AR080263A1 - Inhibidores ns5a de vhc - Google Patents

Inhibidores ns5a de vhc

Info

Publication number
AR080263A1
AR080263A1 ARP090104676A ARP090104676A AR080263A1 AR 080263 A1 AR080263 A1 AR 080263A1 AR P090104676 A ARP090104676 A AR P090104676A AR P090104676 A ARP090104676 A AR P090104676A AR 080263 A1 AR080263 A1 AR 080263A1
Authority
AR
Argentina
Prior art keywords
heteroaryl
group
independently
heterocycle
aryl
Prior art date
Application number
ARP090104676A
Other languages
English (en)
Original Assignee
Presidio Pharnaceuticals 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42233599&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR080263(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Presidio Pharnaceuticals Inc filed Critical Presidio Pharnaceuticals Inc
Publication of AR080263A1 publication Critical patent/AR080263A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Composiciones farmacéuticas y terapias de combinacion para la inhibicion de la hepatitis C. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1): donde A se selecciona del grupo formado por: -(CR2)n-C(O)-(CR2)p-, -(CR2)n-O-(CR2)p-, -(CR2)n-N(RN)-(CR2)p-, -(CR2)n-S(O)k-N(RN)-(CR2)p-, -(CR2)n-C(O)-N(RN)-(CR2)p-, -(CR2)n-N(RN)-C(O)-N(RN)-(CR2)p-, -(CR2)n-C(O)-O-(CR2)p-, -(CR2)n-N(RN)-S(O)k-N(RN)-(CR2)p-, y -(CR2)n-N(RN)-C(O)-O-(CR2)p-, y un grupo heteroarilo seleccionado del grupo formado por: (2) donde X1 es CH2, NH, O o S, Y1, Y2 y Z1 son, cada uno, independientemente, CH o N, X2 es NH, O o S, V es -CH2-CH2-, -CH=CH-, -N=CH-, (CH2)a-N(RN)-(CH2)b- o -(CH2)a-O-(CH2)b-, donde a y b son, independientemente 0, 1, 2, o 3 con la condicion de que a y b no sean ambos 0, (3), incluye opcionalmente 1 o 2 nitrogenos como heteroátomos en el residuo fenilo, los carbonos del grupo heteroarilo están, cada uno, independiente y opcionalmente sustituidos con un sustituyente seleccionado del grupo formado por halogeno, -OH, -CN, -NO2, halogeno, alquilo de C1-12, heteroarilo de C1-12, cicloalquilo, heterociclo, arilo, heteroarilo, aralquilo, alcoxilo, alcoxicarbonilo, alcanoilo, carbamoilo, sulfonilo sustituido, sulfonato, sulfonamida y amino, los nitrogenos del grupo heteroarilo, si están presentes, están, cada uno, independiente y opcionalmente sustituidos con un sustituyente seleccionado del grupo formado por -OH, alquilo de C1-12, heteroarilo de C1-12, cicloalquilo, heterociclo, arilo, heteroarilo, aralquilo, alcoxilo, alcoxicarbonilo, alcanoilo, carbamoilo, sulfonilo sustituido, sulfonato y sulfonamida, a y b son independientemente 1, 2, o 3. c y d son independientemente 1 o 2, n y p son independientemente 0, 1, 2 o 3, k es 0, 1, o 2, cada R se selecciona independientemente del grupo formado por hidrogeno, halogeno, -OH, -CN, -NO2, halogeno, alquilo de C1-12, heteroarilo de C1-12, cicloalquilo, heterociclo, arilo, heteroarilo, aralquilo, alcoxilo, alcoxicarbonilo, alcanoilo, carbamoilo, sulfonilo sustituido, sulfonato, sulfonamida y amino. Cada RN se selecciona independientemente del grupo formado por hidrogeno, -OH, alquilo de C1-12, heteroarilo de C1-12, cicloalquilo, heterociclo, arilo, heteroarilo, aralquilo, alcoxilo, alcoxicarbonilo, alcanoilo, carbamoilo, sulfonilo sustituido, sulfonato y sulfonamida, y donde B puede estar ligado a cualquier lado de A' de manera que, siendo el ejemplo de A': (4) W-B-A' puede ser o (5) o (6); B y B' son, cada uno, independientemente un anillo de 4 a 7 miembros que es un arilo, heteroarilo, cicloalquilo o heterociclo donde cada heteroátomo, si está presente, es, independientemente, N, O o S y donde al menos uno de B o B' es aromático; cada Ra se selecciona independientemente del grupo formado por -OH, -CH, -NO2, halogeno, alquilo de C1-12, heteroarilo de C1-12, cicloalquilo, heterociclo, arilo, heteroarilo, aralquilo, alcoxilo, alcoxicarbonilo, alcanoilo, carbamoilo, sulfonilo sustituido, sulfonato, sulfonamida y amino; y si B o B' no son aromáticos, también puede estar sustituido con uno o más oxo; cada r se selecciona independientemente del grupo formado por 0, 1, 2 y 3; W se selecciona independientemente entre (7) donde: X1 es CH2, NH, O o S, Y1, Y2 y Z1 son, cada uno, independientemente CH o N, X2 es NH, O o S, V es -CH2-CH2-, -CH=CH-, -N=CH-, (CH2)a-N(RN)-(CH2)b- o -(CH2)a-O-(CH2)b-, donde a y b son independientemente 0, 1, 2, o 3 con la condicion de que a y b no sean ambos 0, (3) incluye opcionalmente 1 o 2 nitrogenos como heteroátomos en el residuo fenilo, W está opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo formado por OH, -CH, -NO2, halogeno, alquilo de C1-12, heteroarilo de C1-12, cicloalquilo, heterociclo, arilo, heteroarilo, aralquilo, alcoxilo, alcoxicarbonilo, alcanoilo, carbamoilo, sulfonilo sustituido, sulfonato, sulfonamida y amino, W y el anillo B' pueden estar conectados mediante cualquiera de: un átomo de carbono o nitrogeno en B', y Cy es un cicloalquilo monociclico o bicíclico de 5 a 10 miembros, heterociclo, grupo arilo o grupo heteroarilo donde hasta tres heteroátomos son, independientemente, N, S u O y que está opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo formado por OH, -CH, -NO2, halogeno, alquilo de C1-12, heteroarilo de C1-12, cicloalquilo, heterociclo, arilo, heteroarilo, aralquilo, alcoxilo, alcoxicarbonilo, alcanoilo, carbamoilo, sulfonilo sustituido, sulfonato, sulfonamida y amino; cada Rc, Rd, Re y Rf se selecciona, independientemente, del grupo formado por: alquilo de C1-8, heteroalquilo de C1-8, aralquilo y un anillo de 4 a 8 miembros que puede ser cicloalquilo, heterociclo, heteroarilo o arilo, donde cada heteroátomo, si está presente, es independientemente N, O o S, cada Rc, Rd, Re y Rf puede estar opcionalmente sustituido por alquilo de C1-8, heteroalquilo de C1-8, aralquilo y un anillo de 4 a 8 miembros que puede ser cicloalquilo, heterociclo, heteroarilo o arilo, y donde cada heteroátomo, si está presentes, es independientemente N, O o S, Rc y Rd están opcionalmente ligados para formar un heterociclo de 4 a 8 miembros que está opcionalmente fusionado con otro heterociclo o anillo heteroarilo de 3 a 5 miembros, y Re y Rf están opcionalmente ligados para formar un heterociclo de 4 a 8 miembros que está opcionalmente fusionado con otro heterociclo o anillo heteroarilo de 3 a 5 miembros; Y e Y' son, cada uno, independientemente, carbono o nitrogeno; y Z y Z' se seleccionan independientemente del grupo formado por hidrogeno, alquilo de C1-8, heteroalquilo de C1-8, cicloalquilo, heterociclo, arilo, heteroarilo, aralquilo, 1-3 aminoácidos, -[U-(CR42)t-NR5-C(R42)t]u-U-(CR42)t-NR7-(CR42)t-R8, -U-(CR42)t-R8, y -[U-(CR42)t-NR5-(CR42)t]u-U-(CR42)t-O-(CR42)t-R8, donde U se selecciona del grupo formado por -C(O)-, -C(S)-, y -S(O)2-, cada R4, R5 y R7 se selecciona independientemente del grupo formado por hidrogeno, alquilo de C1-8, heteroalquilo de C1-8, cicloalquilo, hererociclo, arilo, heteroarilo, aralquilo, R8 se selecciona del grupo formado por hidrogeno, alquilo de C1-8, heteroalquilo de C1-8, cicloalquilo, heterociclo, arilo, heteroarilo y aralquilo, -C(O)-R81, -C(S)-R81, -C(O)-O-R81, -C(O)-N-, R812, -S(O)2-R81, -S(O) 2-N-R812, donde cada R81 se elige independientemente del grupo formado por hidrogeno, alquilo de C1-8, heteroalquilo de C1-8, cicloalquilo, heterociclo, arilo, heteroarilo y aralquilo, opcionalmente, R7 y R8 juntos forman un anillo de 4-7 miembros, cada t es independientemente 0, 1, 2, 3, o 4, y u es 0, 1 o 2.
ARP090104676A 2008-12-03 2009-12-03 Inhibidores ns5a de vhc AR080263A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US11972308P 2008-12-03 2008-12-03
US17359009P 2009-04-28 2009-04-28
US21488109P 2009-04-28 2009-04-28
US18295209P 2009-06-01 2009-06-01
US18295809P 2009-06-01 2009-06-01
PCT/US2009/066459 WO2010065674A1 (en) 2008-12-03 2009-12-02 Inhibitors of hcv ns5a

Publications (1)

Publication Number Publication Date
AR080263A1 true AR080263A1 (es) 2012-03-28

Family

ID=42233599

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090104676A AR080263A1 (es) 2008-12-03 2009-12-03 Inhibidores ns5a de vhc

Country Status (27)

Country Link
US (2) US8921369B2 (es)
EP (2) EP2373172B1 (es)
JP (1) JP5762971B2 (es)
KR (1) KR101784830B1 (es)
CN (2) CN102647909B (es)
AR (1) AR080263A1 (es)
AU (1) AU2009322393B2 (es)
BR (1) BRPI0922366B8 (es)
CA (1) CA2746004C (es)
CL (1) CL2011001333A1 (es)
CO (1) CO6390077A2 (es)
CY (1) CY1114509T1 (es)
DK (1) DK2373172T3 (es)
EA (1) EA024853B1 (es)
ES (1) ES2437156T3 (es)
HK (1) HK1203929A1 (es)
HR (1) HRP20130944T1 (es)
IL (2) IL213277A (es)
MX (1) MX2011005898A (es)
PE (2) PE20150939A1 (es)
PL (1) PL2373172T3 (es)
PT (1) PT2373172E (es)
SG (1) SG171889A1 (es)
SI (1) SI2373172T1 (es)
TW (2) TWI573796B (es)
WO (1) WO2010065674A1 (es)
ZA (1) ZA201104833B (es)

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