BRPI0517272A - derivados de pirimidina bicìclicos de inibição de hiv - Google Patents

derivados de pirimidina bicìclicos de inibição de hiv

Info

Publication number
BRPI0517272A
BRPI0517272A BRPI0517272-1A BRPI0517272A BRPI0517272A BR PI0517272 A BRPI0517272 A BR PI0517272A BR PI0517272 A BRPI0517272 A BR PI0517272A BR PI0517272 A BRPI0517272 A BR PI0517272A
Authority
BR
Brazil
Prior art keywords
substituted
alkyl
amino
optionally substituted
halo
Prior art date
Application number
BRPI0517272-1A
Other languages
English (en)
Inventor
Paul Adriaan Jan Janssen
Jerome Emile Georges Guillemont
Mika L Paugam
Bruno Francois Marie Delest
Jan Heeres
Paulus Joannes Lewi
Original Assignee
Tibotec Pharm Ltd
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 Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of BRPI0517272A publication Critical patent/BRPI0517272A/pt

Links

Classifications

    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

Abstract

DERIVADOS DE PIRIMIDINA BICìCLICOS DE INIBIçãO DE HIV. Os inibidores de replicação de HIV de fórmula (I) N-óxidos, sais de adição farmaceuticamente aceitáveis, aminas quartenárias ou formas estereolsoméricas destes, em que -a˜=a-a =a¬ 4¬- é -GH=CH-CH=GH-, -N=CH-CHGH-, -N=CH-N=CH-, -NCH- CHN-, -N=N-CH=CH-; -b˜=b-b=b¬ 4¬- e -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=GH-N=CH-, -N=CH-CH=N-, -N=N- GHCH-; n e m é 0,1, 2, 3 e em certos casos também 4; R¬1¬ é hidrogênio;arila; formila; C~ 1-6~alquilcarbonila; C~ 1-6~alquila opcionalmente substituida; C~ 1-6~alquilóxicarbonila; R é OH; halo; C~ 1-6~alquila opcionalmente substituida, C~ 2-6~alquenila ou C~ 2-6~alquinila; carbonila substituida; carboxila; CN; nitro; amino; amino substituído; polialometila; polialometiltio;-S(=O)~ p~R¬ 6¬ ; C(=NH)R¬ 6¬; R¬ 2a¬ é CN; amino; amino substituído; C~ 16~alquila opcionalmente substituida; halo; C~ 1-6~alquiIóxi opcionalmente substituído; carbonila substituida; -CH=N-NH-C(=O)-R¬ 16¬; C~ 1-6~alquilóxiC~ 1-6~aIquila opcionalmente substituida; C~ 2-6~alqueniía ou C~ 2-6~alquiniía substituida; -C(=N-O-R¬ 8¬)-C~ 1-4~alquila; R¬ 7¬ ou -X-R¬ 7¬; R¬ 3¬ é CN; amino; C~ 1-6~aIquila; halo; C~ 1-6~alquiíóxi opcionalmente substituído; carbonila substituida; -CH=N-NH-C(=O)-R¬ 16¬; C~ 1-6~alquiIa substituida; C~ 16~alquilóxiC~ 1-6~alquila opcionalmente substituida; C~ 2-6~alquenila ou C~ 2-6~alquinila substituida; -C(=N-O-R~ 8~)-C~ 1-4~alquila; R¬ 7¬; -X-R¬ 7¬; R¬ 4¬ é halo; OH; C~ 1-6~aIquiIa, C~ 2-6~alquenila ou C~ 2-6~alquinila opcionalmente substituida; C~ 3-7~acicloalquila; C~ 1-6~alquilóxi; CN; nitro; polialoC~ 1-6~alquila; poliaíoC~ 1-6~alquilóxi; carbonila substituida; formila; amino; mono- ou di(C~ 1-4~alquil)amino ou R¬ 7¬; -A-B- é -CR¬ 5¬=N-, -N=N-, -CH~ 2~-CH~ 2~-, -CS-NH-, -CO-N H-, -CH=CH-; composições farmacêuticas compreendem estes, métodos para a preparação destes compostos e composições; o emprego destes compostos para a prevenção ou o tratamento de infecção de HIV.
BRPI0517272-1A 2004-10-29 2005-10-27 derivados de pirimidina bicìclicos de inibição de hiv BRPI0517272A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04105419 2004-10-29
PCT/EP2005/055589 WO2006045828A1 (en) 2004-10-29 2005-10-27 Hiv inhibiting bicyclic pyrimidine derivatives

Publications (1)

Publication Number Publication Date
BRPI0517272A true BRPI0517272A (pt) 2008-10-07

Family

ID=34929789

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0517272-1A BRPI0517272A (pt) 2004-10-29 2005-10-27 derivados de pirimidina bicìclicos de inibição de hiv

Country Status (16)

Country Link
US (5) US8153640B2 (pt)
EP (1) EP1807430B1 (pt)
JP (1) JP5118972B2 (pt)
KR (1) KR20070085286A (pt)
CN (1) CN101048410B (pt)
AR (1) AR051410A1 (pt)
AU (1) AU2005298637B8 (pt)
BR (1) BRPI0517272A (pt)
CA (1) CA2577588C (pt)
ES (1) ES2508766T3 (pt)
IL (1) IL180963A (pt)
MX (1) MX2007005159A (pt)
RU (1) RU2403254C2 (pt)
TW (1) TW200630370A (pt)
WO (1) WO2006045828A1 (pt)
ZA (1) ZA200703444B (pt)

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CN101048410A (zh) 2007-10-03
ES2508766T3 (es) 2014-10-16
US20180009819A1 (en) 2018-01-11
US20180016281A1 (en) 2018-01-18
US10072015B2 (en) 2018-09-11
JP2008517978A (ja) 2008-05-29
RU2403254C2 (ru) 2010-11-10
WO2006045828A1 (en) 2006-05-04
US10077270B2 (en) 2018-09-18
AU2005298637B2 (en) 2012-06-28
IL180963A0 (en) 2007-07-04
US9487518B2 (en) 2016-11-08
IL180963A (en) 2015-06-30
CA2577588A1 (en) 2006-05-04
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AU2005298637A8 (en) 2012-12-06
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US8153640B2 (en) 2012-04-10
US20120190697A1 (en) 2012-07-26
EP1807430A1 (en) 2007-07-18
RU2007119784A (ru) 2008-12-10
TW200630370A (en) 2006-09-01
JP5118972B2 (ja) 2013-01-16
CN101048410B (zh) 2010-06-23
US20160355519A1 (en) 2016-12-08
ZA200703444B (en) 2008-11-26
US9802943B2 (en) 2017-10-31
EP1807430B1 (en) 2014-07-23
AU2005298637B8 (en) 2012-12-06
AR051410A1 (es) 2007-01-10
MX2007005159A (es) 2007-06-26
US20080085907A1 (en) 2008-04-10
KR20070085286A (ko) 2007-08-27

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