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HRP20151386T1 - Fenil aminopirimidinski spojevi i njihova primjena - Google Patents

Fenil aminopirimidinski spojevi i njihova primjena Download PDF

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Publication number
HRP20151386T1
HRP20151386T1 HRP20151386TT HRP20151386T HRP20151386T1 HR P20151386 T1 HRP20151386 T1 HR P20151386T1 HR P20151386T T HRP20151386T T HR P20151386TT HR P20151386 T HRP20151386 T HR P20151386T HR P20151386 T1 HRP20151386 T1 HR P20151386T1
Authority
HR
Croatia
Prior art keywords
pyrimidin
cyanomethyl
benzamide
morpholinophenylamino
phenylamino
Prior art date
Application number
HRP20151386TT
Other languages
English (en)
Inventor
Christopher John Burns
Andrew Craig Donohue
John Thomas Feutrill
Thao Lien Thi Nguyen
Andrew Frederick Wilks
Jun Zeng
Original Assignee
Ym Biosciences Australia Pty Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ym Biosciences Australia Pty Ltd filed Critical Ym Biosciences Australia Pty Ltd
Publication of HRP20151386T1 publication Critical patent/HRP20151386T1/hr

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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D295/02Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
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Claims (18)

1. Spoj formule Ib [image] u kome je Z je nezavisno odabrano od N i CH; R1 je nezavisno odabran od H, halogena, OH, CONHR2, CON(R2)2, CF3, R2OR2, CN, morfolino, tiomorfolinila, tiomorfolino-1,1-dioksida, supstituiranog ili nesupstituiranog piperidinila, supstituiranog ili nesupstituiranog piperazinila, imidazolila, supstituiranog ili nesupstituiranog pirolidinila i C1-4alkilena u kome su atomi ugljika po izboru zamijenjeni sa NRY i/ili O supstituiranim sa morfolinom, tiomorfolinilom, tiomorfolino-1, 1-dioksidom, supstituiranim ili nesupstituiranim piperidinilom, supstituiranim ili nesupstituiranim piperazinilom, imidazolilom ili supstituiranim ili nesupstituiranim pirolidinilom; R2 je supstituiran ili nesupstituiran sa C1-4alkil; RY je H ili supstituiran ili nesupstituiran C1-4alkil; R8 je RXCN; RX je supstituiran ili nesupstituiran C1-4alkilen u kome do 2 atoma ugljika mogu biti po izboru zamijenjena sa CO, NS2R, NRY, CONRY, SOL, SO2 ili O; R11 je H ili C1-4alkil, U kome su supstituti odabrani iz grupe koja se sastoji od C1-4 alkil, C3-6 cikloalkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkilaril, aril, heterociklil, halo, haloaril, haloheterociklil, hidroksi, C1-4 alkoksi, ariloksi, karboksi, amino, C1-6alkilacil, arilacil, heterociklilacil, acilamino, aciloksi, C1-6alkilsulfenil, arilsulfonil i ciano; ili njegov enantiomer, njegov prolijek ili njegova farmaceutski prihvatljiva sol, gdje su prolijekovi odabrani od: • spojevi u kojima su aminokiselinski ostatak, ili polipeptidni lanac od dva ili više aminokiselinskih ostataka kovalentno vezani peptidnom vezom za slobodnu amino, hidroksi ili karboksilnu grupu spomenutog spojevi formule Ib; • spojevi u kojima su karbonat, karbamat, amid ili alkil estar kovalentno vezani za slobodnu amino, amido, hidroksi grupu ili grupu karboksilne kiseline spomenutog spojevi formule Ib preko karbonilnog ugljika bočnog lanca prolijeka; i • spojevi u kojima je slobodni hidroksil spomenutog spojevi formule Ib pridružen preko veze fosfor-kisik za fosfatni derivat spojevi (kao što je kiselina, sol ili kiselina, ili estar).
2. Spoj prema patentnom zahtjevu 1 gdje R1 je morfolino.
3. Spoj prema patentnom zahtjevu 1 ili patentnom zahtjevu 2 gdje Z je CH.
4. Spoj prema patentnom zahtjevu 1 odabrano od: N-(cianometil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; N-(2-cianopropan-2-il)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(3-morfolinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-tiomorfblinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-jodofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)metansulfonamida; N-(cianometil)-4-(2-(4-(morfolinometil)fenilamino)pirimidin-4-il)benzamida; N-(2-(cianometilamino)-2-oksoetil)-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-(4-hidroksipiperidin-1-il)fenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-(4-metilpiperazin-1-il)fenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-(3-hidroksipiperidin-1-il)fenilamino)-5-metilpirimidin-4-il)benzamida; 4-(2-(4-(1-benzilpiperidin-4-iloksi)fenilamino)pirimidin-4-il)-N-(cianometil)benzamida; N-(cianometil)-4-(2-(6-morfolinopiridin-3-ilamino)pirimidin-4-il)benzamida; 4-(2-(4-(4-acetilpiperazin-1-il)fenilamino)pirimidin-4-il)-N-(cianometil)benzamida; N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)-N-(prop-2-inil)metansulfonamid tozilata; N-(cianometil)-4-(2-(4-(4-hidroksipiperidin-1-il)fenilamino)-5-metilpirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-(piperidin-4-iloksi)fenilamino)pirimidin-4-il)benzamida; 5-(4-(4-(cianometilkarbamoil)fenil)pirimidin-2-ilamino)-N,N-dimetil-2-morfolinobenzamida; N-terc-butil-5-(4-(4-(cianometilkarbamoil)fenil) pirimidin-2-ilamino)-2-morfolinobenzamida; 5-(4-(4-(cianometilkarbamoil)fenil)pirimidin-2-ilamino)-N-etil-2-morfolinobenzamida; N-(cianometil)-4-(2-(3-fluoro-4-morfolinofenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-(4-morfolino-3-(trifluorometil)fenilamino)pirimidin-4-il)benzamida; 5-(4-(4-(N-(cianometil)metilsulfonamido)fenil)pirimidin-2-ilamino)-N-(2-(dimetilamino)etil)-2-morfolinobenzamida; N-(cianometil)-N-(4-(2-(4-morfolino-3-(trifluorometil)fenilamino)pirimidin-4-il)fenil)metansulfonamida; N-(cianometil)-4-(2-(3-(propoksimetil)fenilamino)pirimidin-4-il)benzamida; 4-(2-(3-(aliloksimetil)-4-morfolinofenilamino)pirimidin-4-il)-N-(cianometil)benzamida; N-(cianometil)-4-(2-(4-(1-etilpiperidin-4-iloksi)fenilamino)pirimidin-4-il)benzamida; N-(cianometil)-N-(4-(2-(3-fluoro-4-morfolinofenilamino)pirimidin-4-il)fenil)metansulfonamida; N-(4-(2-(3-ciano-4-morfolinofenilamino)pirimidin-4-il)fenil)-N-(cianometil)metansulfonamida; 2-ciano-N-(4-(2-(4-morfolinofenilamino)pirimidin-4-il)fenil)acetamida; N-(cianometil)-4-(2-(4-(2-morfolinoetoksi)fenilamino)pirimidin-4-il)benzamida; N-(cianometil)-4-(2-{[4-(1,1-diokso-1λ6,4-tiomorpholin-4-il)fenil]amino}pirimidin-4-il)benzamida; N-(cianometil)-4-[2-({4-[(1,1-diokso-1λ6,4-tiomorfolin-4-il)metil]fenil}amino)pirimidin-4-il]benzamida; N-(cianometil)-N-metil-4-(2-(4-morfolinofenilamino)pirimidin-4-il)benzamida; i N-(cianometil)-4-(5-metil-2-(4-morfolinofenilamino)pirimidin-4-il)benzamida. i njihove farmaceutsko prihvatljive soli.
5. Spoj prema patentnom zahtjevu 1 koje je [image] ili njegova farmaceutski prihvatljiva sol.
6. Spoj prema zahtjevu 5 koje je hidrohloridna sol slijedećeg spojevi [image]
7. Spoj prema patentnom zahtjevu 1 koje je [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7, gdje je spoj kinazni inhibitor.
9. Spoj prema patentnom zahtjevu 8, prema kome je kinazni inhibitor JAK2 inhibitor.
10. Proces za pripremu spojevi formule Ib prema patentnom zahtjevu 1, koji sadrži korak vezivanja spojevi formule II [image] gdje je R11 definiran u patentnom zahtjevu 1 i X je klor koji je zatim konvertiran u jod prije vezivanja sa spojevima koja su označena formulama III i IV. [image] pri čemu su Z, R1 i R8 definirani kao što je u patentnom zahtjevu 1; i M je B ili metal.
11. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9, i farmaceutski prihvatljivi nosač.
12. Implant koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9, ili farmaceutska kompozicija prema patentnom zahtjevu 11 za primjenu u metodi liječenja bolesti povezanih sa kinazom, gdje spomenuta metoda uključuje davanje efektivne količine spomenutog spoja ili farmaceutske kompozicije subjektu kod koga postoji takva potreba.
14. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 13, gdje je bolest povezana sa kinazom imunološka ili inflamatorna bolest, bolest hiperproliferacije, virusno oboljenje, bolest metabolizma, ili vaskularno oboljenje.
15. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 14, gdje su imunološko ili inflamatorno oboljenje presađeni organ.
16. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 14, gdje je hiperproliferativno oboljenje rak ili mijeloproliferativna bolest.
17. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 16 gdje je hiperproliferativna bolest mijeloproliferativna bolest odabrana iz grupe koja se sastoji od slijedećih bolesti: policitemija vera (PV), primarna mijelofibroza, trombocitemija, esencijalna trombocitemija (ET), agnoneična mijeloidna metaplazija (AMM), idiopatska mijelofibroza (IMF), hronična mijeloidna leukemija (CML), sistemska mastocistoza (SM), hronična neutrofilna leukemija (CNL), mijelodisplazni sindrom (MDS) i sistemska bolest masnih ćelija (SMCD).
18. Spoj ili farmaceutska kompozicija za primjenu kako je traženo u patentnom zahtjevu 17, gdje je mijeloproliferativna bolest odabrana iz grupe koju čine policitemija vera (PV), primarna mijelofibroza, trombocitemija, i esencijalna trombocitemija (ET).
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Families Citing this family (219)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104030990B (zh) * 2007-03-12 2017-01-04 Ym生物科学澳大利亚私人有限公司 苯基氨基嘧啶化合物及其用途
WO2009032861A1 (en) * 2007-09-04 2009-03-12 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
PT2265607T (pt) 2008-02-15 2017-03-08 Rigel Pharmaceuticals Inc Compostos de pirimidina-2-amina e sua utilização como inibidores de jak cinases
MX2010008700A (es) * 2008-02-22 2010-08-30 Hoffmann La Roche Moduladores de beta-amiloide.
MX2012004313A (es) * 2009-10-12 2012-07-20 Myrexis Inc Compuestos de amino-pirimidina como inhibidores de cinasa 1 de union a tank (tbk1) y/o i-kappa-b-cinasa epsilon (ikk epsilon).
GB201012105D0 (en) 2010-07-19 2010-09-01 Domainex Ltd Novel pyrimidine compounds
JP2014500254A (ja) 2010-11-09 2014-01-09 セルゾーム リミティッド Tyk2阻害剤としてのピリジン化合物およびそのアザ類似体
US20140073643A1 (en) * 2010-12-03 2014-03-13 Ym Biosciences Australia Pty Ltd Treatment of jak2-mediated conditions
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
EP2681193B1 (en) 2011-03-02 2016-01-06 Lead Discovery Center GmbH Pharmaceutically active disubstituted pyridine derivatives
CA2833288A1 (en) 2011-04-19 2012-10-26 Bayer Intellectual Property Gmbh Substituted 4-aryl-n-phenyl-1,3,5-triazin-2-amines
KR20140081757A (ko) * 2011-05-02 2014-07-01 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 다발성골수종 치료방법
TWI555737B (zh) 2011-05-24 2016-11-01 拜耳知識產權公司 含有硫醯亞胺基團之4-芳基-n-苯基-1,3,5-三氮雜苯-2-胺
DE102011112978A1 (de) * 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate
ES2587284T3 (es) 2011-09-16 2016-10-21 Bayer Intellectual Property Gmbh 5-Fluoro-pirimidinas 2,4-disustituidas como inhibidores selectivos de CDK9
CN103930399B (zh) 2011-09-16 2016-03-16 拜耳知识产权有限责任公司 包含亚氨基亚磺酰基的二取代的5-氟嘧啶衍生物
CN103102359B (zh) * 2011-11-15 2016-11-09 江苏先声药业有限公司 嘧啶类化合物及其应用
AU2013287176C1 (en) 2012-06-13 2023-01-19 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US8809359B2 (en) * 2012-06-29 2014-08-19 Ym Biosciences Australia Pty Ltd Phenyl amino pyrimidine bicyclic compounds and uses thereof
CA2888381A1 (en) 2012-10-18 2014-04-24 Bayer Pharma Aktiengesellschaft 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amines containing a sulfone group
US9670161B2 (en) 2012-10-18 2017-06-06 Bayer Pharma Aktiengesellschaft 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group
TW201418243A (zh) 2012-11-15 2014-05-16 Bayer Pharma AG 含有磺醯亞胺基團之n-(吡啶-2-基)嘧啶-4-胺衍生物
WO2014075318A1 (zh) * 2012-11-19 2014-05-22 江苏先声药业有限公司 嘧啶类化合物及其应用
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
ES2672468T3 (es) 2013-01-09 2018-06-14 Concert Pharmaceuticals Inc. Momelotinib deuterado
CN103965114B (zh) * 2013-01-28 2016-01-06 苏州泽璟生物制药有限公司 氘代的苯基氨基嘧啶化合物以及包含该化合物的药物组合物
HUE036571T2 (hu) 2013-04-19 2018-07-30 Incyte Holdings Corp Biciklusos heterociklusok mint FGFR inhibitorok
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
DK3030561T3 (en) * 2013-08-07 2017-03-27 Cadila Healthcare Ltd N-CYANOMETHYLAMIDES AS INHIBITORS OF JANUS KINASE
CA2931615A1 (en) 2013-11-26 2015-06-04 Gilead Sciences, Inc. Therapies for treating myeloproliferative disorders
PL3080100T3 (pl) * 2013-12-11 2023-03-06 Celgene Quanticel Research, Inc. Inhibitory lizyno-specyficznej demetylazy-1
CA2937320A1 (en) 2014-01-20 2015-07-23 Gilead Sciences, Inc. Therapies for treating cancers
AU2015222865B2 (en) 2014-02-28 2019-06-20 Takeda Pharmaceutical Company Limited TYK2 inhibitors and uses thereof
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
TWI681954B (zh) * 2014-06-12 2020-01-11 美商西爾拉癌症醫學公司 N-(氰基甲基)-4-(2-(4-𠰌啉基苯基胺基)嘧啶-4-基)苯甲醯胺
BR112016028642A2 (pt) 2014-06-13 2017-08-22 Gilead Sciences Inc composto, composição farmacêutica, método de tratamento de uma doença ou condição, método de inibição da atividade de um polipeptídeo de fosfatidilinositol 3-quinase, método de inibição de reações imunes ou crescimento excessivo ou destrutivo ou de proliferação de células cancerosas, kit, e, uso de um composto, de um sal, de um isômero ou de uma mistura farmaceuticamente aceitável do mesmo.
KR20170012558A (ko) 2014-06-13 2017-02-02 길리애드 사이언시즈, 인코포레이티드 포스파티딜이노시톨 3-키나제 억제제
AR101504A1 (es) 2014-08-11 2016-12-21 Acerta Pharma Bv Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6
HUE056329T2 (hu) 2014-08-11 2022-02-28 Acerta Pharma Bv BTK-inhibitor és BCL-2-inhibitor terápiás kombinációi
PT3179992T (pt) 2014-08-11 2022-07-12 Acerta Pharma Bv Combinações terapêuticas de um inibidor de btk, um inibidor de pd-1 e/ou um inibidor de pd-l1
WO2016023082A1 (en) 2014-08-12 2016-02-18 Monash University Lymph directing prodrugs
CN104262263B (zh) * 2014-08-29 2017-01-11 西安交通大学 一种N,6二苯基嘧啶-4-胺类Bcr-Abl抑制剂及其制备方法和应用
KR101949624B1 (ko) 2014-09-26 2019-02-18 길리애드 사이언시즈, 인코포레이티드 Tank-결합 키나제 억제제 화합물로서 유용한 아미노트리아진 유도체
JP2017531003A (ja) 2014-10-16 2017-10-19 バイエル ファーマ アクチエンゲゼルシャフト スルホン基を含有するフッ化ベンゾフラニル−ピリミジン誘導体
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA51229A (fr) 2015-02-20 2021-03-24 Incyte Corp Hétérocycles bicycliques utilisés comme inhibiteurs des fgfr
EP3262049B1 (en) 2015-02-27 2022-07-20 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2016150902A1 (en) 2015-03-24 2016-09-29 Bayer Pharma Aktiengesellschaft Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating gastric cancers
JP2018509440A (ja) 2015-03-24 2018-04-05 バイエル ファーマ アクチエンゲゼルシャフト リンパ腫の治療のための4−(4−フルオロ−2−メトキシフェニル)−n−{3−[(s−メチルスルホンイミドイル)メチル]フェニル}−1,3,5−トリアジン−2−アミンの使用
WO2016150893A1 (en) 2015-03-24 2016-09-29 Bayer Pharma Aktiengesellschaft Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating multiple myeloma
CN106316964B (zh) * 2015-06-26 2019-06-25 苏州泽璟生物制药股份有限公司 苯基氨基嘧啶化合物或其盐的多晶型物
CN106316963B (zh) * 2015-06-26 2021-06-08 苏州泽璟生物制药股份有限公司 吗啡啉苯基氨基嘧啶化合物或其盐的多晶型物
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
US10023571B2 (en) 2015-09-02 2018-07-17 Nimbus Lakshimi, Inc. TYK2 inhibitors and uses thereof
CA2997106C (en) 2015-09-08 2024-06-04 Monash University Lymph directing prodrugs
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
WO2017055196A1 (en) 2015-09-29 2017-04-06 Bayer Pharma Aktiengesellschaft Novel macrocyclic sulfondiimine compounds
ES2819869T3 (es) 2015-10-08 2021-04-19 Bayer Pharma AG Nuevos compuestos macrocíclicos modificados
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
HRP20230331T1 (hr) 2015-10-23 2023-07-07 Navitor Pharmaceuticals, Inc. Modulatori interakcije sestrin-gator2 i njihova uporaba
US11370792B2 (en) 2015-12-14 2022-06-28 Raze Therapeutics, Inc. Caffeine inhibitors of MTHFD2 and uses thereof
FI3827838T3 (fi) 2015-12-16 2023-06-19 Walter & Eliza Hall Inst Medical Res Sytokiini-indusoidun sh2-proteiinin estäminen nk-soluissa
EP3884939B1 (en) 2016-03-09 2023-10-25 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
EP4234552A3 (en) 2016-03-09 2023-10-18 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
CN105837515B (zh) * 2016-04-06 2018-08-03 中国药科大学 一种JAK抑制剂Momelotinib的制备方法
EP3440112A4 (en) 2016-04-08 2019-10-09 X4 Pharmaceuticals, Inc. METHOD FOR THE TREATMENT OF CANCER
US11332470B2 (en) 2016-06-21 2022-05-17 X4 Pharmaceuticals, Inc. CXCR4 inhibitors and uses thereof
ES2870920T3 (es) 2016-06-21 2021-10-28 X4 Pharmaceuticals Inc Inhibidores de CXCR4 y usos de los mismos
US10988465B2 (en) 2016-06-21 2021-04-27 X4 Pharmaceuticals, Inc. CXCR4 inhibitors and uses thereof
US10245268B2 (en) 2016-08-10 2019-04-02 Sierra Oncology, Inc. Treatment of ACVR1-mediated diseases
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
WO2018057808A1 (en) 2016-09-23 2018-03-29 Gilead Sciences, Inc. Benzimidazole derivatives and their use as phosphatidylinositol 3-kinase inhibitors
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
TWI763722B (zh) 2016-10-14 2022-05-11 美商林伯士拉克許米公司 Tyk2抑制劑及其用途
WO2018075937A1 (en) 2016-10-21 2018-04-26 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EP3538091A4 (en) 2016-11-08 2020-06-10 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF
CN110177544A (zh) 2016-11-29 2019-08-27 普尔泰克健康有限公司 用于递送治疗剂的外泌体
WO2018106636A1 (en) 2016-12-05 2018-06-14 Raze Therapeutics, Inc. Shmt inhibitors and uses thereof
CN110603261A (zh) 2016-12-23 2019-12-20 拜斯科阿迪有限公司 具有新型键结构的肽衍生物
WO2018127699A1 (en) 2017-01-06 2018-07-12 Bicyclerd Limited Compounds for treating cancer
EP4338802A3 (en) 2017-03-08 2024-09-04 Takeda Pharmaceutical Company Limited Tyk2 inhibitors, uses, and methods for production thereof
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
US11242356B2 (en) 2017-03-28 2022-02-08 Bayer Aktiengesellschaft PTEFb inhibiting macrocyclic compounds
US11254690B2 (en) 2017-03-28 2022-02-22 Bayer Pharma Aktiengesellschaft PTEFb inhibiting macrocyclic compounds
WO2018191146A1 (en) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Heteroaryl rheb inhibitors and uses thereof
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
US10912750B2 (en) 2017-04-26 2021-02-09 Navitor Pharmaceuticals, Inc. Modulators of Sestrin-GATOR2 interaction and uses thereof
EP3615550A1 (en) 2017-04-27 2020-03-04 BicycleTx Limited Bicyclic peptide ligands and uses thereof
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3645549A1 (en) 2017-06-26 2020-05-06 BicycleRD Limited Bicyclic peptide ligands with detectable moieties and uses thereof
SG11202000714QA (en) 2017-07-28 2020-02-27 Nimbus Lakshmi Inc Tyk2 inhibitors and uses thereof
JP2020529427A (ja) 2017-08-04 2020-10-08 バイスクルテクス・リミテッド Cd137に対して特異的な二環式ペプチドリガンド
EP3668550A1 (en) 2017-08-14 2020-06-24 Bicyclerd Limited Bicyclic peptide ligand prr-a conjugates and uses thereof
WO2019034866A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS CONJUGATES AND USES THEREOF
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
WO2019046491A1 (en) 2017-08-29 2019-03-07 Ariya Therapeutics, Inc. LIPIDIC PRODRUGS DIRECTING TO THE LYMPHATIC SYSTEM
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
US11623932B2 (en) 2017-09-22 2023-04-11 Kymera Therapeutics, Inc. Protein degraders and uses thereof
AU2018350683A1 (en) 2017-10-19 2020-04-02 Bayer Animal Health Gmbh Use of fused heteroaromatic pyrrolidones for treatment and prevention of diseases in animals
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID MEDICINAL PRODUCTS AND THEIR USES
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc IRAK joints and used in them
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADANTS AND USES THEREOF
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
TWI816742B (zh) 2018-01-29 2023-10-01 美商維泰克斯製藥公司 Gcn2抑制劑及其用途
TW201940481A (zh) 2018-01-29 2019-10-16 美商維泰克斯製藥公司 Gcn2抑制劑及其用途
KR20200119800A (ko) 2018-02-13 2020-10-20 바이엘 악티엔게젤샤프트 미만성 거대 b-세포 림프종을 치료하기 위한 5-플루오로-4-(4-플루오로-2-메톡시페닐)-n-[4-[(s-메틸술폰이미도일)메틸]피리딘-2-일]피리딘-2-아민의 용도
MY196582A (en) 2018-02-13 2023-04-19 Gilead Sciences Inc PD-1/PD-L1 Inhibitors
US10696663B2 (en) 2018-02-27 2020-06-30 Artax Biopharma Inc. Chromene derivatives as inhibitors of TCR-NCK interaction
WO2019204609A1 (en) 2018-04-19 2019-10-24 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
SG11202009500QA (en) 2018-04-24 2020-11-27 Merck Patent Gmbh Antiproliferation compounds and uses thereof
TW202010744A (zh) 2018-04-24 2020-03-16 美商維泰克斯製藥公司 喋啶酮化合物及其用途
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
PL3793565T3 (pl) 2018-05-14 2022-05-02 Gilead Sciences, Inc. Inhibitory MCL-1
MX2020012503A (es) * 2018-05-25 2021-08-11 Kartos Therapeutics Inc Métodos de tratamiento de neoplasias mieloproliferativas.
HUE067446T2 (hu) 2018-06-15 2024-10-28 Janssen Pharmaceutica Nv Rapamicin analógok és alkalmazásaik
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
CN108707119A (zh) * 2018-06-25 2018-10-26 抚顺大恒化工有限公司 一种Momelotinib的制备方法
EP3817748A4 (en) 2018-07-06 2022-08-24 Kymera Therapeutics, Inc. TRICYCLIC CRBN LIGANDS AND USES THEREOF
KR102625712B1 (ko) 2018-07-13 2024-01-19 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
EP3840752A4 (en) 2018-08-21 2022-05-18 Sierra Oncology, Inc. PLATELET COUNT AGNOSTIC METHODS FOR TREATMENT OF MYELOFIBROSIS
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
CN113164419A (zh) 2018-09-07 2021-07-23 皮克医疗公司 Eif4e抑制剂和其用途
AU2019360941A1 (en) 2018-10-15 2021-04-29 Takeda Pharmaceutical Company Limited TYK2 inhibitors and uses thereof
WO2020084305A1 (en) 2018-10-23 2020-04-30 Bicycletx Limited Bicyclic peptide ligands and uses thereof
US11345654B2 (en) 2018-10-24 2022-05-31 Navitor Pharmaceuticals, Inc. Polymorphic compounds and uses thereof
JP7158577B2 (ja) 2018-10-24 2022-10-21 ギリアード サイエンシーズ, インコーポレイテッド Pd-1/pd-l1阻害剤
WO2020092383A1 (en) 2018-10-30 2020-05-07 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin
WO2020092394A1 (en) 2018-10-30 2020-05-07 Gilead Sciences, Inc. Imidazopyridine derivatives as alpha4beta7 integrin inhibitors
EP3873605B1 (en) 2018-10-30 2024-10-23 Gilead Sciences, Inc. Compounds for inhibition of alpha4beta7 integrin
BR112021007213A2 (pt) 2018-10-30 2021-08-10 Gilead Sciences, Inc. derivados de quinolina como inibidores de integrina alfa4beta7
EP3886843A4 (en) 2018-11-30 2022-08-31 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND THEIR USES
SG11202105424PA (en) 2018-11-30 2021-06-29 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
EP3904356A4 (en) * 2018-12-24 2022-09-21 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. THERAPEUTIC USE OF PYRROLOPYRIMIDINE COMPOUND, AND SOLID PHARMACEUTICAL COMPOSITION OF PYRROLOPYRIMIDINE COMPOUND
EP3914357A4 (en) 2019-01-23 2022-10-12 Nimbus Lakshmi, Inc. TYK2 INHIBITORS AND THEIR USES
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
EP3939979A4 (en) 2019-03-14 2022-04-06 Shanghai Synergy Pharmaceutical Sciences Co., Ltd KINASE JAK INHIBITOR, METHOD FOR PREPARING IT AND ITS APPLICATIONS IN THE FIELD OF MEDICINE
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
JP2022528887A (ja) 2019-04-02 2022-06-16 バイスクルテクス・リミテッド バイシクルトキシンコンジュゲートおよびその使用
CA3135802A1 (en) 2019-04-05 2020-10-08 Kymera Therapeutics, Inc. Stat degraders and uses thereof
CA3141826A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
WO2020256739A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2021091535A1 (en) 2019-11-05 2021-05-14 Constellation Pharmaceuticals, Inc. Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor
WO2020257644A1 (en) 2019-06-21 2020-12-24 Constellation Pharmaceuticals, Inc. Methods of treating myeloproliferative disorders
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN110330484B (zh) * 2019-07-18 2022-08-26 中国药科大学 取代类苯基嘧啶衍生物作为jak激酶抑制剂或其可药用的盐、制备方法及用途
TW202118770A (zh) 2019-07-30 2021-05-16 英商拜西可泰克斯有限公司 異質雙環肽複合物
CN114222730B (zh) 2019-08-14 2024-09-10 吉利德科学公司 用于抑制α4β7整合素的化合物
EP4028385A4 (en) 2019-09-11 2023-11-08 Vincere Biosciences, Inc. USP30 INHIBITORS AND USES THEREOF
AU2020347274A1 (en) 2019-09-13 2022-03-31 Nimbus Saturn, Inc. HPK1 antagonists and uses thereof
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4045151A1 (en) 2019-10-14 2022-08-24 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
MX2022005215A (es) 2019-11-01 2022-06-08 Navitor Pharm Inc Metodos de tratamiento que usan un modulador de la diana mecanicista del complejo 1 de rapamicina (mtorc1).
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CR20220285A (es) 2019-12-04 2022-10-27 Incyte Corp Derivados de un inhibidor de fgfr
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4069223A4 (en) 2019-12-05 2023-12-20 Janssen Pharmaceutica NV RAPAMYCIN ANALOGS AND THEIR USES
WO2021125758A1 (ko) * 2019-12-16 2021-06-24 주식회사 온코빅스 신규한 중수소 치환 피리미딘 유도체 및 이를 포함하는 약제학적 조성물
US11591332B2 (en) 2019-12-17 2023-02-28 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
AU2020407200A1 (en) 2019-12-17 2022-07-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
BR112022012410A2 (pt) 2019-12-23 2022-08-30 Kymera Therapeutics Inc Degradadores smarca e usos dos mesmos
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021159021A1 (en) 2020-02-05 2021-08-12 Puretech Lyt, Inc. Lipid prodrugs of neurosteroids
IL296139A (en) 2020-03-03 2022-11-01 Pic Therapeutics Inc eif4e inhibitors and uses thereof
CN115776887A (zh) 2020-03-19 2023-03-10 凯麦拉医疗公司 Mdm2降解剂和其用途
CA3177532A1 (en) 2020-04-30 2021-11-04 Gilead Sciences, Inc. Macrocyclic inhibitors of peptidylarginine deiminases
CN113583020B (zh) * 2020-04-30 2022-04-22 百极弘烨(广东)医药科技有限公司 一种jak2抑制剂及应用
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
CN116234931A (zh) 2020-08-17 2023-06-06 拜斯科技术开发有限公司 对nectin-4具有特异性的双环缀合物及其用途
CN112142675B (zh) * 2020-10-09 2021-11-30 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的小分子化合物及其用途
JP2023553866A (ja) 2020-12-02 2023-12-26 イケナ オンコロジー, インコーポレイテッド Tead阻害剤、及びその使用
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
EP4267587A2 (en) 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
US20240059673A1 (en) 2020-12-22 2024-02-22 Gilead Sciences, Inc. Substituted indole compounds
US11878965B2 (en) 2020-12-22 2024-01-23 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
AU2022216810A1 (en) 2021-02-02 2023-08-24 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
MX2023009059A (es) 2021-02-02 2023-09-15 Liminal Biosciences Ltd Antagonistas de gpr84 y usos de estos.
CN114874189B (zh) * 2021-02-05 2023-09-29 深圳市塔吉瑞生物医药有限公司 取代的杂芳基衍生物及其组合物及用途
US20240217990A1 (en) 2021-02-09 2024-07-04 Gilead Sciences, Inc. Thienopyrrole compounds
WO2022174269A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
EP4301756A1 (en) 2021-03-05 2024-01-10 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
EP4313989A1 (en) 2021-03-29 2024-02-07 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法
CA3214808A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Thienopyrrole compounds
KR20230172548A (ko) 2021-04-16 2023-12-22 이케나 온콜로지, 인코포레이티드 Mek 억제제 및 이의 용도
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
EP4384181A2 (en) 2021-08-10 2024-06-19 GlaxoSmithKline LLC Momelotinib combination therapy
WO2023023473A1 (en) 2021-08-16 2023-02-23 Sierra Oncology, Inc. Methods of using momelotinib to treat chronic kidney disease
US20230134932A1 (en) 2021-08-25 2023-05-04 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
JP2024534127A (ja) 2021-08-25 2024-09-18 ピク セラピューティクス, インコーポレイテッド eIF4E阻害剤及びその使用
US12070455B2 (en) 2021-09-10 2024-08-27 Gilead Sciences, Inc. Thienopyrrole compounds
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
WO2023147594A2 (en) 2022-01-31 2023-08-03 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2023152773A1 (en) * 2022-02-14 2023-08-17 Dr. Reddy's Institute Of Life Sciences Solid forms of momelotinib salts and improved processes for the preparation of momelotinib
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
TW202404581A (zh) 2022-05-25 2024-02-01 美商醫肯納腫瘤學公司 Mek抑制劑及其用途
CN117304179A (zh) * 2022-06-21 2023-12-29 苏州泽璟生物制药股份有限公司 杰克替尼二盐酸盐一水合物的制备工艺
WO2024028363A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
WO2024028365A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Substituted pyridone gpr84 antagonists and uses thereof
TW202415650A (zh) 2022-08-02 2024-04-16 英商利米那生物科技有限公司 芳基-三唑基及相關gpr84拮抗劑及其用途
WO2024035771A2 (en) * 2022-08-09 2024-02-15 H. Lee Moffitt Cancer Center And Research Institute, Inc. Ulk3 inhibitors and uses thereof
CN115677676B (zh) * 2022-10-19 2024-10-01 黑龙江中医药大学 一种治疗银屑病的药物及其制备方法
US20240208961A1 (en) 2022-11-22 2024-06-27 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
WO2024134481A1 (en) 2022-12-21 2024-06-27 Glaxosmithkline Llc Combination therapy comprising jaktinib

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3481932A (en) * 1967-09-01 1969-12-02 Searle & Co 2-anilino-5-methyl-6-phenylpyrimidines and congeners
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
EP1210099A4 (en) * 1999-08-13 2006-01-18 Scripps Research Inst TECHNIQUES AND COMPOSITIONS SUITABLE FOR THE MODULATION OF ANGIOGENESIS BASED ON RAF PROTEINKINASE AND KINASE RAS
GB9924862D0 (en) * 1999-10-20 1999-12-22 Celltech Therapeutics Ltd Chemical compounds
US7122544B2 (en) * 2000-12-06 2006-10-17 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
DE60223790D1 (de) 2001-03-29 2008-01-10 Vertex Pharma Hemmer von c-jun-terminal kinase (jnk) und andere protein kinase
US6433018B1 (en) 2001-08-31 2002-08-13 The Research Foundation Of State University Of New York Method for reducing hypertrophy and ischemia
RU2295329C2 (ru) 2001-09-12 2007-03-20 ВиРекс Медикал Корпорейшн Перекрывающее кровоток твердофазное средство с покрытием из иммобилизованного связывающего средства
NZ537155A (en) 2002-05-23 2006-09-29 Cytopia Pty Ltd Protein kinase inhibitors
BR0313397A (pt) 2002-08-14 2005-06-28 Vertex Pharmaceuticals Incorpo Inibidores de proteina cinase e usos destes
CA2506772A1 (en) * 2002-11-01 2004-05-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
ATE371656T1 (de) 2002-11-04 2007-09-15 Vertex Pharma Heteroaryl-pyrimidinderivate als jak-inhibitoren
US7348335B2 (en) * 2002-11-05 2008-03-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
JP2007500179A (ja) * 2003-07-30 2007-01-11 サイクラセル・リミテッド キナーゼ阻害剤としての2−アミノフェニル−4−フェニルピリミジン
GB0317841D0 (en) * 2003-07-30 2003-09-03 Cyclacel Ltd Compound
TW200626559A (en) * 2004-10-13 2006-08-01 Wyeth Corp Anilino-pyrimidine analogs
US7593820B2 (en) 2005-05-12 2009-09-22 Cytopia Research Pty Ltd Crystal structure of human Janus Kinase 2 (JAK2) and uses thereof
JP2008543775A (ja) * 2005-06-08 2008-12-04 ターゲジェン インコーポレーティッド 眼の障害を治療するための方法および組成物
BRPI0706747A2 (pt) 2006-01-30 2011-04-05 Exelixis Inc 4-aril-2-amino-pirimidinas ou 4-aril-2-aminoalquil-pirimidinas como moduladores jak-2 e composições farmacêuticas que os contenham
US8410173B2 (en) 2006-02-28 2013-04-02 Ym Biosciences Australia Pty Ltd Inhibition of JAK2 as a treatment of pulmonary arterial hypertension
FR2911139A1 (fr) * 2007-01-05 2008-07-11 Sanofi Aventis Sa Nouveaux derives de phenyl-(4-phenyl-pyrimidin-2-yl)amines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
CN104030990B (zh) 2007-03-12 2017-01-04 Ym生物科学澳大利亚私人有限公司 苯基氨基嘧啶化合物及其用途
WO2009032861A1 (en) * 2007-09-04 2009-03-12 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
WO2009029998A1 (en) 2007-09-06 2009-03-12 Cytopia Research Pty Ltd Retrometabolic compounds
WO2009073575A2 (en) 2007-11-30 2009-06-11 Oregon Health & Science University Methods for treating induced cellular proliferative disorders
CA2732791A1 (en) 2008-08-05 2010-02-11 Targegen, Inc. Methods of treating thalassemia
US20140073643A1 (en) 2010-12-03 2014-03-13 Ym Biosciences Australia Pty Ltd Treatment of jak2-mediated conditions
KR20140081757A (ko) 2011-05-02 2014-07-01 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 다발성골수종 치료방법
US8809359B2 (en) 2012-06-29 2014-08-19 Ym Biosciences Australia Pty Ltd Phenyl amino pyrimidine bicyclic compounds and uses thereof

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