ATE530554T1 - Serinprotease-hemmer - Google Patents

Serinprotease-hemmer

Info

Publication number
ATE530554T1
ATE530554T1 AT06813916T AT06813916T ATE530554T1 AT E530554 T1 ATE530554 T1 AT E530554T1 AT 06813916 T AT06813916 T AT 06813916T AT 06813916 T AT06813916 T AT 06813916T AT E530554 T1 ATE530554 T1 AT E530554T1
Authority
AT
Austria
Prior art keywords
protease inhibitors
serine protease
serine
inhibitors
protease
Prior art date
Application number
AT06813916T
Other languages
English (en)
Inventor
Kevin 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
Application filed by Vertex Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE530554T1 publication Critical patent/ATE530554T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/10—Spiro-condensed 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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 three hetero rings
    • C07D498/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • 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
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
AT06813916T 2005-08-26 2006-08-28 Serinprotease-hemmer ATE530554T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US71153005P 2005-08-26 2005-08-26
PCT/US2006/033770 WO2007025307A2 (en) 2005-08-26 2006-08-28 Inhibitors of serine proteases

Publications (1)

Publication Number Publication Date
ATE530554T1 true ATE530554T1 (de) 2011-11-15

Family

ID=37684363

Family Applications (1)

Application Number Title Priority Date Filing Date
AT06813916T ATE530554T1 (de) 2005-08-26 2006-08-28 Serinprotease-hemmer

Country Status (21)

Country Link
US (2) US7985762B2 (de)
EP (3) EP1917269B1 (de)
JP (1) JP5394063B2 (de)
KR (1) KR20080041715A (de)
CN (1) CN101316852A (de)
AR (1) AR055395A1 (de)
AT (1) ATE530554T1 (de)
AU (1) AU2006282771B2 (de)
BR (1) BRPI0615223A2 (de)
CA (1) CA2620621A1 (de)
EA (1) EA200800670A1 (de)
EC (1) ECSP088258A (de)
ES (1) ES2374943T3 (de)
GE (1) GEP20115280B (de)
IL (1) IL189668A0 (de)
MX (1) MX2008002606A (de)
NO (1) NO20081467L (de)
NZ (1) NZ566197A (de)
TW (1) TW200730533A (de)
WO (1) WO2007025307A2 (de)
ZA (1) ZA200801793B (de)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ298749B6 (cs) * 1996-10-18 2008-01-16 Vertex Pharmaceuticals Incorporated Inhibitory serinových proteáz a farmaceutické prostředky s jejich obsahem
JP4806154B2 (ja) * 2000-04-03 2011-11-02 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼのインヒビター
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
TW200510391A (en) * 2003-04-11 2005-03-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
BRPI0412761A (pt) * 2003-07-18 2006-09-26 Vertex Pharma inibidores de serino proteases, particularmente a protease ns3-ns4a do vhc
PE20050374A1 (es) * 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
CA2538791A1 (en) * 2003-09-18 2005-03-31 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
CA2541634A1 (en) * 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP1677827B1 (de) * 2003-10-27 2008-12-10 Vertex Pharmaceuticals Incorporated Kombinationen für die hcv-behandlung
EP2311851A3 (de) * 2004-02-04 2011-05-25 Vertex Pharmaceuticals Incorporated Inhibitoren der Serinproteasen, insbesondere der HCV-NS3-NS4A-Protease
JP5249028B2 (ja) 2005-07-25 2013-07-31 インターミューン・インコーポレーテッド C型肝炎ウイルス複製の新規大環状阻害剤
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
AR055395A1 (es) 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
US7964624B1 (en) 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
CA2643688A1 (en) 2006-02-27 2007-08-30 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
WO2007109080A2 (en) 2006-03-16 2007-09-27 Vertex Pharmaceuticals Incorporated Deuterated hepatitis c protease inhibitors
CA2643680A1 (en) * 2006-04-11 2007-11-22 Novartis Ag Hcv/hiv inhibitors and their uses
EP2049474B1 (de) 2006-07-11 2015-11-04 Bristol-Myers Squibb Company Hemmer des hepatitis-c-virus
EP2057278A2 (de) * 2006-08-28 2009-05-13 Vertex Pharmceuticals Incorporated Verfahren zur identifikation von protease-hemmern
MX2009003100A (es) * 2006-09-22 2009-05-11 Ranbaxy Lab Ltd Inhibidores de fosfodiesterasa tipo iv.
US8343477B2 (en) 2006-11-01 2013-01-01 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7888464B2 (en) 2006-11-16 2011-02-15 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
EP2125113A2 (de) 2007-02-26 2009-12-02 Achillion Pharmaceuticals, Inc. Tertiäramin-substituierte peptide als hcv-replikationshemmer
GEP20125645B (en) 2007-02-27 2012-09-25 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
FR2914920B1 (fr) 2007-04-11 2011-09-09 Clariant Specialty Fine Chem F Procede de deacetalisation d'alpha-aminoacetals.
ES2381410T3 (es) 2007-05-04 2012-05-28 Vertex Pharmceuticals Incorporated Terapia de combinación paa el tratamiento de infecciones por VHC
MX2009012093A (es) * 2007-05-10 2010-01-25 Intermune Inc Nuevos peptidos inhibidores de la replicacion del virus de la hepatitis c.
EP2100881A1 (de) * 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Pyrimidinyl- oder Pyridinylaminobenzoesäurederivate
UY31272A1 (es) * 2007-08-10 2009-01-30 Almirall Lab Nuevos derivados de ácido azabifenilaminobenzoico
WO2009032198A1 (en) 2007-08-30 2009-03-12 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
BRPI0817881A2 (pt) * 2007-10-10 2015-03-31 Novartis Ag Compostos orgânicos e seus usos
WO2009053828A2 (en) * 2007-10-22 2009-04-30 Enanta Pharmaceuticals, Inc. P3 hydroxyamino macrocyclic hepatitis c serine protease inhibitors
US8383583B2 (en) 2007-10-26 2013-02-26 Enanta Pharmaceuticals, Inc. Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors
US8202996B2 (en) 2007-12-21 2012-06-19 Bristol-Myers Squibb Company Crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N- ((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide
KR20100118991A (ko) 2008-02-04 2010-11-08 아이데닉스 파마슈티칼스, 인코포레이티드 매크로시클릭 세린 프로테아제 억제제
CA2719008A1 (en) 2008-03-20 2009-09-24 Enanta Pharmaceuticals, Inc. Fluorinated macrocyclic compounds as hepatitis c virus inhibitors
US8163921B2 (en) 2008-04-16 2012-04-24 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8044023B2 (en) 2008-05-29 2011-10-25 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7964560B2 (en) 2008-05-29 2011-06-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8207341B2 (en) 2008-09-04 2012-06-26 Bristol-Myers Squibb Company Process or synthesizing substituted isoquinolines
UY32099A (es) 2008-09-11 2010-04-30 Enanta Pharm Inc Inhibidores macrocíclicos de serina proteasas de hepatitis c
US8044087B2 (en) 2008-09-29 2011-10-25 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8563505B2 (en) 2008-09-29 2013-10-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CN102216321A (zh) * 2008-10-15 2011-10-12 因特蒙公司 治疗性抗病毒肽
US8283310B2 (en) 2008-12-15 2012-10-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2210615A1 (de) * 2009-01-21 2010-07-28 Almirall, S.A. Kombinationen, die Methotrexat und DHODH-Inhibitoren umfassen
US8377962B2 (en) 2009-04-08 2013-02-19 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US8232246B2 (en) * 2009-06-30 2012-07-31 Abbott Laboratories Anti-viral compounds
US9284307B2 (en) 2009-08-05 2016-03-15 Idenix Pharmaceuticals Llc Macrocyclic serine protease inhibitors
WO2011041551A1 (en) * 2009-10-01 2011-04-07 Intermune, Inc. Therapeutic antiviral peptides
CA2799414A1 (en) * 2010-05-18 2011-11-24 Merck Sharp & Dohme Corp. Spiro isoxazoline compounds as sstr5 antagonists
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
US8742110B2 (en) 2010-08-18 2014-06-03 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
WO2012092411A2 (en) 2010-12-30 2012-07-05 Enanta Pharmaceuticals, Inc. Phenanthridine macrocyclic hepatitis c serine protease inhibitors
CN103534256B (zh) 2010-12-30 2016-08-10 益安药业 大环丙型肝炎丝氨酸蛋白酶抑制剂
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
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US10201584B1 (en) 2011-05-17 2019-02-12 Abbvie Inc. Compositions and methods for treating HCV
US8691757B2 (en) 2011-06-15 2014-04-08 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CN103304571B (zh) * 2012-03-06 2018-02-16 凯惠科技发展(上海)有限公司 螺环化合物、其制备方法、中间体、药物组合物和应用
TW201408669A (zh) * 2012-08-08 2014-03-01 Merck Sharp & Dohme Hcv ns3蛋白酶抑制劑
SI2909205T1 (sl) 2012-10-19 2017-02-28 Bristol-Myers Squibb Company 9-metil substituiran heksadekahidrociklopropa(e)pirolo(1,2-A)(1,4)diazaciklopentadecinil karbamat derivati kot nestrukturalni 3 (NS3) proteazni inhibitorji za zdravljenje hepatitis C virusnih infekcij
EP2914613B1 (de) 2012-11-02 2017-11-22 Bristol-Myers Squibb Company Inhibitoren des hepatitis-c-virus
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2914598B1 (de) 2012-11-02 2017-10-18 Bristol-Myers Squibb Company Inhibitoren des hepatitis-c-virus
US9409943B2 (en) 2012-11-05 2016-08-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
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
US9580463B2 (en) 2013-03-07 2017-02-28 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2883876A1 (de) 2013-12-16 2015-06-17 Actelion Pharmaceuticals Ltd. Stereoselektive Synthese von substituierten Pyrrolidinen
WO2015103490A1 (en) 2014-01-03 2015-07-09 Abbvie, Inc. Solid antiviral dosage forms
WO2016144654A1 (en) 2015-03-09 2016-09-15 Washington University Inhibitors of growth factor activation enzymes
HK1249101A1 (zh) 2015-07-31 2018-10-26 辉瑞公司 作为magl抑制剂的1,1,1-三氟-3-羟基丙-2-基氨基甲酸酯衍生物及1,1,1-三氟-4-羟基丁-2-基氨基甲酸酯衍生物
EP3426674A4 (de) 2016-03-09 2019-08-14 Blade Therapeutics, Inc. Cyclische keto-amid-verbindungen als calpain-modulatoren sowie verfahren zur herstellung und verwendung davon
JP7076438B2 (ja) * 2016-06-21 2022-05-27 オリオン・オフサルモロジー・エルエルシー 脂肪族プロリンアミド誘導体
EP3481835A4 (de) 2016-07-05 2020-02-26 Blade Therapeutics, Inc. Calpain-modulatoren und therapeutische verwendungen davon
SG10201912574WA (en) 2016-09-28 2020-02-27 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof
BR112019014688A2 (pt) 2017-01-20 2020-02-18 Pfizer Inc. Derivados de carbamato de 1,1,1-trifluoro-3-hidroxipropan-2-il como inibidores de magl
EP3571202B1 (de) 2017-01-23 2021-06-30 Pfizer Inc. Heterocyclische spiro-verbindungen als magl-inhibitoren
RU2650610C1 (ru) 2017-02-28 2018-04-16 Васильевич Иващенко Александр Противовирусная композиция и способ ее применения
CN107954990A (zh) * 2017-11-14 2018-04-24 安徽诺全药业有限公司 一种雷迪帕维的制备方法
SG11202008750XA (en) * 2018-03-28 2020-10-29 Blade Therapeutics Inc Calpain modulators and therapeutic uses thereof

Family Cites Families (194)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US472484A (en) * 1892-04-05 Pneumatic tire
US633770A (en) 1898-10-15 1899-09-26 Diven Brothers & Company Rotary plow.
US3025516A (en) * 1952-11-03 1962-03-13 Stewart Warner Corp Frequency control system for radio identification apparatus
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
EP0204571B1 (de) 1985-06-07 1992-01-22 Ici Americas 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
DE4019586A1 (de) * 1990-06-20 1992-01-02 Bosch Gmbh Robert Kraftstoffeinspritzsystem fuer brennkraftmaschinen
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.
DE69305093T2 (de) 1992-12-29 1997-04-17 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
AU1615895A (en) 1994-03-31 1995-10-12 Bristol-Myers Squibb Company Imidazole-containing inhibitors of farnesyl protein transferase
US5756466A (en) 1994-06-17 1998-05-26 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
US5716929A (en) * 1994-06-17 1998-02-10 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
WO1997019084A1 (en) * 1995-11-23 1997-05-29 Merck Sharp & Dohme Limited 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
CZ298463B6 (cs) * 1996-04-23 2007-10-10 Vertex Pharmaceuticals Incorporated Deriváty mocoviny pro použití jako inhibitory IMPDH enzymu a farmaceutické prostredky, které je obsahují
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
EP0907659A1 (de) 1996-05-10 1999-04-14 Schering Corporation Hepatitis c virus ns3 protease synthetische inhibitoren
US6153579A (en) 1996-09-12 2000-11-28 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
ATE320432T1 (de) * 1996-09-25 2006-04-15 Merck Sharp & Dohme Spiro-azacyclische derivate, deren herstellung und verwendung als tachykinin-antagonisten
ATE250048T1 (de) * 1996-10-08 2003-10-15 Univ Colorado State Res Found Katalytische asymmetrische epoxidierung
CZ298749B6 (cs) 1996-10-18 2008-01-16 Vertex Pharmaceuticals Incorporated Inhibitory serinových proteáz a farmaceutické prostředky s jejich obsahem
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
AU6701598A (en) * 1997-03-14 1998-09-29 Vertex Pharmaceuticals Incorporated Inhibitors of impdh enzyme
GB9707659D0 (en) 1997-04-16 1997-06-04 Peptide Therapeutics Ltd Hepatitis C NS3 Protease inhibitors
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
DE69829381T2 (de) 1997-08-11 2006-04-13 Boehringer Ingelheim (Canada) Ltd., Laval Hepatitis c inhibitor peptide
US6767991B1 (en) 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
EP1012180B1 (de) 1997-08-11 2004-12-01 Boehringer Ingelheim (Canada) Ltd. Peptidanaloga mit inhibitorischer wirkung auf hepatitis c
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
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
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
GB9825946D0 (en) 1998-11-26 1999-01-20 Angeletti P Ist Richerche Bio Pharmaceutical compounds for the inhibition of hepatitis C virus NS3 protease
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
SK13332001A3 (sk) 1999-03-19 2002-02-05 Vertex Pharmaceuticals Incorporated Inhibítory IMPDH enzýmu a ich použitie
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
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
EP1206449A1 (de) 1999-07-26 2002-05-22 Bristol-Myers Squibb Company Lactame als hemmer der 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
WO2001040262A1 (en) 1999-12-03 2001-06-07 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
WO2001058929A1 (en) 2000-02-08 2001-08-16 Schering Corporation Azapeptides useful in the treatment of hepatitis c
WO2001064678A2 (en) 2000-02-29 2001-09-07 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
JP4806154B2 (ja) 2000-04-03 2011-11-02 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼのインヒビター
JP4748911B2 (ja) 2000-04-05 2011-08-17 シェーリング コーポレイション N−環状p2部分を含むc型肝炎ウイルスの大環状ns3‐セリンプロテアーゼ阻害剤
NZ521456A (en) 2000-04-19 2004-07-30 Schering Corp Macrocyclic NS3-Serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties
EP2289888A3 (de) 2000-06-30 2011-07-13 Seikagaku Corporation Epoxidcarboxylsäureamide, Azide und Aminoalkohole sowie Verfahren zur Herstellung von Alpha-Ketoamiden damit
EP1322325A4 (de) 2000-07-20 2004-09-15 Merck & Co Inc Inhibition der prozessierung und replikation des 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
CA2418199A1 (en) 2000-07-21 2002-01-31 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
MXPA03000627A (es) 2000-07-21 2004-07-30 Schering Corp Nuevos peptidos como inhibidores de proteasa serina-ns3 del virus de la hepatitis c.
WO2002008187A1 (en) * 2000-07-21 2002-01-31 Schering Corporation Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
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
CA2429359A1 (en) 2000-11-20 2002-08-08 Bristol-Myers Squibb Company Hepatitis c tripeptide inhibitors
HUP0303436A2 (hu) * 2000-12-12 2004-01-28 Schering Corp. Diaril-peptidek mint a hepatitis C vírus NS3-szerin proteáz inhibitorai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
AU2002230763A1 (en) 2000-12-13 2008-01-03 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
US6653295B2 (en) * 2000-12-13 2003-11-25 Bristol-Myers Squibb 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
SI1355916T1 (sl) 2001-01-22 2007-04-30 Merck & Co Inc Nukleozidni derivati kot inhibitorji RNA-odvisne RNA virusne polimeraze
GB0102342D0 (en) * 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
CA2436518A1 (en) 2001-01-30 2002-08-08 Vertex Pharmaceuticals Incorporated A quantitative assay for nucleic acids
KR100947911B1 (ko) 2001-03-27 2010-03-17 버텍스 파마슈티칼스 인코포레이티드 Hcv 감염에 유용한 조성물 및 방법
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
CA2450545A1 (en) * 2001-07-03 2003-01-16 Altana Pharma Ag Process for the production of 3-phenylisoserine
CA2449504A1 (en) 2001-07-11 2003-01-23 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
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
NZ531681A (en) * 2001-10-24 2007-05-31 Vertex Pharma Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system
CA2672549A1 (en) * 2001-11-14 2003-06-12 Ben-Zion Dolitzky Amorphous and crystalline forms of losartan potassium and process for their preparation
AU2003207625B2 (en) 2002-01-23 2006-09-07 Schering Corporation Proline compounds as NS3-serine protease inhibitors for use in treatment of hepatites C virus infection
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
US6642204B2 (en) 2002-02-01 2003-11-04 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
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
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
WO2004032827A2 (en) 2002-05-20 2004-04-22 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
JP2006507235A (ja) * 2002-08-01 2006-03-02 フアーマセツト・インコーポレイテツド フラビウイルス科ウイルス感染治療のためのビシクロ[4.2.1]ノナン系を有する化合物
AU2003277891A1 (en) 2002-09-23 2004-04-08 Medivir Ab Hcv ns-3 serine protease inhibitors
US20040138109A1 (en) 2002-09-30 2004-07-15 Boehringer Ingelheim Pharmaceuticals, Inc. Potent inhibitor of HCV serine protease
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
US20050159345A1 (en) 2002-10-29 2005-07-21 Boehringer Ingelheim International Gmbh Composition for the treatment of infection by Flaviviridae viruses
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
US7098231B2 (en) 2003-01-22 2006-08-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US7223785B2 (en) 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US20040180815A1 (en) 2003-03-07 2004-09-16 Suanne Nakajima Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
AU2004211637C1 (en) 2003-02-07 2010-08-19 Enanta Pharmaceuticals, Inc. Macrocyclic hepatitis C serine protease inhibitors
MXPA05008106A (es) 2003-02-18 2005-09-21 Pfizer Inhibidores del virus de la hepatitis c, composiciones y tratamientos que los emplean.
EP1601685A1 (de) 2003-03-05 2005-12-07 Boehringer Ingelheim International GmbH Hepatitis-c-inhibitierende verbindungen
JP4682140B2 (ja) 2003-03-05 2011-05-11 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縁体
EP1615949A1 (de) 2003-04-10 2006-01-18 Boehringer Ingelheim International GmbH Verfahren zur herstellung makrozyklischer verbindungen durch rutheniumkomplexkatalysierte metathesereaktion
TW200510391A (en) 2003-04-11 2005-03-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
ATE547412T1 (de) 2003-04-11 2012-03-15 Vertex Pharma Inhibitoren von serinproteasen, insbesondere hcv- ns3-ns4a-protease
EP1629000B1 (de) 2003-04-16 2009-02-18 Bristol-Myers Squibb Company Makrocyclische isochinolinpeptidinhibitoren des hepatitis-c-virus
SI1615613T1 (sl) 2003-04-18 2010-03-31 Enanta Pharm Inc Kinoksalinilni makrociklični inhibitorji serinske proteaze hepatitisa C
HRP20080014T3 (en) 2003-05-21 2008-02-29 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor compounds
WO2004113365A2 (en) 2003-06-05 2004-12-29 Enanta Pharmaceuticals, Inc. Hepatitis c serine protease tri-peptide inhibitors
US7125845B2 (en) 2003-07-03 2006-10-24 Enanta Pharmaceuticals, Inc. Aza-peptide macrocyclic hepatitis C serine protease inhibitors
BRPI0412761A (pt) * 2003-07-18 2006-09-26 Vertex Pharma inibidores de serino proteases, particularmente a protease ns3-ns4a do vhc
WO2005018330A1 (en) * 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
WO2005021584A2 (en) 2003-08-26 2005-03-10 Schering Corporation Novel peptidomimetic ns3-serine protease inhibitors of hepatitis c virus
PE20050374A1 (es) 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
EP1670415A4 (de) * 2003-09-12 2007-12-05 Vertex Pharma Tiermodell für die proteaseaktivität und leberschäden
CA2538791A1 (en) 2003-09-18 2005-03-31 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
RS20060197A (sr) 2003-09-22 2008-09-29 Boehringer Ingelheim International Gmbh., Makrociklični peptidi koji su aktivni protiv hepatitisa c virusa
KR20060085248A (ko) 2003-09-26 2006-07-26 쉐링 코포레이션 C형 간염 바이러스 ns3 세린 프로테아제의마크로사이클릭 억제제
CA2541634A1 (en) 2003-10-10 2005-04-28 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
TW201245229A (en) 2003-10-14 2012-11-16 Hoffmann La Roche Macrocyclic carboxylic acids and acylsulfonamides as inhibitors of HCV replication
JP4890254B2 (ja) 2003-10-27 2012-03-07 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 Hcvns3−ns4aプロテアーゼ耐性突然変異体
US8187874B2 (en) * 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1677827B1 (de) * 2003-10-27 2008-12-10 Vertex Pharmaceuticals Incorporated Kombinationen für die hcv-behandlung
US7250520B2 (en) 2003-10-28 2007-07-31 Vertex Pharmaceuticals Incorporated Processes for preparing pyrroles
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
US7309708B2 (en) 2003-11-20 2007-12-18 Birstol-Myers Squibb Company Hepatitis C virus inhibitors
JP2007532479A (ja) 2003-11-20 2007-11-15 シェーリング コーポレイション C型肝炎ウイルスns3プロテアーゼの脱ペプチド化インヒビター
US7135462B2 (en) 2003-11-20 2006-11-14 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
AU2004295702A1 (en) 2003-12-01 2005-06-16 Vertex Pharmaceuticals Incorporated Compositions comprising fetal liver cells and methods useful for HCV infection
CA2549167A1 (en) 2003-12-11 2005-06-30 Schering Corporation Inhibitors of hepatitis c virus ns3/ns4a serine protease
ATE495185T1 (de) 2004-01-21 2011-01-15 Boehringer Ingelheim Int Makrocyclische peptide mit wirkung gegen das hepatitis-c-virus
KR20120090077A (ko) 2004-01-30 2012-08-16 얀센 알 앤드 디 아일랜드 Hcv ns?3 세린 프로테아제 저해제
EP2311851A3 (de) 2004-02-04 2011-05-25 Vertex Pharmaceuticals Incorporated Inhibitoren der Serinproteasen, insbesondere der HCV-NS3-NS4A-Protease
UY28758A1 (es) 2004-02-20 2005-09-30 Boehringer Ingelheim Int Inhibidores de polimerasa viral
US20050187192A1 (en) 2004-02-20 2005-08-25 Kucera Pharmaceutical Company Phospholipids for the treatment of infection by togaviruses, herpes viruses and coronaviruses
AU2005219824B2 (en) 2004-02-27 2007-11-29 Merck Sharp & Dohme Corp. Novel ketoamides with cyclic p4's as inhibitors of ns3 serine protease of hepatitis c virus
US7205330B2 (en) 2004-02-27 2007-04-17 Schering Corporation Inhibitors of hepatitis C virus NS3 protease
DE602005023224D1 (de) 2004-02-27 2010-10-07 Schering Corp Neuartige Verbindungen als Hemmer von Hepatitis C-Virus NS3-Serinprotease
MY145081A (en) 2004-02-27 2011-12-15 Schering Corp Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease
US7192957B2 (en) 2004-02-27 2007-03-20 Schering Corporation Compounds as inhibitors of hepatitis C virus NS3 serine protease
ES2328589T3 (es) 2004-02-27 2009-11-16 Schering Corporation Compuestos de la prolina 3,4(ciclopentil) fusionados como inhibidores de la proteasa serina ns3 del virus de la hepatitis c.
KR101135765B1 (ko) * 2004-03-12 2012-04-23 버텍스 파마슈티칼스 인코포레이티드 아스파르트산 아세탈 카스파아제 억제제의 제조를 위한방법 및 중간체
AU2005228894B9 (en) 2004-03-30 2011-10-13 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
AR049635A1 (es) 2004-05-06 2006-08-23 Schering Corp (1r,2s,5s)-n-((1s)-3-amino-1-(ciclobutilmetil)-2,3-dioxopropil)-3-((2s)-2-((((1,1-dimetiletil)amino)carbonil)amino)-3,3-dimetil-1-oxobutil)-6,6-dimetil-3-azabiciclo(3.1.0)hexan-2-carboxamida como inhibidor de la ns3/ns4a serina proteasa del virus de la hepatitis c
CN1984922A (zh) 2004-05-20 2007-06-20 先灵公司 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的取代脯氨酸
AU2005253957B2 (en) * 2004-06-08 2011-08-25 Janssen Pharmaceutica Nv Pharmaceutical compositions
WO2006000085A1 (en) 2004-06-28 2006-01-05 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor peptide analogs
UY29016A1 (es) 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
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
US7423113B2 (en) * 2004-08-25 2008-09-09 Vib Vzw Leptin antagonist
CA2577812A1 (en) 2004-08-27 2006-03-09 Schering Corporation Acylsulfonamide compounds as inhibitors of hepatitis c virus ns3 serine protease
CA2583472A1 (en) 2004-10-01 2006-04-13 Chao Lin Hcv ns3-ns4a protease inhibition
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
CA2617679A1 (en) * 2005-08-02 2007-02-08 Steve Lyons Inhibitors of serine proteases
CA2619659A1 (en) * 2005-08-19 2007-02-22 Vertex Pharmaceuticals Incorporated Processes and intermediates
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
CA2643688A1 (en) 2006-02-27 2007-08-30 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
MX2008011869A (es) 2006-03-16 2008-12-03 Vertex Pharma Procedimientos e intermediarios para preparar compuestos estericos.
WO2007109080A2 (en) * 2006-03-16 2007-09-27 Vertex Pharmaceuticals Incorporated Deuterated hepatitis c protease inhibitors
WO2007109604A2 (en) 2006-03-20 2007-09-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
KR20140107691A (ko) 2006-03-20 2014-09-04 버텍스 파마슈티칼스 인코포레이티드 의약 조성물
CN101489530A (zh) * 2006-05-31 2009-07-22 弗特克斯药品有限公司 白介素1β转化酶的口服控制释放制剂

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AU2006282771A1 (en) 2007-03-01
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US20070179167A1 (en) 2007-08-02
KR20080041715A (ko) 2008-05-13
EP1917269B1 (de) 2011-10-26
US7985762B2 (en) 2011-07-26
ES2374943T3 (es) 2012-02-23
CA2620621A1 (en) 2007-03-01
EP2366704A1 (de) 2011-09-21
EP2366704B1 (de) 2013-10-23
EA200800670A1 (ru) 2009-12-30
AR055395A1 (es) 2007-08-22
NZ566197A (en) 2011-07-29
CN101316852A (zh) 2008-12-03
BRPI0615223A2 (pt) 2009-07-14
ECSP088258A (es) 2008-06-30
JP2009506078A (ja) 2009-02-12

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