WO2004072243A3 - Inhibiteurs macrocycliques de la serine protease de l'hepatite c - Google Patents

Inhibiteurs macrocycliques de la serine protease de l'hepatite c Download PDF

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Publication number
WO2004072243A3
WO2004072243A3 PCT/US2004/003479 US2004003479W WO2004072243A3 WO 2004072243 A3 WO2004072243 A3 WO 2004072243A3 US 2004003479 W US2004003479 W US 2004003479W WO 2004072243 A3 WO2004072243 A3 WO 2004072243A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
present
hepatitis
serine protease
relates
Prior art date
Application number
PCT/US2004/003479
Other languages
English (en)
Other versions
WO2004072243A2 (fr
Inventor
Zenwei Miao
Ying Sun
Frank Wu
Suanne Nakajima
Guoyou Xu
Yat Sun Or
Zhe Wang
Original Assignee
Enanta Pharm Inc
Zenwei Miao
Ying Sun
Frank Wu
Suanne Nakajima
Guoyou Xu
Yat Sun Or
Zhe Wang
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
Priority claimed from US10/384,120 external-priority patent/US20040180815A1/en
Application filed by Enanta Pharm Inc, Zenwei Miao, Ying Sun, Frank Wu, Suanne Nakajima, Guoyou Xu, Yat Sun Or, Zhe Wang filed Critical Enanta Pharm Inc
Priority to CNA2004800092686A priority Critical patent/CN1771050A/zh
Priority to EP04709020A priority patent/EP1590442A4/fr
Priority to AU2004211637A priority patent/AU2004211637C1/en
Priority to JP2006503381A priority patent/JP2007524576A/ja
Priority to CA002515216A priority patent/CA2515216A1/fr
Publication of WO2004072243A2 publication Critical patent/WO2004072243A2/fr
Publication of WO2004072243A3 publication Critical patent/WO2004072243A3/fr

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    • CCHEMISTRY; METALLURGY
    • 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
    • C07K5/12Cyclic peptides with only normal peptide bonds in the ring
    • CCHEMISTRY; METALLURGY
    • 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
    • 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
    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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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)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

L'invention concerne des composés de la formule (I, II ou III), ou un sel, un ester ou un promédicament pharmaceutiquement acceptable de ceux-ci, dans laquelle W représente un système de noyau hétérocyclique substitué ou non substitué. Ces composés inhibent l'activité de la sérine protéase, en particulier celle de la protéase du virus de l'hépatite C (VHC) NS3-NS4A. En conséquence, ces composés, qui interfèrent avec le cycle de vie du virus de l'hépatite C, sont également utiles en tant qu'antiviraux. L'invention concerne également des compositions pharmaceutiques comprenant les composés précités à administrer au patient souffrant d'une infection du VHC. L'invention concerne en outre des procédés de traitement d'une infection du VHC chez un patient par administration d'une composition pharmaceutique comprenant lesdits composés.
PCT/US2004/003479 2003-02-07 2004-02-06 Inhibiteurs macrocycliques de la serine protease de l'hepatite c WO2004072243A2 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
CNA2004800092686A CN1771050A (zh) 2003-02-07 2004-02-06 丙型肝炎丝氨酸蛋白酶的大环抑制剂
EP04709020A EP1590442A4 (fr) 2003-02-07 2004-02-06 Inhibiteurs macrocycliques de la serine protease de l'hepatite c
AU2004211637A AU2004211637C1 (en) 2003-02-07 2004-02-06 Macrocyclic hepatitis C serine protease inhibitors
JP2006503381A JP2007524576A (ja) 2003-02-07 2004-02-06 大環状のc型肝炎セリンプロテアーゼ阻害剤
CA002515216A CA2515216A1 (fr) 2003-02-07 2004-02-06 Inhibiteurs macrocycliques de la serine protease de l'hepatite c

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US36094703A 2003-02-07 2003-02-07
US10/360,947 2003-02-07
US36585403A 2003-02-13 2003-02-13
US10/365,854 2003-02-13
US10/384,120 US20040180815A1 (en) 2003-03-07 2003-03-07 Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
US10/384,120 2003-03-07

Publications (2)

Publication Number Publication Date
WO2004072243A2 WO2004072243A2 (fr) 2004-08-26
WO2004072243A3 true WO2004072243A3 (fr) 2005-11-03

Family

ID=32872697

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/003479 WO2004072243A2 (fr) 2003-02-07 2004-02-06 Inhibiteurs macrocycliques de la serine protease de l'hepatite c

Country Status (7)

Country Link
EP (1) EP1590442A4 (fr)
JP (1) JP2007524576A (fr)
KR (1) KR100940619B1 (fr)
CN (1) CN1771050A (fr)
AU (1) AU2004211637C1 (fr)
CA (1) CA2515216A1 (fr)
WO (1) WO2004072243A2 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8993595B2 (en) 2009-04-08 2015-03-31 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
US9284307B2 (en) 2009-08-05 2016-03-15 Idenix Pharmaceuticals Llc Macrocyclic serine protease inhibitors
US9353100B2 (en) 2011-02-10 2016-05-31 Idenix Pharmaceuticals Llc Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating HCV infections

Families Citing this family (105)

* Cited by examiner, † Cited by third party
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KR20050111585A (ko) 2005-11-25
AU2004211637B2 (en) 2009-08-13
AU2004211637A1 (en) 2004-08-26
CA2515216A1 (fr) 2004-08-26
JP2007524576A (ja) 2007-08-30
EP1590442A4 (fr) 2007-07-18
CN1771050A (zh) 2006-05-10
WO2004072243A2 (fr) 2004-08-26
EP1590442A2 (fr) 2005-11-02
AU2004211637C1 (en) 2010-08-19
KR100940619B1 (ko) 2010-02-05

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