WO2004026896A3 - Hcv ns-3 serine protease inhibitors - Google Patents
Hcv ns-3 serine protease inhibitors Download PDFInfo
- Publication number
- WO2004026896A3 WO2004026896A3 PCT/EP2003/010595 EP0310595W WO2004026896A3 WO 2004026896 A3 WO2004026896 A3 WO 2004026896A3 EP 0310595 W EP0310595 W EP 0310595W WO 2004026896 A3 WO2004026896 A3 WO 2004026896A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- alkyl
- hcv
- serine protease
- alkylhet
- alkylaryl
- Prior art date
Links
Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Abstract
Compounds possessing novel P1 amino acid replacements of the formulae (I) or (II) where R1 is a peptidic or peptidomimetic recognition sequence P2-Pn targeting the S2- Sn pockets of HCV NS-3 serine protease, where n is 3-6, which recognition sequence is peptide bonded to formula (I); R2 is H, C1-C3 alkyl; R3 is C1-C3 alkyl, optionally substituted with 1-3 halo atoms or -SH; R4 is =O, halo, amino or -OH; R5 is C1-C6 alkyl, C0-C3-alkylaryl, C0-C3-alkylhet, C0-C3-alkylcycloC3-C6-alkyl, any of which can be optionally substituted with hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 alkoxy C1-C6 alkyl, C1-C6 alkanoyl, amino, halo, carboxy, cyano, azido, mercapto, nitro, C0-C3-alkylaryl, C0-C3-alkylhet, C0-C3-alkylcycloalkyl; R6 is H C1-C3 alkyl or cyclises with the nominal N-terminal to form a macrocycle; with the proviso that if R4 is =O, then the alkyl moiety of R5 as alkylaryl or alkylhet is C1-C3 alkanyl or C2-C3 alkenyl; have utility as HCV NS-3 serine protease inhibitors.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2003277891A AU2003277891A1 (en) | 2002-09-23 | 2003-09-23 | Hcv ns-3 serine protease inhibitors |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02021111.6 | 2002-09-23 | ||
| EP02021111 | 2002-09-23 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2004026896A2 WO2004026896A2 (en) | 2004-04-01 |
| WO2004026896A3 true WO2004026896A3 (en) | 2005-01-13 |
Family
ID=32010923
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP2003/010595 WO2004026896A2 (en) | 2002-09-23 | 2003-09-23 | Hcv ns-3 serine protease inhibitors |
Country Status (2)
| Country | Link |
|---|---|
| AU (1) | AU2003277891A1 (en) |
| WO (1) | WO2004026896A2 (en) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005073216A2 (en) | 2004-01-30 | 2005-08-11 | Medivir Ab | Hcv ns-3 serine protease inhibitors |
| PE20070211A1 (en) | 2005-07-29 | 2007-05-12 | Medivir Ab | MACROCYCLIC COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS |
| AR055395A1 (en) | 2005-08-26 | 2007-08-22 | Vertex Pharma | INHIBITING COMPOUNDS OF THE ACTIVITY OF SERINA PROTEASA NS3-NS4A OF HEPATITIS C VIRUS |
| CN101636407B (en) | 2006-12-14 | 2015-08-26 | 爱勒让治疗公司 | Bis-sulfhydryl macrocyclization systems |
| EP2118123B1 (en) | 2007-01-31 | 2015-10-14 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| JP5631201B2 (en) | 2007-03-28 | 2014-11-26 | プレジデント アンド フェローズ オブ ハーバード カレッジ | Stitched polypeptide |
| CA2744088A1 (en) | 2009-01-14 | 2010-07-22 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| DK2603600T3 (en) | 2010-08-13 | 2019-03-04 | Aileron Therapeutics Inc | PEPTIDOMIMETIC MACROCYCLES |
| MX358886B (en) | 2011-10-18 | 2018-08-31 | Aileron Therapeutics Inc | Peptidomimetic macrocyles. |
| CN112500466B (en) | 2012-02-15 | 2022-05-03 | 艾瑞朗医疗公司 | Peptidomimetic macrocycles |
| AU2013221433B2 (en) | 2012-02-15 | 2018-01-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| BR112015009470A2 (en) | 2012-11-01 | 2019-12-17 | Aileron Therapeutics Inc | disubstituted amino acids and their methods of preparation and use |
| SG10201902598VA (en) | 2014-09-24 | 2019-04-29 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and formulations thereof |
| CN112245565A (en) | 2014-09-24 | 2021-01-22 | 艾瑞朗医疗公司 | Peptidomimetic macrocycles and uses thereof |
| SG11201707750YA (en) | 2015-03-20 | 2017-10-30 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and uses thereof |
| WO2017004548A1 (en) | 2015-07-01 | 2017-01-05 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles |
| JP2018528217A (en) | 2015-09-10 | 2018-09-27 | エルロン・セラピューティクス・インコーポレイテッドＡｉｌｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | Peptidomimetic macrocycles as modulators of MCL-1 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998017679A1 (en) * | 1996-10-18 | 1998-04-30 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
| WO2002008256A2 (en) * | 2000-07-21 | 2002-01-31 | Schering Corporation | Peptides as ns3-serine protease inhibitors of hepatitis c virus |
| WO2002018369A2 (en) * | 2000-08-31 | 2002-03-07 | Eli Lilly And Company | Peptidomimetic protease inhibitors |
-
2003
- 2003-09-23 AU AU2003277891A patent/AU2003277891A1/en not_active Abandoned
- 2003-09-23 WO PCT/EP2003/010595 patent/WO2004026896A2/en not_active Application Discontinuation
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998017679A1 (en) * | 1996-10-18 | 1998-04-30 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease |
| WO2002008256A2 (en) * | 2000-07-21 | 2002-01-31 | Schering Corporation | Peptides as ns3-serine protease inhibitors of hepatitis c virus |
| WO2002018369A2 (en) * | 2000-08-31 | 2002-03-07 | Eli Lilly And Company | Peptidomimetic protease inhibitors |
Non-Patent Citations (2)
| Title |
|---|
| LLINAS-BRUNET M ET AL: "Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 8, no. 19, 6 October 1998 (1998-10-06), pages 2719 - 2724, XP004139608, ISSN: 0960-894X * |
| OSCARSSON KARIN ET AL: "Peptide-based inhibitors of hepatitis C virus full-length NS3 (protease-helicase/NTPase): Model compounds towards small molecule inhibitors.", BIOORGANIC AND MEDICINAL CHEMISTRY, vol. 11, no. 13, 3 July 2003 (2003-07-03), pages 2955 - 2963, XP002291168, ISSN: 0968-0896 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003277891A1 (en) | 2004-04-08 |
| WO2004026896A2 (en) | 2004-04-01 |
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