HUE027316T2 - Kondenzált imidazol-származékok, amelyek IDO inhibitorokként alkalmazhatók - Google Patents
Kondenzált imidazol-származékok, amelyek IDO inhibitorokként alkalmazhatók Download PDFInfo
- Publication number
- HUE027316T2 HUE027316T2 HUE12715295A HUE12715295A HUE027316T2 HU E027316 T2 HUE027316 T2 HU E027316T2 HU E12715295 A HUE12715295 A HU E12715295A HU E12715295 A HUE12715295 A HU E12715295A HU E027316 T2 HUE027316 T2 HU E027316T2
- Authority
- HU
- Hungary
- Prior art keywords
- imidazo
- group
- isoindol
- hydroxy
- cyclohexyl
- Prior art date
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- 239000003112 inhibitor Substances 0.000 title abstract description 32
- 150000002460 imidazoles Chemical class 0.000 title 1
- 229940079865 intestinal antiinfectives imidazole derivative Drugs 0.000 title 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N EtOH Substances CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 201
- 150000001875 compounds Chemical class 0.000 claims description 178
- -1 aryK3i Chemical group 0.000 claims description 156
- 229910052739 hydrogen Inorganic materials 0.000 claims description 101
- 239000001257 hydrogen Substances 0.000 claims description 100
- 239000000203 mixture Substances 0.000 claims description 96
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 79
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 77
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 74
- 125000001072 heteroaryl group Chemical group 0.000 claims description 60
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 56
- 125000003118 aryl group Chemical group 0.000 claims description 52
- 125000000217 alkyl group Chemical group 0.000 claims description 48
- 229910052736 halogen Inorganic materials 0.000 claims description 46
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 45
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims description 39
- 125000005843 halogen group Chemical group 0.000 claims description 32
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 29
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Substances C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 26
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 26
- 150000002367 halogens Chemical class 0.000 claims description 25
- 229910052717 sulfur Inorganic materials 0.000 claims description 25
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 24
- 229910052799 carbon Inorganic materials 0.000 claims description 17
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims description 16
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- 125000003386 piperidinyl group Chemical group 0.000 claims description 11
- 125000004429 atom Chemical group 0.000 claims description 10
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
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- JSPCTNUQYWIIOT-UHFFFAOYSA-N piperidine-1-carboxamide Chemical compound NC(=O)N1CCCCC1 JSPCTNUQYWIIOT-UHFFFAOYSA-N 0.000 claims description 6
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- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 2
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- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
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- AICIYIDUYNFPRY-UHFFFAOYSA-N 1,3-dihydro-2H-imidazol-2-one Chemical compound O=C1NC=CN1 AICIYIDUYNFPRY-UHFFFAOYSA-N 0.000 claims 1
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- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
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- 235000011389 fruit/vegetable juice Nutrition 0.000 claims 1
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- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
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Landscapes
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Claims (2)
- EONIlP^lálT ÍMÍf>AZOL~SZÁEMAZÉKO!L AMELYEK, mo IN IIÍBITÖROKKÉNT A L K ALMA ZHA'FÓK Sznfmdahm igénypotrtok K A következő általános képícrü vegyül«?;vagy annak egy gvógyszerészetifcg elfogadható sója« ahol az η köles egy egyes vagy kettős kötés; « énéke 0, .1, 2« 3· vagy 4; mindegyik R: jelentése egymástól függetlenül haiogénatom, dann csoport. nhro csoport, C: tcdki! csoport. Ci ««kúogéiwlkll csoport -OR, ->RRk\ -ŐR, ·< tOiOR, C*«^NxR'n -CiOtR, AO'R, SoK>R, -öRv>\hR':. vOkK SrtMíK, $(OV»N(Rk -OCVRR. kK*iO‘08^KAO^iR».v VRK RJX.-XtX ROiORvap NU<<RON<RV R2 jelentése ~Cs..;alkil-RA vagy <E-mikenii-R\ ha az a köles egy egyes kötés; és R' jelentése -C(H)R'\ ha az o kötés egy kettős kötés; ahol R* loU'otcse t'N, 0(0>R\ -OOXlRg XVOjNiRWX -€fORBMR;i)(iß), -í\MIK**rRN R°í vagy A\-N-OR'dK, ahol R* idomése hidrogénatom, C.^alkii csoport, Ct^halogêit-aîkil csoport, -CR *,a! ki í-i-R -C\0)R’, -CtOtNtHíR' vagy -XOolK, -tROuCH.haCOOR, CiOKCHa>MiNRiœOR. C0YaKKHo(3Rf\ S(OoOR\ A(OR\'íR ’i\ -( Ι0-01\(>Κ0!Κ- vagy -PíOí{ÖR'"í . ahol RP5 jelentése ciano csoport, nitro estsport, iR .· aikft csop^tk ÍR AKdogeomlkd csopott, -OR,' -NtRX -$R, -0010R. -C{0)NtR>->, -CtOiR. -SfO)R, -$tO>OR, -S(0)N(R}>. vO\R. N<OoOR, AOtA'tRm AX\OdL (X\U'>OR. iK\OA<R> N;KK'tO)R .NíRtCtOíOR vagy -N(R)C(0}N{R}n R° jelentése hidrogénatom, matti csoport* CHfCHRE 4TH>CHtCH*h» -CIROLltCHAI hl heortl csoport, 4-huliox.ohesmd c,sonor?, CH-yc-ntdolilt, RTRSih -OH ΌΜ(Ή „ -CH;ÖH, -CHlCHOOH, -(ClMrNH =. <CH^-N{H)C{“NH)NH,\ -CHM~hnkkuvU\ c nha^lUW'Ht'iH'H C'HAOXR CR<ai;( t*\‘Ik mindegyik R'' jelentése egymástól függetlenül hidrogénatom, Ci^alkil csoport, CnshaFogén-alkíi csoport, aril csoport, heteroarií csoport, C-osctkloalkü csoport, CVscikio&ikenil csoport, 3-10 tagú heterocikiil csoport, aril-Cj.*n!ktl- csoport. he?eroanl--Cuonkii~ csoport, t.\.*c?kk>aikii“C ^alkd- csoport, í..Έs,«»>nki> csoport, (3-10 tagű hetetxxüklil.}-C{.fca!kil· csoport vagy (heteroariD-O-iO tagú heterocikUir- csoport, ahol az alkii csoport, Cí^dkloalUi csoportoCs-scikloaikeníl csoport, 3-10 tagó hettmtciMn csoport, Cí.sctkloaikil-C«.ftalkil·· csoport, CMcikloalkemhCmsdkih csoport- (3-i0 tagé heteroeikhihCi .«alkil* csoport és fleteroarih-iMO tagú hctcrocl;kli!V; csoport opcionálisan és egymástól íüggerleriCi helyettesítve vannak egy ~R "' csoporttá* es mind opcionálisan és egymástól îiggetieoül hej vértesit ve vannak egy, kér három vágy négy Rn csoporttal.; .e ,r n e^yvu htdoioar;! c-mport, ,ιη!Λ\ ,,,ρ,κη cm^o t ^ > fe>oanhi't .„xlhd csoport mind op, mnátisan hcheitOMtsc várniuk eg\, két. hatom sag} négy R"' esopouiuk ahoi mindegyik R3! jelentése egymástól függetlenül hulogenatom, ciano csoport, nitro csoport. Csalán esopori, -€Y>>aiki!-Rx', Cf^halosétv-aíkil csoport. -OR. -baRK -SR. •OöjOR, -CiDiNrRh. ·Γ(0)ΝίΟΗ)Κ. 0.ΟΉ. (bXR'VR .G\R':'\\R dt vOXb -SGRUR, S«,0*.VRn SiO''R. ohOk>X, -S«OvVRk üGU:R, -OikO'.OR •OGOlhbRK NàRiCiOHî VROOK^R. YRVtO'VRp. aim R'5 jelentése elano csoport, -OR Y K o, SR tMJ-t*R, < 3'ΎH ·,, y\{VR, S-nO'R. -S^OtOR. -SíO’NvRV. R. YO> OR. MOyYRm 4X\0'»U. OOtOiOR. NiK'AO'k, -N(R)GO)OR vagy -N!(R}OOiNiRj-e. R' tekmteoe ~0. ~i> ~\iEi, “N«,ORp ~GK Y, ~·,··.ρηο4 ,οοΥο,Ρόη xv'port'4 s*,gx ~{spim-f 3- ! 0 tag« beterocikiil csoport? ?, ahol mimkgyik R ™ jelentése egymástól függetlenül hidrogénatom, halogénatom, cinné csoport. Ci Glied cxopon. -C otlkh-OR. <p, „hulogrn-adkn csoport. 0¾ i lUoalhs· csoport vagy 3 · 10 tagú heterociklil csoport; vagy mindkér R'4 együttvéve az. atommal, amelyhez mindketten kacsolódnak. egy moitocíklttsos Cx.itcikioaikil csoportot sags monod Un mis 3 b tagú heten vKhl csoportot képeznek; R* te >i^‘k Vés vc’vte t ' * JMtCMípirt és mindegyik R jelentése egymástól függetlenül hidrogénatom vagy \V\ ahol R'° jelentése Cj.í,alkil csoport, t , ? fogé.» ,dkd csoport mii t »opott, hmeromd tsopou. <b.*dkloalkil esopoit, Coxcikloalkeníl csoport., 3- lö tagé heteroeiklti csoport, anl"C;.c,alkn csoport, heteroaril-Qc.alkií· csoport, Cb^cikioalkil-Cj.itdkil- csoport, i 3. >cikk«ilkcml-C> ^alkii- csoport vagy (3-Jö tagú heterocíkH!.?-Ci.,..a!kjl-- csoport, mindegyik Rw opcionálisán helyettesítve van egy, két, három vagy négy csoporttal imchck cgsmastol íuggctinml a Uoetke/G Ydogenmont, manó co>pojt, mtio csoport. Csaodkll csoport, CGialogémalkil csoport, -ÖR;l -SR!í, ~QG)ORiS. -CiD}NtEiS;p, -C(C)}E*b -S(Ö)R:\ SiO'iOR b GrthNtfG G G,OeRí!. -S(Oh0K !. •S(0.;.rNt'Rn}>, -OCíOlirk -OnOX)Rl\ a>GOG\RG.'. NiR sXGO)R!\ -N\RlX\OíOR . -XiRs 'GOGcR’G, -\\R,!.\:0) R* rum túrni heteméi ki ü csoport), ahol mindegyik R'! jelentése egymástól függetléiiti hidrógéiuaom vagy CmXikil csoport,2, Vegviilet az. L igénypont szerint, ahol R” jelentése-QllhpR \3, Vegyület az. I. Igénypont vagy 2. igénypont: szerint ahol R'' jdentesc -CM, -GO'GR'' vagy '€<O.íN<R'^t ).4, Vegyidet az 1. igénypont vagy 2, igénypont szerint, ahol R* jelentése XXOXG,5, Vegyület az. 1. igénypont vagy 2. igénypont szerint,, ahol R';' jelentése -O'OR^VB h(Rc). h. V\g>ület a' 1-5, tgonxmxntol bármelyike s/ermt, ahol R' telemébe an! csopou, bcuvo.ml <sop'>rt, C'. „ ikh>al\d csoport, ib xctkto.dkcml csopuit, 3 iu tign heteim iltd χ-ο,νΌ vagy C> íCikloalkü-C italtól- csoport, ahol a t. y vukloalki! is.ypyan (b sCtká>dkcml y.so|v?t. 3'10 tagé hcterociklil csoport és Cyrcikloalkil-Cj-ftiüktl·· csoport mind opdomtiisan és egymástól függetlenül helyeUesttve vannak egy -R*' csoporttal és mind opcionálisan és egymástól függetlenül helyettesítve varinak egy vagy két R:'! csoporttal; ás az anl csapott es hetemmé csapon none opemnahN.m heKeü'CMrte mtmnk eg> > ag\ let R'1 csoporttal. % Vegyület az l-ó. igénypontok bármelyike szedni, ahol R" jelentése lenit csoport vagy egy öt vagy hat tagú hetero&ril csoport, a,melyek mid egymástól függetlenül helyettesítve vannak egy vagy két Rr ! esoporitaí, &. Vegyület az 1-6, igénypontok harmelvtke vitáik ahol R' jelentése fenti csoport, eikiopeníi! csoport, dkfoheiil csoport, eikiohexenil csoport;. futanil csoport, iettahldropiranll csoport, piperidinil csoport, irmdazohl csoport vagy hazohl csoport, amelyek mind opcionálisan helyettesítve vannak egy, két, három vagy négy R'v: csoporttal és ahol a ciklopemil csoport, eiklohextl csoport, cjklohexen.il csoport és pprMml csoport mind opcionálisan helyettesítve kánnak egy ~R '-; csoporttal, f* Vegyület az 1-6. igénypontok bármelyike szerint, ahol jÜ" jelentése a következő: aholaz « kötés egy egyes vagy egy kettős kötést m értéke Ο, I. vagy 2; p értéke 0 vagy i: és ha az a kötés egy egyes kötés, akkor Z jelentőse - CíR:*)r; -C^r% -N(R3·)· vagy -ö··. ahol R'^ elemese l«d:>»gon.aoto. Ck<>alkil s\ü'R, rttOffeR, -G.OjOR, CtO)K>,R);:, N t5 ;OR \ ,ip> N,í í Art< K 0-< ha ,o o kötés e:y, kettes kötés, akkor Z jelentem *.M< vV~ \ag\ -ΛΑ; ! * V egük R ért üc\e » v srmrtol a 'gém mü hidrogénatom vagy R'y ill. Vegyület a 9. igénypont szerint, ahol az a kötés egy egyes kötés és Z jelentőse ~€i.R' "h-vagy 'Cí-R-'-y.. 1L Vegyidet a 9. igénypont szerint, ahol az « kötés egy egyes kötés és 7 leíentéM -R(R '> vagy ··(>-.12. Vegyület az S ..¾. 'por ^ enni tét ko , \c t a m kertetahol :n értéke 0 vagy 1 ; mindegyik R! jelentése egymástól függetlenül lialogénatom, -OR. -NíRh vagy -SR, i v,'e> 1' k 'te-m V or «s ο! V ye k Hi o û\ V" vttum i e'kd 's' * h y svpou* hetumtril esepun, éVuüoalsii >. .söpöri, C\ « lloalkeod c<^n λ o'* ton bo» <u*knd sopo,t v,g y O'^ ikVerkn ¢/ π Ad ».stopon ahol a t' .aikti oopo.u s iukloalktl i.">ps'n, C^oAHAlkoml csoport. '-it- unm noh.-un.iUU a open 0' C: AtkloAlmmUj miül- moport mind opaotdhsats és egymuA'l t,Agilent'. hcheUesine 'trmtk ogv ~R m^pmual on m \Ί opcionálison és egymástól Hlggeüendl helyettesibe vannak egy vagy két K" csoporttal ; az uni csoport és heteroaril csoport mind opcionálisan helyettesítve vannak egy vagy ke? R's csoportod; ahol mindegyik Ri! jelentése egymástól mggedentd it;ikts..'nutom ». uuv csoport, mpo csoport, C; ,s<ilkit csoport, Ci^aiUl-R0', C. ÁaügenAlUi csnpou, -OR, Niiü · SR, -CtOíOR, -C(C»N(R}2. -€|0>R, -S(0}R. SíOjÚR, -S(0}N?Rn, -S(0.?>R, -StOVOR. -SíOi'NtRK ö>OOtR, -OC{Ö)OR. d>( KüNtRK NdU ?0;R, NiRiCiOiOR, -NtRiC'iOiNtRu. ahol K” jelentess' OK. -N«JR)? vagy ~SR; Rv {döntése o\o csoport -O'R'“);?, .s^spiro-CcvCtkloaiUl csoport* vagy ~(spiro-(3-IO tagú heterocikiil csoport)k ahol mindegyik R'-* jelentése egymástól függetlenül hidroglnltotm haiotéhatöhö CWdkü csoport vagy Cüsükloalkil csoport; és lejelentése hidrogénatom vagy €;.{,a!kií csoport,13, Ve§yölet a 12, igénypont szenet, ahol R' jeuntose „ni ».sopon hetenurU Csoport. G^xCikloaikd csoport, Cd.scikloalkem; csopott vagy 3-10 tagú luteavsko! >< Avport. ahol a CYsdkloalkil csoport, Qvgetkioalkenii csoport és 3-ló tagú heteroerkki csoport mmd opesen.dtsun helyotö'sme vannak egy ~R ” csoportút! és egy, kép három vagy négy R>s csoporttal: és ez ,n U mcod es hü η ι 1 sopo m.id o^-ctooi » at he!'odosUve re m, ; eg'-kft három ο,ν·, négv R' e^opo-He,14. Vegyület a 13, igénypont szerint, amely a következő általános képlett!; aholaz a kórós égpegyeaAggy egysklítis kötés; mértéke 0. I 'egx 3; p értéke 0 vagy I : és ha az a kötés egy egyes kötés, ükkor Z jelentése «C\R·'''):-. O«R '"V ~NíR-VV vágj? Ό-, ahol R" tetemese hidrogénatom. C- gökd csoport, -OOrR, ÜyOAR. OOiuR, <30vN!,RV -SíDíjOR vagy -SyOhNtR)/ és ha sa a kötés egy kettes kötés·, akkor Z jelentése vagy -N-; és mindegyik E;sí jelentése egytnlitöl Ikggetlettül hidrogénatom vagy Eí!.15, Yegviist a 1.2, igénypont szerint, amely a következő általános képlete:vagy annak egy gyógyszerébenleg elfogadható sója, ahol a szénatom-1 {€· I ) és a s'zénatonn3 (03> sztereolzomer kcmfígoácMiár (alakját) egyenként t$> .H) képezi; n értéke l és R* jelentése Euoratom vagy klór-atom;R*· jelentése hidrogénatom: 11' jelentése a következe): ahol n\ értéke 0; p értéke 0 vagy I ; m a kikes egy egyen kőién; Z jelentése -€(&**}$-♦ ahol mindegyik Bejelentése egymástól függetlenül hidrogénatom vagy R'kés mindegyik E jelentése egymástól függetlenül hidrogénatom, Cj.4al.kil csoport, Ceshalógémalki! csoport, árit caopott, heteroaril csoport, CEgetkioalkil csoport, CEacikloalkeml csoport, 3-10 tagé heterociklll csoport, ariK3i,mikil csoport, heteroartl 'Ch .^alkih· csoport, CkacikloaikiECh ,#lkil- csoport, C.v«eikloal'keniÍ.~Cj,4alkil-csoport vagy (3-iÖ tagé heteroelklii}-Cs.aalkíl·· csópon. lé, Vegyidet az L, 5, vagy 12-15, igénypontok, bármelyike szerbit, amely a követkézé általános képleté.:ahol a ezéeatormi és a széttatom-3 sztereoizomer konfignáctoját (alakját) egyenként iE R) képezi.17, Vegyidet az !., 5, vagy 12-Ll igénypontok bármelyike szerint, amely a következő ál ódán os képi etil'ahol a szénatom-! és a szénatomé sztereokomer koutlgúseiéjat (alakját) egyenként (S, S) .képezi, 1S». Vegyidet az L- 5. vagy 1245,. Igénypontok bármelyike szériát, amely a követkézé általános képlett!:ahol a zzénatorn-i és a szérndorn-o szieteoixceoer koníiguácu'ign (alakját) (S, £) illetve (5. 5) képez) ás ahol E'’ jelentése ciklohexd csoport és R" 1 jelentése OR, it, Vegyék? az !„ .5, vagy 1244. igénypontok bármelyike szériák amely a következő általános képleté;ahol a szénatom- ! ás a szénatom-3 szíereotzomer konfiguádéját (alakját) (S’; R) Illetve (5, $} képezi és ahol R* jelentése plperidtn csoport és R'! jelentése -C(0)M vagy -C(Ô)ÇNHR), 2D, Végyölet az L Igénypont szerint, amely a kővetkező: 2-( 5 Hon«dazoi4 V1-apeoinéo!·-5-IDetanók eö!~2-(5B~lmidazo· (5,1 -a) izoináo) -5-ü)aéetál; (E)~5 o:2-'brostv-sztirl!)-4ii-lmidazol;5,1 -a]ix.oinéok 2-(é-kiér'· SE 4m idaxof 5,1 ~a|l zomdol-ö 41)-1 -o!k trshexi! -etanol ; .2-(6-'kMr-5H4mMázo[SJ-álizomdoh541)-l.-eiklolíexíl-etáoon;· 2 -(511-1 m kktzo [5,1 -a] ! zomdo! -3 -I I jetik 2-((( 1. R,2E, SS )-2-) soprop) ! -5 -métl Ιο! klohex ! I }m I jacetat; tetc-butü -t 4-(2 4 5 Hí- Imidazol 5,1 -a)lzo)adol-5-i! }acen!)fén!l jkarbamát; l-(4-a.mltn)-fenii)-2'-{5H"m>ïdazo|5J.-a|)zo)ndol'541>etanon; tere 'but d-(4 - í I -hidrox I-2-(5H -) mldazoí 5.1 -a |izolndol-54l.)etll.)Íeml)karfeamát.; l-(4~amino-l4nU)-:3-)5H~i.ntk1a:?x4:k:l-ajiaóiné3.l'5-il)etano); 1 -tok lobex i 1 - 2- ( 5 ki - lm idazo (5.1 -aj Izolntlo! - 5-lljetan öl ; «irua-o N I urnán, " > « (' M ^ -n » »·«* V 2- -Í SB-lmiàa/o[5, ! a jizoindül-S-ii)* i -0 - niîro-feni Octanol; ^í5Himida^r.(5J-αiî^omdo^5'ü}^(2-niïr¢>-fenΠVtaní«u ' XM< mmk s ï ' „"klrtl * i'x. . O mOO 0*\ V ane.; o ' ! «' « ' s 1 ·ϊο'·> ' . » V *\jk»l ' ‘Λ . Γ A-AU'U „„c λ ni U « > óm * Ml mr\u ' N I V îîuhho* ^ i K'i Λ ml ^k< * hamm.: ' x: -mme ,o'\v' : 5 H » 1 <1 ό ' > eko-unni 3 ' V\<oon ^ ïn - s " mï ' i » ^ r ' «K ** *» >-> * s 1 -(2-klôr-femls-2-<SH-imida;?.oi5,1 ap^oiodol·5-iDeumon: I · rS H - iml toîj 5,1 -a Jteoindoi -5 U e-emenk- prnpao-2~ok '-(Máor-íemn ^ ^kmúdvoAMl/omaed ^ UWtanoK } -(3'klór*fenil)-2»(5l-l"imidazo( 5,1- a jizoindol -5 * il »tanoî; 3- (5B muda'dV iî^otrdoI'5''Pi' l-ttíftil ctanom ^-i.51 l-smün -op-l -a jiAtmiáol-S-á'*- i -teml-etanoL Iule áimciá Γΐΐϊ,ίΠ'Vá>-P(6-tlaoo5H-uniáe,Aá5J-ah/<mklok5 nknmmk lu 3 k:3r fenn ? íheiamm: 5 -.'\IoVm1 ' o íkm eH mwm<?0|5-l-adomán, 5 jBekmom Í-ciKluhexil· Mö-tliKsr'-SH'-unidazoiS.I -«Jizoiadiil-S-iDeuaiol; >(5B-1 η>κ1;«ο(5, i · a jizoindol-S-ilV1 -(te trah s dr o- 2 B - pi nm-4- i 1 )et;mol; 2-í?-'kJor-5H*iftúdasr.ü[5.! -a| izoindoî-5-il >-1 -clklohex n-etsnoi ; í Z}- i -c ikiohex 1! - 2-{ 5H-imídazo[5. ! -apz-m «dől- 5 1 Remnon-OX í m ; l·cikk>J.>emil-2«(5l·l'·imidaz;o{ín"ajizoíndo^5-il.liánok lerc-butil^-ü-hîdfoxi^-iSH-im.idazopJ^lizôindol'S-îl^ùDpii'teridia-l-karboxilàu 1~ς^ΙοΗ«χΐΙ-2-(5Η··ί«5?4άΖ0Ρ·,Ι^|{ζο«^ο1-5^Ι.ί«ηίη··Μΐ3ο; tere ouül -,3--¾ Mmho\i-2-i5H irmda/oj5j alsAmtáukSolV'táRemBkarbmmir, 1- {3-aïYnni>fenli^·2··{5H'·ímîda/o[5J-*a]izoindol·5-il}etaπol; 4· {2-{ 6- Üuor- 5 B-l mkia;ío[5, !. -a ]ízoindoí~5-i) h i-hidfox keli í )elkíohexa»l; -eB Kvs 3 ee,-'\ Ml mmkiA>‘\l a (Amtán ' áVUroL ö~(2 -cjklohexlI-2-hid5T>xi--etH} ·5Η-ίΐηΐ<1*εο{5.1 *a)i««odol-9-oU 2- (8-klőr-5H· in\idazo[5,1 -a]koîttdol-5-à! )- I -cikiohexit-eianol·, 1- íclldohex.··? -én- i -11)--2-(5--H--ímlda/o(5,í -a )1α4ϊκ1οΙ-5·-} 1leumol; -k-áfck>hexii*2á8Mluor-5H-imklazoj5J-a}izöindok5dI»etanol; 2- i:in;luor-5H·· om* ό ''1 V *tk >) e ti' I <\ i ύον,νρικ\4 MdAan-x-ihnKsrtok ··4'·(2d6-Πuo^5l·^ùntd^.t2>·>Γ5.l·aiiz«in<k>i-5·'JlH«·hidrox^·etíl>c^kloheκam>π; 311 mnd.íA^dn-anA'nadol·? i !V-1 -1 -t -s nets lé a -o í k a \d etamd ; 1 «(cikloheK-3 -én-1 -i l)-2«(5H-imidazo(5.1 *ajizoindol“$-íl>euinoU i*<4^hkitx>xi-n etil etkk'h \i > ' «tlizoiadol-S-IDecanoi; <4'i 1-hidioxi .? (31 í -íiUíikeojéJ s|îro«fï<Jol 5-?;íek;}ps(>iTi3;>i' 1 -il;(?h'íí'ás-2-11 (metánon: I. (4..{i -hidroxn- 2-(31-Mt«ida3:o( 1 -a jízoindokS-li }etU)plpendtB-1 -il)etanon; 2''(31-k-i(nKk:;20p J--elieoin do k--5-'l 1)-]--{4-ínetilétr-eikké >exd)e(unok 2 (f*-naor-5) I-unkte/-d"-! -aln.omdoí'5-lh-1 -t 4 - me d k d k kthe x 11 kn <s n ol ; 245 B -lnűd;.v/ot 5,1- ajlzoindol -5-11)-- \ - ξ tu(?;ol-4-í|)eianoí; 2-t'SB-bmkh:r/o|5J-ajizomdol-S-d)- kitiaxok-S-nletanoSt ] .{4-n-hk}roxi-2"(s5H"Íroidazo{5J“a|izöimk>l'5*lk>«rli;pipendí»-l-lí)-2,2-dlmeiíl- pmpásnl>o5u 2--(6-fi uor-5B-imídazoC 5,1. -a] nomád -5-11)-1 -(furán-2-il }emnol; ( l Sh l -cik bhexl l-/-(5H-lmldaKO[ 5,1 -a|n.o.áKÍol-3 · iljetanol; ( 1 Rj-1 -dklohexll-2- ( 5H - ínűdasr.o|.5,1 --alizoíndol-S-iOeianok 2 m-Àuoï "H nul kí/α " 1 3n\"aáol A-J> 1 ,4 red moule V\uk - me \ áttenni: ! -H kk'hex :4-2 pH -ismdaaol?,!-a jÎAàmiol-5· u propán- * -ok 2(3 Η -i mkJazof 5,1 - 3 j aoîndcd - 5- iOacetomlnl ; i~ciklol>exH»3-{6"f!uor-$H-H«ídaxo|5,-a|^0^{>í"5~i!}propáft''2-ol; i -eiklohexi!-3-(5H-lmidazoi 3,1 ~a)Í2oindoi''5-il}pfopá«-2~oU Pd-s 1 «hiúroxi 3 · 3 H imsdazopj aU/omdot 3-U iraipipe odor ! d> 2-tVíob.íaanon, I ..(4,4H&fiuar-cik2oUex u}· 2-(6-ílaor-5 Hdmida?.o{5, ! · a j :xo: π d ο 1 - 5 - > 1 )e P no ; ; 1 (4,4 duhan ojüohoxiH 2-PH unPaAPP 1 ---Φ apkK 4 - 5 - ù plat*; -l#(6*ûuor-5H-rmkteoi'5» l-alkokukd-S-n}- 1 -{l-œ.eù1~1 H4ixridaKri-5-il jetAttöh 1- C^-^ikioprop.il-meuMnkikl-ôhexîIj-Sr^-tîuor-slH-imidazoiSJ-a^xomdoî^-iHeumok 2- ( 6-nuor-5H-imida«of S,1 -alîzoindol-S-il )- t “(4*(propàn-2-îlidén}ciîc!ohe?iH)8ïattol; 1E î-3 - ( 2-es lâche x il· vi nil} S H - Imidazof 5, l -aJi xoîadoi ; 2'(9-f1uor--3ï-l"irriidaio|5J-aii?.Oînd(i|-5"in- M4-rneü)~dk4ohexine(aïiol; 1 -(ciklohev-n-en- i d'-2-lc-d0on5H.ímsdiA>i3J-ajÍA^adoí-5-ilVunol; -.SVl-tsUohexil-2-uR!-3H imidayo[5,l-'ttiiÿOitâok'MlxAanoi: ( R>-1 -cjkiohexil-2-ç R }-·5ΗΦ nidaxoj'5, Ha] i/.omdoJ-5-ii tetanol; îRs-1 -cikPhead-5 p>! 3H-in'idj/o|5.i-a|U'MnU»>í'3-iht‘{anoh ; S 1 -dkPhsxx ΰ-φοΡ -31 1 -imidaxof 3 J -a ji/ouPobô-d :a tanok ! -ciklohe xi!»2>(5H-imid3?of 5,2 »ajizoiadol · 5-ilidé« œtanof 3 1 -cikiohexil· 2-(31 i--hradazoi 5, i a jizolnooi - d- û »etil-acctât 1 -(4-(2 -(heazil-oxi }eüliden)ei1dobex i 1)-2-( SH- imidazoj 5,1 -u|i/omdoi-3-il)i;îanoi; i-{|“(ben^U-sx«líoníl}pipendin-4"i}}-2-(5H-ímidazol5J-alí/omdö1-;5-í!}etaöoU i-(4--0'’kidroxi-Ë -iSH-invidazos5J --a|5ZOËKk4-5'il)eîîl}pq>er!din-i ·;Φ3--(ρητηΦΦί-·5- ϋφρηοη: 2 Φ + d.llav'â-L a H X- ,1 hidvx -2-(51 i-m»da?c ^ \ an<?o*ndo * î „.îdpippPa !-dbetanon; <.>klohexd(4-i 1-hidtoxî 5 tpHonnda/oj2.i -a]s>usadol·5-iiledi ppendoi i d »metánon, metH-4-(My^roxl-2'Pibimkla/oj5,l-a]hoamdob5-die?il)eikkP:ex;uvkadnmiak 1-viUobexù 2 Φ1Ί arada/op-î-ajn'omdol 3 dhnd-tVusbkaíbamök Ι-i l -cik ioheN il -2-(5H-i midazoi $, i - a iixoindol -S-ii teioxi}· 4-oxobutàosav; 4-( 1 -hidroxi 3-( SB-nnidaxop,1 -ajlxoimiokvd tedl vddohexanok 1 .c!klohexil-2-(5H“}mida^of5J-a)>^oíod«l·541)eιil-ben^oá^ 4-( 1 -hidr(fxi-2-{ 5H4n»dazo| 5.1 -ajÍKuirjdol-5-iHeii Π- N-(2-( nieiil·-szuîronamido)eiil)clktohexào-karboxamid; PS'»- ΦΦΚ4^χφ3-(5Η-η^1αχο|3,Ι 'φί,·;οηΦο1-5-4νίΗ-3 ,ηΐηηο-,ΦηοηΜηηαηο,ρ !-oikk>hexll-2-(5H'tnudaKoir!,l-alizo'sOdoi-5-ilks‘(il'dihidragi.'n-foszt'd\; 4-(Mi?dmxi-2-ä5H'}mKki?<>|:NJ -3ΐΐχοίη.,1ο1-5-ιΠοι4χ »klohoxan 1 arbonsax, 1- (4-:1 hsdtwxt 2 píí-nnida/opj'aju’otndoM-Jtehlpípííndm 1 th ' ,pnxhn-4 if)e(anom 2(3H nrndx/ol-Rl-ulixoimlol-3 d' Kxpuop -p-kian b-Ootan.'l, 2- (4-cUkv tenir!- \ -:-4--.. t-Pdroxs 2 :5Η-ον,ρ^/',ρΜ-,φκηη4ο1-5·4ΚΦΗρφοπάη:--1- iiptanon; (2S)· I -θϊΧη44χηΰ·-2-(5Η'ηΐ4ί4χχορ.Ρ-ΰ]κ?.0(5·ί4ο|„5„5{)Λ^|χ2"&π^ίηο-ρΓορ4ηο<χ(:; Í",4-(2-h'.d(X'>\! eulidén vik-ohrvl·--2 s,5M mnda/op, l-ajpontdui 5 d Plattok \2Sni-Cíkkíhtfsd-2-ΐΓΉ miokcoR', 1 elvonul*. >1 5 dVt(bonxoKdnv2-karbcxdak (2S;-5-(;-olklonexiKl-oHd uk ' 1 ,3(V' dob? dics 1 1 *\t 2-amtno- pentándioát; 1 -(4-((S > 1 h : d ró :< t - 2 ~ ( (So a H - s -tu da x c> ; $ j -a |Í2oíndoi-3- i!.k4il)pipera.iia -1-: H-2-kaal· eianon; (3-fíuor-|-hidíx>xt-ldid)(4-(i-hsdfoxi-2--(5II-imidaxo[5. i-a iszol ndol-5 -11 >etil Ipiperld ä n -l-iDsnetaaon; 4-( ! rhi<fro'Xî-2~(5l:ï-I{»idazoP, I -alkoinclol-S-iO^^O-'N-fenll-pIpesidin-1 -katboxamid; (4-lluor-fenlI)(4-(l-lúdrpsí-*-(5kí-bBÍda^o[$(i-a]kaindol-5-i!}etiI)pípeí'idln-I-- iljmetantm; (:2S}-2-ant itto- i - (4- (: i -Mdrox i -2-(5 H 4 mi daao(5, I -a)l aomdpl -5 -il )eü I ipiperid ln -1 -il )-3-feml-'propásvl-fM; (4-(!~lBdrosi“2-(5H:-lmid8aöi5J;-a!ixOíndoÍ-5-i!)ei!Í)piparídia-l4ΐΧ{8)-ρΐΓί'ό041η-.2·· üjmetmm; (iR54a)-4-(2-iiS>-6-lla(n-5H-i.midam[5J--aJÍ2öiadoi-5-il)-l-hidíx>si-etiI}cikÍ0he?íii- bemtóát; (lR,4s)“4- (2--((S)-6-l1üor-5B-Ímldaaol5J-a]ia<4öck)!-5'-il)-l-hidT'Oxi'«iil)dk!ohexanol; l~(34j'hîdïmi~2~(5l?"imkteo{5>l^|i.mIndôi-'5'n)et0>s««tidiP~l~i!)--.2-ifcniI.~er.â«orî; 3- ( 1 -bidrcvki-2-(5H-irnidag;o(S( 1 -a]iaoin(M-54|)edj )-N-fmtü-axeMim1-karba« amid; tere- batl 1-3- ( 1 -liidrox 1-2-(511 -1 otldaeo í 5,1 - aj 1 soi név l-S-il )uii 1 jaxeddm-1. -karbóx I Iát l-C8aeddiïï"3~il)-2~(5Ii4nddaaôi5J.~ajiaoindol-5--ii)aiaaôi; teitnbidil-4-((S::^'l-bidrcxai-2-iCib}--slH-'iaiida2o[5,i-aj:izoi.odoi"S-il)etil)pipe.dd:uvt·· karboxi'Mí; tere-bubi-4-<(R)~1 -hidmx l -2-((R)-513-i?rd da?;oi 5 J -a]isoindoI-541)e:b1)piperidi n- ! -karboxilát; tare - buti ! -4 ~C ( R )-1 - ni drox i - 2- ( (S j-SH-imiítasf 5,.1 -a]i sebül ol ~S 41 jetii )pi pari din-1-karboxilát; tei^-badb'4"((S>'!.-bidroxi--2-i(S)-5H-imidaao(5, i-a]lzoindoi-5~il)etil)pspundiu-l.-karboxdáp !,-(( ls,:4a)-4-(be?ntil-oxÍ)cikic4uíxii)"2-({>--.fluca'--51!-Ittd.daapl 5 J-ajiacdndol-'5-d}etanob 245I4-imidas(45J-á!iaoindob-5-ii)-l-(plrMlB-3-iÍ)eta:H:OÍ; (ItaÍT)-4-(2-(d'.fluor--5H-i.midazul5!Í-ajb^oindoI-'5--:il)-l-lxktiBai--etü)ciklohsxaBol; 4- ((8)-Ι-ΡίΡ^χΐ-2-((Ε)'·5Η-ίπή442θ[5,!-ρ|1ρρ1ρ4?5!-5-'ΙΙΐ€41)-Ν-Ι);«ί1-·ρ1ρ«π4ΐ.ύ-1.' karboxamid: 44( R h l -bidroxi-24i R) -5H-i?nidaxoj 5vl ••a|ixolndPk5-d)etil}-N-fei-dl--plpendm- i -karboxamid; 4 -(( Rt-1 -h.idmxi-2--((S)-5H-imidazo(5v 1 -aIixomdöÍ-54Ijetíl)-N-fePti"ptpeíádi:»-1 -karboxamid; 4-((S )-I-h.idfOxi-2“((S)-5H-it«idazof5,1 -ajteömdoI-S-liietil}- N-fetbi-piperidht -1 -kadmaamide; I-C4"((E}-i4Hdmxi-24(S)-5B4.mMaxo[5J.~alkoi«doi-5-ii}e:ííi)pti^.ddin~i-i'i)-2-i:epil·· elánon: (iR.4s)'4-((S)-2-i(R)-6-fiuon5H-iíUÍda2ö!Ssi-aJláoindol--5-ll)-Í-hldro:xi- etil)dklohexa«ol: (IS>4sij-4-((R)-2-(iRp4-41uCH--5bb-in4daao(5,Í.'á]Í2xdm4td--5-il)-l-hkiroai- adi)clk!obexa.uol; CIS?4s)-4-((R)-3-((S)-6-tltuír-5H-ímk!aa.ol5, ! -ajiaoindol-5-4 i b 1 -bidroxi-ed l)ei kloitex attól ; ( ÍRA^4-((Sb24($)~44hor'6H4núáuzol 5,1 -a|íaolndol-5-lí)-1 -Mdtoxi -etlljcikioknxanoi: (IS ,41-)-4-((8:)-2- ( ( S )- 6-tI uor-SH-i mi daxoí 5 > l -aj isoindoI-S 41 )-1 - h idro x t -eüRdklöhexanol; (IS<4r)“4~C(S>2-({E)4-dlimr»51:i4mMtoo|;5J“aji«o|:adoi-5“iI>-l"hidfoxi~ ebije ikiühex attól; (iR.,4r)-4-((R>-2-({Sj-6''Reór-5bl-iótidazo(SJ.'á)ixoi:ndol-S-iÍ)-l-bidföái- etüiclkkahexatiol; {lRxan 4-uRi-J-uRub-îlov-r ΡΗ-ΙτηκΙιιΜS;i.-ajizoinUoI-S-ilh\-hidroxi- euskikkmexamd; I 4. -/viex J: ( ^ V iTi''ktî/o<N i α Λ' ^ ιΙνίιΙίΓη.κ^ιη-ΗΐνΟ-ΐηηηηη,.Ρο-JH -pinn 4*d»etanon; 1- (4-h (¾ n Mbdro.\k24i li }-5H4raida2o{5. i~ali£OînUol-S-il)eUI ipiperkün- 1 --i!}-2-ienü -, elánon; N u K40.-4 (1 hu.o\i J >Mï mrsdtrekJ - vomoob* slnt'Hok o v* Obe·' asmd 1 -hídi'oxk'2-ύR)-5H i?nkb/.oî5s 1 -a jumnidoK?4he; J)pîpe?njm- ΐΠΠ-2-k'nil· elánon; 2'*{5H-imîdaxü[5,Î-â3i2àndol-'5-4ÎV 1 η 1 4Htnil- ko banvd ipcvrd m - ’· -dVu* tton 1 karbamùî; 4*({R)-l-hi<Jm>ti-2-({Sh5?-Mmiaa/o|5J ajmwidol 5 dvnh \ >,(h,4R>-4-hm.ou ciklohexil}píperídín4“karbox<«iúd',· 4- ((5)- l-hidroxi-2'USi-5í-i-imidMo[5J-a|í?.oiíK4okf!5-U)etíl.í->N4?etrahidn>2H-pírán-4-:il)piperidm- l.~karboxamid; 4d\^.Mm!n>xi~2-uSî 5Η*ιπ^νο(5.1-ajummdnl 5-<|νηρ.γα 1r,4S>4#drik#·-ci khhexi i )piperidf n · 1 -k arhoxamid: I -H \ r,4 r}-44 henzü«oxi)ctkIohex i 1>2 4 5H · îmiüaxol 5, i -¾ jizohtdol-S-i iteianol; H< lrOr}'-4 .íhenen-oxOeikk)hexíi)04ó-f1noroH innda/oi5Jxilixoin<iol'54Í}oia?K>;; 1 η 1-4Εΐ-Μη(ΐ5θχίθ·η8ν5Η4ηη4ΐΑ5|?Η '«»li/omdol'5-iîïenUpifwnUHJ-l -d;- J· (îeirehiàro-JH-pn'àn-'4oi ictanon;2- Olf-unidaAHbJ aioomdubb-sl) l φ*η dm-4 iDeuiiol; J· -, >H' unidn/oj 5, k a l i/oindoi- S-il)~ I -(piridhv*2-i.l leianol; 4 R no ' vv^ SH iriKNOoi^ o, i^vcuiv-bVid'i \ ae ml'icio Ή pnms 4 ί 1 ; pipe i i ù i n--l k arbo x a mi d, N-ciUohex i I-4~((R}- i karboxarrnd; N-ü tr,4rH'< i4ddtx>xu245Honnda/o(5J uUi/oiuaoj-5uhe(ihakk>hexihbeii/umid; N-ciklopemi 1 -4-{(R}-1 -hkteoxi-2-((5 bSH-iroidazoi .11 -ajixoindol -5-il jetii ipiperidin - 1 -Icarboxamid; 5- 'ié-nuor-SH-inùdâ/oj.SH-aJia'.oindol-S-üH'H-dnlluof-medDcUHobexnieianoî; 2-í5H-unida2of5J -aji/.0mdob5-iD-M4-(LriHuor--mdilKikiohexir^tanoU i 44-C(RM-hidroxi-2-((S)~5B-í midazoÎ5,î mlkoirsdokS-msid jpipmdiivi-di-J-H· (irifl uor-mets Bfenü }eUmon ; -V((R>-l--hîdrox!“2-(iS;-5/i4mida2oC5J-<îf|Î20îndok5-U;i,tUi-AJ44-'(infl«or- me ü 1 ) fei ; i I} pi per i d i n -1 - k arboxiiïni d ; (4-((^)-1.ρ?ά^χ^24(5)··5Η·-ΐπικΜ/.ι>|5<1>«}ΐΧθΐοαο!*54!>&ΰηρίΐ>«η4ιη··1·-ιυ(ΐΗ-- imkiaxol-l -H miete non; i -^H-ïtnidü/.olS, i raivzoindöÍ-S-dVi-nie-Ui-huUtt-S-pi,:. 245H-imMazo|5H'a1^oindok541)44teinihidro~2Hi«nm-24I}etanolr J-i'SH-uniüazoiSJ-aikonujol-S-ni-i-CpnîendunJ-slïeiômdt i -Cikkmevd-J-tfR OH ùmda/ofM-aji Mmdobc'-d >eimoi; K'4ÍoU‘mí-2-u$s 5H-iusKU\\êJ--/iu''nmdoi 5 iKlaimk 1 -esk loi *\il· 3-(51 kiinidaaof 5,1 -»lizoindol-S-inpropán- i UaUchexil-M-HuoioS! f-smidaM \I a}j/oo*M-54neunoL _ N-( l-d-hidroxi-2 v5H-nmda<\\M eh-muieel 5 ïHenrdond'--.*\^tU'>mbn «H ona" -<™ ikaeeuimid; 2d5: Mmiüiurol5.1 -a|</ouuk'l 5--Π- M1 H -mndaxokJ-rOei^i 2 i5H-'mmWoi5 1 d /omdokS-d! M ΠΙ-unnjj/oS a dVlO'O. 24(>-tliu>î-5il-imiiiazo{5J-aili'/Â'>imloK5-U}-î uiià/ol-2-dOumo:. (:$$V5d2<iklühexd-2dMdroxkeül>-50draida?x>[5J-a]Í2ö?ndoM>-ol; \ '2 ^sr^rstí-okL^VHiU 2 >*11 busd^'o^d klekből *-diCk»nok \ d-osksokw 2 kíycnídc 5 îi»c;n\\'e*<ïïï'ïd. N-<2~(1 diKiroxi-2d5!d'dnüdaxo|’5J~ii}i^nmk>k-5dl)e.u!?cikk>hexd)acehiirud; 1 V 'Uci t‘ví 2 v"h «'UkL<o aíkCJXUi N k-k c> ’UÎ s’\»o a fkd, 2- ((.1»οι{5.ΙοΗ«χιΙ~2'(<$ν$Β*1πΰ<1ίΑχο|5^>»Ηχυ}ηάοΙ·'5·'ΐΓ^ΰΙ}«η«η<>}0^0"}>2«Ηο«»ιιια!ίΙχ 2 ιβ-ihîoi >H-:i''îo»î í a]i/o íocÍ-5 Γ> l J ϊ cíit ps ΐ! r& aK ^ 1 «4 ,4ïivmi-c>k ^í'cxíU-2 oíki>n'd,uoj5 l~akí'C4\k4 5*d\uaHl; i.^ííIrtxxi-^-i.^H-ííoídAKOlS.I-aiízoíftcIol-^^OefiOciklohexilíacetaiiiid; \ -i-{arra no-met:ncikichextl 5-2·12 H - Imidazol 5,1 ~o jszoíndol-5- iOatanoí ; ·, ií Λί 2 Λ'ι » íj m s 1 < of >2 ' 5 -H îetitKtiklohcxan-kmfxcamsd; J ao ic tx\'o' N l· 2 Λ'Β-irmdAtO** ι a|> τΒοΙ 5 2 pH-ssnkLuol5J <dfA>mdol-5 ül ï-ulu4r» 4.ivpindik-2-d-kkiuvccíkioüe^d)C!aucl; 2 (50 mbdazof5,i'ajirouKlol 541)BH{l^r)4Kpíridia-34!“mcíAxi>kikioh«xíhetam'>!.; a-C50-ii?dda^oiiO-alMoindokS-ll)-l-((04r)-4-{p?ridin4-il-mefoxôciklotexil}etano!; 1 ( Jr 4r> í u2 an«i o p obm 4 Μηοι»>\* •ujJoLiíniP 2 ΛΜ , r,d,mo ^ i „ fémmel íljeU^noi; 2>r5Hdmidazol5J'ak/oindok54l}44{lr.4r)4.(pira/m-2dkmeCoNi}cîkJohcxà{.icîanok 2H$H-imid»ÄOiS.ka)i2xMml«k5d0.1-M 1γ<4τ» -ΐ~φηίηύά'ηι~54\~ meioxi)cîkïobexH)eiaïK>i; \ uh\4rV4-ic mmno pinUw 24MneU>v VfUohexd* 2 * B kinnda/o; 5 J - a j f/mndol-·$-dKmmok l-((lr/k44-((kkîmkK>-piridî0-3"5Î)mclosi)cikl0hexij}“2-(5i!-?,kVîûaxO;5<l'-ajiÂ:oindo!-5'· iketaook 1- ïf 1 r,4r hU (3-ammo-ptridin- 2-il)rnetoxi)cik!ohexiO-'2-(5H-imidazo{ 5,1 -alizomdokS- iijetaook ..... î-î(] f}4j'V4..((4-anUnO“pinitiid?n“5-H}u'Cioxí}cikiohexíli-2-öE~imida?.0:5 J -yji^oiïidok $b!}euv?K>.l; i -(( 1 r,404-((5 -a nu no· pi ridî n-2-il bnetox ik iklohex 2.>:2-(5i-imMa4k(5:i:l m}moindoi-5-metamak 4 4 ((( 1 f,4rV4-( 1 -hidroxi-2-(5H*imidaK0Í^i»kffMmdöi'5-il)eO Dciklohexil )oxbmcil|· NkN-dSmetü benzamld; 3- (;{i iT,4ri-4-( 1 -l-idroHi'2-(5H· H«teo!5J-aj;zomdok5-lkcül}clklohexd)oxômetil)-NkN-dimedki.^nzanïidi 2- {(((ir,4r}-4d!-hkifc>;i'fk50dpdte4(5J'-a|izo?kdol'-5-iljedl.!4klohex{l.;o?ii}medl!· NnN-dimeiil-benzamid; 4- ü(ilrÿ4f;-4-( 1 -hUlf«xi-2-(5H~«nida^ofS, k#zobBAlbIj^ mdlrmáiiddi _ 34((^ ir^r^khidmxl^^H^aÄxfPil^JÄÄ^i^iükdklohcxil^x.iftveül.sbeRxol·· .szuiíbnamid; 2- (((( 1 r,4r)-4-{ 1 -bidroxi 2-(5H-indd;«o(5 J -a]kosndd-5-ií)etilíc íSdohexdkui jmstif Ibenzd-xzulíbmtmíd; 4-({ {{1 -\4r)-4-{ 1 · hklroxj-245H-indda?.ol''5,1 · altaaéöks* t Ijeíi Ddklohes i l joB }rm4ii )bef vzamkk 3- \Vxl 1 íkó 4·; Módmx: 3-i5)!'5ínkÍ5<'C[5· 1'4käomdoi-5> dktdVtUohexdiOxsbm'üDhuwmid. 2-" : (( í r,40 í ( ! h?drom-° -( B-l-imula»«»} 5.1 ak/o>u»lok5 iikslihdkUihexiOoxijniatdibcnzanud; me« 1-4-(((( ! rv$rH-f I - hidí0.xk2-í 5H-united ! -í*I«oukM-S-îlft’til}eik!ohexU ïoxÎ}nietiUben£0&; tnenl 2-v-v((ïs.4H I -J hanoM 2 »Mi »e«da.\\\î aU«nn>l>\ s. dVkl K\k k>U«i\i ' V\i ;metü 4xT/o;k ; mHil-2-mür.4r^4-»l-hkko\> 2 (5H sondaroiv* I ab^iiuM-b-ilk'ulVikleheNjrioxd'UierüHx'n/äUk 2-{5H-iTOidazo(5* l-a lixoindöl-s^Uk! ~{\ if-4r' -Mth'toxa-Ciklohexn seknsok 1- ilI^'+rVd eU^i-tiUobe^iíViYH-araiiYOpki -öiSi«irsdol-5-i:·ciánok 2- t 5H moda/op J -o jtzoindol· 5- ?Γ>- - U > > .40-4 - s /.o ps. opo si -c s k ;ohe κ h Jeiantu ; I .« !r,4r^4deiMopivpj!4»eîe\ik ikiobe\ah2-(5H~jn5îda?.oi5.i-a|i2oindoi-5-ii)ctanoi; lH<iMr)~HciklôpeniH-meîoxiHîiW1otiexi!V2-(5H-irnidâ3:ô(5a-(i|i7oimtol»5-il)eUiH‘î); 2-jqj i»»üaio{5J-<iÍJA»jHJ*'í 5-dM~^hHp 4 [Uo^i- " ii k>eio\Pakkfed ciánok l ·(( 1 r»4r>-4-(( 1 M-indo!~3-iBoxi íeiklcfei 1)-24 5H4midux<>[ 5, I -a |i ?cn ndol-5-i I)mmn\; 1 aIrfe4--^H-mdfeMno\Pdkfe.d>-2-^ü-piuhfej apromdoi " ihP-nu-k
- 2-CSB- »tnida?o{5 d-a >- l -i4-utem>hidro-2í!-pirán-4 · íI}meto.KÍ.)dkl«hexníe}anoí; 4.(((4..( |.^f(roxk2--(.SH· iíoidazoí?,!-a |izoindoi“5-il.K.'Ul.icikbhexii)oxj.imenl}ben/oi- szuifonamid; 2 pHonhWopJ a|i. obuiol^'-iU l <4 p>\fe-2-b n^OMkikiehexii/eunoI. 2-(5ΗΊη\Ι<^χ<»Ϊ.5,.{-«}ΙζοΙηίΙοΙ*5-Ηΐ-ί'(4-(ΐίάζοΙ"2-1}-ϊ«εϊθχΐ}άΚΐοΗοχ5Ϊ}05ϋηοΙ; 2-<5H“irnidäÄoi5. i--í*}íKom€l<>i“5-ií >-- í -í" i -í .í -imíno--2--AíniÍ-eíí J >piperi<Jin--4-i !>eianoi; 4- (MVïdro\K? à Sl I-imika/oj 5 J ~a)í/omdoi P-fed x\ dem! -piper *«!*«-i -karboxKvmiamicfc 4'( l-hidroxi' 2-(5H-imida7.o| 5, i -a|ixoi«dol-S-iríe»l)-Kdpindin-4-il}pi(ie.ndin·· 1 - karboxlmidaroid; 4 U -hidrtï \ i · ; · i 5 H - i roídazol 5, i -apxobdoí -5-11 jetit) · N-(ietrahidr«-2 B-pirán -4-iDpiperidm-1 -karboximidamíd; Nd4-aao«-teíMí 4~s 1 - kidrox o 2 -p! !-i in feopd -pi An adui - 5 flVtibpipend*n i hn1>o.xa$nid; \ uOK buu b wdtoM ^ (MI-«íhcLvo|n v a" 'omdol > nspk'pipeífe ! k a rix? x a mid; N-(fôre-hm?l}-4-( I -hidroxl^-CSH-imtoofSH-alizoiodol-S-il^ilipiperym-1 · svr-ulîbïiârmd; •Μ -,! 'ddu'\( 2 öH*t'í»d.i/o|M a) w:omdo)-5-il Yui>p ipumhn-t-il)--2-(i2h{|^r fenihetunon: 2~{ ! -(axeudm ! - karbon!! ípÍperidÍTr-44ip2pdr#;i-!-(4-(Hhídrosi -2- (5H-inddaxo!;5,1 - a|i?,oindo!-5-U !£dd}piperii.iin-i-i!)cu»nog; (-cd.k'píoUn ! P 1 dndroxs-2-pB-kskd poj5 1 .dxomduí-5 ü)edhfip«sdm· ! iHeiimon; , P-i,-bfexi 2 pH inu&/<\5.1~ah/omdoI~$<)etibp!pmdm«Í41x242-meîd üa/oi- 5- dK4anon; \ „4 lobod \ kPo<\ -^α-hídoAt 2-PH uoxBropJ ah/onidob? dYíPpqvndrí !-Larbosamid; N-(4-(2 -(4-( ! -hids'oxi-24 5 H-i«dda;o.>|5J -afemdob5-s!}eb npipenom- ! - i! }-2 - ooeiddcänlbaepavpiiltpiamid: ! kauxxxamkk fedifíuor-1 -i4-t ! -hkb-ONi-2 ·< 5Hdmidn«4;5 J -ajkoindo! -5 - d )etU >pípeddin- ! -il jbatan. ! - on. 1 -* -1-í b-hlkO\t-2-(5H-Í5radakol5J -a]koinde!-5-5keid)p5persdín Ml) .'Sp-Yid \4axon H^^·a»«no^'irimídm2-iΓ.p^pcridin-4-^r^^(5H-ïmu·lí^/^»i^.1 -aVoonndcd-5-ilkunnoL I -{l >ammo~pirimk1m-4-il )pipcriUin»4-il)-2^5H-imWu/.o|5,1 -a]izoindoi-5dlk'banol; N-ctkioproph-^-t l-hidroxi-‘4--(M1--modaz0f$J«-ajjzdndol“5-4l.>eiH ipiperidin-1-karbox atmd, 2-okk-propsI -1 (4 < 1 hiclroxs*2-{5H·imklazo}í-ajixoíodo!~5»ft)eiii/ptperKitn~i-d)etnnon; 2-(4( !-hidroxí”^"(5H”irnHÍáí.o[5%l-á]i2:o}n<|0{.5,|^(í.ij|yjkífíhexllidéníace{o«iínl; 4K1“hitJraxk24^H4n}}da2obJ-a}}2ojnclol"5->8.M®>N44-Urif'!uor'‘metîl)Î5azoî-2« ü jptperiösn -1 -kurb< ï xonnd ; 4-í2(4'(i-hidΓo^i’H^H-imida?Λ(5J^|i^Λ>mdo^5'liH*tü}p^îeridin^in-2- oxoetdíhenzamUj, U* tl-MbeM -eoOooM i ajommdoi > Mvunpí^nűin 1-(hO-M-imebb s κ u i fo!.' hí! 0 o i î }e ta π on ; 441 dudrox ,b 7~i 5 H dmidazo(5, L cikiobí'x ü)pipendi o- 1 -karboxamid; 1- (4-¾ 1 -hiílroxí'2"pH“írnída?.o|5J-a}iíoínd<sl>5-iik'linpipeíidin- Ml nem-diïneül-bután·'.1 “00 ; 4-(2-(4--¾ b-hidruxi'2-'Oli--innd*uol'Sj ndäi-onxkil 5-ϊΓ>οηΠρ1ροΓκΙκΉ to ' oxoenObenxcd-szuifonamid; .N-^tó'd-buuI)~**t 2n4»^i-ludrox.t-2 -;5H mnda o \l-e!n’oa\M'5 'l\ul\\pei»»Un 1 d* >--f·ικ<>ίΐ.ΐ1 >beozc4-,ounfooaond; 4-i2--1.4--¾ i“hiiU'o\n2-vbH-iinuKnvi5,1 yjízomdot ö-n'-dd)plpcfidin-i ű) ?-o,x oo i Π ) ben/. oex a v ; ! »^«it-dí^uw-n^idookííM'Olm trn-2»-t^Bomrdayoi:\ i -vdizomd» ,s-5- -.1 k.ímn>·; 2- (5!Hmnk/op, 1 -uló -.-in-;o!-5oh -1--,4 („?,2-mCloor-eoi?dön'teskloU-\!iseíanol, N4vnzU-4-í2-íbdloor 5!’ ηηκΚηη'|5,ΐ ypzoíadobMI s t -IndroxkefdVokiohoxán-knfhoxanbd; 4--(2-(6-flU!.ír-'5(i'lmidn/o(5d-'ali/omdol--5“U)4--hyíOxnetil}''N~ÍonÍ-oikloteán-· karboxfoísid, N <,4 ,2 -í'-dluoí -H muJktzojóJ <.ds.o>mdm ^ dN ] Unbox* e? d ko k mh e \ n * be r a i η 1 d : I -(4-(2-(6-41 in.>r“5!'Idmldazol'5J<í]lzoindob541pldúdroxneűl}cíkiohexil)-'3-.nn:u!--karbandd; N-(4-(2d6-nuoí'--5H-im{dazoí5J-a|izoíndob5 ils- l -hidíOxs-enlmskkthexUM-deed-acetamid; \a$> azok egy gxogy^erexxetdcg elfogadható $om lKogy$'ere.s/.td.s kexznmem. amely .tartalmaz egy az 1-19. igénypontok bárrodytkc szerimi vegyü tetet és egy gyogyszereszetileg elfogadható htgüós/ert, segédanyagot (excspiensu vagy hordozót.
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