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PE20080355A1 - Compuestos peptidicos como inhibidores de proteasa de serina del virus de hepatitis c - Google Patents

Compuestos peptidicos como inhibidores de proteasa de serina del virus de hepatitis c

Info

Publication number
PE20080355A1
PE20080355A1 PE2007000434A PE2007000434A PE20080355A1 PE 20080355 A1 PE20080355 A1 PE 20080355A1 PE 2007000434 A PE2007000434 A PE 2007000434A PE 2007000434 A PE2007000434 A PE 2007000434A PE 20080355 A1 PE20080355 A1 PE 20080355A1
Authority
PE
Peru
Prior art keywords
alkyl
cycloalkyl
methyl
hepatitis
virus
Prior art date
Application number
PE2007000434A
Other languages
English (en)
Inventor
Dongpeng Wan
Prakash Raman
David Thomas Parker
Mohindra Seepersaud
Jiping Fu
Branko Radetich
Michael Patane
Pascal Rigollier
Stefan Andreas Randl
Claus Ehrhardt
Sylvain Cottens
Oliver Simic
Original Assignee
Novartis Ag
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20080355A1 publication Critical patent/PE20080355A1/es

Links

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
    • C07K5/0812—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
    • C07K5/06—Dipeptides
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • C07K5/06078—Dipeptides 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
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; 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
    • C07K5/04—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
    • 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
    • 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
    • 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
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE X E Y ES 0 O 1; R1 ES H Y ALQUILO; R2 ES ALQUILO(C1-C4), CO-ALQUILO(C1-C4), CICLOALQUILO(C3-C6)ALQUILO(C0-C4), ENTRE OTROS; O R1 Y R2 JUNTOS FORMAN UN ANILLO DE 3 A 7 MIEMBROS; W ES C(O)OR24, C(O)-C(O)-AMINA, CON(H)SO2-AMINA, C(O)-[C(O)]a-HETEROCICLO OPCIONALMENTE SUSTITUIDO; R3 ES H O ALQUILO; R4 Y R6 SON INDEPENDIENTEMENTE H, ALQUILO(C1-C4), CICLOALQUILO(C3-C6), CICLOALQUILO(C3-C6)ALQUILO(C3-C6), ARIL, HETEROCICLO, OPCIONALMENTE SUSTITUIDOS; R5 ES H; R8, R10 Y R11 SON INDEPENDIENTEMENTE H Y ALQUILO; R13 ES H; R12 ES H, ALQUIL(C1-C4),CICLOALQUILO(C3-C6), ARILO, ENTRE OTROS; V ES -Q1-Q2, EN DONDE Q1 ESTA AUSENTE, C(O), S(O)2, N-(ALQUIL(C1-C4), ENTRE OTROS; Q2 ES H, ALQUILO(C1-C4), O-ALQUIL(C1-C4), N(H) ALQUIL(C1-C4),ENTRE OTROS. SON SELECCIONADOS: TERBUTIL-ESTER DEL ACIDO {[(1R,2R)-1-(3-BENCILOXI-BENCEN-SULFONIL-AMINO-CARBONIL)-2-VINIL-CICLOPROPIL-CARBAMOIL]-METIL}-CICLOPENTIL-METIL-CARBAMICO, TERBUTIL-ESTER DEL ACIDO [(S)-1-(CICLOHEXIL-METIL-{[(1S,2S)-2-(1H-INDOL-7-SULFONIL-AMINO-CARBONIL)-BICICLOPROPIL-2-IL-CARBAMOIL]-METIL}-CARBAMOIL)-2-METIL-PROPIL]-CARBAMICO, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON MODULADORES DE LA ACTIVIDAD DE LAS PROTEASAS DE SERINA DEL VIRUS DE HEPATITIS C, EN PARTICULAR LA PROTEASA DE SERINA NS3/ NS4a Y SON UTILES EN EL TRATAMIENTO DE INFECCION POR EL VIRUS DE HEPATITIS C
PE2007000434A 2006-04-11 2007-04-10 Compuestos peptidicos como inhibidores de proteasa de serina del virus de hepatitis c PE20080355A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US79157806P 2006-04-11 2006-04-11

Publications (1)

Publication Number Publication Date
PE20080355A1 true PE20080355A1 (es) 2008-06-02

Family

ID=38516151

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007000434A PE20080355A1 (es) 2006-04-11 2007-04-10 Compuestos peptidicos como inhibidores de proteasa de serina del virus de hepatitis c

Country Status (15)

Country Link
US (1) US20070265281A1 (es)
EP (1) EP2007788A2 (es)
JP (1) JP2009536158A (es)
KR (1) KR20080104366A (es)
CN (1) CN101421292A (es)
AR (1) AR060385A1 (es)
AU (1) AU2007238253A1 (es)
BR (1) BRPI0710183A2 (es)
CA (1) CA2648678A1 (es)
CL (1) CL2007001004A1 (es)
MX (1) MX2008013125A (es)
PE (1) PE20080355A1 (es)
RU (1) RU2008144294A (es)
TW (1) TW200815479A (es)
WO (1) WO2007121125A2 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7825152B2 (en) 2006-04-11 2010-11-02 Novartis Ag Organic compounds and their uses
CN101868452B (zh) 2007-10-10 2014-08-06 诺华股份有限公司 螺环吡咯烷类与其对抗hcv和hiv感染的应用
AR070413A1 (es) 2008-02-04 2010-04-07 Idenix Pharmaceuticals Inc Inhibidores macrociclicos de proteasa de serina
CA2722858C (en) * 2008-04-30 2017-08-29 Siemens Medical Solutions Usa, Inc. Substrate based pet imaging agents
US8377962B2 (en) 2009-04-08 2013-02-19 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
EP2461811B1 (en) 2009-08-05 2016-04-20 Idenix Pharmaceuticals LLC. Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv
CN103108651A (zh) * 2010-07-30 2013-05-15 默沙东公司 Cyp3a药物代谢的抑制
WO2012109398A1 (en) 2011-02-10 2012-08-16 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating hcv infections
JPWO2012176715A1 (ja) * 2011-06-21 2015-02-23 三菱瓦斯化学株式会社 １−アミノ−２−ビニルシクロプロパンカルボン酸アミドおよびその塩、ならびにその製造方法
CN108658826B (zh) * 2018-06-02 2020-05-12 上海三牧化工技术有限公司 一种制备维达列汀的方法
CA3240164A1 (en) * 2021-12-20 2023-06-29 Kyoji TSUCHIKAMA Tripeptide linkers and methods of use thereof

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002008187A1 (en) * 2000-07-21 2002-01-31 Schering Corporation Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
MY139078A (en) * 2000-07-21 2009-08-28 Schering Corp Peptides as ns3-serine protease inhibitors of hepatitis c virus
TWI265927B (en) * 2002-01-23 2006-11-11 Schering Corp Novel compounds as NS3-serine protease inhibitors of hepatitis C virus
CA2370396A1 (en) * 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
US6642204B2 (en) * 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
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
US7635694B2 (en) * 2004-02-27 2009-12-22 Schering Corporation Cyclobutenedione-containing compounds as inhibitors of hepatitis C virus NS3 serine protease
TW200602037A (en) * 2004-02-27 2006-01-16 Schering Corp Novel compounds as inhibitors of hepatitis C virus NS3 serine protease
ATE514691T1 (de) * 2004-02-27 2011-07-15 Schering Corp Neue ketoamide mit cyclischen p4 als inhibitoren der ns3-serinprotease von hepatitis-c-virus
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
WO2005113581A1 (en) * 2004-05-20 2005-12-01 Schering Corporation Substituted prolines as inhibitors of hepatitis c virus ns3 serine protease
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.
WO2006130626A2 (en) * 2005-06-02 2006-12-07 Schering Corporation Method for modulating activity of hcv protease through use of a novel hcv protease inhibitor to reduce duration of treatment period

Also Published As

Publication number Publication date
WO2007121125A3 (en) 2008-04-24
BRPI0710183A2 (pt) 2011-08-09
CA2648678A1 (en) 2007-10-25
KR20080104366A (ko) 2008-12-02
US20070265281A1 (en) 2007-11-15
RU2008144294A (ru) 2010-05-20
WO2007121125A2 (en) 2007-10-25
EP2007788A2 (en) 2008-12-31
AR060385A1 (es) 2008-06-11
AU2007238253A1 (en) 2007-10-25
MX2008013125A (es) 2008-10-21
TW200815479A (en) 2008-04-01
CN101421292A (zh) 2009-04-29
JP2009536158A (ja) 2009-10-08
CL2007001004A1 (es) 2008-03-14

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