IL173627A0 - 2-amido-4-aryloxy-1-carbonylpyrrolidine derivatives and pharmaceutical compositions containing the same - Google Patents

2-amido-4-aryloxy-1-carbonylpyrrolidine derivatives and pharmaceutical compositions containing the same

Info

Publication number
IL173627A0
IL173627A0 IL173627A IL17362706A IL173627A0 IL 173627 A0 IL173627 A0 IL 173627A0 IL 173627 A IL173627 A IL 173627A IL 17362706 A IL17362706 A IL 17362706A IL 173627 A0 IL173627 A0 IL 173627A0
Authority
IL
Israel
Prior art keywords
carbonylpyrrolidine
amido
aryloxy
derivatives
same
Prior art date
Application number
IL173627A
Other languages
English (en)
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 IL173627A0 publication Critical patent/IL173627A0/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION 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
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/60—1,4-Diazines; Hydrogenated 1,4-diazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing 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
    • C04B35/632—Organic additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides 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)4-C(=0), e.g. 'isosters', replacing two amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Manufacturing & Machinery (AREA)
  • Ceramic Engineering (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Inorganic Chemistry (AREA)
  • Materials Engineering (AREA)
  • Structural Engineering (AREA)
  • Dentistry (AREA)
  • Environmental Sciences (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • AIDS & HIV (AREA)
  • Gastroenterology & Hepatology (AREA)
IL173627A 2003-09-05 2006-02-09 2-amido-4-aryloxy-1-carbonylpyrrolidine derivatives and pharmaceutical compositions containing the same IL173627A0 (en)

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
IL173627A0 true IL173627A0 (en) 2006-07-05

Family

ID=34434831

Family Applications (1)

Application Number Title Priority Date Filing Date
IL173627A IL173627A0 (en) 2003-09-05 2006-02-09 2-amido-4-aryloxy-1-carbonylpyrrolidine derivatives and pharmaceutical compositions containing the same

Country Status (19)

Country Link
US (4) US7378422B2 (enExample)
EP (2) EP1667998A2 (enExample)
JP (2) JP4767852B2 (enExample)
KR (2) KR20120051751A (enExample)
CN (2) CN1845920B (enExample)
AR (1) AR045596A1 (enExample)
AU (1) AU2004279800B9 (enExample)
BR (1) BRPI0414176A (enExample)
CA (1) CA2536436C (enExample)
IL (1) IL173627A0 (enExample)
MX (1) MXPA06002476A (enExample)
MY (1) MY148123A (enExample)
NO (1) NO20061426L (enExample)
NZ (2) NZ580205A (enExample)
PE (1) PE20050374A1 (enExample)
RU (2) RU2440368C2 (enExample)
TW (2) TW201127828A (enExample)
UY (1) UY28500A1 (enExample)
WO (1) WO2005035525A2 (enExample)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1133649C (zh) 1996-10-18 2004-01-07 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3蛋白酶的抑制剂
ATE297946T1 (de) * 2000-04-03 2005-07-15 Vertex Pharma Inhibitoren von serin proteasen, speziell der 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
PT1599468E (pt) 2003-01-14 2008-01-14 Arena Pharm Inc Derivados de arilo e heteroarilo 1,2,3.-trissubstituídos comomoduladores do metabolismo, e profilaxia e tratamento dedesordens relacionadas tais como diabetes e hiperglicemia
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
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP1664091A1 (en) 2003-09-18 2006-06-07 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
KR20060130027A (ko) * 2003-10-10 2006-12-18 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 ｈｃｖ ｎｓ3-ｎｓ4ａ 프로테아제의억제제
US7365092B2 (en) * 2003-10-10 2008-04-29 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
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
NZ563909A (en) 2005-05-13 2011-10-28 Virochem Pharma Inc Thiophene derivatives and their use for the treatment or prevention of flavivirus infections
ES2572980T3 (es) * 2005-06-02 2016-06-03 Merck Sharp & Dohme Corp. Combinación de inhibidores de la proteasa del VHC con un tensioactivo
TWI449711B (zh) * 2005-06-30 2014-08-21 Virobay Inc Ｃ型肝炎病毒（ｈｃｖ）抑制劑
US7608592B2 (en) 2005-06-30 2009-10-27 Virobay, Inc. HCV inhibitors
GEP20105124B (en) * 2005-07-25 2010-11-25 Array Biopharma Inc Novel macrocyclic inhibitors of hepatitis c virus replication
EP2402331A1 (en) * 2005-08-02 2012-01-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
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
BRPI0617274A2 (pt) 2005-10-11 2011-07-19 Intermune Inc compostos e métodos para a inibição de replicação viral de hepatite c
US8183413B2 (en) * 2006-01-20 2012-05-22 Kaneka Corporation Process for production of β-amino-α-hydroxy carboxamide derivative
US20090304631A1 (en) * 2006-01-27 2009-12-10 David Alan Campbell Hepatitis c serine protease inhibitors and uses therefor
US8039475B2 (en) 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
KR20080112303A (ko) 2006-03-16 2008-12-24 버텍스 파마슈티칼스 인코포레이티드 중수소화 ｃ형 간염 프로테아제 억제제
WO2007111866A2 (en) * 2006-03-23 2007-10-04 Schering Corporation Combinations of hcv protease inhibitor(s) and cyp3a4 inhibitor(s), and methods of treatment related thereto
KR101059593B1 (ko) 2006-04-11 2011-08-25 노파르티스 아게 Ｈｃｖ/ｈｉｖ 억제제 및 이들의 용도
WO2007137080A2 (en) 2006-05-23 2007-11-29 Irm Llc Compounds and compositions as channel activating protease inhibitors
US7834190B2 (en) * 2006-05-26 2010-11-16 Kaneka Corporation Process for production of optically active-3-amino-2-hydroxypropionic cyclopropylamide derivatives and salts thereof
RU2008152171A (ru) 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
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
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
US20090098085A1 (en) * 2006-08-11 2009-04-16 Ying Sun Tetrazolyl acyclic hepatitis c serine protease inhibitors
NZ576780A (en) 2006-11-15 2011-12-22 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
BRPI0807483A2 (pt) 2007-02-09 2014-05-13 Irm Llc Compostos e composições como inibidores de protease de ativação de canal
PT2114924E (pt) * 2007-02-27 2012-04-03 Vertex Pharma Co-cristais e composições farmacêuticas que compreendem os mesmos
EP2134717A2 (en) * 2007-02-27 2009-12-23 Vertex Pharmceuticals Incorporated Inhibitors of serine proteases
US7910587B2 (en) * 2007-04-26 2011-03-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl dipeptide hepatitis C virus inhibitors
US20080317712A1 (en) * 2007-04-26 2008-12-25 Deqiang Niu Arylpiperidinyl and arylpyrrolidinyl tripeptide hepatitis c serine protease inhibitors
US20080292587A1 (en) * 2007-04-26 2008-11-27 Ying Sun Oximyl dipeptide hepatitis c protease inhibitors
WO2008137779A2 (en) * 2007-05-03 2008-11-13 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
MX2009012093A (es) 2007-05-10 2010-01-25 Intermune Inc Nuevos peptidos inhibidores de la replicacion del virus de la hepatitis c.
JP5443360B2 (ja) 2007-08-30 2014-03-19 バーテックス ファーマシューティカルズ インコーポレイテッド 共結晶体およびそれを含む医薬組成物
JP5095824B2 (ja) 2007-10-10 2012-12-12 ノバルティス アーゲー スピロピロリジン類およびｈｃｖおよびｈｉｖ感染に対するその使用
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
MX2010008109A (es) * 2008-01-24 2010-09-22 Enanta Pharm Inc Tripéptidos difluorizados como inhibidores de proteasa de serina de virus de hepatitis c (hcv).
TW200936131A (en) * 2008-02-04 2009-09-01 Idenix Pharmaceuticals Inc Macrocyclic serine protease inhibitors
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
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
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
AU2010326225A1 (en) 2009-11-25 2012-06-07 Vertex Pharmaceuticals Incorporated 5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections
CA2784036A1 (en) 2009-12-24 2011-06-30 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
WO2011119860A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
WO2011119858A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
CA2794145A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
AU2011232348A1 (en) 2010-03-24 2012-10-11 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of Flavivirus infections
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
WO2012006070A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
EP2585448A1 (en) 2010-06-28 2013-05-01 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
MX2012014918A (es) 2010-06-28 2013-04-08 Vertex Pharma Compuestos y metodos para tratamiento o prevencion de infecciones por flavivirus.
AU2011292040A1 (en) 2010-08-17 2013-03-07 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of Flaviviridae viral infections
JP5941916B2 (ja) 2010-09-22 2016-06-29 アリーナ ファーマシューティカルズ， インコーポレイテッド Ｇｐｒ１１９レセプターのモジュレーターおよびそれに関連する障害の処置
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
WO2013016499A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Methods for preparation of thiophene compounds
WO2013016501A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Formulations of thiophene compounds
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
WO2013123456A1 (en) 2012-02-16 2013-08-22 Rqx Pharmaceuticals, Inc. Linear peptide antibiotics
NZ630805A (en) 2012-03-22 2016-01-29 Alios Biopharma Inc Pharmaceutical combinations comprising 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
PL3242666T3 (pl) 2015-01-06 2025-02-17 Arena Pharmaceuticals, Inc. Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1
DK3310760T3 (da) 2015-06-22 2022-10-24 Arena Pharm Inc Krystallinsk L-argininsalt af (R)-2-(7-(4-cyclopentyl-3-(trifluormethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3- yl)eddikesyre til anvendelse ved S1P1-receptor-associerede lidelser
HK1257565A1 (zh) 2016-03-04 2019-10-25 豪夫迈‧罗氏有限公司 作为htra1抑制剂的新型三氟甲基丙酰胺衍生物
CN108699105A (zh) 2016-03-04 2018-10-23 豪夫迈·罗氏有限公司 作为htra1抑制剂的新型二氟酮酰胺衍生物
WO2017222915A1 (en) 2016-06-21 2017-12-28 Inception 4, Inc. Heterocyclic prolinamide derivatives
EP3472151A4 (en) 2016-06-21 2020-03-04 Orion Ophthalmology LLC CARBOCYCLIC PROLINAMIDE DERIVATIVES
EP3484859B1 (en) 2016-07-18 2021-09-15 F. Hoffmann-La Roche AG New difluoroketamide derivatives as htra1 inhibitors
CN109563084A (zh) * 2016-08-23 2019-04-02 豪夫迈·罗氏有限公司 作为htra1抑制剂的新型三氟甲基丙酰胺衍生物
CN109661389A (zh) 2016-08-23 2019-04-19 豪夫迈·罗氏有限公司 作为htra1抑制剂的新型二氟酮酰胺衍生物
CN110520124A (zh) 2017-02-16 2019-11-29 艾尼纳制药公司 用于治疗原发性胆汁性胆管炎的化合物和方法
BR112020024762A2 (pt) 2018-06-06 2021-03-23 Arena Pharmaceuticals, Inc. métodos de tratamento de condições relacionadas ao receptor s1p1
KR102835299B1 (ko) 2018-12-04 2025-07-18 브리스톨-마이어스 스큅 컴퍼니 다중 동위원소체 반응 모니터링에 의한 샘플내 보정 곡선을 사용한 분석 방법
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
KR20250099192A (ko) 2022-11-09 2025-07-01 베링거 인겔하임 인터내셔날 게엠베하 cGAS 억제제로서 사이클릭 피리딘 유도체

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
CA1341029C (en) 1985-02-04 2000-06-20 Michael Kolb 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
EP0564561A4 (en) 1990-12-28 1994-08-10 Georgia Tech Res Inst Peptides ketoamides, ketoacids, and ketoesters
EP0644892A1 (en) 1992-06-12 1995-03-29 Pfizer Inc. Inhibitors of angiotensin i chymase(s) including human heart chymase
US5371072A (en) 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
ES2150933T3 (es) * 1992-12-22 2000-12-16 Lilly Co Eli Inhibidores de la proteasa vih utiles para el tratamiento del sida.
DE674513T1 (de) 1992-12-29 1996-01-18 Abbott Lab Inhibitoren der retroviralen protease.
US5384410A (en) * 1993-03-24 1995-01-24 The Du Pont Merck Pharmaceutical Company Removal of boronic acid protecting groups by transesterification
US5656600A (en) 1993-03-25 1997-08-12 Corvas International, Inc. α-ketoamide derivatives as inhibitors of thrombosis
US5672582A (en) 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
IL110752A (en) 1993-09-13 2000-07-26 Abbott Lab Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor
US5559158A (en) 1993-10-01 1996-09-24 Abbott Laboratories Pharmaceutical composition
US5468858A (en) 1993-10-28 1995-11-21 The Board Of Regents Of Oklahoma State University Physical Sciences N-alkyl and n-acyl derivatives of 3,7-diazabicyclo-[3.3.1]nonanes and selected salts thereof as multi-class antiarrhythmic agents
IL111991A (en) 1994-01-28 2000-07-26 Abbott Lab Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent
RU95104898A (ru) 1994-03-31 1996-12-27 Бристоль-Мейерз Сквибб Компани (US) Имидазолсодержащие ингибиторы фарнезид-протеинтрансферазы, способ лечения связанных с ней заболеваний
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
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
JP2000500760A (ja) 1995-11-23 2000-01-25 メルク シヤープ エンド ドーム リミテツド スピロピペリジン誘導体およびタキキニン拮抗薬としてのその使用
AU728373B2 (en) 1995-12-07 2001-01-11 Scripps Research Institute, The 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
AU723730B2 (en) 1996-04-23 2000-09-07 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
JPH11513890A (ja) 1996-05-10 1999-11-30 シェーリング コーポレイション Ｃ型肝炎ウイルスｎｓ３プロテアーゼの合成インヒビター
US6153579A (en) 1996-09-12 2000-11-28 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
ATE320432T1 (de) 1996-09-25 2006-04-15 Merck Sharp & Dohme Spiro-azacyclische derivate, deren herstellung und verwendung als tachykinin-antagonisten
AU4898797A (en) 1996-10-08 1998-05-05 Colorado State University Research Foundation Catalytic asymmetric epoxidation
CN1133649C (zh) * 1996-10-18 2004-01-07 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3蛋白酶的抑制剂
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
DE19648011A1 (de) 1996-11-20 1998-05-28 Bayer Ag Cyclische Imine
DE19648793A1 (de) 1996-11-26 1998-05-28 Basf Ag Neue Benzamide und deren Anwendung
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
US6767991B1 (en) 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
EP1003775B1 (en) 1997-08-11 2005-03-16 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor peptides
US6143715A (en) 1997-08-11 2000-11-07 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptide analogues
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
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
EP1066247B1 (en) 1998-03-31 2006-11-22 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
US6251583B1 (en) 1998-04-27 2001-06-26 Schering Corporation Peptide substrates for HCV NS3 protease assays
GB9812523D0 (en) 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
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
EP1027885B1 (en) 1999-02-09 2008-07-09 Pfizer Products Inc. Basic drug compositions with enhanced bioavailability
US20020042046A1 (en) 1999-02-25 2002-04-11 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
CN1196687C (zh) 1999-03-19 2005-04-13 沃泰克斯药物股份有限公司 Impdh酶抑制剂
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
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
WO2001007407A1 (en) 1999-07-26 2001-02-01 Bristol-Myers Squibb Pharma Company Lactam inhibitors of hepatitis c virus ns3 protease
WO2001016300A2 (en) 1999-08-31 2001-03-08 Basf Aktiengesellschaft Method of identifying inhibitors of cdc25
US20020183249A1 (en) 1999-08-31 2002-12-05 Taylor Neil R. Method of identifying inhibitors of CDC25
GB9925955D0 (en) 1999-11-02 1999-12-29 Angeletti P Ist Richerche Bio Hcv n33 protease inhibitors
WO2001040262A1 (en) * 1999-12-03 2001-06-07 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
AU2001234837A1 (en) 2000-02-08 2001-08-20 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
ATE297946T1 (de) * 2000-04-03 2005-07-15 Vertex Pharma Inhibitoren von serin proteasen, speziell der hepatitis-c-virus ns3-protease
HK1047947A1 (zh) 2000-04-05 2003-03-14 Schering Corporation 包含n-环状p2部分的丙型肝炎病毒的大环ns3-丝氨酸蛋白酶抑制剂
PE20011288A1 (es) * 2000-04-19 2001-12-12 Schering Corp Compuestos macrociclicos como inhibidores de la serina proteasa ns3/ns4 del virus de la hepatitis c (vhc)
AU2001267886A1 (en) 2000-06-30 2002-01-14 Seikagaku Corporation Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them
JP2004504356A (ja) 2000-07-20 2004-02-12 メルク　エンド　カムパニー　インコーポレーテッド Ｃ型肝炎ウイルスのプロセシングおよび複製の抑制
CZ2003195A3 (cs) 2000-07-21 2003-04-16 Schering Corporation Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostředek
EP1301527A2 (en) 2000-07-21 2003-04-16 Corvas International, Inc. 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
AR034127A1 (es) 2000-07-21 2004-02-04 Schering Corp Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento
AR029851A1 (es) * 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
SI1385870T1 (sl) 2000-07-21 2010-08-31 Schering Corp Peptidi kot NS3-serin proteazni inhibitorji virusa hepatitisa 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
WO2002060926A2 (en) 2000-11-20 2002-08-08 Bristol-Myers Squibb Company Hepatitis c tripeptide inhibitors
IL155842A0 (en) 2000-12-12 2003-12-23 Schering Corp Diaryl peptides as ns3-serine protease inhibitors of hepatitis c virus
US6653295B2 (en) 2000-12-13 2003-11-25 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
US6727366B2 (en) 2000-12-13 2004-04-27 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis C virus NS3 protease inhibitors
AU2002230763A1 (en) 2000-12-13 2008-01-03 Bristol-Myers Squibb Pharma 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
SK286630B6 (sk) 2001-01-22 2009-02-05 Merck & Co., Inc. Nukleozidové deriváty, farmaceutický prostriedok s ich obsahom a ich použitie
EP1356123A2 (en) 2001-01-30 2003-10-29 Vertex Pharmaceuticals Incorporated A quantitative assay for nucleic acids
GB0102342D0 (en) 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
CA2441688C (en) 2001-03-27 2014-01-21 Vertex Pharmaceuticals Incorporated Compositions and methods useful for hcv infection
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
EP1463699A2 (en) 2001-07-03 2004-10-06 ALTANA Pharma AG Process for the production of 3-phenylisoserine
DE60217114T2 (de) * 2001-07-11 2007-10-25 Vertex Pharmaceuticals Inc., Cambridge Verbrückte bizyklische serinproteaseinhibitoren
JP2003055389A (ja) 2001-08-09 2003-02-26 Univ Tokyo 錯体及びそれを用いたエポキシドの製法
US6824769B2 (en) 2001-08-28 2004-11-30 Vertex Pharmaceuticals Incorporated Optimal compositions and methods thereof for treating HCV infections
NZ531681A (en) * 2001-10-24 2007-05-31 Vertex Pharma Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system
KR20050044450A (ko) 2001-11-14 2005-05-12 테바 파마슈티컬 인더스트리즈 리미티드 로사르탄 칼륨의 무정형 및 결정형 형태 및 이의 제조 방법
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
AR038375A1 (es) 2002-02-01 2005-01-12 Pfizer Prod Inc Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo
US6642204B2 (en) 2002-02-01 2003-11-04 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
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
PL373399A1 (en) * 2002-04-11 2005-08-22 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
BR0309670A (pt) 2002-04-25 2005-03-15 Ono Pharmaceutical Co Compostos derivados dicetohidrazina e drogas contendo os compostos como o ingrediente ativo
CA2494340C (en) 2002-08-01 2012-01-24 Pharmasset Inc. Compounds with the bicyclo[4.2.1]nonane system for the treatment of flaviviridae infections
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
CA2413705A1 (en) 2002-12-06 2004-06-06 Raul Altman Use of meloxicam in combination with an antiplatelet agent for treatment of acute coronary syndrome and related conditions
US7601709B2 (en) 2003-02-07 2009-10-13 Enanta Pharmaceuticals, Inc. Macrocyclic hepatitis C serine protease inhibitors
US7098231B2 (en) 2003-01-22 2006-08-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US7223785B2 (en) 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US20040180815A1 (en) 2003-03-07 2004-09-16 Suanne Nakajima Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
WO2004073599A2 (en) 2003-02-18 2004-09-02 Pfizer Inc. Inhibitors of hepatitis c virus, compositions and treatments using the same
US6908901B2 (en) 2003-03-05 2005-06-21 Boehringer Ingelheim International, Gmbh Hepatitis C inhibitor peptide analogs
CA2516016C (en) 2003-03-05 2012-05-29 Boehringer Ingelheim International Gmbh Hepatitis c inhibiting compounds
JP2006526011A (ja) * 2003-04-11 2006-11-16 バーテックス　ファーマシューティカルズ　インコーポレイテッド セリンプロテアーゼ（特に、ｈｃｖｎｓ３−ｎｓ４ａプロテアーゼ）のインヒビター
ES2297424T3 (es) 2003-05-21 2008-05-01 Boehringer Ingelheim International Gmbh Compuestos inhibidores de la hepatitis c.
CN102020700A (zh) * 2003-07-18 2011-04-20 沃泰克斯药物股份有限公司 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂
WO2005018330A1 (en) 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
NZ545871A (en) 2003-09-12 2010-04-30 Vertex Pharma Animal model for protease activity and liver damage
EP1664091A1 (en) 2003-09-18 2006-06-07 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US6933760B2 (en) 2003-09-19 2005-08-23 Intel Corporation Reference voltage generator for hysteresis circuit
ES2361997T3 (es) 2003-09-22 2011-06-27 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos activos contra el virus de la hepatitis c.
US7365092B2 (en) * 2003-10-10 2008-04-29 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
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
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1677827B1 (en) 2003-10-27 2008-12-10 Vertex Pharmaceuticals Incorporated Combinations for hcv treatment
US7494660B2 (en) 2003-10-27 2009-02-24 Vertex Pharmaceuticals Incorporated HCV NS3-NS4A protease resistance mutants
CN1894211A (zh) 2003-10-28 2007-01-10 沃泰克斯药物股份有限公司 借助费歇尔－芬克型合成和随后的酰化制备4,5－二烷基－3－酰基－吡咯－2－羧酸衍生物
US20050119318A1 (en) 2003-10-31 2005-06-02 Hudyma Thomas W. Inhibitors of HCV replication
US7132504B2 (en) 2003-11-12 2006-11-07 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2005054450A1 (en) 2003-12-01 2005-06-16 Vertex Pharmaceuticals Incorporated Compositions comprising fetal liver cells and methods useful for hcv infection
WO2005070955A1 (en) 2004-01-21 2005-08-04 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis c virus
CN1938332B (zh) * 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂
SG184700A1 (en) 2004-02-20 2012-10-30 Boehringer Ingelheim Int Viral polymerase inhibitors
US20050187192A1 (en) 2004-02-20 2005-08-25 Kucera Pharmaceutical Company Phospholipids for the treatment of infection by togaviruses, herpes viruses and coronaviruses
US7342041B2 (en) 2004-02-27 2008-03-11 Schering Corporation 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease
CA2559303C (en) 2004-03-12 2013-09-10 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
AR049635A1 (es) 2004-05-06 2006-08-23 Schering Corp (1r,2s,5s)-n-((1s)-3-amino-1-(ciclobutilmetil)-2,3-dioxopropil)-3-((2s)-2-((((1,1-dimetiletil)amino)carbonil)amino)-3,3-dimetil-1-oxobutil)-6,6-dimetil-3-azabiciclo(3.1.0)hexan-2-carboxamida como inhibidor de la ns3/ns4a serina proteasa del virus de la hepatitis c
EP1765283A4 (en) * 2004-06-08 2012-11-28 Vertex Pharma PHARMACEUTICAL COMPOSITIONS
CN101068828A (zh) 2004-08-27 2007-11-07 先灵公司 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的酰基磺酰胺化合物
JP2008514723A (ja) * 2004-10-01 2008-05-08 バーテックス ファーマシューティカルズ インコーポレイテッド Ｈｃｖｎｓ３−ｎｓ４ａプロテアーゼの阻害
MY141025A (en) * 2004-10-29 2010-02-25 Vertex Pharma Dose forms
US7863274B2 (en) 2005-07-29 2011-01-04 Concert Pharmaceuticals Inc. Deuterium enriched analogues of tadalafil as PDE5 inhibitors
EP2402331A1 (en) * 2005-08-02 2012-01-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
DE602006013492D1 (de) * 2005-08-19 2010-05-20 Vertex Pharma Verfahren und zwischenprodukte
AR055395A1 (es) * 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
US7964624B1 (en) 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
US7705138B2 (en) * 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
US8039475B2 (en) 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
KR20080112303A (ko) 2006-03-16 2008-12-24 버텍스 파마슈티칼스 인코포레이티드 중수소화 ｃ형 간염 프로테아제 억제제
NZ571281A (en) 2006-03-16 2011-11-25 Vertex Pharma Processes and intermediates for preparing steric compounds
NZ571934A (en) 2006-03-20 2012-05-25 Vertex Pharma Methods of spray drying formulations of vx-950 (telaprevir)
US20070218138A1 (en) 2006-03-20 2007-09-20 Bittorf Kevin J 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
ATE481089T1 (de) 2006-05-31 2010-10-15 Vertex Pharma Orale formulierungen mit kontrollierter freisetzung eines interleukin-1-beta-converting- enzyme inhibitors
US7708294B2 (en) 2006-11-02 2010-05-04 Gm Global Technology Operations, Inc. Detachable dual-use platform apparatus and method
EP2134717A2 (en) 2007-02-27 2009-12-23 Vertex Pharmceuticals Incorporated Inhibitors of serine proteases
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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CA2536436A1 (en) 2005-04-21
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