MX2010005261A - Inhibidores macrocíclicos de proteasa de serina de hepatitis c de tetrazolilo. - Google Patents
Inhibidores macrocíclicos de proteasa de serina de hepatitis c de tetrazolilo.Info
- Publication number
- MX2010005261A MX2010005261A MX2010005261A MX2010005261A MX2010005261A MX 2010005261 A MX2010005261 A MX 2010005261A MX 2010005261 A MX2010005261 A MX 2010005261A MX 2010005261 A MX2010005261 A MX 2010005261A MX 2010005261 A MX2010005261 A MX 2010005261A
- Authority
- MX
- Mexico
- Prior art keywords
- hepatitis
- present
- serine protease
- macrocyclic
- tetrazolyl
- Prior art date
Links
- 208000006454 hepatitis Diseases 0.000 title 1
- 231100000283 hepatitis Toxicity 0.000 title 1
- 239000003001 serine protease inhibitor Substances 0.000 title 1
- 125000003831 tetrazolyl group Chemical group 0.000 title 1
- 241000711549 Hepacivirus C Species 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- 230000000694 effects Effects 0.000 abstract 2
- 208000015181 infectious disease Diseases 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 1
- 102000012479 Serine Proteases Human genes 0.000 abstract 1
- 108010022999 Serine Proteases Proteins 0.000 abstract 1
- 239000003443 antiviral agent Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 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
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/19—Cytokines; Lymphokines; Interferons
- A61K38/21—Interferons [IFN]
- A61K38/212—IFN-alpha
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/19—Cytokines; Lymphokines; Interferons
- A61K38/21—Interferons [IFN]
- A61K38/215—IFN-beta
-
- 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
- C07K5/04—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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Zoology (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención se refiere a compuestos de la fórmula (I), (II), (III) o (IV), o sales farmacéuticamente aceptables, ésteres o profármacos de los mismos, los cuales inhiben la actividad de proteasa de serina, particularmente la actividad de proteasa NS3- NS4A del virus de hepatitis C (HCV). Consecuentemente, los compuestos de la presente invención interfieren con el ciclo de vida del virus de hepatitis C y también son útiles como agentes antivirales. La presente invención también se refiere a composiciones farmacéuticas que comprenden los compuestos antes mencionados para administrarse a un sujeto que padece de infección por HCV. La invención también se refiere a métodos para tratar una infección por HCV en un sujeto, administrando una composición farmacéutica que comprende el compuesto de la presente invención.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US98796207P | 2007-11-14 | 2007-11-14 | |
PCT/US2008/083505 WO2009064955A1 (en) | 2007-11-14 | 2008-11-14 | Macrocyclic tetrazolyl hepatitis c serine protease inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2010005261A true MX2010005261A (es) | 2010-10-15 |
Family
ID=40639138
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2010005261A MX2010005261A (es) | 2007-11-14 | 2008-11-14 | Inhibidores macrocíclicos de proteasa de serina de hepatitis c de tetrazolilo. |
Country Status (7)
Country | Link |
---|---|
US (1) | US8304385B2 (es) |
EP (1) | EP2219454A4 (es) |
JP (1) | JP2011503201A (es) |
CN (1) | CN102026544A (es) |
CA (1) | CA2705803A1 (es) |
MX (1) | MX2010005261A (es) |
WO (1) | WO2009064955A1 (es) |
Families Citing this family (39)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2006119061A2 (en) | 2005-05-02 | 2006-11-09 | Merck & Co., Inc. | Hcv ns3 protease inhibitors |
US7470664B2 (en) | 2005-07-20 | 2008-12-30 | Merck & Co., Inc. | HCV NS3 protease inhibitors |
CA2615896C (en) | 2005-08-01 | 2012-11-13 | Merck & Co., Inc. | Macrocyclic peptides as hcv ns3 protease inhibitors |
GB0609492D0 (en) | 2006-05-15 | 2006-06-21 | Angeletti P Ist Richerche Bio | Therapeutic agents |
GB0612423D0 (en) | 2006-06-23 | 2006-08-02 | Angeletti P Ist Richerche Bio | Therapeutic agents |
US8377873B2 (en) | 2006-10-24 | 2013-02-19 | Merck Sharp & Dohme Corp. | HCV NS3 protease inhibitors |
JP5345941B2 (ja) | 2006-10-24 | 2013-11-20 | メルク・シャープ・アンド・ドーム・コーポレーション | Hcvns3プロテアーゼ阻害剤 |
US8138164B2 (en) | 2006-10-24 | 2012-03-20 | Merck Sharp & Dohme Corp. | HCV NS3 protease inhibitors |
JP5352464B2 (ja) | 2006-10-27 | 2013-11-27 | メルク・シャープ・アンド・ドーム・コーポレーション | Hcvns3プロテアーゼ阻害剤 |
MY164469A (en) | 2006-10-27 | 2017-12-15 | Msd Italia Srl | Hcv ns3 protease inhibitors |
WO2008075103A1 (en) | 2006-12-20 | 2008-06-26 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | Antiviral indoles |
GB0625345D0 (en) | 2006-12-20 | 2007-01-31 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
GB0625349D0 (en) | 2006-12-20 | 2007-01-31 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
CN101801982A (zh) | 2007-07-17 | 2010-08-11 | P.安杰莱蒂分子生物学研究所 | 用于治疗丙型肝炎感染的大环吲哚衍生物 |
CN101754974B (zh) | 2007-07-19 | 2016-02-03 | Msd意大利有限公司 | 作为抗病毒剂的大环化合物 |
US8383583B2 (en) | 2007-10-26 | 2013-02-26 | Enanta Pharmaceuticals, Inc. | Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors |
CL2008003384A1 (es) * | 2007-11-14 | 2009-12-11 | Enanta Pharm Inc | Compuestos derivados de quinoxalina macrocíclica, inhibidores de serina proteasa; composicion farmaceutica que los comprende; y su uso en el tratamiento de la hepatitis c. |
WO2009070689A1 (en) * | 2007-11-29 | 2009-06-04 | Enanta Pharmaceuticals, Inc. | Bicyclic, c5-substituted proline derivatives as inhibitors of the hepatitis c virus ns3 protease |
US8273709B2 (en) | 2007-12-14 | 2012-09-25 | Enanta Pharmaceuticals, Inc. | Triazole-containing macrocyclic HCV serine protease inhibitors |
US8222203B2 (en) * | 2007-12-14 | 2012-07-17 | Enanta Pharmaceuticals, Inc. | Macrocyclic oximyl hepatitis C serine protease inhibitors |
US8283309B2 (en) * | 2007-12-20 | 2012-10-09 | Enanta Pharmaceuticals, Inc. | Bridged carbocyclic oxime hepatitis C virus serine protease inhibitors |
WO2009117594A1 (en) * | 2008-03-20 | 2009-09-24 | Enanta Pharmaceuticals, Inc. | Fluorinated macrocyclic compounds as hepatitis c virus inhibitors |
WO2009134624A1 (en) | 2008-04-28 | 2009-11-05 | Merck & Co., Inc. | Hcv ns3 protease inhibitors |
US8211891B2 (en) * | 2008-04-30 | 2012-07-03 | Enanta Pharmaceuticals, Inc. | Difluoromethyl-containing macrocyclic compounds as hepatitis C virus inhibitors |
EP2310095B1 (en) | 2008-07-22 | 2012-08-29 | Merck Sharp & Dohme Corp. | Macrocyclic quinoxaline compounds as hcv ns3 protease inhibitors |
JP5639155B2 (ja) | 2009-05-13 | 2014-12-10 | エナンタ ファーマシューティカルズ インコーポレイテッド | C型肝炎ウイルスインヒビターとしての大環状化合物 |
WO2011014487A1 (en) | 2009-07-30 | 2011-02-03 | Merck Sharp & Dohme Corp. | Hepatitis c virus ns3 protease inhibitors |
WO2011049908A2 (en) * | 2009-10-19 | 2011-04-28 | Enanta Pharmaceuticals, Inc. | Bismacrokyclic compounds as hepatitis c virus inhibitors |
NZ608720A (en) | 2010-09-21 | 2015-03-27 | Enanta Pharm Inc | Macrocyclic proline derived hcv serine protease inhibitors |
US8957203B2 (en) | 2011-05-05 | 2015-02-17 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
WO2012171332A1 (zh) * | 2011-06-16 | 2012-12-20 | 爱博新药研发(上海)有限公司 | 抑制丙型肝炎病毒的大环状杂环化合物及其制备和应用 |
WO2014062196A1 (en) | 2012-10-19 | 2014-04-24 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
EP2914598B1 (en) | 2012-11-02 | 2017-10-18 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
WO2014070964A1 (en) | 2012-11-02 | 2014-05-08 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
US9643999B2 (en) | 2012-11-02 | 2017-05-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
EP2914614B1 (en) | 2012-11-05 | 2017-08-16 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
US9580463B2 (en) | 2013-03-07 | 2017-02-28 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US11484534B2 (en) | 2013-03-14 | 2022-11-01 | Abbvie Inc. | Methods for treating HCV |
EP2899207A1 (en) | 2014-01-28 | 2015-07-29 | Amikana.Biologics | New method for testing HCV protease inhibition |
Family Cites Families (35)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5861297A (en) | 1996-09-27 | 1999-01-19 | Merck & Co., Inc. | Detergent-free hepatitis C protease |
US6323180B1 (en) | 1998-08-10 | 2001-11-27 | Boehringer Ingelheim (Canada) Ltd | Hepatitis C inhibitor tri-peptides |
US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
DE60137207D1 (de) | 2000-04-05 | 2009-02-12 | Schering Corp | Makrozyklische inhibitoren der ns3-serinprotease des hepatitis c-virus mit stickstoffhaltigen zyklischen p2-gruppen |
JP4368581B2 (ja) | 2000-12-12 | 2009-11-18 | 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阻害剤としてのジアリールペプチド |
MY140680A (en) | 2002-05-20 | 2010-01-15 | Bristol Myers Squibb Co | Hepatitis c virus inhibitors |
US7601709B2 (en) * | 2003-02-07 | 2009-10-13 | Enanta Pharmaceuticals, Inc. | Macrocyclic hepatitis C serine protease inhibitors |
WO2004094452A2 (en) | 2003-04-16 | 2004-11-04 | Bristol-Myers Squibb Company | Macrocyclic isoquinoline peptide inhibitors of hepatitis c virus |
US7176208B2 (en) | 2003-04-18 | 2007-02-13 | Enanta Pharmaceuticals, Inc. | Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors |
WO2004113365A2 (en) | 2003-06-05 | 2004-12-29 | Enanta Pharmaceuticals, Inc. | Hepatitis c serine protease tri-peptide inhibitors |
US7273851B2 (en) | 2003-06-05 | 2007-09-25 | Enanta Pharmaceuticals, Inc. | Tri-peptide hepatitis C serine protease inhibitors |
US7125845B2 (en) | 2003-07-03 | 2006-10-24 | Enanta Pharmaceuticals, Inc. | Aza-peptide macrocyclic hepatitis C serine protease inhibitors |
EA014584B1 (ru) * | 2004-01-30 | 2010-12-30 | Медивир Аб | Ингибиторы ns-3 сериновой протеазы hcv |
NZ552405A (en) | 2004-07-16 | 2011-04-29 | Gilead Sciences Inc | Pyrrolidine containing antiviral compounds |
UY29016A1 (es) | 2004-07-20 | 2006-02-24 | Boehringer Ingelheim Int | Analogos de dipeptidos inhibidores de la hepatitis c |
WO2007001406A2 (en) | 2004-10-05 | 2007-01-04 | Chiron Corporation | Aryl-containing macrocyclic compounds |
US7323447B2 (en) | 2005-02-08 | 2008-01-29 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
WO2006119061A2 (en) | 2005-05-02 | 2006-11-09 | Merck & Co., Inc. | Hcv ns3 protease inhibitors |
US7470664B2 (en) * | 2005-07-20 | 2008-12-30 | Merck & Co., Inc. | HCV NS3 protease inhibitors |
CN101273052B (zh) | 2005-07-29 | 2016-01-13 | 爱尔兰詹森科学公司 | 丙型肝炎病毒的大环抑制剂 |
DK1912997T3 (da) | 2005-07-29 | 2012-01-02 | Tibotec Pharm Ltd | Makrocycliske inhibitorer af hepatitis C virus |
AR055105A1 (es) | 2005-07-29 | 2007-08-08 | Tibotec Pharm Ltd | Inhibidores macrociclicos del virus de la hepatitis c |
JO2768B1 (en) | 2005-07-29 | 2014-03-15 | تيبوتيك فارماسيوتيكالز ليمتد | Large cyclic inhibitors of hepatitis C virus |
CA2615896C (en) | 2005-08-01 | 2012-11-13 | Merck & Co., Inc. | Macrocyclic peptides as hcv ns3 protease inhibitors |
US7728148B2 (en) | 2006-06-06 | 2010-06-01 | Enanta Pharmaceuticals, Inc. | Acyclic oximyl hepatitis C protease inhibitors |
CA2656816A1 (en) | 2006-08-04 | 2008-02-14 | Enanta Pharmaceuticals, Inc. | Tetrazolyl macrocyclic hepatitis c serine protease inhibitors |
US20090035268A1 (en) | 2007-08-01 | 2009-02-05 | Ying Sun | Tetrazolyl acyclic hepatitis c serine protease inhibitors |
MY164469A (en) | 2006-10-27 | 2017-12-15 | Msd Italia Srl | Hcv ns3 protease inhibitors |
CN101754974B (zh) | 2007-07-19 | 2016-02-03 | Msd意大利有限公司 | 作为抗病毒剂的大环化合物 |
US8383583B2 (en) | 2007-10-26 | 2013-02-26 | Enanta Pharmaceuticals, Inc. | Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors |
US8222203B2 (en) | 2007-12-14 | 2012-07-17 | Enanta Pharmaceuticals, Inc. | Macrocyclic oximyl hepatitis C serine protease inhibitors |
US8273709B2 (en) | 2007-12-14 | 2012-09-25 | Enanta Pharmaceuticals, Inc. | Triazole-containing macrocyclic HCV serine protease inhibitors |
US8283309B2 (en) | 2007-12-20 | 2012-10-09 | Enanta Pharmaceuticals, Inc. | Bridged carbocyclic oxime hepatitis C virus serine protease inhibitors |
WO2009117594A1 (en) * | 2008-03-20 | 2009-09-24 | Enanta Pharmaceuticals, Inc. | Fluorinated macrocyclic compounds as hepatitis c virus inhibitors |
US8211891B2 (en) | 2008-04-30 | 2012-07-03 | Enanta Pharmaceuticals, Inc. | Difluoromethyl-containing macrocyclic compounds as hepatitis C virus inhibitors |
-
2008
- 2008-11-14 WO PCT/US2008/083505 patent/WO2009064955A1/en active Application Filing
- 2008-11-14 CA CA2705803A patent/CA2705803A1/en not_active Abandoned
- 2008-11-14 US US12/270,963 patent/US8304385B2/en not_active Expired - Fee Related
- 2008-11-14 CN CN2008801251194A patent/CN102026544A/zh active Pending
- 2008-11-14 EP EP08850897A patent/EP2219454A4/en not_active Withdrawn
- 2008-11-14 MX MX2010005261A patent/MX2010005261A/es not_active Application Discontinuation
- 2008-11-14 JP JP2010534200A patent/JP2011503201A/ja not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
WO2009064955A1 (en) | 2009-05-22 |
EP2219454A4 (en) | 2012-05-30 |
US20090142299A1 (en) | 2009-06-04 |
EP2219454A1 (en) | 2010-08-25 |
US8304385B2 (en) | 2012-11-06 |
JP2011503201A (ja) | 2011-01-27 |
CN102026544A (zh) | 2011-04-20 |
CA2705803A1 (en) | 2009-05-22 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Abandonment or withdrawal |