AU2003223602B8 - Inhibitors of serine proteases, particularly hepatitis C virus NS3-NS4 protease - Google Patents

Inhibitors of serine proteases, particularly hepatitis C virus NS3-NS4 protease Download PDF

Info

Publication number
AU2003223602B8
AU2003223602B8 AU2003223602A AU2003223602A AU2003223602B8 AU 2003223602 B8 AU2003223602 B8 AU 2003223602B8 AU 2003223602 A AU2003223602 A AU 2003223602A AU 2003223602 A AU2003223602 A AU 2003223602A AU 2003223602 B8 AU2003223602 B8 AU 2003223602B8
Authority
AU
Australia
Prior art keywords
aliphatic
aryl
clo
cycloalkyl
independently
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.)
Ceased
Application number
AU2003223602A
Other languages
English (en)
Other versions
AU2003223602A1 (en
AU2003223602B2 (en
Inventor
Kevin M. Cottrell
Lawrence F. Courtney
Luc J. Farmer
Mark A. Murcko
Robert B. Perni
Janos Pitlik
John H. Van Drie
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
Publication of AU2003223602A1 publication Critical patent/AU2003223602A1/en
Priority to AU2009233604A priority Critical patent/AU2009233604A1/en
Application granted granted Critical
Publication of AU2003223602B2 publication Critical patent/AU2003223602B2/en
Publication of AU2003223602B8 publication Critical patent/AU2003223602B8/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; 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
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • 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
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • 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

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)
  • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (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)
AU2003223602A 2002-04-11 2003-04-11 Inhibitors of serine proteases, particularly hepatitis C virus NS3-NS4 protease Ceased AU2003223602B8 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2009233604A AU2009233604A1 (en) 2002-04-11 2009-10-30 Inhibitors of Serine Proteases, Particularly Hepatitis C Virus NS3-NS4 Protease

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US37184602P 2002-04-11 2002-04-11
US60/371,846 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
AU2009233604A Division AU2009233604A1 (en) 2002-04-11 2009-10-30 Inhibitors of Serine Proteases, Particularly Hepatitis C Virus NS3-NS4 Protease

Publications (3)

Publication Number Publication Date
AU2003223602A1 AU2003223602A1 (en) 2003-10-27
AU2003223602B2 AU2003223602B2 (en) 2010-05-13
AU2003223602B8 true AU2003223602B8 (en) 2010-05-27

Family

ID=29250748

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2003223602A Ceased AU2003223602B8 (en) 2002-04-11 2003-04-11 Inhibitors of serine proteases, particularly hepatitis C virus NS3-NS4 protease
AU2009233604A Abandoned AU2009233604A1 (en) 2002-04-11 2009-10-30 Inhibitors of Serine Proteases, Particularly Hepatitis C Virus NS3-NS4 Protease

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2009233604A Abandoned AU2009233604A1 (en) 2002-04-11 2009-10-30 Inhibitors of Serine Proteases, Particularly Hepatitis C Virus NS3-NS4 Protease

Country Status (17)

Country Link
US (3) US7273885B2 (enExample)
EP (2) EP1497282A2 (enExample)
JP (3) JP2005535574A (enExample)
KR (2) KR20040099425A (enExample)
CN (2) CN101245097A (enExample)
AU (2) AU2003223602B8 (enExample)
CA (1) CA2481369C (enExample)
IL (1) IL164455A0 (enExample)
MX (1) MXPA04009938A (enExample)
NO (2) NO20044889L (enExample)
NZ (2) NZ561851A (enExample)
PL (1) PL373399A1 (enExample)
RU (1) RU2004133044A (enExample)
SG (1) SG159385A1 (enExample)
TW (1) TW200403236A (enExample)
WO (1) WO2003087092A2 (enExample)
ZA (1) ZA200408243B (enExample)

Families Citing this family (121)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU227742B1 (en) * 1996-10-18 2012-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
EP1268519B1 (en) * 2000-04-03 2005-06-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
EP1441720B8 (en) * 2001-10-24 2012-03-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4a protease, incorporating a fused ring system
MXPA04009938A (es) * 2002-04-11 2004-12-13 Vertex Pharma Inhibidores de serina proteasas, en particular la proteasa ns3-ns4a del hcv.
CA2521678A1 (en) 2003-04-11 2004-10-28 Vertex Pharmaceuticals, Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP1613620A1 (en) * 2003-04-11 2006-01-11 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
CN102020700A (zh) * 2003-07-18 2011-04-20 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
PE20050374A1 (es) * 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
TW200526686A (en) 2003-09-18 2005-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
EP1692157B1 (en) 2003-10-10 2013-04-17 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
AU2004285972A1 (en) * 2003-10-28 2005-05-12 Vertex Pharmaceuticals, Incorporated Preparation of 4,5-dialkyl-3-acyl-pyrrole-2-carboxylic acid derivatives by Fischer-Fink type synthesis and subsequent acylation
EP1713822B1 (en) 2004-01-30 2010-03-17 Medivir AB Hcv ns-3 serine protease inhibitors
CN1938332B (zh) * 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
CN102160891A (zh) * 2004-10-01 2011-08-24 威特克斯医药股份有限公司 Hcv ns3-ns4a蛋白酶抑制
ATE497395T1 (de) 2004-12-20 2011-02-15 Codman & Shurtleff Hcv inhibitor zur verwendung in einem verfahren zur behandlung von hepatitis c
EP1890602B1 (en) * 2005-04-20 2011-10-12 Philips Intellectual Property & Standards GmbH Patient monitoring system
MX2007014117A (es) 2005-05-13 2008-02-05 Virochem Pharma Inc Compuestos y metodos para el tratamiento o prevencion de infecciones de flavivirus.
CN101263156A (zh) 2005-07-25 2008-09-10 因特蒙公司 C型肝炎病毒复制的新颖大环抑制剂
CN101273030B (zh) 2005-07-29 2012-07-18 泰博特克药品有限公司 丙型肝炎病毒的大环抑制剂
BRPI0614696A2 (pt) 2005-07-29 2011-04-12 Tibotec Pharm Ltd inibidores macrocìclicos de vìrus da hepatite c
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
JP5426164B2 (ja) 2005-07-29 2014-02-26 ヤンセン・アールアンドデイ・アイルランド Ｃ型肝炎ウイルスの大環式インヒビター
DE602006019883D1 (de) 2005-07-29 2011-03-10 Medivir Ab Makrocyclische inhibitoren des hepatitis-c-virus
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
AR055361A1 (es) 2005-07-29 2007-08-22 Medivir Ab Inhibidores macrociclicos del virus de la hepatitis c
MY141245A (en) 2005-07-29 2010-03-31 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis c virus
JO2768B1 (en) * 2005-07-29 2014-03-15 تيبوتيك فارماسيوتيكالز ليمتد Large cyclic inhibitors of hepatitis C virus
PE20070343A1 (es) 2005-07-29 2007-05-12 Medivir Ab Inhibidores macrociclicos del virus de la hepatitis c
RU2441020C2 (ru) 2005-08-02 2012-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы серинпротеазы
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
US7964624B1 (en) 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
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
CN101415705B (zh) 2005-10-11 2011-10-26 因特蒙公司 抑制丙型肝炎病毒复制的化合物和方法
US7705138B2 (en) * 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
JP5409008B2 (ja) 2005-11-11 2014-02-05 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 Ｃ型肝炎ウイルス改変体
EP1991229A2 (en) 2006-02-27 2008-11-19 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
EP2194039A1 (en) 2006-03-16 2010-06-09 Vertex Pharmceuticals Incorporated Process for preparing optically enriched compounds
WO2007120595A2 (en) * 2006-04-11 2007-10-25 Novartis Ag Amines for the treatment of hcv
WO2007133865A2 (en) 2006-04-11 2007-11-22 Novartis Ag Hcv/hiv inhibitors an their uses
AU2007267470B2 (en) * 2006-06-01 2012-09-20 Sanofi-Aventis Spirocyclic nitriles as protease inhibitors
KR20090024834A (ko) * 2006-07-05 2009-03-09 인터뮨, 인크. Ｃ형 간염 바이러스 복제의 신규 억제제
AP2579A (en) 2006-11-15 2013-01-29 Virochem Pharma Inc Thiophene analogues for the treatment or prevention of flavivirus infections
ES2470568T3 (es) 2006-11-17 2014-06-24 Janssen R&D Ireland Inhibidores macroc�clicos del virus de la hepatitis C
BRPI0807907A2 (pt) 2007-02-27 2017-05-16 Vertex Pharma co-cristais e composições farmacêuticas compreendendo os mesmos.
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
EP2160392A2 (en) * 2007-05-03 2010-03-10 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
WO2008141227A1 (en) * 2007-05-10 2008-11-20 Intermune, Inc. Novel peptide inhibitors of hepatitis c virus replication
TW200922933A (en) 2007-08-30 2009-06-01 Vertex Pharma Co-crystals and pharmaceutical compositions comprising the same
CN104557861A (zh) 2007-12-21 2015-04-29 阿维拉制药公司 Hcv蛋白酶抑制剂和其用途
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
EP2237666A4 (en) 2007-12-21 2012-05-16 Avila Therapeutics Inc HCV PROTEASE INHIBITORS AND USES THEREOF
BRPI0911260A2 (pt) 2008-04-15 2015-09-29 Intermune Inc composto, composição farmacêutica, método de inibição de atividade da protease de ns3/ns4 in, vitro e usos de compostos
US8188137B2 (en) 2008-08-15 2012-05-29 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
KR20110075019A (ko) * 2008-10-15 2011-07-05 인터뮨, 인크. 치료용 항바이러스성 펩티드
US20100173939A1 (en) 2008-12-22 2010-07-08 Gilead Sciences, Inc. Antiviral compounds
AR075584A1 (es) 2009-02-27 2011-04-20 Intermune Inc COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO.
AU2010253791A1 (en) 2009-05-29 2011-11-24 Merck Sharp & Dohme Corp. Antiviral compounds composed of three linked Aryl moieties to treat diseases such as Hepatitis C
HUE030402T2 (en) 2009-09-15 2017-05-29 Taigen Biotechnology Co Ltd HCV protease inhibitors
WO2011038293A1 (en) * 2009-09-28 2011-03-31 Intermune, Inc. Cyclic peptide inhibitors of hepatitis c virus replication
WO2011066241A1 (en) 2009-11-25 2011-06-03 Schering Corporation Fused tricyclic compounds and derivatives thereof useful for the treatment of viral diseases
EP2504329A1 (en) 2009-11-25 2012-10-03 Vertex Pharmaceuticals Incorporated 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections
US20130156731A1 (en) 2009-12-22 2013-06-20 Kevin X. Chen Fused tricyclic compounds and methods of use thereof for the treatment of viral diseas
KR20120130173A (ko) 2009-12-24 2012-11-29 버텍스 파마슈티칼스 인코포레이티드 플라비바이러스 감염을 치료 또는 예방하기 위한 유사체들
AR080676A1 (es) 2010-03-09 2012-05-02 Schering Corp Compuestos de sililo triciclicos fusionados y metodos de uso de los mismos para el tratamiento de enfermedades virales
CA2794145A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated 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
TW201141857A (en) 2010-03-24 2011-12-01 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
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
EP2582717A2 (en) 2010-06-15 2013-04-24 Vertex Pharmaceuticals Incorporated Hcv ns5b polymerase mutants
CA2803248A1 (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
WO2012006070A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
CA2805440A1 (en) 2010-07-26 2012-02-09 Merck Sharp & Dohme Corp. Substituted biphenylene compounds and methods of use thereof for the treatment of viral diseases
WO2012024363A2 (en) 2010-08-17 2012-02-23 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flaviviridae viral infections
JP2013540122A (ja) 2010-09-29 2013-10-31 メルク・シャープ・エンド・ドーム・コーポレイション 縮合四環式化合物誘導体およびウィルス疾患治療のためのそれの使用方法
WO2012142075A1 (en) 2011-04-13 2012-10-18 Merck Sharp & Dohme Corp. 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
EA201391519A1 (ru) 2011-04-13 2014-03-31 Мерк Шарп И Доум Корп. 2'-замещенные нуклеозидные производные и способы их применения для лечения вирусных заболеваний
WO2013016499A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Methods for preparation of thiophene compounds
TW201317223A (zh) 2011-07-26 2013-05-01 Vertex Pharma 噻吩化合物
WO2013033901A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
WO2013033900A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases
WO2013033899A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
WO2013039876A1 (en) 2011-09-14 2013-03-21 Merck Sharp & Dohme Corp. Silyl-containing heterocyclic compounds and methods of use thereof for the treatment of viral diseases
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 (en) 2012-03-22 2015-10-28 Alios Biopharma Inc PHARMACEUTICAL COMBINATIONS WITH A THIONUCLEOTIDE ANALOG
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
US20150065439A1 (en) 2013-02-28 2015-03-05 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
WO2015065817A1 (en) 2013-10-30 2015-05-07 Merck Sharp & Dohme Corp. Pseudopolymorphs of an hcv ns5a inhibitor and uses thereof
EP2899207A1 (en) 2014-01-28 2015-07-29 Amikana.Biologics New method for testing HCV protease inhibition
WO2017070089A1 (en) 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
DK3377488T3 (da) 2015-11-19 2022-10-03 Incyte Corp Heterocykliske forbindelser som immunomodulatorer
MY199705A (en) 2015-12-22 2023-11-20 Incyte Corp Heterocyclic compounds as immunomodulators
TW201808950A (zh) 2016-05-06 2018-03-16 英塞特公司 作為免疫調節劑之雜環化合物
US20170342060A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
SG11201811414TA (en) 2016-06-20 2019-01-30 Incyte Corp Heterocyclic compounds as immunomodulators
ES2971784T3 (es) 2016-06-21 2024-06-07 Orion Ophthalmology LLC Derivados heterocíclicos de prolinamida
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC CARBOCYCLIC PROLINAMIDE DERIVATIVES
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
MA46045A (fr) 2016-08-29 2021-04-28 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
WO2018119266A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Benzooxazole derivatives as immunomodulators
US20180179202A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
RU2650610C1 (ru) 2017-02-28 2018-04-16 Васильевич Иващенко Александр Противовирусная композиция и способ ее применения
FI3774791T3 (fi) 2018-03-30 2023-03-21 Incyte Corp Heterosyklisiä yhdisteitä immunomodulaattoreina
BR112020022936A2 (pt) 2018-05-11 2021-02-02 Incyte Corporation derivados de tetra-hidro-imidazo[4,5-c]piridina como imunomoduladores de pd-l1
WO2020247736A1 (en) * 2019-06-07 2020-12-10 University Of Massachusetts Hepatitis c virus ns3/4a protease inhibitors
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
MX2022003578A (es) 2019-09-30 2022-05-30 Incyte Corp Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores.
BR112022009031A2 (pt) 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
MX2023005362A (es) 2020-11-06 2023-06-22 Incyte Corp Proceso para hacer un inhibidor de proteina de muerte programada 1 (pd-1)/ligando de muerte programada 1 (pd-l1) y sales y formas cristalinas del mismo.
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001040262A1 (en) * 1999-12-03 2001-06-07 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
WO2001074768A2 (en) * 2000-04-03 2001-10-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
WO2002008256A2 (en) * 2000-07-21 2002-01-31 Schering Corporation Peptides as ns3-serine protease inhibitors of hepatitis c virus
WO2002008244A2 (en) * 2000-07-21 2002-01-31 Schering Corporation Peptides as ns3-serine protease inhibitors of hepatitis c virus
WO2002018369A2 (en) * 2000-08-31 2002-03-07 Eli Lilly And Company Peptidomimetic protease inhibitors

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5807876A (en) 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
EP0907659A1 (en) 1996-05-10 1999-04-14 Schering Corporation Synthetic inhibitors of hepatitis c virus ns3 protease
HU227742B1 (en) 1996-10-18 2012-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
GB9707659D0 (en) 1997-04-16 1997-06-04 Peptide Therapeutics Ltd Hepatitis C NS3 Protease inhibitors
JP4354632B2 (ja) 1997-08-11 2009-10-28 ベーリンガー インゲルハイム （カナダ） リミテッド Ｃ型肝炎抑制剤ペプチド
NZ503263A (en) 1997-08-11 2002-10-25 Boehringer Ingelheim Ca Ltd Hepatitis C NS3 protease inhibitor peptides and peptide analogues
AU1416099A (en) * 1997-11-28 1999-06-16 Schering Corporation Single-chain recombinant complexes of hepatitis c virus ns3 protease and ns4a cofactor peptide
US6075150A (en) * 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
IT1299134B1 (it) 1998-02-02 2000-02-29 Angeletti P Ist Richerche Bio Procedimento per la produzione di peptidi con proprieta' inibitrici della proteasi ns3 del virus hcv, peptidi cosi' ottenibili e peptidi
ES2281170T3 (es) 1998-03-31 2007-09-16 Vertex Pharmaceuticals Incorporated Inhibidores de serina proteasas, particularmente proteasa ns3 del virus de la hepatitis c.
GB9812523D0 (en) 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
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.
US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
DE19836514A1 (de) 1998-08-12 2000-02-17 Univ Stuttgart Modifikation von Engineeringpolymeren mit N-basischen Gruppe und mit Ionenaustauschergruppen in der Seitenkette
GB9825946D0 (en) 1998-11-26 1999-01-20 Angeletti P Ist Richerche Bio Pharmaceutical compounds for the inhibition of hepatitis C virus NS3 protease
UA74546C2 (en) 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
EP1206449A1 (en) 1999-07-26 2002-05-22 Bristol-Myers Squibb Company Lactam inhibitors of hepatitis c virus ns3 protease
US7122627B2 (en) 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
WO2001016300A2 (en) * 1999-08-31 2001-03-08 Basf Aktiengesellschaft Method of identifying inhibitors of cdc25
US6699855B2 (en) 2000-02-29 2004-03-02 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
DE60137207D1 (de) 2000-04-05 2009-02-12 Schering Corp Makrozyklische inhibitoren der ns3-serinprotease des hepatitis c-virus mit stickstoffhaltigen zyklischen p2-gruppen
SK14952002A3 (sk) 2000-04-19 2003-03-04 Schering Corporation Makrocyklické zlúčeniny, farmaceutický prostriedok s ich obsahom a ich použitie
EP1301527A2 (en) 2000-07-21 2003-04-16 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
AR034127A1 (es) 2000-07-21 2004-02-04 Schering Corp Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento
NZ523781A (en) 2000-07-21 2004-10-29 Corvas Int Inc Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
AU2001282132A1 (en) * 2000-09-12 2002-03-26 Degussa A.G. Isolation and sequencing of the pknb gene of c. glutamicum
US6846806B2 (en) 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
AU2002248147B2 (en) 2000-11-20 2006-04-06 Bristol-Myers Squibb Company Hepatitis C tripeptide inhibitors
AU2002230763A1 (en) 2000-12-13 2008-01-03 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
WO2002048157A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
KR100926244B1 (ko) * 2001-07-11 2009-11-12 버텍스 파마슈티칼스 인코포레이티드 브릿지된 바이사이클릭 세린 프로테아제 억제제
EP1441720B8 (en) * 2001-10-24 2012-03-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4a protease, incorporating a fused ring system
MXPA04009938A (es) * 2002-04-11 2004-12-13 Vertex Pharma Inhibidores de serina proteasas, en particular la proteasa ns3-ns4a del hcv.
EP1613620A1 (en) * 2003-04-11 2006-01-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
CA2521678A1 (en) * 2003-04-11 2004-10-28 Vertex Pharmaceuticals, Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
CN102020700A (zh) * 2003-07-18 2011-04-20 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
CN1938332B (zh) * 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001040262A1 (en) * 1999-12-03 2001-06-07 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
WO2001074768A2 (en) * 2000-04-03 2001-10-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
WO2002008256A2 (en) * 2000-07-21 2002-01-31 Schering Corporation Peptides as ns3-serine protease inhibitors of hepatitis c virus
WO2002008244A2 (en) * 2000-07-21 2002-01-31 Schering Corporation Peptides as ns3-serine protease inhibitors of hepatitis c virus
WO2002018369A2 (en) * 2000-08-31 2002-03-07 Eli Lilly And Company Peptidomimetic protease inhibitors

Also Published As

Publication number Publication date
JP2009185081A (ja) 2009-08-20
MXPA04009938A (es) 2004-12-13
WO2003087092A3 (en) 2004-09-10
JP2010241821A (ja) 2010-10-28
CA2481369A1 (en) 2003-10-23
US20100173851A1 (en) 2010-07-08
KR20040099425A (ko) 2004-11-26
US20070292933A1 (en) 2007-12-20
EP2468744A2 (en) 2012-06-27
PL373399A1 (en) 2005-08-22
CN1649864A (zh) 2005-08-03
RU2004133044A (ru) 2006-01-27
TW200403236A (en) 2004-03-01
KR20110028665A (ko) 2011-03-21
WO2003087092A2 (en) 2003-10-23
AU2003223602A1 (en) 2003-10-27
CA2481369C (en) 2012-07-10
NO20044889L (no) 2005-01-10
NZ561851A (en) 2009-05-31
AU2003223602B2 (en) 2010-05-13
EP1497282A2 (en) 2005-01-19
ZA200408243B (en) 2006-07-26
AU2009233604A1 (en) 2009-11-26
IL164455A0 (en) 2005-12-18
US7273885B2 (en) 2007-09-25
NO20110773L (no) 2005-01-10
JP2005535574A (ja) 2005-11-24
NZ575692A (en) 2009-10-30
HK1081196A1 (zh) 2006-05-12
CN101245097A (zh) 2008-08-20
SG159385A1 (en) 2010-03-30
US20040018986A1 (en) 2004-01-29
CN100381440C (zh) 2008-04-16

Similar Documents

Publication Publication Date Title
AU2003223602B2 (en) Inhibitors of serine proteases, particularly hepatitis C virus NS3-NS4 protease
RU2412198C2 (ru) Ингибиторы сериновых протеаз, в частности нс3-нс4а протеазы
AU2004230946A1 (en) Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
WO2005007681A9 (en) Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP1613620A1 (en) Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AU2011203054B2 (en) Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease
HK1081196B (en) Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AU2011250779A1 (en) Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease

Legal Events

Date Code Title Description
TH Corrigenda

Free format text: IN VOL 24, NO 19, PAGE(S) 2169 UNDER THE HEADING APPLICATIONS ACCEPTED - NAME INDEX UNDER THE NAME VERTEX PHARMACEUTICALS INCORPORATED, APPLICATION NO. 2003223602, UNDER INID (72) CORRECT THE COINVENTOR TO READ PERNI, ROBERT B.

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired