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CO5680449A2 - Inhibidores macrociclicos de la serina proteasa ns3 del virus de la hepatitis c - Google Patents

Inhibidores macrociclicos de la serina proteasa ns3 del virus de la hepatitis c

Info

Publication number
CO5680449A2
CO5680449A2 CO06029608A CO06029608A CO5680449A2 CO 5680449 A2 CO5680449 A2 CO 5680449A2 CO 06029608 A CO06029608 A CO 06029608A CO 06029608 A CO06029608 A CO 06029608A CO 5680449 A2 CO5680449 A2 CO 5680449A2
Authority
CO
Colombia
Prior art keywords
r1and
r2and
nr12r13
r3and
r4and
Prior art date
Application number
CO06029608A
Other languages
English (en)
Inventor
Srikanth Venkatraman
F George Njoroge
Wanli Wu
Vallabhan Viyyoor M Girija
Brian A Mckittrick
Jing Su
Francisco Velasquez
Patrick Pinto
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.)
Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Publication of CO5680449A2 publication Critical patent/CO5680449A2/es

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D245/00Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/04Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/21Interferons [IFN]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/21Interferons [IFN]
    • A61K38/212IFN-alpha
    • 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
    • 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
    • C04CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04BLIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632Organic additives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
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    • 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
    • C07K5/0217Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -C(=O)-C-N-C(=O)-N-C-C(=O)-
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
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  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Materials Engineering (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

1.- Un compuesto que posee la estructura general que se muestra en la Fórmula 1: o sales, solvatos o ésteres aceptables para uso farmacéutico de dicho compuesto en el cual:(1) R1 es -C(O)R5 o -B(OR)2;(2) R5 es H, -OH, -OR8, -NR9R10, -C(O)OR8, -C(O)NR9R10, -CF3, -C2F5, C3F7, -CF2R6, -R6, -C(O)R7 o NR7SO2R8;(3) R7 es H, -OH, -OR8 o -CHR9R10;(4) R6, R8, R9 y R10 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, alquenilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, arilalquilo, heteroarilalquilo, R14, -CH(R1AND#39)CH(R1AND#39)C(O)OR11, -[CH(R1AND#39)]pC(O)OR11, -[CH(R1AND#39)]pC(O)NR12R13,-[CH(R1AND#39)]pS(O2)R11,-[CH(R1AND#39)]pC(O)R11,-[CH(R1AND#39)]pS(O2)NR12R13, -CH(R1AND#39)C(O)N(H)CH(R2AND#39)(RAND#39),-CH(R1AND#39)CH(R1AND#39)C(O)NR12R13,-CH(R1AND#39)CH(R1AND#39)S(O2)R11, -CH(R1AND#39)CH(R1AND#39)S(O2)NR12R13,-CH(R1AND#39)CH(R1AND#39)C(O)R11,-[CH(R1AND#39)]pCH(OH)R11, -CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)OR11,-C(O)N(H)CH(R2AND#39)C(O)OR11, -C(O)N(H)CH(R2AND#39)C(O)R11,-CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)NR12R13,-CH(R1AND#39)C(O)N(H)CH(R2AND#39)RAND#39,-CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)N(H)CH(R3AND#39)C(O)OR11, -CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)CH(R3AND#39)NR12R13, -CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)N(H)CH(R3AND#39)C(O)NR12R13,-CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)N(H)CH(R3AND#39)C(O)N(H)CH (R4AND#39)C(O)OR11, -CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)N(H)CH(R3AND#39)C(O)N(H)CH(R4AND#39)C(O)NR12R13, -CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)N(H)CH(R3AND#39)C(O)N(H)CH(R4AND#39)C(O)N(H)-CH(R5AND#39)-C(O)OR11 y -CH(R1AND#39)C(O)N(H)CH(R2AND#39)C(O)N(H)CH(R3AND#39)C(O)N(H)CH (R4AND#39)C(O)N(H)-CH(R5AND#39)C(O)NR12R13; ...
CO06029608A 2003-09-26 2006-03-24 Inhibidores macrociclicos de la serina proteasa ns3 del virus de la hepatitis c CO5680449A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US50663703P 2003-09-26 2003-09-26

Publications (1)

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CO5680449A2 true CO5680449A2 (es) 2006-09-29

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CO06029608A CO5680449A2 (es) 2003-09-26 2006-03-24 Inhibidores macrociclicos de la serina proteasa ns3 del virus de la hepatitis c

Country Status (21)

Country Link
US (1) US7592419B2 (es)
EP (1) EP1664092B1 (es)
JP (2) JP4525982B2 (es)
KR (1) KR20060085248A (es)
CN (1) CN1894274A (es)
AR (1) AR046166A1 (es)
AT (1) ATE497505T1 (es)
AU (1) AU2004276281A1 (es)
BR (1) BRPI0414814A (es)
CA (1) CA2540031A1 (es)
CO (1) CO5680449A2 (es)
DE (1) DE602004031298D1 (es)
EC (1) ECSP066456A (es)
IL (1) IL174459A0 (es)
MX (1) MXPA06003455A (es)
NO (1) NO20061822L (es)
PE (1) PE20050953A1 (es)
RU (1) RU2006113880A (es)
TW (1) TWI280964B (es)
WO (1) WO2005030796A1 (es)
ZA (1) ZA200602447B (es)

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