BRPI0615223A2 - inibidores das serina proteases - Google Patents

inibidores das serina proteases

Info

Publication number
BRPI0615223A2
BRPI0615223A2 BRPI0615223-6A BRPI0615223A BRPI0615223A2 BR PI0615223 A2 BRPI0615223 A2 BR PI0615223A2 BR PI0615223 A BRPI0615223 A BR PI0615223A BR PI0615223 A2 BRPI0615223 A2 BR PI0615223A2
Authority
BR
Brazil
Prior art keywords
serine protease
protease inhibitors
activity
hepatitis
virus
Prior art date
Application number
BRPI0615223-6A
Other languages
English (en)
Inventor
Kevin M Cottrell
John Maxwell
Qing Tang
Anne-Laure Grillot
Arnaud Le Tiran
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
Publication of BRPI0615223A2 publication Critical patent/BRPI0615223A2/pt

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

Abstract

INIBIDORES DAS SERINA PROTEASES. A presente invenção se refere aos compostos de fórmula (1); ou um sal farmaceuticamente aceitável ou misturas suas que inibem a atividade da serina protease, particularmente a atividade da N93-NS4A protease do vírus da hepatite C.
BRPI0615223-6A 2005-08-26 2006-08-28 inibidores das serina proteases BRPI0615223A2 (pt)

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
BRPI0615223A2 true BRPI0615223A2 (pt) 2009-07-14

Family

ID=37684363

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0615223-6A BRPI0615223A2 (pt) 2005-08-26 2006-08-28 inibidores das serina proteases

Country Status (21)

Country Link
US (2) US7985762B2 (pt)
EP (3) EP2364984A1 (pt)
JP (1) JP5394063B2 (pt)
KR (1) KR20080041715A (pt)
CN (1) CN101316852A (pt)
AR (1) AR055395A1 (pt)
AT (1) ATE530554T1 (pt)
AU (1) AU2006282771B2 (pt)
BR (1) BRPI0615223A2 (pt)
CA (1) CA2620621A1 (pt)
EA (1) EA200800670A1 (pt)
EC (1) ECSP088258A (pt)
ES (1) ES2374943T3 (pt)
GE (1) GEP20115280B (pt)
IL (1) IL189668A0 (pt)
MX (1) MX2008002606A (pt)
NO (1) NO20081467L (pt)
NZ (1) NZ566197A (pt)
TW (1) TW200730533A (pt)
WO (1) WO2007025307A2 (pt)
ZA (1) ZA200801793B (pt)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EE04023B1 (et) * 1996-10-18 2003-04-15 Vertex Pharmaceuticals Incorporated Seriinproteaaside, eriti C-hepatiidi viiruse NS3-proteaasi inhibiitorid
EP1268519B1 (en) * 2000-04-03 2005-06-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
EP1613620A1 (en) * 2003-04-11 2006-01-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
NZ544789A (en) * 2003-07-18 2010-01-29 Vertex Pharma Dithia-azaspiro-nonane and decane derivatives as inhibitors of serine proteases
UY28500A1 (es) * 2003-09-05 2005-04-29 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc.
TW200526686A (en) * 2003-09-18 2005-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
RU2006115558A (ru) * 2003-10-10 2007-11-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы сериновых протеаз, особенно hcv ns3-ns4a протеазы
PT1677827E (pt) * 2003-10-27 2009-03-13 Vertex Pharma Associações para o tratamento do vhc
US7683033B2 (en) * 2004-02-04 2010-03-23 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly 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
WO2007098270A2 (en) 2006-02-27 2007-08-30 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
MX2008013119A (es) 2006-04-11 2008-10-21 Novartis Ag Inhibidores de hcv/vih y sus usos.
US7935670B2 (en) 2006-07-11 2011-05-03 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
AU2007290535A1 (en) * 2006-08-28 2008-03-06 Vertex Pharmaceuticals Incorporated Method for identifying protease inhibitors
CA2664247A1 (en) * 2006-09-22 2008-03-27 Ranbaxy Laboratories Limited Inhibitors of phosphodiesterase type-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
US8003604B2 (en) 2006-11-16 2011-08-23 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7763584B2 (en) 2006-11-16 2010-07-27 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7888464B2 (en) 2006-11-16 2011-02-15 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2125113A2 (en) * 2007-02-26 2009-12-02 Achillion Pharmaceuticals, Inc. Tertiary amine substituted peptides useful as inhibitors of hcv replication
CN101903392A (zh) * 2007-02-27 2010-12-01 弗特克斯药品有限公司 丝氨酸蛋白酶的抑制剂
JP2010519330A (ja) 2007-02-27 2010-06-03 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 共結晶体およびそれを含む医薬組成物
FR2914920B1 (fr) * 2007-04-11 2011-09-09 Clariant Specialty Fine Chem F Procede de deacetalisation d'alpha-aminoacetals.
EP2494991A1 (en) 2007-05-04 2012-09-05 Vertex Pharmaceuticals Incorporated Combination therapy for the treatment of HCV infection
AR066528A1 (es) * 2007-05-10 2009-08-26 Array Biopharma Inc Peptidos inhibidores de la replicacion del virus de la hepatitis c
UY31272A1 (es) * 2007-08-10 2009-01-30 Almirall Lab Nuevos derivados de ácido azabifenilaminobenzoico
EP2100881A1 (en) * 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Pyrimidyl- or pyridinylaminobenzoic acid derivatives
CN101835774B (zh) 2007-08-30 2014-09-17 弗特克斯药品有限公司 共晶体和包含该共晶体的药物组合物
AR068756A1 (es) 2007-10-10 2009-12-02 Novartis Ag Compuestos peptidicos, formulacion farmaceutica y sus usos como moduladores del virus de la hepatitis c
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
RU2490272C2 (ru) 2008-02-04 2013-08-20 Айденикс Фармасьютикалз, Инк. Макроциклические ингибиторы серинпротеазы
CN102015652A (zh) 2008-03-20 2011-04-13 益安药业 作为丙型肝炎病毒抑制剂的氟化大环化合物
US8163921B2 (en) 2008-04-16 2012-04-24 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7964560B2 (en) 2008-05-29 2011-06-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2300491B1 (en) 2008-05-29 2016-01-06 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
US8563505B2 (en) 2008-09-29 2013-10-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8044087B2 (en) 2008-09-29 2011-10-25 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
JP2012505897A (ja) * 2008-10-15 2012-03-08 インターミューン・インコーポレーテッド 治療用抗ウイルス性ペプチド
US8283310B2 (en) 2008-12-15 2012-10-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2210615A1 (en) * 2009-01-21 2010-07-28 Almirall, S.A. Combinations comprising methotrexate and DHODH inhibitors
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
TW201116540A (en) * 2009-10-01 2011-05-16 Intermune Inc Therapeutic antiviral peptides
US20130040978A1 (en) * 2010-05-18 2013-02-14 Joseph L. Duffy 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
WO2012092409A2 (en) 2010-12-30 2012-07-05 Enanta Phararmaceuticals, Inc Macrocyclic hepatitis c serine protease inhibitors
PE20140039A1 (es) 2010-12-30 2014-03-01 Enanta Pharm Inc Inhibidores de serina proteasa de hepatitis c a base de macrociclicos de fenantridina
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
ES2613766T3 (es) 2012-10-19 2017-05-25 Bristol-Myers Squibb Company Derivados de carbamato de hexadecahidrociclopropa(e)pirrolo(1,2-a)(1,4)diazaciclopentadecinilo sustituidos con 9-metilo como inhibidores de la proteasa no estructural 3 (NS3) para el tratamiento de infecciones del virus de la hepatitis C
US9334279B2 (en) 2012-11-02 2016-05-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US9598433B2 (en) 2012-11-02 2017-03-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014070974A1 (en) 2012-11-05 2014-05-08 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
JP6342922B2 (ja) 2013-03-07 2018-06-13 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｃ型肝炎ウイルス阻害剤
EP2883876A1 (en) 2013-12-16 2015-06-17 Actelion Pharmaceuticals Ltd. Stereoselective synthesis of substituted pyrrolidines
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
KR102096349B1 (ko) 2015-07-31 2020-04-02 화이자 인코포레이티드 Magl 억제제로서의 1,1,1-트리플루오로-3-히드록시프로판-2-일 카르바메이트 유도체 및 1,1,1-트리플루오로-4-히드록시부탄-2-일 카르바메이트 유도체
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
WO2017222917A1 (en) * 2016-06-21 2017-12-28 Inception 4, Inc. Aliphatic prolinamide derivatives
US11292801B2 (en) 2016-07-05 2022-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
CN110023304A (zh) 2016-09-28 2019-07-16 布莱德治疗公司 钙蛋白酶调节剂及其治疗用途
CA3050625C (en) 2017-01-20 2021-07-20 Pfizer Inc. 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives as magl inhibitors
AU2018208848A1 (en) 2017-01-23 2019-07-18 Pfizer Inc., Heterocyclic spiro compounds as MAGL inhibitors
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
CA3095164A1 (en) * 2018-03-28 2019-10-03 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
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
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
EP0604182B1 (en) * 1992-12-22 2000-10-11 Eli Lilly And Company Inhibitors of HIV protease useful for the treatment of Aids
DE69332616T2 (de) 1992-12-29 2003-11-06 Abbott Lab Hemmer 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
IL113196A0 (en) 1994-03-31 1995-06-29 Bristol Myers Squibb Co Imidazole derivatives and pharmaceutical compositions containing the same
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) 1995-06-05 2002-07-16 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
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
EP1019410A1 (en) * 1995-11-23 2000-07-19 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
CN1116288C (zh) * 1996-04-23 2003-07-30 沃泰克斯药物股份有限公司 用作肌苷－5'－一磷酸脱氢酶抑制剂的脲衍生物
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
WO1997043310A1 (en) 1996-05-10 1997-11-20 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
AU723414B2 (en) * 1996-09-25 2000-08-24 Merck Sharp & Dohme Limited Spiro-azacyclic derivatives, their preparation and their use as tachykinin antagonists
DE69725023T2 (de) * 1996-10-08 2004-08-05 Colorado State University Research Foundation, Fort Collins Katalytische asymmetrische epoxidierung
EE04023B1 (et) * 1996-10-18 2003-04-15 Vertex Pharmaceuticals Incorporated Seriinproteaaside, eriti C-hepatiidi viiruse NS3-proteaasi inhibiitorid
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
HUP0004853A3 (en) 1997-08-11 2001-12-28 Boehringer Ingelheim Ca Ltd Hepatitis c inhibitor peptides, process for preparation thereof, pharmaceutical compositions comprising thereof, their use and their intermediates
US6767991B1 (en) 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
HUP0100100A3 (en) 1997-08-11 2001-12-28 Boehringer Ingelheim Ca Ltd Hepatitis c inhibitor peptide analogues, pharmaceutical compositions comprising thereof and their use
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
WO1999028482A2 (en) * 1997-11-28 1999-06-10 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
EP1066247B1 (en) 1998-03-31 2006-11-22 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly 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
AU6371900A (en) 1999-07-26 2001-02-13 Du Pont Pharmaceuticals Company Lactam inhibitors of hepatitis c virus ns3 protease
US7122627B2 (en) 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
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
AU2055301A (en) 1999-12-03 2001-06-12 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
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
EP1268519B1 (en) 2000-04-03 2005-06-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
CN1441806A (zh) * 2000-04-05 2003-09-10 先灵公司 包含n－环p2部分的丙型肝炎病毒的大环ns3－丝氨酸蛋白酶抑制剂
AU2001253621A1 (en) 2000-04-19 2001-11-07 Schering Corporation Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties
AU2001267886A1 (en) 2000-06-30 2002-01-14 Seikagaku Corporation Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them
JP2004504356A (ja) 2000-07-20 2004-02-12 メルク　エンド　カムパニー　インコーポレーテッド Ｃ型肝炎ウイルスのプロセシングおよび複製の抑制
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
CZ303213B6 (cs) 2000-07-21 2012-05-23 Schering Corporation Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostredek
AU2001277967A1 (en) * 2000-07-21 2002-02-05 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
CA2410682A1 (en) 2000-07-21 2002-01-31 Schering Corporation Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
AR034127A1 (es) * 2000-07-21 2004-02-04 Schering Corp Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
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
MXPA03004299A (es) 2000-11-20 2004-02-12 Bristol Myers Squibb Co Inhibidores de tripeptido de hepatitis c.
IL155842A0 (en) * 2000-12-12 2003-12-23 Schering Corp Diaryl peptides as ns3-serine protease inhibitors of hepatitis c virus
WO2002048116A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
AU2002230764A1 (en) * 2000-12-13 2002-06-24 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
US6653295B2 (en) * 2000-12-13 2003-11-25 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
CA2434386C (en) * 2001-01-22 2006-12-05 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
WO2002061149A2 (en) 2001-01-30 2002-08-08 Vertex Pharmaceuticals Incorporated A quantitative assay for nucleic acids
GB0102342D0 (en) * 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
MXPA03008882A (es) 2001-03-27 2003-12-08 Vertex Pharma Composiciones y metodos utiles para la infeccion por hcv.
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
JP2005500322A (ja) * 2001-07-03 2005-01-06 アルタナ　ファルマ　アクチエンゲゼルシャフト ３−フェニルイソセリンの製法
CN100402549C (zh) 2001-07-11 2008-07-16 沃泰克斯药物股份有限公司 桥连二环的丝氨酸蛋白酶抑制剂
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
HUP0501067A2 (en) * 2001-11-14 2006-02-28 Teva Pharma Amorphous and crystalline forms of losartan potassium and process for their preparation
ATE443703T1 (de) 2002-01-23 2009-10-15 Schering Corp Prolinderivate als ns3-serine protease hemmer, zur verwendung bei der bekämpfung von hepatitis c virusinfektion
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
CA2370396A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh 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
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
CA2369970A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
CN100381440C (zh) 2002-04-11 2008-04-16 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3-ns4蛋白酶的抑制剂
ES2361011T3 (es) 2002-05-20 2011-06-13 Bristol-Myers Squibb Company Inhibidores del virus de la hepatitis c.
KR20050040912A (ko) * 2002-08-01 2005-05-03 파마셋 인코포레이티드 플라비비리다에 감염 치료용의 비사이클로[4.2.1]노난시스템을 가지는 화합물
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
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
EP1590442A4 (en) 2003-02-07 2007-07-18 Enanta Pharm Inc MACROCYCLIC HEPATITIS C SERIN PROTEASE INHIBITORS
US20040180815A1 (en) 2003-03-07 2004-09-16 Suanne Nakajima Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
JP2006517960A (ja) 2003-02-18 2006-08-03 ファイザー インコーポレイテッド Ｃ型肝炎ウイルスの阻害剤、それを使用する組成物および治療法
JP4550824B2 (ja) 2003-03-05 2010-09-22 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃ型肝炎抑制化合物
CA2516018C (en) 2003-03-05 2011-08-23 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor peptide analogs
KR20060008877A (ko) 2003-04-10 2006-01-27 베링거 인겔하임 인터내셔날 게엠베하 루테늄 착물 촉매 존재하의 복분해 반응에 의한거대사이클릭 화합물의 제조방법
ES2381548T3 (es) 2003-04-11 2012-05-29 Vertex Pharmaceuticals Incorporated Inhibidores de serina proteasas, particularmente de la proteasa VHC NS3-NS4A
EP1613620A1 (en) 2003-04-11 2006-01-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP1629000B1 (en) 2003-04-16 2009-02-18 Bristol-Myers Squibb Company Macrocyclic isoquinoline peptide inhibitors of hepatitis c virus
PL1615613T3 (pl) 2003-04-18 2010-04-30 Enanta Pharm Inc Chinoksalinylowe makrocykliczne inhibitory proteazy serynowej zapalenia wątroby typu C
PE20050204A1 (es) * 2003-05-21 2005-05-04 Boehringer Ingelheim Int Compuestos inhibidores de la hepatitis c
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
NZ544789A (en) 2003-07-18 2010-01-29 Vertex Pharma Dithia-azaspiro-nonane and decane derivatives as inhibitors of serine proteases
WO2005018330A1 (en) * 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
EP1664090A2 (en) 2003-08-26 2006-06-07 Schering Corporation Novel peptidomimetic ns3-serine protease inhibitors of hepatitis c virus
UY28500A1 (es) * 2003-09-05 2005-04-29 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc.
US20050120398A1 (en) * 2003-09-12 2005-06-02 Vertex Pharmaceuticals Incorporated Animal model for HCV infection
TW200526686A (en) 2003-09-18 2005-08-16 Vertex Pharma 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
CA2536182C (en) 2003-09-22 2012-07-24 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis c virus
TWI280964B (en) 2003-09-26 2007-05-11 Schering Corp Macrocyclic inhibitors of hepatitis C virus NS3 serine protease
RU2006115558A (ru) 2003-10-10 2007-11-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы сериновых протеаз, особенно hcv ns3-ns4a протеазы
AR045870A1 (es) * 2003-10-11 2005-11-16 Vertex Pharma Terapia de combinacion para la infeccion de virus de hepatitis c
WO2005037214A2 (en) 2003-10-14 2005-04-28 Intermune, Inc. Macrocyclic carboxylic acids and acylsulfonamides as inhibitors of hcv replication
PT1677827E (pt) * 2003-10-27 2009-03-13 Vertex Pharma Associações para o tratamento do vhc
US8187874B2 (en) * 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1678202B1 (en) * 2003-10-27 2012-06-13 Vertex Pharmaceuticals Incorporated Hcv ns3-ns4a protease resistance mutants
ES2330944T3 (es) 2003-10-28 2009-12-17 Vertex Pharmaceuticals Incorporated Preparacion de derivados del acido 4,5-dialquil-3-acil-pirrol-2-carboxilico mediante sintesis de tipo fischer-fink y acilacion subsiguiente.
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
CN1902216A (zh) 2003-11-20 2007-01-24 先灵公司 丙肝病毒ns3蛋白酶的去肽化抑制剂
US7309708B2 (en) 2003-11-20 2007-12-18 Birstol-Myers Squibb Company Hepatitis C virus inhibitors
US7135462B2 (en) 2003-11-20 2006-11-14 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CA2547787A1 (en) 2003-12-01 2005-06-16 Vertex Pharmaceuticals Incorporated Compositions comprising fetal liver cells and methods useful for hcv infection
WO2005058821A1 (en) 2003-12-11 2005-06-30 Schering Corporation Inhibitors of hepatitis c virus ns3/ns4a serine protease
EP1730167B1 (en) 2004-01-21 2011-01-12 Boehringer Ingelheim International GmbH Macrocyclic peptides active against the hepatitis c virus
EP1713822B1 (en) 2004-01-30 2010-03-17 Medivir AB Hcv ns-3 serine protease inhibitors
US7683033B2 (en) 2004-02-04 2010-03-23 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
CN102911161A (zh) 2004-02-20 2013-02-06 贝林格尔.英格海姆国际有限公司 病毒聚合酶抑制剂
DE602005015093D1 (de) 2004-02-27 2009-08-06 Schering Corp Neue verbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
US7173057B2 (en) 2004-02-27 2007-02-06 Schering Corporation Ketoamides with cyclic P4'S as inhibitors of NS3 protease of hepatitis C virus
US7205330B2 (en) 2004-02-27 2007-04-17 Schering Corporation Inhibitors of hepatitis C virus NS3 protease
DE602005021760D1 (de) 2004-02-27 2010-07-22 Schering Corp Schwefelverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
ATE438622T1 (de) 2004-02-27 2009-08-15 Schering Corp 3,4-(cyclopentyl)kondensierte prolinverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
JP2007525510A (ja) 2004-02-27 2007-09-06 シェーリング　コーポレイション Ｃ型肝炎ウイルスｎｓ３セリンプロテアーゼのインヒビターとしての化合物
EP1725548B1 (en) * 2004-03-12 2015-01-14 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
AU2005228894B9 (en) 2004-03-30 2011-10-13 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
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
WO2005113581A1 (en) 2004-05-20 2005-12-01 Schering Corporation Substituted prolines as inhibitors of hepatitis c virus ns3 serine protease
KR101370580B1 (ko) * 2004-06-08 2014-03-06 버텍스 파마슈티칼스 인코포레이티드 약학 조성물
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
ATE512971T1 (de) 2004-07-20 2011-07-15 Boehringer Ingelheim Int Peptidanaloga als hepatitis c-hemmer
US7423113B2 (en) * 2004-08-25 2008-09-09 Vib Vzw Leptin antagonist
CN101068828A (zh) 2004-08-27 2007-11-07 先灵公司 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的酰基磺酰胺化合物
EP1804821A4 (en) 2004-10-01 2009-07-15 Vertex Pharma INHIBITION OF HCV NS3-NS4A PROTEASE
TW201424733A (zh) * 2004-10-29 2014-07-01 Vertex Pharma 劑量型式
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
EP2357170A1 (en) * 2005-08-19 2011-08-17 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
WO2007098270A2 (en) 2006-02-27 2007-08-30 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
US20070244334A1 (en) 2006-03-16 2007-10-18 Tanoury Gerald J Processes and intermediates for preparing steric compounds
CN101494979A (zh) 2006-03-20 2009-07-29 沃泰克斯药物股份有限公司 药物组合物
CA2646335A1 (en) 2006-03-20 2007-09-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
PT2037887E (pt) * 2006-05-31 2010-12-07 Vertex Pharma Formulações orais de libertação controlada de um inibidor da enzima conversora de interleucina-1 beta

Also Published As

Publication number Publication date
AU2006282771B2 (en) 2012-08-09
AR055395A1 (es) 2007-08-22
ATE530554T1 (de) 2011-11-15
KR20080041715A (ko) 2008-05-13
NO20081467L (no) 2008-05-15
US20070179167A1 (en) 2007-08-02
TW200730533A (en) 2007-08-16
NZ566197A (en) 2011-07-29
US8440706B2 (en) 2013-05-14
ES2374943T3 (es) 2012-02-23
EP1917269B1 (en) 2011-10-26
EP1917269A2 (en) 2008-05-07
AU2006282771A1 (en) 2007-03-01
IL189668A0 (en) 2008-06-05
US7985762B2 (en) 2011-07-26
EP2366704A1 (en) 2011-09-21
EP2366704B1 (en) 2013-10-23
EP2364984A1 (en) 2011-09-14
MX2008002606A (es) 2008-03-14
JP2009506078A (ja) 2009-02-12
CA2620621A1 (en) 2007-03-01
WO2007025307A2 (en) 2007-03-01
EA200800670A1 (ru) 2009-12-30
JP5394063B2 (ja) 2014-01-22
ECSP088258A (es) 2008-06-30
WO2007025307A3 (en) 2007-04-26
CN101316852A (zh) 2008-12-03
GEP20115280B (en) 2011-09-12
US20110165120A1 (en) 2011-07-07
ZA200801793B (en) 2008-12-31

Similar Documents

Publication Publication Date Title
BRPI0615223A2 (pt) inibidores das serina proteases
MX2009009174A (es) Inhibidores de serina-proteasas para el tratamiento de infecciones por el virus de hepatitis c.
RS52534B (en) MACROCYCLIC COMPOUNDS OF HINOXALINE AS HCV NS3 PROTEASE INHIBITORS
BRPI0615029A2 (pt) processos e intermediários
ATE513844T1 (de) Acylsulfonamidverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
ES2240446T3 (es) Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.
DE602005015834D1 (de) 3,4-(cyclopentyl)kondensierte prolinverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
MY145081A (en) Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease
BRPI0416902A (pt) inibidores de ns3/ns4a serina protease do vìrus da hepatite c
NO20064357L (no) Nye forbindelser som inhibitorer for hepatitt C-virus-NS3-serinprotease
TW200602037A (en) Novel compounds as inhibitors of hepatitis C virus NS3 serine protease
EA200901101A1 (ru) Макроциклические соединения в качестве ингибиторов протеазы ns3 вгс
RS53209B (en) PHARMACEUTICAL COMPOSITION FOR VIRAL HEPATITIS C PROTEASE INHIBITOR
EA200800371A1 (ru) Ингибиторы ns3 протеазы вгс
WO2008057995A3 (en) Hcv protease inhibitors
MX2009011064A (es) Compuestos de azufre como inhibidores de la serina proteasa ns3 del virus de la hepatitis c.
GT200600134A (es) Compuestos novedosos de derivados de aminosulfonilo
DE502005008057D1 (de) Substituierte cyclopenten-verbindungen
CL2007003540A1 (es) Compuestos derivados de macrociclos, inhibidores de la proteasa serina de hepatitis c; procedimiento de preparacion; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la hepatitis c.
MX2009008925A (es) Compuestos de la formula (i) como inhibidores de proteasa de serina.
NO20074544L (no) Inhibering av HER2-losriving med matriksmetalloproteaseantagonister
DE602005010421D1 (de) Neue Cysteine Protease Hemmers und ihre therapeutische Anwendungen
MX2010004704A (es) Inhibidores macrociclicos de la ns3 serina proteasa del virus de la hepatitis c.
EA200970372A1 (ru) Ингибитор развития болезни альцгеймера, содержащий гетероциклическое соединение
UA90909C2 (en) Hcv ns3 protease inhibitors

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2256 DE 01/04/2014.