ATE539744T1 - Hemmer von serin-protease, insbesondere von hepatitis-c-virus-ns3-ns4a-protease, mit einem kondensierten ringsystem - Google Patents

Hemmer von serin-protease, insbesondere von hepatitis-c-virus-ns3-ns4a-protease, mit einem kondensierten ringsystem

Info

Publication number
ATE539744T1
ATE539744T1 AT02782236T AT02782236T ATE539744T1 AT E539744 T1 ATE539744 T1 AT E539744T1 AT 02782236 T AT02782236 T AT 02782236T AT 02782236 T AT02782236 T AT 02782236T AT E539744 T1 ATE539744 T1 AT E539744T1
Authority
AT
Austria
Prior art keywords
virus
protease
inhibitors
ring system
condensed ring
Prior art date
Application number
AT02782236T
Other languages
English (en)
Inventor
Robert Perni
Janos Pitlik
Drie John Van
Luc Farmer
Original Assignee
Vertex Pharma
Pernie Robert B
Janos Pitlik
Drie John H Van
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 Pharma, Pernie Robert B, Janos Pitlik, Drie John H Van filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE539744T1 publication Critical patent/ATE539744T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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 three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • 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
    • 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
    • C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • 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
    • 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)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (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)
AT02782236T 2001-10-24 2002-10-24 Hemmer von serin-protease, insbesondere von hepatitis-c-virus-ns3-ns4a-protease, mit einem kondensierten ringsystem ATE539744T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34386201P 2001-10-24 2001-10-24
PCT/US2002/034248 WO2003035060A1 (en) 2001-10-24 2002-10-24 Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4a protease, incorporating a fused ring system

Publications (1)

Publication Number Publication Date
ATE539744T1 true ATE539744T1 (de) 2012-01-15

Family

ID=23348006

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02782236T ATE539744T1 (de) 2001-10-24 2002-10-24 Hemmer von serin-protease, insbesondere von hepatitis-c-virus-ns3-ns4a-protease, mit einem kondensierten ringsystem

Country Status (10)

Country Link
US (3) US7241796B2 (de)
EP (2) EP1441720B8 (de)
JP (2) JP4460294B2 (de)
AT (1) ATE539744T1 (de)
AU (1) AU2002348414B2 (de)
CA (1) CA2462163A1 (de)
MX (1) MXPA04003825A (de)
NZ (1) NZ531681A (de)
WO (1) WO2003035060A1 (de)
ZA (1) ZA200401538B (de)

Families Citing this family (56)

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UA66767C2 (uk) * 1996-10-18 2004-06-15 Вертекс Фармасьютикалс Інкорпорейтед Інгібітори серин-протеаз, фармацевтична композиція, спосіб інгібування активності та спосіб лікування або профілактики вірусної інфекції гепатиту с
DE60111509T2 (de) * 2000-04-03 2006-05-11 Vertex Pharmaceuticals Inc., Cambridge Inhibitoren von Serin-Proteasen, insbesondere der Hepatitis-C-Virus NS23-Protease
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
EP1441720B8 (de) * 2001-10-24 2012-03-28 Vertex Pharmaceuticals Incorporated Hemmer von serin-protease, insbesondere von hepatitis-c-virus-ns3-ns4a-protease, mit einem kondensierten ringsystem
CA2481369C (en) * 2002-04-11 2012-07-10 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 - ns4 protease
TW200523270A (en) * 2003-07-18 2005-07-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV ns3-ns4a protease
MXPA06002250A (es) * 2003-08-26 2006-05-17 Schering Corp Inhibidores peptidomimeticos novedosos de la serina proteasa ns3 del virus de la hepatitis c.
TWI359147B (en) * 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
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RU2006115558A (ru) * 2003-10-10 2007-11-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы сериновых протеаз, особенно hcv ns3-ns4a протеазы
US7365092B2 (en) * 2003-10-10 2008-04-29 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
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EP2374464A3 (de) * 2004-10-01 2011-10-26 Vertex Pharmaceuticals Incorporated HCV N3S-NS4A-Proteasehemmung
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NZ565540A (en) * 2005-08-02 2011-06-30 Vertex Pharma Inhibitors of serine proteases
DE602006013492D1 (de) * 2005-08-19 2010-05-20 Vertex Pharma Verfahren und zwischenprodukte
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
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
US7964624B1 (en) 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
US8039475B2 (en) 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
WO2007109080A2 (en) * 2006-03-16 2007-09-27 Vertex Pharmaceuticals Incorporated Deuterated hepatitis c protease inhibitors
BRPI0718915A2 (pt) 2006-11-15 2013-12-03 Virochem Pharma Inc Análogos de tiofeno para o tratamento ou prevenção de infecções por flavivírus
JP2010519330A (ja) * 2007-02-27 2010-06-03 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 共結晶体およびそれを含む医薬組成物
CN101903392A (zh) 2007-02-27 2010-12-01 弗特克斯药品有限公司 丝氨酸蛋白酶的抑制剂
CN101835774B (zh) 2007-08-30 2014-09-17 弗特克斯药品有限公司 共晶体和包含该共晶体的药物组合物
MX2010014500A (es) 2008-06-24 2011-05-30 Codexis Inc Procedimientos biocataliticos para la preparacion de compuestos de prolina biciclica fusionada sustancialmente estereomericamente puros.
MX2012006026A (es) 2009-11-25 2012-08-15 Vertex Pharma Derivados de acido 5-alquinil-tiofen-2-carboxilico y usos para tratamiento o prevencion de infecciones por flavivirus.
JP2013515746A (ja) 2009-12-24 2013-05-09 ヴァーテックス ファーマシューティカルズ、 インコーポレイテッド フラビウイルス感染症の治療又は予防のための類似体
EP2550278A1 (de) 2010-03-24 2013-01-30 Vertex Pharmaceuticals Incorporated Analoga zur behandlung oder vorbeugung von flavivirus-infektionen
MX2012010918A (es) 2010-03-24 2013-01-18 Vertex Pharma Analogos para el tratamiento o prevencion de infecciones por flavivirus.
WO2011119858A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
TW201141857A (en) 2010-03-24 2011-12-01 Vertex Pharma Analogues for the treatment or prevention of flavivirus infections
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
EP2582717A2 (de) 2010-06-15 2013-04-24 Vertex Pharmaceuticals Incorporated Hcv-ns5b-polymerasemutanten
JP2013531011A (ja) 2010-06-28 2013-08-01 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 フラビウイルス感染の処置または予防のための化合物および方法
WO2012006070A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
WO2012006055A2 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
JP2013534249A (ja) 2010-08-17 2013-09-02 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 フラビウイルス科ウイルス感染の処置または予防のための化合物および方法
WO2013016499A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Methods for preparation of thiophene compounds
TW201313697A (zh) 2011-07-26 2013-04-01 Vertex Pharma 製備噻吩化合物之方法
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Also Published As

Publication number Publication date
MXPA04003825A (es) 2004-07-08
EP1441720A1 (de) 2004-08-04
US20030134889A1 (en) 2003-07-17
EP2402009A1 (de) 2012-01-04
JP4460294B2 (ja) 2010-05-12
NZ531681A (en) 2007-05-31
AU2002348414B2 (en) 2009-10-01
JP2005526002A (ja) 2005-09-02
CA2462163A1 (en) 2003-05-01
US20080045480A1 (en) 2008-02-21
WO2003035060A1 (en) 2003-05-01
US8486989B2 (en) 2013-07-16
US20140010784A1 (en) 2014-01-09
US7241796B2 (en) 2007-07-10
JP2010090150A (ja) 2010-04-22
EP1441720B1 (de) 2012-01-04
EP1441720B8 (de) 2012-03-28
ZA200401538B (en) 2005-04-25

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