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NO20061426L - Inhibitorer av serinproteaser, spesielt HCV NS3-NS4A-protease - Google Patents

Inhibitorer av serinproteaser, spesielt HCV NS3-NS4A-protease

Info

Publication number
NO20061426L
NO20061426L NO20061426A NO20061426A NO20061426L NO 20061426 L NO20061426 L NO 20061426L NO 20061426 A NO20061426 A NO 20061426A NO 20061426 A NO20061426 A NO 20061426A NO 20061426 L NO20061426 L NO 20061426L
Authority
NO
Norway
Prior art keywords
inhibitors
compounds
serine proteases
ns4a protease
relates
Prior art date
Application number
NO20061426A
Other languages
English (en)
Inventor
Janos Pitlik
Robert Perni
John H Van Drie
John J Court
Shawn D Britt
Original Assignee
Vertex Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of NO20061426L publication Critical patent/NO20061426L/no

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    • 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
    • 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
    • A01N43/00Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/601,4-Diazines; Hydrogenated 1,4-diazines
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    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • A61P31/18Antivirals for RNA viruses for HIV
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    • C04CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04BLIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
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    • C04B35/626Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
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    • 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
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    • 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
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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Abstract

Foreliggende oppfinnelse vedrører forbindelser som hemmer serinproteaseaktivitet, spesielt aktiviteten av hepatitt Cvirus NS3-NS4A-protease. Som sådanne virker de ved å gripe forstyrrende inn i livssyklusen for hepatitt C-viruset, og de er også nyttige som antivirale midler. Oppfinnelsen vedrører videre sammensetninger omfattende disse forbindelser enten for anvendelse ex vivo eller for administrasjon til en pasient som lider av HCV-infeksjon. Oppfinnelsen vedrører også metoder for å behandle en HCV-infeksjon i en pasient ved å administrere en sammensetning omfattende en forbindelse ifølge denne oppfinnelse. Oppfinnelsen vedrører videre fremgangsmåter for å fremstille disse forbindelser.
NO20061426A 2003-09-05 2006-03-29 Inhibitorer av serinproteaser, spesielt HCV NS3-NS4A-protease NO20061426L (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US50067003P 2003-09-05 2003-09-05
PCT/US2004/029093 WO2005035525A2 (en) 2003-09-05 2004-09-07 2-amido-4-aryloxy-1-carbonylpyrrolidine derivatives as inhibitors of serine proteases, particularly hcv ns3-ns4a protease

Publications (1)

Publication Number Publication Date
NO20061426L true NO20061426L (no) 2006-03-29

Family

ID=34434831

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20061426A NO20061426L (no) 2003-09-05 2006-03-29 Inhibitorer av serinproteaser, spesielt HCV NS3-NS4A-protease

Country Status (19)

Country Link
US (4) US7378422B2 (no)
EP (2) EP2573083A1 (no)
JP (2) JP4767852B2 (no)
KR (2) KR20120051751A (no)
CN (2) CN1845920B (no)
AR (1) AR045596A1 (no)
AU (1) AU2004279800B9 (no)
BR (1) BRPI0414176A (no)
CA (1) CA2536436C (no)
IL (1) IL173627A0 (no)
MX (1) MXPA06002476A (no)
MY (1) MY148123A (no)
NO (1) NO20061426L (no)
NZ (2) NZ580205A (no)
PE (1) PE20050374A1 (no)
RU (2) RU2440368C2 (no)
TW (2) TW201127828A (no)
UY (1) UY28500A1 (no)
WO (1) WO2005035525A2 (no)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU227742B1 (en) 1996-10-18 2012-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
EP1268519B1 (en) * 2000-04-03 2005-06-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
JP2003007697A (ja) * 2001-06-21 2003-01-10 Hitachi Kokusai Electric Inc 半導体装置の製造方法、基板処理方法および基板処理装置
DE602004009295T2 (de) 2003-01-14 2008-07-03 Arena Pharmaceuticals, Inc., San Diego 1,2,3-trisubstituierte aryl- und heteroarylderivate als modulatoren des metabolismus zur vorbeugung und behandlung von metabolismus-bedingten krankheiten wie diabetes oder hyperglykämie
EP1613620A1 (en) * 2003-04-11 2006-01-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AR045047A1 (es) 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
CN102020700A (zh) 2003-07-18 2011-04-20 沃泰克斯药物股份有限公司 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂
PE20050374A1 (es) 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
TW200526686A (en) 2003-09-18 2005-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
EP1692157B1 (en) * 2003-10-10 2013-04-17 Vertex Pharmaceuticals Incorporated 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
EP1677827B1 (en) * 2003-10-27 2008-12-10 Vertex Pharmaceuticals Incorporated Combinations for hcv treatment
CN1938332B (zh) * 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂
MX2007014117A (es) 2005-05-13 2008-02-05 Virochem Pharma Inc Compuestos y metodos para el tratamiento o prevencion de infecciones de flavivirus.
JP5160415B2 (ja) * 2005-06-02 2013-03-13 メルク・シャープ・アンド・ドーム・コーポレーション 医薬処方物およびそれを用いる治療方法
US7608592B2 (en) 2005-06-30 2009-10-27 Virobay, Inc. HCV inhibitors
CN101242816B (zh) * 2005-06-30 2012-10-31 维罗贝股份有限公司 Hcv抑制剂
CN101263156A (zh) 2005-07-25 2008-09-10 因特蒙公司 C型肝炎病毒复制的新颖大环抑制剂
RU2441020C2 (ru) 2005-08-02 2012-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы серинпротеазы
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
AR055395A1 (es) * 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
US7964624B1 (en) * 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
CN101415705B (zh) 2005-10-11 2011-10-26 因特蒙公司 抑制丙型肝炎病毒复制的化合物和方法
WO2007083620A1 (ja) * 2006-01-20 2007-07-26 Kaneka Corporation β-アミノ-α-ヒドロキシ酸アミド誘導体の製造法
WO2007089618A2 (en) * 2006-01-27 2007-08-09 Phenomix Corporation Hepatitis c serine protease inhibitors and uses therefor
EP1991229A2 (en) 2006-02-27 2008-11-19 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
EP2194039A1 (en) 2006-03-16 2010-06-09 Vertex Pharmceuticals Incorporated Process for preparing optically enriched compounds
EP1998759A2 (en) * 2006-03-23 2008-12-10 Schering Corporation Combinations of hcv protease inhibitor(s) and cyp3a4 inhibitor(s), and methods of treatment related thereto
WO2007133865A2 (en) 2006-04-11 2007-11-22 Novartis Ag Hcv/hiv inhibitors an their uses
EP2027143A2 (en) 2006-05-23 2009-02-25 Irm Llc Compounds and compositions as channel activating protease inhibitors
EP2039689A4 (en) 2006-05-26 2011-12-28 Kaneka Corp PROCESS FOR PREPARING OPTICALLY ACTIVE 3-AMINO-2-HYDROXYPROPIONIC ACID CYCLOPROPYLAMID DERIVATIVES AND SALTS THEREOF
KR20090024834A (ko) 2006-07-05 2009-03-09 인터뮨, 인크. C형 간염 바이러스 복제의 신규 억제제
EP1881001A1 (en) * 2006-07-20 2008-01-23 Tibotec Pharmaceuticals Ltd. HCV NS-3 serine protease inhibitors
CA2656816A1 (en) * 2006-08-04 2008-02-14 Enanta Pharmaceuticals, Inc. Tetrazolyl macrocyclic hepatitis c serine protease inhibitors
US7687459B2 (en) * 2006-08-11 2010-03-30 Enanta Pharmaceuticals, Inc. Arylalkoxyl hepatitis C virus protease inhibitors
US20090098085A1 (en) * 2006-08-11 2009-04-16 Ying Sun Tetrazolyl acyclic hepatitis c serine protease inhibitors
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
AP2579A (en) 2006-11-15 2013-01-29 Virochem Pharma Inc Thiophene analogues for the treatment or prevention of flavivirus infections
WO2008086053A1 (en) * 2007-01-03 2008-07-17 Virobay, Inc. Hcv inhibitors
EA016327B1 (ru) 2007-02-09 2012-04-30 Айрм Ллк Соединения и композиции в качестве ингибиторов протеазы, активирующей каналы
BRPI0807907A2 (pt) * 2007-02-27 2017-05-16 Vertex Pharma co-cristais e composições farmacêuticas compreendendo os mesmos.
CN101903392A (zh) * 2007-02-27 2010-12-01 弗特克斯药品有限公司 丝氨酸蛋白酶的抑制剂
US20080317712A1 (en) * 2007-04-26 2008-12-25 Deqiang Niu Arylpiperidinyl and arylpyrrolidinyl tripeptide hepatitis c serine protease inhibitors
US7910587B2 (en) * 2007-04-26 2011-03-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl dipeptide hepatitis C virus inhibitors
US20080292587A1 (en) * 2007-04-26 2008-11-27 Ying Sun Oximyl dipeptide hepatitis c protease inhibitors
EP2160392A2 (en) * 2007-05-03 2010-03-10 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
WO2008141227A1 (en) 2007-05-10 2008-11-20 Intermune, Inc. Novel peptide inhibitors of hepatitis c virus replication
TW200922933A (en) 2007-08-30 2009-06-01 Vertex Pharma Co-crystals and pharmaceutical compositions comprising the same
AU2008309589B2 (en) 2007-10-10 2012-07-05 Novartis Ag Spiropyrrolidines and their use against HCV and HIV infection
JP2011051896A (ja) * 2007-12-21 2011-03-17 Kaneka Corp N−シクロプロピル−3−アミノ−2−ヒドロキシヘキサン酸アミド塩酸塩の製造方法
WO2009094443A1 (en) * 2008-01-24 2009-07-30 Enanta Pharmaceuticals, Inc. Difluorinated tripeptides as hcv serine protease inhibitors
CN101977915B (zh) * 2008-02-04 2014-08-13 埃迪尼克斯医药公司 大环丝氨酸蛋白酶抑制剂
US8321151B2 (en) 2008-12-30 2012-11-27 The Invention Science Fund I, Llc Computational methods and systems for treatment in relation to modulation of CYP450 enzyme activity
US8073632B2 (en) * 2008-12-30 2011-12-06 The Invention Science Fund I, Llc Computational methods and systems for treatment in relation to modulation of CYP450 enzyme activity
US8315815B2 (en) 2008-12-30 2012-11-20 The Invention Science Fund I, Llc Computational methods and systems for suggesting modulators of CYP450 as treatment options
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US8324417B2 (en) 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
EP2504329A1 (en) 2009-11-25 2012-10-03 Vertex Pharmaceuticals Incorporated 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections
KR20120130173A (ko) 2009-12-24 2012-11-29 버텍스 파마슈티칼스 인코포레이티드 플라비바이러스 감염을 치료 또는 예방하기 위한 유사체들
CA2794145A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
WO2011119870A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
TW201139438A (en) 2010-03-24 2011-11-16 Vertex Pharma Analogues for the treatment or prevention of flavivirus infections
TW201141857A (en) 2010-03-24 2011-12-01 Vertex Pharma Analogues for the treatment or prevention of flavivirus infections
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
JP2013531011A (ja) 2010-06-28 2013-08-01 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の処置または予防のための化合物および方法
CA2803248A1 (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
WO2012024363A2 (en) 2010-08-17 2012-02-23 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flaviviridae viral infections
PH12013500547A1 (en) 2010-09-22 2013-06-10 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
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
TW201317223A (zh) 2011-07-26 2013-05-01 Vertex Pharma 噻吩化合物
WO2013016499A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Methods for preparation of thiophene compounds
US20130123276A1 (en) 2011-11-14 2013-05-16 Sven Ruf Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases
CN104254518A (zh) * 2012-02-16 2014-12-31 阿奇克斯制药公司 线性肽抗生素
EP2827876A4 (en) 2012-03-22 2015-10-28 Alios Biopharma Inc PHARMACEUTICAL COMBINATIONS WITH A THIONUCLEOTIDE ANALOG
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
US20150065439A1 (en) 2013-02-28 2015-03-05 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
ES2995737T3 (en) 2015-01-06 2025-02-11 Arena Pharm Inc Compound for use in treating conditions related to the s1p1 receptor
MA42807A (fr) 2015-06-22 2018-07-25 Arena Pharm Inc Sel l-arginine cristallin d'acide (r)-2-(7-(4-cyclopentyl-3-(trifluorométhyl)benzyloxy)-1,2,3,4-tétrahydrocyclo-penta[b]indol-3-yl)acétique (composé 1) pour une utilisation dans des troubles associés au récepteur de s1p1
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
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC CARBOCYCLIC PROLINAMIDE DERIVATIVES
ES2971784T3 (es) 2016-06-21 2024-06-07 Orion Ophthalmology LLC Derivados heterocíclicos de prolinamida
JP2019522673A (ja) 2016-07-18 2019-08-15 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なジフルオロケトアミド誘導体
JP2019526564A (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なトリフルオロメチルプロパンアミド誘導体
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
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
EP3801459B1 (en) 2018-06-06 2024-08-07 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
CN113167802B (zh) 2018-12-04 2025-02-07 百时美施贵宝公司 通过多同位素体反应监测使用样品内校准曲线的分析方法
JP2024519306A (ja) 2021-05-12 2024-05-10 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング cGAS阻害薬としてのN結合環状置換基を有するピリジン誘導体
IL319969A (en) 2022-11-09 2025-05-01 Boehringer Ingelheim Int History of cyclic pyridines as CGAS inhibitors

Family Cites Families (184)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3226768A1 (de) 1981-11-05 1983-05-26 Hoechst Ag, 6230 Frankfurt Derivate der cis, endo-2-azabicyclo-(3.3.0)-octan-3-carbonsaeure, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung
DE3211676A1 (de) 1982-03-30 1983-10-06 Hoechst Ag Neue derivate von cycloalka (c) pyrrol-carbonsaeuren, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung sowie neue cycloalka (c) pyrrol-carbonsaeuren als zwischenstufen und verfahren zu deren herstellung
US4499082A (en) * 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
FR2575753B1 (fr) 1985-01-07 1987-02-20 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5496927A (en) 1985-02-04 1996-03-05 Merrell Pharmaceuticals Inc. Peptidase inhibitors
IL77748A (en) 1985-02-04 1991-11-21 Merrell Dow Pharma Amino acid and peptide derivatives as peptidase inhibitors
ATE71934T1 (de) 1985-06-07 1992-02-15 Ici America Inc Selektionierte difluorverbindungen.
US5231084A (en) 1986-03-27 1993-07-27 Hoechst Aktiengesellschaft Compounds having a cognition adjuvant action, agents containing them, and the use thereof for the treatment and prophylaxis of cognitive dysfuncitons
NZ223148A (en) 1987-01-16 1989-10-27 Merrell Dow Pharma Peptide derivatives having peptidase inhibition activity
EP0356595A1 (en) 1988-09-01 1990-03-07 Merrell Dow Pharmaceuticals Inc. Novel peptidase inhibitors
US5736520A (en) 1988-10-07 1998-04-07 Merrell Pharmaceuticals Inc. Peptidase inhibitors
ZA897514B (en) 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
EP0371179A1 (en) 1988-10-28 1990-06-06 Merrell Dow Pharmaceuticals Inc. Novel analogs of peptidase substrates
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
JPH06504547A (ja) 1990-12-28 1994-05-26 ジョージア・テック・リサーチ・コーポレーション ペプチドケトアミド、ケト酸およびケトエステル
JP2668003B2 (ja) 1992-06-12 1997-10-27 ファイザー インク. ヒトの心臓キマーゼを含むアンギオテンシンiキマーゼに関する阻害剤
US5371072A (en) 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
ES2150933T3 (es) * 1992-12-22 2000-12-16 Lilly Co Eli Inhibidores de la proteasa vih utiles para el tratamiento del sida.
EP1090914B1 (en) 1992-12-29 2003-01-02 Abbott Laboratories 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
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
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5861267A (en) 1995-05-01 1999-01-19 Vertex Pharmaceuticals Incorporated Methods, nucleotide sequences and host cells for assaying exogenous and endogenous protease activity
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
WO1997019084A1 (en) 1995-11-23 1997-05-29 Merck Sharp & Dohme Limited Spiro-piperidine derivatives and their use as tachykinin antagonists
EP0873519A4 (en) 1995-12-07 2005-04-27 Scripps Research Inst HIV PROTEASE INHIBITORS
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
WO1997040028A1 (en) 1996-04-23 1997-10-30 Vertex Pharmaceuticals Incorporated Urea derivatives as inhibitors of impdh enzyme
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
EP0907659A1 (en) 1996-05-10 1999-04-14 Schering Corporation Synthetic inhibitors of hepatitis c virus ns3 protease
US6153579A (en) 1996-09-12 2000-11-28 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
AU723414B2 (en) 1996-09-25 2000-08-24 Merck Sharp & Dohme Limited Spiro-azacyclic derivatives, their preparation and their use as tachykinin antagonists
CA2268255A1 (en) 1996-10-08 1998-04-16 Colorado State University Research Foundation Catalytic asymmetric epoxidation
HU227742B1 (en) * 1996-10-18 2012-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
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
DE19648793A1 (de) 1996-11-26 1998-05-28 Basf Ag Neue Benzamide und deren Anwendung
CA2282398A1 (en) 1997-03-14 1998-09-17 Steven M. Ronkin 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
JP4354632B2 (ja) 1997-08-11 2009-10-28 ベーリンガー インゲルハイム (カナダ) リミテッド C型肝炎抑制剤ペプチド
US6767991B1 (en) 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
NZ503263A (en) 1997-08-11 2002-10-25 Boehringer Ingelheim Ca Ltd Hepatitis C NS3 protease inhibitor peptides and peptide analogues
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
AU1416099A (en) 1997-11-28 1999-06-16 Schering Corporation Single-chain recombinant complexes of hepatitis c virus ns3 protease and ns4a cofactor peptide
US6075150A (en) 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
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
ES2281170T3 (es) 1998-03-31 2007-09-16 Vertex Pharmaceuticals Incorporated Inhibidores de serina proteasas, particularmente proteasa ns3 del virus de la hepatitis c.
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
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.
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
US6686335B1 (en) 1998-09-22 2004-02-03 Cephalon, Inc. Hydroxamate-containing cysteine and serine protease inhibitors
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
US6117870A (en) 1998-11-12 2000-09-12 Fujirebio Kabushiki Kaisha Cyclic amide derivatives
GB9825946D0 (en) 1998-11-26 1999-01-20 Angeletti P Ist Richerche Bio Pharmaceutical compounds for the inhibition of hepatitis C virus NS3 protease
ES2306646T3 (es) 1999-02-09 2008-11-16 Pfizer Products Inc. Composiciones de farmacos basicos con biodisponibilidad incrementada.
US20020042046A1 (en) 1999-02-25 2002-04-11 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
WO2000056331A1 (en) 1999-03-19 2000-09-28 Vertex Pharmaceuticals Incorporated 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
AU5788800A (en) * 1999-07-07 2001-01-22 Du Pont Pharmaceuticals Company Peptide boronic acid inhibitors of hepatitis c virus protease
US7122627B2 (en) * 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
EP1206449A1 (en) 1999-07-26 2002-05-22 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
WO2001016300A2 (en) 1999-08-31 2001-03-08 Basf Aktiengesellschaft Method of identifying inhibitors of cdc25
GB9925955D0 (en) 1999-11-02 1999-12-29 Angeletti P Ist Richerche Bio Hcv n33 protease inhibitors
US6774212B2 (en) * 1999-12-03 2004-08-10 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis C virus NS3 protease
US6624290B2 (en) 2000-02-08 2003-09-23 Schering Corporation Azapeptides useful in the treatment of Hepatitis C
US6699855B2 (en) 2000-02-29 2004-03-02 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
EP1268519B1 (en) * 2000-04-03 2005-06-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
DE60137207D1 (de) 2000-04-05 2009-02-12 Schering Corp Makrozyklische inhibitoren der ns3-serinprotease des hepatitis c-virus mit stickstoffhaltigen zyklischen p2-gruppen
SK14952002A3 (sk) * 2000-04-19 2003-03-04 Schering Corporation Makrocyklické zlúčeniny, farmaceutický prostriedok s ich obsahom a ich použitie
WO2002002546A1 (en) 2000-06-30 2002-01-10 Seikagaku Corporation EPOXYCARBOXYLIC ACID AMIDES, AZIDES AND AMINO ALCOHOLS AND PROCESSES FOR PREPARATION OF α-KETO AMIDES BY USING THEM
EP1322325A4 (en) 2000-07-20 2004-09-15 Merck & Co Inc INHIBITION OF PROCESSING AND REPLICATION OF HEPATITIS C VIRUS
RU2355700C9 (ru) 2000-07-21 2010-03-20 Шеринг Корпорейшн Новые пептиды как ингибиторы ns3-серинпротеазы вируса гепатита с
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
NZ523781A (en) 2000-07-21 2004-10-29 Corvas Int Inc Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
EP1301527A2 (en) 2000-07-21 2003-04-16 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
AR029851A1 (es) * 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
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
JP2002198723A (ja) * 2000-11-02 2002-07-12 Ace Technol Co Ltd 広帯域指向性アンテナ
US6602718B1 (en) 2000-11-08 2003-08-05 Becton, Dickinson And Company Method and device for collecting and stabilizing a biological sample
AU2002248147B2 (en) 2000-11-20 2006-04-06 Bristol-Myers Squibb Company Hepatitis C tripeptide inhibitors
HUP0303436A2 (hu) 2000-12-12 2004-01-28 Schering Corp. Diaril-peptidek mint a hepatitis C vírus NS3-szerin proteáz inhibitorai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
WO2002048157A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
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
JP4848528B2 (ja) 2000-12-28 2011-12-28 株式会社Ihi イオン質量分離方法及び装置、並びにイオンドーピング装置
CN1267446C (zh) 2001-01-22 2006-08-02 默克公司 作为依赖于rna的rna病毒聚合酶的抑制剂的核苷衍生物
GB0102342D0 (en) 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
CA2436518A1 (en) 2001-01-30 2002-08-08 Vertex Pharmaceuticals Incorporated A quantitative assay for nucleic acids
EP1381673B1 (en) 2001-03-27 2009-05-13 Vertex Pharmaceuticals Incorporated Compositions and methods useful for hcv infection
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
CA2450545A1 (en) 2001-07-03 2003-01-16 Altana Pharma Ag Process for the production of 3-phenylisoserine
KR100926244B1 (ko) * 2001-07-11 2009-11-12 버텍스 파마슈티칼스 인코포레이티드 브릿지된 바이사이클릭 세린 프로테아제 억제제
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
EP1441720B8 (en) * 2001-10-24 2012-03-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4a protease, incorporating a fused ring system
AU2002360386A1 (en) 2001-11-14 2003-06-17 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
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
CA2369970A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
AR038375A1 (es) 2002-02-01 2005-01-12 Pfizer Prod Inc Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo
MXPA04009938A (es) * 2002-04-11 2004-12-13 Vertex Pharma Inhibidores de serina proteasas, en particular la proteasa ns3-ns4a del hcv.
KR100838333B1 (ko) 2002-04-25 2008-06-13 오노 야꾸힝 고교 가부시키가이샤 디케토히드라진 유도체 화합물 및 그 화합물을 유효성분으로서 함유하는 약제
MXPA05001298A (es) 2002-08-01 2005-11-04 Pharmasset Inc Compuestos con el sistema biciclo[4.2.1] nonano para el tratamiento de infecciones por flaviviridae.
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
JP2006517960A (ja) 2003-02-18 2006-08-03 ファイザー インコーポレイテッド C型肝炎ウイルスの阻害剤、それを使用する組成物および治療法
EP1601685A1 (en) 2003-03-05 2005-12-07 Boehringer Ingelheim International GmbH Hepatitis c inhibiting compounds
WO2004101602A2 (en) 2003-03-05 2004-11-25 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor peptide analogs
EP1613620A1 (en) * 2003-04-11 2006-01-11 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
CA2521678A1 (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.
CN102020700A (zh) * 2003-07-18 2011-04-20 沃泰克斯药物股份有限公司 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂
WO2005018330A1 (en) 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
PE20050374A1 (es) 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
CA2538843A1 (en) 2003-09-12 2005-03-24 Vertex Pharmaceuticals Incorporated Animal model for protease activity and liver damage
TW200526686A (en) * 2003-09-18 2005-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US6933760B2 (en) 2003-09-19 2005-08-23 Intel Corporation Reference voltage generator for hysteresis circuit
US7642235B2 (en) 2003-09-22 2010-01-05 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
EP1692157B1 (en) * 2003-10-10 2013-04-17 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AR045870A1 (es) 2003-10-11 2005-11-16 Vertex Pharma Terapia de combinacion para la infeccion de virus de hepatitis c
EP1677827B1 (en) 2003-10-27 2008-12-10 Vertex Pharmaceuticals Incorporated Combinations for hcv treatment
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
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
AU2004285972A1 (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
AU2004295702A1 (en) 2003-12-01 2005-06-16 Vertex Pharmaceuticals Incorporated Compositions comprising fetal liver cells and methods useful for HCV infection
CA2549851C (en) 2004-01-21 2012-09-11 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis c virus
CN1938332B (zh) 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂
KR20120091276A (ko) 2004-02-20 2012-08-17 베링거 인겔하임 인터내셔날 게엠베하 바이러스 폴리머라제 억제제
US20050187192A1 (en) 2004-02-20 2005-08-25 Kucera Pharmaceutical Company Phospholipids for the treatment of infection by togaviruses, herpes viruses and coronaviruses
CN1946692A (zh) 2004-02-27 2007-04-11 先灵公司 作为丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的3,4-(环戊基)-稠合的脯氨酸化合物
CA2768700C (en) 2004-03-12 2014-04-29 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
WO2005107745A1 (en) 2004-05-06 2005-11-17 Schering Corporation An inhibitor of 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
CN102160891A (zh) * 2004-10-01 2011-08-24 威特克斯医药股份有限公司 Hcv ns3-ns4a蛋白酶抑制
TWI437990B (zh) * 2004-10-29 2014-05-21 Vertex Pharma Vx-950之醫藥用途
US7863274B2 (en) 2005-07-29 2011-01-04 Concert Pharmaceuticals Inc. Deuterium enriched analogues of tadalafil as PDE5 inhibitors
RU2441020C2 (ru) * 2005-08-02 2012-01-27 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы серинпротеазы
PT1934179E (pt) * 2005-08-19 2010-07-12 Vertex Pharma PROCESSOS E INTERMEDIáRIOS
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
EP1991229A2 (en) 2006-02-27 2008-11-19 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
EP2194039A1 (en) 2006-03-16 2010-06-09 Vertex Pharmceuticals Incorporated Process for preparing optically enriched compounds
MX2008011869A (es) 2006-03-16 2008-12-03 Vertex Pharma Procedimientos e intermediarios para preparar compuestos estericos.
NZ571934A (en) 2006-03-20 2012-05-25 Vertex Pharma Methods of spray drying formulations of vx-950 (telaprevir)
AU2007226983A1 (en) 2006-03-20 2007-09-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
US7651520B2 (en) * 2006-05-30 2010-01-26 Ostial Solutions, Llc Means and method for the accurate placement of a stent at the ostium of an artery
EP2037887B1 (en) 2006-05-31 2010-09-15 Vertex Pharmaceuticals Incorporated Oral controlled release formulations of an interleukin-1 beta converting enzyme inhibitor
US7708294B2 (en) 2006-11-02 2010-05-04 Gm Global Technology Operations, Inc. Detachable dual-use platform apparatus and method
CN101903392A (zh) 2007-02-27 2010-12-01 弗特克斯药品有限公司 丝氨酸蛋白酶的抑制剂
US7910587B2 (en) * 2007-04-26 2011-03-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl dipeptide hepatitis C virus inhibitors
US7959488B2 (en) * 2007-10-15 2011-06-14 Tania Alessandra Talamo Brassiere pad system

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