JP2005535574A - セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター - Google Patents

セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター Download PDF

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JP2005535574A
JP2005535574A JP2003584048A JP2003584048A JP2005535574A JP 2005535574 A JP2005535574 A JP 2005535574A JP 2003584048 A JP2003584048 A JP 2003584048A JP 2003584048 A JP2003584048 A JP 2003584048A JP 2005535574 A JP2005535574 A JP 2005535574A
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aliphatic
compound
aryl
cycloalkyl
ring
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JP2005535574A5 (US08039623-20111018-C00020.png
Inventor
ジャノス ピットリック,
ケビン エム. コットレル,
ルック ジェイ. ファーマー,
ロバート ビー. ペルニ,
ロレンス エフ. コートニー,
ドリー, ジョン エイチ. ヴァン
マーク エー. ムルコ,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of JP2005535574A publication Critical patent/JP2005535574A/ja
Publication of JP2005535574A5 publication Critical patent/JP2005535574A5/ja
Pending legal-status Critical Current

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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
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
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    • 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
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12Radicals substituted by oxygen atoms
    • 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
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    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
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    • 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
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    • 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
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    • 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
    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
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    • 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
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
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    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/08Tripeptides
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    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/10Tetrapeptides
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic
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    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/10Tetrapeptides
    • C07K5/1027Tetrapeptides containing heteroatoms different from O, S, or N

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
JP2003584048A 2002-04-11 2003-04-11 セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター Pending JP2005535574A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37184602P 2002-04-11 2002-04-11
PCT/US2003/011459 WO2003087092A2 (en) 2002-04-11 2003-04-11 Inhibitors of serine proteases, particularly hepatitis c virus ns3 - ns4 protease

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2009128587A Division JP2009185081A (ja) 2002-04-11 2009-05-28 セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター

Publications (2)

Publication Number Publication Date
JP2005535574A true JP2005535574A (ja) 2005-11-24
JP2005535574A5 JP2005535574A5 (US08039623-20111018-C00020.png) 2006-06-01

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ID=29250748

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2003584048A Pending JP2005535574A (ja) 2002-04-11 2003-04-11 セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター
JP2009128587A Pending JP2009185081A (ja) 2002-04-11 2009-05-28 セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター
JP2010151000A Pending JP2010241821A (ja) 2002-04-11 2010-07-01 セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター

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JP2009128587A Pending JP2009185081A (ja) 2002-04-11 2009-05-28 セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター
JP2010151000A Pending JP2010241821A (ja) 2002-04-11 2010-07-01 セリンプロテアーゼ、特にhcvns3−ns4aプロテアーゼのインヒビター

Country Status (18)

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US (3) US7273885B2 (US08039623-20111018-C00020.png)
EP (2) EP2468744A2 (US08039623-20111018-C00020.png)
JP (3) JP2005535574A (US08039623-20111018-C00020.png)
KR (2) KR20110028665A (US08039623-20111018-C00020.png)
CN (2) CN100381440C (US08039623-20111018-C00020.png)
AU (2) AU2003223602B8 (US08039623-20111018-C00020.png)
CA (1) CA2481369C (US08039623-20111018-C00020.png)
HK (1) HK1081196A1 (US08039623-20111018-C00020.png)
IL (1) IL164455A0 (US08039623-20111018-C00020.png)
MX (1) MXPA04009938A (US08039623-20111018-C00020.png)
NO (2) NO20044889L (US08039623-20111018-C00020.png)
NZ (2) NZ561851A (US08039623-20111018-C00020.png)
PL (1) PL373399A1 (US08039623-20111018-C00020.png)
RU (1) RU2004133044A (US08039623-20111018-C00020.png)
SG (1) SG159385A1 (US08039623-20111018-C00020.png)
TW (1) TW200403236A (US08039623-20111018-C00020.png)
WO (1) WO2003087092A2 (US08039623-20111018-C00020.png)
ZA (1) ZA200408243B (US08039623-20111018-C00020.png)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007504251A (ja) * 2003-09-05 2007-03-01 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にhcvns3‐ns4aの阻害剤
JP2007532474A (ja) * 2003-10-10 2007-11-15 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にhcvのns3−ns4aプロテアーゼの阻害剤
US8314141B2 (en) 1996-10-18 2012-11-20 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease

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TW200510391A (en) * 2003-04-11 2005-03-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
EP2332935A1 (en) 2003-04-11 2011-06-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
AU2011203054B2 (en) * 2003-04-11 2012-04-26 Vertex Pharmaceuticals, Incorporated Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease
CN1852920B (zh) 2003-07-18 2010-12-15 沃泰克斯药物股份有限公司 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂
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