TWI319763B - Peptidomimetic protease inhibitors - Google Patents

Peptidomimetic protease inhibitors

Info

Publication number
TWI319763B
TWI319763B TW090121629A TW90121629A TWI319763B TW I319763 B TWI319763 B TW I319763B TW 090121629 A TW090121629 A TW 090121629A TW 90121629 A TW90121629 A TW 90121629A TW I319763 B TWI319763 B TW I319763B
Authority
TW
Taiwan
Prior art keywords
protease inhibitors
peptidomimetic protease
peptidomimetic
inhibitors
protease
Prior art date
Application number
TW090121629A
Other languages
English (en)
Chinese (zh)
Inventor
Edward Babine Orbert
Hui Chen Shu
Nmn Collado Ivan
Nmn Garcia-Paredes Cristina
Irvin Glass John
Nmn Jin Ling
Eric Lamar Jason
Samuel Parker Raymond Iii
June Snyder Nancy
David Sun Xicheng
Joseph Tebbe Mark
Victor Frantz
May Wang Q
Yee Mai Yip Yvonne
Guo Edqi
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=TWI319763(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed filed Critical
Application granted granted Critical
Publication of TWI319763B publication Critical patent/TWI319763B/zh

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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (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)
TW090121629A 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors TWI319763B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22939800P 2000-08-31 2000-08-31
US27764101P 2001-03-21 2001-03-21

Publications (1)

Publication Number Publication Date
TWI319763B true TWI319763B (en) 2010-01-21

Family

ID=26923261

Family Applications (6)

Application Number Title Priority Date Filing Date
TW099107492A TWI359145B (en) 2000-08-31 2001-08-31 Process for preparing intermediates of peptidomime
TW099107489A TWI378927B (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors
TW090121629A TWI319763B (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors
TW097127487A TWI339661B (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors
TW099107488A TWI359144B (en) 2000-08-31 2001-08-31 Intermediates of peptidomimetic protease inhibitor
TW099107493A TW201022244A (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors

Family Applications Before (2)

Application Number Title Priority Date Filing Date
TW099107492A TWI359145B (en) 2000-08-31 2001-08-31 Process for preparing intermediates of peptidomime
TW099107489A TWI378927B (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors

Family Applications After (3)

Application Number Title Priority Date Filing Date
TW097127487A TWI339661B (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors
TW099107488A TWI359144B (en) 2000-08-31 2001-08-31 Intermediates of peptidomimetic protease inhibitor
TW099107493A TW201022244A (en) 2000-08-31 2001-08-31 Peptidomimetic protease inhibitors

Country Status (36)

Country Link
US (5) US7820671B2 (enExample)
EP (9) EP2368901A1 (enExample)
JP (4) JP4689938B2 (enExample)
KR (10) KR20100042296A (enExample)
CN (7) CN102504014A (enExample)
AR (1) AR030591A1 (enExample)
AT (2) ATE431358T1 (enExample)
AU (2) AU8831801A (enExample)
BR (1) BR0113666A (enExample)
CA (2) CA2419607C (enExample)
CL (1) CL2010000330A1 (enExample)
CY (2) CY1109216T1 (enExample)
CZ (1) CZ2003595A3 (enExample)
DE (4) DE60143233D1 (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) NZ541302A (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) TWI359145B (enExample)
UA (2) UA81600C2 (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
JP4080541B2 (ja) * 1996-10-18 2008-04-23 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
IL152022A0 (en) * 2000-04-03 2003-04-10 Vertex Pharma Compounds useful as protease inhibitors and pharmaceutical compositions containing the same
MY164523A (en) 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
IL153020A0 (en) 2000-05-26 2003-06-24 Idenix Cayman Ltd Methods and compositions for treating flaviviruses and pestiviruses
CN102372764A (zh) 2000-07-21 2012-03-14 先灵公司 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
RU2003105221A (ru) 2000-07-21 2004-09-20 Шеринг Корпорейшн (US) Новые пептиды, как ингибиторы ns3-серинпротеазы вируса гепатита с
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
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
MXPA04003825A (es) * 2001-10-24 2004-07-08 Vertex Pharma Inhibidores de serina proteasa, en particular la ns3-ns4a proteasa del virus de hepatitis c, que incorpora un sistema de anillo fusionado.
US7119072B2 (en) 2002-01-30 2006-10-10 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis C virus
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
MXPA04009938A (es) * 2002-04-11 2004-12-13 Vertex Pharma Inhibidores de serina proteasas, en particular la proteasa ns3-ns4a del hcv.
ATE503764T1 (de) * 2002-05-20 2011-04-15 Bristol Myers Squibb Co Inhibitoren des hepatitis-c-virus
US7608600B2 (en) 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
EP1523489B1 (en) 2002-06-28 2014-03-12 IDENIX Pharmaceuticals, Inc. Modified 2' and 3' -nucleoside produgs for treating flaviridae 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
DE60331367D1 (de) 2002-12-30 2010-04-01 Angiotech Int Ag Wirkstofffreisetzung von schnell gelierender polymerzusammensetzung
AU2011203054B2 (en) * 2003-04-11 2012-04-26 Vertex Pharmaceuticals, Incorporated Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease
EP1613620A1 (en) * 2003-04-11 2006-01-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US20050090450A1 (en) * 2003-04-11 2005-04-28 Farmer Luc J. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
WO2004103996A1 (en) 2003-05-21 2004-12-02 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor compounds
ES2906207T3 (es) 2003-05-30 2022-04-13 Gilead Pharmasset Llc Análogos de nucleósidos fluorados modificados
US7109172B2 (en) 2003-07-18 2006-09-19 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
TWI359147B (en) 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
US20050120398A1 (en) * 2003-09-12 2005-06-02 Vertex Pharmaceuticals Incorporated Animal model for HCV infection
US20050119189A1 (en) 2003-09-18 2005-06-02 Cottrell Kevin M. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
ATE500264T1 (de) 2003-09-22 2011-03-15 Boehringer Ingelheim Int Makrozyklische peptide mit wirkung gegen das hepatitis-c-virus
KR20060130027A (ko) 2003-10-10 2006-12-18 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 hcv ns3-ns4a 프로테아제의억제제
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
KR20060120162A (ko) * 2003-10-27 2006-11-24 버텍스 파마슈티칼스 인코포레이티드 Hcv 치료용 배합물
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
CN1894276B (zh) 2003-10-27 2010-06-16 威特克斯医药股份有限公司 Hcv ns3-ns4a蛋白酶抗药性突变体
WO2005043118A2 (en) 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Drug discovery method
JP2007513971A (ja) * 2003-12-11 2007-05-31 シェーリング コーポレイション C型肝炎ウイルスns3/ns4aプロテアーゼの阻害剤
DE602005025855D1 (de) 2004-01-21 2011-02-24 Boehringer Ingelheim Pharma Makrocyclische peptide mit wirkung gegen das hepatitis-c-virus
EP1711515A2 (en) * 2004-02-04 2006-10-18 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
ATE438622T1 (de) * 2004-02-27 2009-08-15 Schering Corp 3,4-(cyclopentyl)kondensierte prolinverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
AR048241A1 (es) * 2004-02-27 2006-04-12 Schering Corp Compuestos azufrados como inhibidores de la serina proteasa ns3 del virus de la hepatitis c .
US7205330B2 (en) 2004-02-27 2007-04-17 Schering Corporation Inhibitors of hepatitis C virus NS3 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
CN102512372A (zh) * 2004-06-08 2012-06-27 沃泰克斯药物股份有限公司 药物组合物
UY29016A1 (es) 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
ES2366478T3 (es) 2004-07-20 2011-10-20 Boehringer Ingelheim International Gmbh Análogos peptídicos inhibidores de la hepatitis c.
MX2007003812A (es) * 2004-10-01 2007-05-24 Vertex Pharma Inhibicion de proteasa ns3-ns4a del virus de la hepatitis c (vhc).
TWI437990B (zh) * 2004-10-29 2014-05-21 Vertex Pharma Vx-950之醫藥用途
US7488848B2 (en) 2005-03-21 2009-02-10 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
EP2546246A3 (en) 2005-05-13 2013-04-24 Virochem Pharma Inc. Compounds and methods for the treatment or prevention of flavivirus infections
US20060276404A1 (en) * 2005-06-02 2006-12-07 Anima Ghosal Medicaments and methods combining a HCV protease inhibitor and an AKR competitor
US8119602B2 (en) 2005-06-02 2012-02-21 Schering Corporation Administration of HCV protease inhibitors in combination with food to improve bioavailability
WO2006130553A2 (en) * 2005-06-02 2006-12-07 Schering Corporation Hcv protease inhibitors
CA2611155A1 (en) 2005-06-02 2006-12-07 Schering Corporation Pharmaceutical formulations and methods of treatment using the same
US7608592B2 (en) 2005-06-30 2009-10-27 Virobay, Inc. HCV inhibitors
MY139988A (en) 2005-07-29 2009-11-30 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis c virus
ATE524475T1 (de) 2005-07-29 2011-09-15 Tibotec Pharm Ltd Makrocyclische inhibitoren des hepatitis-c-virus
JP5230414B2 (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環状阻害剤
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de hepatitis c
MY142972A (en) 2005-07-29 2011-01-31 Tibotec Pharm Ltd Macrocyclic inhibitors of hepatitis c virus
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
JO2768B1 (en) 2005-07-29 2014-03-15 تيبوتيك فارماسيوتيكالز ليمتد Large cyclic inhibitors of hepatitis C virus
EA013475B1 (ru) 2005-07-29 2010-04-30 Тиботек Фармасьютикалз Лтд. Макроциклические ингибиторы вируса гепатита с
CA2617679A1 (en) 2005-08-02 2007-02-08 Steve Lyons Inhibitors of serine proteases
NZ593214A (en) 2005-08-19 2013-02-22 Vertex Pharma Compounds and Processes for preparing serine protease inhibitors
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
CA2629343A1 (en) 2005-11-11 2007-05-24 Vertex Pharmaceuticals, Inc. Hepatitis c virus variants
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
ATE509941T1 (de) * 2006-01-11 2011-06-15 Seikagaku Kogyo Co Ltd Cycloalkylcarbonylaminosäureester-derivat und herstellungsverfahren dafür
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
US8183413B2 (en) 2006-01-20 2012-05-22 Kaneka Corporation Process for production of β-amino-α-hydroxy carboxamide derivative
WO2007098270A2 (en) * 2006-02-27 2007-08-30 Vertex Pharmaceuticals Incorporated Co-crystals comprising vx-950 and pharmaceutical compositions comprising the same
EP2007381A4 (en) * 2006-03-06 2010-11-17 Abbott Lab COMPOSITIONS AND METHODS OF USING RITONAVIR FOR THE TREATMENT OF HEPATITIS C VIRUS
BRPI0709568A2 (pt) 2006-03-16 2011-07-12 Vertex Pharmaceuticals Incorporarted processos e intermediários para preparar compostos estéricos
JP2009531315A (ja) 2006-03-16 2009-09-03 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 重水素化c型肝炎プロテアーゼインヒビター
JP2009530416A (ja) 2006-03-20 2009-08-27 バーテックス ファーマシューティカルズ インコーポレイテッド 医薬組成物
CA2647158C (en) * 2006-03-23 2012-07-31 Schering Corporation Combinations of hcv protease inhibitor(s) and cyp3a4 inhibitor(s), and methods of treatment related thereto
NZ571826A (en) 2006-04-11 2012-01-12 Novartis Ag HCV/HIV inhibitors and their uses
WO2007120595A2 (en) * 2006-04-11 2007-10-25 Novartis Ag Amines for the treatment of hcv
MX2008014839A (es) 2006-05-23 2008-12-05 Irm Llc Compuestos y composiciones en la forma de inhibidores de proteasa de activacion mediante canal.
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
AU2007321677B2 (en) 2006-11-15 2013-04-11 Vertex Pharmaceuticals (Canada) Incorporated Thiophene analogues for the treatment or prevention of flavivirus infections
JP2010510192A (ja) 2006-11-17 2010-04-02 テイボテク・フアーマシユーチカルズ・リミテツド C型肝炎ウイルスの大環状阻害剤
EP2428204A3 (en) 2006-12-07 2012-07-04 Schering Corporation pH sensitive matrix formulation
WO2008074035A1 (en) * 2006-12-27 2008-06-19 Abbott Laboratories Hcv protease inhibitors and uses thereof
US20080207528A1 (en) * 2007-02-01 2008-08-28 Syaulan Yang Hcv protease inhibitors
ES2541660T3 (es) 2007-02-08 2015-07-23 Janssen Sciences Ireland Uc Inhibidores del VHC macrocíclicos sustituidos con pirimidina
AU2008214217B2 (en) 2007-02-09 2011-10-13 Irm Llc Compounds and compositions as channel activating protease inhibitors
WO2008106058A2 (en) 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
EP2463284A1 (en) 2007-02-27 2012-06-13 Vertex Pharmceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
WO2008127613A1 (en) * 2007-04-11 2008-10-23 Scynexis, Inc. New pharmaceutical compositions
JP2010526143A (ja) 2007-05-04 2010-07-29 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 Hcv感染の処置のための併用療法
WO2009018609A1 (en) * 2007-08-03 2009-02-12 Biotrom Limited Hepatitis c antiviral compositions and methods
AU2008297015B2 (en) 2007-08-30 2013-08-22 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
PT2061513E (pt) 2007-09-14 2011-10-17 Schering Corp Método para tratar doentes com hepatite c
US20090082366A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched telaprevir
EP2205584A1 (en) 2007-10-10 2010-07-14 Novartis Ag Spiropyrrolidines and their use against hcv and hiv infection
EP2215076A4 (en) 2007-10-24 2012-05-02 Virobay Inc COMPOUNDS CAPABLE OF INHIBITING CATHEPSIN S PROTEASE AND HCV REPLICATION
WO2009055335A2 (en) * 2007-10-25 2009-04-30 Taigen Biotechnology Co., Ltd. Hcv protease inhibitors
BRPI0821836A2 (pt) 2007-12-24 2015-06-16 Tibotec Pharm Ltd Indóis macrocíclicos como inibidores do vírus da hepatite c
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
EP2307419B1 (en) 2008-06-24 2013-11-06 Codexis, Inc. Biocatalytic processes for the preparation of substantially stereomerically pure fused bicyclic proline compounds
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
AU2009322393B2 (en) 2008-12-03 2017-02-02 Presidio Pharmaceuticals, Inc. Inhibitors of HCV NS5A
AU2009322400A1 (en) 2008-12-03 2011-06-30 Presidio Pharmaceuticals, Inc. Inhibitors of HCV NS5A
GB0900914D0 (en) 2009-01-20 2009-03-04 Angeletti P Ist Richerche Bio Antiviral agents
JP2012517478A (ja) 2009-02-12 2012-08-02 バーテックス ファーマシューティカルズ インコーポレイテッド ペグ化インターフェロン、リバビリンおよびテラプレビルを含む、hcv組合せ治療剤
JP5735482B2 (ja) 2009-03-27 2015-06-17 プレシディオ ファーマシューティカルズ インコーポレイテッド 縮合環のc型肝炎阻害剤
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
US20100324059A1 (en) 2009-06-23 2010-12-23 Gilead Sciences, Inc. Pharmaceutical compositions useful for treating hcv
CA2774145C (en) * 2009-09-15 2015-10-27 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
JP2013512247A (ja) 2009-11-25 2013-04-11 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 フラビウイルス感染症の治療または予防のための5−アルキニル−チオフェン−2−カルボン酸誘導体およびそれらの使用
CA2784748A1 (en) * 2009-12-18 2011-06-23 Idenix Pharmaceuticals, Inc. 5,5-fused arylene or heteroarylene hepatitis c virus inhibitors
SG181614A1 (en) 2009-12-24 2012-07-30 Vertex Pharma Analogues for the treatment or prevention of flavivirus infections
US20110178107A1 (en) * 2010-01-20 2011-07-21 Taigen Biotechnology Co., Ltd. Hcv protease inhibitors
EP2528922B1 (en) 2010-01-27 2017-08-02 AB Pharma Ltd Polyheterocyclic compounds 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
JP2013522375A (ja) 2010-03-24 2013-06-13 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 フラビウイルス感染を処置または予防するためのアナログ
EP2550268A1 (en) 2010-03-24 2013-01-30 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
CN103038237A (zh) 2010-03-24 2013-04-10 沃泰克斯药物股份有限公司 用于黄病毒感染治疗或预防的类似物
TW201139438A (en) 2010-03-24 2011-11-16 Vertex Pharma Analogues for the treatment or prevention of flavivirus infections
MX2012011222A (es) 2010-04-01 2013-01-18 Centre Nat Rech Scient Compuestos y composiciones farmaceuticas para el tratamiento de infecciones virales.
CA2800509A1 (en) 2010-05-24 2011-12-01 Presidio Pharmaceuticals, Inc. Inhibitors of hcv ns5a
KR20130082137A (ko) 2010-06-03 2013-07-18 버텍스 파마슈티칼스 인코포레이티드 방법 및 중간체
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
WO2012006060A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
WO2012006070A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
MX2012014918A (es) 2010-06-28 2013-04-08 Vertex Pharma Compuestos y metodos para tratamiento o prevencion de infecciones por flavivirus.
EP2593105A1 (en) 2010-07-14 2013-05-22 Vertex Pharmaceuticals Incorporated Palatable pharmaceutical composition comprising vx-950
AR082619A1 (es) 2010-08-13 2012-12-19 Hoffmann La Roche Inhibidores del virus de la hepatitis c
WO2012024363A2 (en) 2010-08-17 2012-02-23 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flaviviridae viral infections
WO2012040127A1 (en) 2010-09-22 2012-03-29 Alios Biopharma, Inc. Substituted nucleotide analogs
AU2011311880B2 (en) 2010-10-08 2014-07-24 Novartis Ag Vitamin E formulations of sulfamide NS3 inhibitors
WO2012054870A2 (en) 2010-10-21 2012-04-26 Vertex Pharmaceuticals Incorporated Biomarkers for hcv infected patients
WO2012058125A1 (en) 2010-10-26 2012-05-03 Presidio Pharmaceuticals, Inc. Inhibitors of hepatitis c virus
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
CN103842369A (zh) 2011-03-31 2014-06-04 埃迪尼克斯医药公司 用于治疗病毒感染的化合物和药物组合物
US8680152B2 (en) 2011-05-02 2014-03-25 Virobay, Inc. Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain
CN103814001A (zh) 2011-05-13 2014-05-21 弗特克斯药品有限公司 方法和中间体
AU2012269643A1 (en) 2011-06-16 2014-02-06 AB Pharma Ltd. Macrocyclic heterocyclic compound for inhibiting hepatitis C virus and preparation and use thereof
CN103732242A (zh) 2011-06-23 2014-04-16 迪格纳生物技术公司 用与IFN-α2b组合的IFN-α5在患者群体中治疗慢性丙型肝炎
US20120328565A1 (en) 2011-06-24 2012-12-27 Brinkman John A Antiviral compounds
WO2013016499A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Methods for preparation of thiophene compounds
AR087346A1 (es) 2011-07-26 2014-03-19 Vertex Pharma Formulaciones de compuestos de tiofeno
US8951985B2 (en) 2011-09-12 2015-02-10 Idenix Pharmaceuticals, Inc. Compounds and pharmaceutical compositions for the treatment of viral infections
CA2850003C (en) 2011-09-27 2020-01-07 Kansas State University Research Foundation Broad-spectrum antivirals against 3c or 3c-like proteases of picornavirus-like supercluster: picornaviruses, caliciviruses and coronaviruses
EP2766365A1 (en) 2011-10-10 2014-08-20 F.Hoffmann-La Roche Ag Antiviral compounds
IN2014CN02806A (enExample) 2011-10-14 2015-07-03 Bristol Myers Squibb Co
EP2766347B1 (en) 2011-10-14 2016-05-04 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
AU2012322085B2 (en) 2011-10-14 2017-05-04 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor Xia inhibitors
US8492386B2 (en) 2011-10-21 2013-07-23 Abbvie Inc. Methods for treating HCV
CN104023726A (zh) 2011-10-21 2014-09-03 艾伯维公司 用于治疗hcv的一种或多种daa的联合治疗(例如,与abt-072或abt-333)
GB2506086A (en) 2011-10-21 2014-03-19 Abbvie Inc Methods for treating HCV comprising at least two direct acting antiviral agent, ribavirin but not interferon
US8466159B2 (en) 2011-10-21 2013-06-18 Abbvie Inc. Methods for treating HCV
ES2564906T3 (es) 2011-12-16 2016-03-29 F. Hoffmann-La Roche Ag Inhibidores de NS5A del VHC
JP5982007B2 (ja) 2011-12-20 2016-08-31 リボサイエンス・エルエルシー Hcvrna複製の阻害薬としての2’,4’−ジフルオロ−2’−メチル置換されたヌクレオシド誘導体
WO2013092447A1 (en) 2011-12-20 2013-06-27 F. Hoffmann-La Roche Ag 4'-azido, 3'-fluoro substituted nucleoside derivatives as inhibitors of hcv rna replication
US9126986B2 (en) 2011-12-28 2015-09-08 Janssen Sciences Ireland Uc Hetero-bicyclic derivatives as HCV inhibitors
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
EP2814807A4 (en) * 2012-02-16 2015-10-07 Rqx Pharmaceuticals Inc LINEAR PEPTIDANTIBIOTICS
CA2857262A1 (en) 2012-02-24 2013-08-29 F. Hoffmann-La Roche Ag Antiviral compounds
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
WO2013136265A1 (en) 2012-03-13 2013-09-19 Dipharma Francis S.R.L. Synthesis of an intermediate of an antiviral compound
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
HK1206362A1 (zh) 2012-03-21 2016-01-08 Alios Biopharma, Inc. 硫代氨基磷酸酯核苷酸前藥的固體形式
NZ630805A (en) 2012-03-22 2016-01-29 Alios Biopharma Inc Pharmaceutical combinations comprising a thionucleotide analog
EP2844249A4 (en) 2012-05-02 2016-03-09 Univ Kansas State MACROCYCLIC AND PEPTIDOMIMETIC COMPOUNDS AS VIRUZIDES AGAINST 3C OR 3C LIKE PROTEASES OF PICORNIVERS, CALICIVIRES AND CORONA VIRUSES
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
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
AR091192A1 (es) 2012-05-30 2015-01-21 Chemo Iberica Sa Procedimiento multicomponente para la preparacion de compuestos biciclicos
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
LT2906551T (lt) 2012-10-12 2018-04-25 Bristol-Myers Squibb Company Faktoriaus xia kristalinės formos
WO2014059214A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014059202A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
JP2015536940A (ja) 2012-10-29 2015-12-24 シプラ・リミテッド 抗ウイルス性ホスホネート類似体及びその製造方法
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
MX2015009176A (es) 2013-01-23 2015-11-09 Hoffmann La Roche Derivados de triazola antivirales.
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
TW201526899A (zh) 2013-02-28 2015-07-16 Alios Biopharma Inc 醫藥組成物
CA2900319A1 (en) 2013-03-05 2014-09-12 F. Hoffmann-La Roche Ag Antiviral compounds
CN105228996B (zh) 2013-03-25 2017-11-28 百时美施贵宝公司 作为因子XIa抑制剂的含取代唑类的四氢异喹啉
ITMI20130706A1 (it) 2013-04-30 2014-10-31 Dipharma Francis Srl Procedimento per la preparazione di un inibitore delle proteasi virali e suoi intermedi
BR112015028764B1 (pt) 2013-05-16 2022-09-27 Riboscience Llc Derivados de nucleosídeo de 4-fluoro-2-metil substituídos como inibidores de replicação de rna do hcv
US20180200280A1 (en) 2013-05-16 2018-07-19 Riboscience Llc 4'-Fluoro-2'-Methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication
US9249176B2 (en) 2013-05-16 2016-02-02 Riboscience Llc 4′-azido, 3′-deoxy-3′-fluoro 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
WO2014203208A1 (en) 2013-06-21 2014-12-24 Ranbaxy Laboratories Limited Process for the preparation of telaprevir and intermediates thereof
WO2014203224A1 (en) 2013-06-21 2014-12-24 Ranbaxy Laboratories Limited Process for the preparation of telaprevir and its intermediates
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
NO2760821T3 (enExample) 2014-01-31 2018-03-10
NZ761182A (en) 2014-01-31 2023-04-28 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2’ groups as factor xia inhibitors
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
US10240427B2 (en) 2014-07-07 2019-03-26 Halliburton Energy Services, Inc. Downhole tools comprising aqueous-degradable sealing elements
US10081623B2 (en) 2014-09-04 2018-09-25 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
EP3423469A1 (en) 2016-03-04 2019-01-09 H. Hoffnabb-La Roche Ag New trifluoromethylpropanamide derivatives as htra1 inhibitors
EP3423467B1 (en) 2016-03-04 2021-04-28 F. Hoffmann-La Roche AG New difluoroketamide derivatives as htra1 inhibitors
US11192914B2 (en) 2016-04-28 2021-12-07 Emory University Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto
WO2017222914A1 (en) 2016-06-21 2017-12-28 Inception 4, Inc. Carbocyclic prolinamide derivatives
KR102595723B1 (ko) 2016-06-21 2023-10-27 오리온 옵탈몰로지 엘엘씨 헤테로시클릭 프롤린아미드 유도체
UA123836C2 (uk) * 2016-06-21 2021-06-09 Оріон Офтальмолоджі Ллс Аліфатичні похідні пролінаміду
JP2019526563A (ja) * 2016-08-23 2019-09-19 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Htra1阻害剤としての新規ジフルオロケタミド誘導体
KR102735678B1 (ko) 2017-09-21 2024-11-27 리보사이언스 엘엘씨 Hcv rna 복제의 억제제로서 4'-플루오로-2'-메틸 치환된 뉴클레오시드 유도체
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
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
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
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
EP0204571B1 (en) * 1985-06-07 1992-01-22 Ici Americas Inc. Selected difluoro derivatives
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
DE69329544T2 (de) 1992-12-22 2001-05-31 Eli Lilly And Co., Indianapolis HIV Protease hemmende Verbindungen
ES2189721T3 (es) 1992-12-29 2003-07-16 Abbott Lab Inhibidores de proteasa retroviral.
US5384410A (en) 1993-03-24 1995-01-24 The Du Pont Merck Pharmaceutical Company Removal of boronic acid protecting groups by transesterification
US5656600A (en) * 1993-03-25 1997-08-12 Corvas International, Inc. α-ketoamide derivatives as inhibitors of thrombosis
US5672582A (en) 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
IL110752A (en) 1993-09-13 2000-07-26 Abbott Lab Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor
US5559158A (en) 1993-10-01 1996-09-24 Abbott Laboratories Pharmaceutical composition
US5468858A (en) 1993-10-28 1995-11-21 The Board Of Regents Of Oklahoma State University Physical Sciences N-alkyl and n-acyl derivatives of 3,7-diazabicyclo-[3.3.1]nonanes and selected salts thereof as multi-class antiarrhythmic agents
IL111991A (en) 1994-01-28 2000-07-26 Abbott Lab Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent
HUT72440A (en) 1994-03-31 1996-04-29 Bristol Myers Squibb Co Imidazole-containing inhibitors of farnesyl protein transferase and pharmaceutical compositions containing them
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5861267A (en) 1995-05-01 1999-01-19 Vertex Pharmaceuticals Incorporated Methods, nucleotide sequences and host cells for assaying exogenous and endogenous protease activity
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
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
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
IL126674A (en) 1996-04-23 2005-08-31 Vertex Pharma Use of cyclic and heterocyclic compounds for preparing pharmaceutical compositions inhibiting impdh activity, pharmaceutical compositions containing the same and novel thiazole and oxazole urea derivatives
US6127422A (en) 1996-05-06 2000-10-03 Eli Lilly And Company Anti-viral method
EP0907659A1 (en) 1996-05-10 1999-04-14 Schering Corporation Synthetic inhibitors of hepatitis c virus ns3 protease
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
CN1218479A (zh) 1996-05-17 1999-06-02 咨询卡有限公司 可固化的表面涂层组合物及其使用方法
US6245919B1 (en) 1996-06-28 2001-06-12 Haruhiko Shinozaki Cyclopropylglycine derivatives and agonists for metabotronic L-glutamate receptors
EP0913389A4 (en) * 1996-06-28 2000-02-02 Nippon Chemiphar Co CYCLOPROPYLGLYCINE DERIVATIVES AND AGONISTS OF THE L-GLUTAMATE RECEPTOR TYPE OF METABOLITE REGULATION
US6153579A (en) 1996-09-12 2000-11-28 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
DE69735482T2 (de) 1996-09-25 2006-10-19 Merck Sharp & Dohme Ltd., Hoddesdon 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
JP4080541B2 (ja) 1996-10-18 2008-04-23 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子
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
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
DE69827956T2 (de) * 1997-08-11 2005-04-14 Boehringer Ingelheim (Canada) Ltd., Laval Peptidanaloga mit inhibitorischer wirkung auf hepatitis c
US6183121B1 (en) 1997-08-14 2001-02-06 Vertex Pharmaceuticals Inc. Hepatitis C virus helicase crystals and coordinates that define helicase binding pockets
US20040058982A1 (en) 1999-02-17 2004-03-25 Bioavailability System, Llc Pharmaceutical compositions
US20020017295A1 (en) 2000-07-07 2002-02-14 Weers Jeffry G. Phospholipid-based powders for inhalation
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
AP1498A (en) 1999-03-19 2005-11-21 Vertex Pharma Inhibitors of impdh enzyme.
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
JP2003526634A (ja) 1999-12-03 2003-09-09 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α−ケトアミド阻害剤
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
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
IL152022A0 (en) 2000-04-03 2003-04-10 Vertex Pharma Compounds useful as protease inhibitors and pharmaceutical compositions containing the same
US6846802B2 (en) 2000-04-05 2005-01-25 Schering Corporation Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties
JP4748912B2 (ja) 2000-04-19 2011-08-17 シェーリング コーポレイション アルキルおよびアリールアラニンp2部分を含むc型肝炎ウイルスに対する大員環ns3−セリンプロテアーゼ阻害剤
CA2414960C (en) 2000-06-30 2012-04-10 Seikagaku Corporation Epoxycarboxamide compound, azide compound, and amino alcohol compound, and process for preparing .alpha.keto amide compound using them
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
US20020068702A1 (en) 2000-07-21 2002-06-06 Marguerita Lim-Wilby Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
CN102372764A (zh) 2000-07-21 2012-03-14 先灵公司 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
RU2003105221A (ru) 2000-07-21 2004-09-20 Шеринг Корпорейшн (US) Новые пептиды, как ингибиторы ns3-серинпротеазы вируса гепатита с
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation 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
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
ES2263687T3 (es) 2000-11-20 2006-12-16 Bristol-Myers Squibb Company Inhibidores tripeptidicos de la hepatitis c.
AR031905A1 (es) 2000-12-12 2003-10-08 Schering Corp Peptidos diarilicos como inhibidores de ns3-serina proteasa en hepatitis de virus c
US6653295B2 (en) 2000-12-13 2003-11-25 Bristol-Myers Squibb 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
ATE526339T1 (de) 2001-01-22 2011-10-15 Merck Sharp & Dohme Nukleosidderivate als inhibitoren der rna- abhängigen viralen rna-polymerase
GB0102342D0 (en) 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
AU2002237982A1 (en) 2001-01-30 2002-08-12 Vertex Pharmaceuticals Incorporated A quantitative assay for nucleic acids
ES2328466T3 (es) 2001-03-27 2009-11-13 Vertex Pharmaceuticals Incorporated 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
ATE349463T1 (de) 2001-07-11 2007-01-15 Vertex Pharma 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
MXPA04003825A (es) 2001-10-24 2004-07-08 Vertex Pharma Inhibidores de serina proteasa, en particular la ns3-ns4a proteasa del virus de hepatitis c, que incorpora un sistema de anillo fusionado.
HRP20040510A2 (en) 2001-11-14 2005-08-31 Teva Pharmaceutical Industries Ltd. Amorphous and crystalline forms of losartan potassium and process for their preparation
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
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
MXPA04009938A (es) 2002-04-11 2004-12-13 Vertex Pharma Inhibidores de serina proteasas, en particular la proteasa ns3-ns4a del hcv.
KR20050040912A (ko) 2002-08-01 2005-05-03 파마셋 인코포레이티드 플라비비리다에 감염 치료용의 비사이클로[4.2.1]노난시스템을 가지는 화합물
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
BRPI0407587A (pt) 2003-02-18 2006-02-14 Pfizer inibidores do vìrus da hepatite c, composições e tratamentos que os utilizam
DE602004029866D1 (de) 2003-03-05 2010-12-16 Boehringer Ingelheim Pharma Peptidanaloga mit inhibitorischer wirkung auf hepatitis c
WO2004101605A1 (en) 2003-03-05 2004-11-25 Boehringer Ingelheim International Gmbh Hepatitis c inhibiting compounds
US20050090450A1 (en) 2003-04-11 2005-04-28 Farmer Luc J. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
EP1613620A1 (en) 2003-04-11 2006-01-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2004103996A1 (en) 2003-05-21 2004-12-02 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor compounds
US7109172B2 (en) 2003-07-18 2006-09-19 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
WO2005018330A1 (en) 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
TWI359147B (en) 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
US20050120398A1 (en) 2003-09-12 2005-06-02 Vertex Pharmaceuticals Incorporated Animal model for HCV infection
US20050119189A1 (en) 2003-09-18 2005-06-02 Cottrell Kevin M. 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
ATE500264T1 (de) 2003-09-22 2011-03-15 Boehringer Ingelheim Int Makrozyklische peptide mit wirkung gegen das hepatitis-c-virus
KR20060130027A (ko) 2003-10-10 2006-12-18 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 hcv ns3-ns4a 프로테아제의억제제
AR045870A1 (es) 2003-10-11 2005-11-16 Vertex Pharma Terapia de combinacion para la infeccion de virus de hepatitis c
KR20060120162A (ko) 2003-10-27 2006-11-24 버텍스 파마슈티칼스 인코포레이티드 Hcv 치료용 배합물
CN1894276B (zh) 2003-10-27 2010-06-16 威特克斯医药股份有限公司 Hcv ns3-ns4a蛋白酶抗药性突变体
WO2005043118A2 (en) 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Drug discovery method
WO2005042484A1 (en) 2003-10-28 2005-05-12 Vertex Pharmaceuticals, Incorporated Preparation of 4,5-dialkyl-3-acyl-pyrrole-2-carboxylic acid derivatives by fischer-fink type synthesis and subsequent acylation
US20050119318A1 (en) 2003-10-31 2005-06-02 Hudyma Thomas W. Inhibitors of HCV replication
US7132504B2 (en) 2003-11-12 2006-11-07 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CN1910275B (zh) 2003-12-01 2011-04-27 威特克斯医药股份有限公司 包含胎儿肝细胞的组合物及其用于hcv感染的方法
DE602005025855D1 (de) 2004-01-21 2011-02-24 Boehringer Ingelheim Pharma Makrocyclische peptide mit wirkung gegen das hepatitis-c-virus
EP1711515A2 (en) 2004-02-04 2006-10-18 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
PT1718608E (pt) 2004-02-20 2013-08-01 Boehringer Ingelheim Int Inibidores da polimerase viral
ATE438622T1 (de) 2004-02-27 2009-08-15 Schering Corp 3,4-(cyclopentyl)kondensierte prolinverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
PL2399916T3 (pl) 2004-03-12 2015-06-30 Vertex Pharma Sposoby i związki pośrednie do wytwarzania acetali asparaginowych jako inhibitorów kaspazy
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
CN102512372A (zh) 2004-06-08 2012-06-27 沃泰克斯药物股份有限公司 药物组合物
US7550559B2 (en) 2004-08-27 2009-06-23 Schering Corporation Acylsulfonamide compounds as inhibitors of hepatitis C virus NS3 serine protease
US7863274B2 (en) 2005-07-29 2011-01-04 Concert Pharmaceuticals Inc. Deuterium enriched analogues of tadalafil as PDE5 inhibitors
CA2617679A1 (en) 2005-08-02 2007-02-08 Steve Lyons Inhibitors of serine proteases
NZ593214A (en) 2005-08-19 2013-02-22 Vertex Pharma Compounds and Processes for preparing serine protease inhibitors
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
JP2009531315A (ja) 2006-03-16 2009-09-03 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 重水素化c型肝炎プロテアーゼインヒビター
BRPI0709568A2 (pt) 2006-03-16 2011-07-12 Vertex Pharmaceuticals Incorporarted processos e intermediários para preparar compostos estéricos
JP2009530416A (ja) 2006-03-20 2009-08-27 バーテックス ファーマシューティカルズ インコーポレイテッド 医薬組成物
AU2007226983A1 (en) 2006-03-20 2007-09-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
RU2446800C2 (ru) 2006-05-31 2012-04-10 Вертекс Фармасьютикалз Инкорпорейтед Препаративные формы с контролируемым высвобождением
WO2008106058A2 (en) 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases

Also Published As

Publication number Publication date
CN1451014A (zh) 2003-10-22
AU8831801A (en) 2002-03-13
HUP0300855A2 (hu) 2003-10-28
IL185644A0 (en) 2008-01-06
ES2489115T3 (es) 2014-09-01
TW201022243A (en) 2010-06-16
KR20080007515A (ko) 2008-01-21
KR20100042296A (ko) 2010-04-23
EP1849797A3 (en) 2008-01-23
UA99895C2 (uk) 2012-10-25
MXPA03001780A (es) 2003-06-04
TWI359145B (en) 2012-03-01
NO329929B1 (no) 2011-01-24
US20120064034A1 (en) 2012-03-15
IL215892A (en) 2015-03-31
WO2002018369A8 (en) 2003-11-06
PL365836A1 (en) 2005-01-10
CA2419607A1 (en) 2002-03-07
PL211019B1 (pl) 2012-03-30
IL154671A (en) 2011-11-30
NO20030928D0 (no) 2003-02-27
HRP20030139B1 (hr) 2015-08-28
JP2012197289A (ja) 2012-10-18
NO20100999L (no) 2003-04-16
EA200300318A1 (ru) 2004-02-26
KR20030041981A (ko) 2003-05-27
KR20100043293A (ko) 2010-04-28
EP1878720B1 (en) 2010-10-06
EP1958956A2 (en) 2008-08-20
DE20122915U1 (de) 2010-04-08
EP1849797A2 (en) 2007-10-31
EA011547B1 (ru) 2009-04-28
AU2001288318C1 (en) 2002-03-13
HK1163061A1 (en) 2012-09-07
CN103232381A (zh) 2013-08-07
ATE483686T1 (de) 2010-10-15
TW201022241A (en) 2010-06-16
KR100945975B1 (ko) 2010-03-09
US20050197299A1 (en) 2005-09-08
IL215892A0 (en) 2011-12-29
NO20100093L (no) 2003-04-16
ZA200301641B (en) 2004-06-21
EP1958956B1 (en) 2013-12-11
EA200701869A1 (ru) 2008-02-28
ES2352804T3 (es) 2011-02-23
ES2450815T3 (es) 2014-03-25
HRP20030139B8 (hr) 2015-11-06
EP2368877A1 (en) 2011-09-28
TWI378927B (en) 2012-12-11
PE20020474A1 (es) 2002-06-18
EP2368877B1 (en) 2014-05-07
BR0113666A (pt) 2005-09-27
DZ3438A1 (fr) 2002-03-07
EP1320540B1 (en) 2009-05-13
ES2325481T3 (es) 2009-09-07
EP2368901A1 (en) 2011-09-28
SK2492003A3 (en) 2004-11-03
DK1320540T5 (da) 2012-05-29
JP2004517047A (ja) 2004-06-10
US8529882B2 (en) 2013-09-10
US20100137583A1 (en) 2010-06-03
HK1057758A1 (en) 2004-04-16
CN101693672B (zh) 2014-11-12
ECSP077217A (es) 2007-04-26
AR030591A1 (es) 2003-08-27
KR20080104383A (ko) 2008-12-02
UA81600C2 (en) 2008-01-25
JP2011079835A (ja) 2011-04-21
US20120282219A1 (en) 2012-11-08
CY2012007I2 (el) 2014-07-02
ATE431358T1 (de) 2009-05-15
TW200918523A (en) 2009-05-01
CN100522991C (zh) 2009-08-05
CN102504014A (zh) 2012-06-20
DE122012000015I1 (de) 2012-05-24
CN101693672A (zh) 2010-04-14
IL215891A (en) 2015-04-30
ES2325481T9 (es) 2012-07-10
TW201022244A (en) 2010-06-16
HRP20030139A2 (en) 2005-04-30
IL215890A0 (en) 2011-12-29
SV2003000617A (es) 2003-01-13
CY1109216T1 (el) 2014-07-02
KR20080104382A (ko) 2008-12-02
TWI339661B (en) 2011-04-01
DK1878720T3 (da) 2011-01-24
KR20090120013A (ko) 2009-11-23
IL154671A0 (en) 2003-09-17
NZ541302A (en) 2007-04-27
CN101633636B (zh) 2013-03-13
LU91960I2 (fr) 2012-05-21
DE60138717D1 (de) 2009-06-25
JP2007284444A (ja) 2007-11-01
KR20080104384A (ko) 2008-12-02
US20140294763A1 (en) 2014-10-02
KR20080096718A (ko) 2008-10-31
EP1876173A1 (en) 2008-01-09
US8252923B2 (en) 2012-08-28
NO20030928L (no) 2003-04-16
SI1320540T1 (sl) 2009-10-31
NO2012006I2 (no) 2012-04-03
HK1114090A1 (en) 2008-10-24
PT1320540E (pt) 2009-07-14
CZ2003595A3 (cs) 2003-06-18
JP4689938B2 (ja) 2011-06-01
CA2419607C (en) 2012-03-13
IL215891A0 (en) 2011-12-29
NO330807B1 (no) 2011-07-18
WO2002018369A2 (en) 2002-03-07
CN101696232A (zh) 2010-04-21
DK1320540T3 (da) 2009-07-27
CL2010000330A1 (es) 2010-09-21
AU2001288318B2 (en) 2007-09-06
CA2697205C (en) 2014-07-29
CN1869061B (zh) 2013-04-24
EP2371839A1 (en) 2011-10-05
TWI359144B (en) 2012-03-01
KR20110088600A (ko) 2011-08-03
HUP0300855A3 (en) 2012-01-30
CN101633636A (zh) 2010-01-27
EP1320540B9 (en) 2012-03-21
ECSP034493A (es) 2003-04-25
CY2012007I1 (el) 2014-07-02
EP1878720A1 (en) 2008-01-16
TW201022242A (en) 2010-06-16
CN1869061A (zh) 2006-11-29
WO2002018369A3 (en) 2002-08-15
JP5269035B2 (ja) 2013-08-21
KR100968295B1 (ko) 2010-07-07
EA017556B1 (ru) 2013-01-30
CA2697205A1 (en) 2002-03-07
EP1320540A2 (en) 2003-06-25
NZ569670A (en) 2010-03-26
NO2012006I1 (no) 2012-04-30
KR100876472B1 (ko) 2008-12-31
EP1958956A3 (en) 2008-09-24
EP2368878A1 (en) 2011-09-28
DE60143233D1 (de) 2010-11-18
US7820671B2 (en) 2010-10-26

Similar Documents

Publication Publication Date Title
TWI319763B (en) Peptidomimetic protease inhibitors
AU4344101A (en) Protease inhibitors
GB9917909D0 (en) Cysteine protease inhibitors
IL153421A0 (en) Protease inhibitors
EP1235577A4 (en) PROTEASE INHIBITORS
EP1232155A4 (en) PROTEASE INHIBITORS
IL151087A0 (en) Protease inhibitors
EP1231921A4 (en) PROTEASE INHIBITORS
EP1229915A4 (en) PROTEASE INHIBITORS
EP1229914A4 (en) PROTEASE INHIBITORS
EP1229912A4 (en) PROTEASE INHIBITORS
EP1229911A4 (en) PROTEASE INHIBITORS
EP1173429A4 (en) PROTEASE INHIBITORS
EP1233771A4 (en) PROTEASE INHIBITORS
EP1351930A4 (en) PROTEASE INHIBITORS
EP1161237A4 (en) PROTEASE INHIBITORS
EP1231923A4 (en) PROTEASE INHIBITORS
IL155961A0 (en) Cysteine protease inhibitors
HUP0301964A3 (en) Protease inhibitors
EP1232154A4 (en) PROTEASE INHIBITORS
EP1231922A4 (en) PROTEASE INHIBITORS
AU6407701A (en) Serine protease inhibitors
GB0009123D0 (en) Protease inhibitor

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees