UA81600C2 - Peptidomimetic protease inhibitors - Google Patents

Peptidomimetic protease inhibitors Download PDF

Info

Publication number
UA81600C2
UA81600C2 UA2003021834A UA200321834A UA81600C2 UA 81600 C2 UA81600 C2 UA 81600C2 UA 2003021834 A UA2003021834 A UA 2003021834A UA 200321834 A UA200321834 A UA 200321834A UA 81600 C2 UA81600 C2 UA 81600C2
Authority
UA
Ukraine
Prior art keywords
compound
group
mmol
solution
compounds
Prior art date
Application number
UA2003021834A
Other languages
English (en)
Russian (ru)
Ukrainian (uk)
Inventor
Роберт Эдвард Бабин
Чжу Цзюй Чен
Джейсон Эрик Леймар
Цзичень Дейвид Сан
Марк Семюель Теббе
Франтц Виктор
К. Мей Уанг
Айвен Колладо
Кристина Гарсиа-Паредес
Паркер Раймонд Семюэль, III
Линь Джин
Деки Гуо
Джон Эрвин Гласс
Original Assignee
Вертекс Фармасевтикалз Инкорпорейтыд
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=26923261&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UA81600(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Вертекс Фармасевтикалз Инкорпорейтыд filed Critical Вертекс Фармасевтикалз Инкорпорейтыд
Priority to UAA200710133A priority Critical patent/UA99895C2/uk
Publication of UA81600C2 publication Critical patent/UA81600C2/uk

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07Tetrapeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/21Interferons [IFN]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/21Interferons [IFN]
    • A61K38/212IFN-alpha
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/21Interferons [IFN]
    • A61K38/215IFN-beta
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/005Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • 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
    • C07K5/06052Val-amino acid
    • 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
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1016Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/095Oxytocins; Vasopressins; Related peptides
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2770/00MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA ssRNA viruses positive-sense
    • C12N2770/00011Details
    • C12N2770/24011Flaviviridae
    • C12N2770/24211Hepacivirus, e.g. hepatitis C virus, hepatitis G virus
    • C12N2770/24222New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Zoology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (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)
  • Plural Heterocyclic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
UA2003021834A 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors UA81600C2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
UAA200710133A UA99895C2 (uk) 2000-08-31 2001-08-31 Пептидоміметичний інгібітор протеаз

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22939800P 2000-08-31 2000-08-31
US27764101P 2001-03-21 2001-03-21
PCT/US2001/026008 WO2002018369A2 (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors

Publications (1)

Publication Number Publication Date
UA81600C2 true UA81600C2 (en) 2008-01-25

Family

ID=26923261

Family Applications (2)

Application Number Title Priority Date Filing Date
UAA200710133A UA99895C2 (uk) 2000-08-31 2001-08-31 Пептидоміметичний інгібітор протеаз
UA2003021834A UA81600C2 (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors

Family Applications Before (1)

Application Number Title Priority Date Filing Date
UAA200710133A UA99895C2 (uk) 2000-08-31 2001-08-31 Пептидоміметичний інгібітор протеаз

Country Status (36)

Country Link
US (5) US7820671B2 (enExample)
EP (9) EP1958956B1 (enExample)
JP (4) JP4689938B2 (enExample)
KR (10) KR20090120013A (enExample)
CN (7) CN102504014A (enExample)
AR (1) AR030591A1 (enExample)
AT (2) ATE431358T1 (enExample)
AU (2) AU8831801A (enExample)
BR (1) BR0113666A (enExample)
CA (2) CA2697205C (enExample)
CL (1) CL2010000330A1 (enExample)
CY (2) CY1109216T1 (enExample)
CZ (1) CZ2003595A3 (enExample)
DE (4) DE20122915U1 (enExample)
DK (2) DK1320540T5 (enExample)
DZ (1) DZ3438A1 (enExample)
EA (2) EA017556B1 (enExample)
EC (2) ECSP034493A (enExample)
ES (4) ES2489115T3 (enExample)
HR (1) HRP20030139B8 (enExample)
HU (1) HUP0300855A3 (enExample)
IL (6) IL154671A0 (enExample)
LU (1) LU91960I2 (enExample)
MX (1) MXPA03001780A (enExample)
NO (4) NO329929B1 (enExample)
NZ (2) NZ569670A (enExample)
PE (1) PE20020474A1 (enExample)
PL (1) PL211019B1 (enExample)
PT (1) PT1320540E (enExample)
SI (1) SI1320540T1 (enExample)
SK (1) SK2492003A3 (enExample)
SV (1) SV2003000617A (enExample)
TW (6) TWI359144B (enExample)
UA (2) UA99895C2 (enExample)
WO (1) WO2002018369A2 (enExample)
ZA (1) ZA200301641B (enExample)

Families Citing this family (241)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1133649C (zh) * 1996-10-18 2004-01-07 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蛋白酶的抑制剂
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
ATE297946T1 (de) * 2000-04-03 2005-07-15 Vertex Pharma Inhibitoren von serin proteasen, speziell der hepatitis-c-virus ns3-protease
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
CZ301182B6 (cs) 2000-05-26 2009-12-02 Idenix (Cayman) Limited Použití nukleosidových derivátu pro výrobu farmaceutických prostredku pro lécení infekcí vyvolaných flaviviry a pestiviry
SI1385870T1 (sl) 2000-07-21 2010-08-31 Schering Corp Peptidi kot NS3-serin proteazni inhibitorji virusa hepatitisa C
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
CZ2003195A3 (cs) 2000-07-21 2003-04-16 Schering Corporation Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostředek
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
GB2368339B (en) 2000-10-26 2002-09-18 Yissum Res Dev Co Complex incorporating a plurality of antioxidants
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
US7119072B2 (en) 2002-01-30 2006-10-10 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis C virus
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
PL373399A1 (en) 2002-04-11 2005-08-22 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AU2003299519A1 (en) * 2002-05-20 2004-05-04 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
CN104193791A (zh) 2002-06-28 2014-12-10 埃迪尼克斯医药公司 用于治疗黄病毒感染的修饰的2’和3’-核苷前药
US7608600B2 (en) 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
AU2003277891A1 (en) * 2002-09-23 2004-04-08 Medivir Ab Hcv ns-3 serine protease inhibitors
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
ATE457716T1 (de) 2002-12-30 2010-03-15 Angiotech Int Ag Wirkstofffreisetzung von schnell gelierender polymerzusammensetzung
JP2006526011A (ja) * 2003-04-11 2006-11-16 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ(特に、hcvns3−ns4aプロテアーゼ)のインヒビター
AU2011203054B2 (en) * 2003-04-11 2012-04-26 Vertex Pharmaceuticals, Incorporated Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease
ES2297424T3 (es) 2003-05-21 2008-05-01 Boehringer Ingelheim International Gmbh Compuestos inhibidores de la hepatitis c.
EP2345659A1 (en) 2003-05-30 2011-07-20 Pharmasset, Inc. Modified fluorinated nucleoside analogues
CN102020700A (zh) 2003-07-18 2011-04-20 沃泰克斯药物股份有限公司 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
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
ES2361997T3 (es) 2003-09-22 2011-06-27 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos activos contra el virus de la hepatitis c.
KR20060130027A (ko) * 2003-10-10 2006-12-18 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 hcv ns3-ns4a 프로테아제의억제제
US7365092B2 (en) * 2003-10-10 2008-04-29 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
ZA200602937B (en) * 2003-10-10 2007-06-27 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US7491794B2 (en) 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
US7494660B2 (en) 2003-10-27 2009-02-24 Vertex Pharmaceuticals Incorporated HCV NS3-NS4A protease resistance mutants
EP1677827B1 (en) * 2003-10-27 2008-12-10 Vertex Pharmaceuticals Incorporated Combinations for hcv treatment
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
EP1742913A1 (en) 2003-12-11 2007-01-17 Schering Corporation Inhibitors of hepatitis c virus ns3/ns4a serine protease
WO2005070955A1 (en) 2004-01-21 2005-08-04 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis c virus
CN1938332B (zh) 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂
CA2557495C (en) * 2004-02-27 2014-04-15 Schering Corporation Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease
RU2006134000A (ru) * 2004-02-27 2008-04-10 Шеринг Корпорейшн (US) Новые кетоамиды с циклическим p4s, действующие как ингибиторы сериновой протеазы ns3 ируса гепатита с
US7342041B2 (en) 2004-02-27 2008-03-11 Schering Corporation 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease
WO2005085275A1 (en) 2004-02-27 2005-09-15 Schering Corporation Inhibitors of hepatitis c virus ns3 protease
EP1765283A4 (en) * 2004-06-08 2012-11-28 Vertex Pharma PHARMACEUTICAL COMPOSITIONS
UY29016A1 (es) 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
CA2573346C (en) 2004-07-20 2011-09-20 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor peptide analogs
JP2008514723A (ja) * 2004-10-01 2008-05-08 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プロテアーゼの阻害
MY141025A (en) 2004-10-29 2010-02-25 Vertex Pharma Dose forms
HRP20130419T1 (en) 2005-03-21 2013-06-30 Virobay, Inc. Alpha ketoamide compounds as cysteine protease inhibitors
CA2604640A1 (en) * 2005-04-12 2006-10-19 Romark Laboratories L.C. Methods for treating diseases through interruption of protein maturation, compounds that inhibit the function of molecular chaperones such as protein disulfide isomerases or interfere with glycosylation, pharmaceutical compositions comprising them, and screening methods for identifying therapeutic agents
NZ563909A (en) 2005-05-13 2011-10-28 Virochem Pharma Inc Thiophene derivatives and their use for the treatment or prevention of flavivirus infections
US20070004635A1 (en) * 2005-06-02 2007-01-04 Schering Corporation Method of treating interferon non-responders using HCV protease inhibitor
US8119602B2 (en) 2005-06-02 2012-02-21 Schering Corporation Administration of HCV protease inhibitors in combination with food to improve bioavailability
ES2572980T3 (es) 2005-06-02 2016-06-03 Merck Sharp & Dohme Corp. Combinación de inhibidores de la proteasa del VHC con un tensioactivo
WO2006130666A2 (en) * 2005-06-02 2006-12-07 Schering Corporation Medicaments and methods combining a hcv protease inhibitor and an akr competitor
US7608592B2 (en) * 2005-06-30 2009-10-27 Virobay, Inc. HCV inhibitors
RS52058B (sr) 2005-07-29 2012-04-30 Tibotec Pharmaceuticals Makrociklički inhibitori virusa hepatitisa c
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
JO2768B1 (en) 2005-07-29 2014-03-15 تيبوتيك فارماسيوتيكالز ليمتد Large cyclic inhibitors of hepatitis C virus
TWI393723B (zh) 2005-07-29 2013-04-21 Tibotec Pharm Ltd C型肝炎病毒之大環抑制劑(九)
JP5230415B2 (ja) 2005-07-29 2013-07-10 テイボテク・フアーマシユーチカルズ C型肝炎ウイルスの大員環状阻害剤
US8183277B2 (en) 2005-07-29 2012-05-22 Tibotec Pharmaceuticals Ltd. Macrocylic inhibitors of hepatitis C virus
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
DE602006019883D1 (de) 2005-07-29 2011-03-10 Medivir Ab Makrocyclische inhibitoren des hepatitis-c-virus
EP2402331A1 (en) * 2005-08-02 2012-01-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
DE602006013492D1 (de) * 2005-08-19 2010-05-20 Vertex Pharma Verfahren und zwischenprodukte
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
US7964624B1 (en) 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
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
KR20140098867A (ko) 2005-11-11 2014-08-08 버텍스 파마슈티칼스 인코포레이티드 C형 간염 바이러스 변이체
JP4047365B2 (ja) * 2006-01-11 2008-02-13 生化学工業株式会社 シクロアルカンカルボキサミド誘導体及びその製造方法
JP3975226B2 (ja) * 2006-01-11 2007-09-12 生化学工業株式会社 シクロアルキルカルボニルアミノ酸誘導体及びその製造方法
WO2007080884A1 (ja) * 2006-01-11 2007-07-19 Seikagaku Corporation シクロアルキルカルボニルアミノ酸エステル誘導体及びその製造方法
US8183413B2 (en) 2006-01-20 2012-05-22 Kaneka Corporation Process for production of β-amino-α-hydroxy carboxamide derivative
US8039475B2 (en) * 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
JP5646814B2 (ja) * 2006-03-06 2014-12-24 アッヴィ・インコーポレイテッド Hcvを治療するためのリトナビルの組成物及び使用方法
NZ571281A (en) * 2006-03-16 2011-11-25 Vertex Pharma Processes and intermediates for preparing steric compounds
KR20080112303A (ko) 2006-03-16 2008-12-24 버텍스 파마슈티칼스 인코포레이티드 중수소화 c형 간염 프로테아제 억제제
NZ571934A (en) 2006-03-20 2012-05-25 Vertex Pharma Methods of spray drying formulations of vx-950 (telaprevir)
WO2007111866A2 (en) * 2006-03-23 2007-10-04 Schering Corporation Combinations of hcv protease inhibitor(s) and cyp3a4 inhibitor(s), and methods of treatment related thereto
KR101059593B1 (ko) 2006-04-11 2011-08-25 노파르티스 아게 Hcv/hiv 억제제 및 이들의 용도
WO2007120595A2 (en) * 2006-04-11 2007-10-25 Novartis Ag Amines for the treatment of hcv
WO2007137080A2 (en) 2006-05-23 2007-11-29 Irm Llc Compounds and compositions as channel activating protease inhibitors
DE102006059317A1 (de) * 2006-07-04 2008-01-10 Evonik Degussa Gmbh Verfahren zur Herstellung von β-Amino-α-hydroxy-carbonsäureamiden
EP1886685A1 (en) 2006-08-11 2008-02-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods, uses and compositions for modulating replication of hcv through the farnesoid x receptor (fxr) activation or inhibition
US20120220520A1 (en) * 2006-10-17 2012-08-30 Van T Klooster Gerben Albert Eleutherius Bioavailable combinations for hcv treatment
NZ576780A (en) 2006-11-15 2011-12-22 Virochem Pharma Inc Thiophene analogues for the treatment or prevention of flavivirus infections
ES2470568T3 (es) 2006-11-17 2014-06-24 Janssen R&D Ireland Inhibidores macroc�clicos del virus de la hepatitis C
CA2673111A1 (en) 2006-12-07 2008-06-19 Schering Corporation Ph sensitive matrix formulation
WO2008074035A1 (en) * 2006-12-27 2008-06-19 Abbott Laboratories Hcv protease inhibitors and uses thereof
WO2008095058A1 (en) * 2007-02-01 2008-08-07 Taigen Biotechnology Co. Ltd. Hcv protease inhibitors
KR20090110314A (ko) 2007-02-08 2009-10-21 티보텍 파마슈티칼즈 리미티드 피리미딘 치환된 마크로사이클릭 hcv 억제제
BRPI0807483A2 (pt) 2007-02-09 2014-05-13 Irm Llc Compostos e composições como inibidores de protease de ativação de canal
EP2134717A2 (en) 2007-02-27 2009-12-23 Vertex Pharmceuticals Incorporated Inhibitors of serine proteases
PT2114924E (pt) * 2007-02-27 2012-04-03 Vertex Pharma Co-cristais e composições farmacêuticas que compreendem os mesmos
WO2008127613A1 (en) * 2007-04-11 2008-10-23 Scynexis, Inc. New pharmaceutical compositions
CN101815533A (zh) 2007-05-04 2010-08-25 弗特克斯药品有限公司 用于治疗hcv感染的组合治疗
EP2194976B1 (en) * 2007-08-03 2015-12-09 Biotron Limited Hepatitis C antiviral compositions comprising 5-(1-methylpyrazol-4-yl)2-naphthoylguanidine and 2'-C-methyladenosine or 2'-C-methylcytidine
JP5443360B2 (ja) * 2007-08-30 2014-03-19 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
DK2061513T3 (da) 2007-09-14 2011-11-21 Schering Corp Fremgangsmåde til behandling af patienter med hepatitis C
US20090082366A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched telaprevir
JP5095824B2 (ja) 2007-10-10 2012-12-12 ノバルティス アーゲー スピロピロリジン類およびhcvおよびhiv感染に対するその使用
WO2009055467A2 (en) * 2007-10-24 2009-04-30 Virobay, Inc. Compounds that inhibit protease cathepsin s and hcv replication
WO2009055335A2 (en) * 2007-10-25 2009-04-30 Taigen Biotechnology Co., Ltd. Hcv protease inhibitors
CA2710644C (en) 2007-12-24 2016-03-29 Tibotec Pharmaceuticals Macrocyclic indoles as hepatitis c virus inhibitors
DE102008009761A1 (de) 2008-02-19 2009-08-27 Bayer Materialscience Ag Verfahren zur Herstellung von Isocyanaten
EP2101173A1 (en) 2008-03-14 2009-09-16 Vivalis In vitro method to determine whether a drug candidate active against a target protein is active against a variant of said protein
CN101580535B (zh) * 2008-05-16 2012-10-03 太景生物科技股份有限公司 丙型肝炎病毒蛋白酶抑制剂
CN102816106A (zh) 2008-06-24 2012-12-12 默沙东公司 用于制备基本上立体异构纯的稠合二环脯氨酸化合物的生物催化方法
US8569337B2 (en) 2008-07-23 2013-10-29 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
WO2010014744A1 (en) * 2008-07-29 2010-02-04 The Scripps Research Institute Inhibitors of hepatitis c virus infection
US8188137B2 (en) 2008-08-15 2012-05-29 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
BRPI0922366B8 (pt) 2008-12-03 2021-05-25 Presidio Pharmaceuticals Inc composto, composição farmacêutica e uso de um composto
SG171890A1 (en) 2008-12-03 2011-07-28 Presidio Pharmaceuticals Inc Inhibitors of hcv ns5a
GB0900914D0 (en) 2009-01-20 2009-03-04 Angeletti P Ist Richerche Bio Antiviral agents
EP2396028A2 (en) 2009-02-12 2011-12-21 Vertex Pharmceuticals Incorporated Hcv combination therapies comprising pegylated interferon, ribavirin and telaprevir
EP2410843A4 (en) 2009-03-27 2012-08-08 Presidio Pharmaceuticals Inc FUSIONED CORE INHIBITORS OF HEPATITIS C
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
WO2010151487A1 (en) 2009-06-23 2010-12-29 Gilead Sciences, Inc. Combination of telaprevir with 5- ({6- [2,4-bis (trifluoromethyl) phenyl] pyridazin-3 -yl)methyl) -2- (2 -fluorophenyl) -5h- imidazo [4, 5-c]pyridine for the treatment of hcv
EP2477980B1 (en) 2009-09-15 2016-06-08 Taigen Biotechnology Co., Ltd. Hcv protease inhibitors
TWI404269B (zh) * 2009-09-18 2013-08-01 Advanced Connectek Inc High speed plug connector
UA108211C2 (uk) 2009-11-04 2015-04-10 Янссен Рід Айрленд Бензімідазолімідазольні похідні
AU2010326225A1 (en) 2009-11-25 2012-06-07 Vertex Pharmaceuticals Incorporated 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections
AR079528A1 (es) * 2009-12-18 2012-02-01 Idenix Pharmaceuticals Inc Inhibidores de arileno o heteroarileno 5,5-fusionado del virus de la hepatitis c
CA2784036A1 (en) 2009-12-24 2011-06-30 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
US20110178107A1 (en) * 2010-01-20 2011-07-21 Taigen Biotechnology Co., Ltd. Hcv protease inhibitors
CA2788155C (en) 2010-01-27 2018-04-24 AB Pharma Ltd. Polyheterocyclic compounds highly potent as hcv inhibitors
EP2528605A1 (en) 2010-01-29 2012-12-05 Vertex Pharmaceuticals Incorporated Therapies for treating hepatitis c virus infection
WO2011112516A1 (en) 2010-03-08 2011-09-15 Ico Therapeutics Inc. Treating and preventing hepatitis c virus infection using c-raf kinase antisense oligonucleotides
WO2011119860A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
CA2794145A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
AU2011232348A1 (en) 2010-03-24 2012-10-11 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of Flavivirus infections
WO2011119858A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
BR112012024661A2 (pt) 2010-04-01 2015-09-15 Centre Nat Rech Scient composto, composição farmacêutica e método de tratamento de um hospedeiro infectado com vírus de hepatite c
EP2575866A4 (en) 2010-05-24 2013-10-16 Presidio Pharmaceuticals Inc HCV NS5A INHIBITORS
JP2013528624A (ja) 2010-06-03 2013-07-11 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 方法および中間体
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
EP2582717A2 (en) 2010-06-15 2013-04-24 Vertex Pharmaceuticals Incorporated Hcv ns5b polymerase mutants
MX2012014918A (es) 2010-06-28 2013-04-08 Vertex Pharma Compuestos y metodos para tratamiento o prevencion de infecciones por flavivirus.
WO2012006070A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
EP2585448A1 (en) 2010-06-28 2013-05-01 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
AR082215A1 (es) 2010-07-14 2012-11-21 Vertex Pharma Composicion farmaceutica agradable al paladar
WO2012020036A1 (en) 2010-08-13 2012-02-16 F. Hoffmann-La Roche Ag Hepatitis c virus inhibitors
AU2011292040A1 (en) 2010-08-17 2013-03-07 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of Flaviviridae viral infections
EA025341B1 (ru) 2010-09-22 2016-12-30 Алиос Биофарма, Инк. Замещенные аналоги нуклеотидов
EA201390532A1 (ru) 2010-10-08 2013-09-30 Новартис Аг Композиции сульфамидых ингибиторов ns3, содержащие витамин е
CA2815416A1 (en) 2010-10-21 2012-04-26 Vertex Pharmaceuticals Incorporated Biomarkers for hcv infected patients
BR112013009789A2 (pt) 2010-10-26 2016-07-19 Presidio Pharmaceuticals Inc inibidores do vírus da hepatite c
WO2012109646A1 (en) 2011-02-11 2012-08-16 Vertex Pharmaceuticals Incorporated Treatment of hcv in hiv infection patients
WO2012107589A1 (en) 2011-02-11 2012-08-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment and prevention of hcv infections
WO2012123298A1 (en) 2011-03-11 2012-09-20 F. Hoffmann-La Roche Ag Antiviral compounds
US9243025B2 (en) 2011-03-31 2016-01-26 Idenix Pharmaceuticals, Llc Compounds and pharmaceutical compositions for the treatment of viral infections
WO2012151319A1 (en) 2011-05-02 2012-11-08 Virobay, Inc. Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain
EP2707347A1 (en) 2011-05-13 2014-03-19 Vertex Pharmaceuticals Inc. Processes and intermediates
WO2012171332A1 (zh) 2011-06-16 2012-12-20 爱博新药研发(上海)有限公司 抑制丙型肝炎病毒的大环状杂环化合物及其制备和应用
RU2014102102A (ru) 2011-06-23 2015-07-27 Дигна Байотек, С.Л. КОМПОЗИЦИЯ И КОМБИНИРОВАННЫЙ ПРЕПАРАТ ИНТЕРФЕРОНА-а5 С ИНТЕРФЕРОНОМ-а2 И СПОСОБ ЛЕЧЕНИЯ ХРОНИЧЕСКОГО ГЕПАТИТА С
WO2012175581A1 (en) 2011-06-24 2012-12-27 F. Hoffmann-La Roche Ag Antiviral compounds
WO2013016499A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Methods for preparation of thiophene compounds
WO2013016501A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Formulations of thiophene compounds
AU2012308900A1 (en) 2011-09-12 2013-05-09 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
US9474759B2 (en) 2011-09-27 2016-10-25 Kansas State University Research Foundation Broad-spectrum antivirals against 3C or 3C-like proteases of picornavirus-like supercluster: picornaviruses, caliciviruses and coronaviruses
BR112014008616A2 (pt) 2011-10-10 2017-04-18 Hoffmann La Roche compostos antivirais
PH12014500625B1 (en) 2011-10-14 2018-12-12 Bristol Myers Squibb Co Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
CN103987696B (zh) 2011-10-14 2016-12-21 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
CN103987697B (zh) 2011-10-14 2017-04-26 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
US8466159B2 (en) 2011-10-21 2013-06-18 Abbvie Inc. Methods for treating HCV
PT107924A (pt) 2011-10-21 2014-12-03 Abbvie Inc Tratamento de combinação de daa (eg. com abt-072 ou abt-333) para utilização no tratamento de hcv
ES2572329B1 (es) 2011-10-21 2017-08-24 Abbvie Inc. Combinación de al menos dos agentes antivirales de acción directa y ribavirina pero no interferón, para uso en el tratamientodel vhc
US8492386B2 (en) 2011-10-21 2013-07-23 Abbvie Inc. Methods for treating HCV
ES2564906T3 (es) 2011-12-16 2016-03-29 F. Hoffmann-La Roche Ag Inhibidores de NS5A del VHC
AU2012357986B2 (en) 2011-12-20 2017-02-02 Riboscience Llc 4'-Azido, 3'-fluoro substituted nucleoside derivatives as inhibitors of HCV RNA replication
EP2794629B1 (en) 2011-12-20 2017-05-24 Riboscience LLC 2',4'-difluoro-2'-methyl substituted nucleoside derivatives as inhibitors of hcv rna replication
CN104203940B (zh) 2011-12-28 2017-01-18 爱尔兰詹森科学公司 作为hcv抑制剂的杂双环衍生物
WO2013116339A1 (en) 2012-01-31 2013-08-08 Vertex Pharmaceuticals Incorporated High potency formulations of vx-950
ITMI20120192A1 (it) 2012-02-13 2013-08-14 Dipharma Francis Srl Procedimento per la preparazione di un inibitore delle proteasi virali e suoi intermedi
WO2013123456A1 (en) * 2012-02-16 2013-08-22 Rqx Pharmaceuticals, Inc. Linear peptide antibiotics
KR20140130449A (ko) 2012-02-24 2014-11-10 에프. 호프만-라 로슈 아게 항바이러스 화합물
ITMI20120359A1 (it) 2012-03-07 2013-09-08 Dipharma Francis Srl Procedimento per la preparazione di intermedi utili nella preparazione di un inibitore delle proteasi virali
ITMI20120391A1 (it) * 2012-03-13 2013-09-14 Dipharma Francis Srl Procedimento per la sintesi di un intermedio ciclopropilammidico utile nella preparazione di un inibitore delle proteasi virali
WO2013136265A1 (en) 2012-03-13 2013-09-19 Dipharma Francis S.R.L. Synthesis of an intermediate of an antiviral compound
US8916538B2 (en) 2012-03-21 2014-12-23 Vertex Pharmaceuticals Incorporated Solid forms of a thiophosphoramidate nucleotide prodrug
NZ630805A (en) 2012-03-22 2016-01-29 Alios Biopharma Inc Pharmaceutical combinations comprising a thionucleotide analog
CA2872147A1 (en) 2012-05-02 2013-11-07 Kansas State University Research Foundation Macrocyclic and peptidomimetic compounds as broad-spectrum antivirals against 3c or 3c-like proteases of picornaviruses, caliciviruses and coronaviruses
ITMI20120800A1 (it) * 2012-05-10 2013-11-11 Dipharma Francis Srl Procedimento per la preparazione di un intermedio utile nella preparazione di un inibitore delle proteasi virali
WO2013178682A2 (en) 2012-05-30 2013-12-05 Chemo Ibérica, S.A. Multicomponent process for the preparation of bicyclic compounds
CN103450066B (zh) * 2012-05-30 2017-03-15 博瑞生物医药(苏州)股份有限公司 特拉匹韦中间体的制备方法
US20140010783A1 (en) 2012-07-06 2014-01-09 Hoffmann-La Roche Inc. Antiviral compounds
WO2014015217A1 (en) 2012-07-19 2014-01-23 Vertex Pharmaceuticals Incorporated Biomarkers for hcv infected patients
WO2014033667A1 (en) 2012-08-30 2014-03-06 Ranbaxy Laboratories Limited Process for the preparation of telaprevir
WO2014045263A2 (en) * 2012-09-24 2014-03-27 Dr. Reddy's Laboratories Limited Process for preparation of intermediates of telaprevir
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
MX351848B (es) 2012-10-12 2017-10-31 Bristol Myers Squibb Co Formas cristalinas de inhibidor del factor xia.
WO2014059202A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
CA2889903C (en) 2012-10-29 2021-03-09 Manjinder Singh Phull Antiviral phosphonate analogues and process for preparation thereof
ITMI20122036A1 (it) 2012-11-29 2014-05-30 Dipharma Francis Srl Sintesi di un intermedio di un composto antivirale
WO2014096374A1 (en) 2012-12-21 2014-06-26 Sandoz Ag Process for the synthesis of pyrrolidines and pyrroles
CN105073726B (zh) 2013-01-23 2017-05-31 弗·哈夫曼-拉罗切有限公司 抗病毒三唑衍生物
CN103113288B (zh) * 2013-02-04 2015-05-20 苏州永健生物医药有限公司 一种八氢环戊烯并[c]吡咯羧酸衍生物的合成方法
US20150065439A1 (en) 2013-02-28 2015-03-05 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
CN105008350B (zh) 2013-03-05 2018-05-08 弗·哈夫曼-拉罗切有限公司 抗病毒化合物
WO2014160668A1 (en) 2013-03-25 2014-10-02 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
ITMI20130706A1 (it) 2013-04-30 2014-10-31 Dipharma Francis Srl Procedimento per la preparazione di un inibitore delle proteasi virali e suoi intermedi
US9895442B2 (en) 2013-05-16 2018-02-20 Riboscience Llc 4′-fluoro-2′-methyl substituted nucleoside derivatives as inhibitors of HCV RNA replication
MA38678A1 (fr) 2013-05-16 2017-07-31 Riboscience Llc Dérivés nucléosidiques 4'-azido, 3'désoxy-3'-fluoro substitués
US20180200280A1 (en) 2013-05-16 2018-07-19 Riboscience Llc 4'-Fluoro-2'-Methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication
CN104163851B (zh) * 2013-05-20 2019-03-05 湘北威尔曼制药股份有限公司 氟代的α-羰基类HCV NS3/4A丝氨酸蛋白酶抑制剂
CN103288671B (zh) * 2013-06-20 2014-10-29 上海步越化工科技有限公司 一种(3s)-3-氨基-n-环丙基-2-羟基己酰胺盐酸盐的合成方法
WO2014203224A1 (en) 2013-06-21 2014-12-24 Ranbaxy Laboratories Limited Process for the preparation of telaprevir and its intermediates
WO2014203208A1 (en) 2013-06-21 2014-12-24 Ranbaxy Laboratories Limited Process for the preparation of telaprevir and intermediates thereof
CN104292146B (zh) * 2013-06-24 2017-04-26 上海医药工业研究院 特拉匹韦中间体及其制备方法
CN104558106B (zh) * 2013-10-19 2019-12-10 广东东阳光药业有限公司 一种治疗丙肝药物的制备方法
CN104610272B (zh) * 2013-11-05 2017-03-29 上海唐润医药科技有限公司 环状黄酮或异黄酮类化合物及其用途
EP2899207A1 (en) 2014-01-28 2015-07-29 Amikana.Biologics New method for testing HCV protease inhibition
SG10201908467RA (en) 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2760821T3 (enExample) 2014-01-31 2018-03-10
CN104926831A (zh) * 2014-03-20 2015-09-23 上海医药工业研究院 合成特拉匹韦的中间体及其制备方法
CN104926712B (zh) * 2014-03-20 2018-03-23 上海医药工业研究院 合成特拉匹韦的中间体及其制备方法
MX392718B (es) 2014-07-07 2025-03-24 Halliburton Energy Services Inc Herramientas de fondo de pozo que comprenden elementos de sellado degradables en fluido acuoso.
WO2016036893A1 (en) 2014-09-04 2016-03-10 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
CN108699105A (zh) 2016-03-04 2018-10-23 豪夫迈·罗氏有限公司 作为htra1抑制剂的新型二氟酮酰胺衍生物
HK1257565A1 (zh) 2016-03-04 2019-10-25 豪夫迈‧罗氏有限公司 作为htra1抑制剂的新型三氟甲基丙酰胺衍生物
CA3022119A1 (en) 2016-04-28 2017-11-02 Emory University Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto
WO2017222915A1 (en) 2016-06-21 2017-12-28 Inception 4, Inc. Heterocyclic prolinamide derivatives
BR112018076766A2 (pt) 2016-06-21 2019-04-02 Orion Ophthalmology LLC derivados de prolinamida alifática
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC CARBOCYCLIC PROLINAMIDE DERIVATIVES
CN109661389A (zh) * 2016-08-23 2019-04-19 豪夫迈·罗氏有限公司 作为htra1抑制剂的新型二氟酮酰胺衍生物
CN111194217B (zh) 2017-09-21 2024-01-12 里伯赛恩斯有限责任公司 作为hcv rna复制抑制剂的4’-氟-2’-甲基取代的核苷衍生物
CN109337537B (zh) * 2018-09-26 2022-10-25 河北晨阳工贸集团有限公司 一种起重机专用单组分水性面漆及其制备方法
CN110668538B (zh) * 2019-09-20 2021-10-22 济南大学 一种聚合氯化钛的制备方法
CN115960088B (zh) * 2020-07-31 2024-07-26 四川大学 一种新型冠状病毒主蛋白酶的抑制剂及其制备方法和用途
CN114057702B (zh) * 2020-07-31 2022-09-30 四川大学 一种新型冠状病毒主蛋白酶的抑制剂及其制备方法和用途
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
WO2023149981A1 (en) * 2022-02-07 2023-08-10 Purdue Research Foundation Compounds for the treatment of sars
CN114703003B (zh) * 2022-04-14 2023-04-28 上海绿晟环保科技有限公司 一种负载碳量子点的纳米材料润滑添加剂及其制备方法
CN115417790A (zh) * 2022-10-09 2022-12-02 山东大学 一类新型偶氮类发泡剂及合成方法
KR102829944B1 (ko) 2023-05-16 2025-07-03 최유성 하천 준설토 관리시스템

Family Cites Families (163)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3719667A (en) 1970-08-24 1973-03-06 Lilly Co Eli Epimerization of 6-acylamido and 6-imido penicillin sulfoxide esters
US3840556A (en) 1971-05-28 1974-10-08 Lilly Co Eli Penicillin conversion by halogen electrophiles and anti-bacterials derived thereby
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
FR2570695A1 (fr) * 1984-09-27 1986-03-28 Synthelabo Diphenylazomethines a chaine ramifiee ou cyclique, leur preparation et leur application en therapeutique
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
ATE71934T1 (de) * 1985-06-07 1992-02-15 Ici America Inc Selektionierte difluorverbindungen.
US4835168A (en) 1985-12-16 1989-05-30 Eli Lilly And Company Thiadiazole antiviral agents
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.
DE674513T1 (de) 1992-12-29 1996-01-18 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
RU95104898A (ru) 1994-03-31 1996-12-27 Бристоль-Мейерз Сквибб Компани (US) Имидазолсодержащие ингибиторы фарнезид-протеинтрансферазы, способ лечения связанных с ней заболеваний
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
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
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
JPH09124691A (ja) * 1995-08-25 1997-05-13 Green Cross Corp:The ペプチド化合物およびそれを含有する医薬組成物
JP2000500760A (ja) 1995-11-23 2000-01-25 メルク シヤープ エンド ドーム リミテツド スピロピペリジン誘導体およびタキキニン拮抗薬としてのその使用
US6054472A (en) 1996-04-23 2000-04-25 Vertex Pharmaceuticals, Incorporated Inhibitors of IMPDH enzyme
US5807876A (en) 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
ZA972195B (en) 1996-03-15 1998-09-14 Du Pont Merck Pharma Spirocycle integrin inhibitors
AU723730B2 (en) 1996-04-23 2000-09-07 Vertex Pharmaceuticals Incorporated Urea derivatives as inhibitors of IMPDH enzyme
US6127422A (en) 1996-05-06 2000-10-03 Eli Lilly And Company Anti-viral method
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
JPH11513890A (ja) 1996-05-10 1999-11-30 シェーリング コーポレイション C型肝炎ウイルスns3プロテアーゼの合成インヒビター
AU3073297A (en) 1996-05-17 1997-12-05 Data Card Corporation Curable topcoat composition and methods for use
US6245919B1 (en) * 1996-06-28 2001-06-12 Haruhiko Shinozaki Cyclopropylglycine derivatives and agonists for metabotronic L-glutamate receptors
WO1998000391A1 (en) * 1996-06-28 1998-01-08 Nippon Chemiphar Co., Ltd. Cyclopropylglycine derivatives and metabolic-regulation type l-glutamate receptor agonist
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
AU4898797A (en) 1996-10-08 1998-05-05 Colorado State University Research Foundation Catalytic asymmetric epoxidation
CN1133649C (zh) * 1996-10-18 2004-01-07 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蛋白酶的抑制剂
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
WO1998040381A1 (en) 1997-03-14 1998-09-17 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
EP1003775B1 (en) * 1997-08-11 2005-03-16 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor peptides
US6143715A (en) 1997-08-11 2000-11-07 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptide analogues
US6767991B1 (en) 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
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
EP1066247B1 (en) 1998-03-31 2006-11-22 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
US6518305B1 (en) * 1998-04-23 2003-02-11 Abbott Laboratories Five-membered carbocyclic and heterocyclic inhibitors of neuraminidases
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
AR022061A1 (es) * 1998-08-10 2002-09-04 Boehringer Ingelheim Ca Ltd Peptidos inhibidores de la hepatitis c, una composicion farmaceutica que los contiene, el uso de los mismos para preparar una composicion farmaceutica, el uso de un producto intermedio para la preparacion de estos peptidos y un procedimiento para la preparacion de un peptido analogo de los mismos.
DE19836514A1 (de) 1998-08-12 2000-02-17 Univ Stuttgart Modifikation von Engineeringpolymeren mit N-basischen Gruppe und mit Ionenaustauschergruppen in der Seitenkette
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
EP1027885B1 (en) 1999-02-09 2008-07-09 Pfizer Products Inc. Basic drug compositions with enhanced bioavailability
US20020042046A1 (en) 1999-02-25 2002-04-11 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
CN1196687C (zh) 1999-03-19 2005-04-13 沃泰克斯药物股份有限公司 Impdh酶抑制剂
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
WO2001040262A1 (en) 1999-12-03 2001-06-07 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
US6365380B2 (en) * 2000-02-23 2002-04-02 Pcbu Services, Inc. Method for stereoselectively inverting a chiral center of a chemical compound using an enzyme and a metal catalyst
US6699855B2 (en) 2000-02-29 2004-03-02 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
ATE297946T1 (de) 2000-04-03 2005-07-15 Vertex Pharma Inhibitoren von serin proteasen, speziell der hepatitis-c-virus ns3-protease
HK1047947A1 (zh) 2000-04-05 2003-03-14 Schering Corporation 包含n-环状p2部分的丙型肝炎病毒的大环ns3-丝氨酸蛋白酶抑制剂
PE20011288A1 (es) 2000-04-19 2001-12-12 Schering Corp Compuestos macrociclicos como inhibidores de la serina proteasa ns3/ns4 del virus de la hepatitis c (vhc)
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
CZ2003195A3 (cs) 2000-07-21 2003-04-16 Schering Corporation Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostředek
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
SI1385870T1 (sl) 2000-07-21 2010-08-31 Schering Corp Peptidi kot NS3-serin proteazni inhibitorji virusa hepatitisa C
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
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
WO2002060926A2 (en) 2000-11-20 2002-08-08 Bristol-Myers Squibb Company Hepatitis c tripeptide inhibitors
IL155842A0 (en) 2000-12-12 2003-12-23 Schering Corp Diaryl peptides as ns3-serine protease inhibitors of hepatitis c virus
US6653295B2 (en) 2000-12-13 2003-11-25 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
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
SK286630B6 (sk) 2001-01-22 2009-02-05 Merck & Co., Inc. Nukleozidové deriváty, farmaceutický prostriedok s ich obsahom a ich použitie
EP1356123A2 (en) 2001-01-30 2003-10-29 Vertex Pharmaceuticals Incorporated A quantitative assay for nucleic acids
GB0102342D0 (en) 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
CA2441688C (en) 2001-03-27 2014-01-21 Vertex Pharmaceuticals Incorporated Compositions and methods useful for hcv infection
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
EP1463699A2 (en) 2001-07-03 2004-10-06 ALTANA Pharma AG Process for the production of 3-phenylisoserine
DE60217114T2 (de) 2001-07-11 2007-10-25 Vertex Pharmaceuticals Inc., Cambridge Verbrückte bizyklische serinproteaseinhibitoren
US7029561B2 (en) 2001-07-25 2006-04-18 The United States Of America As Represented By The Secretary Of Commerce Fluidic temperature gradient focusing
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
KR20050044450A (ko) 2001-11-14 2005-05-12 테바 파마슈티컬 인더스트리즈 리미티드 로사르탄 칼륨의 무정형 및 결정형 형태 및 이의 제조 방법
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
US7091184B2 (en) 2002-02-01 2006-08-15 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
CA2369970A1 (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
PL373399A1 (en) 2002-04-11 2005-08-22 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
CA2494340C (en) 2002-08-01 2012-01-24 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
US20040180815A1 (en) 2003-03-07 2004-09-16 Suanne Nakajima Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
WO2004073599A2 (en) 2003-02-18 2004-09-02 Pfizer Inc. Inhibitors of hepatitis c virus, compositions and treatments using the same
CA2516016C (en) 2003-03-05 2012-05-29 Boehringer Ingelheim International Gmbh Hepatitis c inhibiting compounds
US6908901B2 (en) 2003-03-05 2005-06-21 Boehringer Ingelheim International, Gmbh Hepatitis C inhibitor peptide analogs
JP2006526011A (ja) 2003-04-11 2006-11-16 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ(特に、hcvns3−ns4aプロテアーゼ)のインヒビター
ES2297424T3 (es) 2003-05-21 2008-05-01 Boehringer Ingelheim International Gmbh Compuestos inhibidores de la hepatitis c.
CN102020700A (zh) 2003-07-18 2011-04-20 沃泰克斯药物股份有限公司 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂
WO2005018330A1 (en) 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
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
ES2361997T3 (es) 2003-09-22 2011-06-27 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos activos contra el virus de la hepatitis c.
KR20060130027A (ko) 2003-10-10 2006-12-18 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 hcv ns3-ns4a 프로테아제의억제제
US7365092B2 (en) 2003-10-10 2008-04-29 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
US7494660B2 (en) 2003-10-27 2009-02-24 Vertex Pharmaceuticals Incorporated HCV NS3-NS4A protease resistance mutants
EP1677827B1 (en) 2003-10-27 2008-12-10 Vertex Pharmaceuticals Incorporated Combinations for hcv treatment
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
CN1894211A (zh) 2003-10-28 2007-01-10 沃泰克斯药物股份有限公司 借助费歇尔-芬克型合成和随后的酰化制备4,5-二烷基-3-酰基-吡咯-2-羧酸衍生物
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
WO2005070955A1 (en) 2004-01-21 2005-08-04 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis c virus
CN1938332B (zh) 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂
SG184700A1 (en) 2004-02-20 2012-10-30 Boehringer Ingelheim Int Viral polymerase inhibitors
US20050187192A1 (en) 2004-02-20 2005-08-25 Kucera Pharmaceutical Company Phospholipids for the treatment of infection by togaviruses, herpes viruses and coronaviruses
US7342041B2 (en) 2004-02-27 2008-03-11 Schering Corporation 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease
CA2559303C (en) 2004-03-12 2013-09-10 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
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
EP1765283A4 (en) 2004-06-08 2012-11-28 Vertex Pharma PHARMACEUTICAL COMPOSITIONS
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
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
DE602006013492D1 (de) 2005-08-19 2010-05-20 Vertex Pharma Verfahren und zwischenprodukte
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
US8039475B2 (en) 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
KR20080112303A (ko) 2006-03-16 2008-12-24 버텍스 파마슈티칼스 인코포레이티드 중수소화 c형 간염 프로테아제 억제제
NZ571281A (en) 2006-03-16 2011-11-25 Vertex Pharma Processes and intermediates for preparing steric compounds
US20070218138A1 (en) 2006-03-20 2007-09-20 Bittorf Kevin J Pharmaceutical Compositions
NZ571934A (en) 2006-03-20 2012-05-25 Vertex Pharma Methods of spray drying formulations of vx-950 (telaprevir)
ATE481089T1 (de) 2006-05-31 2010-10-15 Vertex Pharma Orale formulierungen mit kontrollierter freisetzung eines interleukin-1-beta-converting- enzyme inhibitors
EP2134717A2 (en) 2007-02-27 2009-12-23 Vertex Pharmceuticals Incorporated Inhibitors of serine proteases

Also Published As

Publication number Publication date
EP2368877B1 (en) 2014-05-07
HK1057758A1 (en) 2004-04-16
KR100968295B1 (ko) 2010-07-07
LU91960I2 (fr) 2012-05-21
PL211019B1 (pl) 2012-03-30
CN102504014A (zh) 2012-06-20
KR100876472B1 (ko) 2008-12-31
WO2002018369A3 (en) 2002-08-15
ES2325481T3 (es) 2009-09-07
ES2489115T3 (es) 2014-09-01
JP4689938B2 (ja) 2011-06-01
TW201022244A (en) 2010-06-16
ATE431358T1 (de) 2009-05-15
NZ541302A (en) 2007-04-27
PL365836A1 (en) 2005-01-10
DE20122915U1 (de) 2010-04-08
JP2007284444A (ja) 2007-11-01
EP1320540B1 (en) 2009-05-13
PT1320540E (pt) 2009-07-14
BR0113666A (pt) 2005-09-27
US8529882B2 (en) 2013-09-10
IL215892A0 (en) 2011-12-29
EP1878720B1 (en) 2010-10-06
NO2012006I1 (no) 2012-04-30
EP2368878A1 (en) 2011-09-28
CN101633636A (zh) 2010-01-27
HUP0300855A3 (en) 2012-01-30
TW201022241A (en) 2010-06-16
TW201022242A (en) 2010-06-16
TWI359145B (en) 2012-03-01
EP2371839A1 (en) 2011-10-05
JP2012197289A (ja) 2012-10-18
TW201022243A (en) 2010-06-16
TWI339661B (en) 2011-04-01
IL215892A (en) 2015-03-31
CY1109216T1 (el) 2014-07-02
CZ2003595A3 (cs) 2003-06-18
AR030591A1 (es) 2003-08-27
CN100522991C (zh) 2009-08-05
AU2001288318C1 (en) 2002-03-13
TWI319763B (en) 2010-01-21
DK1320540T3 (da) 2009-07-27
NO2012006I2 (no) 2012-04-03
CN1869061B (zh) 2013-04-24
HRP20030139A2 (en) 2005-04-30
CN101633636B (zh) 2013-03-13
NZ569670A (en) 2010-03-26
CY2012007I1 (el) 2014-07-02
US8252923B2 (en) 2012-08-28
EP2368901A1 (en) 2011-09-28
NO330807B1 (no) 2011-07-18
IL215891A (en) 2015-04-30
KR100945975B1 (ko) 2010-03-09
US20050197299A1 (en) 2005-09-08
DZ3438A1 (fr) 2002-03-07
IL154671A (en) 2011-11-30
KR20080104384A (ko) 2008-12-02
KR20090120013A (ko) 2009-11-23
CA2419607A1 (en) 2002-03-07
NO20100999L (no) 2003-04-16
CA2697205C (en) 2014-07-29
ES2325481T9 (es) 2012-07-10
CN1869061A (zh) 2006-11-29
EP1320540B9 (en) 2012-03-21
JP2011079835A (ja) 2011-04-21
US20100137583A1 (en) 2010-06-03
EA200701869A1 (ru) 2008-02-28
ES2352804T3 (es) 2011-02-23
DE122012000015I1 (de) 2012-05-24
CA2419607C (en) 2012-03-13
IL215891A0 (en) 2011-12-29
SK2492003A3 (en) 2004-11-03
EA017556B1 (ru) 2013-01-30
EP1849797A2 (en) 2007-10-31
KR20080096718A (ko) 2008-10-31
SI1320540T1 (sl) 2009-10-31
NO20030928L (no) 2003-04-16
DK1320540T5 (da) 2012-05-29
NO20030928D0 (no) 2003-02-27
TWI359144B (en) 2012-03-01
KR20110088600A (ko) 2011-08-03
AU2001288318B2 (en) 2007-09-06
PE20020474A1 (es) 2002-06-18
WO2002018369A8 (en) 2003-11-06
ES2450815T3 (es) 2014-03-25
HRP20030139B1 (hr) 2015-08-28
EP1849797A3 (en) 2008-01-23
CN101693672A (zh) 2010-04-14
IL215890A0 (en) 2011-12-29
HUP0300855A2 (hu) 2003-10-28
UA99895C2 (uk) 2012-10-25
US20120064034A1 (en) 2012-03-15
EP2368877A1 (en) 2011-09-28
HRP20030139B8 (hr) 2015-11-06
EA200300318A1 (ru) 2004-02-26
HK1163061A1 (en) 2012-09-07
SV2003000617A (es) 2003-01-13
KR20080007515A (ko) 2008-01-21
ATE483686T1 (de) 2010-10-15
NO20100093L (no) 2003-04-16
ZA200301641B (en) 2004-06-21
CY2012007I2 (el) 2014-07-02
EP1320540A2 (en) 2003-06-25
ECSP077217A (es) 2007-04-26
EP1878720A1 (en) 2008-01-16
EP1958956A3 (en) 2008-09-24
TWI378927B (en) 2012-12-11
IL154671A0 (en) 2003-09-17
EP1876173A1 (en) 2008-01-09
EA011547B1 (ru) 2009-04-28
NO329929B1 (no) 2011-01-24
CN103232381A (zh) 2013-08-07
CN101696232A (zh) 2010-04-21
US20120282219A1 (en) 2012-11-08
CA2697205A1 (en) 2002-03-07
KR20100042296A (ko) 2010-04-23
KR20030041981A (ko) 2003-05-27
KR20100043293A (ko) 2010-04-28
WO2002018369A2 (en) 2002-03-07
KR20080104382A (ko) 2008-12-02
CL2010000330A1 (es) 2010-09-21
JP2004517047A (ja) 2004-06-10
KR20080104383A (ko) 2008-12-02
JP5269035B2 (ja) 2013-08-21
CN1451014A (zh) 2003-10-22
IL185644A0 (en) 2008-01-06
CN101693672B (zh) 2014-11-12
ECSP034493A (es) 2003-04-25
AU8831801A (en) 2002-03-13
MXPA03001780A (es) 2003-06-04
EP1958956A2 (en) 2008-08-20
DE60143233D1 (de) 2010-11-18
US20140294763A1 (en) 2014-10-02
EP1958956B1 (en) 2013-12-11
DK1878720T3 (da) 2011-01-24
US7820671B2 (en) 2010-10-26
HK1114090A1 (en) 2008-10-24
DE60138717D1 (de) 2009-06-25
TW200918523A (en) 2009-05-01

Similar Documents

Publication Publication Date Title
UA81600C2 (en) Peptidomimetic protease inhibitors
AU2012201015B2 (en) Peptidomimetic protease inhibitors
AU2007240156B2 (en) Peptidomimetic protease inhibitors
HK1115886A (en) Peptidomimetic protease inhibitors
HK1115886B (en) Peptidomimetic protease inhibitors
HK1114088A (en) Chiral intermediates for the preparation of peptidomimetic protease inhibitors
HK1163061B (en) Peptidomimetic protease inhibitors and intermediates for their preparation as treatment for hcv infection
HK1108700A (en) Peptidomimetic protease inhibitors
HK1163112A (en) Peptidomimetic protease inhibitors
HK1114090B (en) Process for preparing chiral bicycloprolinates as intermediates for the preparation of peptidomimetic protease inhibitors
HK1057758B (en) Peptidomimetic protease inhibitors
HK1163062A (en) Peptidomimetic protease inhibitors