AR057703A1 - INHIBIDORES MACROCíCLICOS DEL VIRUS DE LA HEPATITIS C. PROCESO DE PREPARACIoN Y COMPOSICIONES FARMACÉUTICAS. - Google Patents
INHIBIDORES MACROCíCLICOS DEL VIRUS DE LA HEPATITIS C. PROCESO DE PREPARACIoN Y COMPOSICIONES FARMACÉUTICAS.Info
- Publication number
- AR057703A1 AR057703A1 ARP060103309A AR057703A1 AR 057703 A1 AR057703 A1 AR 057703A1 AR P060103309 A ARP060103309 A AR P060103309A AR 057703 A1 AR057703 A1 AR 057703A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- alkoxy
- cycloalkyl
- group
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
Reivindicacion 1: Un compuesto que tiene la formula (1) un N-oxido, sal, o estereoisomero de éste, donde cada línea de puntos (representada por -----) representa un doble enlace opcional; X es N, CH y cuando X lleva un doble enlace es C; R1 es -OR6, -NH-SO2R7; R2 es hidrogeno, y cuando X es C o CH, R2 también puede ser alquilo C1-6; R3 es hidrogeno, alquilo C1-6, alcoxi C1-6alquilo C1-6, o cicloalquilo C3-7; n es 3, 4, 5, o 6; R4 y R5 tomados junto con el atomo de nitrogeno al cual están unidos forman un sistema anular bicíclico seleccionado del grupo de formulas (2) donde dicho sistema anular puede estar sustituido en forma opcional con uno, dos o tres sustituyentes seleccionados en forma independiente de halo, hidroxi, oxo, nitro, ciano, carboxilo, alquilo C1-6, alcoxi C1-6, alcoxi C1-6alquilo C1-6, alquilcarbonilo C1-6, alcoxicarbonilo C1-6, amino, azido, mercapto, polihaloalquiloC1-6; R6 es hidrogeno; arilo; Het; cicloalquilo C3-7 sustituido en forma opcional con alquilo C1-6; o alquilo C1-6 sustituido en forma opcional con cicloalquilo C3-7, arilo o con Het; R7 es arilo; Het; cicloalquilo C3-7 sustituido en forma opcional con alquilo C1-6; o alquilo C1-6 sustituido en forma opcional con cicloalquilo C3-7, arilo o con Het; arilo como grupo o parte de un grupo es fenilo o naftilo, cada uno de los cuales puede estar sustituido en forma opcional con uno, dos o tres sustituyentes seleccionados de halo, hidroxi, nitro, ciano, carboxilo, alquilo C1-6, alcoxi C1-6, alcoxi C1- 6-alquilo C1-6, alquilcarbonilo, C1-6, amino, mono- o dialquilamino C1-6, azido, mercapto, polihaloalquilo C1-6, polihaloalcoxi C1-6, cicloalquilo C3-7, pirrolidinilo, piperidinilo, piperazinilo, 4-alquil C1-6-piperazinilo, 4-alquilcarbonil C1-6- piperazinilo, y morfolinilo; donde los grupos morfolinilo y piperidinilo pueden estar sustituidos en forma opcional con uno o dos radicales alquilo C1-6; Het como grupo o parte de un grupo es un anillo heterocíclico saturado, parcialmente insaturado o completamente insaturado de 5 o 6 miembros que contiene 1 a 4 heteroátomos seleccionado cada uno en forma independiente de nitrogeno, oxígeno y azufre, y sustituido en forma opcional con uno, dos o tres sustituyentes seleccionados, cada uno en forma independiente, del grupo que consiste en halo, hidroxi, nitro, ciano, carboxilo, alquilo C1-6, alcoxi C1-6, alcoxi C1-6alquilo C1-6, alquilcarbonilo C1-6, amino, mono- o di-alquilamino C1-6, azido, mercapto, polihaloalquilo C1-6, polihaloalcoxi C1-6, cicloalquilo C3-7, pirrolidinilo, piperidinilo, pieprazinilo, 4-alquil C1-6-piperazinilo, 4-alquilcarbonil C1-6-piperazinilo, y morfolinilo; donde los grupos morfolinilo y piperidinilo pueden estar sustituidos en forma opcional con uno o dos radicales alquilo C1-6. Composiciones farmacéuticas que contienen compuestos (I) y procesos para preparar los compuestos (I). También se proporcionan combinaciones biodisponibles de los inhibidores del VHC de formula (I) con ritonavir.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP05107071 | 2005-07-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR057703A1 true AR057703A1 (es) | 2007-12-12 |
Family
ID=35589621
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP060103309 AR057703A1 (es) | 2005-07-29 | 2006-07-28 | INHIBIDORES MACROCíCLICOS DEL VIRUS DE LA HEPATITIS C. PROCESO DE PREPARACIoN Y COMPOSICIONES FARMACÉUTICAS. |
Country Status (19)
Country | Link |
---|---|
US (1) | US9023808B2 (es) |
EP (1) | EP1919899B1 (es) |
JP (1) | JP5230415B2 (es) |
KR (1) | KR101381176B1 (es) |
CN (1) | CN101273028B (es) |
AR (1) | AR057703A1 (es) |
AT (1) | ATE496042T1 (es) |
AU (1) | AU2006274862B2 (es) |
BR (1) | BRPI0614620A2 (es) |
CA (1) | CA2617099C (es) |
DE (1) | DE602006019741D1 (es) |
DK (1) | DK1919899T3 (es) |
EA (1) | EA013475B1 (es) |
ES (1) | ES2359939T3 (es) |
MY (1) | MY141245A (es) |
PL (1) | PL1919899T3 (es) |
SI (1) | SI1919899T1 (es) |
TW (1) | TWI382025B (es) |
WO (1) | WO2007014923A1 (es) |
Families Citing this family (45)
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MY140680A (en) | 2002-05-20 | 2010-01-15 | Bristol Myers Squibb Co | Hepatitis c virus inhibitors |
KR101159575B1 (ko) | 2004-01-30 | 2012-07-06 | 얀센 알 앤드 디 아일랜드 | Hcv ns―3 세린 프로테아제 저해제 |
PE20070211A1 (es) | 2005-07-29 | 2007-05-12 | Medivir Ab | Compuestos macrociclicos como inhibidores del virus de hepatitis c |
ES2373685T3 (es) | 2005-07-29 | 2012-02-07 | Tibotec Pharmaceuticals | Inhibidores macrocíclicos del virus de la hepatitis c. |
PL1913015T3 (pl) | 2005-07-29 | 2014-04-30 | Janssen R&D Ireland | Makrocykliczne inhibitory wirusa zapalenia wątroby typu C |
US7741281B2 (en) | 2005-11-03 | 2010-06-22 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
WO2008008776A2 (en) | 2006-07-11 | 2008-01-17 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
US8343477B2 (en) | 2006-11-01 | 2013-01-01 | Bristol-Myers Squibb Company | Inhibitors of hepatitis C virus |
US7772180B2 (en) | 2006-11-09 | 2010-08-10 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US7763584B2 (en) | 2006-11-16 | 2010-07-27 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US8003604B2 (en) | 2006-11-16 | 2011-08-23 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US7888464B2 (en) | 2006-11-16 | 2011-02-15 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
WO2008096002A1 (en) * | 2007-02-08 | 2008-08-14 | Tibotec Pharmaceuticals Ltd. | Hcv inhibiting macrocyclic phosphonates and amidophosphates |
EP2111396B1 (en) * | 2007-02-08 | 2013-08-07 | Janssen R&D Ireland | Hcv inhibiting macrocyclic phenylcarbamates |
US8383583B2 (en) | 2007-10-26 | 2013-02-26 | Enanta Pharmaceuticals, Inc. | Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors |
US8426360B2 (en) * | 2007-11-13 | 2013-04-23 | Enanta Pharmaceuticals, Inc. | Carbocyclic oxime hepatitis C virus serine protease inhibitors |
US8263549B2 (en) | 2007-11-29 | 2012-09-11 | Enanta Pharmaceuticals, Inc. | C5-substituted, proline-derived, macrocyclic hepatitis C serine protease inhibitors |
WO2009085978A1 (en) | 2007-12-20 | 2009-07-09 | Enanta Pharceuticals, Inc. | Bridged carbocyclic oxime hepatitis c virus serine protease inhibitors |
US8202996B2 (en) | 2007-12-21 | 2012-06-19 | Bristol-Myers Squibb Company | Crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N- ((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide |
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US8163921B2 (en) | 2008-04-16 | 2012-04-24 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
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US8207341B2 (en) | 2008-09-04 | 2012-06-26 | Bristol-Myers Squibb Company | Process or synthesizing substituted isoquinolines |
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US8563505B2 (en) | 2008-09-29 | 2013-10-22 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
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US8283310B2 (en) | 2008-12-15 | 2012-10-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
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US9334279B2 (en) | 2012-11-02 | 2016-05-10 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
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KR100940619B1 (ko) | 2003-02-07 | 2010-02-05 | 이난타 파마슈티칼스, 인코포레이티드 | 마크로사이클릭 씨형 간염 세린 단백효소 억제제 |
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US7642235B2 (en) * | 2003-09-22 | 2010-01-05 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis C virus |
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-
2006
- 2006-07-28 SI SI200630978T patent/SI1919899T1/sl unknown
- 2006-07-28 CN CN2006800355619A patent/CN101273028B/zh not_active Expired - Fee Related
- 2006-07-28 WO PCT/EP2006/064817 patent/WO2007014923A1/en active Application Filing
- 2006-07-28 EP EP20060778070 patent/EP1919899B1/en active Active
- 2006-07-28 PL PL06778070T patent/PL1919899T3/pl unknown
- 2006-07-28 KR KR20087003697A patent/KR101381176B1/ko not_active IP Right Cessation
- 2006-07-28 EA EA200800478A patent/EA013475B1/ru not_active IP Right Cessation
- 2006-07-28 DE DE200660019741 patent/DE602006019741D1/de active Active
- 2006-07-28 AU AU2006274862A patent/AU2006274862B2/en not_active Ceased
- 2006-07-28 MY MYPI20063663 patent/MY141245A/en unknown
- 2006-07-28 CA CA2617099A patent/CA2617099C/en not_active Expired - Fee Related
- 2006-07-28 ES ES06778070T patent/ES2359939T3/es active Active
- 2006-07-28 AT AT06778070T patent/ATE496042T1/de not_active IP Right Cessation
- 2006-07-28 BR BRPI0614620-1A patent/BRPI0614620A2/pt not_active IP Right Cessation
- 2006-07-28 DK DK06778070T patent/DK1919899T3/da active
- 2006-07-28 TW TW95127586A patent/TWI382025B/zh not_active IP Right Cessation
- 2006-07-28 AR ARP060103309 patent/AR057703A1/es unknown
- 2006-07-28 JP JP2008523379A patent/JP5230415B2/ja not_active Expired - Fee Related
-
2008
- 2008-01-16 US US11/995,869 patent/US9023808B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
PL1919899T3 (pl) | 2011-06-30 |
SI1919899T1 (sl) | 2011-05-31 |
AU2006274862A1 (en) | 2007-02-08 |
EP1919899A1 (en) | 2008-05-14 |
US9023808B2 (en) | 2015-05-05 |
CA2617099C (en) | 2014-03-25 |
US20090247512A1 (en) | 2009-10-01 |
EA200800478A1 (ru) | 2008-08-29 |
JP5230415B2 (ja) | 2013-07-10 |
EA013475B1 (ru) | 2010-04-30 |
DK1919899T3 (da) | 2011-08-01 |
WO2007014923A1 (en) | 2007-02-08 |
KR20080039422A (ko) | 2008-05-07 |
JP2009502886A (ja) | 2009-01-29 |
ATE496042T1 (de) | 2011-02-15 |
TW200800949A (en) | 2008-01-01 |
AU2006274862B2 (en) | 2012-03-22 |
MY141245A (en) | 2010-03-31 |
CA2617099A1 (en) | 2007-02-08 |
BRPI0614620A2 (pt) | 2011-04-12 |
TWI382025B (zh) | 2013-01-11 |
EP1919899B1 (en) | 2011-01-19 |
DE602006019741D1 (de) | 2011-03-03 |
ES2359939T3 (es) | 2011-05-30 |
CN101273028A (zh) | 2008-09-24 |
KR101381176B1 (ko) | 2014-04-11 |
CN101273028B (zh) | 2013-08-21 |
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