HUE025411T2 - Azetidinszármazékok - Google Patents

Azetidinszármazékok Download PDF

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Publication number
HUE025411T2
HUE025411T2 HUE09716712A HUE09716712A HUE025411T2 HU E025411 T2 HUE025411 T2 HU E025411T2 HU E09716712 A HUE09716712 A HU E09716712A HU E09716712 A HUE09716712 A HU E09716712A HU E025411 T2 HUE025411 T2 HU E025411T2
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Hungary
Prior art keywords
phenyl
yloxy
azetidine
pyridin
optionally substituted
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HUE09716712A
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English (en)
Inventor
Stephen Roughley
Steven Walls
Terrence Hart
Rachel Parsons
Paul Brough
Christopher Graham
Alba Macias
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Vernalis R&D Ltd
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Priority claimed from GBGB0804006.5A external-priority patent/GB0804006D0/en
Priority claimed from GBGB0821694.7A external-priority patent/GB0821694D0/en
Application filed by Vernalis R&D Ltd filed Critical Vernalis R&D Ltd
Publication of HUE025411T2 publication Critical patent/HUE025411T2/hu

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Claims (8)

  1. Szabadalmi igénypontok 1 „ Egy (!) képletű vegyűiet, vagy egy gyógyszerészetileg elfogadható sója:
    ω ahol a képletben Ar jelentése adott esetben szubsztituált feni- vagy adott esetben szubsztituált δ vagy S gyűrű atomot tartalmazó monodklusos heteroanlcsoport; Ar2 jelentése adott esetben szubsztituált fenil-, adott esetben szubsztituált 5 vagy δ gyűrű atomot tartalmazó monociklusos heteroahlesoport vagy adod esetben szubsztituált kondenzált, mindegyik kondenzált gyűrűben 5 vagy 6 gyűrű atomot tartalmazó foicíklusos heteroanlcsopori; és Ar3 jelentése az alábbiakból álló csoportból választott kétértékű csoport: adott esetben szubsztituált ferdén- és adott esetben szubsztituált δ vagy δ gyűrű atomot tartalmazó monodklusos heteroarlléncsoportok; és ahol az Ar1, Ar2 és Ar3 csoportokban adott esetben található bármely szubsztituens jelentése egymástól függetlenül klór, fluor, bróm, dkiopropil, metil, mono-, dí- vagy tri-metll, trifluor-metll, difluor-metil, monofluor-metil, metoxi, etoxi. propoxi, buíoxi, pentoxí, 2-metoxl~eioxi: 2-benzil-oxi-etoxi, 2-hldoxl-etoxl, mono-, dl- vagy trl-fluor-metoxl, ciano, bidoxil; -CO2R1 és -SO2R1 ahol Rí jelentése hidrogén, metil vagy etil; tetrazoüi; -NR2R3, -CH2MR2R3 és -0^O):NR2R3 ahol R2 és R3 jelentése egymástól függetlenül hidrogén, metil vagy etil.
  2. 2. Az 1. igénypont szerinti vegyűiet ahol Ar1 jelentése adott esetben szubsztituált fenilcsoport. 3» Az 1. vagy 2. igénypont szerinti vegyűiet, ahol Ar2 jelentése fenil, piridil, pirimidinil, piraziní! vagy plrídazlnilcsoport, amelyek közül bármelyik csoport adott esetben szubsztituált
  3. 4. Az 1 vagy 2. igénypont szerinti vegyűiet, ahol Ar2 jelentése 3-piridI, pirimkJ!n-4~H, pirazin-2-8 vagy piridazin-3-i, amelyek közül bármelyik csoport adott esetben szubsztituált,
  4. 5, Az előző Igénypontok bármelyike szennti vegyület ahol Ár3 jelentése adott esetben szubsztííuált kétértékű lenién- vagy piridiléncsopori
  5. 6. Az 5. Igénypont szerinti vegyület, ahol Ár3 jelentése adott esetben; szubsztííuált kétértékű 1 ,4-fenlíén- vagy az
    alábbi képlete 2,5-pindiIéncsoporí: aho! az egy csillaggal letölt kötés Ar csoporthoz kapcsolódik és a két csillaggal jeléit csoport oxigénhez kapcsolódik. ?> Az 1. igénypont szerinti vegyülel ahol: Ar2 jelentése 3-piridi, pirimtötn-édl, pirazln-2-lí vagy pridazin~3»il: Ar jelentése adott esetben szubsztííuált kétértékű 1,4-fenílén- vagy az alábbi képié-tű 2,5-pirldinlíéncsopön
    ahol az egy csillaggal jelölt kötés Ar1 csoporthoz kapcsolódik és a két csillaggal jelölt Ar1 jelentése adott esetben szybsztltuált fenllcsopork 8. A 7. Igénypont szerint vegyülel, ahol Ar1 jelentése feni, 2-fluor~fenil, 3-(2--metoxi-etoxi)~fenlL vagy 2~meioxi-5~(2-rneioxi~etoxi)-fenii., 8* A 7. vagy 8. igénypont szerinti vegyület, ahol Ar2 jelentése piriéazín~3-ií.
  6. 10. Az 1. igénypont szerinti alábbi vegyület: í3~(8ifenli-4-ii-Dxi)-azetidin~1-karbonsavHplridin-3-ll“amidjt [3-{5~FenIS-píndín-2~il-oxi}-azetidin~1~karbonsavHpirídazín~3-ií-8míd], {3-[5-(2-fv1etoxí~fenII}-piridin-2-iI~oxij-azetidín~1-karbonsav}-[pirídazin-3-il-amin}, {3-j5~(2-Fiüor"fens])-'piridin''2-il-'OXÍj-azetidin-'1-karbonsav}-íp!ndazin-3-il~arnidj) {S-IS-^-jS-yetoxl-etoxiHenilj-piridín^-iboxIVazetidin-l-karbonsavj-jpIndin-S-Ii-amidj, {S-jS-jS-CS-yetoxi-etoxiHenílj-pindín^-ii-oxij-azetídln-l-karbonsavHpiridazín-S-ll--amid], (3-{S-13-{2-Benzíi-oxi-etoxi)-feniIj-piridín-2-Ii~oxi}-a2et)din-1-karbonsav}-rplridazin-3-iI~ -amid], f3~ͧ-|2~:FIuor-fenilj-píndIn-2-il-oxi]-azetÍdÍn~1-ka:rbonsav}~[pirazín~2-il'arn3d| t3-[5-{2,6-Dif!üor-fenil}-píridin~2-i!-oxn~azetidirs~1-karbonsav}-ípirídazin-3-il-amíd]:< {345~|2-Kiôr“5~{2~metQxî'-eioxâ)4enil|~pMdin~2~îl-ox|~azetid:i:n-1-karbonsavHPW^az^n”3~ -íj-amid], 11« Gyógyszerkészítmény, amely az előzd igénypontok bármelyike szerinti vegyöletet egy vagy több gyógyszerészetíieg elfogadható vivőanyaggal és/vagy kötőanyaggal együtt tartalmazza,
  7. 12. Az 1-íÖ. Igénypontok bármelyike szedeti vegyuiet a gyógyításban: történő alkalmazásra, 13« Az 1-10. igénypontok bármelyike szerinti vegyuiet a FAAH aktivitás gátlására Javuló betegségek vagy orvosi állapotok kezelésére, amelyeket az alábbiak közűi választunk: akut vagy krónikus fájdalom, szédülés, hányás, hányinger, evési rendellenességek, neurológiai és pszichiátriai kórok, akut vagy krónikus neurodegenerativ betegségek, epilepszia, alvási rendellenességek, kardiovaszkuláris betegségek, vese ischémie, rákos betegségek, immunrendszer! rendellenességek, allergiás betegségek, parazita, vírusos vagy bakteriális fertőző betegségek, gyulladásos betegségek, csontritkulás. szemészeti panaszok, tüdő panaszok, gasztrointesztináfis betegségek, giau-kómával összefüggő magas vérnyomás és vizeiét inkontínencia.
  8. 14. Az 1-10. igénypontok bármelyike szerinti vegyületek szorongás, depresz-szió, fájdalom, gyulladás, bőrviszketés, alvási rendellenesség vagy mozgási rendellenesség kezelésére.
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