HUE029515T2 - FGF-receptor-agonista (FGFR-agonista) dimer vegyületek, eljárás elõállításukra és terápiás alkalmazásuk - Google Patents

FGF-receptor-agonista (FGFR-agonista) dimer vegyületek, eljárás elõállításukra és terápiás alkalmazásuk Download PDF

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HUE029515T2
HUE029515T2 HUE12824734A HUE12824734A HUE029515T2 HU E029515 T2 HUE029515 T2 HU E029515T2 HU E12824734 A HUE12824734 A HU E12824734A HU E12824734 A HUE12824734 A HU E12824734A HU E029515 T2 HUE029515 T2 HU E029515T2
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phenyl
pyrazolo
treatment
álás
carbamoyl
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HUE12824734A
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Marie-Line Clary-Ceccato
Nathalie Guillo
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Sanofi Sa
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61P19/00—Drugs for skeletal disorders
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Claims (3)

  1. FiíF-Rkt.'ErrOR-ACÏONISTÂ. (SR.;?·8-MiOmWA) ölM kl SR VK<ÎYD1,FTFIC, FU ÁHÁS ëlôâllItAsukra és τκηΛγιΛ» alkalmazásuk Saabadsiml IgènypôaUsk
    1. Vegyölstek, amelyek álísSáfiös képlet«: ahol Ml <?¥ M > H'Umestf, am* h km à/m^ v:g\ .'lsm\ îyggrtkmü! M mswmer egv-so: <*> i tek·»· rés«· kihöcsopo», amely M1-*t &amp; MM ky^k^4^^ödí:«sssi;pfe«im^,fc^mammm ogv^g megOs# vSUi kÖU'íks^V \Í < '-:, ‘i V kCpk^fU k
    ahol *-;&amp;::.mo}8*K«s<?:-ÍS:.!-a»:4.küîôesôpyn közötti kötés-helyét. jeiölka&amp;ö œMi «s :M„> ömMKeregysőg fimsit-spifeèrsek kötési holy* aa R vagy R? szabaztimem-egysk*« öohw^od&amp;sl, - R jelentése hidrogénatom (amely esetbe» M L· è% M kötési helve as<H#a MyeÄtk et) vagy 0- >s|H* kepksù export, :s Rs jelentőse hldrogéna-omsiagjvsgj^nssjáasú(Crt5 talk! iesogast, R; COHH? «μ|^$μ^«Φνι a* I. é*M:Ässih«§e : C0NH* Kepleré csoport. .? (F kleaiese -COJt.< esöp^ &amp;r ipp<;8töse^ä<l^>#Äm vagvisgyeoes:Íáöök:pp®íjaSli?!«söpört, -- X jeréraése isaiogéítatofii. aasdy a iövetkezök kö^k^fesÄöti: ílstar, felér es btoktsysnp r: L- jelentése a kővetkező PH<y:«^^£Ébk Mfme.íy*&amp;é*: #öl
    * ♦ telöli síi az atomot, amely összeköti '*> **í* VAihsmíhönsgsii·: - « értéke !!·<>, bármely egös-z^zánk Kt^N VSéS sS'-U Sogs ϊ’Λ ísvu vőkoréb ΚΜο'ί X \ö lv>'» Ö ilv'i $ν·Α2· k igénypont ssaifits vegy'älekk, av/al baztA Va£v s&amp;vvat vagy bázissal alkotott adsliciös sb ktnH&amp;jâban. 3. A? előző igonypontok bátmelyike szerinti vogvbkbdú azzsl jellemezve« hogy jéietttésp evopott. ahoi R» jeiettfé.ve hypagéotaotn. b&amp;ziv· vagy saw«] vagy ttáztssol ttlkotottoddkio!. sa íormágava?· ï V Jv.\m a wiâüî b«, "ex s * ,,< y, ολ a-.a si pllmme, bogs \ 5 mh>v. 1 '! kî^ bat-o x«c\ savvA \âgv l\t<· vy*i a \".ot* ad 1 > 0 'tó ab a ígé«y^b&amp;#Mrb|g{y|k® xiertati vegyietek, ÂÎ jelli'BHSCve, bag£' - R Mentése -COMB* csoport, aboi * jelöli azt a helyek ahoi L k&amp;ptsoíödtk először M; moaotoer «vy-séggei, másodszor Mj tnotR>mer egységgel, R <eb sK'v1 tu 'rog«netoi" s< ux >«ous gt'-x ,'aiktl ν-ι"υ>ι, \ t". sag> «v<s, vau» \><k- R «, Rototkpddksbs .vo forttxajabatu ·$, Az 1Λ tgettypowok bármelyike szcdnîl vegyUletek, azasti jellemezve, hogy R mm vagy gara -helyzetben r&amp;», bázis, vagy saw&amp;l vagy bázissá! alkotott aödkáóx sê formájába».': 'b à/ ' a ^'i\po >«k «.0 >'tx Μ vo'Pt! xcvvSLkk. oxswti fdiemovve, hogy. - R jelentése húhogesatottt, • K > jelentése -COMM* csoport, aboi * jelöl* azt tt helyet, ab«} L kapcsolódik először is Mä monomer ogv ségget. máSink/o;" is M_. moootner egységgel, bázis, vagy «savval vagy bázissal alkotott addldós sô formája- bas,; .Ri à» 1-3, igénypontok bármelyike szerinti vogyületek·» aszal jellemezve*: hogy- « értéke 3 vagy 4, bá:zi.y vag;·, savval vagy bázissal alkotott adtkeiès m formájában % Az ékkő igénypontok bármelyike szerint* vegv&amp;ict, azzal jeMeemzve, hegy a következő vegyítetek .RôglîfyfeætoRÿ 1.. vpgyítiet: iU‘-1était*I.2dijllskéjoylpropán- ki·<1ΐί1κρζΐ50ΐηοΙΐΡ·>^οΙί'ί/%Ιί«ζν$}ν»ρ,4ό^ρ1ΐ imn-4,ivdlífijj-bkzf ö- tlnotbetkottsav:}' 2, vegyidet: >-Ι·Ή{ ib-iedb-foatvObd-fltioriMSl}\vMíXíidk--pfoizotóp.'ik!josís<itji'4éikjk'Oso'4v'?Jtt··!!·;·· o»a 4 ae «P» nta» ον I ti xttbtf'kn) ' kni >' g monoi < *'ρ- ««ο d ! Booth' ívovíx :k vegyidet ' 5-f4-( { lő-(ó-í3'koiní\t*4-fi ttot fedi)· l-fenU- 1 Af-ptrazoÍo[3.4·éj|>irídi»-4*i1|*16-oscö-3,ő.9, I2*tetik: nsoxsa-]5ovtóbvxídee-iol|k«tb!inosl)-i4eo|i-l//'p!iTsztiio;3.;kbjplrkltíí"ő'ik-2'5laíírben.zoesav'.: » «,,>dk‘t « x i λ 4-íluof ni s-mn '- < ' , \ , ' - >| 'ΐ!» n ti, »v> 4 e a ' -pentaoza-1 b-st/unonade» -i-ií s karitatrioli.tO'lbutk I /ópoasoioi k-kólptráiin-b··; ;l-2· i1«t«b®j«»t:sáv;·· S. vegyfilei iH-t-t i~ I-{d-t k-kât bozt^-fiuorfentl s à - fettil· i //"pitazoká 3.4 ·0]ρα·ΐ£ϋη·4-»Ιΐ-^ I ·*Ρ5«*Κ?,Η>> i SJo» • -phtaoMt-2b>azsiitenkt)S> i *ti ) kartosot})· 3-íentl'i //-pife{2oteC3y4'^N!ä»s^'itlJ*3^l8örti®8»^^i. 6. vegyüld: Μ 4 AorMoToAkM-Hy ; v(Mj44:aAtadMi-4M '-ksibviî;-4-nuorft;n!âï»lf/'pifâ2<sl«niv4»6jiimijin'· " 4 , <vî> h ->v.'~í ' H* «rovs Ma s. - * .'<e MM ι \OK-d \ ! S ί/*Ήν?οΐοξ\4 bjp'rdf** >s h ' ' Hnosbenzoesav, %, vt-gyOka: J,.V. IeîànM ,2 Mii!bb;4^>i«Ä'2, ! .'|p««i*a» ' "> MM ]''!->.« O il.K<!X'»ZOVs.O. \ 8. vt-gvipd' 5-<4-4;arlxsms>M:'- H 4 (î MM-HAdbaftnOMoi V-korbosiMMluoridMs-1&amp;ypà&amp;2QÎo{'3.4-l>jptf iám* M-MkoMMl 5-ök<í"4,'’,lil-ír-»Kib·14-azapísMai«.· \ 41 iksífeasooti jieoil \ I//*ptra®i>So|3,4“è]p’H(5iîî-6--iH-2-• IM őrben zoesav; fv wolltet· 1J jeun« I J^HIb^josîçtàn-2,l-däffeamsmoSbea^Mvl*dhl(4>Kaït^ÂI-||#pr#4^|I4i: blptridm-? .tVdMyj j biâ^ê4korb«fiîyesav>: 50. 1 îjrtKM a/ Î-*5 o.\n> peolok IxMvd', sM s.v>îf'<' vegyítsetek zlo.iîht.mM, a*wb, tanísinxízza segakjbb #^ÂW«savts«>îK»««i tartalmazó legalább .égy n»«m>«?er reagáltatfciát ílaN*L-NHíj kápléSi ipykïàpssai. aktiválás ütés*. 11, öyógysz«;·. «zaai gellmsz.Yt?, bogy do-ilox;/ ,*./ 1¾ sgeaypofikM bármelyike sztmnb veg\ Mou·.; vagy tiyen vegyit lel gyógyássatilag eiios.MísSSós.sV'M vagy 5 cp-om ,MMd6s sóját
  2. 12. Az MA igénypontok bárnsehsk? \/emos végűdéi gyógyszerként történő alkalmazásra. U. Gyógyászati iMaxHîaé^yâ^ijÂOîOiïve, 0«gy tartaîmaMM 1-0. igény|Kíni«k feántsdyike saints u-r.voïeoo s mi un v, eUMi g> 'gs.ru.V'ugv.í.'t A-sö vSsát.. -iumMm, Ou.MMleg .tinim egy yvPgsáv.i Mag elfogadható vegé<.ó«s> egot.
  3. 14. Az MA ;gettyp<mMk hártneiyike sxsMsM segyöiet r;Gf--retej«vr #tÈlàÉÂjg#ji0. bltegségek kezelésére szánt gyégpisrele 15. A® iAIblife5ÍOnM8 bármelyike szÄti vsgyöíét a következők bánoelyskéMs® íOrisnl zMlmMzm, sziviszkémi» követkexméítyeínek kezdése, íu artériák szűkítésével vagy1 elzáródásával oss/eftiggő betegségek vagy ,a terms* ku-ebue. ongou pednn UvMú<u Ooofolxuoemn, d>hter»»\ Uzek-sO, tteíM/kierod- kezesbe angroplasztika utáni vagy égdmsrtefeklömis aíaOifOsMéiMgM gátira szolgáló keg^iés* gyAgyífö kogeisy, ízöM--regenerációt célzó Ssli ipiöbktsztok tOiaiiÄ szolgáló kezdés. szærkopènià kezelése. a záróizom-•simaizmok ihstkeio vesztésének kezelése. íKicicapciá és krOnikns föjdak»« k«asiéae, iH-rilönás nearopáiia Ä:e·· U"sfe, blomestairsége« imnyáisn»ng>’-graft toléle^enek javítására ::gMgásM kvgeífc cíík«>rbv5agak5>«n; kol^gtorin·· v:oí·! csökkíotóséfv. szolgáló kezelés, elhízást v^kkontó kezdes. g^aíl «jraeresedésénak ás grail iúléiésánok javítására szolgáló kezelés, .reüisa-degínífaMO, retinitis pigmesttsvs kezelése. oszteoaTUiri-M kezg|gspj pre·-ekiatnitszla kezdése, vaszknláris iáziók g? akat replratorlkus áisnessz szirtüróma kezelése. esonteéUelÉ szolgáié kozdév, szörtíMzö védelniére szolgáló kezelés szabctíyozása.
HUE12824734A 2011-12-28 2012-12-26 FGF-receptor-agonista (FGFR-agonista) dimer vegyületek, eljárás elõállításukra és terápiás alkalmazásuk HUE029515T2 (hu)

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FR1162485A FR2985257B1 (fr) 2011-12-28 2011-12-28 Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique

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US (1) US9034898B2 (hu)
EP (1) EP2797917B1 (hu)
JP (1) JP6049756B2 (hu)
KR (1) KR20140105578A (hu)
CN (1) CN104136434B (hu)
AR (1) AR089452A1 (hu)
AU (1) AU2012360095B2 (hu)
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WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
LT3176170T (lt) 2012-06-13 2019-04-25 Incyte Holdings Corporation Pakeisti tricikliniai junginiai, kaip fgfr inhibitoriai
CN109627239B (zh) * 2012-07-11 2021-10-12 缆图药品公司 成纤维细胞生长因子受体的抑制剂
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
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