AR045916A1 - Tetrapeptidos con actividad inhibitoria de proteasas serinas, en especial proteasa ns3-ns4a del vhc y composiciones farmaceuticas que las contienen. - Google Patents
Tetrapeptidos con actividad inhibitoria de proteasas serinas, en especial proteasa ns3-ns4a del vhc y composiciones farmaceuticas que las contienen.Info
- Publication number
- AR045916A1 AR045916A1 ARP040102546A ARP040102546A AR045916A1 AR 045916 A1 AR045916 A1 AR 045916A1 AR P040102546 A ARP040102546 A AR P040102546A AR P040102546 A ARP040102546 A AR P040102546A AR 045916 A1 AR045916 A1 AR 045916A1
- Authority
- AR
- Argentina
- Prior art keywords
- aliphatic
- acetyl
- dithia
- azaspiro
- cyclohexylglycyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
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- 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
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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
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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
- A61P31/14—Antivirals for RNA viruses
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- 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
Abstract
Compuestos de la fórmula (1) o sales de las mismas farmacéuticamente aceptables, que inhiben la actividad de proteasa de serina, particularmente la actividad del virus de hepatitis C de la proteasa NS3-NS4A. Como tal, actúan interfiriendo con el ciclo de vida del virus de la hepatitis C y son útiles como agentes antivirales. Composiciones farmacéuticamente aceptables que comprenden dichos compuestos. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable de la misma, donde: X y X' son ambos flúor; o X y X' son independientemente C(H), N, NH, O, ó S; y X y X' son tomados junto con los átomos de carbono al cual se enlazan para formar un anillo parcialmente insaturado o saturado de 5- a 7- miembros que posee hasta 4 heteroátomos independientemente seleccionados de N, NH, O, S, SO, y SO2; donde cualquiera de los átomos es opcionalmente sustituidos en particular o en conjunto con hasta 3 sustituyentes seleccionados independientemente de J; y donde dicho anillo es opcionalmente fundido a un segundo anillo seleccionado de arilo de (C6-10), heteroarilo (C5-10), cicloalquilo (C3-10), y un heterociclilo (C3-10), donde dicho segundo anillo posee hasta 3 sustituyentes seleccionados independientemente de J; J es halógeno, -OR', -NO2, -CN, -CF3, -OCF3, -R', oxo, tioxo, =N(R'), =N(OR'), 1,2-metilendioxi, 1,2-etilenedioxi, -N(R')2, -SR', -SOR', -SO2R', -SO2N(R')2, -SO3R', -C(O)R', -C(O)C(O)R', -C(O)C(O)OR', -C(O)C(O)NR', - C(O)CH2C(O)R', -C(S)R', -C(S)OR', -C(O)OR', -OC(O)R', -C(O)N(R')2, -OC(O)N(R')2, -C(S)N(R')2, -(CH2)0-2NHC(O)R', -N(R')N(R')COR', -N(R')N(R')C(O)OR', -N(R')N(R')CON(R')2, -N(R')SO2R', -N(R')SO2N(R')2, -N(R')C(O)OR', -N(R')C(O)R', -N(R')C(S)R', - N(R')C(O)N(R')2, -N(R')C(S)N(R')2, -N(COR')COR', -N(OR')R', -C(=NH)N(R')2, -C(O)N(OR')R', -C(=NOR')R', -OP(O)(OR')2, -P(O)(R')2, -P(O)(OR')2, o -P(O)(H)(OR'); donde: R' es seleccionado independientemente de: hidrógeno-; (C1-12)-alifático-; (C3-10)- cicloalquilo- o -cicloalquenilo-; [(C3-10)-cicloalquilo o -cicloalquenilo]-(C1-12)-alifático-; (C6-10)-arilo-; (C6-10)-arilo-(C1-12)alifático-; (C3-10)-heterociclilo-; (C3-10)-heterociclilo-(C1-12)alifático-; (C5-10)-heteroarilo-; y (C5-10)- heteroarilo-(C1-12)-alifático-; donde hasta 5 átomos en R' son opcionalmente e independientemente sustituidos con J; donde dos grupos R' se enlazan al mismo átomo para formar un anillo no aromático o aromático de 3- a 10- miembros que posee hasta 3 heteroátomos independientemente seleccionados de N, NH, O, S, SO, y SO2, donde dicho anillo es opcionalmente fundido en un arilo (C6-10), heteroarilo (C5-10), cicloalquilo (C3-10), o un heterociclilo (C3-10), donde cualquiera de los anillos posee hasta 3 sustituyentes seleccionados independientemente de J; Y y Y' son independientemente: hidrógeno-; (C1-12)-alifático-; (C3-10)-cicloalquilo- o -cicloalquenilo-; (C3-10)-cicloalquilo-(C1-12)-alifático-; (C6-10)-arilo-; (C3-10)-heterociclilo-; o (C5-10)-heteroarilo-; donde hasta tres de los átomos de carbono alifáticos en Y y Y' pueden ser reemplazados por O, N, NH, S, SO, o SO2; donde cada uno de Y y Y' es independientemente y opcionalmente sustituido con hasta 3 sustituyentes seleccionados independientemente de J; R1 y R3 son independientemente: (C1-12)-alifático-; (C3-10)-cicloalquilo- o -cicloalquenilo-; [(C3-10)-cicloalquilo o -cicloalquenilo]-(C1-12)-alifático-; (C6-10)-arilo-(C1-12)alifático-; o (C5-10)-heteroarilo- (C1-12)-alifático-; donde hasta 3 átomos de carbono alifáticos en R1 y R3 pueden ser reemplazados por un heteroátomo seleccionado de O, N, NH, S, SO, ó SO2 en una disposición estable químicamente; donde cada uno de R1 y R3 es independiente y opcionalmente sustituido con hasta 3 sustituyentes independientemente seleccionados de J; R2, R4, y R7 son independientemente: hidrógeno-; (C1-12)-alifático-; (C3-10)-cicloalquilo-(C1-12)-alifático-; o (C6-10)-arilo-(C1-12)-alifático-; donde hasta dos átomos de carbono alifáticos en R2, R4, y R7 pueden reemplazarse por un heteroátomo seleccionado de O, N, NH, S, SO, y SO2 en una disposición estable químicamente; donde cada uno de R2, R4, y R7 es opcionalmente e independientemente sustituido con hasta 3 sustituyentes independientes seleccionados de J; R5 y R5' son independientemente hidrógeno o (C1-12)-alifático, donde cualquier hidrógeno es opcionalmente reemplazado con halógeno; donde cualquier átomo de carbono terminal de R5 es sustituido opcionalmente con sulfidrilo o hidroxi; o R5 es Ph o -CH2Ph y R5' es H, donde dicho Ph o grupo -CH2Ph es opcionalmente sustituido con hasta 3 sustituyentes seleccionados independientemente de J; o R5 y R5' junto con el átomo al cual se enlazan forman un anillo de 3- a 6- miembros saturados o parcialmente no saturados que poseen hasta 2 heteroátomos seleccionados de N, NH, O, SO, y SO2; donde el anillo posee hasta 2 sustituyentes seleccionados independientemente de J; W es un resto de grupo de fórmula (2), donde cada R6 es independientemente: hidrógeno-; (C1-12)-alifático-; (C6-10)-arilo-; (C6-10)-arilo-(C1-12)alifático-; (C3-10)-cicloalquilo- o cicloalquenilo-; [(C3-10)-cicloalquilo- o cicloalquenilo]-(C1-12)-alifático-; (C3- 10)-heterociclilo-; (C3-10)-heterociclilo-(C1-12)-alifático-; (C5-10)-heteroarilo-; o (C5-10)-heteroarilo-(C1-12)-alifático-; o dos grupos R6, que son enlazados al mismo átomo de nitrógeno, se forman junto con ese átomo de nitrógeno, un anillo (C3- 10)-heterocíclico; donde R6 es sustituido opcionalmente con hasta 3 J sustituyentes; donde cada R8 es independientemente -OR'; o los grupos R8 junto con los átomos de boron, componen un anillo heterocíclico (C3-10) miembros- que posee además del boron hasta 3 heteroátomos adicionales seleccionados de N, NR', O, SO, y SO2; V es O o enlace de valencia; y T es: (C1-12)-alifático-; (C6-10)-arilo-; (C6-10)-arilo-(C1-12)alifático-; (C3-10)-cicloalquilo o -cicloalquenilo-; [(C3-10)-cicloalquilo o - cicloalquenilo]-(C1-12)-alifático-; (C3-10)-heterociclilo-; (C3-10)-heterociclilo-(C1-12)-alifático-; (C5-10)-heteroarilo-; o (C5-10)-heteroarilo-(C1-12)-alifático-; donde hasta 3 átomos de carbono alifáticos en T pueden reemplazarse por un heteroátomo seleccionado de O, N, NH, S, SO, o SO2 en una disposición químicamente estable; donde cada T es sustituido opcionalmente con hasta 3 sustituyentes J; siempre que los siguientes compuestos sean excluidos: a) N-acetil-L-leucilo-(2S)-2- ciclohexilglicil-(3S)-6,10-ditia-2-azaspiro[4.5]decano-3-carbonil-3-amino-2-oxohexanoilglicil-2-fenilo-1,1-éster glicino dimetiletilo; b) N-acetil-L-leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2-azaspiro[4.5]decano-3-carbonil-3-amino-2- oxohexanoilglicil-2-fenilo-glicina; c) N-acetil-L-leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2-azaspiro[4.5]decano-3-carbonil-3-amino-2-oxohexanoilglicil-2-fenil-glicinamida; d) N-acetil-L-leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2- azaspiro[4.5]decano-3-carbonil-3-amino-2-oxohexanoilglicil-N,N-dimetil-2-fenil-glicinamida; e) N-acetil-L-leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2-azaspiro[4.5]decano-3-carbonil-3-amino-2-oxohexanoilglicilo-N-metoxi-N-metil-2-fenil- glicinamida; f) (2S)-N-acetil-L-leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2-azaspiro[4.5]decano-3-carbonil-3-amino-2-oxohexanoilglicil-2-fenilo-1,1-éster dimetiletil, glicina; g) (2S)-N-acetil-L-leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2- azaspiro[4.5]decano-3-carbonil-3-amino-2-oxohexanoilglicil-2-fenil-glicinao; h) (2S)-N-acetil-L-leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2-azaspiro[4.5]decano-3-carbonil-3-amino-2-oxohexanoilglicil-2-fenilo-glicinamida; i) (2S)-N-acetil-L- leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2-azaspiro[4.5]decano-3-carbonil-3-amino-2-oxohexanoilglicil-N,N-dimetil-2-fenilo-glicinamida; j) (2S)-N-acetil-L-leucil-(2S)-2-ciclohexilglicil-(3S)-6,10-ditia-2-azaspiro[4.5]decano-3-carbonil-3-amino- 2-oxohexanoilglicil-N-metoxi-N-metil-2-fenil-glicinamida; k) N-acetil-L-alfa-glutamil-L-alfa-glutamil-L-valil-L-valil-N-[1-[oxo(2-propenilamina)acetil]butil]-, bis(1,1-dimetiletil)éster-(8S)-1,4-ditia-7-azaspiro[4.4]nonano-8-carboxamida; l) N-acetil- L-alfa-glutamil-L-alfa-glutamil-L-valil-L-valil-N-[1-[oxo(2-propenilamino)acetil]butil]-, 2-(1,1-dimetiletil)éster-(8S)-1,4-ditia-7-azaspiro[4.4]nonano-8-carboxamida; m) N-acetil-L-alfa-glutamil-L-alfa-glutamil-L-valil-L-valil-N-[1-[oxo(2- propenilamina)acetil]butil]-(8S)-1,4-ditia-7-azaspiro[4.4]nonano-8-carboxamida; n) N-acetil-L-alfa-glutamil-L-alfa-glutamil-L-valil-2-ciclohexilglicil-(8S)-1,4-ditia-7-azaspiro[4.4]nonano-8-carbonil-3-amino-2-oxohexanoil-glicina; o) N-acetil-L-alfa- glutamil-L-alfa-glutamil-L-valil-2-ciclohexilglicil-(8S)-1,4-ditia-7-azaspiro[4.4]nonano-8-carbonil-3-amino-2-oxohexanoilglicil-2-fenil-glicinamida; p) N-acetil-L-alfa-glutamil-L-alfa-glutamil-L-valil-2-ciclohexilglicil-(8S)-1,4-ditia-7- azaspiro[4.4]nonano-8-carbonil-3-amino-2-oxohexanoil-1,2-bis(1,1-dimetiletil)-7-(2-propenil)éster de glicina; y q) N-acetil-L-alfa-glutamil-L-alfa-glutamil-L-valil-2-ciclohexilglicil-(8S)-1,4-ditia-7-azaspiro[4.4]nonano-8-carbonil-3-amino-2- oxohexanoil-1,2,-bis(1,1-dimetiletil)éster de glicina.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US48853503P | 2003-07-18 | 2003-07-18 |
Publications (1)
Publication Number | Publication Date |
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AR045916A1 true AR045916A1 (es) | 2005-11-16 |
Family
ID=34079432
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040102546A AR045916A1 (es) | 2003-07-18 | 2004-07-19 | Tetrapeptidos con actividad inhibitoria de proteasas serinas, en especial proteasa ns3-ns4a del vhc y composiciones farmaceuticas que las contienen. |
Country Status (19)
Country | Link |
---|---|
US (2) | US7109172B2 (es) |
EP (3) | EP2368900A3 (es) |
JP (2) | JP4745230B2 (es) |
KR (2) | KR20060052836A (es) |
CN (3) | CN102020700A (es) |
AR (1) | AR045916A1 (es) |
AU (2) | AU2004257288A1 (es) |
BR (1) | BRPI0412761A (es) |
CA (1) | CA2532664A1 (es) |
HK (1) | HK1098164A1 (es) |
IL (2) | IL173180A0 (es) |
NO (1) | NO20060706L (es) |
NZ (1) | NZ544789A (es) |
PE (1) | PE20050251A1 (es) |
RU (1) | RU2412198C2 (es) |
TW (1) | TW200523270A (es) |
UY (1) | UY28423A1 (es) |
WO (1) | WO2005007681A2 (es) |
ZA (1) | ZA200601420B (es) |
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- 2004-07-16 AU AU2004257288A patent/AU2004257288A1/en not_active Abandoned
- 2004-07-16 CN CN2010105148844A patent/CN102020700A/zh active Pending
- 2004-07-16 EP EP10182578A patent/EP2368900A3/en not_active Withdrawn
- 2004-07-16 PE PE2004000685A patent/PE20050251A1/es not_active Application Discontinuation
- 2004-07-16 EP EP10176709A patent/EP2341065A3/en not_active Withdrawn
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- 2004-07-16 CN CN200910225229A patent/CN101724022A/zh active Pending
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