HUE026827T2 - 5-szubsztituált kinazolinon-származékok, mint rákellenes szerek - Google Patents

5-szubsztituált kinazolinon-származékok, mint rákellenes szerek Download PDF

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Publication number
HUE026827T2
HUE026827T2 HUE11174055A HUE11174055A HUE026827T2 HU E026827 T2 HUE026827 T2 HU E026827T2 HU E11174055 A HUE11174055 A HU E11174055A HU E11174055 A HUE11174055 A HU E11174055A HU E026827 T2 HUE026827 T2 HU E026827T2
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Hungary
Prior art keywords
esetben esetben
methyl
mmol
alkyl
oxo
Prior art date
Application number
HUE11174055A
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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 HUE026827T2 publication Critical patent/HUE026827T2/hu

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Claims (9)

  1. Srsxutetítoáií Mnazö8Bon-^rm82#iöU, mint rákellenes szerek Szabadalmi igénypontok UM
    këpletû vegytléí vagy valamely gyógyaszarilaf elJogadbató sója, sxoívaíja vagy sztereölxomerie, vér vagy csontvelő-ráis|a kezelési kontrollálási vagy mvgoiêzësi o|j:i|rás||>ar! Zêütézê' alkalmazásra* ;$»k lts : bidrogénatom; balogéeatom; Κ(ΓΚ^ΟΗ;!:: aáotíséei ©gy vagy *bbb lÂgèoaioranral szubsztteáb (M széaatomos^alkíi' adott esetheti egy vagy több balögétmtömma! szubsÂaill (1-6 sxéoatomospalkoîô; vagy riCH^NBR^esapori, É®í Rs: hidrogénatom; adott esetben egy vagy több halogénatomroal szuhsztímált {1-6 szinatomosy-aikilesoport; '(CH2}fi-(6 - 10 tagú aril) csoport; -C(OHCH2)sr(6O0 tagú art!) vagy -C(()HClH?..v(6-10 tagú heteroarií} csoport, ahol az aril vagy öeísroariksoport adott esetben egy vagy több kaloglnatoraraal; -Süfb; adott esetben egy vagy több baiogépatopítotal <;zubpztituátt.t I-:b,széoaunnos}--alkíl; vagy adott esetben egy vagy több halogénalpmppl sxbhsztttóáli (M szénatömoíO-aikoxicsopoitíat sxobsxtltmlt; dŰ|ÖHl-8 széoatötoósjralkbcsopett, ahol az alkilesopoTt adott esetben egy vagy "több halo-« géKátómnral szábsztlteált; .szénaiomox cikloalkil) csoport; csoport*: ahol R° és Rc jelentése egymástól függeílenül; hidrogénatom; adott esetben egy vagy több haiogénatornmal szabszíiteált (1 -b szenafotoost-alkypsopori; adoiosetben egy vagy több haiogéttatommal szubsziituáli ( 1 -6 széiatomos Ntikoxsesoporí; vagy adott esetben egy v agy több baiogénatontmab adott esetben egy vágy több halogénaioíMal vagy adott esetben egy vagy több halogén- ttommal saibsebíttalt IHi^natniî0s|-Âoxie^poittal Mítoszt? teáit 6 » Mi tage tólesepotig -C(0)*t ΓΚ>}»··0··(1 -6 szém^mùs)~âïkll^c>^M;^f •dXÔHCFIï »«-(HC!b)!Sd6 - 10 tagié aril) csoport: Rb hidrogénatom; -íCH-AÖif; fe?bf; -0-(1-6 szénatom, »s^gcso^; vagy adott esetben @gy vagy több initogénatornmai szbbszlööáh ( tol szenatomosValkilesoport; hidtöglnaíom; vágy adott esettet egy vagy több balogén atommai szubsztMoáittl-b szsn-aíomos)-áÍÜiesoport; és n értéke: Cl1, vagy 2. ± (11);
    szerkezeti vegyiikt vagy valamely gybgyászaítiag elfogadható sója, szolvátla vagy sztereoizomer|e m 1, tgebypont szentéi alkalnmásta ^ot:; if: hidrogénatom; bálögénatom; -(ClBa|rOll;aiott esetben egy vagy több baiogénatomma! szuhsziituáh ( 1 -6 szénatotnosVaiki lesöpört; vagy adott esetben egy vagy több haiogénaíom-mai sz.ubsztituált ( i -6 szénatomosVaikoxicsopött;· R5; hidrogénatom; -(CH^ON: fenik -0-(1-6 szenatotr5os)-alkilcsoport: vagy adott esetben egy vagy több halogénatommal szubszíituáli (i-d SKenatoiaosl-alkllesopat; B?:< bldrögénafem; vagy adott esetben egy vagy több halogénatömma! sznbsstotnâlt (1-b tzin-atomos)~alkílcsopoft; és n értéke Oy 1, vagy 2.
  2. 3. Vegyület a 2:. igénypont mmmú alkalmazásra,. vagy valamely gvógyászatilag el fogadható sáp, szolyátia vagy sztereopomepe, ahol R” metil vagy metosttosopert; vagy aboi if F vagy Cl; vagy aho): It* ~CF3,
  3. 4, Vegyikt a 2. igénypoaí sz&amp;ánii alkalmam^, mely:
    képleíii vagy valamely gyógyászati lag elfogadható sója. sxoívátja vagy szkreoizonierje. 5:. (III):
    $zeÉ«tik?együieí vagy valamely gvógyászatilag elfogadható söfa, szolvátjá vagy sktereokoínetje az 1. igénypont szerinti alkalmazásra, ahol: Rá: Mdmgénatom:; adott esetben egy vagy több haiogesiatommal szubsztituáit: (1-6 szénatonios)^allifeopöít; -0(0)-(1 -8 sz0naiomos}~alkiiesopork ahol az aikilesöpört adott esetben egy vagy több hak> génatonirnai szubszíiíaáll; -C(O)'(C2I;?)fS -(5? -10 szênatoraos-eîkloajMî;} csoport: «^OMCHï^NR^.^roîK^ Rf egymástól 6 jggetlenük BÍdrogéoaíom; adott esetben e|y vagy iöbb halogénaíommid szobs/rúnáit (06· saénatomosl-alki lesöpört; vagy adott esetben egy vagy több haiogènaîoîpmal sznbszhínáit p>6: szénatom os)~afevlesóport; vagy -C(0 Η (Ί i :h-0~i 1-6 szénatomos nolkilcsoport; R : hidrogénatom: RCHs^ÓÍI; feniI; »©^t-btszÉiatoTnosl-alkí!; vagy adott esetben egy vagy több Mlogénaiomma! szubsztítuált (1-6 szénatOmos|~aÍltilesoport; Es: hidrogénatom; vagy adott esetben egy vagy több balogéhatommaf szubsztinilí (1-6 szírt-axomosHlMkaopott; és n értéke t, |, vagy 2. 6. 'Vegyidet 5- igénypont szerinti alkalmazásra,: vág}· valamely gvógyászatilag elfogadható sója, szóivá!!®, vagy sztéreofeomerje, ahoi R' metllcsoporti'fag^' ahol Rd ~Cí 0)-( 1. -6 szénatomosj-alkiicsoport: vagy ábolld -0(0)-6112-0-(1-6 szenatomosj-alkilcsoport. 7\ Vegyük! az 5. igénypom szeri tili alkalmazásra, vagy valamely gyógyásxatHag elfogadható sója, szolvátja. vagy szíereskomeije, mely
    képkín.
    1, ÍÍV):
    ^egyölei vagy mlmúf gyógytablag el fogadhat sója, súlyába vagy * %&amp;iypoo£:s^Äi afkattsazásra, ahol: &amp;&amp; ~(CH2),r (6-H) tagú aril} csoport: - <:;({:>)··(€!-!>},r(í> I0 tagú aril) vagy -€(C))'(CH2)r(6~10 tagú heteroaríi) csoport, ahol az anl vagy heíeroariIcsoport séíI esetben egy vagy több haiogénaiommal; -SCFj csoporttal ; ado tt esetben egy vagy több haiogénatomma! szitbszibált ( I -6 szénatomosj-aikilcsoporttal; vagy adott esethenegy vagy több balogénaíótnmal sEbbszttoált O-b szÉtatotooal-alkoxípppotttal szobszütuáU; -0(0)-((1 b VHHR* csoport, ahol Rh: b~lü: tagú ariksoport, Mely adott espbco egy vagy több halogénatotomal; adott esetbe*? egy vagy több haiogcnatonunal szuhsztltuák (Ob szeoatoínosyalkilesoporitat; vagy adott esetbe?? egy vagy több ha!ogénato?n?ua! szubsztituált (1-6 széaatpröoál-alkozlosOpórttal szubsztiipálí; vagy - csoport; Re: bidrogeÄöm;-(CblalsÖH; ímk~(-Hkb szenátortos)^alkll;v^y adottesefbeu egy vagy több haiogémnommal szubsztituált ( i-6 szénaiomos)-alkik$oport; R ;' : hldmgeuatom; vagy adott esetben egy vagy több baiogénatornrna! szdbaztítuib (I -6 sz.cnatomosi-alkilesopoT't; es « értéke ö, k vagy 2.
  4. 9. Vegyület a &amp; igénypont szerinti alkalmazásra, ahol R'? nietiksoport; vagy abol R'; -CfPi-tenil, -C ( <) )-C f k - feni I, vagy ~C(0)~N ri'tenOcso|X>trt; ahol a tenilcsoport adott esetben egy vagy több metiksoporttak -(¾ csoporttal, vagy balögénatomrnal sznbsztltuáli
  5. 10. Vegyülei a S. igénypont szmnii alkalmazásra, mely ;
    képiem, vagy valamely gyógyászatiig elfogadható sója, szolváija vagy saercob.onteije. I !... Vegyüld íz ! -10, igény pontok bármelyike szerinél alkalmazásra, átel a vêt vagy csontvelő rákja leukémia vagy lim Com a,
  6. 12, Vegyulet az Ϊ-IQ« igényportefe: bê^aeîyîke SiSemii alkalmazásra, aW â: vár vagy csonttá 16 rákja: my^foma #alíí|á«^4^3piSngö:'myok)TT*a,fag3f l^íiplerrs: utyeioma,
  7. 13, Vegyulet all. &amp;MÍMÍ' alkalraassiliKa, atel a firafoma: Hodgkin limiopa,
  8. 14, Vegyidet a IL igénypont szerinti alkalmazásra, átel a lirnídma noR-l’ïodgkrn ItMÉ&amp;maL t$. Vegyidet a 14. igénypont szerinti; alkalmazásra* atel a norvlfedgkin limloma ter T-séfi Imüma, ter B sp Imiittta, dilik: npyseites B sejt limloma, Waldenstrom maetögiobineima, kőpenysp limloma vagy íollikoiáris Imfóma. lé. Vegyöte á ll, rglnypopt szerinti alkalmazásra, ahol a IciÉéíakkrómtediíö'tóíás·íétfer kémia, krénikns myebcytás leukémia, akus íymphobiasuás leukémia, akut myékrgén leukémia vagy akut rnyeloblastiás leukemia,
  9. 17. Vegyüleí az 1. igénypont szerinti alkalmazásra, ahol a ter vagy csontvelő rákja egy myeiteisplastiás szíteréma és myeloprolileraiv temgség közéi kikerülő rák előtti állapot,
HUE11174055A 2006-09-26 2007-09-25 5-szubsztituált kinazolinon-származékok, mint rákellenes szerek HUE026827T2 (hu)

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