[go: up one dir, main page]

PE20081792A1 - Inhibidores de serina proteasas - Google Patents

Inhibidores de serina proteasas

Info

Publication number
PE20081792A1
PE20081792A1 PE2008000396A PE2008000396A PE20081792A1 PE 20081792 A1 PE20081792 A1 PE 20081792A1 PE 2008000396 A PE2008000396 A PE 2008000396A PE 2008000396 A PE2008000396 A PE 2008000396A PE 20081792 A1 PE20081792 A1 PE 20081792A1
Authority
PE
Peru
Prior art keywords
protease inhibitors
serine protease
aryl
compounds
refers
Prior art date
Application number
PE2008000396A
Other languages
English (en)
Inventor
Kevin M Cottrell
John Maxwell
Qing Tang
Anne-Laure Grillot
Tiran Arnaud Le
Emanuele Perola
Original Assignee
Vertex Pharma
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39469472&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20081792(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of PE20081792A1 publication Critical patent/PE20081792A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/235Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
    • A61K31/24Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I, DONDE A Y B SON -CH2-; R1 ES -ZAR4; ZA ES -C(O)-; R4 ES ALQUILO; R2 ES -ZBR5; ZB ES UN ENLACE, CADENA ALIFATICA SUSTITUIDA; R5 ES NH2, -CN, HALO, ENTRE OTROS; R3 ES AMINO, -O-R3A, ARILO, HETEROCICLOALIFATICO, ENTRE OTROS; R3A ES ARILO, HETEROARILO; Y E Y' SON H. SON PREFERIDOS II, III, ENTRE OTROS. SE REFIERE TAMBIEN A PROCEDIMIENTOS DE PREPARACION Y COMPOSICIONES FARMACEUTICAS CONTENIENDO ADICIONALMENTE UN SEGUNDO COMPUESTO INMUNOMODULATORIO COMO TIMOSINA, ANTIVIRAL COMO RIBAVIRIN O INHIBIDOR P450 COMO RITONAVIR. DICHOS COMPUESTOS SON INHIBIDORES SERINA PROTEASA, PARTICULARMENTE NS3-NS4A DEL VIRUS DE HEPATITIS C
PE2008000396A 2007-02-27 2008-02-27 Inhibidores de serina proteasas PE20081792A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11/711,845 US7964624B1 (en) 2005-08-26 2007-02-27 Inhibitors of serine proteases

Publications (1)

Publication Number Publication Date
PE20081792A1 true PE20081792A1 (es) 2008-12-18

Family

ID=39469472

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000396A PE20081792A1 (es) 2007-02-27 2008-02-27 Inhibidores de serina proteasas

Country Status (22)

Country Link
US (2) US7964624B1 (es)
EP (2) EP2631238A1 (es)
JP (1) JP2010523474A (es)
KR (1) KR20090127292A (es)
CN (1) CN102015727A (es)
AP (1) AP2009004971A0 (es)
AR (1) AR065499A1 (es)
AU (1) AU2008219689A1 (es)
BR (1) BRPI0807904A2 (es)
CA (1) CA2679429A1 (es)
CL (1) CL2008000579A1 (es)
CO (1) CO6220931A2 (es)
EA (1) EA200970805A1 (es)
EC (1) ECSP099601A (es)
GE (1) GEP20125683B (es)
IL (1) IL200611A0 (es)
MX (1) MX2009009174A (es)
NZ (1) NZ579296A (es)
PE (1) PE20081792A1 (es)
TW (1) TW200843738A (es)
UY (1) UY30941A1 (es)
WO (1) WO2008106139A1 (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ335276A (en) 1996-10-18 2000-09-29 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis C virus (HCV) NS3 (Non Structural Protein 3) protease
PE20050374A1 (es) 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
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
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
KR20090024834A (ko) 2006-07-05 2009-03-09 인터뮨, 인크. C형 간염 바이러스 복제의 신규 억제제
TW201040181A (en) 2009-04-08 2010-11-16 Idenix Pharmaceuticals Inc Macrocyclic serine protease inhibitors
WO2011003063A2 (en) * 2009-07-02 2011-01-06 Dr. Reddy's Laboratories Ltd. Enzymes and methods for resolving amino vinyl cyclopropane carboxylic acid derivatives
US9284307B2 (en) 2009-08-05 2016-03-15 Idenix Pharmaceuticals Llc Macrocyclic serine protease inhibitors
TW201116540A (en) * 2009-10-01 2011-05-16 Intermune Inc Therapeutic antiviral peptides
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
AR085352A1 (es) 2011-02-10 2013-09-25 Idenix Pharmaceuticals Inc Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv
AR086113A1 (es) 2011-04-30 2013-11-20 Abbott Lab Isoxazolinas como agentes terapeuticos
JP5669984B2 (ja) 2011-05-18 2015-02-18 エナンタ ファーマシューティカルズ インコーポレイテッド 5−アザスピロ[2.4]ヘプタン−6−カルボン酸およびその誘導体の製造方法
BR112014029295B1 (pt) 2012-05-25 2021-04-27 Nutech Ventures Ciclobutenos e ciclobutanos anfifílicos e composição farmacêutica que os compreende
TW201408669A (zh) 2012-08-08 2014-03-01 Merck Sharp & Dohme Hcv ns3蛋白酶抑制劑
FR3000064A1 (fr) * 2012-12-21 2014-06-27 Univ Lille Ii Droit & Sante Composes de type spiroisoxazoline ayant une activite potentialisatrice de l'activite d'un antibiotique-composition et produit pharmaceutiques comprenant de tels composes
US9887974B2 (en) 2013-11-27 2018-02-06 Architecture Technology Corporation Method for network communication past encryption devices
US9191377B2 (en) * 2013-11-27 2015-11-17 Architecture Technology Corporation Method for network communication past encryption devices
US9160553B2 (en) 2013-11-27 2015-10-13 Architecture Technology Corporation Adaptive multicast network communications
CN105153005A (zh) * 2015-08-05 2015-12-16 上海瑞博化学有限公司 一种4-羰基-脯氨酸衍生物的制备方法
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
EP3472130B1 (en) 2016-06-21 2022-02-16 Orion Ophthalmology LLC Aliphatic prolinamide derivatives
CN105924353A (zh) * 2016-06-29 2016-09-07 山东未名生物医药股份有限公司 2-羟基酸酯的制备方法
US11292801B2 (en) 2016-07-05 2022-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
PE20191153A1 (es) 2016-09-28 2019-09-05 Blade Therapeutics Inc Moduladores de calpainas y usos terapeuticos de los mismos
CN112204014A (zh) * 2018-03-28 2021-01-08 布莱德治疗公司 钙蛋白酶调节剂及其治疗用途
JP7584418B2 (ja) 2018-12-04 2024-11-15 ブリストル-マイヤーズ スクイブ カンパニー 多重反応同位体分子種反応モニタリングによる、サンプル内検量線を用いた分析方法
CN113440609A (zh) * 2020-03-27 2021-09-28 北京市农林科学院 一种双链rna复合物autp及其在疫苗制备中的应用

Family Cites Families (153)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3226768A1 (de) 1981-11-05 1983-05-26 Hoechst Ag, 6230 Frankfurt Derivate der cis, endo-2-azabicyclo-(3.3.0)-octan-3-carbonsaeure, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung
DE3211676A1 (de) 1982-03-30 1983-10-06 Hoechst Ag Neue derivate von cycloalka (c) pyrrol-carbonsaeuren, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung sowie neue cycloalka (c) pyrrol-carbonsaeuren als zwischenstufen und verfahren zu deren herstellung
US4499082A (en) 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
FR2575753B1 (fr) 1985-01-07 1987-02-20 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5496927A (en) 1985-02-04 1996-03-05 Merrell Pharmaceuticals Inc. Peptidase inhibitors
DE3683541D1 (de) 1985-06-07 1992-03-05 Ici America Inc Selektionierte difluorverbindungen.
US5231084A (en) 1986-03-27 1993-07-27 Hoechst Aktiengesellschaft Compounds having a cognition adjuvant action, agents containing them, and the use thereof for the treatment and prophylaxis of cognitive dysfuncitons
US5736520A (en) 1988-10-07 1998-04-07 Merrell Pharmaceuticals Inc. Peptidase inhibitors
NZ235155A (en) 1989-09-11 1993-04-28 Merrell Dow Pharma Peptidase substrates in which the carboxy terminal group has been replaced by a tricarbonyl radical
US5371072A (en) 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
ES2150933T3 (es) 1992-12-22 2000-12-16 Lilly Co Eli Inhibidores de la proteasa vih utiles para el tratamiento del sida.
ATE143262T1 (de) 1992-12-29 1996-10-15 Abbott Lab Inhibitoren der retroviralen protease
US5384410A (en) 1993-03-24 1995-01-24 The Du Pont Merck Pharmaceutical Company Removal of boronic acid protecting groups by transesterification
US5656600A (en) 1993-03-25 1997-08-12 Corvas International, Inc. α-ketoamide derivatives as inhibitors of thrombosis
US5672582A (en) 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
IL110752A (en) 1993-09-13 2000-07-26 Abbott Lab Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor
US5559158A (en) 1993-10-01 1996-09-24 Abbott Laboratories Pharmaceutical composition
US5468858A (en) 1993-10-28 1995-11-21 The Board Of Regents Of Oklahoma State University Physical Sciences N-alkyl and n-acyl derivatives of 3,7-diazabicyclo-[3.3.1]nonanes and selected salts thereof as multi-class antiarrhythmic agents
IL111991A (en) 1994-01-28 2000-07-26 Abbott Lab Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent
HUT72440A (en) 1994-03-31 1996-04-29 Bristol Myers Squibb Co Imidazole-containing inhibitors of farnesyl protein transferase and pharmaceutical compositions containing them
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5861267A (en) 1995-05-01 1999-01-19 Vertex Pharmaceuticals Incorporated Methods, nucleotide sequences and host cells for assaying exogenous and endogenous protease activity
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US6060469A (en) 1995-11-23 2000-05-09 Merck Sharp & Dohme Ltd. Spiro-piperidine derivatives and their use as tachykinin antagonists
US5807876A (en) 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US6054472A (en) 1996-04-23 2000-04-25 Vertex Pharmaceuticals, Incorporated Inhibitors of IMPDH enzyme
ZA972195B (en) 1996-03-15 1998-09-14 Du Pont Merck Pharma Spirocycle integrin inhibitors
WO1997040028A1 (en) 1996-04-23 1997-10-30 Vertex Pharmaceuticals Incorporated Urea derivatives as inhibitors of impdh enzyme
WO1997043310A1 (en) 1996-05-10 1997-11-20 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
US6153579A (en) 1996-09-12 2000-11-28 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
JP2001501203A (ja) 1996-09-25 2001-01-30 メルク シヤープ エンド ドーム リミテツド スピロアザシクロ誘導体、該誘導体の製造およびタキキニン拮抗薬としての該誘導体の使用
WO1998015544A1 (en) 1996-10-08 1998-04-16 Colorado State University Research Foundation Catalytic asymmetric epoxidation
NZ335276A (en) 1996-10-18 2000-09-29 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis C virus (HCV) NS3 (Non Structural Protein 3) protease
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
DE19648011A1 (de) 1996-11-20 1998-05-28 Bayer Ag Cyclische Imine
CA2282398A1 (en) 1997-03-14 1998-09-17 Steven M. Ronkin Inhibitors of impdh enzyme
GB9708484D0 (en) 1997-04-25 1997-06-18 Merck Sharp & Dohme Therapeutic agents
GB9711114D0 (en) 1997-05-29 1997-07-23 Merck Sharp & Dohme Therapeutic agents
US6767991B1 (en) 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
AU757072B2 (en) 1997-08-11 2003-01-30 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptide analogues
US6183121B1 (en) 1997-08-14 2001-02-06 Vertex Pharmaceuticals Inc. Hepatitis C virus helicase crystals and coordinates that define helicase binding pockets
US20040058982A1 (en) 1999-02-17 2004-03-25 Bioavailability System, Llc Pharmaceutical compositions
US20020017295A1 (en) 2000-07-07 2002-02-14 Weers Jeffry G. Phospholipid-based powders for inhalation
US6211338B1 (en) 1997-11-28 2001-04-03 Schering Corporation Single-chain recombinant complexes of hepatitis C virus NS3 protease and NS4A cofactor peptide
DK1066247T3 (da) 1998-03-31 2007-04-02 Vertex Pharma Inhibitorer af serinproteaser, især hepatitis C virus NS3 protease
US6251583B1 (en) 1998-04-27 2001-06-26 Schering Corporation Peptide substrates for HCV NS3 protease assays
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
DE19836514A1 (de) 1998-08-12 2000-02-17 Univ Stuttgart Modifikation von Engineeringpolymeren mit N-basischen Gruppe und mit Ionenaustauschergruppen in der Seitenkette
US6117639A (en) 1998-08-31 2000-09-12 Vertex Pharmaceuticals Incorporated Fusion proteins, DNA molecules, vectors, and host cells useful for measuring protease activity
US6025516A (en) 1998-10-14 2000-02-15 Chiragene, Inc. Resolution of 2-hydroxy-3-amino-3-phenylpropionamide and its conversion to C-13 sidechain of taxanes
ATE400251T1 (de) 1999-02-09 2008-07-15 Pfizer Prod Inc Zusammensetzungen basischer arzneistoffe mit verbesserter bioverfügbarkeit
US20020042046A1 (en) 1999-02-25 2002-04-11 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
TR200103428T2 (tr) 1999-03-19 2002-04-22 Vertex Pharmaceuticals Incorporated IMPDH enzim inhibitörleri.
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
US7122627B2 (en) 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
US20020183249A1 (en) 1999-08-31 2002-12-05 Taylor Neil R. Method of identifying inhibitors of CDC25
GB9925955D0 (en) 1999-11-02 1999-12-29 Angeletti P Ist Richerche Bio Hcv n33 protease inhibitors
CA2390349A1 (en) 1999-12-03 2001-06-07 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
US6624290B2 (en) 2000-02-08 2003-09-23 Schering Corporation Azapeptides useful in the treatment of Hepatitis C
EP1261611A2 (en) 2000-02-29 2002-12-04 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
PT1268519E (pt) 2000-04-03 2005-08-31 Vertex Pharma Inibidores de serina protease, particularmente protease ns3 do virus da hepatite c
SK14192002A3 (sk) 2000-04-05 2003-03-04 Schering Corporation Makrocyklické zlúčeniny, farmaceutický prostriedok s ich obsahom a ich použitie
PL358591A1 (en) 2000-04-19 2004-08-09 Schering Corporation Macrocyclic ns3-serine protease inhibitors of hepatitis c virus comprising alkyl and aryl alanine p2 moieties
WO2002002546A1 (en) 2000-06-30 2002-01-10 Seikagaku Corporation EPOXYCARBOXYLIC ACID AMIDES, AZIDES AND AMINO ALCOHOLS AND PROCESSES FOR PREPARATION OF α-KETO AMIDES BY USING THEM
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
NZ523782A (en) 2000-07-21 2005-10-28 Dendreon Corp Peptides as NS3-serine protease inhibitors of hepatitis C virus
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
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
HUP0303358A3 (en) 2000-07-21 2005-10-28 Schering Corp Novel peptides as ns3-serine protease inhibitors of hepatitis c virus and pharmaceutical compositions containing them
US6777400B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
US6939692B2 (en) 2000-09-12 2005-09-06 Degussa Ag Nucleotide sequences coding for the pknB gene
US6846806B2 (en) 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
PE20020707A1 (es) 2000-11-20 2002-08-11 Bristol Myers Squibb Co Compuestos tripeptidicos como inhibidores de la proteasa ns3 del virus de hepatitis c
JP4368581B2 (ja) 2000-12-12 2009-11-18 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阻害剤としてのジアリールペプチド
US6727366B2 (en) 2000-12-13 2004-04-27 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
EP1539188B1 (en) 2001-01-22 2015-01-07 Merck Sharp & Dohme Corp. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
MXPA03006794A (es) 2001-01-30 2003-11-13 Vertex Pharma Un analisis cuantitativo para acidos nucleicos.
GB0102342D0 (en) 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
ATE431396T1 (de) 2001-03-27 2009-05-15 Vertex Pharma Für hcv-infektion geeignete zusammensetzungen und verfahren
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
WO2003003804A2 (en) 2001-07-03 2003-01-16 Altana Pharma Ag Process for the production of optically active 3-phenylisoserine
DE60217114T2 (de) 2001-07-11 2007-10-25 Vertex Pharmaceuticals Inc., Cambridge Verbrückte bizyklische serinproteaseinhibitoren
JP2003055389A (ja) 2001-08-09 2003-02-26 Univ Tokyo 錯体及びそれを用いたエポキシドの製法
US6824769B2 (en) 2001-08-28 2004-11-30 Vertex Pharmaceuticals Incorporated Optimal compositions and methods thereof for treating HCV infections
MXPA04003825A (es) 2001-10-24 2004-07-08 Vertex Pharma Inhibidores de serina proteasa, en particular la ns3-ns4a proteasa del virus de hepatitis c, que incorpora un sistema de anillo fusionado.
AU2002360386A1 (en) 2001-11-14 2003-06-17 Teva Pharmaceutical Industries Ltd. Amorphous and crystalline forms of losartan potassium and process for their preparation
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
AR038375A1 (es) 2002-02-01 2005-01-12 Pfizer Prod Inc Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo
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
CA2370396A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
SG159385A1 (en) 2002-04-11 2010-03-30 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 - ns4 protease
US8093380B2 (en) 2002-08-01 2012-01-10 Pharmasset, Inc. Compounds with the bicyclo[4.2.1]nonane system for the treatment of Flaviviridae infections
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
CA2413705A1 (en) 2002-12-06 2004-06-06 Raul Altman Use of meloxicam in combination with an antiplatelet agent for treatment of acute coronary syndrome and related conditions
US7601709B2 (en) 2003-02-07 2009-10-13 Enanta Pharmaceuticals, Inc. Macrocyclic hepatitis C serine protease inhibitors
US7223785B2 (en) 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US7098231B2 (en) 2003-01-22 2006-08-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
CA2515216A1 (en) 2003-02-07 2004-08-26 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
EP1596846A2 (en) 2003-02-18 2005-11-23 Pfizer Inc. Inhibitors of hepatitis c virus, compositions and treatments using the same
EP1599496B1 (en) 2003-03-05 2010-11-03 Boehringer Ingelheim International GmbH Hepatitis c inhibitor peptide analogs
WO2004101605A1 (en) 2003-03-05 2004-11-25 Boehringer Ingelheim International Gmbh Hepatitis c inhibiting compounds
TW200510391A (en) 2003-04-11 2005-03-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US20050090450A1 (en) 2003-04-11 2005-04-28 Farmer Luc J. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
PE20050204A1 (es) 2003-05-21 2005-05-04 Boehringer Ingelheim Int Compuestos inhibidores de la hepatitis c
US7109172B2 (en) 2003-07-18 2006-09-19 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
WO2005018330A1 (en) 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
PE20050374A1 (es) 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
NZ545871A (en) 2003-09-12 2010-04-30 Vertex Pharma Animal model for protease activity and liver damage
EP1664091A1 (en) 2003-09-18 2006-06-07 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US6933760B2 (en) 2003-09-19 2005-08-23 Intel Corporation Reference voltage generator for hysteresis circuit
MXPA06003141A (es) 2003-09-22 2006-06-05 Boehringer Ingelheim Int Peptidos macrociclicos activos contra el virus de la hepatitis c.
EP2361925A1 (en) 2003-10-10 2011-08-31 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
AR045870A1 (es) 2003-10-11 2005-11-16 Vertex Pharma Terapia de combinacion para la infeccion de virus de hepatitis c
KR20060120166A (ko) 2003-10-27 2006-11-24 버텍스 파마슈티칼스 인코포레이티드 Hcv ns3-ns4a 단백질분해효소 저항성 돌연변이
RU2006118359A (ru) 2003-10-27 2007-12-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Комбинации для лечения вирусного гепатита с (hcv)
WO2005043118A2 (en) 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1678134B1 (en) 2003-10-28 2009-09-09 Vertex Pharmaceuticals Incorporated Preparation of 4,5-dialkyl-3-acyl-pyrrole-2-carboxylic acid derivatives by fischer-fink type synthesis and subsequent acylation
US20050119318A1 (en) 2003-10-31 2005-06-02 Hudyma Thomas W. Inhibitors of HCV replication
US7132504B2 (en) 2003-11-12 2006-11-07 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2005054450A1 (en) 2003-12-01 2005-06-16 Vertex Pharmaceuticals Incorporated Compositions comprising fetal liver cells and methods useful for hcv infection
CA2549851C (en) 2004-01-21 2012-09-11 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis c virus
WO2005077969A2 (en) 2004-02-04 2005-08-25 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US20050187192A1 (en) 2004-02-20 2005-08-25 Kucera Pharmaceutical Company Phospholipids for the treatment of infection by togaviruses, herpes viruses and coronaviruses
EA201301284A1 (ru) 2004-02-20 2014-03-31 Бёрингер Ингельхайм Интернациональ Гмбх Способ получения соединений, являющихся ингибиторами вирусной полимеразы и способ получения фармацевтических композиций, а также промежуточные соединения
CA2557307A1 (en) 2004-02-27 2005-09-22 Schering Corporation 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis c virus ns3 serine protease
CA2768700C (en) 2004-03-12 2014-04-29 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
US20050249702A1 (en) 2004-05-06 2005-11-10 Schering Corporation (1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease
WO2005123076A2 (en) 2004-06-08 2005-12-29 Vertex Pharmaceuticals, Inc. Pharmaceutical compositions
EP1797111B1 (en) 2004-08-27 2011-06-22 Schering Corporation Acylsulfonamide compounds as inhibitors of hepatitis c virus ns3 serine protease
MX2007003812A (es) 2004-10-01 2007-05-24 Vertex Pharma Inhibicion de proteasa ns3-ns4a del virus de la hepatitis c (vhc).
MY141025A (en) 2004-10-29 2010-02-25 Vertex Pharma Dose forms
US7863274B2 (en) 2005-07-29 2011-01-04 Concert Pharmaceuticals Inc. Deuterium enriched analogues of tadalafil as PDE5 inhibitors
EP2402331A1 (en) 2005-08-02 2012-01-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
US7776887B2 (en) 2005-08-19 2010-08-17 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
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
CN101489557B (zh) 2006-02-27 2013-12-18 弗特克斯药品有限公司 包含vx-950的共晶体和包含所述共晶体的药物组合物
EP1993993A1 (en) 2006-03-16 2008-11-26 Vertex Pharmaceuticals Incorporated Processes and intermediates for preparing steric compounds
NZ571280A (en) 2006-03-16 2011-10-28 Vertex Pharma Deuterated hepatitis C protease inhibitors
JP2009530415A (ja) 2006-03-20 2009-08-27 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 医薬組成物
MX2008011976A (es) 2006-03-20 2009-04-07 Vertex Pharma Composiciones farmaceuticas.
MX2008015253A (es) 2006-05-31 2008-12-17 Vertex Pharma Formulaciones de liberacion controlada.

Also Published As

Publication number Publication date
EA200970805A1 (ru) 2010-02-26
NZ579296A (en) 2012-10-26
BRPI0807904A2 (pt) 2015-02-03
TW200843738A (en) 2008-11-16
JP2010523474A (ja) 2010-07-15
AU2008219689A1 (en) 2008-09-04
CL2008000579A1 (es) 2009-03-06
MX2009009174A (es) 2009-09-07
IL200611A0 (en) 2010-05-17
WO2008106139A1 (en) 2008-09-04
UY30941A1 (es) 2008-09-30
GEP20125683B (en) 2012-11-12
CA2679429A1 (en) 2008-09-04
KR20090127292A (ko) 2009-12-10
CN102015727A (zh) 2011-04-13
US20110182856A1 (en) 2011-07-28
CO6220931A2 (es) 2010-11-19
ECSP099601A (es) 2009-10-30
AP2009004971A0 (en) 2009-10-31
US7964624B1 (en) 2011-06-21
EP2631238A1 (en) 2013-08-28
US8372873B2 (en) 2013-02-12
AR065499A1 (es) 2009-06-10
EP2114958A1 (en) 2009-11-11

Similar Documents

Publication Publication Date Title
PE20081792A1 (es) Inhibidores de serina proteasas
JO2593B1 (en) Protease inhibitors NS3 hepatitis C HCV virus
MY164469A (en) Hcv ns3 protease inhibitors
PE20080457A1 (es) Compuestos de oximilo macrociclico inhibidores de proteasas de hepatitis c
DK1615613T3 (da) Quinoxalinyl-makrocykliske hepatitis C serin protease-inhibitorer
MX2007016324A (es) Inhibidores hcv.
TW200615275A (en) Hepatitis C inhibitor dipeptide analogs
EP1771454A4 (en) PEPTIDE ANALOGUE AS HEPATITIS C HEMMER
NO20081086L (no) Makrosykliske peptider som HCV NS3-proteaseinhibitorer
UA116616C2 (uk) Інгібітори hcv серинової протеази, отримані з макроциклічного проліну
MY148123A (en) Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
SG159385A1 (en) Inhibitors of serine proteases, particularly hepatitis c virus ns3 - ns4 protease
MX2009009176A (es) Inhibidores de serina-proteasas.
ATE547103T1 (de) Hemmer des hepatitis-c-virus
EA200901101A1 (ru) Макроциклические соединения в качестве ингибиторов протеазы ns3 вгс
MX2010006210A (es) Inhibidores de serina proteasa de hcv de tripeptido fluorado.
ES2240446T3 (es) Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.
PE20091237A1 (es) Derivados de pirrolidina como moduladores de serina proteasas
CU23787B7 (es) Compuestos macrocíclicos como inhibidores de la replicación viral
MX2011006631A (es) Inhibidores de proteasa ns3 del virus hcv.
ATE503764T1 (de) Inhibitoren des hepatitis-c-virus
EA200802346A1 (ru) Циклопропилконденсированные индолобензазепиновые ингибиторы белка ns5b вируса гепатита с
WO2004113365A3 (en) Hepatitis c serine protease tri-peptide inhibitors
WO2006119061A3 (en) Hcv ns3 protease inhibitors
PE20080072A1 (es) Compuestos heterociclicos como inhibidores de proteasas serinas

Legal Events

Date Code Title Description
FC Refusal