HUE034979T2 - Aminopirimidin-származékok a kináz-aktivitás modulátoraiként történõ alkalmazásra - Google Patents

Aminopirimidin-származékok a kináz-aktivitás modulátoraiként történõ alkalmazásra Download PDF

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HUE034979T2
HUE034979T2 HUE12766773A HUE12766773A HUE034979T2 HU E034979 T2 HUE034979 T2 HU E034979T2 HU E12766773 A HUE12766773 A HU E12766773A HU E12766773 A HUE12766773 A HU E12766773A HU E034979 T2 HUE034979 T2 HU E034979T2
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phenyl
amino
pyrimidin
obsd
ethyl
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HUE12766773A
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Ruoxi Lan
Bayard R Huck
Xiaoling Chen
Lizbeth Celeste Deselm
Yufang Xiao
Hui Qiu
Constantin Neagu
Igor Mochalkin
Theresa L Johnson
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Merck Patent Gmbh
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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 (3)

  1. Szabadalmi igénypontok 1:. (D képisítü vegyüleí
    vagy gyógyszerészetileg eltagaéhátő sója, .saoIváíjévVSgy &amp; só szoívátja,ahol: X jelentése N vagy CM; Y jelentése N vagy CtC; B jelentése egyenes vagy elágazó, I, X 3, 4, 5, ó vagy 7 C atomot; tartalmazd alMl kapeaölóéso-port, amely lehet szobsztltuálaiian vagy mono- vágy disAibszbitsáit Hal Öli CN vagy N1B csoporttal, amelyben egy CM? csoport fel lehet cserélve Gyei Cvel CÖNLB* CF? csoporttal, és amelyben egy, kettő vagy három C% csoport fél lehet cserélve -Ö- vagy 4MH* csoporttal és amelyben egy CM csoport tél leltet cserélve -N·· -atommal;. vagy ha Y jelentése €NH;>, E lehet ő ség .CH{R !)~NH'CÖ" vagy -CO~Ni l-Ci li IC) - csoport is; R! jelentése CN; CÖN%,· Hal*1.,4, 0(1.,0), Ar, Gye' vagy Gye"; R'' jelentése M, NIL, Hal vagy CIN; RJ jelentése: 1-1 vagy LA, Hal jelentése F, Cl Br vagy I; LA jelentése egyenes vagy elágazó, egyenes telített vagy részlegesen telítetlen szénhidrogén lánc, amely F 2, 3 4, 5 vagy ó € atomot tartalmaz» ahol L 2 vagy 3 H atom lel lehet cserélve fial vagy OH esöpörttai Ar jelenése mono-' vagy bieikiusos aromás homo- vagy hetsrodklcs, amely Ö, l, 2, .3 vagy 4 N, 0 és/vagy S atomot és 3,. 6, 7, 4, % vagy 10 vágatomat tartalmaz, és lehet szobsztíiaálaílao, vagy egymástól függetlenül mono- vagy dlsrabsztmuilí Hal, LA, OH, SE, O(l.A), Nli, N'M(LA), NÍI,A}.;, NCX CN, OCN, COOH, COO(LA), C0N1F, OONfi(LA), CONc.í A};.. NECQí’LA), NilCÖNHCLA}, NIlCONii, CEO és CO(l.A) csoporttal, és/vngy ínOnOsAsbsziituált '€:VC<: vagy O-CvC csoporttal; CyC jelentésé: 3. 4* 5 vagy thtsgh montK-ikhisos álíils hetno- vagy hétmöMö'S> «mely' ö~2 sMfematomot fartalma* Ö. S és N köHil választva, és fehet mono- vagy disvnbsvtiloálí Hal. LA. TOh*. NHif'LÁ}* MCI-A):}. MÖ(LÁ·}* csoporttal; €yc': jeíestíése: § vagy ti· tagú tnotutesklusos aromás homo·' vagy heterocikhss, amely h-3 beteroatoroot tartalmaz O. S és N közű! választva, és lehet mono·· vagy ds-szubsztituált Hal vagy I .A csoporttal; év 33: .Mentése I vagy 2, ti Áit 1. igénypont- s«óimti;'Vogy®l#%,:áö: £ tésdetospfete; lem. jelöl: ^a^aékok jmjtptése- %z I . Igénypont s/vrasfí (I) képiemé! megadott, de a a se ív her! m. I alképlethen: X jelentése M, vagy a 2 alképietbest Y jelentése N vagy CH, vagy a 3 alképleiheit IC jekmtése Hal. LA, O(LA), Cyc! vagy Cyc\ Vágy a 4 alképietbest Árjelentése fenil vagy pírldll, amely vsubsatlmálatlao vagy ntopo- y&amp;gv :§í^bmit«álí' Séjy tó. vagy 0( LA jesoporttai, vagy -az. 5. slképletbest 1 jeletstáse ttteilí kapesbíóevoport. astteK· nminometU-csoporttaí szubsztitoálí, aís»si az ammesmefil amiaoesopöftja smsfesztlmáfeüast. xas.> t A csoporttal mono- vagy dMubsAttuu, \ag> b jeJctttoso ístctií kapseléesopoA, aalOÍy (azetídin-l -IDmatil-csoporttal szubsatHisált, vagy a 7 a I képletbe;! X jelentése M, Y jelentése N vstgy CH, R.! jelentése Ital, LA, Ö(LA}, Cyc: vagy €ye\ vagya 8 alképlesbesi X jelentése N, Y jeienscse N vagy CH, Árjelentése testű vagy pindil, amely vmbsatiiuásaSlan vagy mono- vagy dbzubszíuuák Hal. LA vágy Oil.A) csoporttal. vagy a 9 atképlelheg X jelentése N, Y jelentése N vagy Ok E |©bt«ése mcül köpcsnlócsoport, ötnek- amu^éi^f^rttal ilsmsbsatítsSlt,: S® amfipmatil «Iftítesopoitji Yagy t-&amp; ösöpöstlsl ::mo90·· vagy : diszuljs^Á: vagy E jelentése jnetÜ kapcsol»-csoport, study {a?.eüdro-1 * tl)metjl"£sopo*líö]L vagy a 10 alképletltett :X jelentése N, Y jelentése í..'NH2í L jéleótésé -'C^IkE'^HH'-CíJ-- vagy AótYíR-Llí^lLL, W jelentése Hal.* LA, ÖíLAj* €ycs vagy Cyc*» :lf jelentése H vagy 1¾ vagy a I I afképfetben X jelembe N, Y pl&amp;iúéss CNH?, E jelentése -βίΗ:?ΕΧΙ ί-·Γ()- vagy -CO-NH-Cl-HíLK R* jelentése Hal, LA, Ö(LA>, Gye5 vagy Gyek R* jelentése I I vagy LA, Ar jelentése fent! vagy psrtdíl amely sgubxAnuálatlan vagy mono- vagy dísaubssUltuált I lak LA vagy O(LA) csoporttal vagy a 12 atképtetben X jelentése N, Y jelentése €Nt L, C jelentése -CI1{R'>NHO>- ΌΕΧ-Ι ECHí R' K kf jelentése M vagy LA, Árjelentése fell vagy psridlk amely sautetituáládán: vagy mono- Ha|LA: vagy OtLA) csoporttal vagy a 13 aíképíetbeo X jelentése M Y jelentése N vagy öi E jelentése rnetn kapcsolöe-scport» amely anbnometibesoporttal sstubsztiu-álL ahol az tnninomeul anbwoesopsrtja sxabsxijtailapap, vagy LA esoporttai mono* vagy AEa:absgPtuáls vagy i jelentésé mettl kapesoióesoport, amely (azetklm-i --ΑροοΕΙ-csoporttal szubsxtituált. jelpiPisg ffesi! vagy pirkiM, sssssly saufesgits^álailaB vagy igtoao·- vagy dÍsKu1:?s%Htuálí i-A vagy 0{LA) csoportúd.; g; jelentése Hal, LA, Ö{LA), Cye! vagy Cycj vas,y ^pgysá^íysa'ctlfeg díbgsdlwttö sója, szol válla, vagy a so szolváija
  2. 3, A tiö^eitezókbél álló gsgppp&amp;ól ygfssztafct L igáoypoat szór tali vagyaiét :q.. {;í|->róS5-2-ísmlw<>' I >íy*^tíl0:tsorm^ i1>~etí 1 j«písíiΐΐ-:I -il l -5-{4-l1tK>rfcn-lhptnmkHn-4· Uamtn: i>(4-(2--amato í ~t 4-ut'ia oímvKKtlh'm'fcullptpeta; *' ' ti} i 11 pfrazoí~441}psrimidm-4-asni«; O- i -i-p y)· 2 -amiin. -! (4 -lt tUtmrmvtib foto! Kis I l-ptpct tdm-I - Π *->-^ I ilttor-fetm l-píriraidin-4 · dasma; {4--|6'-aaiíaO'S'(4''nuoí''ic;Pn-psrimid|pi4'ír)-pipefazia-IAiy-(ó-tnnuormetll--p5ndm'34ík acetooítrii; ó- |4-[3-azeitdia· I - ti -1 -(·Ι-4Ιόν-1κοΐί)-ρίορί!]·-ρίρο^χΙο44Ι}'-§4441οοΓΐ^ί%ρ^?5ϊό4®~4-ί&amp;0θό; (S)--6-(4-(2-a:obío-l g4-{a'ith.torsyictji}t«tiii)edl}pipomziri44lj~S'-pli'-pi{'azok44ilpir»i<iisi-4s amist; tg f 4~ j L-amáio-d:4t~Íuos-#oil;|~ctikpiparazia~l 4!} -S'(4-«lsdor-'feóil)«pirisPidln-4-llamia: á44424szalííÍűS'-!4j)'-i~{4-fírfcóMUsiii)fessíÍ)etií|plpOf8zm-U-s0--S44-4lapí4siilÍ|piriö|itlist''4i·' tttnin; 644424'dintetUamtHo)4-(4--<iriniKitmcii!}femi)etll)piperazin44j)-54441siorfenU)plritnkim“4- apáti; p..p1..,(;y8mítK>'-1444tríi1t!onoeíj!)feníl)eííl)píperKÍÍH-i“t!)--5HÍl'l--pífazo!'-4--tÍ!pitlar4lHv4-aittin; |;-;3-a!nlno->Í-jÍ^anano-5'í4~fipoulö!'ilj'4i5ymvídiiS--4-íÍppírroiióiife3:“lisavtiik2,4-dlÍPOÍ'- benzatoíd; 6- jA42-&amp;a'dpp44ő-4rífiöörmsilkpk^^^4~iij ~3444|«αΑο^ iiaodn; 6 · 14 - |(S}- 2~am sno-144 'kíór-fettiiVets! |-pipeffízi>i·-1 -í l} --5 -eb kp? nmídisv4--Hamin; &amp;4<l42-a?ní«o-4"(^4{riííaöitaeíibtbaslVtil)pípvsaztO'l - d 14 - vkv< i p i d ab <iin--!-a nst a; d-amlno-i-jo- ane-sv-ág 1ΙΙ-ρπ,?οΊ--ί bt plrim tdm 4“d]~ptpvnditv44%8rhonvtY--[iS)-i-tΛ -Idór-fc55Íi}-'propsl)-astsid; 6-14-( 2-astboo I -(4-trlfl»onneul-ksbS)~e? í Ij-píperazisk1 -II >-5 'kkSr-piriM|í«-4i»lka#»' ás av6e\szvrés/etdeg elfomulharó síd vaov saolvátjai. (^gy&amp;zztémái készítmény, amely tartalmaz egy 1 -3 ígái5y|?ísjíö| MbMíIysM igeriMí vsiyöís^ ^iF'^Sys«edM«tí1^i-élfog«Mlható s^ti Mgy sko^||éí mfeí hatóanyagot gyógpzer#^t|l#g '0&amp;-gadhaíó hordozóval együtt. S> Az 1-3 sgéoypoíteh bármelyike szerisAi vegyidet vagy a győgyszerészetileg elfogadható sója vagy szolvátja, gyógyszerként történő alkalmazásra. tk Az 1-3 igénypontok bármelyike szerinti vegyidet vagy a gyógyszere szelik g elfogadható sója vagy szolvátja, rák kezelésében történő alkalmazásra.
  3. 7. A tk igénypont szerinti vegyfdet: vagy a gyógyszerészeti leg eiibgadltati sója yagy szakága rák kezelésében történő alkalmazásra , ahol a rák a kővetkezők közöl választott: agy-, tndö~, vastagbél-, epidermoid, laphám-; hólyag· , gyomor-·, hasnyálmirigy-, mell·, írni, nvaki, vese-, mái-, peteleszek··, prosztata-* vastag- és végbél-, méh-, végbe!-, öplőcstH here-, nogyögyiszsíL pafzsmirigy-rák, meiamSmp, vérképző rendszer rösszloddlatn betegségei, mint például akut nóelogón feukemiar mielonut multiplex, krónikás miéiogln leukémia, ntieloid sejtes leukémia, glioma M Kapóst-szarkóma. tk Készlét: (kit):, amely aikövetkézők kalönáiléresontagiaittahalmazza: g) egy vagy több 1-3 igénypontok Moplyike szerinti vegyidet vagy a gyógyszerészeifcg eifbpd-bató sója vagy szolvátja lunásos mehbylsége, és I) további gyógyszei'hatöanyag haíásos mennyisége.
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