JP4748911B2 - 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 - Google Patents
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 Download PDFInfo
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- JP4748911B2 JP4748911B2 JP2001575586A JP2001575586A JP4748911B2 JP 4748911 B2 JP4748911 B2 JP 4748911B2 JP 2001575586 A JP2001575586 A JP 2001575586A JP 2001575586 A JP2001575586 A JP 2001575586A JP 4748911 B2 JP4748911 B2 JP 4748911B2
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- 0 CC(C)(C)OC(N(C1)C(*)CC1O)=O Chemical compound CC(C)(C)OC(N(C1)C(*)CC1O)=O 0.000 description 2
- GJHAATSCLJSKJQ-VPXRBHCHSA-N CCCC(C(C(NCC(NC(C(C)N(C)C)c1ccccc1)=O)O)=O)NC([C@H](C[C@H](C1)SCCCOc2cc(CC(N[C@H]3C4CCCCC4)=O)ccc2)N1C3=O)=O Chemical compound CCCC(C(C(NCC(NC(C(C)N(C)C)c1ccccc1)=O)O)=O)NC([C@H](C[C@H](C1)SCCCOc2cc(CC(N[C@H]3C4CCCCC4)=O)ccc2)N1C3=O)=O GJHAATSCLJSKJQ-VPXRBHCHSA-N 0.000 description 1
- JQYOUERZBDLNBO-XKBQFAPISA-N CCCC(C(C(NCC(NC(C(O)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCCOc2cccc(CC(N[C@H]3C4CCCCC4)=O)c2)N1C3=O)=O Chemical compound CCCC(C(C(NCC(NC(C(O)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCCOc2cccc(CC(N[C@H]3C4CCCCC4)=O)c2)N1C3=O)=O JQYOUERZBDLNBO-XKBQFAPISA-N 0.000 description 1
- SEYUNHVIYVFKNT-FFNCAFBRSA-N CCCC(C(C(NCC(N[C@H](C(N(C)C)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCCC(C2)C2c2cc(CC(N[C@H]3C4CCCCC4)=O)ccc2)N1C3=O)=O Chemical compound CCCC(C(C(NCC(N[C@H](C(N(C)C)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)OCCCCC(C2)C2c2cc(CC(N[C@H]3C4CCCCC4)=O)ccc2)N1C3=O)=O SEYUNHVIYVFKNT-FFNCAFBRSA-N 0.000 description 1
- STDKCAAAVGRJPO-ZHKAWACISA-N CCC[C@@H](C(C(NCC(NC(C(N(C)C)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)SCCCOc2cc(CC(N[C@H]3C4CCCCC4)=O)ccc2)N1C3=O)=O Chemical compound CCC[C@@H](C(C(NCC(NC(C(N(C)C)=O)c1ccccc1)=O)=O)=O)NC([C@H](C[C@H](C1)SCCCOc2cc(CC(N[C@H]3C4CCCCC4)=O)ccc2)N1C3=O)=O STDKCAAAVGRJPO-ZHKAWACISA-N 0.000 description 1
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
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
-
- 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
- C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
-
- 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
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
-
- 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
-
- 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
-
- 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
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
-
- 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)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Analytical Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19460700P | 2000-04-05 | 2000-04-05 | |
| US60/194,607 | 2000-04-05 | ||
| PCT/US2001/010869 WO2001077113A2 (en) | 2000-04-05 | 2001-04-03 | Macrocyclic ns3-serine protease inhibitors of hepatitis c virus comprising n-cyclic p2 moieties |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003530401A JP2003530401A (ja) | 2003-10-14 |
| JP2003530401A5 JP2003530401A5 (enExample) | 2008-02-28 |
| JP4748911B2 true JP4748911B2 (ja) | 2011-08-17 |
Family
ID=22718227
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001575586A Expired - Fee Related JP4748911B2 (ja) | 2000-04-05 | 2001-04-03 | 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 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US6846802B2 (enExample) |
| EP (1) | EP1268525B1 (enExample) |
| JP (1) | JP4748911B2 (enExample) |
| KR (1) | KR20030036152A (enExample) |
| CN (1) | CN1441806A (enExample) |
| AR (1) | AR029903A1 (enExample) |
| AT (1) | ATE419270T1 (enExample) |
| AU (1) | AU2001253124A1 (enExample) |
| BR (1) | BR0109861A (enExample) |
| CA (1) | CA2405521C (enExample) |
| CZ (1) | CZ20023321A3 (enExample) |
| DE (1) | DE60137207D1 (enExample) |
| EC (1) | ECSP014009A (enExample) |
| ES (1) | ES2317900T3 (enExample) |
| HK (1) | HK1047947A1 (enExample) |
| HU (1) | HUP0400456A3 (enExample) |
| IL (1) | IL151934A0 (enExample) |
| MX (1) | MXPA02009920A (enExample) |
| NO (1) | NO20024797L (enExample) |
| NZ (1) | NZ521455A (enExample) |
| PE (1) | PE20020188A1 (enExample) |
| PL (1) | PL359359A1 (enExample) |
| RU (1) | RU2002129564A (enExample) |
| SK (1) | SK14192002A3 (enExample) |
| WO (1) | WO2001077113A2 (enExample) |
| ZA (1) | ZA200207845B (enExample) |
Families Citing this family (152)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN183120B (enExample) | 1996-10-18 | 1999-09-11 | Vertex Pharma | |
| US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the 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 |
| 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 |
| DE60336986D1 (de) | 2002-03-05 | 2011-06-16 | Sumitomo Chemical Co | Verfahren zur herstellung von biarylverbindungen |
| US7273885B2 (en) * | 2002-04-11 | 2007-09-25 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
| US20050075279A1 (en) | 2002-10-25 | 2005-04-07 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis C virus |
| AU2004240704B9 (en) | 2003-05-21 | 2009-10-22 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor compounds |
| JP4928261B2 (ja) | 2003-06-18 | 2012-05-09 | トランザイム・ファーマ・インコーポレイテッド | モチリン受容体の大環状拮抗薬 |
| CA2536570A1 (en) | 2003-08-26 | 2005-03-10 | Schering Corporation | Novel peptidomimetic ns3-serine protease inhibitors of hepatitis c virus |
| UY28500A1 (es) | 2003-09-05 | 2005-04-29 | Vertex Pharma | Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc. |
| US7642235B2 (en) | 2003-09-22 | 2010-01-05 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis C virus |
| US7592419B2 (en) | 2003-09-26 | 2009-09-22 | Schering Corporation | Macrocyclic inhibitors of hepatitis C virus NS3-serine protease |
| EP1692157B1 (en) | 2003-10-10 | 2013-04-17 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
| US7491794B2 (en) * | 2003-10-14 | 2009-02-17 | Intermune, Inc. | Macrocyclic compounds as inhibitors of viral replication |
| WO2005043118A2 (en) | 2003-10-27 | 2005-05-12 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
| EP1944042A1 (en) | 2003-10-27 | 2008-07-16 | Vertex Pharmceuticals Incorporated | Combinations for HCV treatment |
| JP2007532479A (ja) | 2003-11-20 | 2007-11-15 | シェーリング コーポレイション | C型肝炎ウイルスns3プロテアーゼの脱ペプチド化インヒビター |
| CA2549851C (en) | 2004-01-21 | 2012-09-11 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis c virus |
| UA84050C2 (en) * | 2004-01-30 | 2008-09-10 | Медивир Аб | Hcv ns-3-serine protease inhibitors |
| EP1711515A2 (en) | 2004-02-04 | 2006-10-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hcv ns3-ns4a protease |
| PT1719773E (pt) | 2004-02-24 | 2009-06-03 | Japan Tobacco Inc | Compostos heterotetracíclicos fundidos e a sua utilização como inibidores da polimerase do hcv |
| US20070049593A1 (en) | 2004-02-24 | 2007-03-01 | Japan Tobacco Inc. | Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor |
| US7816326B2 (en) | 2004-02-27 | 2010-10-19 | Schering Corporation | Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease |
| ATE470660T1 (de) | 2004-02-27 | 2010-06-15 | Schering Corp | Schwefelverbindungen als inhibitoren der ns3- serinprotease des hepatitis-c-virus |
| TW200602037A (en) | 2004-02-27 | 2006-01-16 | Schering Corp | Novel 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 |
| JP4745327B2 (ja) | 2004-02-27 | 2011-08-10 | シェーリング コーポレイション | C型肝炎ウイルスns3プロテアーゼのインヒビター |
| RU2006134002A (ru) | 2004-02-27 | 2008-04-10 | Шеринг Корпорейшн (US) | Новые соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с |
| WO2005113581A1 (en) | 2004-05-20 | 2005-12-01 | Schering Corporation | Substituted prolines as inhibitors of hepatitis c virus ns3 serine protease |
| JP2005350417A (ja) * | 2004-06-11 | 2005-12-22 | Dai Ichi Seiyaku Co Ltd | 還元的エーテル化法を用いたピロリジン誘導体の製造法 |
| 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 |
| MX2007002371A (es) | 2004-08-27 | 2007-04-23 | Schering Corp | Compuestos de acilsulfonamida como inhibidores de la serina proteasa ns3 del virus de la hepatitis c. |
| WO2007001406A2 (en) * | 2004-10-05 | 2007-01-04 | Chiron Corporation | Aryl-containing macrocyclic compounds |
| US7659263B2 (en) | 2004-11-12 | 2010-02-09 | Japan Tobacco Inc. | Thienopyrrole compound and use thereof as HCV polymerase inhibitor |
| US7879797B2 (en) | 2005-05-02 | 2011-02-01 | Merck Sharp & Dohme Corp. | HCV NS3 protease inhibitors |
| EP1919478B1 (en) * | 2005-06-02 | 2016-03-23 | Merck Sharp & Dohme Corp. | Combination of hcv protease inhibitors with a surfactant |
| US20110104109A1 (en) * | 2005-07-13 | 2011-05-05 | Frank Bennett | Tetracyclic indole derivatives and their use for treating or preventing viral infections |
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| BRPI0613962A2 (pt) * | 2005-07-25 | 2009-03-24 | Intermune Inc | inibidores macrocìclicos inovadores de replicação de vìrus da hepatite c |
| AU2006275605B2 (en) * | 2005-08-01 | 2011-01-06 | Merck Sharp & Dohme Corp. | Macrocyclic peptides as HCV NS3 protease inhibitors |
| WO2007016589A2 (en) * | 2005-08-02 | 2007-02-08 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
| BRPI0615029A2 (pt) | 2005-08-19 | 2009-06-16 | Vertex Pharma | processos e intermediários |
| US8399615B2 (en) | 2005-08-19 | 2013-03-19 | Vertex Pharmaceuticals Incorporated | Processes and intermediates |
| AR055395A1 (es) * | 2005-08-26 | 2007-08-22 | Vertex Pharma | Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c |
| US7964624B1 (en) * | 2005-08-26 | 2011-06-21 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
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| JP5409008B2 (ja) | 2005-11-11 | 2014-02-05 | 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 | C型肝炎ウイルス改変体 |
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| CA2667146C (en) * | 2006-10-24 | 2016-01-19 | Merck & Co., Inc. | Hcv ns3 protease inhibitors |
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| EP2463284A1 (en) * | 2007-02-27 | 2012-06-13 | Vertex Pharmceuticals Incorporated | Co-crystals and pharmaceutical compositions comprising the same |
| AU2008219704A1 (en) | 2007-02-27 | 2008-09-04 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
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| NZ580917A (en) | 2007-05-04 | 2012-06-29 | Vertex Pharma | Combinations of protease inhibitors such as VX-950 and polymerase inhibitors for the treatment of HCV infection |
| BRPI0811447A2 (pt) | 2007-05-10 | 2014-10-29 | Intermune Inc | Compostos, composição farmacêutica e métodos de inibição da atividade da protease ns3/ns4, de tratamento da fibrose hepática e de intensificação da função hepática num indivíduo tendo infecção de vírus da hepatite c. |
| CN101754970B (zh) | 2007-07-17 | 2013-07-10 | P.安杰莱蒂分子生物学研究所 | 用于治疗丙型肝炎的大环吲哚衍生物 |
| WO2009010804A1 (en) | 2007-07-19 | 2009-01-22 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Macrocyclic compounds as antiviral agents |
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| SK14192002A3 (sk) | 2003-03-04 |
| CN1441806A (zh) | 2003-09-10 |
| PL359359A1 (en) | 2004-08-23 |
| NO20024797D0 (no) | 2002-10-04 |
| PE20020188A1 (es) | 2002-03-13 |
| CA2405521C (en) | 2010-06-29 |
| US20020107181A1 (en) | 2002-08-08 |
| WO2001077113A3 (en) | 2002-06-20 |
| CZ20023321A3 (cs) | 2003-01-15 |
| AU2001253124A1 (en) | 2001-10-23 |
| ES2317900T3 (es) | 2009-05-01 |
| ATE419270T1 (de) | 2009-01-15 |
| JP2003530401A (ja) | 2003-10-14 |
| DE60137207D1 (de) | 2009-02-12 |
| EP1268525A2 (en) | 2003-01-02 |
| HUP0400456A3 (en) | 2005-09-28 |
| NO20024797L (no) | 2002-12-04 |
| BR0109861A (pt) | 2003-06-10 |
| ZA200207845B (en) | 2004-02-11 |
| HK1047947A1 (zh) | 2003-03-14 |
| CA2405521A1 (en) | 2001-10-18 |
| US6846802B2 (en) | 2005-01-25 |
| ECSP014009A (es) | 2003-03-31 |
| WO2001077113A2 (en) | 2001-10-18 |
| AR029903A1 (es) | 2003-07-23 |
| IL151934A0 (en) | 2003-04-10 |
| MXPA02009920A (es) | 2003-03-27 |
| EP1268525B1 (en) | 2008-12-31 |
| RU2002129564A (ru) | 2004-05-10 |
| HUP0400456A2 (hu) | 2004-06-28 |
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