BR112015007742A2 - composto, composição farmacêutica, método para a profilaxia ou tratamento da infecção pelo hiv ou para a profilaxia, tratamento, ou retardo do início da aids em um indivíduo, e, uso de um composto - Google Patents

composto, composição farmacêutica, método para a profilaxia ou tratamento da infecção pelo hiv ou para a profilaxia, tratamento, ou retardo do início da aids em um indivíduo, e, uso de um composto

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Publication number
BR112015007742A2
BR112015007742A2 BR112015007742A BR112015007742A BR112015007742A2 BR 112015007742 A2 BR112015007742 A2 BR 112015007742A2 BR 112015007742 A BR112015007742 A BR 112015007742A BR 112015007742 A BR112015007742 A BR 112015007742A BR 112015007742 A2 BR112015007742 A2 BR 112015007742A2
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BR
Brazil
Prior art keywords
prophylaxis
treatment
compound
onset
delay
Prior art date
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BR112015007742A
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English (en)
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BR112015007742B8 (pt
BR112015007742B1 (pt
Inventor
Burgey Christopher
Sing Li Chun
Xu Jiayi
L Arrington Kenneth
Patel Mehul
Gilfillan Robert
Li Yaozong
Han Yongxin
Luo Yunfu
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Merck Sharp & Dohme
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Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of BR112015007742A2 publication Critical patent/BR112015007742A2/pt
Publication of BR112015007742B1 publication Critical patent/BR112015007742B1/pt
Publication of BR112015007742B8 publication Critical patent/BR112015007742B8/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56One oxygen atom and one sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

1 / 1 resumo “composto, composiã‡ãƒo farmacãšutica, mã‰todo para a profilaxia ou tratamento da infecã‡ãƒo pelo hiv ou para a profilaxia, tratamento, ou retardo do inãcio da aids em um indivãduo, e, uso de um composto” os compostos da fã³rmula i sã£o inibidores da transcriptase 1 2 e reversa do hiv, em que r , r , r , l, m e z sã£o aqui definidos. os compostos da fã³rmula i e seus sais farmaceuticamente aceitã¡veis sã£o ãºteis na inibiã§ã£o da transcriptase reversa do hiv, na profilaxia e tratamento da infecã§ã£o pelo hiv e na profilaxia, retardo do inã­cio ou progressã£o, e tratamento da aids. os compostos e seus sais podem ser utilizados como ingredientes em composiã§ãµes farmacãªuticas, opcionalmente em combinaã§ã£o com outros antivirais, imunomoduladores, antibiã³ticos ou vacinas.
BR112015007742A 2012-10-08 2013-10-07 composto, composição farmacêutica, e, uso do referido composto BR112015007742B8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2012001358 2012-10-08
PCT/US2013/063612 WO2014058747A1 (en) 2012-10-08 2013-10-07 5-phenoxy-3h-pyrimidin-4-one derivatives and their use as hiv reverse transcriptase inhibitors

Publications (3)

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BR112015007742A2 true BR112015007742A2 (pt) 2017-08-08
BR112015007742B1 BR112015007742B1 (pt) 2021-01-19
BR112015007742B8 BR112015007742B8 (pt) 2023-04-25

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EP (3) EP3656384B1 (pt)
JP (2) JP5877281B2 (pt)
KR (1) KR101696128B1 (pt)
CN (1) CN104822670B (pt)
AP (1) AP2015008355A0 (pt)
AR (1) AR092876A1 (pt)
AU (1) AU2013329552B8 (pt)
BR (1) BR112015007742B8 (pt)
CA (1) CA2887312C (pt)
CL (1) CL2015000880A1 (pt)
CO (1) CO7350655A2 (pt)
CR (1) CR20150183A (pt)
CY (2) CY1119655T1 (pt)
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DO (1) DOP2015000082A (pt)
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PT (3) PT2903977T (pt)
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WO2014058747A1 (en) 2014-04-17
AU2013329552B8 (en) 2017-01-12
ES2645638T3 (es) 2017-12-07
CN104822670A (zh) 2015-08-05
ES2770774T3 (es) 2020-07-03
PT3295942T (pt) 2020-02-18
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