HUE035308T2 - 5-szubsztituált kinazolin-származékok rákellenes szerként - Google Patents

5-szubsztituált kinazolin-származékok rákellenes szerként Download PDF

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Publication number
HUE035308T2
HUE035308T2 HUE11174056A HUE11174056A HUE035308T2 HU E035308 T2 HUE035308 T2 HU E035308T2 HU E11174056 A HUE11174056 A HU E11174056A HU E11174056 A HUE11174056 A HU E11174056A HU E035308 T2 HUE035308 T2 HU E035308T2
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Hungary
Prior art keywords
mmol
methyl
oxo
quinazolin
mixture
Prior art date
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HUE11174056A
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English (en)
Inventor
George W Muller
Hon-Wah Man
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Celgene Corp
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Publication of HUE035308T2 publication Critical patent/HUE035308T2/hu

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    • 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
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Claims (8)

  1. M/uhvutuaU UïiaA'h«on'$A'inu<i.'*.*k'k utkdlevtes a/mkeut Äfeadalmi igénypontok ifi):
    képletü vegyület vagy gyógyásntiiag elfogadható sója. szoh-átja vagy Ä#|gblt«i?jf á bor, Uki6. petefészek, prosztata, vastagbél, végbél, agy. fej és nyak, tötök, hasnyálmirigy, csont, máj vagy hólyag rakjanak kezelési, szinte« tartási vagy megelőzési eljárásában történő alkalmazásra. ahol: R* hidrogénatom; halogénatom; ~{O^)p0H; adott, esetben egy vagy több haiogénatomma! szubsztituált (1-6 szénafomosjalkil: vagy adott esetben egy vagy több halogenatommal szuhszütuáit {I;~6 szénatomosMkoxicvsoport; R5 hidrogénatom: -ί€1Ι?.)«ΟΗ; fenik -0-(1-6 szénatomos)alkil; vagy adott esetben egy vagy több ha jogén atommal szuhsztitaáíi t1 -6 széaatomos)aIkstesoport: Rf' hidrogénatom; vagy adott esetben egy vagy több halogenatommal szubsztituált ( I -6 szén* a 5 n mos ad ki I e Mipo : t és n orteke Ο, I, x.tg> a,
  2. 2. A vegyülct vagy gyógyászatilag elfogadható sója, szolvátja vagy s/.tsreofoomerje az. 1. ?geropmn termit alkalma, av<i, ahol 1Γ metil vagy metoxiesoport; vagy ahol R” F vagy Cl; vagy ahol R* -Cl;\ csoport. .1. A vcgyüfeí ax I . Igérrypom azcnnü alkalmazásra, mely;
    képlett, vagy gyogyásttliltg elltpéhMt soft, s-ætMffi vagy sMettolKdmens, 4. (Ill):
    képiéin vegyük* vagy gyôgy&amp;zatUug <1 fogadható sója, szokatja vagy sztereobomerje a bőr, tüdő, petefészek, prosztata, vastagból, végből agy, íej és nyak, torok, hasnyálmirigy, csont, máj vagy hólyag rákiának kezelési, szinten tartási vagy megelőzési eljárás#» történő alkok mazásra, ahol: IIe: hidrogénatom; adott esetben egy vagy több halogénatommal szubszütuálí (1-6 szénatomomat besöpört; -C{0}-(I-8 szénatornos}aikil, ahol az aikliesoport adott esetben egy vagy több haloglnaÄn mal s/.ubsztUuiUî: -(.'(ÖMCWeV» 3-10 szènatomos-cikloalkil); C\Oi.<i1 y..'ο Ml"R\ ahol II' es R* eg>mástól ihggztienal bKuvgenatotn; adott esetben egy vagy több halogénatemntal szuhszűiualt i I -6 sAmatomosaitkilesopon, agy adott esetben, eg> sagy több ladogénananmal a/nbs/muáit (] -6 szutmonnedalkoxtc^epon, vagy -C\í >M( IkVO-tJ -6 s/emOnmesHdUjesí>pen, R' hidrogënpom; -fCHjfoöH; fenik ”0~(l4széhpomos}alkiSt va0'tħ|. épf||p több halogénatotntnál szabsz! tluált (1*6 szénátomöi)alkilesöpört: R' hidrogénatom; vagy adón esetben egs vagy több ImlegérnHonnná! szubsziituált (1-6 szénát omos )a! ki I e söpört ; és n értéke 0, 1, vagy 2,
  3. 5, A vegyülei vagy gyógyászati lag e) fogadható sója, szolt átjn vagy sztereoizomerk a 4. igénypont szeműi a: kalauz,» a, ahol 11' tneUlosoport; vagy ahol Ra *C<OV(l>6 szénatomos)alkl!csoport; vagy ahol R’; -CíObCHrÖ-tJ ~6 szénatomoslaiktlesoport. ^ wyst vî a I »m > - et m k > n j/ v η»
    Mpiíífö, Mgy gpégYásgiidlag ellbgadlíaíé söfs, ^aalf itj&amp;ffgy f£íaíföitóm&amp;rjf, ?, A vegyüld a 6. igénypont smmti alkalmasrism* mely:
    képletü, ?agy gyégyásiaülsg dfegaáMtó aó|íi, sfoif&amp;tjf vagy s^iefsóföoísepf,
  4. 8. ÍÍV):
    képlciû vegyidet vagy gyógyászatdrsg d fogadható sója, szolvátja vagy szíereoizojtnetje a bőr. tüdő, petefészek, prosztata, vastagbél, végbél, agy, fej és nyak, torok, hasnyálmirigy, csont, máj vagy hölvag rákjának kezelési, szinten tartási vagy megelőzési eljárásában történő alkal-mazásra, altok R8 -tC) 1:),,-(6-10 tagú ariicsoportg C(UH( (i->Vló-lö taon ,ηίΟ vage 0(0)-((010,,-(6-10 tagú hetes, aisDcsepsu! ahol a/ ars', vagy heíetmari lesöpört adott cselben szubsztituált egy vagy több hatogénammroak -SCK· í l-ö :sgdpton5oa)alkiicsnporttál, :m:ely adott esetben maga Is szssbsztitssák egy yagy töbl laloggn-álammak vagy (l-ő azibátrtmos)aikoxscsopos'ttat mely adott esetben maga is sziÉsszötuált egy vagy több ImlogpätomMaii -(.((())-(6:11.3.),,-NBR* csoport, ahol Rh; ö-löszioatomos atíleartpMk: trsely adbRefdlM szisbsBíináh egy vágy több hatögénatornniák: (1-6 szénatoraosjalkifcsoporUal, sneiy adott esetben maga is sznbsztin.iált egy vagy több haio-genatonmsal; vagy mely adott esetbpn tnagaass szubsztituáli egy vagy több halogénatommak vagy -0(0)-(6¾);rÖ-(CK:)n~(6-1(i tagit arií)esroport; R'* hidrogénatom; -(CIRROH; fenil; -0-(1-6 szénatomosjalkil; vagy adott esetben egy vágy-több halogénatommal szubszünsálí {1-6 szénntöínos)alkilcsopört:; Rlv hidrogénatom; vagy adott esetben egy vagy több balogénatommal smdtsztrtdiií (mb wm>· atomos talks lesöpört; és n értéke 0, 1, vagy 2.
  5. 9. A vegyidet a 8, igénypont szersrtíi alkahoa.zásra, ahoi R'? «iahMesopost;. vagy ahol Es ^|Ö^Cl:^lÄL y%$y «CEÖ-l-MH^feöicÄpöiti ahol a ΙοοΙΙοοοροό ahoh esofkm egg \?agv tíSbfe oMip *£% csoporttal vagy halogénatommal sfehsÄoälb
  6. 10, A vcgyiiet: a S, igénypont szerinti alkaJmazâéoô $»!fi
    Ifpietu, vagy szóivá!; a vagy sztereoizometjc.
  7. 11. A vegyület ax 1-10- igénypontok bármelyike szerinti s lkai maxisra, ahol a bőrrák melanoma. 1.1 A végsőiét az MÖ, igénypontok bármelyike szerinti alkalmazásra, ahol a rák rectal is adenokarcinóma, nem-kímets/heto eolorectalis kard oá-na. áHetdes máj sejt kardnóma. perkoneaíi's karcinoma, papillaris savős karcinoma, nem-kimetszhetó mápejt: kardnóma, papillaris pajzsrairigy karcMnta, iblheniaris paizsmirigy kMol#nm«p-M^ilt8aiS'p|^íl:« rigy kardnóma.
  8. 13, Λ veg>Üld a I Is igénypont szerinti aikalmazfeáí ahol a melanomaáltieles indanáTnás .14. Â vegyüld az 1-10, igénypontok bármelyike szerimi alkalmazásra, ahol a rák Kaposi-szárkőma, nbiyogylszaii szarkóina, ligyszös'eti sxarknma, Mmdázdt nagy Aztko|n M|pzl-veti szarkóma vágy leiomyosarcoma.
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