JP2009505966A - セリンプロテアーゼのインヒビター - Google Patents

セリンプロテアーゼのインヒビター Download PDF

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Publication number
JP2009505966A
JP2009505966A JP2008525128A JP2008525128A JP2009505966A JP 2009505966 A JP2009505966 A JP 2009505966A JP 2008525128 A JP2008525128 A JP 2008525128A JP 2008525128 A JP2008525128 A JP 2008525128A JP 2009505966 A JP2009505966 A JP 2009505966A
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optionally substituted
mixture
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membered
compounds according
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JP2008525128A
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Japanese (ja)
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JP2009505966A5 (https=
Inventor
スティーブ・ライオンズ
ロバート・ビー・パーニ
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37654834&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP2009505966(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2009505966A publication Critical patent/JP2009505966A/ja
Publication of JP2009505966A5 publication Critical patent/JP2009505966A5/ja
Pending legal-status Critical Current

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    • 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
    • A01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/44Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
    • A01N37/46N-acyl derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/005Enzyme inhibitors
    • 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
    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic
    • 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
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/99Enzyme inactivation by chemical treatment
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pest Control & Pesticides (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Agronomy & Crop Science (AREA)
  • General Engineering & Computer Science (AREA)
  • Plant Pathology (AREA)
  • Dentistry (AREA)
  • Environmental Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2008525128A 2005-08-02 2006-08-01 セリンプロテアーゼのインヒビター Pending JP2009505966A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US70477205P 2005-08-02 2005-08-02
PCT/US2006/029988 WO2007016589A2 (en) 2005-08-02 2006-08-01 Inhibitors of serine proteases

Publications (2)

Publication Number Publication Date
JP2009505966A true JP2009505966A (ja) 2009-02-12
JP2009505966A5 JP2009505966A5 (https=) 2009-12-24

Family

ID=37654834

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008525128A Pending JP2009505966A (ja) 2005-08-02 2006-08-01 セリンプロテアーゼのインヒビター

Country Status (17)

Country Link
US (4) US20070105781A1 (https=)
EP (3) EP1910341B1 (https=)
JP (1) JP2009505966A (https=)
KR (1) KR20080033481A (https=)
CN (1) CN101277950B (https=)
AR (1) AR057716A1 (https=)
AU (1) AU2006275413B2 (https=)
CA (1) CA2617679A1 (https=)
ES (1) ES2401661T3 (https=)
IL (1) IL189192A0 (https=)
MX (1) MX2008001528A (https=)
NO (1) NO20081012L (https=)
NZ (1) NZ565540A (https=)
RU (2) RU2441020C2 (https=)
TW (1) TW200740813A (https=)
WO (1) WO2007016589A2 (https=)
ZA (1) ZA200801114B (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018092724A1 (ja) * 2016-11-15 2018-05-24 学校法人東京理科大学 分子動態評価方法及びスクリーニング方法

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100509388B1 (ko) * 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 c 바이러스 ns3 프로테아제의 저해제
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
TWI359147B (en) * 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
MX2008001166A (es) 2005-07-25 2008-03-18 Intermune Inc Nuevos inhibidores macrociclicos de la replicacion del virus de hepatitis c.
KR20080033481A (ko) * 2005-08-02 2008-04-16 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제의 억제제
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
EP1991229A2 (en) 2006-02-27 2008-11-19 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
EP1993994A2 (en) 2006-03-16 2008-11-26 Vertex Pharmceuticals Incorporated Deuterated hepatitis c protease inhibitors
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
EP2007789B1 (en) 2006-04-11 2015-05-20 Novartis AG Spirocyclic HCV/HIV inhibitors and their uses
JP2010519329A (ja) * 2007-02-27 2010-06-03 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ阻害剤
DK2114924T3 (da) * 2007-02-27 2012-04-10 Vertex Pharma Co-krystaller og farmaceutiske sammensætninger omfattende disse
CN101835774B (zh) * 2007-08-30 2014-09-17 弗特克斯药品有限公司 共晶体和包含该共晶体的药物组合物
AR068756A1 (es) * 2007-10-10 2009-12-02 Novartis Ag Compuestos peptidicos, formulacion farmaceutica y sus usos como moduladores del virus de la hepatitis c
RU2490272C2 (ru) 2008-02-04 2013-08-20 Айденикс Фармасьютикалз, Инк. Макроциклические ингибиторы серинпротеазы
EP2358736A1 (en) * 2008-10-15 2011-08-24 Intermune, Inc. Therapeutic antiviral peptides
CN102300871A (zh) * 2008-12-19 2011-12-28 吉里德科学公司 Hcv ns3蛋白酶抑制剂
US8102720B2 (en) * 2009-02-02 2012-01-24 Qualcomm Incorporated System and method of pulse generation
TWI519530B (zh) 2009-02-20 2016-02-01 艾伯維德國有限及兩合公司 羰醯胺化合物及其作為鈣蛋白酶(calpain)抑制劑之用途
JP5690286B2 (ja) 2009-03-04 2015-03-25 イデニク プハルマセウティカルス,インコーポレイテッド ホスホチオフェン及びホスホチアゾールhcvポリメラーゼ阻害剤
WO2010118078A1 (en) 2009-04-08 2010-10-14 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US8236798B2 (en) 2009-05-07 2012-08-07 Abbott Gmbh & Co. Kg Carboxamide compounds and their use as calpain inhibitors
US20120244122A1 (en) * 2009-05-28 2012-09-27 Masse Craig E Peptides for the Treatment of HCV Infections
TW201117812A (en) 2009-08-05 2011-06-01 Idenix Pharmaceuticals Inc Macrocyclic serine protease inhibitors
IN2012DN02693A (https=) * 2009-09-28 2015-09-04 Intermune Inc
TW201116540A (en) * 2009-10-01 2011-05-16 Intermune Inc Therapeutic antiviral peptides
WO2011063076A1 (en) 2009-11-19 2011-05-26 Itherx Pharmaceuticals, Inc. Methods of treating hepatitis c virus with oxoacetamide compounds
MX2012006877A (es) 2009-12-18 2012-08-31 Idenix Pharmaceuticals Inc Inhibidores de virus de hepatitis c de arileno o heteroarileno 5, 5 - fusionado.
US8598211B2 (en) 2009-12-22 2013-12-03 Abbvie Inc. Carboxamide compounds and their use as calpain inhibitors IV
US9051304B2 (en) 2009-12-22 2015-06-09 AbbVie Deutschland GmbH & Co. KG Carboxamide compounds and their use as calpain inhibitors V
JP2013544866A (ja) 2010-12-09 2013-12-19 アッヴィ・ドイチュラント・ゲー・エム・ベー・ハー・ウント・コー・カー・ゲー カルボキサミド化合物及びカルパイン阻害剤vとしてのその使用
PT2661433T (pt) 2011-01-04 2017-10-24 Novartis Ag Compostos de indole ou seus análogos úteis para o tratamento da degeneração macular relacionada com a idade (amd)
US9353100B2 (en) 2011-02-10 2016-05-31 Idenix Pharmaceuticals Llc Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating HCV infections
US20120252721A1 (en) 2011-03-31 2012-10-04 Idenix Pharmaceuticals, Inc. Methods for treating drug-resistant hepatitis c virus infection with a 5,5-fused arylene or heteroarylene hepatitis c virus inhibitor
US8492386B2 (en) 2011-10-21 2013-07-23 Abbvie Inc. Methods for treating HCV
DE202012012955U1 (de) 2011-10-21 2014-07-14 Abbvie Inc. Eine Kombination aus mindestens zwei direkt wirkenden antiviralen Wirkstoffen (DAAs) für die Verwendung zur Behandlung von HCV
EP2583677A3 (en) 2011-10-21 2013-07-03 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
WO2013072328A1 (en) 2011-11-14 2013-05-23 Sanofi Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases
SG11201406345XA (en) 2012-04-03 2014-11-27 Abbvie Deutschland Carboxamide compounds and their use as calpain inhibitors v
WO2014002058A2 (en) 2012-06-28 2014-01-03 Novartis Ag Complement pathway modulators and uses thereof
US9815819B2 (en) 2012-06-28 2017-11-14 Novartis Ag Complement pathway modulators and uses thereof
CN104379579B (zh) 2012-06-28 2017-03-08 诺华股份有限公司 吡咯烷衍生物及其作为补体途径调节剂的用途
EP2867225B1 (en) 2012-06-28 2017-08-09 Novartis AG Pyrrolidine derivatives and their use as complement pathway modulators
ES2644700T3 (es) 2012-06-28 2017-11-30 Novartis Ag Derivados de pirrolidina y su uso como moduladores de la ruta del complemento
CA2882724A1 (en) 2012-07-12 2014-01-16 Novartis Ag Complement pathway modulators and uses thereof
WO2014053533A1 (en) 2012-10-05 2014-04-10 Sanofi Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation
WO2015042375A1 (en) 2013-09-20 2015-03-26 Idenix Pharmaceuticals, Inc. Hepatitis c virus inhibitors
WO2015134561A1 (en) 2014-03-05 2015-09-11 Idenix Pharmaceuticals, Inc. Pharmaceutical compositions comprising a 5,5-fused heteroarylene flaviviridae inhibitor and their use for treating or preventing flaviviridae infection
US20170066779A1 (en) 2014-03-05 2017-03-09 Idenix Pharmaceuticals Llc Solid forms of a flaviviridae virus inhibitor compound and salts thereof
EA201892448A1 (ru) 2016-04-28 2019-06-28 Эмори Юниверсити Алкинсодержащие нуклеотидные и нуклеозидные терапевтические композиции и связанные с ними способы применения

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996011697A1 (en) * 1994-10-12 1996-04-25 Merck & Co., Inc. Thrombin inhibitors
WO2002008244A2 (en) * 2000-07-21 2002-01-31 Schering Corporation Peptides as ns3-serine protease inhibitors of hepatitis c virus
WO2002018369A2 (en) * 2000-08-31 2002-03-07 Eli Lilly And Company Peptidomimetic protease inhibitors
WO2003087092A2 (en) * 2002-04-11 2003-10-23 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 - ns4 protease
WO2005007681A2 (en) * 2003-07-18 2005-01-27 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2005035525A2 (en) * 2003-09-05 2005-04-21 Vertex Pharmaceuticals Incorporated 2-amido-4-aryloxy-1-carbonylpyrrolidine derivatives as inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2005042570A1 (en) * 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Hcv ns3-ns4a protease resistance mutants

Family Cites Families (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4499082A (en) * 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
FR2575753B1 (fr) * 1985-01-07 1987-02-20 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5496927A (en) * 1985-02-04 1996-03-05 Merrell Pharmaceuticals Inc. Peptidase inhibitors
US5736520A (en) * 1988-10-07 1998-04-07 Merrell Pharmaceuticals Inc. Peptidase inhibitors
EP0604182B1 (en) * 1992-12-22 2000-10-11 Eli Lilly And Company Inhibitors of HIV protease useful for the treatment of Aids
CA2170020C (en) * 1992-12-29 2005-08-02 Dale J. Kempf Retroviral protease inhibiting compounds
US5384410A (en) * 1993-03-24 1995-01-24 The Du Pont Merck Pharmaceutical Company Removal of boronic acid protecting groups by transesterification
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
IL111991A (en) * 1994-01-28 2000-07-26 Abbott Lab Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5756466A (en) * 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5861267A (en) * 1995-05-01 1999-01-19 Vertex Pharmaceuticals Incorporated Methods, nucleotide sequences and host cells for assaying exogenous and endogenous protease activity
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
EP1019410A1 (en) * 1995-11-23 2000-07-19 MERCK SHARP & DOHME LTD. Spiro-piperidine derivatives and their use as tachykinin antagonists
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
HUP0004421A3 (en) 1996-04-23 2002-10-28 Vertex Pharmaceuticals Inc Cam Urea derivatives and pharmaceutical compositions containing them, use thereof for the treatment of deseases mediated by impdh enzyme
WO1997043310A1 (en) 1996-05-10 1997-11-20 Schering Corporation Synthetic inhibitors of hepatitis c virus ns3 protease
EP0929554B1 (en) * 1996-09-25 2006-03-15 MERCK SHARP & DOHME LTD. Spiro-azacyclic derivatives, their preparation and their use as tachykinin antagonists
WO1998015544A1 (en) * 1996-10-08 1998-04-16 Colorado State University Research Foundation Catalytic asymmetric epoxidation
KR100509388B1 (ko) 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 c 바이러스 ns3 프로테아제의 저해제
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
EP0966465B1 (en) * 1997-03-14 2003-07-09 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
US6767991B1 (en) * 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
ES2234144T3 (es) * 1997-08-11 2005-06-16 Boehringer Ingelheim (Canada) Ltd. Analogos de peptidos inhibidores de la hepatitis c.
WO1999007733A2 (en) 1997-08-11 1999-02-18 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
IT1299134B1 (it) 1998-02-02 2000-02-29 Angeletti P Ist Richerche Bio Procedimento per la produzione di peptidi con proprieta' inibitrici della proteasi ns3 del virus hcv, peptidi cosi' ottenibili e peptidi
ATE346035T1 (de) * 1998-03-31 2006-12-15 Vertex Pharma Inhibitoren von serin proteasen, insbesondere von hepatitis c virus ns3 protease
US6251583B1 (en) * 1998-04-27 2001-06-26 Schering Corporation Peptide substrates for HCV NS3 protease assays
GB9812523D0 (en) 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
US6323180B1 (en) * 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
DE19836514A1 (de) 1998-08-12 2000-02-17 Univ Stuttgart Modifikation von Engineeringpolymeren mit N-basischen Gruppe und mit Ionenaustauschergruppen in der Seitenkette
US6117639A (en) * 1998-08-31 2000-09-12 Vertex Pharmaceuticals Incorporated Fusion proteins, DNA molecules, vectors, and host cells useful for measuring protease activity
US6025516A (en) * 1998-10-14 2000-02-15 Chiragene, Inc. Resolution of 2-hydroxy-3-amino-3-phenylpropionamide and its conversion to C-13 sidechain of taxanes
GB9825946D0 (en) 1998-11-26 1999-01-20 Angeletti P Ist Richerche Bio Pharmaceutical compounds for the inhibition of hepatitis C virus NS3 protease
ATE400251T1 (de) * 1999-02-09 2008-07-15 Pfizer Prod Inc Zusammensetzungen basischer arzneistoffe mit verbesserter bioverfügbarkeit
US20020042046A1 (en) * 1999-02-25 2002-04-11 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
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
UA74546C2 (en) 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
AU6371900A (en) 1999-07-26 2001-02-13 Du Pont Pharmaceuticals Company Lactam inhibitors of hepatitis c virus ns3 protease
US7122627B2 (en) * 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
CA2396504A1 (en) 2000-02-29 2001-09-07 Dupont Pharmaceuticals Company Inhibitors of hepatitis c virus ns3 protease
ES2240446T3 (es) * 2000-04-03 2005-10-16 Vertex Pharma Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.
AR029903A1 (es) * 2000-04-05 2003-07-23 Schering Corp Inhibidores macrociclicos de la ns3-serina proteasa, del virus de la hepatitis c, que comprenden partes p2 n-ciclicas, composiciones farmaceuticas y utilizacion de los mismos para la manufactura de un medicamento
CN101580536A (zh) 2000-04-19 2009-11-18 先灵公司 含有烷基和芳基丙氨酸p2部分的丙型肝炎病毒的大环ns3-丝氨酸蛋白酶抑制剂
KR20030081297A (ko) * 2000-07-21 2003-10-17 쉐링 코포레이션 C형 간염 바이러스의 ns3-세린 프로테아제억제제로서의 신규한 펩티드
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
AR034127A1 (es) * 2000-07-21 2004-02-04 Schering Corp Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento
CA2418199A1 (en) * 2000-07-21 2002-01-31 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
GB0021286D0 (en) 2000-08-30 2000-10-18 Gemini Genomics Ab Identification of drug metabolic capacity
US6846806B2 (en) 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
DE60119968T2 (de) 2000-11-20 2007-01-18 Bristol-Myers Squibb Co. Hepatitis c tripeptid inhibitoren
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
AU2002230763A1 (en) 2000-12-13 2008-01-03 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
US6653295B2 (en) * 2000-12-13 2003-11-25 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
SK286630B6 (sk) * 2001-01-22 2009-02-05 Merck & Co., Inc. Nukleozidové deriváty, farmaceutický prostriedok s ich obsahom a ich použitie
GB0102342D0 (en) * 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
AU2002354739A1 (en) * 2001-07-03 2003-01-21 Altana Pharma Ag Process for the production of optically active 3-phenylisoserine
CA2449504A1 (en) * 2001-07-11 2003-01-23 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
US6824769B2 (en) * 2001-08-28 2004-11-30 Vertex Pharmaceuticals Incorporated Optimal compositions and methods thereof for treating HCV infections
US7241796B2 (en) * 2001-10-24 2007-07-10 Vertex Pharmaceuticals Inc. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
ES2234451T1 (es) * 2001-11-14 2005-07-01 Teva Pharmaceutical Industries Ltd. Formas cristalinas y amorfas de losartan potasio y procedimiento para su preparacion.
WO2004013300A2 (en) * 2002-08-01 2004-02-12 Pharmasset Inc. Compounds with the bicyclo[4.2.1]nonane system for the treatment of flaviviridae infections
WO2004013298A2 (en) * 2002-08-01 2004-02-12 Pharmasset Ltd. 2',3'-dideoxynucleoside analogues for the treatment or prevention of flavivitridae 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
US20040180815A1 (en) * 2003-03-07 2004-09-16 Suanne Nakajima Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
CA2515216A1 (en) 2003-02-07 2004-08-26 Enanta Pharmaceuticals, Inc. Macrocyclic hepatitis c serine protease inhibitors
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
WO2004092161A1 (en) * 2003-04-11 2004-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
CL2004001161A1 (es) * 2003-05-21 2005-04-08 Boehringer Ingelheim Int Compuestos describe compuestos derivados de quinolina; composicion farmaceutica; y su uso para tratar una enfermedad causada por el virus de la hepatitis c.
WO2005018330A1 (en) * 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
EP1670415A4 (en) * 2003-09-12 2007-12-05 Vertex Pharma ANIMAL MODEL FOR STUDYING PROTEASES ACTIVITY AND HEPATIC DISORDERS
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.
WO2005037860A2 (en) * 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incoporated 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
JP2007509950A (ja) * 2003-10-27 2007-04-19 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 Hcv処置の組合せ剤
US8187874B2 (en) * 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
US20050119318A1 (en) * 2003-10-31 2005-06-02 Hudyma Thomas W. Inhibitors of HCV replication
AR049635A1 (es) * 2004-05-06 2006-08-23 Schering Corp (1r,2s,5s)-n-((1s)-3-amino-1-(ciclobutilmetil)-2,3-dioxopropil)-3-((2s)-2-((((1,1-dimetiletil)amino)carbonil)amino)-3,3-dimetil-1-oxobutil)-6,6-dimetil-3-azabiciclo(3.1.0)hexan-2-carboxamida como inhibidor de la ns3/ns4a serina proteasa del virus de la hepatitis c
AR049297A1 (es) * 2004-06-08 2006-07-12 Vertex Pharma Una composicion farmaceutica y dispersiones solidas de vx-950 (inhibidor de la proteasa de hcv ns3/4a) y proceso de obtencion
ATE513844T1 (de) * 2004-08-27 2011-07-15 Schering Corp Acylsulfonamidverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
TW201424733A (zh) * 2004-10-29 2014-07-01 Vertex Pharma 劑量型式
KR20080033481A (ko) * 2005-08-02 2008-04-16 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제의 억제제
PL385229A1 (pl) * 2005-08-19 2008-09-29 Vertex Pharmaceuticals Incorporated Sposoby i związki pośrednie
US20080070972A1 (en) * 2006-05-31 2008-03-20 Kadiyala Irina N Controlled release formulations
US8402690B2 (en) 2010-09-09 2013-03-26 Sterling International Inc. Bedbug trap

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996011697A1 (en) * 1994-10-12 1996-04-25 Merck & Co., Inc. Thrombin inhibitors
WO2002008244A2 (en) * 2000-07-21 2002-01-31 Schering Corporation Peptides as ns3-serine protease inhibitors of hepatitis c virus
WO2002018369A2 (en) * 2000-08-31 2002-03-07 Eli Lilly And Company Peptidomimetic protease inhibitors
WO2003087092A2 (en) * 2002-04-11 2003-10-23 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 - ns4 protease
WO2005007681A2 (en) * 2003-07-18 2005-01-27 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2005035525A2 (en) * 2003-09-05 2005-04-21 Vertex Pharmaceuticals Incorporated 2-amido-4-aryloxy-1-carbonylpyrrolidine derivatives as inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2005042570A1 (en) * 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Hcv ns3-ns4a protease resistance mutants

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
JPN6011066010; Bioorg. Med. Chem. Lett., 2000, Vol.10, p.711-713 *
JPN6011066012; Bioorg. Med. Chem. Lett., 2004, Vol.14, p.1441-1446 *
JPN6011066015; Bioorg. Med. Chem. Lett., 2004, Vol.14, p.5007-5011 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018092724A1 (ja) * 2016-11-15 2018-05-24 学校法人東京理科大学 分子動態評価方法及びスクリーニング方法

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