HUE026705T2 - Vegyületek béta-amyloid termelés csökkentésére - Google Patents

Vegyületek béta-amyloid termelés csökkentésére Download PDF

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Publication number
HUE026705T2
HUE026705T2 HUE10747095A HUE10747095A HUE026705T2 HU E026705 T2 HUE026705 T2 HU E026705T2 HU E10747095 A HUE10747095 A HU E10747095A HU E10747095 A HUE10747095 A HU E10747095A HU E026705 T2 HUE026705 T2 HU E026705T2
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Hungary
Prior art keywords
mmol
chloro
dihydro
rti
preparation
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HUE10747095A
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English (en)
Inventor
Kenneth M Boy
Jason M Guernon
John E Macor
Richard E Olson
Jianliang Shi
Iii Lorin A Thompson
Yong-Jin Wu
Li Xu
Yunhui Zhang
Dmitry S Zuev
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Bristol Myers Squibb Co
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Publication of HUE026705T2 publication Critical patent/HUE026705T2/hu

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    • C07D239/72—Quinazolines; Hydrogenated quinazolines
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    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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Claims (4)

  1. SZABADALMI B3ÉNYFONITOL
    1. Vegyek· a képlet {1} «mint
    vagy A rn '&amp; 'mM 1$ ®é< Ä Âsœ *®ßmm %eMrMômoi stóy Μ vsmvàlaMAa à RöMfeÄ Iái: stepM Mp&amp;> m Ms; tó s Mtermaxtó :g^M -imwßm mümMfo* **» mM “ tó>otó; »tóv ki * mmm » ifesfe* ΜΑΗ: Mô» àafcCs^lMï» Mroxî, tóftR Csgakrm» A» Ls^aMI; B Mvaa vàM^vs s «ító§k:MÍ:: ^ «« prnàml·, tó z-imi m-priding qjÄsÄa m?m **Λ »A»*b«w»j ßggeöeM» amely ki vm vámm« a Mtóstótólk C^któ C^IM, »s> C5.#&amp;lkasmia^q^lk<H Ui% kdoCiAilkii, tódttad, metóstó és amise; DM vsa váDstós «következők közál:
    %->íí wS a szüJó taöfeMai&amp;a^i0|^áá«{. s 8ÍBo|éa#össMA
    fc^tókklM poöwksIíM ss B- stóhez; M* %w&amp;:Ä%M'-Ä^teöiifÄ &amp;Ä#ß, îlij^ï^y^âik^ Äi; JR* -MRéRR #M R* äs R* fsgg«kiiüí M vsa választva s következők közül; lőtógőü, CR gdkaxg Ci^&amp;UoexlCiMki}, CtMkoxifatboaiL C^elMl» €$.>cikfoa$hk {C^?cxkjhslkli>C; »alkil, iBáröMC·-^alkîl» és eAlextkromeöL aboi a (€v?eüciMfei}CiMioi alkii része opdoMlsaj· szubsztiíuálMé egy Ck, gáksm csoportsai; vagy, R* ás R\ egyiist a oisogéa atommal, amelybe« kapcsolódaak» sáptó tagé moooclkiikas vagy gyilte aikteak, asoeiy ogpoaaikao: ggl^nap m- Ä és Ιχ4βκη«ηοό teleld väa vàksz&amp;ft^liv^átóök^iteöJiíO»:KX*,Ä%. sikís R* ki v&amp;n· vaiasKva &amp; köv«fc#k ki>s»S: hkirogén, Cs .gabch, m Êà^alteÉkbosâi és ató a gyára opcionálisa« axoteditnáiva vais egy vagy kettö sKabsxbmenssei ífBggotfeil«. snssly ki vsavaiastes g k&amp;veíkeahiéködűk €e*aifem, <.^.*8lfc!^#slo« ksiokí^alkih tàârmfe· HÄ* oxo, spboerklikvs dioxokoii; sixű li' és Rs iűggetiéaűl ki vaa válsssava y követeik késük károgék C'j .^Bsxikamomk és ßysÄüy :0 ki -vsa váisssiva a kövktk&amp;kik k&amp;diif hxlrdgé«., ßkglkilssnlibsii, C^pükiisxöiifeßibialdo» amincg €;..,alkte:oio<a C, {;<ks;kiiâ»kîK>. €;<. ydkioaikikrnino, bidtoxi, és; C^aikesd; Éá U -mi vsíassska &amp; ktedkeail Äi Mdrogén, C^aUui, eí.^ítelCi.iSikiiksrbodL Spj, tekoxikanxsnll. C^,aű.kiikarixe5:il, €;.4áikiis£«l honik CVvCikioalktiszulfba!». Cvg:kkadkii.knebosiL £h-«di&amp;ikUaîH»aoC5 .«alkükaífeonil, «s haioC^alkÜ, aboi az álkor: ikarhoni! alaki! réssé, ax alkilksrbot-ü, és as: aikiissrateii opcionálisa« sxubssbáíáiv'a vssca egy ssubsBtlítjetíssei, Id mn: yiksgiya a kvsvgsíkggök kô;dà; €5.4<üaikil&amp;mbK>, és Q^aDcoxi; és Béki vá&amp;''*#aMv*· a :kteÄISk Msük C > .„aikil,. C^MoatÍöl| {C4.70ikiödks!|Gj,4Äl ixteil, teli és égy bí-lísí tagi aæœly mnaiax® egy vggy ksbb rteogeo mmA, «bai a :&amp;8Ü> « berooi feaü rész^ és a mmmmák gyűrű sá»d«gyike <f ekmálisas sKgfcsüîdaàlvs vas egy, kete vsgy károsa saAmitesseil liiggedmïiik amel| ki 'vaa vMasatva a Ikketesűk kosű|; fê^aü#, £|.«alk<Ä. elate halo, haldCî.^fca^^^ei^üi·
  2. 2. Ax I. igénypont ssteaii vegyük??, vagy anask gyngysstessetileg ebopdbgib sója, ahoi A egy ö«agú hetcnmrosm gyűrik sorely tanaim«* i-3 nibrogéo atomot; aboi s hetetoaomte gyűrű epeiooáiís&amp;o szabsxűtelva vsa agy csoportsai, amely M vsa yáiesates kbyefesűk kosuk halo és Ctesikü· 3. A 2. igényperé: sxednű vegyük«, vagy gsoak gyögysserésxenieg elfogadható sója, ahol B ks van välaÄ^^M^kea^l^k.Äisi^firidM» shoi a kah és piÄtni efefoaálisa« s&amp;tedítaálvs vas egy vagy kg?!#·^sxabsaridäessseliSggdfeüi, tpssly ki vas vűiasxiva a Mvetksxok kikül: Cj-galkoxí és Mr 4. A 3, igénypont ssenati vegyük«, vagy annak gyogytmeteeetiigg eitbgsáhaíó éÉja, ahoi B teli, stnely opcimtóihaa sznbssdöstBva van egy, keixű, vagy három szsbssxsárenssei ilggeheslií, arnoiy ki vsa választva a kltetkeabk kiválik €<.saikiS, C'^salkoxi, eiape, bak;, hak>Cä,;alkoxi, és beioC:.;,aikü, 5. A 4. igány:x;ni asesintl vagÿsiet, vagy anaak győgysaorésgetissg oilbpáhalb sója, abo! D ki van váksidva a köve-kesök kokii.
    $> Ax ű, igériypsn? ssednil vegyibe·., vagy annak : gyégyagerésséhlog eiibgaéi-iSfö sósa, ahoi K" is-NR5ky aboi R* és Ry BggefäßMM van vàiasarva aMvóíiSéxSk kűpill: hkirngén. C'MalkoxitV^itól, Q. ÿSlkil, Ca^dklöalkil, imbosiG|,4ií!ÍdÍ? és nideatemmebl, siói a |By.?é&amp;loaikii)Ct.48Íkil aikii seake ígseionáhsaa sxöbsx?|űíáteió egy G|,gílkmi csopostiaí. ?, ÂZ 5. igètsypont szerinti vegyaieg vag? asraak gyègyvzerèszeiileg dfcgadöaiő sója, ak>l E'! '· NR'R-y ahol R* ÉE együtt a nitrogén atosnsnal asneivhez kacsolódnak, 4-7 tagst mnnoctklikns v&amp;gy bielkiskas gyűrő* alkotnak. asssly ^eisssslissti tmtateäf*p h>vÄt lÄmsismsk ^ ^ vtóa$pm &amp; következük ibâzüs: O ŐS : MR*; 'tótul R* Id vaa választva s következők közsil: Rjpikil, és £·'«.. pkoxikarbonil; és ahol a gy%Ö ^pctonőlisars szatohutóva vas* vagy pÄÄtaeösm IsggeíiessnI,, &amp;mly ki vas vPPMvákkŐvetkezök közük Cs,«tóta:í, Cä^Ä*::^,Ä«C:.4aöäk hiároxk -MRfc oxo, és spltwikius dioxotami; tótul R* és R* a föggetísnü! Is vau vÉm0m- kővetkezőkközül: hidrogén, Copkoaikas-bossii. és t\ (.slkil, 8. A 4 igéftypoí-í. sïsîdsii vegyülei, vagy isnpk gyôgys3«ré»2Âùisg:«3i>gÂsié só}«, abuM.1 ki váts választva a kövaike/ók közük
    9. A 8. Igéssyposü sserimi vegyölet, vagy áinsak gyogy^kisäsiilgg ollopíjkíiö sója, ahol Efe β, « R* és Ry Ríggctkmíl ki vsa választva a kdvPkeMik közül: hitogen, ü:,ptkoss€Mslkik Cs.fiSMl, Sgptóoslfd!, hidnsxlCVndkik és tridrsitessnaetrl, ahol a {(^jcildsaîkiÎp^sâài tótól Térne opdpÄsan spbszhtuálssíő egy €< pltei csoporttal, 10. A % igésypoat szemsts vegyület, vagy tartsak gyögyszerészpleg tóíbptóp» sój% ahtó R* >MRN1R, ahoi Is és Wf együtt a snszogán atommal, amelyhez ^c«tóédatóí,.4f tap ioosocíklikas v*§y hP&amp;Hkss gyűrik alkotnák, amely opcionálisan ;&amp;ttal»x&amp;z egy további heteroatersoi, amely H vats vágtatva a köveikéxők Msük Ö és RE*; alsói Rf ki v&amp;n választva a következők lökül: Cä,Ä és Stpfteikathpsa; és tótól a gyűrő opcionálisa» szobms tusivá van agy vagy kettő szubssdiapése! iSgpiptük astsély ki: vau választva a kövatkezök közül: CI:,äSMoxi, Ct^alfei, haló. hahCsPlkst, tódroxi. d4R.*R*, oxo, és spirocskkis dioxolanll; ahoi R! és R* inggédenül ki van választva a kővetkezők közül: hiorogésg Ci^&amp;ikoxíkarhoiük év Cs.piki, i l. A: 4. igénypont szenet: vegyülök "vagy annak gyögpzerészenleg alRpalbatő sspt ahol ISI* mss válaPlm a kővetkezők közül:
  3. 12. Az 11. Igénypont szerinti yegpíük vagy sasnak győgyszcrészosiieg dlogadlsaté sója, ahol Rh -KR*RV, ahol Is ás Rv tüggetlesül ki van választva a kővetkezők közöl : hidrogén, Cs,.#ikt5XsC;,.iaitói, galkik C^olldtsalksl RidsxsviCbpkiL és iidouteronséil, ahol * (C^MÄii>Ct4ÄMÄ ÄI része opcionálisan wbs&amp;titoálható egy Cs..,aik;s;i caoportiai. O, A 1R-. igéttyposn szerinti vegpiet, vagy annak győpazesnsptilég eibpÄsio apja, ahol 1? - MRMR, alsói E* és Ws együtt a mtsögen aévntsnal anselylséz ktgresoidőssaig 4~? tap snotsssolkltkns vagy Incikiikus gytsőt aRoünsk, ssstely opoiopliaan trnlaisnax agy további^Istóeszssánaotl amoly ii -vm xilászlva s következők közül: O é» HR*; ahol R* ki vas yÄs#?a a. |$veifce*dk közük C^lkR ès C-„ odk;mk&amp;ího«ik :¾ ahol &amp; gyűrű opcionálisa« sisibsals^iâivs yga egy vsg> kenő sEubsztkiienssei fruggctiesüh amely ki van választva; a koveik&amp;dîklœlæi: Cu^koxk C'ashlkls íhaiös lihiöC^.#&amp;i| MdRixi -&amp;KfR4öM, és ásokslssdl’ aM R ks íüggeíiemil, amely ki vsa váitasvo a kővetkezők kik»!; Äogsik <ii::.^ű:ks>xikstfeeni:k # €W1$·
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N24IH'iï^oi*^5B-^^tlkf'feî^k^J-okiîilro-5}^ïikU'pç!;tâjd;p;ninsdi!Vi;'i-d;aîXii5:i; i«ttI->ii,7-dsbidri>'SH'Ciyop«rta[i!|pis^:8s!ift-'2(4^ dkístp; Ν' « *< Κγ/' d «‘ ' '< ' t» 0 \* « % -1 v> m&amp;c>-5H<^kk^ma|dljp«imj<{ia-'2,4| disssm; P^ös;kk'M2-(Í~K5enkd8-:íí:iácdk-i1}-7-fePi-6.?'áihIdí^-SH-<:Ík!opema[d]i5ídmidis^i4'-3kííöa; >J4'!îv'i' \2*x Nr»eit>Mv>'J<l **»»·. ol »'*ι8 '' diatîîiîî; N2«(44m<hv!-í•»^'äoxifviid's-Nd-ir.et!;·'? feo» 1-6 ?-íithsdr<^siH-cMopemaidjp'.riniul;.n-2.4•dixikp: ;i:^4.|4.|sSs:!|kssoo}.?"fe8ä:-'k>7'diiädäX).-5H-idyi>|iSSfe4^ip^äS3:kiö^2.ilämmo)feAil)«toi>8i N2'.{4-cikidpk5pi!á8sil>7.{4-Slu:orfeívü)-N4.-íHed1:>ds7-dih!<k-o~5H'CÍkfcps:8ta[djpb'í]tíí.idiíi-3:,4.' dessin: ''|<|¾vf4^Säi½^iMK44½<rh‘^xö^^%me$iHJ-i|â4m'5H<¾¼?p(mt8[dlρ^Iíßχldt$^2¾¾iijgih; •áiav-bís: annak gyögysz^wdktg eliög&amp;ddaté soja. î# Ov^'em^! kompiw;>\ «hty- tmdmm m 145, ,%é»5^ö#ídl Élnaelyike «triftS vegybku vagy annak ójánál: gyógysasíessebfeg Mîtes uKOHtesgét együtt &amp;\ogysz<równlei al|?plli#^áoxóa83f{ifga? vsgy Mgbbvíb ; r. A;? H; ö 4; toy pora bennelykke loenob vegyidet if sónak gyégyszatenbeg dfog&amp;dMtrsèjs IbitesÄra eharáten iS-anükád popod tamteís eÂtesére yeszgemk betegségek (tersére emibskeo. a««nek erre sebksége var·. ahol a besegaég k; van választva a kSveitesak WMi .Másmmr ktíegség (AD), Pows szterotna* enyhe ktígoasv zavarok (MCI). ceteteiA amdeiá angiopaba (€ΛΛ). !.ewy seat <ktnencia (DLB), antyotraí Isu-erah« soïen** (ALS· D.k îek lûtes (estes mydÄ C^Mk ês kea&amp;ggi I l, Λ Π igénypert; wrimi vggyäkä ielhssteiasra, aboi 3 betegség ki vas választva a kft ve tietek kCxik AlsdMrner betegség és W&amp;vm ssattdÄtäi yp, A 18. vegyidet teiastetea. tel s betegség betegség.
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