EA200970656A1 - Вич-ингибирующие 5,6-замещенные пиримидины - Google Patents

Вич-ингибирующие 5,6-замещенные пиримидины

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Publication number
EA200970656A1
EA200970656A1 EA200970656A EA200970656A EA200970656A1 EA 200970656 A1 EA200970656 A1 EA 200970656A1 EA 200970656 A EA200970656 A EA 200970656A EA 200970656 A EA200970656 A EA 200970656A EA 200970656 A1 EA200970656 A1 EA 200970656A1
Authority
EA
Eurasian Patent Office
Prior art keywords
6alkyl
cyano
amino
6alkynyl
het
Prior art date
Application number
EA200970656A
Other languages
English (en)
Other versions
EA020749B1 (ru
Inventor
Жером Эмиль Жорж Гийемон
Селин Изабелль Мордан
Бенуа Антуан Шмитт
Original Assignee
Тиботек Фармасьютикалз Лтд.
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 Тиботек Фармасьютикалз Лтд. filed Critical Тиботек Фармасьютикалз Лтд.
Publication of EA200970656A1 publication Critical patent/EA200970656A1/ru
Publication of EA020749B1 publication Critical patent/EA020749B1/ru

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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

Rозначает атом водорода; арил; формил; Cалкилкарбонил; Cалкил; Cалкилоксикарбонил; R, R, Rи Rозначают атом водорода; гидрокси; атом галогена; Сциклоалкил; Cалкилокси; карбоксил; Cалкилоксикарбонил; циано; нитро; амино; моно- или ди(Cалкил)амино; полигалогенСалкил; полигалогенСалкилокси; -C(=O)R; Cалкил, необязательно замещенный атомом галогена, цианогруппой или -C(=O)R; необязательно замещенный Cалкил, Салкенил или Салкинил; Rи Rозначают гидрокси; атом галогена; Сциклоалкил; Cалкилокси; карбоксил; Cалкилоксикарбонил; формил; циано; нитро; амино; моно- или ди(Cалкил)амино; полигалогенСалкил; полигалогенСалкилокси; -C(=O)R; циано; -S(=O)R; -NH-S(=O)R; -NHC(=O)H; -C(=O)NHNH; -NHC(=O)R; Het; -Y-Het; необязательно замещенный Cалкил, Cалкенил или Cалкинил; Rозначает С-алкенил или Салкинил, оба замещенные цианогруппой, аминокарбонильной, моно- или ди(Cалкил)аминокарбонильной, арильной, пиридильной, тиенильной, фуранильной или одной или двумя Cалкилоксигруппами; Het; -С(=O)NRR; -СН(OR)R; X означает -NR-, -О-, -CH- или -S-; фармацевтические композиции, содержащие указанные соединения в качестве активного ингредиента, и способы получения указанных соединений и композиций.
EA200970656A 2006-12-29 2007-12-28 Вич-ингибирующие 5,6-замещенные пиримидины EA020749B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06127328 2006-12-29
PCT/EP2007/064606 WO2008080965A2 (en) 2006-12-29 2007-12-28 Hiv inhibiting 5,6-substituted pyrimidines

Publications (2)

Publication Number Publication Date
EA200970656A1 true EA200970656A1 (ru) 2009-12-30
EA020749B1 EA020749B1 (ru) 2015-01-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA200970656A EA020749B1 (ru) 2006-12-29 2007-12-28 Вич-ингибирующие 5,6-замещенные пиримидины

Country Status (12)

Country Link
US (1) US8318736B2 (ru)
EP (2) EP2114902B1 (ru)
JP (1) JP5283633B2 (ru)
KR (1) KR20090094084A (ru)
CN (2) CN106045965A (ru)
AU (1) AU2007341228B2 (ru)
BR (1) BRPI0722079B8 (ru)
CA (2) CA2674185C (ru)
EA (1) EA020749B1 (ru)
ES (2) ES2618057T3 (ru)
MX (1) MX2009007006A (ru)
WO (1) WO2008080965A2 (ru)

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BRPI0722079A2 (pt) 2014-04-08
EA020749B1 (ru) 2015-01-30
US8318736B2 (en) 2012-11-27
BRPI0722079B8 (pt) 2021-05-25
ES2618057T3 (es) 2017-06-20
WO2008080965A2 (en) 2008-07-10
CA2923637C (en) 2018-10-02
CA2923637A1 (en) 2008-07-10
EP2781510B1 (en) 2016-12-14
JP5283633B2 (ja) 2013-09-04
MX2009007006A (es) 2009-07-09
CN101573342A (zh) 2009-11-04
BRPI0722079B1 (pt) 2020-01-14
US20100261722A1 (en) 2010-10-14
AU2007341228A1 (en) 2008-07-10
AU2007341228B2 (en) 2013-04-18
CN106045965A (zh) 2016-10-26
CA2674185C (en) 2017-02-28
EP2781510A1 (en) 2014-09-24
ES2523863T3 (es) 2014-12-02
WO2008080965A3 (en) 2008-09-04
CA2674185A1 (en) 2008-07-10
JP2010514736A (ja) 2010-05-06
EP2114902A2 (en) 2009-11-11
EP2114902B1 (en) 2014-09-17
KR20090094084A (ko) 2009-09-03

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