CN102372764A - 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽 - Google Patents

用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽 Download PDF

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Publication number
CN102372764A
CN102372764A CN2011102287110A CN201110228711A CN102372764A CN 102372764 A CN102372764 A CN 102372764A CN 2011102287110 A CN2011102287110 A CN 2011102287110A CN 201110228711 A CN201110228711 A CN 201110228711A CN 102372764 A CN102372764 A CN 102372764A
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CN
China
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mmol
solution
concentrated
compound
added
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CN2011102287110A
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English (en)
Chinese (zh)
Inventor
A·K·萨克塞纳
V·M·吉里亚瓦拉班
R·G·洛维
E·E·尧
F·本尼特
J·L·麦克科尔米克
H·王
R·E·皮克
S·L·伯根
覃天佑
刘怡宗
朱昭宁
F·G·恩约罗格
A·阿拉萨潘
T·N·帕雷克
A·K·甘古利
陈新海
S·文卡特拉曼
H·A·瓦卡罗
P·A·平托
B·桑塔纳姆
W·吴
S·亨德拉塔
Y·黄
S·J·坎普
O·E·莱维
M·利姆-维尔比
S·Y·塔穆拉
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
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Schering Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22822095&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102372764(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of CN102372764A publication Critical patent/CN102372764A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides 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)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CN2011102287110A 2000-07-21 2001-07-19 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽 Pending CN102372764A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22010800P 2000-07-21 2000-07-21
US60/220108 2000-07-21

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CNA018131115A Division CN1498224A (zh) 2000-07-21 2001-07-19 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽

Publications (1)

Publication Number Publication Date
CN102372764A true CN102372764A (zh) 2012-03-14

Family

ID=22822095

Family Applications (3)

Application Number Title Priority Date Filing Date
CN2011102287110A Pending CN102372764A (zh) 2000-07-21 2001-07-19 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
CNA018131115A Pending CN1498224A (zh) 2000-07-21 2001-07-19 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
CN2011100651916A Expired - Fee Related CN102206247B (zh) 2000-07-21 2001-07-19 一种具有HCV NS3/NS4a蛋白酶抑制活性的化合物

Family Applications After (2)

Application Number Title Priority Date Filing Date
CNA018131115A Pending CN1498224A (zh) 2000-07-21 2001-07-19 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
CN2011100651916A Expired - Fee Related CN102206247B (zh) 2000-07-21 2001-07-19 一种具有HCV NS3/NS4a蛋白酶抑制活性的化合物

Country Status (31)

Country Link
US (4) US7012066B2 (https=)
EP (1) EP1385870B1 (https=)
JP (3) JP4298289B2 (https=)
KR (2) KR100904788B1 (https=)
CN (3) CN102372764A (https=)
AR (2) AR033985A1 (https=)
AT (1) ATE461207T1 (https=)
AU (2) AU2001276988B2 (https=)
BR (1) BR0112540A (https=)
CA (1) CA2410662C (https=)
CY (2) CY1112267T1 (https=)
CZ (1) CZ303213B6 (https=)
DE (2) DE60141608D1 (https=)
DK (1) DK1385870T3 (https=)
EC (1) ECSP034438A (https=)
ES (1) ES2341534T3 (https=)
HU (1) HU229997B1 (https=)
IL (2) IL153670A0 (https=)
LU (1) LU91910I2 (https=)
MX (1) MXPA03000627A (https=)
MY (2) MY139078A (https=)
NO (2) NO332329B1 (https=)
NZ (1) NZ523782A (https=)
PL (1) PL206255B1 (https=)
PT (1) PT1385870E (https=)
RU (2) RU2355700C9 (https=)
SI (1) SI1385870T1 (https=)
SK (1) SK288064B6 (https=)
TW (1) TWI324611B (https=)
WO (1) WO2002008244A2 (https=)
ZA (1) ZA200210312B (https=)

Families Citing this family (276)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100509388B1 (ko) 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 ｃ 바이러스 ｎｓ３ 프로테아제의 저해제
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
DK1385870T3 (da) * 2000-07-21 2010-07-05 Schering Corp Peptider som inhibitorer af NS3-serinprotease fra hepatitis C-virus
US7244721B2 (en) * 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
GB2367816A (en) * 2000-10-09 2002-04-17 Bayer Ag Urea- and thiourea-containing derivatives of beta-amino acids
KR20030091946A (ko) * 2000-12-12 2003-12-03 쉐링 코포레이션 Ｃ형 간염 바이러스의 ｎｓ3-세린 프로테아제억제제로서의 디아릴 펩티드
US6989385B2 (en) 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2449504A1 (en) 2001-07-11 2003-01-23 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
US7241796B2 (en) 2001-10-24 2007-07-10 Vertex Pharmaceuticals Inc. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US6894072B2 (en) * 2002-01-23 2005-05-17 Schering Corporation Compounds as NS3-serine protease inhibitors of hepatitis C virus
US7119072B2 (en) 2002-01-30 2006-10-10 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis C virus
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
KR20040099425A (ko) * 2002-04-11 2004-11-26 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 ｃ형 간염 바이러스 ｎｓ3-ｎｓ4프로테아제의 억제제
MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
JP2006526011A (ja) 2003-04-11 2006-11-16 バーテックス　ファーマシューティカルズ　インコーポレイテッド セリンプロテアーゼ（特に、ｈｃｖｎｓ３−ｎｓ４ａプロテアーゼ）のインヒビター
AU2011203054B2 (en) * 2003-04-11 2012-04-26 Vertex Pharmaceuticals, Incorporated Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease
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.
CN100591662C (zh) * 2003-06-17 2010-02-24 先灵公司 制备3-(氨基)-3-环丁基甲基-2-羟基-丙酰胺或其盐的方法和中间体
ES2354817T3 (es) 2003-06-17 2011-03-18 Schering Corporation Procedimiento y productos intermedios para la preparación de 3-azabiciclo[3.1.0]hexano-2-carboxilatos de (1r,2s,5s)-6,6-dimetilo o sus sales.
AR044694A1 (es) * 2003-06-17 2005-09-21 Schering Corp Proceso y compuestos intermedios para la preparacion de (1r, 2s,5s) - 3 azabiciclo [3,1,0] hexano-2- carboxamida, n- [3- amino-1- (ciclobutilmetil) - 2, 3 - dioxopropil] -3- [ (2s) - 2 - [[ [ 1,1- dimetiletil] amino] carbonilamino] -3,3-dimetil -1- oxobutil]-6,6 dimetilo
CN1852920B (zh) 2003-07-18 2010-12-15 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
US7449447B2 (en) 2003-08-26 2008-11-11 Schering Corporation Peptidomimetic NS3-serine protease inhibitors of hepatitis C virus
TWI359147B (en) 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
EP1664091A1 (en) * 2003-09-18 2006-06-07 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
ES2361997T3 (es) 2003-09-22 2011-06-27 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos activos contra el virus de la hepatitis c.
RU2006113880A (ru) * 2003-09-26 2007-11-20 Шеринг Корпорейшн (US) Макроциклические ингибиторы сериновой протеиназы ns3 вируса гепатита с
WO2005037860A2 (en) 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incoporated 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
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
KR20060120166A (ko) 2003-10-27 2006-11-24 버텍스 파마슈티칼스 인코포레이티드 Ｈｃｖ ｎｓ３－ｎｓ４ａ 단백질분해효소 저항성 돌연변이
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
MXPA06005683A (es) 2003-11-20 2006-12-14 Schering Corp Inhibidores despeptidizados de la proteasa ns3 del virus de la hepatitis c.
WO2005058821A1 (en) * 2003-12-11 2005-06-30 Schering Corporation Inhibitors of hepatitis c virus ns3/ns4a serine protease
ATE495185T1 (de) 2004-01-21 2011-01-15 Boehringer Ingelheim Int Makrocyclische peptide mit wirkung gegen das hepatitis-c-virus
JP4902361B2 (ja) * 2004-01-30 2012-03-21 メディヴィル・アクチエボラーグ Ｈｃｖｎｓ−３セリンプロテアーゼインヒビター
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
US20070049593A1 (en) 2004-02-24 2007-03-01 Japan Tobacco Inc. Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor
PT1719773E (pt) 2004-02-24 2009-06-03 Japan Tobacco Inc Compostos heterotetracíclicos fundidos e a sua utilização como inibidores da polimerase do hcv
AU2005219859A1 (en) 2004-02-27 2005-09-15 Schering Corporation Inhibitors of hepatitis C virus NS3 protease
US7186747B2 (en) * 2004-02-27 2007-03-06 Schering Corporation Compounds as inhibitors of hepatitis C virus NS3 serine protease
US7816326B2 (en) 2004-02-27 2010-10-19 Schering Corporation Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease
JP4874227B2 (ja) * 2004-02-27 2012-02-15 シェーリング コーポレイション Ｃ型肝炎ウイルスのｎｓ３セリンプロテアーゼインヒビターとしての環状ｐ４’ｓを有する新規ケトアミド
CN1946691A (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化合物
US7635694B2 (en) 2004-02-27 2009-12-22 Schering Corporation Cyclobutenedione-containing compounds as inhibitors of hepatitis C virus NS3 serine protease
EP1737821B1 (en) 2004-02-27 2009-08-05 Schering Corporation 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis c virus ns3 serine protease
DE602005021760D1 (de) 2004-02-27 2010-07-22 Schering Corp Schwefelverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
EP1742914A1 (en) * 2004-02-27 2007-01-17 Schering Corporation Cyclobutenedione groups-containing compounds as inhibitors of hepatitis c virus ns3 serine protease
EP2399916B1 (en) * 2004-03-12 2014-12-10 Vertex Pharmaceuticals Incorporated Process and intermediates for the preparation of aspartic acetal caspase ihnhibitors
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
ES2328596T3 (es) * 2004-05-20 2009-11-16 Schering Corporation Prolinas sustituidas como inhibidores de la serina proteasa del virus ns3 de la hepatitis c.
UY29016A1 (es) 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
JP4914355B2 (ja) 2004-07-20 2012-04-11 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 Ｃ型肝炎インヒビターペプチド類似体
ATE513844T1 (de) 2004-08-27 2011-07-15 Schering Corp Acylsulfonamidverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
RU2007116265A (ru) 2004-10-01 2008-11-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибирование протеазы ns3-ns4a вируса hcv
SI1802650T1 (sl) * 2004-10-01 2012-03-30 Scynexis Inc Eter in tioeter substituirani ciklosporinski derivati za zdravljenje in preventivo pred infekcijami s hepatitisom c
US7196161B2 (en) * 2004-10-01 2007-03-27 Scynexis Inc. 3-ether and 3-thioether substituted cyclosporin derivatives for the treatment and prevention of hepatitis C infection
US7659263B2 (en) 2004-11-12 2010-02-09 Japan Tobacco Inc. Thienopyrrole compound and use thereof as HCV polymerase inhibitor
GB0426661D0 (en) * 2004-12-06 2005-01-05 Isis Innovation Pyrrolidine compounds
US20060276407A1 (en) * 2005-06-02 2006-12-07 Schering Corporation Methods of treating hepatitis C virus
AU2006252623A1 (en) * 2005-06-02 2006-12-07 Schering Corporation Controlled-release formulation useful for treating disorders associated with hepatitis C virus
US20060275366A1 (en) * 2005-06-02 2006-12-07 Schering Corporation Controlled-release formulation
WO2006130552A2 (en) * 2005-06-02 2006-12-07 Schering Corporation Methods of treating hepatitis c virus
WO2006130627A2 (en) * 2005-06-02 2006-12-07 Schering Corporation Methods for treating hepatitis c
NZ563365A (en) * 2005-06-02 2011-02-25 Schering Corp Combination of HCV protease inhibitors with a surfactant
US20070021351A1 (en) * 2005-06-02 2007-01-25 Schering Corporation Liver/plasma concentration ratio for dosing hepatitis C virus protease inhibitor
AU2006252519B2 (en) 2005-06-02 2012-08-30 Merck Sharp & Dohme Corp. HCV protease inhibitors in combination with food
US20060281689A1 (en) * 2005-06-02 2006-12-14 Schering Corporation Method for modulating activity of HCV protease through use of a novel HCV protease inhibitor to reduce duration of treatment period
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
US20110104109A1 (en) * 2005-07-13 2011-05-05 Frank Bennett Tetracyclic indole derivatives and their use for treating or preventing viral infections
MX2008001166A (es) 2005-07-25 2008-03-18 Intermune Inc Nuevos inhibidores macrociclicos de la replicacion del virus de hepatitis c.
JP5230416B2 (ja) 2005-07-29 2013-07-10 テイボテク・フアーマシユーチカルズ Ｃ型肝炎ウイルスの大員環状阻害剤
ES2373685T3 (es) 2005-07-29 2012-02-07 Tibotec Pharmaceuticals Inhibidores macrocíclicos del virus de la hepatitis c.
KR20080033481A (ko) * 2005-08-02 2008-04-16 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제의 억제제
PL385229A1 (pl) 2005-08-19 2008-09-29 Vertex Pharmaceuticals Incorporated Sposoby i związki pośrednie
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
EP1931696B1 (en) * 2005-09-30 2011-02-16 Scynexis, Inc. Arylalkyl and heteroarylalkyl derivatives of cyclosporine a for the treatment and prevention of viral infection
JP5517454B2 (ja) * 2005-09-30 2014-06-11 スシネキス インク Ｃ型肝炎感染の治療及び予防のための方法及び医薬組成物
AU2006301966A1 (en) 2005-10-11 2007-04-19 Array Biopharma, Inc. Compounds and methods for inhibiting hepatitis C viral replication
MX2008005814A (es) 2005-11-03 2008-10-15 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasa.
EP2392589A3 (en) 2005-11-11 2012-06-20 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
AR056805A1 (es) 2005-11-14 2007-10-24 Schering Corp Un proceso para oxidacion para la preparcion de n- (3- amino-1- ( ciclobutilmetil) -2,3- dioxopropil ) -3-(n-(( ter-butilamino) carbonil )-3- metil- l- valil) -6,6- dimetil-3- azabiciclo (3.1.0) hexano -2- carboxamida y compuestos ralacionados
WO2007075790A1 (en) * 2005-12-22 2007-07-05 Schering Corporation Process for the preparation of 6, 6-dimethyl-3-azabicyclo-[3.1.0]-hexane compounds and enantiomeric salts thereof
UA96283C2 (uk) 2005-12-23 2011-10-25 Зіланд Фарма А/С Модифіковані міметики лізину
US7816348B2 (en) 2006-02-03 2010-10-19 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
WO2007092645A2 (en) * 2006-02-09 2007-08-16 Schering Corporation Novel hcv inhibitor combinations and methods
MX2008010355A (es) * 2006-02-09 2008-10-31 Schering Corp Combinaciones que comprenden inhibidores de proteasa del virus de la hepatitis c e inhibidores de polimerasa del virus de la hepatitis c, y metodos de tratamiento relacionados con los mismos.
EP1991229A2 (en) 2006-02-27 2008-11-19 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
US20090220457A1 (en) * 2006-03-03 2009-09-03 Lahser Frederick C Combinations comprising hcv protease inhibitor(s) and hcv ires inhibitor(s), and methods of treatment related thereto
CN101460166B (zh) * 2006-03-06 2014-11-19 Abbvie公司 用于治疗c型肝炎病毒的利托那韦组合物及其用途
EP1993994A2 (en) 2006-03-16 2008-11-26 Vertex Pharmceuticals Incorporated Deuterated hepatitis c protease inhibitors
US20080045530A1 (en) * 2006-04-11 2008-02-21 Trixi Brandl Organic Compounds and Their Uses
EP2007789B1 (en) * 2006-04-11 2015-05-20 Novartis AG Spirocyclic HCV/HIV inhibitors and their uses
AR060385A1 (es) * 2006-04-11 2008-06-11 Novartis Ag Compuestos organicos y sus usos
US8017612B2 (en) 2006-04-18 2011-09-13 Japan Tobacco Inc. Piperazine compound and use thereof as a HCV polymerase inhibitor
US8420122B2 (en) 2006-04-28 2013-04-16 Merck Sharp & Dohme Corp. Process for the precipitation and isolation of 6,6-dimethyl-3-aza-bicyclo [3.1.0] hexane-amide compounds by controlled precipitation and pharmaceutical formulations containing same
CN101495095B (zh) * 2006-04-28 2013-05-29 默沙东公司 通过受控的沉淀来沉淀和分离6,6-二甲基-3-氮杂-双环[3.1.0]己烷-酰胺化合物的方法和含有其的药学制剂
US20080193518A1 (en) * 2006-04-28 2008-08-14 Schering Corporation Process for the precipitation and isolation of 6,6-Dimethyl-3-Aza Bicyclo [3.1.0] Hexane-Amide compounds by controlled precipitation and pharmaceutical formulations containing same
EP2023918B1 (en) 2006-05-19 2011-03-23 Scynexis, Inc. Cyclosporins for the treatment and prevention of ocular disorders
JP5270538B2 (ja) * 2006-05-23 2013-08-21 アイアールエム・リミテッド・ライアビリティ・カンパニー チャネル活性化プロテアーゼ阻害剤としての化合物および組成物
CA2651762A1 (en) 2006-05-23 2007-11-29 Irm Llc Compounds and compositions as channel activating protease inhibitors
CN101502196A (zh) * 2006-06-02 2009-08-05 克洛德·安妮·佩里西恩 激活电子的管理
KR20090024834A (ko) * 2006-07-05 2009-03-09 인터뮨, 인크. Ｃ형 간염 바이러스 복제의 신규 억제제
EP2049474B1 (en) 2006-07-11 2015-11-04 Bristol-Myers Squibb Company Hepatitis c virus 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
JP2010500978A (ja) 2006-08-17 2010-01-14 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 ウイルスポリメラーゼインヒビター
AU2007286754A1 (en) * 2006-08-25 2008-02-28 Viropharma Incorporated Identification and characterization of HCV replicon variants with reduced susceptibility to HCV-796, and methods related thereto
BRPI0716733A2 (pt) * 2006-09-13 2015-08-11 Novartis Ag Compostos orgânicos e seus usos
US8343477B2 (en) 2006-11-01 2013-01-01 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8003604B2 (en) 2006-11-16 2011-08-23 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7763584B2 (en) 2006-11-16 2010-07-27 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7888464B2 (en) 2006-11-16 2011-02-15 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2008069917A2 (en) 2006-11-20 2008-06-12 Scynexis, Inc. Novel cyclic peptides
JP2010510245A (ja) * 2006-11-21 2010-04-02 スミスクライン ビーチャム コーポレーション 抗ウイルス化合物
EP2099778A2 (en) * 2006-11-21 2009-09-16 Smithkline Beecham Corporation Amido anti-viral compounds
CA2673111A1 (en) * 2006-12-07 2008-06-19 Schering Corporation Ph sensitive matrix formulation
MX2009006477A (es) * 2006-12-15 2009-06-26 Schering Corp Purificacion de bisulfito de una alfa-ceto amida.
CA2672620A1 (en) * 2006-12-20 2008-07-03 Schering Corporation Process for preparing (1r,2s,5s)-n-[(1s)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2s)-2-[[[(1,1-dimethylethyl)amino]-carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
EP2074087A2 (en) 2006-12-21 2009-07-01 Wyeth Synthesis of pyrrolidine compounds
WO2008082488A1 (en) * 2006-12-22 2008-07-10 Schering Corporation 4, 5-ring annulated indole derivatives for treating or preventing of hcv and related viral infections
US8557848B2 (en) 2006-12-22 2013-10-15 Merck Sharp & Dohme Corp. 4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections
CN101611025A (zh) 2006-12-22 2009-12-23 先灵公司 5,6-环化的吲哚衍生物及其使用方法
US20080161254A1 (en) * 2007-01-03 2008-07-03 Virobay, Inc. Hcv inhibitors
AU2008214217B2 (en) 2007-02-09 2011-10-13 Irm Llc Compounds and compositions as channel activating protease inhibitors
DK2114924T3 (da) * 2007-02-27 2012-04-10 Vertex Pharma Co-krystaller og farmaceutiske sammensætninger omfattende disse
JP2010519329A (ja) * 2007-02-27 2010-06-03 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ阻害剤
JP2010522172A (ja) * 2007-03-23 2010-07-01 シェーリング コーポレイション Ｈｃｖｎｓ３プロテアーゼのｐ１−非エピメリ化ケトアミド阻害剤
EP2160392A2 (en) * 2007-05-03 2010-03-10 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
EP2142215B1 (en) 2007-05-04 2012-03-07 Vertex Pharmceuticals Incorporated Combination therapy for the treatment of hcv infection
WO2008141227A1 (en) * 2007-05-10 2008-11-20 Intermune, Inc. Novel peptide inhibitors of hepatitis c virus replication
CA2693997C (en) 2007-08-03 2013-01-15 Pierre L. Beaulieu Viral polymerase inhibitors
EP2408761B1 (en) * 2007-08-29 2014-01-01 Merck Sharp & Dohme Corp. Substituted indole derivatives and methods of use thereof
ATE541845T1 (de) * 2007-08-29 2012-02-15 Schering Corp 2,3-substituierte azaindolderivate zur behandlung von virusinfektionen
WO2009032116A1 (en) * 2007-08-29 2009-03-12 Schering Corporation 2, 3-substituted indole derivatives for treating viral infections
CN101835774B (zh) 2007-08-30 2014-09-17 弗特克斯药品有限公司 共晶体和包含该共晶体的药物组合物
EP2489369A1 (en) 2007-09-14 2012-08-22 Merck Sharp & Dohme Corp. A method of treating Hepatitis C patients
AR068756A1 (es) * 2007-10-10 2009-12-02 Novartis Ag Compuestos peptidicos, formulacion farmaceutica y sus usos como moduladores del virus de la hepatitis c
US8419332B2 (en) * 2007-10-19 2013-04-16 Atlas Bolt & Screw Company Llc Non-dimpling fastener
US8377928B2 (en) * 2007-11-16 2013-02-19 Merck Sharp & Dohme Corp. 3-aminosulfonyl substituted indole derivatives and methods of use thereof
MX2010005356A (es) * 2007-11-16 2010-05-27 Schering Corp Derivados de indol 3-heterociclico sustituidos y metodos de uso de los mismos.
EP2225203A1 (en) * 2007-11-28 2010-09-08 Schering Corporation Dehydrohalogenation process for the preparation of intermediates useful in providing 6,6-dimethyl-3-azabicyclo-[3.1.0]-hexane compounds
CN101903351B (zh) 2007-12-19 2014-09-10 贝林格尔.英格海姆国际有限公司 病毒聚合酶抑制剂
US8202996B2 (en) 2007-12-21 2012-06-19 Bristol-Myers Squibb Company Crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N- ((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide
JP5203468B2 (ja) * 2007-12-21 2013-06-05 メルク・シャープ・アンド・ドーム・コーポレーション ３−アミノ−３−シクロブチルメチル−２−ヒドロキシプロピオンアミドまたはその塩の合成のための方法
RU2490272C2 (ru) 2008-02-04 2013-08-20 Айденикс Фармасьютикалз, Инк. Макроциклические ингибиторы серинпротеазы
EA201071034A1 (ru) * 2008-04-15 2011-06-30 Интермьюн, Инк. Новые макроциклические ингибиторы репликаций вируса гепатита с
US8163921B2 (en) 2008-04-16 2012-04-24 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2009148923A1 (en) 2008-05-29 2009-12-10 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US7964560B2 (en) 2008-05-29 2011-06-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US20090306033A1 (en) * 2008-06-06 2009-12-10 Keqiang Li Novel cyclic peptides
CN102083852A (zh) * 2008-06-06 2011-06-01 西尼克斯公司 环孢菌素类似物及其在治疗hcv感染中的应用
MX2010013630A (es) * 2008-06-13 2010-12-21 Schering Corp Derivados triciclicos de indol y metodos de uso de los mismos.
MX2010014500A (es) * 2008-06-24 2011-05-30 Codexis Inc Procedimientos biocataliticos para la preparacion de compuestos de prolina biciclica fusionada sustancialmente estereomericamente puros.
US8188137B2 (en) 2008-08-15 2012-05-29 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
US8470834B2 (en) 2008-08-20 2013-06-25 Merck Sharp & Dohme Corp. AZO-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
EP2326627A1 (en) 2008-08-20 2011-06-01 Schering Corporation Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
TW201020245A (en) 2008-08-20 2010-06-01 Schering Corp Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
ES2439009T3 (es) 2008-08-20 2014-01-21 Merck Sharp & Dohme Corp. Derivados de piridina y pirimidina sustituidos con etenilo y su uso en el tratamiento de infecciones virales
US8207341B2 (en) 2008-09-04 2012-06-26 Bristol-Myers Squibb Company Process or synthesizing substituted isoquinolines
US8563505B2 (en) 2008-09-29 2013-10-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8044087B2 (en) 2008-09-29 2011-10-25 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2358736A1 (en) * 2008-10-15 2011-08-24 Intermune, Inc. Therapeutic antiviral peptides
US8283310B2 (en) 2008-12-15 2012-10-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2376524B1 (en) * 2008-12-31 2017-03-15 Cypralis Limited Derivatives of cyclosporin a
JP2012514605A (ja) 2009-01-07 2012-06-28 サイネクシス，インコーポレーテッド Ｈｃｖおよびｈｉｖ感染の治療への使用におけるシクロスポリン誘導体
GB0900914D0 (en) 2009-01-20 2009-03-04 Angeletti P Ist Richerche Bio Antiviral agents
US8102720B2 (en) * 2009-02-02 2012-01-24 Qualcomm Incorporated System and method of pulse generation
AR075584A1 (es) * 2009-02-27 2011-04-20 Intermune Inc COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO.
JP5690286B2 (ja) 2009-03-04 2015-03-25 イデニク プハルマセウティカルス，インコーポレイテッド ホスホチオフェン及びホスホチアゾールｈｃｖポリメラーゼ阻害剤
WO2010118078A1 (en) 2009-04-08 2010-10-14 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
US20110182850A1 (en) * 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US20120244122A1 (en) 2009-05-28 2012-09-27 Masse Craig E Peptides for the Treatment of HCV Infections
JP2012528195A (ja) 2009-05-29 2012-11-12 メルク・シャープ・アンド・ドーム・コーポレーション Ｃ型肝炎などの疾患を処置するための３つの結合アリール部分で構成された抗菌性化合物
US20100324060A1 (en) 2009-06-23 2010-12-23 Gilead Sciences, Inc. Pharmaceutical compositions useful for treating hcv
US20110034469A1 (en) 2009-08-04 2011-02-10 Takeda Pharmaceutical Company Limited Heterocyclic Compound
TW201117812A (en) 2009-08-05 2011-06-01 Idenix Pharmaceuticals Inc Macrocyclic serine protease inhibitors
US9156818B2 (en) 2009-09-11 2015-10-13 Enanta Pharmaceuticals, Inc. Hepatitis C virus inhibitors
IN2012DN02693A (https=) * 2009-09-28 2015-09-04 Intermune Inc
TW201116540A (en) * 2009-10-01 2011-05-16 Intermune Inc Therapeutic antiviral peptides
WO2011063076A1 (en) 2009-11-19 2011-05-26 Itherx Pharmaceuticals, Inc. Methods of treating hepatitis c virus with oxoacetamide compounds
EP2503881B1 (en) 2009-11-25 2015-05-13 Merck Sharp & Dohme Corp. Fused tricyclic compounds and derivatives thereof useful for the treatment of viral diseases
MX2012006877A (es) 2009-12-18 2012-08-31 Idenix Pharmaceuticals Inc Inhibidores de virus de hepatitis c de arileno o heteroarileno 5, 5 - fusionado.
AU2010341537A1 (en) 2009-12-22 2012-08-09 Merck Sharp & Dohme Corp. Fused Tricyclic Compounds and methods of use thereof for the treatment of viral diseases
WO2011103441A1 (en) 2010-02-18 2011-08-25 Schering Corporation Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
US8686145B2 (en) * 2010-02-25 2014-04-01 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patientenzorg C/O Technology Transfer Officer VU & Vumc Process for the preparation of α-acyloxy β-formamido amides
EP2545060B1 (en) 2010-03-09 2015-11-25 Merck Sharp & Dohme Corp. Fused tricyclic silyl compounds and methods of use thereof for the treatment of viral diseases
AU2011286276A1 (en) 2010-07-26 2013-01-24 Merck Sharp & Dohme Corp. Substituted biphenylene compounds and methods of use thereof for the treatment of viral diseases
JP2013540122A (ja) 2010-09-29 2013-10-31 メルク・シャープ・エンド・ドーム・コーポレイション 縮合四環式化合物誘導体およびウィルス疾患治療のためのそれの使用方法
US9353100B2 (en) 2011-02-10 2016-05-31 Idenix Pharmaceuticals Llc Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating HCV infections
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
US20120252721A1 (en) 2011-03-31 2012-10-04 Idenix Pharmaceuticals, Inc. Methods for treating drug-resistant hepatitis c virus infection with a 5,5-fused arylene or heteroarylene hepatitis c virus inhibitor
EP2697242B1 (en) 2011-04-13 2018-10-03 Merck Sharp & Dohme Corp. 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
BR112013026345A2 (pt) 2011-04-13 2019-04-24 Merck Sharp & Dohe Corp. composto, composição farmacêutica, uso de um composto, e, método para tratar um paciente infectado com hcv
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8691757B2 (en) 2011-06-15 2014-04-08 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2013033899A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
WO2013033901A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
WO2013033900A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases
EP2755981A4 (en) 2011-09-14 2015-03-25 Merck Sharp & Dohme SILICULAR HETEROCYCLIC DERIVATIVES AND METHOD FOR THEIR USE FOR THE TREATMENT OF VIRUS DISEASES
DE202012012955U1 (de) 2011-10-21 2014-07-14 Abbvie Inc. Eine Kombination aus mindestens zwei direkt wirkenden antiviralen Wirkstoffen (DAAs) für die Verwendung zur Behandlung von HCV
US8466159B2 (en) 2011-10-21 2013-06-18 Abbvie Inc. Methods for treating HCV
US8492386B2 (en) 2011-10-21 2013-07-23 Abbvie Inc. Methods for treating HCV
EP2583677A3 (en) 2011-10-21 2013-07-03 Abbvie Inc. Methods for treating HCV comprising at least two direct acting antiviral agent, ribavirin but not interferon.
US20130123325A1 (en) 2011-11-14 2013-05-16 Sven Ruf Use of boceprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases
AR091192A1 (es) * 2012-05-30 2015-01-21 Chemo Iberica Sa Procedimiento multicomponente para la preparacion de compuestos biciclicos
CN103508918B (zh) * 2012-06-18 2015-09-09 上海医药工业研究院 带有环丁基的α-羟基β-氨基酯类化合物及其制备方法
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
WO2014061034A1 (en) * 2012-10-18 2014-04-24 Msn Laboratories Limited Process for preparation of boceprevir and intermediates thereof
EA025560B1 (ru) 2012-10-19 2017-01-30 Бристол-Майерс Сквибб Компани Ингибиторы вируса гепатита с
EP2912047B1 (en) 2012-10-29 2016-08-24 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2914613B1 (en) 2012-11-02 2017-11-22 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US9334279B2 (en) 2012-11-02 2016-05-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US9409943B2 (en) 2012-11-05 2016-08-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014083575A2 (en) 2012-11-29 2014-06-05 Mylan Laboratories Ltd Improved process for the preparation of boceprevir intermediate
CN103936818B (zh) * 2013-01-18 2017-09-29 上海医药工业研究院 抗丙肝药物Boceprevir的中间体Ⅰ及其制备方法和应用
CN103936652B (zh) * 2013-01-18 2016-07-06 上海医药工业研究院 抗丙肝药物Boceprevir的中间体IV及其制备方法和应用
CN103936627B (zh) * 2013-01-18 2016-08-31 上海医药工业研究院 抗丙肝药物Boceprevir的中间体Ⅶ及其制备方法和应用
JP6342922B2 (ja) 2013-03-07 2018-06-13 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｃ型肝炎ウイルス阻害剤
EA030957B1 (ru) 2013-03-14 2018-10-31 Оникс Терапьютикс, Инк. Дипептидные и трипептидные эпоксикетонные ингибиторы протеазы
AR095426A1 (es) 2013-03-14 2015-10-14 Onyx Therapeutics Inc Inhibidores tripeptídicos de la epoxicetona proteasa
EP3184095A1 (en) 2013-05-23 2017-06-28 IP Gesellschaft für Management mbH Administration units comprising polymorph 1 of 2-(2-methylamino-pyrimidin-4-yl]-1h-indole-5-carboxylic acid [(s)-1-carbamoyl-2-(phenyl-pyrimidin-2-yl-amino)-ethyl]-amide
CN103387510B (zh) * 2013-08-08 2015-09-09 苏州永健生物医药有限公司 一种β-氨基-alpha-羟基环丁基丁酰胺盐酸盐的合成方法
WO2015042375A1 (en) 2013-09-20 2015-03-26 Idenix Pharmaceuticals, Inc. Hepatitis c virus inhibitors
AU2014340110B2 (en) * 2013-10-24 2018-07-12 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
EP3063140A4 (en) 2013-10-30 2017-11-08 Merck Sharp & Dohme Corp. Pseudopolymorphs of an hcv ns5a inhibitor and uses thereof
EP2899207A1 (en) 2014-01-28 2015-07-29 Amikana.Biologics New method for testing HCV protease inhibition
WO2015134561A1 (en) 2014-03-05 2015-09-11 Idenix Pharmaceuticals, Inc. Pharmaceutical compositions comprising a 5,5-fused heteroarylene flaviviridae inhibitor and their use for treating or preventing flaviviridae infection
US20170066779A1 (en) 2014-03-05 2017-03-09 Idenix Pharmaceuticals Llc Solid forms of a flaviviridae virus inhibitor compound and salts thereof
CN106810485A (zh) * 2015-11-27 2017-06-09 上海现代制药股份有限公司 一种手性联苯吡咯烷酮的制备方法及其中间体
EA201892448A1 (ru) 2016-04-28 2019-06-28 Эмори Юниверсити Алкинсодержащие нуклеотидные и нуклеозидные терапевтические композиции и связанные с ними способы применения
PL3472149T3 (pl) 2016-06-21 2024-02-12 Orion Ophthalmology LLC Heterocykliczne pochodne prolinamidu
EA201990070A1 (ru) * 2016-06-21 2019-06-28 ОРИОН ОФТАЛМОЛОДЖИ ЭлЭлСи Производные алифатического пролинамида
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
WO2018073110A1 (en) 2016-10-20 2018-04-26 Basf Se Quinoline compounds as fungicides
WO2018134127A1 (en) 2017-01-23 2018-07-26 Basf Se Fungicidal pyridine compounds
US20200187500A1 (en) 2017-04-06 2020-06-18 Basf Se Pyridine compounds
CN110709096B (zh) 2017-05-05 2023-10-31 泽兰德制药公司 细胞间隙连接通讯调节剂及其在糖尿病性眼病治疗中的应用
WO2020169593A1 (en) 2019-02-19 2020-08-27 Univerza V Ljubljani Antibacterials based on monocyclic fragments coupled to aminopiperidine naphthyridine scaffold
US20230218644A1 (en) 2020-04-16 2023-07-13 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
JP2023533016A (ja) 2020-07-11 2023-08-01 ファイザー・インク 抗ウイルス性ヘテロアリールケトン誘導体
US20220033383A1 (en) * 2020-07-20 2022-02-03 Enanta Pharmaceuticals, Inc. Functionalized peptides as antiviral agents
US11351149B2 (en) 2020-09-03 2022-06-07 Pfizer Inc. Nitrile-containing antiviral compounds
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
US12540141B2 (en) 2020-11-23 2026-02-03 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
KR20230124583A (ko) 2020-11-23 2023-08-25 이난타 파마슈티칼스, 인코포레이티드 신규한 스피로피롤리딘 유래 항바이러스제
CA3213008A1 (en) * 2021-04-01 2022-10-06 Miles Stuart Congreve Sars-cov-2 mpro inhibitor compounds
RS66213B1 (sr) 2021-04-16 2024-12-31 Fujian Akeylink Biotechnology Co Ltd Jedinjenje kratkog peptida prolina modifikovanog prstenom i upotreba istog
WO2022235605A1 (en) 2021-05-04 2022-11-10 Enanta Pharmaceuticals, Inc. Novel macrocyclic antiviral agents
US12398147B2 (en) 2021-05-11 2025-08-26 Enanta Pharmaceuticals, Inc. Macrocyclic spiropyrrolidine derived antiviral agents
AU2022306289A1 (en) 2021-07-09 2024-01-18 Aligos Therapeutics, Inc. Anti-viral compounds
US12479854B2 (en) 2021-07-29 2025-11-25 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
WO2023043816A1 (en) 2021-09-17 2023-03-23 Aligos Therapeutics, Inc. Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections
US11858945B2 (en) 2021-11-12 2024-01-02 Enanta Pharmaceuticals, Inc. Alkyne-containing antiviral agents
US11919910B2 (en) 2021-11-12 2024-03-05 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
US11912714B2 (en) 2021-11-12 2024-02-27 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
US12145941B2 (en) 2021-12-08 2024-11-19 Enanta Pharmaceuticals, Inc. Heterocyclic antiviral agents
WO2023107419A1 (en) 2021-12-08 2023-06-15 Enanta Pharmaceuticals, Inc. Saturated spirocyclics as antiviral agents
CN114133350B (zh) * 2021-12-16 2023-05-23 浙江乐普药业股份有限公司 一种抗新冠药物Paxlovid中间体的制备方法
WO2023149981A1 (en) * 2022-02-07 2023-08-10 Purdue Research Foundation Compounds for the treatment of sars
WO2023196307A1 (en) 2022-04-05 2023-10-12 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents
CN114736151B (zh) * 2022-04-13 2023-04-21 湖南复瑞生物医药技术有限责任公司 一种帕罗韦德关键中间体制备方法及化合物的结构式
CN115160205B (zh) * 2022-07-08 2024-06-07 上海皓鸿生物医药科技有限公司 一种制备(s)-1-(叔丁氧羰基)-2,5-二氢-1h-吡咯-2-羧酸及盐的方法

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU177134B (en) * 1977-07-18 1981-07-28 Richter Gedeon Vegyeszet Process for preparing angiotensin ii analogues containing alpha-hydroxy-acid in position 1 with angiotensin ii antagonist activity
DE2936099A1 (de) * 1979-09-06 1981-04-02 Victor Dipl.- Chem. 8000 München Brantl Pharmakologisch aktive peptide
JPS5781447A (en) * 1980-11-11 1982-05-21 Toyo Jozo Co Ltd Human chorionic gonadotropic hormone c-terminal fragment
EP0124317B1 (en) * 1983-04-27 1990-04-11 Ici Americas Inc. Proline derivatives
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
JPH02500880A (ja) 1987-11-18 1990-03-29 カイロン　コーポレイション Ｎａｎｂｖの診断用薬およびワクチン
ZA897515B (en) 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
EP0381216B1 (en) 1989-02-01 1995-12-27 Asahi Glass Company Ltd. Hydrochlorofluorocarbon azeotropic or azeotropic-like mixture
US5162500A (en) 1989-04-15 1992-11-10 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Poststatin and related compounds or salts thereof
US5359138A (en) 1989-04-15 1994-10-25 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Poststatin and related compounds or salts thereof
DE69133402T2 (de) 1990-04-04 2004-11-11 Chiron Corp. (N.D.Ges.D. Staates Delaware), Emeryville Protease von hepatitis-c-virus
JP2804817B2 (ja) 1990-04-13 1998-09-30 財団法人微生物化学研究会 ３―アミノ―２―オキソ脂肪酸誘導体の製造法
JPH04149166A (ja) 1990-10-12 1992-05-22 Nippon Kayaku Co Ltd 新規ケト酸アミド誘導体
CA2098609A1 (en) 1990-12-28 1992-06-29 Raymond T. Bartus Use of calpain inhibitors in the inhibition and treatment of neurodegeneration
FR2686086A1 (fr) * 1992-01-15 1993-07-16 Adir Nouveaux derives de peptides et de pseudopeptides therapeutiquement actifs dans la cascade de coagulation sanguine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
JP3439209B2 (ja) 1992-01-31 2003-08-25 アボツト・ラボラトリーズ Ｈｃｖ蛋白のための哺乳動物発現システム
EP0650368A1 (en) 1992-06-24 1995-05-03 Cortex Pharmaceuticals, Inc. Use of calpain inhibitors in the inhibition and treatment of medical conditions associated with increased calpain activity
US5514694A (en) 1992-09-21 1996-05-07 Georgia Tech Research Corp Peptidyl ketoamides
US5414018A (en) 1993-09-24 1995-05-09 G. D. Searle & Co. Alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol compounds for treatment of hypertension
US5843450A (en) 1994-02-14 1998-12-01 Abbott Laboratories Hepatitis GB Virus synthetic peptides and uses thereof
IT1272179B (it) 1994-02-23 1997-06-16 Angeletti P Ist Richerche Bio Metodologia per riprodurre in vitro l'attivita' proteolitica della proteasi ns3 del virus hcv.
US6285380B1 (en) * 1994-08-02 2001-09-04 New York University Method and system for scripting interactive animated actors
RU2104284C1 (ru) * 1994-10-20 1998-02-10 Научно-исследовательский институт вирусологии им.Д.И.Ивановского РАМН Синтетические олигопептиды, специфически взаимодействующие с антителами к вирусу гепатита с, способы диагностики hcv-инфекции (варианты)
US5843752A (en) 1995-05-12 1998-12-01 Schering Corporation Soluble active hepatitis C virus protease
US5919765A (en) 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
GB9517022D0 (en) 1995-08-19 1995-10-25 Glaxo Group Ltd Medicaments
US5763576A (en) 1995-10-06 1998-06-09 Georgia Tech Research Corp. Tetrapeptide α-ketoamides
IL120310A (en) 1996-03-01 2002-02-10 Akzo Nobel Nv Serine protease inhibitors and pharmaceuticals containing them
US5633388A (en) 1996-03-29 1997-05-27 Viropharma Incorporated Compounds, compositions and methods for treatment of hepatitis C
US5736576A (en) * 1996-06-04 1998-04-07 Octamer, Inc. Method of treating malignant tumors with thyroxine analogues having no significant hormonal activity
WO1998007734A1 (en) 1996-08-21 1998-02-26 Hybridon, Inc. Oligonucleotide prodrugs
IT1285158B1 (it) 1996-09-17 1998-06-03 Angeletti P Ist Richerche Bio Polipeptidi solubili con l'attivita' di serino-proteasi di ns3 del virus dell'epatite c, e procedimento per la loro preparazione e il
BR9712115A (pt) 1996-09-24 1999-08-31 Procter & Gamble Detergentes líquidos contendo enzima proteolítica, aldeído peptídeo e uma fonte de ácido bórico.
US5922757A (en) 1996-09-30 1999-07-13 The Regents Of The University Of California Treatment and prevention of hepatic disorders
KR100509388B1 (ko) 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 ｃ 바이러스 ｎｓ３ 프로테아제의 저해제
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
ATE261988T1 (de) 1996-12-27 2004-04-15 Boehringer Ingelheim Ca Ltd Peptidomimetische inhibitoren von der protease des menschlichen cytomegalovirus
WO1998037180A2 (en) 1997-02-22 1998-08-27 Abbott Laboratories Hcv fusion protease and polynucleotide encoding same
WO1999007733A2 (en) 1997-08-11 1999-02-18 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor peptides
ES2234144T3 (es) * 1997-08-11 2005-06-16 Boehringer Ingelheim (Canada) Ltd. Analogos de peptidos inhibidores de la hepatitis c.
GB9809664D0 (en) 1998-05-06 1998-07-01 Hoffmann La Roche a-Ketoamide derivatives
GB9812523D0 (en) 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
US6576613B1 (en) * 1998-07-24 2003-06-10 Corvas International, Inc. Title inhibitors of urokinase
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
JP2000256396A (ja) * 1999-03-03 2000-09-19 Dainippon Pharmaceut Co Ltd 複素環式化合物およびその中間体ならびにエラスターゼ阻害剤
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
JP2003526634A (ja) * 1999-12-03 2003-09-09 ブリストル−マイヤーズ スクイブ ファーマ カンパニー Ｃ型肝炎ウイルスＮＳ３プロテアーゼのα−ケトアミド阻害剤
ES2240446T3 (es) * 2000-04-03 2005-10-16 Vertex Pharma Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
DK1385870T3 (da) * 2000-07-21 2010-07-05 Schering Corp Peptider som inhibitorer af NS3-serinprotease fra 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
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m

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