ECSP10010413A - Inhibidores macrociclicos de serina proteasa - Google Patents

Inhibidores macrociclicos de serina proteasa

Info

Publication number
ECSP10010413A
ECSP10010413A EC2010010413A ECSP10010413A ECSP10010413A EC SP10010413 A ECSP10010413 A EC SP10010413A EC 2010010413 A EC2010010413 A EC 2010010413A EC SP10010413 A ECSP10010413 A EC SP10010413A EC SP10010413 A ECSP10010413 A EC SP10010413A
Authority
EC
Ecuador
Prior art keywords
macrociclic
inhibitors
proteasa
serina
serina proteasa
Prior art date
Application number
EC2010010413A
Other languages
English (en)
Inventor
Christophe Claude Parsy
Francois-Rene Alexandre
Dominique Surleraux
Michel Derock
Frederic Leroy
Adel Moussa
Bejamin Alexander Mayes
Elodie Rosinovsky
Arumugasamy Jeevanandam
Original Assignee
Idenix 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 Idenix Pharmaceuticals Inc filed Critical Idenix Pharmaceuticals Inc
Publication of ECSP10010413A publication Critical patent/ECSP10010413A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Aqui se proporcionan compuestos macrociclicos inhibidores de resina proteasa, por ejemplo, de la Formula (I), composiciones farmaceuticas que comprenden los compuestos, y proceso para la preparacion de los mismos.Tambien se proporcionan los metodos para su uso, para el tratamiento de una infeccion por HCV en un hospedero en necesidad del mismo.
EC2010010413A 2008-02-04 2010-08-20 Inhibidores macrociclicos de serina proteasa ECSP10010413A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US2608608P 2008-02-04 2008-02-04
US8386708P 2008-07-25 2008-07-25

Publications (1)

Publication Number Publication Date
ECSP10010413A true ECSP10010413A (es) 2010-11-30

Family

ID=40568607

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2010010413A ECSP10010413A (es) 2008-02-04 2010-08-20 Inhibidores macrociclicos de serina proteasa

Country Status (21)

Country Link
US (2) US8003659B2 (es)
EP (1) EP2250174B1 (es)
JP (1) JP5574982B2 (es)
KR (1) KR20100118991A (es)
CN (1) CN101977915B (es)
AR (1) AR070413A1 (es)
AU (1) AU2009210789B2 (es)
BR (1) BRPI0908021A2 (es)
CA (1) CA2712971A1 (es)
CO (1) CO6501153A2 (es)
CR (1) CR11618A (es)
EC (1) ECSP10010413A (es)
ES (1) ES2437147T3 (es)
IL (1) IL207333A0 (es)
MX (1) MX2010008523A (es)
NI (1) NI201000136A (es)
NZ (1) NZ587133A (es)
RU (1) RU2490272C2 (es)
TW (1) TW200936131A (es)
WO (1) WO2009099596A2 (es)
ZA (1) ZA201005318B (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY140680A (en) * 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
KR20090024834A (ko) * 2006-07-05 2009-03-09 인터뮨, 인크. Ｃ형 간염 바이러스 복제의 신규 억제제
WO2008141227A1 (en) 2007-05-10 2008-11-20 Intermune, Inc. Novel peptide inhibitors of hepatitis c virus replication
EA201071034A1 (ru) 2008-04-15 2011-06-30 Интермьюн, Инк. Новые макроциклические ингибиторы репликаций вируса гепатита с
UY32099A (es) 2008-09-11 2010-04-30 Enanta Pharm Inc Inhibidores macrocíclicos de serina proteasas de hepatitis c
CA2737376A1 (en) 2008-09-17 2010-03-25 Boehringer Ingelheim International Gmbh Combination of hcv ns3 protease inhibitor with interferon and ribavirin
WO2010090976A1 (en) * 2009-02-03 2010-08-12 Idenix Pharmaceuticals, Inc. Phosphinate ruthenium complexes
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.
JP2012520891A (ja) * 2009-03-19 2012-09-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング スルホニルキノリンの製造方法
WO2010118078A1 (en) 2009-04-08 2010-10-14 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
MY154683A (en) 2009-07-07 2015-07-15 Boehringer Ingelheim Int Pharmaceutical composition for a hepatitis c viral protease inhibitor
US20110034469A1 (en) 2009-08-04 2011-02-10 Takeda Pharmaceutical Company Limited Heterocyclic Compound
TW201117812A (en) * 2009-08-05 2011-06-01 Idenix Pharmaceuticals Inc Macrocyclic serine protease inhibitors
EA201200650A1 (ru) 2009-10-30 2012-12-28 Бёрингер Ингельхайм Интернациональ Гмбх Курсы комбинированного лечения вируса гепатита с, включающие bi201335, интерферон-альфа и рибавирин
MX2012006877A (es) 2009-12-18 2012-08-31 Idenix Pharmaceuticals Inc Inhibidores de virus de hepatitis c de arileno o heteroarileno 5, 5 - fusionado.
US20120014912A1 (en) * 2010-07-14 2012-01-19 Vertex Pharmaceuticals Incorporated Palatable pharmaceutical composition
CA2822556A1 (en) 2010-12-30 2012-07-05 Enanta Pharmaceuticals, Inc Macrocyclic hepatitis c serine protease inhibitors
EA201390988A1 (ru) 2010-12-30 2014-04-30 Энанта Фармасьютикалз, Инк. Фенантридиновые макроциклические ингибиторы сериновой протеазы вируса гепатита c
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
US20120252721A1 (en) 2011-03-31 2012-10-04 Idenix Pharmaceuticals, Inc. Methods for treating drug-resistant hepatitis c virus infection with a 5,5-fused arylene or heteroarylene hepatitis c virus inhibitor
US10201584B1 (en) 2011-05-17 2019-02-12 Abbvie Inc. Compositions and methods for treating HCV
WO2013106631A1 (en) 2012-01-11 2013-07-18 Abbvie Inc. Processes for making hcv protease inhibitors
UA119315C2 (uk) 2012-07-03 2019-06-10 Гіліад Фармассет Елелсі Інгібітори вірусу гепатиту с
US20140100364A1 (en) 2012-10-08 2014-04-10 Abbvie Inc. Compounds Useful For Making HCV Protease Inhibitors
WO2014145095A1 (en) 2013-03-15 2014-09-18 Gilead Sciences, Inc. Macrocyclic and bicyclic inhibitors of hepatitis c virus
WO2015042375A1 (en) 2013-09-20 2015-03-26 Idenix Pharmaceuticals, Inc. Hepatitis c virus inhibitors
WO2015103490A1 (en) 2014-01-03 2015-07-09 Abbvie, Inc. Solid antiviral dosage forms
US20170066779A1 (en) 2014-03-05 2017-03-09 Idenix Pharmaceuticals Llc Solid forms of a flaviviridae virus inhibitor compound and salts thereof
WO2015134561A1 (en) 2014-03-05 2015-09-11 Idenix Pharmaceuticals, Inc. Pharmaceutical compositions comprising a 5,5-fused heteroarylene flaviviridae inhibitor and their use for treating or preventing flaviviridae infection
EP3454856B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
ES2990061T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros espirocíclicos para la degradación de proteínas diana
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体

Family Cites Families (168)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69132332T2 (de) 1990-04-06 2000-11-30 Genelabs Technologies, Inc. Hepatitis c-virus-epitope
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
KR100509388B1 (ko) 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 ｃ 바이러스 ｎｓ３ 프로테아제의 저해제
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
US6004933A (en) 1997-04-25 1999-12-21 Cortech Inc. Cysteine protease inhibitors
ES2234144T3 (es) 1997-08-11 2005-06-16 Boehringer Ingelheim (Canada) Ltd. Analogos de peptidos inhibidores de la hepatitis c.
US6767991B1 (en) * 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
GB9806815D0 (en) 1998-03-30 1998-05-27 Hoffmann La Roche Amino acid derivatives
US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
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
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
AR029903A1 (es) 2000-04-05 2003-07-23 Schering Corp Inhibidores macrociclicos de la ns3-serina proteasa, del virus de la hepatitis c, que comprenden partes p2 n-ciclicas, composiciones farmaceuticas y utilizacion de los mismos para la manufactura de un medicamento
CN101580536A (zh) 2000-04-19 2009-11-18 先灵公司 含有烷基和芳基丙氨酸p2部分的丙型肝炎病毒的大环ns3-丝氨酸蛋白酶抑制剂
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
DK1385870T3 (da) 2000-07-21 2010-07-05 Schering Corp Peptider som inhibitorer af NS3-serinprotease fra hepatitis C-virus
CA2418199A1 (en) 2000-07-21 2002-01-31 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
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
KR20030081297A (ko) 2000-07-21 2003-10-17 쉐링 코포레이션 Ｃ형 간염 바이러스의 ｎｓ3-세린 프로테아제억제제로서의 신규한 펩티드
DE60119968T2 (de) 2000-11-20 2007-01-18 Bristol-Myers Squibb Co. Hepatitis c tripeptid inhibitoren
KR20030091946A (ko) 2000-12-12 2003-12-03 쉐링 코포레이션 Ｃ형 간염 바이러스의 ｎｓ3-세린 프로테아제억제제로서의 디아릴 펩티드
AU2002230763A1 (en) 2000-12-13 2008-01-03 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
AU2002230764A1 (en) 2000-12-13 2002-06-24 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
US6653295B2 (en) 2000-12-13 2003-11-25 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
JP2004520839A (ja) * 2001-03-08 2004-07-15 ベーリンガー インゲルハイム （カナダ） リミテッド Ｈｃｖのｒｎａ依存性ｒｎａポリメラーゼ（ｎｓ５ｂ）の阻害剤を同定するための分析法
CA2448737C (en) * 2001-07-20 2010-06-01 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US6867185B2 (en) * 2001-12-20 2005-03-15 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
US7119072B2 (en) 2002-01-30 2006-10-10 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis C virus
CA2370396A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
CA2370400A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
CA2369970A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US6828301B2 (en) 2002-02-07 2004-12-07 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for hepatitis C viral protease inhibitors
MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
US20060199773A1 (en) 2002-05-20 2006-09-07 Sausker Justin B Crystalline forms of (1R,2S)-N-[(1,1-dimethylethoxy)carbonyl]-3-methyl-L-valyl-(4R)-4-[(6-methoxy-1-isoquinolinyl)oxy]-L-prolyl-1-amino-N-(cyclopropylsulfonyl)-2-ethenyl-cyclopropanecarboxamide, monopotassium salt
JP4271148B2 (ja) 2002-05-20 2009-06-03 ブリストル−マイヤーズ スクイブ カンパニー 置換シクロアルキルｐ１’ｃ型肝炎ウイルスインヒビター
JP4312711B2 (ja) 2002-05-20 2009-08-12 ブリストル−マイヤーズ スクイブ カンパニー ヘテロ環式スルホンアミドｃ型肝炎ウイルス阻害剤
WO2004032827A2 (en) 2002-05-20 2004-04-22 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US20040033959A1 (en) * 2002-07-19 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Pharmaceutical compositions for hepatitis C viral protease inhibitors
AU2003264038A1 (en) * 2002-08-12 2004-02-25 Bristol-Myers Squibb Company Combination pharmaceutical agents as inhibitors of hcv replication
US20050075279A1 (en) * 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
US7601709B2 (en) 2003-02-07 2009-10-13 Enanta Pharmaceuticals, Inc. Macrocyclic hepatitis C serine protease inhibitors
US20040180815A1 (en) 2003-03-07 2004-09-16 Suanne Nakajima Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
CA2515216A1 (en) * 2003-02-07 2004-08-26 Enanta Pharmaceuticals, Inc. Macrocyclic hepatitis c serine protease inhibitors
US6908901B2 (en) 2003-03-05 2005-06-21 Boehringer Ingelheim International, Gmbh Hepatitis C inhibitor peptide analogs
CA2516016C (en) * 2003-03-05 2012-05-29 Boehringer Ingelheim International Gmbh Hepatitis c inhibiting compounds
UY28240A1 (es) 2003-03-27 2004-11-08 Boehringer Ingelheim Pharma Fases cristalinas de un potente inhibidor de la hcv
WO2004089974A1 (en) 2003-04-10 2004-10-21 Boehringer Ingelheim International Gmbh Process for the preparation of macrocyclic compounds by ruthenium complex catalysed metathesis reaction
US7148347B2 (en) * 2003-04-10 2006-12-12 Boehringer Ingelheim International Gmbh Process for preparing macrocyclic compounds
JP2006526011A (ja) 2003-04-11 2006-11-16 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
JP4733023B2 (ja) * 2003-04-16 2011-07-27 ブリストル−マイヤーズ スクイブ カンパニー Ｃ型肝炎ウイルスの大環状イソキノリンペプチド阻害剤
KR101031825B1 (ko) * 2003-04-18 2011-04-29 이난타 파마슈티칼스, 인코포레이티드 거대고리형 퀴녹살리닐 ｃ형 간염 세린 단백질분해효소억제제
US7176208B2 (en) 2003-04-18 2007-02-13 Enanta Pharmaceuticals, Inc. Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors
CL2004001161A1 (es) 2003-05-21 2005-04-08 Boehringer Ingelheim Int Compuestos describe compuestos derivados de quinolina; composicion farmaceutica; y su uso para tratar una enfermedad causada por el virus de la hepatitis c.
US7273851B2 (en) 2003-06-05 2007-09-25 Enanta Pharmaceuticals, Inc. Tri-peptide hepatitis C serine protease inhibitors
US7125845B2 (en) 2003-07-03 2006-10-24 Enanta Pharmaceuticals, Inc. Aza-peptide macrocyclic hepatitis C serine protease inhibitors
TWI359147B (en) * 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
ES2361997T3 (es) * 2003-09-22 2011-06-27 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos activos contra el virus de la hepatitis c.
WO2005037860A2 (en) 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incoporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2005037214A2 (en) 2003-10-14 2005-04-28 Intermune, Inc. Macrocyclic carboxylic acids and acylsulfonamides as inhibitors of hcv replication
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
DE10348044A1 (de) * 2003-10-15 2005-05-19 Imtm Gmbh Duale Alanyl-Aminopeptidase- und Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
US7132504B2 (en) * 2003-11-12 2006-11-07 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CA2539575C (en) * 2003-11-20 2015-01-20 Boehringer Ingelheim International Gmbh Method of removing transition metals, especially from metathesis reaction products
US7135462B2 (en) 2003-11-20 2006-11-14 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7309708B2 (en) * 2003-11-20 2007-12-18 Birstol-Myers Squibb Company Hepatitis C virus inhibitors
MXPA06005683A (es) 2003-11-20 2006-12-14 Schering Corp Inhibidores despeptidizados de la proteasa ns3 del virus de la hepatitis c.
US7109344B2 (en) * 2003-12-04 2006-09-19 Boehringer Ingelheim International Gmbh Ruthenium catalyst
EP1699558B1 (en) * 2003-12-08 2009-03-11 Boehringer Ingelheim International GmbH Removal of ruthenium by-product by supercritical fluid processing
RU2006125441A (ru) 2003-12-15 2008-01-27 Джапан Тобакко Инк. (Jp) Производные циклопропана и их фармацевтическое применение
DE10359791A1 (de) 2003-12-19 2005-07-21 Bayer Healthcare Ag Substituierte Thiophene
ATE495185T1 (de) 2004-01-21 2011-01-15 Boehringer Ingelheim Int Makrocyclische peptide mit wirkung gegen das hepatitis-c-virus
ATE416187T1 (de) 2004-01-28 2008-12-15 Boehringer Ingelheim Int Verfahren zum entfernen von übergangsmetallen aus übergangsmetallnebenprodukte enthaltenden reaktionslösungen
JP4902361B2 (ja) 2004-01-30 2012-03-21 メディヴィル・アクチエボラーグ Ｈｃｖｎｓ−３セリンプロテアーゼインヒビター
JP4874227B2 (ja) 2004-02-27 2012-02-15 シェーリング コーポレイション Ｃ型肝炎ウイルスのｎｓ３セリンプロテアーゼインヒビターとしての環状ｐ４’ｓを有する新規ケトアミド
CN1946691A (zh) 2004-02-27 2007-04-11 先灵公司 作为丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的化合物
RU2006136084A (ru) * 2004-03-15 2008-04-27 БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) Способ получения микроциклических соединений
CA2568008C (en) 2004-05-25 2014-01-28 Boehringer Ingelheim International Gmbh Process for preparing acyclic hcv protease inhibitors
CA2556669C (en) 2004-06-28 2012-05-01 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor peptide analogs
DE102004033312A1 (de) * 2004-07-08 2006-01-26 Boehringer Ingelheim Pharma Gmbh & Co. Kg Kontinuierliches Metatheseverfahren mit Ruthenium-Katalysatoren
RS51974B (sr) 2004-07-16 2012-02-29 Gilead Sciences Inc. Antivirusna jedinjenja
JP4914355B2 (ja) * 2004-07-20 2012-04-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃ型肝炎インヒビターペプチド類似体
UY29016A1 (es) * 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
ATE513844T1 (de) 2004-08-27 2011-07-15 Schering Corp Acylsulfonamidverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
WO2006033851A1 (en) * 2004-09-17 2006-03-30 Boehringer Ingelheim International, Gmbh Ring-closing metathesis process in supercritical fluid
WO2007001406A2 (en) 2004-10-05 2007-01-04 Chiron Corporation Aryl-containing macrocyclic compounds
MX2007004783A (es) 2004-10-21 2007-05-11 Pfizer Inhibidores de la proteasa del virus de la hepatitis c, y composiciones y tratamientos que los usan.
DE102005002336A1 (de) * 2005-01-17 2006-07-20 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Durchführung von kontinuierlichen Olefin-Ringschluss-Metathesen in komprimiertem Kohlendioxid
US7323447B2 (en) * 2005-02-08 2008-01-29 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
AU2006242475B2 (en) 2005-05-02 2011-07-07 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
US7592336B2 (en) * 2005-05-10 2009-09-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US20070021351A1 (en) 2005-06-02 2007-01-25 Schering Corporation Liver/plasma concentration ratio for dosing hepatitis C virus protease inhibitor
US20070237818A1 (en) 2005-06-02 2007-10-11 Malcolm Bruce A Controlled-release formulation of HCV protease inhibitor and methods using the same
US7601686B2 (en) * 2005-07-11 2009-10-13 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
TWI389908B (zh) 2005-07-14 2013-03-21 Gilead Sciences Inc 抗病毒化合物類
TW200738742A (en) 2005-07-14 2007-10-16 Gilead Sciences Inc Antiviral compounds
TWI387603B (zh) * 2005-07-20 2013-03-01 Merck Sharp & Dohme Ｈｃｖ ｎｓ３蛋白酶抑制劑
JP2009501732A (ja) 2005-07-20 2009-01-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃ型肝炎インヒビターペプチド類似体
MX2008001166A (es) 2005-07-25 2008-03-18 Intermune Inc Nuevos inhibidores macrociclicos de la replicacion del virus de hepatitis c.
JP5230416B2 (ja) 2005-07-29 2013-07-10 テイボテク・フアーマシユーチカルズ Ｃ型肝炎ウイルスの大員環状阻害剤
US7700552B2 (en) * 2005-07-29 2010-04-20 Medivir Ab Macrocyclic inhibitors of hepatitis C virus
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
ES2373685T3 (es) * 2005-07-29 2012-02-07 Tibotec Pharmaceuticals Inhibidores macrocíclicos del virus de la hepatitis c.
PE20070211A1 (es) * 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
KR20080033481A (ko) 2005-08-02 2008-04-16 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제의 억제제
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
EP1934243B1 (en) 2005-09-09 2011-05-25 Boehringer Ingelheim International GmbH Ring-closing metathesis process for the preparation of macrocyclic peptides
US7399758B2 (en) 2005-09-12 2008-07-15 Meanwell Nicholas A Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
US7473688B2 (en) 2005-09-13 2009-01-06 Bristol-Myers Squibb Company Indolobenzazepine HCV NS5B inhibitors
US7772183B2 (en) 2005-10-12 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7741281B2 (en) 2005-11-03 2010-06-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2007104919A1 (en) * 2006-03-15 2007-09-20 British Telecommunications Public Limited Company Video coding
AR060385A1 (es) 2006-04-11 2008-06-11 Novartis Ag Compuestos organicos y sus usos
US20080045530A1 (en) * 2006-04-11 2008-02-21 Trixi Brandl Organic Compounds and Their Uses
US8268776B2 (en) * 2006-06-06 2012-09-18 Enanta Pharmaceuticals, Inc. Macrocylic oximyl hepatitis C protease inhibitors
US20070281884A1 (en) 2006-06-06 2007-12-06 Ying Sun Macrocyclic oximyl hepatitis C protease inhibitors
US9526769B2 (en) 2006-06-06 2016-12-27 Enanta Pharmaceuticals, Inc. Macrocylic oximyl hepatitis C protease inhibitors
US20080187516A1 (en) 2006-06-06 2008-08-07 Ying Sun Acyclic oximyl hepatitis c protease inhibitors
US7728148B2 (en) * 2006-06-06 2010-06-01 Enanta Pharmaceuticals, Inc. Acyclic oximyl hepatitis C protease inhibitors
PE20080992A1 (es) * 2006-06-26 2008-08-06 Enanta Pharm Inc Quinoxalinil macrociclicos inhibidores de serina proteasa del virus de la hepatitis c
KR20090024834A (ko) * 2006-07-05 2009-03-09 인터뮨, 인크. Ｃ형 간염 바이러스 복제의 신규 억제제
EP2049474B1 (en) * 2006-07-11 2015-11-04 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
NZ574605A (en) * 2006-07-13 2011-11-25 Achillion Pharmaceuticals Inc 4-amino-4-oxobutanoyl peptides as inhibitors of viral replication
EP1881002A1 (en) 2006-07-20 2008-01-23 Tibotec Pharmaceuticals Ltd. HCV NS-3 serine protease inhibitors
DE112007002231A5 (de) * 2006-07-21 2009-06-25 Schaeffler Kg Verfahren zum Erkennen eines Laschentyps bei einer Kette
US20090035267A1 (en) * 2007-07-31 2009-02-05 Moore Joel D Acyclic, pyridazinone-derived hepatitis c serine protease inhibitors
CA2656816A1 (en) * 2006-08-04 2008-02-14 Enanta Pharmaceuticals, Inc. Tetrazolyl macrocyclic hepatitis c serine protease inhibitors
US7635683B2 (en) * 2006-08-04 2009-12-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl tripeptide hepatitis C virus inhibitors
US7718612B2 (en) * 2007-08-02 2010-05-18 Enanta Pharmaceuticals, Inc. Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
US20090035271A1 (en) * 2007-08-01 2009-02-05 Ying Sun Tetrazolyl macrocyclic hepatitis c serine protease inhibitors
US7687459B2 (en) * 2006-08-11 2010-03-30 Enanta Pharmaceuticals, Inc. Arylalkoxyl hepatitis C virus protease inhibitors
US20080038225A1 (en) * 2006-08-11 2008-02-14 Ying Sun Triazolyl acyclic hepatitis c serine protease inhibitors
US7662779B2 (en) * 2006-08-11 2010-02-16 Enanta Pharmaceuticals, Inc. Triazolyl macrocyclic hepatitis C serine protease inhibitors
US7582605B2 (en) * 2006-08-11 2009-09-01 Enanta Pharmaceuticals, Inc. Phosphorus-containing hepatitis C serine protease inhibitors
US20090035268A1 (en) * 2007-08-01 2009-02-05 Ying Sun Tetrazolyl acyclic hepatitis c serine protease inhibitors
US7605126B2 (en) * 2006-08-11 2009-10-20 Enanta Pharmaceuticals, Inc. Acylaminoheteroaryl hepatitis C virus protease inhibitors
US20080107625A1 (en) * 2006-11-01 2008-05-08 Bristol-Myers Squibb Company Inhibitors of Hepatitis C Virus
US20080107623A1 (en) * 2006-11-01 2008-05-08 Bristol-Myers Squibb Company Inhibitors of Hepatitis C Virus
US8343477B2 (en) * 2006-11-01 2013-01-01 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
WO2008057995A2 (en) * 2006-11-02 2008-05-15 Taigen Biotechnology Co., Ltd. Hcv protease inhibitors
US7772180B2 (en) * 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7763584B2 (en) * 2006-11-16 2010-07-27 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8003604B2 (en) * 2006-11-16 2011-08-23 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
JP5390510B2 (ja) 2007-04-24 2014-01-15 エフ．ホフマン−ラ ロシュ アーゲー Ｈｃｖプロテアーゼ阻害剤中間体の製造方法
WO2008134398A1 (en) 2007-04-26 2008-11-06 Enanta Pharmaceuticals, Inc. Oximyl dipeptide hepatitis c protease inhibitors
US20080267917A1 (en) 2007-04-26 2008-10-30 Deqiang Niu N-functionalized amides as hepatitis c serine protease inhibitors
US20080274082A1 (en) 2007-04-26 2008-11-06 Yonghua Gai Oximyl hydroxyamic analogs as hepatitis c virus protease inhibitor
US8377872B2 (en) 2007-04-26 2013-02-19 Enanta Pharmaceuticals, Inc. Cyclic P3 tripeptide hepatitis C serine protease inhibitors
US20080274080A1 (en) 2007-04-26 2008-11-06 Yat Sun Or Aza-peptide macrocyclic hepatitis c serine protease inhibitors
US20080286233A1 (en) 2007-04-26 2008-11-20 Ying Sun Piperizinyl macrocyclic hepatitis c serine protease inhibitors
US20080317712A1 (en) 2007-04-26 2008-12-25 Deqiang Niu Arylpiperidinyl and arylpyrrolidinyl tripeptide hepatitis c serine protease inhibitors
US7910587B2 (en) 2007-04-26 2011-03-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl dipeptide hepatitis C virus inhibitors
US20080279821A1 (en) 2007-04-26 2008-11-13 Deqiang Niu Arylpiperidinyl and arylpyrrolidinyl macrocyclic hepatitis c serine protease inhibitors
US7906513B2 (en) 2007-04-26 2011-03-15 Enanta Pharmaceuticals, Inc. Hydrazide-containing hepatitis C serine protease inhibitors
WO2008134397A1 (en) 2007-04-26 2008-11-06 Enanta Pharmaceuticals, Inc. Aza-tripeptide hepatitis c serine protease inhibitors
US20090005387A1 (en) * 2007-06-26 2009-01-01 Deqiang Niu Quinoxalinyl macrocyclic hepatitis c virus serine protease inhibitors
AR067180A1 (es) * 2007-06-29 2009-09-30 Gilead Sciences Inc Compuestos antivirales
EA019749B1 (ru) * 2007-06-29 2014-06-30 Джилид Сайэнс, Инк. Противовирусные соединения
WO2009005677A2 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Antiviral compounds
WO2009014730A1 (en) * 2007-07-26 2009-01-29 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
WO2009042668A2 (en) * 2007-09-24 2009-04-02 Achillion Pharmaceuticals, Inc. Urea-containing peptides as inhibitors of viral replication
US8383583B2 (en) * 2007-10-26 2013-02-26 Enanta Pharmaceuticals, Inc. Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors
US8426360B2 (en) * 2007-11-13 2013-04-23 Enanta Pharmaceuticals, Inc. Carbocyclic oxime hepatitis C virus serine protease inhibitors
WO2009070692A1 (en) * 2007-11-29 2009-06-04 Enanta Pharmaceuticals, Inc. C5-substituted, proline-derived, macrocyclic hepatitis c serine protease inhibitors
CN101932242A (zh) * 2007-12-05 2010-12-29 益安药业 喹喔啉基衍生物
US8193346B2 (en) * 2007-12-06 2012-06-05 Enanta Pharmaceuticals, Inc. Process for making macrocyclic oximyl hepatitis C protease inhibitors

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