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AR110298A1 - Compuestos de heterociclo tetracíclicos útiles como inhibidores de la integrasa del vih - Google Patents

Compuestos de heterociclo tetracíclicos útiles como inhibidores de la integrasa del vih

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Publication number
AR110298A1
AR110298A1 ARP170103360A ARP170103360A AR110298A1 AR 110298 A1 AR110298 A1 AR 110298A1 AR P170103360 A ARP170103360 A AR P170103360A AR P170103360 A ARP170103360 A AR P170103360A AR 110298 A1 AR110298 A1 AR 110298A1
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AR
Argentina
Prior art keywords
alkyl
independently selected
group
ring
tetracyclic
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Application number
ARP170103360A
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English (en)
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Merck Sharp & Dohme
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=60703169&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR110298(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of AR110298A1 publication Critical patent/AR110298A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/407Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/22Heterocyclic 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 systems contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16Peri-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C12N15/1131Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against viruses
    • C12N15/1132Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against viruses against retroviridae, e.g. HIV

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biophysics (AREA)
  • Physics & Mathematics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente solicitud se refiere a compuestos de heterociclo tetracíclicos y a sales o profármaco farmacéuticamente aceptables de los mismos, a composiciones que comprenden al menos un compuesto de heterociclo tetracíclico y a procedimientos de uso de los compuestos de heterociclo tetracíclicos para tratar o prevenir la infección por VIH en un sujeto. Reivindicación 1: Un compuesto que tiene la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que: - - - - - representa un doble enlace opcional; el anillo A, incluyendo el átomo de carbono y el átomo de nitrógeno con los que se condensa el anillo A, es un grupo heterocicloalquilo monocíclico o bicíclico de 5 a 8 miembros, que se puede sustituir opcional e independientemente en un átomo de carbono de anillo A con un grupo seleccionado de alquilo C₁₋₆, -O-(alquilo C₁₋₆) y cicloalquilo C₃₋₇, y que se puede sustituir opcional e independientemente en un átomo de nitrógeno de anillo con un grupo seleccionado de alquilo C₁₋₆, -C(O)-(alquilo C₁₋₆) y -S(O)₂-(alquilo C₁₋₆); X se selecciona de heteroarilo monocíclico de 5 ó 6 miembros y -N(R⁴)C(O)-; R¹ es un grupo fenilo que se sustituye opcionalmente con desde 1 a 3 grupos, cada uno seleccionado independientemente de alquilo C₁₋₆, halo, -O-(alquilo C₁₋₆), haloalquilo C₁₋₆, -O-(haloalquilo C₁₋₆), -CN, -NO₂, -N(R⁴)₂, -C(O)OR⁶, -C(O)N(R⁴)₂ y -NHC(O)R⁶; R² se selecciona de H, alquilo C₁₋₆, cicloalquilo C₃₋₇, halo, haloalquilo C₁₋₆, -OR⁵, -N(R⁴)₂, -C(O)R⁵, -C(O)N(R⁴)₂ y -NHC(O)R⁵, en el que dicho grupo alquilo C₁₋₆ se sustituye opcionalmente con uno o más grupos, cada uno seleccionado independientemente de halo, -OH, -o(alquilo C₁₋₆) y -N(R⁴)₂; R³ se selecciona de H, alquilo C₁₋₆ y -O-(alquilo C₁₋₆), -N(R⁴)₂; cada aparición de R⁴ se selecciona independientemente de H y alquilo C₁₋₆; cada aparición de R⁵ se selecciona independientemente de H, alquilo C₁₋₆ y cicloalquilo C₃₋₇; cada aparición de R⁶ se selecciona independientemente de H y alquilo C₁₋₆; y R⁷ se selecciona de H y alquilo C₁₋₆.
ARP170103360A 2016-12-02 2017-11-30 Compuestos de heterociclo tetracíclicos útiles como inhibidores de la integrasa del vih AR110298A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662429470P 2016-12-02 2016-12-02

Publications (1)

Publication Number Publication Date
AR110298A1 true AR110298A1 (es) 2019-03-13

Family

ID=60703169

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170103360A AR110298A1 (es) 2016-12-02 2017-11-30 Compuestos de heterociclo tetracíclicos útiles como inhibidores de la integrasa del vih

Country Status (26)

Country Link
US (2) US10479801B2 (es)
EP (1) EP3548493B1 (es)
JP (1) JP6778325B2 (es)
KR (1) KR102345924B1 (es)
CN (1) CN110214142B (es)
AR (1) AR110298A1 (es)
AU (1) AU2017367610B2 (es)
BR (1) BR112019010924B1 (es)
CA (1) CA3045311C (es)
CL (1) CL2019001495A1 (es)
CO (1) CO2019005534A2 (es)
CR (1) CR20190257A (es)
DO (1) DOP2019000140A (es)
EA (1) EA039853B1 (es)
EC (1) ECSP19041050A (es)
ES (1) ES2837806T3 (es)
GE (2) GEP20227353B (es)
IL (1) IL266908A (es)
JO (1) JOP20190130A1 (es)
MX (1) MX389104B (es)
PE (1) PE20190968A1 (es)
PH (1) PH12019501198A1 (es)
TN (1) TN2019000170A1 (es)
TW (1) TWI756312B (es)
UA (1) UA125472C2 (es)
WO (1) WO2018102485A1 (es)

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