HUP0401729A2 - IV típusú foszfodiészteráz inhibitor hatású alkin-aril-naftiridin-4(1H)-on-származékok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

IV típusú foszfodiészteráz inhibitor hatású alkin-aril-naftiridin-4(1H)-on-származékok és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0401729A2
HUP0401729A2 HU0401729A HUP0401729A HUP0401729A2 HU P0401729 A2 HUP0401729 A2 HU P0401729A2 HU 0401729 A HU0401729 A HU 0401729A HU P0401729 A HUP0401729 A HU P0401729A HU P0401729 A2 HUP0401729 A2 HU P0401729A2
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alkyl
group
son
hydroxyl
optionally substituted
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HU0401729A
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Daniel Guay
Mario Girard
Pierre Hamel
Sebastien Laliberte
Richard Friesen
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Merck Frosst Canada & Co.
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Publication of HUP0401729A2 publication Critical patent/HUP0401729A2/hu
Publication of HUP0401729A3 publication Critical patent/HUP0401729A3/hu

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Abstract

A találmány szerinti (I) általános képletű vegyületek ésgyógyszerészetileg elfogadható sóik foszfodiészteráz-4 inhibitorok,így asztmaellenes és gyulladásgátló szerként használhatók. A képletbenR jelentése hidrogénatom, alkil- vagy cikloalkilcsoport; R1 jelentésehidrogénatom, alkil-, cikloalkil-, alkoxi-, alkenil-, alkinil-, -C(O)-alkil-, -C(O)-aril-, alkil-SOn-alku-, alkil-SOn-(aril)-, fenil-,heteroaril- vagy heterocikloalkil-csoport, ahol valamennyi csoportadott esetben szubsztituálva van 1-3 egymástól függetlenül választottalkil-, alkoxi-, hidroxil-, -N-alkil-alkil-, alkil-SOn-alkil-, nitro-,CN, =N-O-alkil-, -O-N=alkil-csoporttal vagy halogénatommal; R2jelentése hiányzik, hidrogénatom, halogénatom, alkil-, cikloalkil-,alkil-cikloalkil-cikloalkil-, alkoxi-, fenil-, heteroaril-,heterocikloalkil-, nitro-, CN, =N-O-alkil-, -O-N=alkil-, -N-alkil-alkil-, -NHSOn-alkil-, -NHC(O)-alkil-, -NHC(O)-aril-, -C(O)-alkil-, -C(O)-O-alkil-, alkil(=N-OH)-, -C(N-NOH)-alkil-, alkil(oxi)alkil-fenil-, -SOnNH-alkil- vagy alkil-SOn-alkil-csoport, ahol a fenil-heteroaril- vagy heterocikloalkil-csoport adott esetben szubsztituálvavan halogénatommal, alkil-, alkoxi-, hidroxil-, -N-alkil-alkil- vagy -C(O)-O-alkil-csoporttal, és valamennyi alkilcsoport adott esetbenszubsztituálva van egymástól függetlenül 1-6 halogénatommal vagyhidroxilcsoporttal; n értéke 0, 1 vagy 2; R3 hiányzik, vagy jelentésehidrogénatom, hidroxil-, -N-alkil-alkil-csoport, halogénatom vagyalkilcsoport, ahol valamennyi alkilcsoport adott esetbenszubsztituálva van egymástól függetlenül 1-6 halogénatommal,hidroxilcsoporttal vagy -N-alkil-alkil-csoporttal; R4, R5, R6 és R7jelentése egymástól függetlenül hidrogén-, halogénatom, alkil-,alkoxi-, -SOn-alkil-, nitro-, ciano- vagy -N-alkil-alkil-csoport, ésvalamennyi alkilcsoport adott esetben szubsztituálva van egymástólfüggetlenül 1-6 halogénatommal vagy hidroxilcsoporttal; és R8jelentése fenil-, piridil-, pirimidil-, indolil-, kinolinil-, tienil-,piridonil-, oxazolil-, oxadiazolil-, tiazolil-, tiadiazolil- vagyimidazolilcsoport; vagy ezek oxidjai, amikor R8 jelentéseheteroarilcsoport; vagy hidrogénatom, alkil- vagy cikloalkilcsoport,és valamennyi alkilcsoport adott esetben szubsztituálva van 1-6egymástól független halogénatommal, -N-alkil-alkil-, -N-cikloalkil-alkil-, -N-cikloalkil-cikloalkil-, N-heterociklo-alkil-, -SOn-alkil-,-SOn-(aril)- vagy hidroxilcsoporttal. A találmány kiterjed avegyületeket tartalmazó gyógyszerkészítményekre is. Ó
HU0401729A 2001-08-29 2002-08-27 Alkyne-aryl-naphthyridin-4(1h)-one derivaties as phosphodiesterase-4 inhibitors and pharmaceutical compositions containing them HUP0401729A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31609301P 2001-08-29 2001-08-29
PCT/CA2002/001324 WO2003018579A1 (en) 2001-08-29 2002-08-27 Alkyne-aryl phosphodiesterase-4 inhibitors

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HUP0401729A2 true HUP0401729A2 (hu) 2004-12-28
HUP0401729A3 HUP0401729A3 (en) 2012-09-28

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HU0401729A HUP0401729A3 (en) 2001-08-29 2002-08-27 Alkyne-aryl-naphthyridin-4(1h)-one derivaties as phosphodiesterase-4 inhibitors and pharmaceutical compositions containing them

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US (2) US6743802B2 (hu)
EP (2) EP2305677A1 (hu)
JP (1) JP4157035B2 (hu)
KR (1) KR100928849B1 (hu)
CN (1) CN100338061C (hu)
AR (1) AR036365A1 (hu)
AU (1) AU2002322940B2 (hu)
BR (1) BR0212042A (hu)
CA (1) CA2456817C (hu)
DO (1) DOP2002000456A (hu)
EA (1) EA006800B1 (hu)
EC (1) ECSP044992A (hu)
GE (1) GEP20063805B (hu)
HK (1) HK1080073B (hu)
HR (1) HRP20040151A2 (hu)
HU (1) HUP0401729A3 (hu)
IL (1) IL160213A0 (hu)
IS (1) IS7138A (hu)
JO (1) JO2311B1 (hu)
MX (1) MXPA04001889A (hu)
NO (1) NO330521B1 (hu)
NZ (1) NZ530931A (hu)
PE (1) PE20030416A1 (hu)
PL (1) PL367716A1 (hu)
RS (1) RS17004A (hu)
UA (1) UA75957C2 (hu)
WO (1) WO2003018579A1 (hu)
ZA (1) ZA200400952B (hu)

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