AR079130A1 - Compuestos inhibidores de la hepatitis c - Google Patents

Compuestos inhibidores de la hepatitis c

Info

Publication number
AR079130A1
AR079130A1 ARP100104321A ARP100104321A AR079130A1 AR 079130 A1 AR079130 A1 AR 079130A1 AR P100104321 A ARP100104321 A AR P100104321A AR P100104321 A ARP100104321 A AR P100104321A AR 079130 A1 AR079130 A1 AR 079130A1
Authority
AR
Argentina
Prior art keywords
alkyl
halo
optionally substituted
hepatitis
compounds
Prior art date
Application number
ARP100104321A
Other languages
English (en)
Inventor
Melissa Leblanc
Benoit Moreau
Montse Llinas-Brunet
Jeffrey O'meara
Josee Bordeleau
Cedrickx Godbout
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR079130A1 publication Critical patent/AR079130A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • C07K5/0804—Tripeptides 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
    • C07K5/10—Tetrapeptides
    • C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
    • 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)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Los compuestos mantienen actividad frente a proteasas NS3 que contienen mutaciones de resistencia R155K en el genotipo 1a y D168V en el genotipo 1b clínicamente relevantes. Los compuestos son inhibidores de la proteasa NS3 de VHC para el tratamiento de una infeccion por el virus de la hepatitis C. Composiciones farmacéuticas y usos. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1) o un racemato, diastereoisomero, isomero optico o sal de éste en la que R1 es H o alquilo C1-6; R2 es alquilo C1-6 sustituido opcionalmente 1-3 veces con halo o cicloalquilo C3-7; R3 es aIquilo C1-6), -O-aIquilo C1-6 o halo; R4 es -O-alquilo C1-6, -OH o halo; R5 es Het sustituido opcionalmente 1-3 veces con alquilo C1-6, -aIquilo C1-6-C(=O)- N(alquilo C1-6))2, -alquilo C1-6-O-alquilo C1-6 o haloalquilo C1-6; o R5 es -N(RA)(RB) en el que RA y RB son alquilo C1-6 o RA y RB están unidos junto con el N al que están unidos para formar un anillo saturado de 4 a 7 miembros, en el que dicho anillo está sustituido opcionalmente 1-3 veces con alquilo C1-6, -O-aIquilo C1-6, -OH o halo.
ARP100104321A 2009-11-24 2010-11-23 Compuestos inhibidores de la hepatitis c AR079130A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26413609P 2009-11-24 2009-11-24

Publications (1)

Publication Number Publication Date
AR079130A1 true AR079130A1 (es) 2011-12-28

Family

ID=44065772

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100104321A AR079130A1 (es) 2009-11-24 2010-11-23 Compuestos inhibidores de la hepatitis c

Country Status (6)

Country Link
US (1) US20110294778A1 (es)
EP (1) EP2504344A4 (es)
JP (1) JP2013511562A (es)
AR (1) AR079130A1 (es)
TW (1) TW201129369A (es)
WO (1) WO2011063502A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY32099A (es) 2008-09-11 2010-04-30 Enanta Pharm Inc Inhibidores macrocíclicos de serina proteasas de hepatitis c
CN103380132B (zh) 2010-12-30 2016-08-31 益安药业 菲啶大环丙型肝炎丝氨酸蛋白酶抑制剂
CA2822556A1 (en) 2010-12-30 2012-07-05 Enanta Pharmaceuticals, Inc Macrocyclic hepatitis c serine protease inhibitors
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US10201584B1 (en) 2011-05-17 2019-02-12 Abbvie Inc. Compositions and methods for treating HCV
US8691757B2 (en) 2011-06-15 2014-04-08 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CN102408386B (zh) * 2011-07-27 2014-05-07 雅本化学股份有限公司 2,4-二取代-2h-1,2,3-三氮唑衍生物的制备方法
JP2015533124A (ja) * 2012-10-08 2015-11-19 アッヴィ・インコーポレイテッド Ｈｃｖプロテアーゼ阻害剤を作製するのに有用な化合物
EA025560B1 (ru) 2012-10-19 2017-01-30 Бристол-Майерс Сквибб Компани Ингибиторы вируса гепатита с
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014070964A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
WO2014071007A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
EP2914614B1 (en) 2012-11-05 2017-08-16 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
WO2014137869A1 (en) 2013-03-07 2014-09-12 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
WO2015103490A1 (en) 2014-01-03 2015-07-09 Abbvie, Inc. Solid antiviral dosage forms
KR20180107261A (ko) 2016-02-16 2018-10-01 메사추세츠 인스티튜트 오브 테크놀로지 Myc 조정제로서의 MAX 결합제 및 그의 용도

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US6867185B2 (en) * 2001-12-20 2005-03-15 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
US20050159345A1 (en) * 2002-10-29 2005-07-21 Boehringer Ingelheim International Gmbh Composition for the treatment of infection by Flaviviridae viruses
ES2358333T3 (es) * 2004-01-21 2011-05-09 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos con acción contra el virus de la hepatitis c.
UY30437A1 (es) * 2006-06-26 2008-01-31 Enanta Pharm Inc Quinoxalinil macroceclicos inhibidores de serina proteasa del virus de la hepatitis c
EA200970493A1 (ru) * 2006-11-17 2009-10-30 Тиботек Фармасьютикалз Лтд. Макроциклические ингибиторы вируса гепатита с

Also Published As

Publication number Publication date
TW201129369A (en) 2011-09-01
EP2504344A4 (en) 2013-06-05
WO2011063502A1 (en) 2011-06-03
US20110294778A1 (en) 2011-12-01
EP2504344A1 (en) 2012-10-03
JP2013511562A (ja) 2013-04-04

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