JP4080541B2 - セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 - Google Patents
セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子Info
- Publication number
- JP4080541B2 JP4080541B2 JP51956898A JP51956898A JP4080541B2 JP 4080541 B2 JP4080541 B2 JP 4080541B2 JP 51956898 A JP51956898 A JP 51956898A JP 51956898 A JP51956898 A JP 51956898A JP 4080541 B2 JP4080541 B2 JP 4080541B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- compound
- heteroaryl
- aralkyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
Links
- 0 C*N(*C(C)=N)NC Chemical compound C*N(*C(C)=N)NC 0.000 description 4
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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 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
- 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
- C07K5/02—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
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Virology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Crystallography & Structural Chemistry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2829096P | 1996-10-18 | 1996-10-18 | |
| US60/028,290 | 1996-10-18 | ||
| PCT/US1997/018968 WO1998017679A1 (en) | 1996-10-18 | 1997-10-17 | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007290832A Division JP4783353B2 (ja) | 1996-10-18 | 2007-11-08 | セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2001502694A JP2001502694A (ja) | 2001-02-27 |
| JP4080541B2 true JP4080541B2 (ja) | 2008-04-23 |
Family
ID=21842625
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP51956898A Expired - Fee Related JP4080541B2 (ja) | 1996-10-18 | 1997-10-17 | セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 |
| JP2007290832A Expired - Fee Related JP4783353B2 (ja) | 1996-10-18 | 2007-11-08 | セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 |
| JP2010279518A Expired - Fee Related JP5301523B2 (ja) | 1996-10-18 | 2010-12-15 | セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007290832A Expired - Fee Related JP4783353B2 (ja) | 1996-10-18 | 2007-11-08 | セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 |
| JP2010279518A Expired - Fee Related JP5301523B2 (ja) | 1996-10-18 | 2010-12-15 | セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 |
Country Status (33)
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011093912A (ja) * | 1996-10-18 | 2011-05-12 | Vertex Pharmaceuticals Inc | セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 |
Families Citing this family (353)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7135584B2 (en) | 1995-08-07 | 2006-11-14 | Wake Forest University | Lipid analogs for treating viral infections |
| DE69535758D1 (de) | 1994-08-29 | 2008-07-03 | Univ Wake Forest | Lipid-analoge zur behandlung von viralen infektionen |
| GB9707659D0 (en) * | 1997-04-16 | 1997-06-04 | Peptide Therapeutics Ltd | Hepatitis C NS3 Protease inhibitors |
| DK1003775T3 (da) * | 1997-08-11 | 2005-05-30 | Boehringer Ingelheim Ca Ltd | Hepatitis C-inhibitorpeptider |
| US6767991B1 (en) | 1997-08-11 | 2004-07-27 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis C inhibitor peptides |
| WO1999007734A2 (en) * | 1997-08-11 | 1999-02-18 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis c inhibitor peptide analogues |
| GB9806815D0 (en) | 1998-03-30 | 1998-05-27 | Hoffmann La Roche | Amino acid derivatives |
| EP1066247B1 (en) * | 1998-03-31 | 2006-11-22 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
| 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 |
| 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 |
| JP2002538151A (ja) | 1999-03-02 | 2002-11-12 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | カテプシンの可逆的インヒビターとして有用な化合物 |
| 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 |
| US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
| AU5788800A (en) * | 1999-07-07 | 2001-01-22 | Du Pont Pharmaceuticals Company | Peptide boronic acid inhibitors of hepatitis c virus protease |
| WO2001007407A1 (en) * | 1999-07-26 | 2001-02-01 | Bristol-Myers Squibb Pharma Company | Lactam inhibitors of hepatitis c virus ns3 protease |
| US7122627B2 (en) | 1999-07-26 | 2006-10-17 | Bristol-Myers Squibb Company | Lactam inhibitors of Hepatitis C virus NS3 protease |
| US6420364B1 (en) | 1999-09-13 | 2002-07-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compound useful as reversible inhibitors of cysteine proteases |
| US7026469B2 (en) | 2000-10-19 | 2006-04-11 | Wake Forest University School Of Medicine | Compositions and methods of double-targeting virus infections and cancer cells |
| CA2390349A1 (en) | 1999-12-03 | 2001-06-07 | Bristol-Myers Squibb Pharma Company | Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease |
| CA2392028C (en) * | 1999-12-07 | 2009-08-18 | Theravance, Inc. | Carbamate derivatives having muscarinic receptor antagonist activity |
| EP1261611A2 (en) | 2000-02-29 | 2002-12-04 | Bristol-Myers Squibb Pharma Company | Inhibitors of hepatitis c virus ns3 protease |
| AU2006202124B2 (en) * | 2000-04-03 | 2010-01-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of Serine Proteases, Particularly Hepatitis C Virus NS3 Protease |
| DE60111509T2 (de) * | 2000-04-03 | 2006-05-11 | Vertex Pharmaceuticals Inc., Cambridge | Inhibitoren von Serin-Proteasen, insbesondere der Hepatitis-C-Virus NS23-Protease |
| JP4748911B2 (ja) | 2000-04-05 | 2011-08-17 | シェーリング コーポレイション | N−環状p2部分を含むc型肝炎ウイルスの大環状ns3‐セリンプロテアーゼ阻害剤 |
| CN1432022A (zh) | 2000-04-19 | 2003-07-23 | 先灵公司 | 含有烷基和芳基丙氨酸p2部分的丙型肝炎病毒的大环ns3-丝氨酸蛋白酶抑制剂 |
| PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
| MY164523A (en) | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
| JP5230052B2 (ja) | 2000-05-26 | 2013-07-10 | イデニクス(ケイマン)リミテツド | フラビウイルスおよびペスチウイルス治療のための方法および組成物 |
| US20020007324A1 (en) * | 2000-06-09 | 2002-01-17 | Centner David J. | System and method for effectively conducting transactions between buyers and suppliers |
| CZ303213B6 (cs) | 2000-07-21 | 2012-05-23 | Schering Corporation | Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostredek |
| RU2003105221A (ru) * | 2000-07-21 | 2004-09-20 | Шеринг Корпорейшн (US) | Новые пептиды, как ингибиторы ns3-серинпротеазы вируса гепатита с |
| AR029851A1 (es) | 2000-07-21 | 2003-07-16 | Dendreon Corp | Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c |
| 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 |
| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| EP2301565A1 (de) * | 2000-10-12 | 2011-03-30 | ViroLogik GmbH | Verwendung von Proteasome Hemmern zur Behandlung von Virus-Infektionen |
| ATE491459T1 (de) | 2000-10-18 | 2011-01-15 | Pharmasset Inc | Modifizierte nukleoside zur behandlung von virusinfektionen und abnormaler zellulärer proliferation |
| US7309696B2 (en) | 2000-10-19 | 2007-12-18 | Wake Forest University | Compositions and methods for targeting cancer cells |
| US6846806B2 (en) | 2000-10-23 | 2005-01-25 | Bristol-Myers Squibb Company | Peptide inhibitors of Hepatitis C virus NS3 protein |
| CN1301994C (zh) | 2000-12-12 | 2007-02-28 | 先灵公司 | 作为c型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的二芳基肽 |
| 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 |
| DZ3487A1 (fr) | 2001-01-22 | 2002-07-25 | Merck Sharp & Dohme | Derives de nucleoside comme inhibiteurs de l'arn polymerase virale d'arn-dependant |
| JP4455056B2 (ja) | 2001-07-11 | 2010-04-21 | 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 | 架橋二環式セリンプロテアーゼ阻害剤 |
| US7551837B2 (en) | 2001-08-31 | 2009-06-23 | Thomson Licensing | Sequence counter for an audio visual stream |
| WO2003026589A2 (en) | 2001-09-28 | 2003-04-03 | Idenix (Cayman) Limited | Methods and compositions for treating hepatitis c virus using 4'-modified nucleosides |
| EP1441720B8 (en) * | 2001-10-24 | 2012-03-28 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4a protease, incorporating a fused ring system |
| MY151199A (en) * | 2001-11-02 | 2014-04-30 | Rigel Pharmaceuticals Inc | Substituted diphenyl heterocycles useful for treating hcv infection |
| NZ533861A (en) | 2002-01-23 | 2006-03-31 | Schering Corp | Proline compounds as NS3-serine protease inhibitors for use in treatment of hepatitis C virus infection |
| US7119072B2 (en) | 2002-01-30 | 2006-10-10 | Boehringer Ingelheim (Canada) Ltd. | Macrocyclic peptides active against the hepatitis C virus |
| US6642204B2 (en) | 2002-02-01 | 2003-11-04 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| US7091184B2 (en) | 2002-02-01 | 2006-08-15 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
| NZ575692A (en) | 2002-04-11 | 2009-10-30 | Vertex Pharma | Inhibitors of Serine Proteases, Particularly Hepatitis C Virus NS3-NS4 Protease |
| PL213029B1 (pl) | 2002-05-20 | 2012-12-31 | Bristol Myers Squibb Co | Podstawiona pochodna cykloalkilowa, zawierajaca ja kompozycja oraz ich zastosowanie |
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| CN100503628C (zh) | 2003-05-30 | 2009-06-24 | 法莫赛特股份有限公司 | 修饰的氟化核苷类似物 |
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| CN1852915A (zh) | 2003-07-25 | 2006-10-25 | 艾登尼科斯(开曼)有限公司 | 治疗包括丙型肝炎的黄病毒科病毒所致疾病的嘌呤核苷类似物 |
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| WO2005028502A1 (en) * | 2003-09-18 | 2005-03-31 | Vertex Pharmaceuticals, Incorporated | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
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| BRPI0414814A (pt) | 2003-09-26 | 2006-11-14 | Schering Corp | inibidores macrocìclicos de protease de serina ns3 de vìrus de hepatite c |
| AU2004282148A1 (en) | 2003-10-10 | 2005-04-28 | Vertex Pharmaceuticals Incoporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
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| HRP20130098T1 (hr) | 2003-10-14 | 2013-02-28 | F. Hoffmann - La Roche Ag | MAKROCIKLIÄŚKE KARBOKSILNE KISELINE I ACILSULFONAMIDNI SPOJEVI KAO INHIBITORI REPLIKACIJE HCV-a |
| WO2005042570A1 (en) | 2003-10-27 | 2005-05-12 | Vertex Pharmaceuticals Incorporated | Hcv ns3-ns4a protease resistance mutants |
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| CN1902216A (zh) | 2003-11-20 | 2007-01-24 | 先灵公司 | 丙肝病毒ns3蛋白酶的去肽化抑制剂 |
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| BRPI0506948B1 (pt) | 2004-01-30 | 2018-09-18 | Medivir Ab | inibidores de serina protease ns-3 de hcv |
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| US20070049593A1 (en) | 2004-02-24 | 2007-03-01 | Japan Tobacco Inc. | Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor |
| ATE428714T1 (de) | 2004-02-24 | 2009-05-15 | Japan Tobacco Inc | Kondensierte heterotetracyclische verbindungen und deren verwendung als hcv-polymerase-inhibitor |
| US7816326B2 (en) | 2004-02-27 | 2010-10-19 | Schering Corporation | Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease |
| EP1737881B1 (en) | 2004-02-27 | 2009-06-24 | Schering Corporation | Novel compounds as inhibitors of hepatitis c virus ns3 serine protease |
| EP1730165A1 (en) | 2004-02-27 | 2006-12-13 | Schering Corporation | Inhibitors of hepatitis c virus ns3 protease |
| BRPI0508085A (pt) | 2004-02-27 | 2007-07-17 | Schering Corp | compostos de enxofre como inibidores da ns3 serina protease do vìrus da hepatite c |
| 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 |
| CN102225936B (zh) * | 2004-03-12 | 2013-09-11 | 弗特克斯药品有限公司 | 制备化合物的方法 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011093912A (ja) * | 1996-10-18 | 2011-05-12 | Vertex Pharmaceuticals Inc | セリンプロテアーゼ、特にc型肝炎ウイルスns3プロテアーゼの阻害因子 |
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