KR20110028665A - 세린 프로테아제, 특히 c형 간염 바이러스 ns3-ns4 프로테아제의 억제제 - Google Patents

세린 프로테아제, 특히 c형 간염 바이러스 ns3-ns4 프로테아제의 억제제 Download PDF

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KR20110028665A
KR20110028665A KR1020117004808A KR20117004808A KR20110028665A KR 20110028665 A KR20110028665 A KR 20110028665A KR 1020117004808 A KR1020117004808 A KR 1020117004808A KR 20117004808 A KR20117004808 A KR 20117004808A KR 20110028665 A KR20110028665 A KR 20110028665A
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aliphatic
compound
ring
aryl
cycloalkyl
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KR1020117004808A
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Korean (ko)
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자노스 핏릭
케빈 엠 커트렐
룩 제이 파머
로버트 비 퍼니
로렌스 에프 커트니
드리 존 에이치 반
마크 에이 머코
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버텍스 파마슈티칼스 인코포레이티드
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Publication of KR20110028665A publication Critical patent/KR20110028665A/ko

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    • C07D471/02Heterocyclic 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
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  • Indole Compounds (AREA)
KR1020117004808A 2002-04-11 2003-04-11 세린 프로테아제, 특히 c형 간염 바이러스 ns3-ns4 프로테아제의 억제제 KR20110028665A (ko)

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US37184602P 2002-04-11 2002-04-11
US60/371,846 2002-04-11

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KR10-2004-7016168A Division KR20040099425A (ko) 2002-04-11 2003-04-11 세린 프로테아제, 특히 c형 간염 바이러스 ns3-ns4프로테아제의 억제제

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KR10-2004-7016168A KR20040099425A (ko) 2002-04-11 2003-04-11 세린 프로테아제, 특히 c형 간염 바이러스 ns3-ns4프로테아제의 억제제
KR1020117004808A KR20110028665A (ko) 2002-04-11 2003-04-11 세린 프로테아제, 특히 c형 간염 바이러스 ns3-ns4 프로테아제의 억제제

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EP (2) EP2468744A2 (US08039623-20111018-C00020.png)
JP (3) JP2005535574A (US08039623-20111018-C00020.png)
KR (2) KR20040099425A (US08039623-20111018-C00020.png)
CN (2) CN100381440C (US08039623-20111018-C00020.png)
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Families Citing this family (120)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL129407A0 (en) 1996-10-18 2000-02-17 Vertex Pharma Inhibitors of serine proteases particularly hepatitis C virus NS3 protease pharmaceutical compositions containing the same and the use thereof
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
AU2002348414B2 (en) * 2001-10-24 2009-10-01 Vertex Pharmaceuticals Incorporated 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
ES2381548T3 (es) * 2003-04-11 2012-05-29 Vertex Pharmaceuticals Incorporated Inhibidores de serina proteasas, particularmente de la proteasa VHC NS3-NS4A
AU2011203054B2 (en) * 2003-04-11 2012-04-26 Vertex Pharmaceuticals, Incorporated Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease
WO2004092161A1 (en) * 2003-04-11 2004-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
UY28423A1 (es) * 2003-07-18 2005-02-28 Vertex Pharma Inhibidores de proteasas serinas, en especial proteasa ns3-ns4a del vhc.-
MY148123A (en) * 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
JP4685775B2 (ja) * 2003-09-18 2011-05-18 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、とりわけhcvns3−ns4aプロテアーゼの阻害剤
RU2006115558A (ru) * 2003-10-10 2007-11-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы сериновых протеаз, особенно hcv ns3-ns4a протеазы
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
KR20060122872A (ko) 2003-10-28 2006-11-30 버텍스 파마슈티칼스 인코포레이티드 피셔-핑크형 합성 및 후속 아실화에 의한4,5-디알킬-3-아실-피롤-2-카복실산 유도체의 제조
ATE461209T1 (de) 2004-01-30 2010-04-15 Medivir Ab Hcv ns-3 serine protease inhibitoren
EP2311851A3 (en) * 2004-02-04 2011-05-25 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
EP2374464A3 (en) * 2004-10-01 2011-10-26 Vertex Pharmaceuticals Incorporated HCV N3S-NS4A protease inhibition
AU2005319333A1 (en) 2004-12-20 2006-06-29 Codman & Shurtleff, Inc. A method and system for treating Hepatitis C
EP1890602B1 (en) * 2005-04-20 2011-10-12 Philips Intellectual Property & Standards GmbH Patient monitoring system
EP2546246A3 (en) 2005-05-13 2013-04-24 Virochem Pharma Inc. Compounds and methods for the treatment or prevention of flavivirus infections
BRPI0613962A2 (pt) 2005-07-25 2009-03-24 Intermune Inc inibidores macrocìclicos inovadores de replicação de vìrus da hepatite c
PE20070343A1 (es) 2005-07-29 2007-05-12 Medivir Ab Inhibidores macrociclicos del virus de la hepatitis c
AR055105A1 (es) 2005-07-29 2007-08-08 Tibotec Pharm Ltd Inhibidores macrociclicos del virus de la hepatitis c
US7666834B2 (en) 2005-07-29 2010-02-23 Tibotec Pharmaceuticals Ltd. Macrocyclic inhibitors of hepatitis C virus
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
AU2006274862B2 (en) 2005-07-29 2012-03-22 Medivir Ab Macrocyclic inhibitors of hepatitis C virus
JO2768B1 (en) 2005-07-29 2014-03-15 تيبوتيك فارماسيوتيكالز ليمتد Large cyclic inhibitors of hepatitis C virus
WO2007014925A1 (en) 2005-07-29 2007-02-08 Tibotec Pharmaceuticals Ltd. Macrocylic inhibitors of hepatitis c virus
AR057704A1 (es) 2005-07-29 2007-12-12 Tibotec Pharm Ltd Inhibidores macrociclicos del virus de la hepatitis c, composicion farmaceutica y proceso de preparacion del compuesto
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
AR054882A1 (es) * 2005-07-29 2007-07-25 Tibotec Pharm Ltd Inhibidores macrociclicos del virus de la hepatitis c
US20070105781A1 (en) * 2005-08-02 2007-05-10 Steve Lyons Inhibitors of serine proteases
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
GEP20104956B (en) * 2005-10-11 2010-04-12 Array Biopharma Inc Compounds for inhibiting hepatitis c viral replication and use thereof
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
EP2392589A3 (en) 2005-11-11 2012-06-20 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
AU2007217355B2 (en) 2006-02-27 2012-06-21 Vertex Pharmaceuticals Incorporated Co-crystals comprising VX-950 and pharmaceutical compositions comprising the same
CA2646229A1 (en) * 2006-03-16 2007-09-27 Vertex Pharmaceuticals Incorporated Deuterated hepatitis c protease inhibitors
CA2643680A1 (en) 2006-04-11 2007-11-22 Novartis Ag Hcv/hiv inhibitors and their uses
WO2007120595A2 (en) * 2006-04-11 2007-10-25 Novartis Ag Amines for the treatment of hcv
CA2653662C (en) * 2006-06-01 2015-02-10 Sanofi-Aventis Spirocyclic nitriles as protease inhibitors
KR20090024834A (ko) * 2006-07-05 2009-03-09 인터뮨, 인크. C형 간염 바이러스 복제의 신규 억제제
CA2670260A1 (en) 2006-11-15 2008-05-22 Virochem Pharma Inc. Thiophene analogues for the treatment or prevention of flavivirus infections
KR20090079881A (ko) 2006-11-17 2009-07-22 티보텍 파마슈티칼즈 리미티드 C형 간염 바이러스의 마크로사이클릭 억제제
TW200846343A (en) * 2007-02-27 2008-12-01 Vertex Pharma Co-crystals and pharmaceutical compositions comprising the same
WO2008106058A2 (en) * 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
NZ581606A (en) * 2007-05-03 2012-06-29 Intermune Inc Novel macrocyclic inhibitors of hepatitis c virus replication
AU2008251425A1 (en) * 2007-05-10 2008-11-20 Array Biopharma, Inc. Novel peptide inhibitors of hepatitis C virus replication
ATE530546T1 (de) * 2007-08-30 2011-11-15 Vertex Pharma Kokristalle und pharmazeutische zusammensetzungen damit
CN101951770B (zh) 2007-12-21 2014-12-31 阿维拉制药公司 Hcv蛋白酶抑制剂和其用途
TW201546079A (zh) 2007-12-21 2015-12-16 Celgene Avilomics Res Inc Hcv蛋白酶抑制劑及其用途(一)
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
AP2010005416A0 (en) * 2008-04-15 2010-10-31 Intermune Inc Novel macrocyclic inhibitors of hepatitis c virus replication.
US8188137B2 (en) 2008-08-15 2012-05-29 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
CN102216321A (zh) * 2008-10-15 2011-10-12 因特蒙公司 治疗性抗病毒肽
AR074758A1 (es) 2008-12-22 2011-02-09 Gilead Sciences Inc Compuestos macrociclicos antivirales
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
DK2477980T3 (en) 2009-09-15 2016-09-12 Taigen Biotechnology Co Ltd HCV protease inhibitors
CN102741270B (zh) * 2009-09-28 2015-07-22 英特穆恩公司 C型肝炎病毒复制的环肽抑制剂
WO2011068715A1 (en) 2009-11-25 2011-06-09 Vertex Pharmaceuticals Incorporated 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections
AU2010324871A1 (en) 2009-11-25 2012-06-14 Merck Sharp & Dohme Corp. Fused tricyclic compounds and derivatives thereof useful for the treatment of viral diseases
AU2010341537A1 (en) 2009-12-22 2012-08-09 Merck Sharp & Dohme Corp. Fused Tricyclic Compounds and methods of use thereof for the treatment of viral diseases
KR20120130173A (ko) 2009-12-24 2012-11-29 버텍스 파마슈티칼스 인코포레이티드 플라비바이러스 감염을 치료 또는 예방하기 위한 유사체들
SG183526A1 (en) 2010-03-09 2012-09-27 Merck Sharp & Dohme Fused tricyclic silyl compounds and methods of use thereof for the treatment of viral diseases
WO2011119860A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
CA2794145A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
AU2011232348A1 (en) 2010-03-24 2012-10-11 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
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
EP2585448A1 (en) 2010-06-28 2013-05-01 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
WO2012006070A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
UY33473A (es) 2010-06-28 2012-01-31 Vertex Pharma Compuestos y métodos para el tratamiento o la prevencion de infecciones por flavivirus
JP2013541499A (ja) 2010-07-26 2013-11-14 メルク・シャープ・エンド・ドーム・コーポレイション 置換されたビフェニレン化合物およびウイルス性疾患の治療のためのその使用方法
WO2012024363A2 (en) 2010-08-17 2012-02-23 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flaviviridae viral infections
AU2011314168A1 (en) 2010-09-29 2013-04-04 Merck Sharp & Dohme Corp. Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases
BR112013026345A2 (pt) 2011-04-13 2019-04-24 Merck Sharp & Dohe Corp. composto, composição farmacêutica, uso de um composto, e, método para tratar um paciente infectado com hcv
US9156872B2 (en) 2011-04-13 2015-10-13 Merck Sharp & Dohme Corp. 2′-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
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
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
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
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
EP2755981A4 (en) 2011-09-14 2015-03-25 Merck Sharp & Dohme HETEROCYCLIC COMPOUNDS CONTAINING SILYL AND METHODS OF USING THE SAME FOR TREATING 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
WO2013142157A1 (en) 2012-03-22 2013-09-26 Alios Biopharma, Inc. Pharmaceutical combinations comprising 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
TW201526899A (zh) 2013-02-28 2015-07-16 Alios Biopharma Inc 醫藥組成物
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
US20170107216A1 (en) 2015-10-19 2017-04-20 Incyte Corporation Heterocyclic compounds as immunomodulators
AU2016358100B2 (en) 2015-11-19 2021-05-27 Incyte Corporation Heterocyclic compounds as immunomodulators
DK3394033T3 (da) 2015-12-22 2021-01-04 Incyte Corp Heterocykliske forbindelser som immunmodulatorer
MA44860A (fr) 2016-05-06 2019-03-13 Incyte Holdings Corp Composés hétérocycliques utilisés comme immunomodulateurs
US20170342060A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
BR112018076534A2 (pt) 2016-06-20 2019-04-02 Incyte Corporation compostos heterocíclicos como imunomoduladores
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
DK3472149T3 (da) 2016-06-21 2023-11-27 Orion Ophthalmology LLC Heterocykliske prolinamidderivater
ES2930092T3 (es) 2016-07-14 2022-12-07 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3504198B1 (en) 2016-08-29 2023-01-25 Incyte Corporation Heterocyclic compounds as immunomodulators
MA47120A (fr) 2016-12-22 2021-04-28 Incyte Corp Dérivés pyridine utilisés en tant qu'immunomodulateurs
EP3558985B1 (en) 2016-12-22 2022-09-07 Incyte Corporation Benzooxazole derivatives as immunomodulators
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
RU2650610C1 (ru) 2017-02-28 2018-04-16 Васильевич Иващенко Александр Противовирусная композиция и способ ее применения
CR20200520A (es) 2018-03-30 2021-03-09 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3790877B1 (en) 2018-05-11 2023-03-01 Incyte Corporation Tetrahydro-imidazo[4,5-c]pyridine derivatives as pd-l1 immunomodulators
US20220227806A1 (en) * 2019-06-07 2022-07-21 University Of Massachusetts Hepatitis c virus ns3/4a protease inhibitors
TW202115059A (zh) 2019-08-09 2021-04-16 美商英塞特公司 Pd—1/pd—l1抑制劑之鹽
TW202126652A (zh) 2019-09-30 2021-07-16 美商英塞特公司 作為免疫調節劑之吡啶并[3,2—d]嘧啶化合物
AU2020385113A1 (en) 2019-11-11 2022-05-19 Incyte Corporation Salts and crystalline forms of a PD-1/PD-L1 inhibitor
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
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
CA3200844A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof

Family Cites Families (45)

* 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
EP0907659A1 (en) 1996-05-10 1999-04-14 Schering Corporation Synthetic inhibitors of hepatitis c virus ns3 protease
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
IL129407A0 (en) * 1996-10-18 2000-02-17 Vertex Pharma Inhibitors of serine proteases particularly hepatitis C virus NS3 protease pharmaceutical compositions containing the same and the use thereof
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
NZ503263A (en) 1997-08-11 2002-10-25 Boehringer Ingelheim Ca Ltd Hepatitis C NS3 protease inhibitor peptides and peptide analogues
ES2241157T3 (es) 1997-08-11 2005-10-16 Boehringer Ingelheim (Canada) Ltd. Peptidos inhibidores de la hepatitis c.
WO1999028482A2 (en) * 1997-11-28 1999-06-10 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
AU3376699A (en) 1998-03-31 1999-10-18 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
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.
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
US7122627B2 (en) 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
CA2376961A1 (en) 1999-07-26 2001-02-01 Bristol-Myers Squibb Pharma Company Lactam inhibitors of hepatitis c virus ns3 protease
CA2383603A1 (en) * 1999-08-31 2001-03-08 Neil R. Taylor Method of identifying inhibitors of cdc25
AU2055301A (en) * 1999-12-03 2001-06-12 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
JP2003525294A (ja) 2000-02-29 2003-08-26 ブリストル−マイヤーズ スクイブ ファーマ カンパニー C型肝炎ウイルスns3プロテアーゼの阻害剤
DE60111509T2 (de) * 2000-04-03 2006-05-11 Vertex Pharmaceuticals Inc., Cambridge Inhibitoren von Serin-Proteasen, insbesondere der Hepatitis-C-Virus NS23-Protease
PL359359A1 (en) 2000-04-05 2004-08-23 Schering Corporation Macrocyclic ns3-serine protease inhibitors of hepatitis c virus comprising n-cyclic p2 moieties
CZ20023473A3 (cs) 2000-04-19 2003-01-15 Schering Corporation Makrocyklická sloučenina a farmaceutický prostředek
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
BR0112666A (pt) 2000-07-21 2003-06-10 Schering Corp Peptìdeos como inibidores de ns3-serina protease de vìrus da hepatite c
EP1301527A2 (en) 2000-07-21 2003-04-16 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
RU2355700C9 (ru) * 2000-07-21 2010-03-20 Шеринг Корпорейшн Новые пептиды как ингибиторы ns3-серинпротеазы вируса гепатита с
AR029851A1 (es) * 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
WO2002022828A1 (en) * 2000-09-12 2002-03-21 Degussa Ag 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
WO2002060926A2 (en) 2000-11-20 2002-08-08 Bristol-Myers Squibb Company Hepatitis c tripeptide inhibitors
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
WO2002048116A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
US6909000B2 (en) * 2001-07-11 2005-06-21 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
AU2002348414B2 (en) * 2001-10-24 2009-10-01 Vertex Pharmaceuticals Incorporated 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
ES2381548T3 (es) * 2003-04-11 2012-05-29 Vertex Pharmaceuticals Incorporated Inhibidores de serina proteasas, particularmente de la proteasa VHC NS3-NS4A
WO2004092161A1 (en) * 2003-04-11 2004-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
UY28423A1 (es) * 2003-07-18 2005-02-28 Vertex Pharma Inhibidores de proteasas serinas, en especial proteasa ns3-ns4a del vhc.-
EP2311851A3 (en) * 2004-02-04 2011-05-25 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease

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