilo; alquinilo; arilo; cicloalquilo; heterocicloalquilo; heteroarilo; alcoxi; isopropilo; t-butilo; -(CH2)zCN donde z es un entero de 1 a 4; =NH; -NHOH; -OH; -OCH3, -OCH2-; -OCH2CH3; -C(O)H; -OC(O)H; -C(O)OH; -CH2CH(O)OCH3; -OC(O)OH; -OC(O)OC(O)H; -OOH; -C(NH)NH2; -NHC(NH)NH2; -C(S)NH2; -NHC(S)NH2; -NHC(O)NH2; -S(O2)H; -S(O)H; -NH2; -C(O)NH2; -OC(O)NH2; -NHC(O)H; -NHC(O)OH; -NHC(NH)NH2; -C(S)NH2; -NHC(S)NH2; -NHC(O)NH2; -S(O2)H; -S(O)H; -NH2; -C(O)NH2; -OC(O)NH2; -NHC(O)H; -NHC(O)OH; -C(O)NHC(O)H; -OS(O2)H; -OS(O)H; -OSH; -SC(O)H; -S(O)C(O)OH; -SO2C(O)OH; -SO2CH3; -NHSH; -NHS(O)H; -NHSO2H; -C(O)SH; -C(O)S(O)H; -C(O)S(O2)H; -C(S)OH; -C(SO)OH; -C (SO2)OH; -NHC(S)H; -OC(S)H; -OC(S)OH; -OC(SO2)H; -S(O2)NH2; -S(O)NH2; -SNH2; -NHCS(O2)H; -NHC(SO)H; -NHC(S)H; y -SH, sin substituir o substituidos con uno o más substituyentes seleccionados entre el grupo compuesto por halógenos; =O; =S; -CN; -NO2; alcano, ramificado o no ramificado; alquilo; heteroalquilo; alquenilo; alquinilo; arilo; cicloalquilo; heterocicloalquilo; heteroarilo; alcoxi; -(CH2)zCN donde z es un entero de 1 a 4; =NH; -NHOH; -OH; -C(O)H; -OC(O)H; -C(O)OH; -C(O)OC(CH3)n, donde n es un entero de 1 a 3; -OC(O)OH; -OC(O)OC(O)H; -OOH; -C(NH)NH2; -NHC(NH)NH2; -C(S)NH2; -NHC(S)NH2; -NHC(O)NH2; -S(O2)H; -S(O)H; -NH2; -C(O)NH2; -OC(O)NH2; -NHC(O)H; -NHC(O)OH; -C(O)NHC(O)H; -OS(O2)H; -OS(O)H; -OSH; -SC(O)H; -SCH2CH3; -S(O)C(O)OH; -SO2C(O)OH; -NHSH; -NHS(O)H; -NHSO2H; -C(O)SH; -C (O)S(O)H; -C(O)S(O2)H; -C(S)H; -C(SO)OH; -C(SO2)OH; -NHC(S)H; -OC(S)H; -OC(S)OH; -OC(SO2)H; -S(O2)NH2; -S(O)NH2; -SNH2; -NHCS(O2)H; -NHC(SO)H; -NHC(S)H; y -SH sin substituir o substituido con uno o más substituyentes seleccionados entre el grupo compuesto por halógenos; arilo; cicloalquilo; -OR5; haloalquilo; y alquilo; y R5 es un alquilo o H.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US37943302P | 2002-05-10 | 2002-05-10 |
Publications (1)
Publication Number | Publication Date |
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AR040411A1 true AR040411A1 (es) | 2005-04-06 |
Family
ID=29420530
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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AR20030101630A AR040411A1 (es) | 2002-05-10 | 2003-05-09 | Inhibidores de la arn polimerasa dependiente de arn del virus de la hepatitis c y composiciones y tratamientos que los usan |
Country Status (10)
Country | Link |
---|---|
US (1) | US7115658B2 (es) |
AR (1) | AR040411A1 (es) |
AU (1) | AU2003224371A1 (es) |
DO (1) | DOP2003000641A (es) |
GT (1) | GT200300105A (es) |
PA (1) | PA8573401A1 (es) |
PE (1) | PE20040472A1 (es) |
TW (1) | TW200306813A (es) |
UY (1) | UY27798A1 (es) |
WO (1) | WO2003095441A1 (es) |
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WO2011098452A1 (en) | 2010-02-10 | 2011-08-18 | Glaxosmithkline Llc | 6-amino-2-{ [ (1s)-1-methylbutyl] oxy}-9-[5-(1-piperidinyl)-7,9-dihydro-8h-purin-8-one maleate |
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KR101949108B1 (ko) | 2015-12-03 | 2019-02-15 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | Sting의 조정제로서의 시클릭 푸린 디뉴클레오티드 |
EA201892128A1 (ru) | 2016-04-07 | 2019-04-30 | Глаксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Гетероциклические амиды, полезные в качестве модуляторов |
EP3440076B1 (en) | 2016-04-07 | 2022-06-01 | GlaxoSmithKline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
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GB201807924D0 (en) | 2018-05-16 | 2018-06-27 | Ctxt Pty Ltd | Compounds |
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GB201910304D0 (en) | 2019-07-18 | 2019-09-04 | Ctxt Pty Ltd | Compounds |
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US6005103A (en) * | 1993-11-19 | 1999-12-21 | Warner-Lambert Company | Pyrone derivatives as protease inhibitors and antiviral agents |
AU689158B2 (en) | 1993-11-19 | 1998-03-26 | Parke, Davis & Company | 5,6-dihydropyrone derivatives as protease inhibitors and antiviral agents |
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AU9198698A (en) * | 1997-09-15 | 1999-04-05 | Warner-Lambert Company | Process for the preparation of substituted 5,6-dihydro-2h-pyran-2-ones |
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AU2203800A (en) * | 1999-01-07 | 2000-07-24 | Warner-Lambert Company | Antiviral method using mek inhibitors |
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ATE337309T1 (de) * | 2002-04-01 | 2006-09-15 | Pfizer | Pyranon- und pyrandioninhibitoren der rna- abhängigen rna-polymerase des hepatitis-c-virus |
-
2003
- 2003-05-02 DO DO2003000641A patent/DOP2003000641A/es unknown
- 2003-05-07 GT GT200300105A patent/GT200300105A/es unknown
- 2003-05-07 PE PE2003000446A patent/PE20040472A1/es not_active Application Discontinuation
- 2003-05-07 AU AU2003224371A patent/AU2003224371A1/en not_active Abandoned
- 2003-05-07 WO PCT/IB2003/001905 patent/WO2003095441A1/en not_active Application Discontinuation
- 2003-05-08 UY UY27798A patent/UY27798A1/es not_active Application Discontinuation
- 2003-05-08 PA PA20038573401A patent/PA8573401A1/es unknown
- 2003-05-09 TW TW092112696A patent/TW200306813A/zh unknown
- 2003-05-09 US US10/434,702 patent/US7115658B2/en not_active Expired - Fee Related
- 2003-05-09 AR AR20030101630A patent/AR040411A1/es not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
UY27798A1 (es) | 2003-12-31 |
AU2003224371A1 (en) | 2003-11-11 |
TW200306813A (en) | 2003-12-01 |
US7115658B2 (en) | 2006-10-03 |
US20040023958A1 (en) | 2004-02-05 |
PE20040472A1 (es) | 2004-08-12 |
DOP2003000641A (es) | 2003-11-15 |
WO2003095441A1 (en) | 2003-11-20 |
GT200300105A (es) | 2004-03-17 |
PA8573401A1 (es) | 2003-12-10 |
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