ES2240446T3 - Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c. - Google Patents

Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.

Info

Publication number
ES2240446T3
ES2240446T3 ES01924516T ES01924516T ES2240446T3 ES 2240446 T3 ES2240446 T3 ES 2240446T3 ES 01924516 T ES01924516 T ES 01924516T ES 01924516 T ES01924516 T ES 01924516T ES 2240446 T3 ES2240446 T3 ES 2240446T3
Authority
ES
Spain
Prior art keywords
protease
compounds
hepatitis
protease inhibitors
serine
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES01924516T
Other languages
English (en)
Inventor
Robert Perni
John Court
Ethan O'malley
Govinda BHISETTI
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2240446T3 publication Critical patent/ES2240446T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • 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)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

Un compuesto de **fórmula**, en la que: R1 se selecciona de alquilo (C1-C6) lineal o ramificado, o alquenilo o alquinilo (C2-C6) lineal o ramificado, en las que hasta 4 átomos de carbono en R1 están opcional e independientemente sustituidos con un halógeno; y en las que cualquier átomo de hidrógeno unido a cualquier átomo de carbono terminal en R1 está opcional e independientemente sustituido con ¿SH u ¿OH; R3 se selecciona de en las que cada R2 se selecciona independientemente de ¿R11, -Ar, -O-R11, -O-Ar, -O-R11-Ar, -R11-C(O)-R11, -N(R11)2, -N(R11)-C(O)O-R11, -N(R11)-C(O)O-R11-Ar, - C(O)O-R11, -O-C(O)-N(R11)2, halo, -CN, -NO2, -R11-C(O)-R11, -R11-C(O)O-R11, -C(O)-N(R11)2, -C(O)-N(R11)-Ar, -S(O)2-R11, o ¿S(O)2-N(R11)2; en las que hasta 2 átomos de hidrógeno en R2 se sustituyen opcional e independientemente con un grupo diferente seleccionado de ¿R11, -Ar, -O-R11, -O-Ar, -O- R11-Ar, -R11-C(O)-R11, -NH-(R11)2, -N(R11)-C(O)O-R11, - N(R11)-C(O)O-R11-Ar, -C(O)O-R11, -O-C(O)- N(R11)2, halo, -CN, -NO2, -R11-C(O)-R11, -R11-C(O)O-R11, -O-C(O)-R11, -C(O)-N(R11)2, -C(O)-N(R11)-Ar, -N(R11)-C(O)- R11, -R11-C(O)-N(R11)2, -S(O)2-R11 o ¿S(O)2-N(R11)2; en las que cada R11 se selecciona de hidrógeno, alquilo (C1-C6) lineal o ramificado o alquenilo o alquinilo (C2-C6) lineal o ramificado, y en las que hasta 3 átomos de hidrógeno en dicho alquilo, alquenilo o alquinilo están opcional e independientemente sustituidos con halo.
ES01924516T 2000-04-03 2001-03-29 Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c. Expired - Lifetime ES2240446T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19456300P 2000-04-03 2000-04-03
US19833000P 2000-04-18 2000-04-18

Publications (1)

Publication Number Publication Date
ES2240446T3 true ES2240446T3 (es) 2005-10-16

Family

ID=26890159

Family Applications (1)

Application Number Title Priority Date Filing Date
ES01924516T Expired - Lifetime ES2240446T3 (es) 2000-04-03 2001-03-29 Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.

Country Status (11)

Country Link
US (1) US7494988B2 (es)
EP (1) EP1268519B1 (es)
JP (1) JP4806154B2 (es)
AT (1) ATE297946T1 (es)
AU (1) AU2001251165A1 (es)
CA (1) CA2405043A1 (es)
DE (1) DE60111509T2 (es)
ES (1) ES2240446T3 (es)
IL (2) IL152022A0 (es)
PT (1) PT1268519E (es)
WO (1) WO2001074768A2 (es)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117105928A (zh) * 2023-08-22 2023-11-24 上海蓝木化工有限公司 一种蛋白酶抑制剂及其制备方法

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MY148123A (en) * 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
JP4685775B2 (ja) * 2003-09-18 2011-05-18 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、とりわけｈｃｖｎｓ３−ｎｓ４ａプロテアーゼの阻害剤
RU2006115558A (ru) * 2003-10-10 2007-11-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы сериновых протеаз, особенно hcv ns3-ns4a протеазы
EP2311851A3 (en) * 2004-02-04 2011-05-25 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
AR055395A1 (es) * 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117105928A (zh) * 2023-08-22 2023-11-24 上海蓝木化工有限公司 一种蛋白酶抑制剂及其制备方法
CN117105928B (zh) * 2023-08-22 2024-03-26 上海蓝木化工有限公司 一种蛋白酶抑制剂及其制备方法

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JP4806154B2 (ja) 2011-11-02
IL152022A0 (en) 2003-04-10
US7494988B2 (en) 2009-02-24
EP1268519B1 (en) 2005-06-15
WO2001074768A3 (en) 2002-06-06
ATE297946T1 (de) 2005-07-15
IL152022A (en) 2008-07-08
AU2001251165A1 (en) 2001-10-15
WO2001074768A2 (en) 2001-10-11
JP2003529583A (ja) 2003-10-07
US20030236242A1 (en) 2003-12-25
CA2405043A1 (en) 2001-10-11
DE60111509D1 (de) 2005-07-21
EP1268519A2 (en) 2003-01-02
DE60111509T2 (de) 2006-05-11

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