HUE028954T2 - Heterociklusos vegyületek és alkalmazásuk - Google Patents

Heterociklusos vegyületek és alkalmazásuk Download PDF

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HUE028954T2
HUE028954T2 HUE08727163A HUE08727163A HUE028954T2 HU E028954 T2 HUE028954 T2 HU E028954T2 HU E08727163 A HUE08727163 A HU E08727163A HU E08727163 A HUE08727163 A HU E08727163A HU E028954 T2 HUE028954 T2 HU E028954T2
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mmol
nrara
chloro
mixture
alkyl
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HUE08727163A
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Yi Chen
Timothy D Cushing
Jason A Duquette
Lopez De Turiso Felix Gonzalez
Xiaolin Hao
Xiao He
Brian Lucas
Lawrence R Mcgee
Andreas Reichelt
Robert M Rzasa
Jennifer Seganish
Youngsook Shin
Dawei Zhang
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Amgen Inc
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Publication of HUE028954T2 publication Critical patent/HUE028954T2/hu

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    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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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    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
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    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (5)

  1. HEi^Kociiassos vegyöleter is âijkalmazAsus: lëabaàÂti %éæyps3stbk 1, Á:k8yfeíkex§ :SKsrks2eís %iáiSÍ«ííÍ vëgyfe::
    vagy hàrë^y.gyôgyàmft%g'©îfesgÂaté mÿi, akd ,X: jelzésé 00^ X; jdentésebí' V jelentéseN(R!l},()vagyS; Z MeÄeCES-agyN:; &amp; értéke 0. %, 2 mg y 3; S! jebatése közvetlen kíáessel vagy ^sg^«^«fe^í-^s!Sö|ó# tÄst, resafeea-fölítea vagy tetíRtkax Ss '&amp;· vagy /-tagú. N, O vagy S kézül választott ö,. 1, 2, 3 vagy 4 atomot taiíaítnasó, dg egynél több O vagy S gtomaknom tartalmazó msjoocik&amp;i«? akti a §y#rü Eqzsiprbéíö széttâtottïiai 0, 1 vagy 2 φχο vagy ioxo csoporttal szabsztít»altak. aWagyíírú 0 vagy l R? saxbs^tteRaseí sstobsztitnáít. és a gyűrű tovább sssabsztitnák % 1, 2 vagy 3 ssobsztónopásd, aiKeîî^k'.«^àsÈÂ'%^fe^i' a kővetkezők kézül választottak: bab, intro, oiano, C^albt, OCs.^«, OC^hsbdkii, és q^kaloaÄ R2 jelentése bab, G.Jukxdkíl ciaao, nitro. -CÍ~0}R<!, -a<>)OR\ -QK>)NR*R*, -Ct-lsR^N^R3, -OR*, -ocb-o)R\ -ocqopÄ -oe^MW$í*:0^ ~SRS, -s<*o)R*, -S(<>)2r, -SbCOxN^R'', •${-0}jN(R;,}C(K)}Rt>: ·ΚΕ;Έ;', ••NíR^K:;{<).íOR\ -ΗίΕ^ό^Ρ^» -NÍR’jC^T'^NR'R*, -NíR*)S{K>hR8s «^slk|er és ÄC^aiyiö^köaäl válasrtc·«; vagy Ra jelentése C,*a!ldl, lepik tesal, teroarsi teroelklos, -^jalkil^ewpasl ^CMÄi)hetaöÄ$, -<3(e|.:3Äii}haioroadi,; aíCi.yiMl^etertícikte -Mqet,jatkil}batomartk Ä|Ct.;;aM13bobtxtciksos, ,(Ç.paMpi«i, -ÖiC,.#;-és -ME3CC:.3áM|&amp;si MbM választott, arndyek «iaé^tfee 0, 1, 2 vagy I szebszíttitcfissel srabsznatsH, antety Cí .«hsloalkik OCiaslkik Br, Cl, P, Î és C:.4aikít közül választott; R3 jelentése H, hé* Ct4MmMl attno, nitro, -CH»R*, -CK>)GR\ -C<-0)M<sRs, -C{»NR*)NR*R*, -OR*, -OCó- 0)R\ -0C(«0)NR*R*, -0€{-0}Ν(Β8)$(=<);·:»Ε;). -OC^Uk0MRÄRÄ, -OC^alRilOR3, -Síi5, -S(0)R* -S(==0),R3, ~SbO}5RR*R\ -S(-Ô3>N{R5)C(-0)RX -S{-0)iN(B.a}C(-0)HRsRs, ÄSR\ -N(R*)C{*0)R*, PirjGHïpE5, -N(RstC(»t.)pRsR5, -ifiP« -N{R*)$H>)jR\ -NtROSC-öi-NR^R3, «IJIÄBn -RR^^itiMiOR3 C;.^!kii, tont!, benztk heteroarik és heterodk- lus közül vámmii, ám » C^lfeR, toMvUtteni# és feetenscifelus tovább szübsztlmált % 3,, 2 3 szubsztituenssel, amely C) .ploslkíl, OC-^aikik Br, Cl, F, 3 cs C^-sikH közöl választót;; R4 jeiontése nimden esetben, egymástól föggetletmL bak;, nitro, eiano, €(..ριΜ1, OCt.$a!kií, ÖC^baioalkil, N'HC')...ia;kjl, N(C;.4aikil)C:,4alktl vagy Ci.pdoalkil; Is jelentése miacfeu essifcesï,; egymástól függetlenül, B, Si; Ci,sÄk €},patoaI3al, vagy Ci^aMl 1, 2 vagy 3 sxubszístoeassol szifesztkuák. amely hale, e;ar,o, OH, OC'i^alkk, CPalkii, Ctohaloalkil, OCj ^alkiS, NH2, Ni;C;.,:alkiL ííP^álktpG^M közöl válássá*««; vagy mindkét RÍ csoport együtt C^sptroaikii csoportot alkot, amely ü, 1, 2 vagy 3· szubszdtuenssel .^abssáeA graety sgabs^ltuoíts tío, dano, OH., OCMaik!k Cj 4alMl, O, oíMoalktl, fX^ksí, WCt ^ÄfÄÄil vMaszfelt; R8 jsleaiése H, halo, 0;i,salki, Cf^haloatkik ciano, nkro, -C{“-'Ö)R\ -k;{ '0)0R\ *C('::0)Nk''Re, C(:-N.R‘> KR8R:\ -S(--Ö)R\ -S{= 0}>RS, -S(-€%NR.8R8, -S(«Oj,N(Ral€0-0)R:i, -StpO^CR^e^OlOR8, -S(-Ô)>N-(RíjCÍ-OlkíR^R* közöl választott; Rí jeleotése M, haló, C(,galkti £f .«haindkii, ®iano, nitro, .Ç{“R)}R8 4d^ö)(lR'·, X(~NRÍ)-· NR8R8, -Sfe€>)E\ ~S(-0}>Rs, -%0}sNÄ ~$ί~0)2Π- (Rs)C;-05BRaRs közRl vákisztoít; Is jblemése !!:, pjtsioalkíl,:B*,Cl, F, 3, ÖR* BR*R*.:C^sMî» IstÄ berni, heteroarlésbeterooíklas közül választott, ahol &amp; C^&amp;lMh Jeni,. bemal, heteroazíl ;ós heteroctkáus tovább szabsztitaált Ö, .1,2 vagy 3 szs^. szíjtucnssd, amely Cj.jhaloaifcii, Bt, CL F, 1 és iCj^alkti közül választott; R® }de»tése H, haló, C;..:haioalkil, cisno, nitro, ·€ό::0)Κ3, -€(=-Ö)OR8XpO)NR3R3, -GÍ-MR^MSÍSÍ, -ÖR", -0C(-'Oííi8, -OCPÖ)NR*R\ -OCC-OlNCriSC-OkR8, -OC^aik'iiÄ* -OC^aíídlOR8, ·«* -SpÖ)!3, -8{-0};;Rs: -8{-Οί>ΝΠ:\ - 8Ρ0);Ν(|13)0(“0}Κ*, -SpOhNCRlÇ^jOR8, -NR8R8,: wM(R*)C(-0)R*. -N(Rä)C(-OlORa, -Nt R")< ’{«Ö)NR*R* PlfR*)€pBR*)NÄ*,. -:B(Is)S:(^0);NRsRa, -BRsCMalkilNR*R*, -NR'O.„alküOR5. Csalid;, fen!;, benzd, fétefeadl és Moro-oikkäs: közöl vál&amp;szíött, ahol a Cj^alkií, -fesltí, henal, hetesxTaril és hetetocikios -tovább szufesztshi&amp;b 0. 1, 2 vagy 3 sanbSgti&amp;eísssol, aáfely haló, Ci.^fcűoaifeil, etano, nitro, -€<=“0)R*, -C(--O)OR!l, Ό “OlNR^Rk C("=NRS)N'RÄR8 >OBÍ, *Ú€F pÖ}R*, -OC(~ö)NRaRa, -OCeOlNtR^iSe-O)^, -OC^alkilNRaRa, -C.X;, .aîkilOR*, -SR*, :*5(«0}R% -•Sí-OgR5, -‘Sí-OjNR^ -S^feNÍR^CHlip15,, -St-OhNtR^a^OpRÍ -S(^N(R^|*<>)NR*K*.· -NR*Re. -NíR3)C(K:0)Ra, ^(I^ef-OIORÍ, -N^í.^-0}NRaRa< -N(R*)C(“NR*)NR*R*, -N(R*)S(-0)2BR*R* -NRAe2,mMORs közöl választott; vagy Rs jelentése tellett, feszbeo íglRett víígy Mhetlet; 5», 6* vagy 7'tagó, M, 0 vagy S közül ydassttotk 1, i, 2., 3 yagÿ 4: &amp;toínot:tartabuazó toottosÉlosos gyűrő, de öem tartaímaz egynél toll Ö vagy 8 atotttoí,: aboí a gyqrü hozzáfethetö szeoatottgai ö, 1; vagy 2 oxo vagy tiaxo csoporttal: szabsztltuáltak, altoía gyürü B,, 3,2,3 Vi^: 4 .S23tis2toáiU fedte, C irkálóé Ildi, ciaao, ttitro, -C(-0)R*, -0(^0)0¾ 'Ct'-OpRlRí, PH4RS}B«, -ÖR8, -OGpÖjR^ -ÖÍ^ÖjNRP*, -OayOp(RnS( <0jRö -«atliÄ <QGmah RtlOR8, -SR8, -S(~Ö)R3, PpO)p?J: -SH1NÄ -SCKljPCRnCC-OlR8, -SH<))P(R8)C(-O)0R:i: PH>)ÄH3)CO<))lN®CR8: prR3, .MV; -MpOCHBOR8, -NfR8)- C(=-NR3)BRSRS, --BtiriSpQiprR8, -'NR3Cj.yükllN:R8R8 és -NR3Q>.öalkilOR3 közül vá lasztott; R! ! jefeatése M vagy C^alkil; Ra jdesíése mirKiea esePsea, egymástól ifeggetlessöl, 11 vagy Rb; és IIs jdestese m&amp;úm «sæfee», egymástól taggedesäl, ímö, beazil vagy Cj^alkii, a IPetl, berrnil és Cj^alkü 0. 1, 2 vagy 3 ssabszíáae®«) sxataftaáK. lefed, és a ss'efesdifeseas halo, -CjuAílj Cs.jb&amp;baMI» ΌΟί,.^ΙΙίϋ, 'MH;;, ^KCmsSî», ·Μ<€í,4aBíií}€:í.«aikP kézál választolt 2, ,4z Ϊ. Igétypoat szentfei kö vetkézé szerkezeti képteíü vegyülsl;
  2. 3. Az L Sgenypoßt szerinti, következő szerkezeti kép-tető vegyetek-
  3. 4. Az Î, tgéííypöMszeíisti következő szetiesett képiető vegyőtef:
  4. 5, M L igénypont szednss ve-gyölet, afeoli R! jelentése F, Cl vagy Sr; és a értéke 0. &amp;M i. igénypont SKemti yegyßtet, ahoi R! jelentése 0 vagy Í ïi! szubsruitueassdsmMzätoMtfeniks* a feni Ci, I, 2 vagy 3 s^fcsatíteesssel tovább halo» nitro, ciano, €;. ^alkil, €€:.4&amp;ΓκΙ1, OC^iMalklÄCiÄ, NÎC:; .4si:kii>C.;.4aIksJ: és CMhstoafkM fösüi Mksxto&amp;
  5. 7, Az L %éftÿge8t vrerMt vegyik*, ahokR1 jekstése kärveüea Mfesset vagy okígánea ksrmzí&amp;l kaja ösoíoiib tóiietb réxaben-tfôiîvfVvagy teliteken >.. 6- vagy 7-tagä, N', D vagy S közül választott, i, 2,3 vagy 4 sttnset ísnateszái». de egysei s§bb 0 vagyis atontot nen; iastaltnazó rsgiissaiMöses gyitrik iW a gysM tmsfek kékésre álló szénatomjai 0, I vagy 3 am vagy iloxo essforUal sxabsKtifeÄk, fel a gyikf § vagy l io SKsbsziibíbösSd SíbbsKtiíuált, ás a gytrü tovább »ánbsatiátáli ë.,·. 1, 2: vagy 3 sanbsxktaénsseij aníejy egÿniasîôt feggíklenül a kbvstk&amp;Ä lbzä! válásaiéit: halo,. nitre, tism, C^sSM, ÖQ4ÄM, MCi4â}ki)C<.#ïkil «s CiJbdo&amp;Mi'y g. As: 1. igénypont szerinti, kővetkező szerkezek képiéül vegyüist
    vagy a> b) ás <?) bánts«!yíká»ek Mrœdy gybgyászatilsg slfögü$»® sfeä· 9 Ag ;gányx»i5t sserinö vegyük* szabad bázis femfejsban' 'ϋϊι Aa 1*9. igénypontok. feánaelyike szAKki vegyűietet és gyágydszablag: «IpgMbató Éigííésszert vagy hordozói tartaknaxó gyógyászati készítmény. II , Az ÏA. igetîypsbôk bfeielyiké szeséái vegyül# rhemaisldid artîihssî, spoiixMiiis aækylapiæM** osieoarbitm, p^oáékm |>S2&amp;#Ä gyulladásos betegségek és sstósa»* ^betegségeik, gyulladási bélb«®gseg«^ gyulfeddsos î«!Ç8Âi«s^» gyulladásos vagy tefc8>$ l^ylélyág-íesdsIfertöSsegek, bár panaszok gy#laáásos elemekkel kÄkus gyulladásos MI#xáok, autoimrnuö betegségek, ssisziémás îyji órylhfiOiáfesós ISLE):, myaatííesia grakts,: yeyb?aiotd aidrítisz, akut disszidált ebcspkateisyslitis, Mopá&amp;ás troïisbo(Ok>jïeb||$ p«â|îarif, sskteréiss: multiplex, Stógiési-sziudréíua és aetoimmüb IäoIÄss süéttiía, allergiás állapotok# tűlébAkeííység keMésám idrl#» alkslraazásfá, II, Az W. }0iÿpœêï!k bármelyike szeripi vegyuleí p l 10§ aMvI^ssalMzvgfkg«, apái iiggŐ vágy ab-hoz kapcsolódé Ä'Äsi^s%i?attoaS.ais:^masÄ^> Í3. M 1-9. igéaypffiíííok bámtelyifce szermis vegyulet vaslagbélrák, glioi#s#áma, vziáomeiééHs Mm-:#53ga, bsgaíseetolám fék, ííklórák, msktftóssta, vesese|í-ksrdsófSa, palxstmrjgy-kiim, imíöma, iimfopro·· ']%$mÉ$·. w^élíesess^elj Ötsejtss tüdSrék, pikkelyes sejtes ISdirák, gbbi^gj epíískak, prosx!»tik, peíe%^k·· yâk. pébayakrák, leukémia, akatdiékíM |öiké»kas myelödysplpiás sgmdrdtsrav sfildopmliletstik ttiegbetegedé-sífkj krónikus myelolá: leukémia, Τ#ρ|ί«&amp; akiit )te|pblssxk>s leakémia, B- sejtes stet bmíobIaá#ós leukémia, oesxvHodgkm lipîiiSi&amp;a, B-seiliesÄÄ^didÄPä '^atpr#;:k««»í^élTO történd .alkalmsaim
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Families Citing this family (128)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
WO2007114926A2 (en) 2006-04-04 2007-10-11 The Regents Of The University Of California Kinase antagonists
RS53151B (sr) * 2007-03-23 2014-06-30 Amgen Inc. 3-supstituisani derivati hinolina ili hinoksalina i njihova upotreba kao inhibitora fosfatidilinozitol 3-kinaze (pi3k)
EA017389B1 (ru) * 2007-03-23 2012-12-28 Амген Инк. Гетероциклические соединения и их применение
GB2467670B (en) 2007-10-04 2012-08-01 Intellikine Inc Chemical entities and therapeutic uses thereof
WO2009081105A2 (en) 2007-12-21 2009-07-02 Ucb Pharma S.A. Quinoxaline and quinoline derivatives as kinase inhibitors
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
US8637542B2 (en) 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
JP5599783B2 (ja) 2008-05-30 2014-10-01 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
JP5788316B2 (ja) 2008-07-08 2015-09-30 インテリカイン， エルエルシー キナーゼインヒビターおよび使用方法
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
WO2010045542A2 (en) 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
GB0819593D0 (en) 2008-10-24 2008-12-03 Ucb Pharma Sa Therapeutic agents
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
GB0821693D0 (en) * 2008-11-27 2008-12-31 Ucb Pharma Sa Therapeutic agents
CA2752150A1 (en) * 2009-02-11 2010-08-19 Reaction Biology Corp. Selective kinase inhibitors
WO2010092340A1 (en) 2009-02-13 2010-08-19 Ucb Pharma S.A. Fused pyridine and pyrazine derivatives as kinase inhibitors
US8785628B2 (en) 2009-03-06 2014-07-22 Ucb Pharma, S.A. Triazine derivatives as kinase inhibitors
TW201103943A (en) 2009-04-27 2011-02-01 Shionogi & Co Urea derivative having pi3k inhibitory activity
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
GB0908957D0 (en) * 2009-05-22 2009-07-01 Ucb Pharma Sa Therapeutic agents
EA201270013A1 (ru) 2009-06-25 2012-06-29 Амген Инк. Гетероциклические соединения и их применение
CN104945420A (zh) 2009-06-29 2015-09-30 因塞特公司 作为pi3k抑制剂的嘧啶酮类
TW201111385A (en) * 2009-08-27 2011-04-01 Biocryst Pharm Inc Heterocyclic compounds as janus kinase inhibitors
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
WO2011058112A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Fused bicyclic pyrazole derivatives as kinase inhibitors
EP2499144B1 (en) 2009-11-12 2013-10-23 UCB Pharma, S.A. Quinoline and quinoxaline derivatives as kinase inhibitors
ES2520345T3 (es) 2009-11-12 2014-11-11 Ucb Pharma, S.A. Derivados de quinolina y quinoxalina en calidad de inhibidores de quinasa
WO2011058109A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Fused bicyclic pyrrole and imidazole derivatives as kinase inhibitors
WO2011058111A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Aminopurine derivatives as kinase inhibitors
ES2534096T3 (es) 2009-11-12 2015-04-17 Ucb Pharma, S.A. Derivados de piridina y pirazina bicíclicos condensados como inhibidores de quinasa
US8633313B2 (en) 2009-12-18 2014-01-21 Amgen Inc. Heterocyclic compounds and their uses
US8680108B2 (en) * 2009-12-18 2014-03-25 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
WO2011093365A1 (ja) * 2010-01-27 2011-08-04 協和発酵キリン株式会社 含窒素複素環化合物
AR081823A1 (es) 2010-04-14 2012-10-24 Incyte Corp DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd
CA2799579A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
US20130079342A1 (en) * 2010-06-30 2013-03-28 Paul John Dransfield Heterocyclic compounds and their uses
JP2013530238A (ja) * 2010-07-01 2013-07-25 アムジエン・インコーポレーテツド Ｐｉ３ｋ活性の阻害剤としての複素環化合物及びその使用
EP2588468B1 (en) * 2010-07-01 2014-03-26 Amgen Inc. Heterocyclic compounds and their use as inhibitors of pi3k activity
JP2013533884A (ja) 2010-07-02 2013-08-29 アムジエン・インコーポレーテツド Ｐｉ３ｋ活性阻害剤としての複素環化合物およびそれらの使用
AR082799A1 (es) * 2010-09-08 2013-01-09 Ucb Pharma Sa Derivados de quinolina y quinoxalina como inhibidores de quinasa
EP2616442B8 (en) * 2010-09-14 2018-10-17 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
EP2635565A1 (en) * 2010-11-04 2013-09-11 Amgen Inc. 5 -cyano-4, 6 -diaminopyrimidine or 6 -aminopurine derivatives as pi3k- delta inhibitors
JP2013545749A (ja) * 2010-11-10 2013-12-26 インフィニティー ファーマシューティカルズ， インコーポレイテッド 複素環化合物及びその使用
EP2640715A1 (en) * 2010-11-17 2013-09-25 Amgen Inc. Quinoline derivatives as pik3 inhibitors
EP2655374B1 (en) 2010-12-20 2019-10-23 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2012135009A1 (en) 2011-03-25 2012-10-04 Incyte Corporation Pyrimidine-4,6-diamine derivatives as pi3k inhibitors
MX2014000648A (es) 2011-07-19 2014-09-25 Infinity Pharmaceuticals Inc Compuestos heterociclicos y sus usos.
WO2013012915A1 (en) 2011-07-19 2013-01-24 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
KR20140075693A (ko) 2011-08-29 2014-06-19 인피니티 파마슈티칼스, 인코포레이티드 헤테로사이클릭 화합물 및 그의 용도
KR102507287B1 (ko) 2011-09-02 2023-03-07 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
MX370814B (es) 2011-09-02 2020-01-08 Univ California Pirazolo[3,4-d]pirimidinas sustituidas y usos de las mismas.
MX352672B (es) 2011-09-27 2017-12-04 Amgen Inc Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer.
JP2014528451A (ja) * 2011-10-04 2014-10-27 ギリアード カリストガ エルエルシー Ｐｉ３ｋの新規キノキサリン阻害剤
DK2790705T3 (en) 2011-12-15 2018-03-12 Novartis Ag Use of inhibitors of the activity or function of PI3K
WO2013090725A1 (en) * 2011-12-15 2013-06-20 Philadelphia Health & Education Corporation NOVEL PI3K p110 INHIBITORS AND METHODS OF USE THEREOF
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
MX2015003874A (es) 2012-09-26 2015-12-16 Univ California Modulacion de ire1.
EP2914296B2 (en) 2012-11-01 2021-09-29 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
CN105073738B (zh) * 2013-01-31 2018-01-05 沃泰克斯药物股份有限公司 作为钠通道调节剂的喹啉及喹喔啉酰胺类
US20160002185A1 (en) 2013-02-19 2016-01-07 Amgen Inc. Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer
AU2014236812B2 (en) 2013-03-14 2018-03-01 Amgen Inc. Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
CN105358530A (zh) 2013-06-10 2016-02-24 美国安进公司 制备mdm2抑制剂的方法及其结晶形式
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX2021012208A (es) 2013-10-04 2023-01-19 Infinity Pharmaceuticals Inc Compuestos heterocíclicos y usos de los mismos.
HRP20220718T1 (hr) 2013-11-11 2022-09-30 Amgen Inc. Kombinacijska terapija uključujući inhibitor mdm2 i jedan ili više dodatnih farmaceutski aktivnih sredstava za liječenje raka
EA201691169A1 (ru) 2013-12-05 2016-09-30 Асерта Фарма Б.В. Терапевтическая комбинация ингибитора pi3k и ингибитора btk
NZ724368A (en) 2014-03-19 2023-07-28 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
WO2015160975A2 (en) 2014-04-16 2015-10-22 Infinity Pharmaceuticals, Inc. Combination therapies
AR100289A1 (es) 2014-05-06 2016-09-21 Amgen Inc Formas de un inhibidor de pi3k
CN104086551B (zh) * 2014-06-06 2016-09-21 人福医药集团股份公司 化合物及其制备方法和用途
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
MX2017000208A (es) 2014-07-04 2017-05-01 Lupin Ltd Derivados de quinolizinona como inhibidores de pi3k.
EP2974729A1 (en) 2014-07-17 2016-01-20 Abivax Quinoline derivatives for use in the treatment of inflammatory diseases
US20170239351A1 (en) 2014-08-11 2017-08-24 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, a PD-1 Inhibitor, and/or a PD-L1 Inhibitor
TW201618773A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、及／或ｃｄｋ４／６抑制劑的治療組合物
MA40596B1 (fr) 2014-08-11 2021-12-31 Acerta Pharma Bv Combinaisons thérapeutiques d'un inhibiteur de btk et d'un inhibiteur de bcl-2
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN107427506A (zh) * 2014-10-14 2017-12-01 拉霍拉敏感及免疫学研究所 低分子量蛋白酪氨酸磷酸酶的抑制剂及其用途
ES2928714T3 (es) * 2015-01-16 2022-11-22 Massachusetts Gen Hospital Compuestos para mejorar el empalme del ARNm
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
SI3831833T1 (sl) 2015-02-27 2023-03-31 Incyte Holdings Corporation Postopki za pripravo inhibitorja PI3K
CN106008479B (zh) * 2015-03-06 2020-01-10 南京圣和药业股份有限公司 作为磷脂酰肌醇3-激酶δ抑制剂的取代嘧啶类化合物及其应用
GB201506786D0 (en) * 2015-04-21 2015-06-03 Ucb Biopharma Sprl Therapeutic use
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
EP4585268A3 (en) 2015-09-14 2025-10-15 Twelve Therapeutics, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
CN108472298B (zh) 2015-11-24 2021-04-20 深圳阿拉丁医疗科技有限公司 选择性激酶抑制剂
CN112250665A (zh) * 2016-03-05 2021-01-22 杭州征祥医药有限公司 作为磷脂酰肌醇3-激酶抑制剂的喹啉类似物
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
RU2754507C2 (ru) 2016-06-24 2021-09-02 Инфинити Фармасьютикалз, Инк. Комбинированная терапия
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
CN108069899B (zh) * 2016-11-18 2021-01-08 中国科学院大连化学物理研究所 一种制备2,3-取代喹啉类衍生物的方法
WO2018204176A1 (en) 2017-05-01 2018-11-08 Sanford Burnham Prebys Medical Discovery Institute Inhibitors of low molecular weight protein tyrosine phosphatase (lmptp) and uses thereof
EA201992781A1 (ru) 2017-05-22 2020-04-01 Эмджен Инк. Ингибиторы g12c kras и способы их применения
MA50077A (fr) 2017-09-08 2020-07-15 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
US10442799B1 (en) 2018-04-07 2019-10-15 Fuqiang Ruan Heterocyclic compounds and uses thereof
WO2019213516A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3101323A1 (en) 2018-06-01 2019-12-05 Incyte Corporation Dosing regimen for the treatment of pi3k related disorders
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
ES3060664T3 (en) 2018-06-12 2026-03-27 Amgen Inc Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer
IL315550A (en) 2018-08-31 2024-11-01 Amgen Inc A process for preparing an MDM2 inhibitor
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
EP3669873A1 (en) 2018-12-20 2020-06-24 Abivax Quinoline derivatives for use ine the traeatment of inflammation diseases
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
NZ782284A (en) 2019-05-21 2024-11-29 Amgen Inc Solid state forms
CN112574176B (zh) * 2019-09-27 2024-03-15 隆泰申医药科技(南京)有限公司 一种杂芳基类化合物及其应用
WO2021076655A1 (en) 2019-10-15 2021-04-22 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
WO2021126816A1 (en) 2019-12-16 2021-06-24 Amgen Inc. Dosing regimen of a kras g12c inhibitor
CN114276326B (zh) * 2021-03-09 2022-11-11 南京征祥医药有限公司 喹啉化合物的盐及制备方法和应用
CN113218936B (zh) * 2021-06-07 2021-09-10 江苏欣诺科催化剂有限公司 锇酸钾的纯度检测方法
WO2023016477A1 (en) * 2021-08-11 2023-02-16 Taizhou Eoc Pharma Co., Ltd. A cyclin-dependent kinase inhibitor
US12168662B1 (en) 2023-12-15 2024-12-17 King Faisal University Pyrido[4′,3′:4,5]pyrrolo[2,3-c][2,7]naphthyridines compounds as CK2 inhibitors

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US6043062A (en) 1995-02-17 2000-03-28 The Regents Of The University Of California Constitutively active phosphatidylinositol 3-kinase and uses thereof
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
US5822910A (en) 1997-10-02 1998-10-20 Shewmake; I. W. Fishing line tensioning device
EP1257546A1 (en) * 2000-02-17 2002-11-20 Amgen Inc. Kinase inhibitors
WO2005067546A2 (en) * 2004-01-13 2005-07-28 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
WO2005117909A2 (en) * 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
JP5033119B2 (ja) 2005-04-25 2012-09-26 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング キナーゼ阻害剤としての新規アザ複素環化合物
US20090082349A1 (en) 2006-03-02 2009-03-26 Dashyant Dhanak Thiazolones for use as pi3 kinase inhibitors
EP1993537A4 (en) 2006-03-02 2010-05-19 Glaxosmithkline Llc THIAZOLONES AS INHIBITORS OF P13-KINASES
WO2008097976A1 (en) 2007-02-09 2008-08-14 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
EA017389B1 (ru) * 2007-03-23 2012-12-28 Амген Инк. Гетероциклические соединения и их применение
JP5564947B2 (ja) 2007-09-26 2014-08-06 アステラス製薬株式会社 キノロン誘導体
WO2009081105A2 (en) * 2007-12-21 2009-07-02 Ucb Pharma S.A. Quinoxaline and quinoline derivatives as kinase inhibitors
US8703778B2 (en) * 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
GB0819593D0 (en) * 2008-10-24 2008-12-03 Ucb Pharma Sa Therapeutic agents
GB0821693D0 (en) * 2008-11-27 2008-12-31 Ucb Pharma Sa Therapeutic agents
WO2010092340A1 (en) 2009-02-13 2010-08-19 Ucb Pharma S.A. Fused pyridine and pyrazine derivatives as kinase inhibitors
EP2427195B1 (en) * 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
EA201270013A1 (ru) * 2009-06-25 2012-06-29 Амген Инк. Гетероциклические соединения и их применение
ES2534096T3 (es) 2009-11-12 2015-04-17 Ucb Pharma, S.A. Derivados de piridina y pirazina bicíclicos condensados como inhibidores de quinasa
US8633313B2 (en) 2009-12-18 2014-01-21 Amgen Inc. Heterocyclic compounds and their uses

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