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HUE033448T2 - Janus kináz inhibitor N-cianometilamidok - Google Patents

Janus kináz inhibitor N-cianometilamidok Download PDF

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Publication number
HUE033448T2
HUE033448T2 HUE14793899A HUE14793899A HUE033448T2 HU E033448 T2 HUE033448 T2 HU E033448T2 HU E14793899 A HUE14793899 A HU E14793899A HU E14793899 A HUE14793899 A HU E14793899A HU E033448 T2 HUE033448 T2 HU E033448T2
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Hungary
Prior art keywords
phenyl
amino
benzamide
pyrimidin
piperidin
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HUE14793899A
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English (en)
Inventor
Ranjit C Desai
Jigar Desai
Pankaj Patel
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Cadila Healthcare Ltd
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Publication of HUE033448T2 publication Critical patent/HUE033448T2/hu

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Claims (10)

  1. Janus kínáz inhibitor N - e i ano m e it 1 ami d o k Szabadalmi igénypontok 1. (I):
    A szerkezetű vegyüîet vagy gyógyászati lag elfogadható sója, ahol X valamennyi jelenléte eseten egymástól függetlenül X vagy CH közül, választott; X valamennyi jelenléte esetén egymástól függetlenül N vagy CE közül választott; n 0 és 1 közül választott, A egymástól függetlenül hidrogénatom, halogénatom, (1*4 szénatomos)- alki L OS, CN, CONtR.:};?, Ö(l~4 szénatomosj-alkilesöpört közül választott; a B gyűrű az alábbi:
    gyűrürendszerek közűi választóit, melyek mindegyike szubsztituált lehet.
  2. 2. Az i. igénypont szeműi vegy öletek. ahoi a B gyűrű szubsztituensei, amennyiben jelen vannak. egymástól függetlenül H, OH, CN, NHj, halogénatom, oxo, OOb, CF3, (1-6 szénato* mos)~aikil, 0(1*6 szé;natomos)-aikík (CH2)í*$ö(1*6 szénatomos}-a!kil, 0-(€l:b}o.,*0(1*6 szén* atomos)-«! ki 1, C(0)NH(1~6 szénatomos)-aikiI, NHC{())(1-6 szénatomos)-alkil, S(0)o.;(l-6 szénatomos)~alk ü, (CH2)^N(Rt)?, (CH2)^NHCí=0)0Rj, (CThh-cNI ICOOjR,, CíOlOR;, Ci—OjRi, NHR\, (CB^VAKCHjliMÁrj, {(.11;)0. N H{ C112k-4Ar5, ((.Ή,Ο^Λΐ''., (()lh)íi.4C(0)-{CH2)i>^Afh (C 1.(2)0-4(.-(=-0) 0(CH2)o-4Ari, (CH2)(mC(~Ü)NR *(CH2)^.4Ar * csö~ portok közül választottak. E Az 1. vagy 2. igénypont szerinti vegyület, ahol R* valamennyi jelenléte esetén egymástól függetlenül hidrogénatom, (1*4 szénátomos)~aikiL (1*4 szénatomos)-halogénalkii.
  3. (3-7 szénatomos j-cikloalkilcsopttfiok közül választott,
  4. 4. A 2, igénypont szerinti vegyület, ahol valamennyi Art jelentése egymástól függőtlenül szubsztituálatían vagy szubsztituált aril vagy egy, két, bárom vagy négy szidszfithenf| tártak mázó heterociklusos gyűrű közül választott.
  5. 5. A 4. igénypont szerinti vegyületek, ahol az Ar* csoporton álló szubsztíluensek egymástól függetlenül OH, CN, NH?, halogénatom, OCF;, CF3, (1 -6 szénatomos)-alkiK 0(1-6 szénatomos fal kik ((Hb)-.-60(1-6 szénatomos) -alkil, 0-(CHj)o-jÖ(l-6szénatomos)-alkíl, C(Ö)NHC( 1-6 szénatomos )-alk.ü, NHC(Ö)( 1 -6 szénatomos)~alki 1, S(0.)oo( > -6 szénatomos)-alkil, (CH3)?.6N(Ri)2, (CH2)uNHC(!!!0)0R|, (CH2)i-6NHC(=Q)Rt, CCO)ORS vagy -C(~0)Rj, CH2(CH2)o-4C{-0)NHRi csoportok közül választottak.
  6. 6. Az alábbiak közül választott 1. igénypont szerinti vegyület' N-(cianoinetí])"4-(2'({4«(4-(2*oxopirro!ídín'i»il)piperídin-l-il)fenn}araino)-píriínidin-4- ibbenzamid; N~(ciaiiometil)-4'-(2-((4~(4-'{l,l-dioxidoizotiaiïoIid?n“2“.il)piperklin*]~i])fenil)amîno)piriîuk.!in- 4-ij)benzamki; N-(cÍanomeUl)-4-'(2~((4-{4-morí'blinopiperidin''l-'iI)fenil)amjno)pírímidm-4-il}benz.anűcl;. 4-(2-í(4-(4-(lH-l,2>44nazobb-iI)pípOTdin-í-i:i)fenii)amino)pírímÍdin'4-ií)”N-(ciánométíl)benzamid ; 4-(2'<(4-i4~(lí:bpirazo}TÍ4l)píperidín44})íbmi)amino)pirímidin-4~il}”N~ (ciánomén bbenzam ki; 4-(2-((4-( [l,3?“bipînx>Hdin}-îMI}fenii)aTnino)pirimidin-4~U)“N*(cianümetH )-benzamid; N-(cÍanonieíi 1)-4-(2-((4-(4-( 1 (1 *diox|dotetmhidrO“2H>fciopiraní4>*il)piper«jzín-1 -iI)tenil)amino)pirimidin-4-i ! íben/amid; N-(eianometii )-4-(2-( (4-(4-(fim»i-2-íl)piperidin-l-il)feiiii)aniíno)pmraidia-4-il}benzamid; N-(cianometilj-4-(2-( (4-(4-( IJ-diöxidotetrahidrotíofen-S-ibpiperazin-l-ii }ícnil }amino}pirinndín~4~íI}benzamid; N-(eianom:etiI)-4-(2-((4~(4-(2,5-dioxopi.iTolidín-l-ü)piperidin-1 -il)fenil)« amino)piriniidin-4-íijbenzamid; \'-(cianomehb-4-(2-((444-{t?ofen-2-ü)piperidin-i«ibreni!}amino) pírimidín*4-ií)benzamid; N~(cíanometii}-4-(2-((4-{4-(2~oxooxazolídin-3-íl)piperidin-Í-ii)fenil)-amino)píriiTíidirí-4» ibbenzamid; N-(ciano.roetil )-4~(2-((4-(4~(tetrahidrofuran--2-1 bpiperkiin-1 -ií)feníi)amino j-pirim idin-4-il}benzamid; N-'(cíaftometib~4“(2~((4-(4-(5~meti!fiH'an-2-il)piperidin-I-il)feíiíi)amino.}pirimidin-4- ibbenzamid; N~(cianomelil)-4-(2-((4-(4-(íetrahidro~2Id-piran-4-il}piperazin'!-il)fefűba.núno)-pirimídin-4- ibbenzamid; N4cianometil)-4~(2-(í4-(4-(5-metiitetixdndK>iuran-2-ibpip®ridin-l-ibfeHÍl}amino)-pirímsdin- 4~il)benzan;iid' 4-(2-((4-(4-(6~oxa-3-axabkikíoj;3 J, .1 |hepUm-3-il)pipcridin- ! -iÍ)fen5!}í«nino)-pirimidin--4-í! .)-N-(ciánomét il)-benzamid; N-(eÍanometil)-4--(2-((4-(4“(2-oxoimidfKo!idin-l'-il)piperidi.n-l-il)feníí)amino)-piriniidin-4~ i{)benzamíd; 4-(2“((4--(4-(l>3í4-oxadiazoI-2-i!}piperídin-1-íl.)fenií)anúno) pirimidin-4-ib-N-(cimiometíl)benzamid* 4~(2-((4-(4~(2H~i;2,3--triazo]"24l)piperidir^l~íl}íeníI)aniino)pirimidin-4-il)-N“ (ciánoméi! nbeœamid; 4-(2-((4-(4-( i H-i J3~iriazoi~] - ü )p i per i d i n -1 - il)fcnillamiíio)pirimi cl i n-4 - i Π-N-(e iam> me~ tiijbenzamíd: N~ícianonietil)-4-(2-({4~(4-(5-oxo-]H-13z*4riazo!~4($H)-ii)piperidin~l-ií)teml)- aminü)pírimidín-4-.U)bcnzamid; N-(cianomot.il)-4-í2~((4-(4-{5-oxo-4f5-'díhidfo~l H~ 1,2,4-triazol-1 -il)ptperidin- 1 -Í1 )feni 1 }amino)pírimklm-4-il)benzanúd ; 4-(2-((4-(4-(1 -oxa-8~azaspiroj4,Sjdekan~8-il)píperidin”i-ií)feml}amino)pirimidi.n-4'i!)-N-> (cianomeíi 1 ibenzam id; N~(cianomcti ! )-4-(2-(( 4-(4-(5-metii-l 3?4-öxadifizoi~2-inp!poridm·'I -ilifenii)-ami no)pirirn i di n-4~i I ) benzamid; N-icianometil )-4-(2 -((4-(4-(5-metif~ 1,3.4-tiadiazol-2-il }pi peridin-1 -i Dlcníl }-araino)pirirnidín-4~:d)benzamid; N-(cia:noínetii)~4-(2-((4~(4-(íetrahidro-21i~(K4|dioxinoí2,3-c'Spirrobő(3il)-il}piperidín~l-i 1 ) feni ! ) am ino)pir im idin-4-i bbenzam id ; N-(eianometil)“4-(2-((4-(4-{2-oxo-l-oxa-8-azaspiro[4,5|dekan-8-ii)piperidin-l-ii)íeníi)aniino)pírimidm-4-il)beiizamid:; N-(cíanonmnil)-4~(2-((4-(4~(5-oxö-4>5“dihÍdro-l,3,4-oxadiazo]~2-il)piperidin-i- iÍ)feníl)amino)pi.rímidin-4-il)benzamid' K!'*(eianom.e{UM''(2,i!'((4-(4Hí4-eiklopi!opiÍ“5-metH'4H-l J,4-tnazoi-3-i!)piperidin-l-il)fenií)Mríno)pirimidín-4-íi)benzamid; ΝΚεΐ8πο.ηΐϋΐι1)'4»(2-((4·'(4·-(5~ιη«{οχί-^3'4“θχ»(ΪΪ82(θ!*24ί)ρ.ίρβίκ1ΐη-Ϊ>ΐφ·δ;ηΗ)''· a m ino)pi rím idm -4-d }benzarn í d ; 4-(2-((4-(4-( L4-dioxi(pan-6-il}piperaziiirl-iI)iemi)am:ino)pirinndin~4-.i!)-N-(ciarionietil) henzamid; N«(cíanometil>4-(2>*((4-(4-(4,$*clthidrO“lH4midaKOl-2~U)piperazin*'.l «U )feail> ami no)pi ri m i di n-4-ί I ) beaza mid ; N -( c tanom éti I)-4~f 2~({ 4-(4 ~(4?5-0ί hí dro~ 1Ϊ î-i m idaÄol-2-ΊΙ >pi peri cl í íi -1 -i l)fen íl )-ami no)pirimi din-4-il)henzanmi; N-(ciaHomt4i{)-4-(2-((4-(3-(tetîaliidro-2îl-f L4|dioxi.maf'2J-cjpirrol-6{3i:í)-íi)pirrolidin-l·-í Illeni barnino Jpírim idi n-4-ü)benza.nríd : N-(eíaftometil)~4-í2~((4~(4~í 5-meti 1 -1 >3,4-oxad iazol-2-i bpiperazin- Î -ii)íenil> amí nojpirirö ídiÉ*4»Í í )feenzamid; N-{cia)K?metií}~4-(2~((4-(4^3,4-dil'adro>;ipírroíkHn~l-ií)pipüríd.in~l~i])íeníl)araino}-p5rÍ!Tíidin~ 441)benzamkl; 4-(2~({4-(4'-{8"í>Ka~3'-azabiciklo[3.2.I }ocian~3~íÍ)píperidín~l -il)fení})amino)- pirímkün-4-ii}-N~(cianometi!)benzamid; 4424(4«(4-(ő-aceíik3,6«diazahiciklo(34 J]heρtan-341)pipefidin-14!)fenil)~amino)pirím^din-44 i)- N -í c i anom et i l)benzam id ; N-(cianoraetíÍ)«4^{5*metíb2-((4-(4rraoríbiínopiperidin--14í)fenil)aniiiio)pífimidin-4'· ii)benzami<l; N-(eianometi í)~4-(5-meti í-2-((4 - ( 4-(2 ~ o xo p i rro i í di n ~ 14 í)piperkün-l 41) feni i pamínojpirúníditn 441)benzamid; 442^((4^(4~(l^oxa-8”azaspiro[4.5idekan-'S~íl}piperidin-]~íi.)feml)aniino)~5-'meti!pirimidín-4- iÍ)^N-(cianomeUi)benzamid;. N»(cianometil)-4*‘(5«.rnetib24(4*{4’'(5«inaetik L3,4OxadiazoÍ-2“U}piperidin-Í -fl}fenii)aínhK>)pirimidíív-4-íl)benz.a,wíd; N-(cíanomt4iI}4-(5-iíiior-2>'((4'44'mofik4inopiperidin-l4i)fenil)aniíno)pífímidin->4- iljbenxannd; 4-(5-kÍór-2-{(4-(4~morrolínopiperidín~i”il)fenil)aiívino)pírií«ídin'-44Í}~N- icianoineblfbenzamid:; N-(eianometii}>4-(5~fluor*2'{(4"(4-{2-oxopinOtidin>l“U)piperidin"i"il)fenii)-amino}pirjmidin“ 44l)benzamid; 4-(54dór«2-((4*(4~(2“OxopKToUdin> I 4 i)piperidin~ ! 4l)feni! }auTtino)pí rimîdin-4-nj>N,> (ci anom etíl)benzamid; 4-(24(4~(4~(6~oxa-3-azabktklo(3. í. \ ]heptan>3~U)ptperidifl-l 41)foni1)ammo>5* metiÍpÍnmidin-44!)~N-{eianometü)benzamid; 4~(2-((4-(4-(6-oxa»3«azabicik}o(3.i. 1 ]hepian-3-il }piperidi«-I 4 ! }tbmI}atn!no)-5~fluofpifimidir5-4 - i 1 )-N- (ciánoméit l)benzamid ; 442*((4-(4-(6-oxa-3~azabicíkioj'3,l.i ]hep?an-34Í)píperidin44i)fenii)amirio)-54dórpirímídm-44 !)-N-( c í anom éti 1 )benzan í íd ; N-(cíanometil)-4-(5-meti!-2-({4“(4-(íetrahidro-2H-(L4]dioxino[253-c]pirroi"6(3H)·' ii)piperidin-141}fenii}andno)pirimidin-4”il)benzainid; N'{cia3iCHnetii)-4"(5“iluor~2~((4444tetrahsdro-'2I-b}’ 14]díoxíno|2.3*c]pirrol-6(3HV i))piperidm~i41}fenil)amino}pinmidin-441)benzamid; 4”($-klór-2-((4-(4-(tetrahídro-2í L4 i .4jdio.Kinof2,3~e]piffol-6(3I-l)41)pipendin-l -íÍ)ílnnl)amino}pirhnidm"441}'N-4cia3K>meüÍ)benzamid; N-(cíanoraetil)-4-(5-i1uor~2'-((4»(4-(5^oHít.ii-I3i4"DxadiazoI-2~íl)píptóridin-l- ii)fenil)aíTÚívo)pirivn\dín-4~U}benzamíd'. 4«(5-klór-2-((4-(4-( 5«metil-l,3,4~oxadjazol-2-iÍ)piperidin”i-ü)feml)am.uK>}-pirimidin~441)~N-(c i anom éti ! )be nzam i d ; N-(C:ianoTriet.il)~4-(5~metiK2~({4-(4-(5-'iíietibl3i4r05iadía/.ob2dí)pípcraíí;ÍB^Í^ i ijfenil )am.ino}pírimidi n-4-i 1 )benzam id: N~(cianomeii!}-4"(5-fluoi'“24(4-{4-(5-iTietii-'K3,4~oxadiazoi~2-äl}piperazin-l- íl}fertií}öSTÚTK3)piriniídm~4~íl}benzamid: 4-(5-kiór*24(4<445-metÍl-l,?K4HXxadiazoi-2~ii)pipera/Jn-4 41)feíil)amino)~p:irímidin-4--ii)-N-(ciánomét! Dbenzamid : 4-(2-((4-(4-(3-tia-6~azabicík]o[3> 1.1 Jheptan*64l)piperidm» 1 -ii)fenil}amíno}~pírim?din-4~H}-N-' (ciánomét! i)beirz.amid: 4-{2~((444~(3“tiö'4>-azabiciklo[34 J|hepían-6-ii)piperidin-l”ii)feni!}amjno)~5-'ír!eíÍlpiriniidíi}-44ί)4Ν-(οί3ηοπΊ^ΗΐΙ}Β6ηζ3ΐηίί1; 4-(2-í (4-(4-( 3“da-6-azabíciklö[3.l d]hcptaiv-64i}piperidía-l4í).femi.)annno)-5-i']uorpíríaddi% 4ril)~N-(cianomedi)benzamid; 4-(2-((4~(4-(3~tia-6~azabieik}o[3,L1 jhepta«-6~íi)piperidín-l-il)fenil)amÍ3io)-5-kk>rpiriirddia^ 4-i 1) -N-{e ianometi i)benzaro i d.
  7. 7. Az előző igénypontok bármelyike szerinti vegy öletek közül választott alábbi vegyületek: N-(cianometil)-4-(2~{(4-{4~(2~oxopin'olidin-l-il)piperidiTi-1~ii)fenii)amino)"piriniidir!-4- il)benzamíd; N!-('eianometii)-4-(2-((4-(4-(lJ'dioxidoi/otíazi.'lidin-2-ü}piperidin~l -ti)- fenil)ammo) p í r im í d i n-4 ~H ) be nzamid ; N-(c)anometil)~4-{2-{{4-(4-mot1blinopiperidin~ I-íDlenil )am ino)pmmidin-4-il)benzamíd; 4-(2-((4-(4-(lΗ-1.,2,4-triazol-l -il ipiperidin-i ~il)íéni 1 }amino) pírimidin-4-ií)~N-(ciariometíí)benzamid; 4-(2-(4-((4-( l H-pirazo.!~l -.11 }pl peri din-1 ~i 1> feni l)amino)pirimidin-4-il )-N-(cianometil)benzamid; 4-(2-((4-([‘î!r3,-bîpîrroîidin|-lî-U)fenii)iU'nmo)pirimidm~4-ii)~'N-(cianometii)- benzamid; N-(eianometil)-4-(2-({4~(4-í I, ! -dioxídotetrahtdro-2H -1iopíran-4-í 1 )piperuzin-1 -i 1} ten i 1 tat π i no )ptri mi di n-4-i l)benzam id ; N~(eíanometil)~4-(2-((4-í 4-t íuran-2-il }piperidin4~il Jiénil )amino)ptrtmitlitt-4-il }benzamid; N-(cianoroeiil )-4-(2-( {4-(4-(1,1 -dioxidotetmhidtx>{iofeß-3ril)ptperazin~ 1 -i lifers i l)ami no ) pi ri m tdín-4-i 1) benzamid ; NH'd8nome{jl)-4~(2-((4-(4-(2i3-dioxöpirroIidin-]-ii)piperidin-i-il)ieniI)amino}~pirimidin-4- il)benzarnid; N-(cianotneíiÍ)-4-(2"((4'(4-(tiofeíJ-2-n)piperidin-l*il)fcni!)amino) pi ri m id i n-4 -11 ) benzam id : N-(cíano-m6til)“4-(2“((4-(4-(2-o.'cooxazolidin-3-il)piperidin-l”ií)feníI) amino )- pirimi di n-4-lllbenzamid; N“(cíanom<ííi!)-4“(2'((4-{4-(ic{röhidrojíuran-2-il)píperídm-i-iÍ)ieníl.)amÍno}”pinmidin“4- il)benzarn.id; N~(ciaxKmmtí].)-4~(2-{(4-(4~(5-meníiuran-2-ii)pipcrídin-1-il)íe«il)amíno)pírímídin~4~ 31)benzm«id; N'-(cianometíl)-4-(2-((4-(4-(tetrabidro-2íi-píran-4-il)pipcrazin~l*il)ft*nil)amino)-pirhnidin-4- iljbenzamid; N-(cianometii}“4-(2'((4-(4-{5-metíitetrahidroíUran-2-ii)pipendin-l-il)rerHÍ)-amino)pirimidin- 4-il)benzamid; 4-(2 ~((4-{4~(6-oxa-3-azabiciklo[ 3.1.1 jheptaTK3-iI)piperidin-14I)fenil)amino)-pirimidin-4-il)-N ~( cb.mom etil )benzam id ; N-(eianometd)-4-(2-((4-(4~(2-oxoimida2olidin-'l”il}pipeHdiiel -ii)}eTvil)amino)-pirtmidin-4-il)benzamid; 4-(2-((4-(4-( 1 * 3,4-ox adi azol -241 )p i per i d ί η - i. -U)fenil)amino) pirimi din-4-ii)-N~ (cianomeiil)benzamid; 4-(2-((4-( 4~(2H-L2.3-triazol-2-il)piperidm-1 ~il)feni! )am ino )pi rim id in-4 - i !)-N ~ t eianometiijhenzamid; 4-(2-((4-(4-( lJ:l~i;2,3-triaKol-i-iI)pipiaidin-i-ri)forir)amiru.^irimidm-4-iJ)-N-(cianomeii 1 ihenxamid ; N-(ciaxxoinetti)-4~(2-((4~(445-oxo-lII-L2,44riazol-4(Sid)-il)piperidire1-il.)fenil) amino) pírímidin-4-ií)benzamid; N-(eianonietil)-4-(2-((4~(4-(5-oxu~4f 5-díhidro-1 H-1,2,4 -tri azo 1-1- i 1 )pi peridin-1 -i I ) fen í I )ami no )pi ri mid i n -4-i l)hers zam i d ; 4-(2-((4-(4-( I -oxa-8-azaspíro[4,5]dekan-8-il)piperidin-1 -il)fenil)anitno)~pirimidin-4-ii )-N-( c : arsons eti 1 }benzam id: N-( ciánom etil )-4-(2 -( ( 4-( 4-(5-meti I- Î ,3s4-oxadiazoI-2-H)pÍperidin-Í-H)fenil}-a m i no )phimi di n-4 ~i 1 ) be nza m I d ; N-(cianomeül)«4-(2>((4-(4-(5-metií~] ,34Μΐ3ΐ.ϋαζοΪ”2-ϋ}ρ{ροπ<ϋη·Ί”ϋ)Γοηί1}··αΐΏίηο)ρΙι·ΐπΰίϋη-4~íl)benzaraid; N-(cianometi l)-4-(2-((4-(4-(tetïahidro-2H-[ 1 ^|dioxmoí2,3~c]pirroí~6{3H)~}l)piperidin-> 1 -i í )íenü)am inö)pirímid m-4~íi)benzam i d ; N4ciano.metíl)-4a24(444~(2H)xo-í-oxa--8~azaspiro[4.5]dekaH"8"il}piperídín-i-íijfeni i )am ino)pif imMin-4»il)benzamid ; ·ΝΚα3ΐι.οιηβΐί1>4-(2-((4^(4~(5·'θχο«·4<5*^Ι^ΐώΌ“ί,3»4*οχ8^Ϊ32οΙ*24Ι)ρίρβτΐά*η«·Ϊ·“· i 1 ) fen i I )am i no )pi inni di n-4-i í }benzam í d ; 'N-(cianofneUI)-4-(2-((4-<'4-(4'CiWopropii~5-metn"'4H-K2,4-iriaïrol-?)-il)piperidin-l- ií}tenií)aHvmo)pirimkiíí\-4^i]}beu£amid; N-(cianomctU)-4”f 2«((4*(4-(5-metoxj» 1^4-oxadiazo!~2~ü)píperidm-1 -? l)fenü>· ammo)pinnúdln~4-il)benzamki; 4-{ 2-((4-(4-( l(4-dioxepan-6-il)pipera?in-J-i})feni])amino}pirimidin-4-il)-N-(cianometii) benzarnid; Ν'-í cianomeül )-4-(2-((4-(4-(4,5 ~d i h kirn -1 H-imidazol-2-il )piperazin-1 ~í) )feni !)-ara i no )pí rimidin-4 -II ) henzam íd ; N''(ciauoraetil)-4-(2-((4-(4-(4,5'dihklrO'lH4midazo!-2-!l)pipcridin-l-ii)fenil)- ainino)pirimidin-4-i!)benzaTrfid: N-(cíanomeíi!)-4~(2-((4-(3~((aírahidro-2H-[l,4)dioxino[2,3-c|pínOl~6(3H)~Il)pirfo!idin-l" d)fenii)airnjK>)pirimídiív-4~i])henzamid; N'(cianoractii)-4-(2"((4-(4-(5-nraíi!~L3,4-oxadiírao!-2-il')píperaziivi'-il)fenií)“ amino)piríraidín-4-!Í)benzaraid; N~(cianomedl)”4~(2-((4-(4-(354-dibidroxipirroiidin~i~ü)pipefidin-l-'ii)fen.ü'hamiiK})pirimidira 4~i])benzamid; 4-{2-'((4-(4-(8"Oxa~3-a^abiciklo[ 3,2. l]ocían-341 jpiperlüi«- 1-il )íenil)amino) -pirimidin~4“ií)-N-(danoraeíi!)benzaraid; 4-(2-((4-f4-(6~Aceti!-34kdiazabicikio|34djhepían~2)-ií)piperidin~l~íl)íenii}-amino)pk>iínidin- 4-íl)-N'(cíanonietií)benza!rad( N~(c:íai»3iíraül)-4-(5-mcníl-2-((4-(4-raorfolínopiperídifs-l-'il)fenii)araii'io)piríittídin-4- ii)benzanbd; N-(cjarto«ieti!)'44S-«jetil-2-((4-(4-(2-oxopi.rro}.idin-i-iU)pipendin«14} )í2röil}-ann.no)pjriraidin-4-il)benzainid; 4-|2~((4"(4*|l><-nxa-S-azaspiro|4.5]dekaii-84i)píperidm' i -il)feiií)amjno)'-5~metilpínraidinr4·* i í)-N-(cianomet.í l)benzaraid: N»(cianometi!)-4-(5~metil-2H(4-{4"(5-metii-í ^^-oxadiaz.oi^-iOpiperidin-l-iiJfenilJaminoJpirimidin-d-il)^^ N“(cÍaímmetíl)-4-(5-nuor-2-((4-{4~morfotínopi peridin-l-ii)téníl)ammo )pirimidin-4-il)benzanűd; 4-{S”klór«2~í(4-(4~rnorfolinöpiperídín~14l)fenií)amíno)pirimidin-4~Íl)-N- (eianometil)benzamid,
  8. 8. Gyógyászati készítmény, mely terápiásán hatékony mennyiségű előző igénypontok bármelyike szerinti vegyüietef és adott esetben egy vagy több gyógyászati lag elfogadható hordozóanyagot., hígílőszert vagy kötőanyagot- tártálm az.
  9. 9. Az előző igénypontok bármelyike szerinti vegyidet gyulladásos állapotok, autoimmun betegségek, proliferativ betegségek, allergia és transzplantálum kilökődés, porc mozgás romlásával, veleszületett porcelváhozásokkal összefüggő betegségek és/vagy 1L6 vagy interferonok túltermelésével - aboi a JAK kínáznak patoílziológiás funkciója van - összefüggő betegségek kezelésében történő alkalmazásra.
  10. 10. Gyulladásos állapotok, autoimmun betegségek, proliferativ betegségek, allergia és transzplantálum kilökődés, porc mozgás romlásával, veleszületett porcelváhozásokkal összefüggő betegségek és/vagy 11,6 vagy interferonok túltermelésévei összefüggő betegségek kezelésére alkalmas gyógyászati készítmény, mely az l. igénypont szerinti vegyületeket megfelelő kötőanyagokkal együtt tartalmazza. Π. 4;
    képlető intermedier, ahoi B, Z, X, n és A az 1, igénypontban megadott.
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