AR078461A1 - Inhibidores macrociclicos de la replicacion de virus de la hepatitis c - Google Patents

Inhibidores macrociclicos de la replicacion de virus de la hepatitis c

Info

Publication number
AR078461A1
AR078461A1 ARP100103511A ARP100103511A AR078461A1 AR 078461 A1 AR078461 A1 AR 078461A1 AR P100103511 A ARP100103511 A AR P100103511A AR P100103511 A ARP100103511 A AR P100103511A AR 078461 A1 AR078461 A1 AR 078461A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
group
cycloalkyl
independently selected
Prior art date
Application number
ARP100103511A
Other languages
English (en)
Inventor
Timothy Thrailkill
Scott D Seiwert
Antitsa D Stoycheva
Brad Buckman
John B Nicholas
Leonid Beigelman
Vladimir Serebryany
Original Assignee
Intermune Inc
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 Intermune Inc filed Critical Intermune Inc
Publication of AR078461A1 publication Critical patent/AR078461A1/es

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Classifications

    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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]
    • A61K38/217—IFN-gamma
    • 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
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Zoology (AREA)
  • Communicable Diseases (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Cultivation Of Seaweed (AREA)
  • Artificial Fish Reefs (AREA)
  • Apparatus Associated With Microorganisms And Enzymes (AREA)

Abstract

La presente adicionalmente proporciona métodos de tratamiento, lo que incluye los métodos para el tratamiento de una infeccion con el virus de la hepatitis C y los métodos para el tratamiento de la fibrosis hepática, métodos éstos que por lo general implican la administracion a un individuo que así lo requiere de una cantidad efectiva de un compuesto o composicion de la presente solicitud. Reivindicacion 1: Se reivindica un compuesto que se rige por la estructura de la formula (1), o una sal o prodroga farmacéuticamente aceptable del mismo, donde W1, W2, W3 y W4 independientemente representan -D o -H, siempre que al menos uno de W1, W2, W3 y W4 sea -D; R1 es seleccionado a partir del grupo constituido por -C(O)OR1e, heteroarilo opcionalmente sustituido y arilo opcionalmente sustituido con uno o más sustituyentes, cada uno seleccionado de manera independiente a partir del grupo constituido por halo, amino, alquilo C1-6 opcionalmente sustituido con hasta 5 fluores, alcoxi C1-6 opcionalmente sustituido con hasta 5 fluores, alquenilo C2-6, alquinilo C2-6, -C(O)NR1aR1b, -NHC(O)NR1aR1b, -C(O)OR1c y heteroarilo; R1e es seleccionado a partir del grupo constituido por t-butilo, cicloalquilo y heterociclilo; R1a y R1b son tomados conjuntamente con el nitrogeno al cual se encuentran unidos y forman un piperazinilo o morfolinilo, cada uno opcionalmente sustituido con uno o más sustituyentes seleccionados de manera independiente a partir de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, C(O)OR1c, -C(O)R1d, arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido; R1c y R1d son cada uno seleccionado de manera independiente a partir del grupo constituido por -H, alcoxi C1-4, alquilo C1-6, cicloalquilo C3-7, arilo, arilalquilo y heteroarilo; R3 es -OH, -NHS(O)2R3a, -NHS(O)2OR3a o -NHS(O)2NR3bR3c; donde R3a es seleccionado a partir del grupo constituido por alquilo C1-6, -(CH2)q-cicloalquilo C3-7, -(CH2)q-arilo C6 o 10 y un heteroarilo, cada uno opcionalmente sustituido con uno o más sustituyentes, cada uno seleccionado de manera independiente a partir del grupo constituido por halo, ciano, nitro, hidroxi, -COOH, -(CH2)t-cicloalquilo C3-7, alquenilo C2-6, hidroxi-alquilo C1-6, alquilo C1-6 opcionalmente sustituido con hasta 5 fluores y alcoxi C1-6 opcionalmente sustituido con hasta 5 fluores; donde cada uno de R3b y R3c independientemente representa un átomo de hidrogeno o es seleccionado de manera independiente a partir del grupo constituido por alquilo C1-6, -(CH2)q-cicloalquilo C3-7 y arilo C6 o 10, cada uno opcionalmente sustituido con uno o más sustituyentes y cada uno seleccionado de manera independiente a partir del grupo constituido por halo, ciano, nitro, hidroxi, -(CH2)t-cicloalquilo C3-7, alquenilo C2-6, hidroxi-alquilo C1-6, fenilo, alquilo C1-6 sustituido con hasta 5 fluores y alcoxi C1-6 sustituido con hasta 5 fluores; o R3b y R3c, tomados conjuntamente con el nitrogeno al cual se encuentran unidos, forman un anillo heterocíclico de tres a seis miembros acoplado a la estructura base a través de un nitrogeno y el anillo heterocíclico es opcionalmente sustituido con uno o más sustituyentes, cada uno seleccionado de manera independiente a partir del grupo constituido por halo, ciano, nitro, alquilo C1-6, alcoxi C1-6 y fenilo; cada t independientemente representa 0, 1 o 2; cada q independientemente representa 0, 1 o 2; y todo enlace representado por una línea continua y punteada representa un enlace seleccionado a partir del grupo constituido por un enlace simple y un enlace doble.
ARP100103511A 2009-09-28 2010-09-28 Inhibidores macrociclicos de la replicacion de virus de la hepatitis c AR078461A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24646509P 2009-09-28 2009-09-28
US32425110P 2010-04-14 2010-04-14

Publications (1)

Publication Number Publication Date
AR078461A1 true AR078461A1 (es) 2011-11-09

Family

ID=43796239

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103511A AR078461A1 (es) 2009-09-28 2010-09-28 Inhibidores macrociclicos de la replicacion de virus de la hepatitis c

Country Status (12)

Country Link
US (1) US20110129444A1 (es)
EP (1) EP2483273A4 (es)
JP (1) JP2013505951A (es)
KR (1) KR20120110090A (es)
CN (1) CN102712644A (es)
AR (1) AR078461A1 (es)
BR (1) BR112012006835A2 (es)
CA (1) CA2774387A1 (es)
MX (1) MX2012003171A (es)
RU (1) RU2012117395A (es)
TW (1) TW201124136A (es)
WO (1) WO2011038283A1 (es)

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US20090148407A1 (en) * 2005-07-25 2009-06-11 Intermune, Inc. Novel Macrocyclic Inhibitors of Hepatitis C Virus Replication
ATE493409T1 (de) * 2005-10-11 2011-01-15 Intermune Inc Verbindungen und verfahren zur inhibierung der replikation des hepatitis-c-virus
AP2010005416A0 (en) * 2008-04-15 2010-10-31 Intermune Inc Novel macrocyclic inhibitors of hepatitis c virus replication.
AU2009303483A1 (en) * 2008-10-15 2010-04-22 Intermune, Inc. Therapeutic antiviral peptides
AR075584A1 (es) 2009-02-27 2011-04-20 Intermune Inc COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO.
TW201116540A (en) * 2009-10-01 2011-05-16 Intermune Inc Therapeutic antiviral peptides
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2726475B1 (en) * 2011-05-27 2017-10-25 Bristol-Myers Squibb Company Tripeptides incorporating deuterium as inhibitors of hepatitis c virus
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EA025560B1 (ru) 2012-10-19 2017-01-30 Бристол-Майерс Сквибб Компани Ингибиторы вируса гепатита с
WO2014071007A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
WO2014070964A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
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WO2014137869A1 (en) 2013-03-07 2014-09-12 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
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Also Published As

Publication number Publication date
EP2483273A1 (en) 2012-08-08
US20110129444A1 (en) 2011-06-02
JP2013505951A (ja) 2013-02-21
RU2012117395A (ru) 2013-11-10
CA2774387A1 (en) 2011-03-31
TW201124136A (en) 2011-07-16
CN102712644A (zh) 2012-10-03
MX2012003171A (es) 2012-04-11
WO2011038283A1 (en) 2011-03-31
EP2483273A4 (en) 2013-05-01
BR112012006835A2 (pt) 2016-06-07
KR20120110090A (ko) 2012-10-09

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