AR048241A1 - Compuestos azufrados como inhibidores de la serina proteasa ns3 del virus de la hepatitis c . - Google Patents

Compuestos azufrados como inhibidores de la serina proteasa ns3 del virus de la hepatitis c .

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Publication number
AR048241A1
AR048241A1 ARP050100679A ARP050100679A AR048241A1 AR 048241 A1 AR048241 A1 AR 048241A1 AR P050100679 A ARP050100679 A AR P050100679A AR P050100679 A ARP050100679 A AR P050100679A AR 048241 A1 AR048241 A1 AR 048241A1
Authority
AR
Argentina
Prior art keywords
heterocyclyl
heteroaryl
aryl
cycloalkyl
alkyl
Prior art date
Application number
ARP050100679A
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English (en)
Original Assignee
Schering Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Schering Corp filed Critical Schering Corp
Publication of AR048241A1 publication Critical patent/AR048241A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D411/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Abstract

La presente trata de compuestos azufrados como inhibidores de la serina proteasa NS3 del virus de la hepatitis C, composiciones farmacéuticas que los contienen, usos y métodos de preparacion. Reivindicacion 1: Un compuesto, o enantiomeros, estereoisomeros, rotámeros, tautomeros y racematos de dicho compuesto, o una sal o solvato o éster aceptables desde el punto de vista farmacéutico de dicho compuesto, teniendo dicho compuesto la estructura general que se muestra en la formula (1): en la cual: R1 es H, OR8, NR9R10, o CHR9R10, en los cuales R8, R9, y R10 pueden ser iguales o diferentes, seleccionándose cada uno en forma independiente del grupo formado por: H, alquilo, alquenilo-, alquinilo-, arilo-, heteroalquilo-, heteroarilo- , cicloalquilo-, heterociclilo-, arilalquilo- y heteroarilalquilo; A y M pueden ser iguales o diferentes, seleccionándose cada uno en forma independiente e R, OR, NHR, NRR', SR, SO2R y halo; o A y M están conectados uno al otro de modo tal que el resto de formula (2) que se mostro anteriormente en la formula (1) forma tanto un cicloalquilo de tres, cuatro, seis, siete y ocho miembros, un heterociclilo de cuatro a ocho miembros, un arilo de seis a diez miembros, o un heteroarilo de cinco a diez miembros; E es C(H) o C( R ); L es C(H), C( R ), CH2C( R ), o C( R )CH2; R, R', R2 y R3 pueden ser iguales o diferentes, seleccionándose cada uno en forma independiente del grupo formado por H, alquilo, heteroalquilo, alquenilo, heteroalquenilo, alquinilo, heteroalquinilo, cicloalquilo, heterociclilo, arilo, arilalquilo, heteroarilo, y heteroarilalquilo, o alternativamente R y R' en NRR' están conectados uno al otro e manera tal que NRR' forma un heterociclilo de cuatro a ocho miembros; e Y se selecciona de los siguientes restos de formulas (3), en los cuales G es NH u O; y R15, R16, R17 y R18 pueden ser iguales o diferentes, seleccionándose cada uno en forma independiente del grupo formado por H, alquilo, heteroalquilo, alquenilo, heteroalquenilo, alquinilo, heteroalquinilo, cicloalquilo, heterociclilo, arilo, y heteroarilo, o alternativamente, (i) R15 y R16 están conectados entre sí para formar una estructura cíclica de cuatro a ocho miembros, y (ii) del mismo modo, en forma independiente R17 y R18 están conectados uno al otro para formar un cicloalquilo o heterociclilo de tres a ocho miembros; donde cada uno de dichos alquilo, arilo, heteroarilo, cicloalquilo o heterociclilo pueden estar no sustituidos o estar sustituidos en forma opcional e independiente con uno o más restos seleccionados del grupo formado por: hidroxi, alcoxi, ariloxi, tio, alquiltio, ariltio, amino, amido, alquilamino, arilamino, alquilsulfonilo, arilsulfonilo, sulfonamido, alquilsulfonamido, arilsulfonamido, alquilo, arilo, heteroarilo, ceto, carboxi, carbalcoxi, carboxamido, alcoxicarbonilamino, alcoxicarboniloxi, alquilureido, arilureido, halo, ciano y nitro.
ARP050100679A 2004-02-27 2005-02-24 Compuestos azufrados como inhibidores de la serina proteasa ns3 del virus de la hepatitis c . AR048241A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US54867004P 2004-02-27 2004-02-27

Publications (1)

Publication Number Publication Date
AR048241A1 true AR048241A1 (es) 2006-04-12

Family

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Family Applications (1)

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ARP050100679A AR048241A1 (es) 2004-02-27 2005-02-24 Compuestos azufrados como inhibidores de la serina proteasa ns3 del virus de la hepatitis c .

Country Status (31)

Country Link
US (1) US8067379B2 (es)
EP (1) EP1730110B9 (es)
JP (1) JP4714732B2 (es)
KR (2) KR101316137B1 (es)
CN (2) CN103102389A (es)
AR (1) AR048241A1 (es)
AT (1) ATE470660T1 (es)
AU (1) AU2005222060A1 (es)
BR (1) BRPI0508085A (es)
CA (1) CA2557495C (es)
CY (1) CY1111212T1 (es)
DE (1) DE602005021760D1 (es)
DK (1) DK1730110T3 (es)
EC (1) ECSP066791A (es)
ES (1) ES2346233T3 (es)
HK (1) HK1095819A1 (es)
HR (1) HRP20100416T1 (es)
IL (1) IL177544A (es)
MY (1) MY145081A (es)
NO (1) NO20064358L (es)
NZ (1) NZ549223A (es)
PE (1) PE20051150A1 (es)
PL (1) PL1730110T3 (es)
PT (1) PT1730110E (es)
RS (1) RS51394B (es)
RU (1) RU2428428C9 (es)
SG (1) SG186041A1 (es)
SI (1) SI1730110T1 (es)
TW (2) TWI393704B (es)
WO (1) WO2005087731A1 (es)
ZA (1) ZA200607096B (es)

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US20070042968A1 (en) 2007-02-22
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