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) EP2402009A1 (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 (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ298749B6 (cs) * 1996-10-18 2008-01-16 Vertex Pharmaceuticals Incorporated Inhibitory serinových proteáz a farmaceutické prostředky s jejich obsahem
JP4806154B2 (ja) * 2000-04-03 2011-11-02 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 セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼのインヒビター
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
NZ531681A (en) * 2001-10-24 2007-05-31 Vertex Pharma Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system
JP2005535574A (ja) * 2002-04-11 2005-11-24 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プロテアーゼのインヒビター
TW200510391A (en) * 2003-04-11 2005-03-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
BRPI0412761A (pt) * 2003-07-18 2006-09-26 Vertex Pharma inibidores de serino proteases, particularmente a protease ns3-ns4a do vhc
WO2005021584A2 (en) * 2003-08-26 2005-03-10 Schering Corporation Novel peptidomimetic ns3-serine protease inhibitors of hepatitis c virus
PE20050374A1 (es) * 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
CA2538791A1 (en) 2003-09-18 2005-03-31 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
CA2541634A1 (en) * 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1944042A1 (de) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Kombinationen für die HCV-Behandlung
WO2005067454A2 (en) * 2003-12-23 2005-07-28 Valeant Pharmaceuticals North America Combination therapy for treating hepatitis c virus infection
KR20120090077A (ko) 2004-01-30 2012-08-16 얀센 알 앤드 디 아일랜드 Ｈｃｖ ｎｓ?３ 세린 프로테아제 저해제
EP2311851A3 (de) * 2004-02-04 2011-05-25 Vertex Pharmaceuticals Incorporated Inhibitoren der Serinproteasen, insbesondere der HCV-NS3-NS4A-Protease
AU2005219824B2 (en) * 2004-02-27 2007-11-29 Merck Sharp & Dohme Corp. Novel ketoamides with cyclic p4's as inhibitors of ns3 serine protease of hepatitis c virus
MY145081A (en) * 2004-02-27 2011-12-15 Schering Corp Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease
US7192957B2 (en) * 2004-02-27 2007-03-20 Schering Corporation Compounds as inhibitors of hepatitis C virus NS3 serine protease
CA2583472A1 (en) * 2004-10-01 2006-04-13 Chao Lin Hcv ns3-ns4a protease inhibition
US7465537B2 (en) * 2005-05-01 2008-12-16 The Board Of Trustees Of The University Of Arkansas Compounds and methods for inhibiting hepatitis C virus replication
CN101218224B (zh) 2005-05-13 2013-05-08 Viro化学制药公司 治疗或预防黄病毒感染的组合物和方法
US20070021434A1 (en) * 2005-06-24 2007-01-25 Migenix Inc. Non-nucleoside anti-hepacivirus agents and uses thereof
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
CA2617679A1 (en) * 2005-08-02 2007-02-08 Steve Lyons Inhibitors of serine proteases
CA2619659A1 (en) * 2005-08-19 2007-02-22 Vertex Pharmaceuticals Incorporated Processes and intermediates
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
CA2643688A1 (en) 2006-02-27 2007-08-30 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
PT2104674E (pt) 2006-11-15 2013-07-26 Virochem Pharma Inc Análogos de tiofeno para o tratamento ou prevenção de infeções por flavivírus
WO2008106058A2 (en) 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
GEP20125645B (en) * 2007-02-27 2012-09-25 Vertex Pharma Co-crystals and pharmaceutical compositions comprising the same
WO2009032198A1 (en) 2007-08-30 2009-03-12 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
CA2728226A1 (en) 2008-06-24 2010-01-21 Codexis, Inc. Biocatalytic processes for the preparation of substantially stereomerically pure fused bicyclic proline compounds
JP2013512247A (ja) 2009-11-25 2013-04-11 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症の治療または予防のための５−アルキニル−チオフェン−２−カルボン酸誘導体およびそれらの使用
US20130072523A1 (en) 2009-12-24 2013-03-21 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
TW201139438A (en) 2010-03-24 2011-11-16 Vertex Pharma Analogues for the treatment or prevention of flavivirus infections
WO2011119870A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
MX2012010918A (es) 2010-03-24 2013-01-18 Vertex Pharma Analogos para el tratamiento o prevencion de infecciones por flavivirus.
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
WO2011159826A2 (en) 2010-06-15 2011-12-22 Vertex Pharmaceuticals Incorporated Hcv ns5b protease mutants
EP2585447A2 (de) 2010-06-28 2013-05-01 Vertex Pharmaceuticals Incorporated Verbindungen und verfahren zur behandlung oder vorbeugung von flavivirus-infektionen
WO2012006070A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
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
MX2013001869A (es) 2010-08-17 2013-06-28 Vertex Pharma Compuestos y metodos para el tratamiento o prevencion de infecciones virales por flaviviridae.
AU2012286853A1 (en) 2011-07-26 2013-05-02 Vertex Pharmaceuticals Incorporated Thiophene compounds
WO2013016499A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Methods for preparation of thiophene compounds
US20130123276A1 (en) 2011-11-14 2013-05-16 Sven Ruf Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases
EP2827876A4 (de) 2012-03-22 2015-10-28 Alios Biopharma Inc Pharmazeutische kombinationen mit einem thionucleotidanalog
WO2014053533A1 (en) 2012-10-05 2014-04-10 Sanofi Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation
TW201526899A (zh) 2013-02-28 2015-07-16 Alios Biopharma Inc 醫藥組成物
EP2899207A1 (de) 2014-01-28 2015-07-29 Amikana.Biologics Neues Verfahren zum Testen von HCV-Proteasehemmung
US10728694B2 (en) * 2016-03-08 2020-07-28 Tinoq Inc. Systems and methods for a compound sensor system
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EP0907659A1 (de) 1996-05-10 1999-04-14 Schering Corporation Hepatitis c virus ns3 protease synthetische inhibitoren
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GB9812523D0 (en) 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
US6323180B1 (en) * 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
AR022061A1 (es) * 1998-08-10 2002-09-04 Boehringer Ingelheim Ca Ltd Peptidos inhibidores de la hepatitis c, una composicion farmaceutica que los contiene, el uso de los mismos para preparar una composicion farmaceutica, el uso de un producto intermedio para la preparacion de estos peptidos y un procedimiento para la preparacion de un peptido analogo de los mismos.
WO2001040262A1 (en) * 1999-12-03 2001-06-07 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
JP4806154B2 (ja) 2000-04-03 2011-11-02 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 セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼのインヒビター
MXPA03000627A (es) * 2000-07-21 2004-07-30 Schering Corp Nuevos peptidos como inhibidores de proteasa serina-ns3 del virus de la hepatitis c.
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
CA2449504A1 (en) * 2001-07-11 2003-01-23 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
NZ531681A (en) * 2001-10-24 2007-05-31 Vertex Pharma Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system
JP2005535574A (ja) * 2002-04-11 2005-11-24 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プロテアーゼのインヒビター

Also Published As

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

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