HRP20161127T1 - Derivati indazolil triazola kao inhibitori irak - Google Patents

Derivati indazolil triazola kao inhibitori irak Download PDF

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HRP20161127T1
HRP20161127T1 HRP20161127TT HRP20161127T HRP20161127T1 HR P20161127 T1 HRP20161127 T1 HR P20161127T1 HR P20161127T T HRP20161127T T HR P20161127TT HR P20161127 T HRP20161127 T HR P20161127T HR P20161127 T1 HRP20161127 T1 HR P20161127T1
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HRP20161127TT
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Catherine Jorand-Lebrun
Stefano Crosignani
Jérôme DORBAIS
Tania Grippi-Vallotton
Adeline Pretre
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Merck Serono S.A.
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Claims (14)

1. Spoj s formulom (I) [image] naznačen time da Q označava Ar ili Het, E označava -(CH2)mCO-, -(CH2),SO2, -(CH2)q-, -(CH2)mNHCO-, ili jednostruku vezu, R1 označava H, OH, NH-C1-C6-alkil, OC1-C6-alkil, C1-C6-alkil, C2-C6-alkenil, C2-C6- alkinil, Cyc, Hal, Het1, O-Het1, CO-Het1, NH-Het1, CO-AR1, O-AR1, AR1, NH-AR1, - (CH2)qHet1, -CONH-(CH2)qHet1, -CONH-Het1,-(CH2)qO-Het1, -(CH2)qO-AR1, - (CH2)qAR1, -CONH-(CH2)qAR1, -CONH-AR1, -CONHC3-C6-cikloalkil, -(CH)qHal, - (CH2)qCyc, CF3, -(CH2)sNH-(CH2)q-Het1, -(CH2)sNH-(CH2)q-AR1, pri čemu NH-C1-C6-alkil, OC1-C6-alkil, C1-C6-alkil, C2-C6-alkenil, C2-C6-alkinil, C3-C6-cikloalkil mogu biti supstituirani s 1 do 3 skupine koje se neovisno biraju od OC1-C3-alkil, OH, CONH2, NH2, R2 označava H, C1-C6-alkil, C2-C6-alkenil, C2-C6-alkinil, Hal, CF3, poželjno H, R3 označava Het1, AR1, NRaRb, COOH, -(CH2)qHet1, -(CH2)qAR1, -(CH2)qNRaRb, - (CH2)qCOOH, ili C1-C6-alkil pri čemu 1 do 3 vodikovih atoma može biti neovisno zamijenjeno s OH ili CF3. R4 označava H, C1-C6-alkil, C2-C6-alkenil, Hal; Ra označava H, ravni, razgranati ili ciklički C1-C6-alkil, Rb označava H, Hetb, ARb, -CO-Hetb, -CO-ARb, a C3-C8-cikloalkil ili ravni ili razgranati alkil koji ima 1 do 6 ugljikovih atoma, pri čemu 1 do 3 vodikovih atoma može biti zamijenjeno s Hetb, ARb, NH2, N(C1-C6-alkil)2, NH(C1-C6-alkil), N(C1-C6- alkil)(C3-C8-cikloalkil), NH(C3-C8-cikloalkil), O(C1-C6,-alkil), CN, OH, CF3, Hal, n je 0, 1, 2, 3 ili 4, m je 0, 1, 2, 3 ili 4, q je 1, 2, ili 3, s je 0, i, 2 ili 3, Hal označava Cl, Br, I, F, poželjno Cl ili F. Ar označava dvovalentnu monocikličku ili kondenziranu bicikličku arilen skupinu koja ima 6 do 14 ugljikovih atoma, koja može biti dalje supstituirana s 1 do 4 supstituenata koji se biraju od Hal, C1-C6-alkil, -(CH2)mOC1-C6-alkil, CN, OH, NO2, CF3, -(CH2)mCOOH, - (CH2)mCOOC1-C6-alkil; Het označava dvovalentnu monocikličku ili kondenziranu bicikličku nezasićenu, zasićenu ili aromatsku heterocikličku skupinu koja ima 1 do 5 heteroatoma koji se neovisno biraju od N, O, S i/ili od skupine -C=O, koja može biti dalje supstituirana s 1 do 4 supstituenata koji se biraju od Hal, C1-C6-alkil, -(CH2)mOC1-C6-alkil, CN, OH, NO2, CF3, - (CH2)mCOOH, -(CH2)mCOOC1-C6-alkil; AR1 označava monociklički ili biciklički, aromatski karbociklički prsten koji ima 6 do 14 ugljikovih atoma, koji je nesupstituiran ili jednostruko supstituiran, dvostruko supstituiran ili trostruko supstituiran s Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalkilom, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalkil, ravnim ili razgranatim C1-C6-alkilom, cikloalkilom, -OH, -OC1-C6-alkilom, -COC1-C6-alkilom, -NH2, -COH, -COOH, -CONH2, skupinom Rb kao što je -CH2O(C1-C6-alkil), - SO2NRaRb ili SO2(C1-C6alkil), Het1 označava monociklički ili biciklički (kondenziran, premošten ili spiro) zasićen, nezasićen ili aromatski heterociklički prsten koji ima 1 do 4 heteroatoma koji se neovisno biraju od N, O, S i/ili skupine CO, koji je nesupstituiran ili jednostruko supstituiran, dvostruko supstituiran ili trostruko supstituiran s Hal, -CF3, -OCF3, - NO2, -CN, perfluoroalkil, ravni ili razgranati C1-C6-alkil, C3-C8-cikloalkil, -OH, - OC1-C6-alkil, -NH2, -N(C1-C6-alkil)2, -COH, -COOH, -CONH2, -COC1-C6-alkil, - NHCO(C3-C6cikloalkil), skupina Rb -SO2NRaRb ili SO2(C1-C6alkil), Hetb označava monociklički ili biciklički (kondenziran ili spiro) zasićen, nezasićen ili aromatski heterociklički prsten koji ima 1 do 4 heteroatoma koji se neovisno biraju od N, O, S i/ili od skupine CO, koji je nesupstituiran ili jednostruko supstituiran, dvostruko supstituiran ili trostruko supstituiran s Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalkilom, -OH, -OC1-C6-alkilom, - NH2, -COH, -COOH, -CONH2, ili s ravnim ili razgranatim C1-C6-alkilom pri čemu 1 do 3 vodikovih atoma može biti zamijenjeno s NH2, N(C1-C6-alkil)2, NH(C1-C6-alkil), N(C1-C6-alkil)(C3-C8- cikloalkil), NH(C3-C8-cikloalkil), O(C1-C6-alkil), CN, OH, CF3, Hal, C3-C8-cikloalkil, ili s 4 do 8-članim heterocikličkim prstenom koji sadrži jedan heteroatom koji se bira od O, S i N, ARb označava monociklički ili biciklički, aromatski kARbociklički prsten koji ima 6 do 14 ugljikovih atoma, koji je nesupstituiran ili jednostruko supstituiran, dvostruko supstituiran ili trostruko supstituiran s Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalkilom, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalkilom, -OH, -OC1-C6- alkilom, -NH2, -COH, -COOH, -CONH2, ili s ravnim ili razgranatim C1-C6-alkilom pri čemu 1 do 3 vodikovih atoma može biti zamijenjeno s NH2, N(C1-C6-alkil)2, NH(C1-C6,-alkil), N(C1-C6-alkil)(C3-C8-cikloalkil), NH(C3-C8-cikloalkil), O(C1-C6- alkil), CN, OH, CF3, Hal, C3-C8-cikloalkil, ili s 4 do 8-članim heterocikličkim prstenom koji sadrži jedan heteroatom koji se bira od O, S i N, Cyc označava zasićeni ili nezasićeni kARbociklički prsten koji ima 3 do 8 ugljikovih atoma, poželjno 5 ili 6 ugljikovih atoma, pri čemu 1 do 5 atoma H su zamijenjeni s Hal, -CF3, - OCF3, -NO2, -CN, perfluoroalkilom, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalkilom, ravnim ili razgranatim C1-C6-alkilom, cikloalkilom, -OH, -OC1-C6- alkilom, -COC1-C6-alkilom,-NH2, -COH, -COOH, -CONH2, skupinom Rb kao što je - CH2O(C1-C6-alkil), -SO2NRaRb ili SO2(C1-C6alkil). i njihovi farmaceutski prihvatljivi solvati, tautomeri, soli, hidrati i stereoizomeri, uključujući njihove smjese u svim omjerima.
2. Spoj s formulom (I) prema zahtjevu 1 naznačen time da skupina Q-E-R3 označava jednu od slijedećih skupina: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image]
3. Spoj s formulom (I) prema zahtjevima 1 ili 2 naznačen time da R1 označava H, Hal, metil, trifluorometil, metoksi, hidroksi ili jednu od sljedećih skupina: [image] [image] [image]
4. Spoj s formulom (I) prema zahtjevima 1 do 3 naznačen time da je spoj izabran iz sljedeće skupine: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image]
5. Spoj s formulom (I) prema zahtjevu 1: [image] pri čemu Q označava Ar ili Het, E označava -(CH2)mCO-, -(CH2)mSO2, -(CH2)q-, -(CH2)mNHCO-, ili jednostruku vezu, R1 označava H, OH, NH-C1-C6-alkil, OC1-C6-alkil, C1-C6-alkil, C2-C6-alkenil, C2-C6- alkinil, Cyc, Hal, Het1, O-Het1, CO-Het1, NH-Het1, CO-AR1, O-AR1, AR1, NH-AR1, - (CH2)qHet1, -CONH-(CH2)qHet1, -CONH-Het1,-(CH2)qO-Het1, -(CH2)qO-AR1,- (CH2)qAR1, -CONH-(CH2)qAR1, -CONH-AR1, -CONHC3-C6-cikloalkil, -(CH2)q Hal,- (CH2)qCyc, CF3, -(CH2)qNH-(CH2)q-Het1, -(CH2)qNH-(CH2)q-AR1 pri čemu NH-C1-C6-alkil, OC1-C6-alkil, C1-C6-alkil, C2-C6-alkenil, C2-C6-alkinil, C3-C6-cikloalkil može biti dodatno supstituiran s 1 do 3 skupine koje su neovisno odabrane od OC1-C3-alkil, OH, CONH2, NH2, R2 označava H, C1-C6-alkil, C2-C6-alkenil, C2-C6-alkinil, Hal, CF3, poželjno H, R3 označava Het1, AR1, NRaRb, COOH, -(CH2)qHet1, -(CH2)qAR1, -(CH2)qNRaRb,- (CH2)qCOOH, ili C1-C6-alkil pri čemu 1 do 3 vodikovih atoma može biti neovisno zamijenjeno s OH ili CF3, R4 označava H, C1-C6-alkil, C2-C6-alkenil, Hal; Ra označava H, ravni, razgranati ili ciklički C1-C6-alkil, Rb označava H, Hetb, ARb, -CO-Hetb, -CO-ARb, C3-C6-cikloalkil ili ravni ili razgranati alkil koji ima 1 do 6 ugljikovih atoma, pri čemu 1 do 3 vodikovih atoma može biti zamijenjeno s Hetb, ARb, NH2, N(C1-C6-alkil)2, NH(C1-C6-alkil), N(C1-C6-alkil)(C3- C8-cikloalkil), NH(C3-C8-cikloalkil), O(C1-C6-alkil), CN, OH, CF3, Hal, n je 0, 1, 2, 3 ili 4, m je 0, 1, 2 , 3 ili 4, q je 1, 2, ili 3, s je 0, 1, 2 ili 3 Hal označava Cl, Br, I, F, poželjno Cl ili F, Ar označava dvovalentnu monocikličku ili kondenziranu bicikličku arilen skupinu koja ima 6 do 14 ugljikovih atoma, koja može biti dalje supstituirana s 1 do 4 supstituenata koji se biraju od Hal, C1-C6-alkil, -(CH2)mOC1-C6-alkil, CN, OH, NO2 CF3, -(CH2)mCOOH,-(CH2)mCOOC1-C6-alkil; Het označava dvovalentnu monocikličku ili kondenziranu bicikličku nezasićenu, zasićenu ili aromatsku heterocikličku skupinu koja ima 1 do 5 heteroatoma koji se neovisno biraju od N, O, S i/ili od skupine -C=O, koja može biti dalje supstituirana s 1 do 4 supstituenata koji se biraju od Hal, C1-C6-alkil, -(CH2)mOC1-C6-alkil, CN, OH, NO2 CF3,-(CH2)mCOOH, -(CH2)mCOOC1-C6-alkil; AR1 označava monociklički ili biciklički, aromatski karbociklički prsten koji ima 6 do 14 ugljikovih atoma, koji je nesupstituiran ili jednostruko supstituiran, dvostruko supstituiran ili trostruko supstituiran s Hal, -CF3, -OCF3, -NO2 -CN, perfluoroalkil, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalkil, ravni ili razgranati C1-C6-alkil, cikloalkil, -OH, -OC1-C6-alkil, -COC1-C6-alkil, -NH2, -COH, -COOH, -CONH2, skupina Rb kao što je -CH2O(C1-C6-alkil),-SO2NRaRb ili SO2(C1-C6alkil). Het1 označava monociklički ili biciklički (kondenzirani, premošteni ili spiro) zasićeni, nezasićeni ili aromatski heterociklički prsten koji ima 1 do 4 heteroatoma koji se neovisno biraju od N, O, S i/ili CO skupine, koji je nesupstituiran ili jednostruko supstituiran, dvostruko supstituiran ili trostruko supstituiran s Hal, -CF3, -OCF3, -NO2 -CN, perfluoroalkil, ravni ili razgranati C1-C6-alkil, C3-C8-cikloalkil, -OH, -OC1-C6- alkil, -NH2, -N(C1-C6-alkil)2, -COH, -COOH, -CONH2, -COC1-C6-alkil, -NHCO(C3- C6cikloalkil), skupina Rb ,-SO2NRaRb ili SO2(C1-C6alkil). Hetb označava monociklički ili biciklički (kondenzirani ili spiro) zasićeni, nezasićeni ili aromatski heterociklički prsten koji ima 1 do 4 heteroatoma koji se neovisno biraju od N, O, S i/ili CO skupine, koji je nesupstituiran ili jednostruko supstituiran, dvostruko supstituiran ili trostruko supstituiran s Hal, -CF3, -OCF3, -NO2 -CN, perfluoroalkil, -OH, -OC1-C6-alkil,-NH2, -COH, -COOH, -CONH2, ili s ravnim ili razgranatim C1-C6-alkilom pri čemu 1 do 3 vodikovih atoma može biti zamijenjeno s NH2, N(C1-C6-alkil)2, NH(C1-C6-alkil), N(C1-C6-alkil)(C3-C8-cikloalkil), NH(C3-C8- cikloalkil), O(C1-C6-alkil), CN, OH, CF3, Hal, C3-C8-cikloalkil, ili s 4 do 8-članim heterocikličkim prstenom koji sadrži jedan heteroatom koji se bira od O, S i N, ARb označava monociklički ili biciklički, aromatski kARbociklički prsten koji ima 6 do 14 ugljikovih atoma, koji je nesupstituiran ili jednostruko supstituiran, dvostruko supstituiran ili trostruko supstituiran s Hal, -CF3, -OCF3, -NO2 -CN, perfluoroalkilom, Hal, -CF3, -OCF3, -NO2 -CN, perfluoroalkilom, -OH, -OC1-C6-alkilom, -NH2, -COH, -COOH, -CONH2, ili s ravnim ili razgranatim C1-C6-alkilom pri čemu 1 do 3 vodikovih atoma može biti zamijenjeno s NH2, N(C1-C6-alkil)2, NH(C1-C6-alkil), N(C1-C6-alkil)(C3-C8-cikloalkil), NH(C3-C8-cikloalkil), O(C1-C6-alkil), CN, OH, CF3, Hal, C3-C8-cikloalkil, ili sa 4 do 8-članim heterocikličkim prstenom koji sadrži jedan heteroatom koji se bira od O, S i N, Cyc označava zasićeni ili nezasićeni kARbociklički prsten koji ima 3 do 8 ugljikovih atoma, poželjno 5 ili 6 ugljikovih atoma, pri čemu 1 do 5 H atoma su zamijenjeni s Hal, -CF3,-OCF3, -NO2, -CN, perfluoroalkilom, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalkilom, ravnim ili razgranatim C1-C6-alkilom, cikloalkilom, -OH, -OC1-C6- alkilom, -COC1-C6-alkilom,-NH2, -COH, -COOH, -CONH2, skupinom Rb kao što je - CH2O(C1-C6-alkil), -SO2NRaRb ili SO2(C1-C6alkil). i njihovi farmaceutski prihvatljivi solvati, tautomeri, soli, hidrati i stereoizomeri, uključujući njihove smjese u svim omjerima, naznačen time da je za uporabu kao lijek.
6. Spoj prema zahtjevu 5, naznačen time da je za uporabu za liječenje ili sprječavanje upalne bolesti, autoimunog poremećaja, raka ili mraultiple skleroze i srodnih poremećaja.
7. Spoj prema zahtjevu 6, naznačen time da se autoimuna bolest bira iz skupa koji čine astma, reumatoidni artritis, akutni diseminirani encefalomijelitis (ADEM), Addisonova bolest, alopecija areata, ankilozni spondilitis, sindrom antifosfolipidnih antitijela (APS), autoimuna hemolitička anemija, autoimuni hepatitis, autoimuna bolest unutarnjeg uha, bulozni pemfigoid, Behcetova bolest, celijakija, anti- transglutaminaza, Chagasova bolest, kronična opstruktivna plućna bolest, Crohnova bolest, dermatomiozitis, dijabetes melitus tip 1, endometrioza, Goodpasturov sindrom, Gravesova bolest, Guillain-Barreov sindrom (GBS), Hashimotova bolest, supurativni hidradenitis, Kawasaki bolesti, IgA nefropatija, idiopatska trombocitopenična purpura, intersticijski cistitis, eritematozni lupus, miješana bolest vezivnog tkiva, morfea, multipla skleroza (MS), mijastenija gravis, narkolepsija, neuromiotonija, pemfigus vulgaris, perniciozna anemija, psorijaza, psorijatični artritis, polimiozitis, primarna bilijarna ciroza, reumatoidni artritis, shizofrenija, skleroderma, Sjogrenov sindrom, sindrom ukočene osobe, sistemska skleroza, temporalni arteritis, ulcerativni kolitis, vaskulitis, vitiligo, Wegenerova granulomatoza.
8. Spoj prema zahtjevu 6, naznačen time da se bolest bira iz skupa koji čine reumatoidni artritis, psorijatični artritis, osteoartritis, sistemski eritematozni lupus, lupus nefritis, ankilozni spondilitis, osteoporoza, sistemska skleroza, multipla skleroza, psorijaza, dijabetes tipa I, dijabetes tipa II, upalna bolest crijeva (Cronhova bolest i ulcerozni kolitis), hiperimunoglobulinemija D i sindrom periodičke groznice, periodični sindromi vezani za kriopirin, Schnitzlerov sindrom, sistemski juvenilni idiopatski artritis, Stillova bolest odrasle dobi, giht, pseudogout, SAPHO sindrom, Castlemanova bolest, sepsa, udar, ateroskleroza, celijakija, DIRA (nedostatak antagonista IL-1 receptora) Alzheimerova bolest, Parkinsonova bolest, rak.
9. Spoj prema zahtjevu 6, naznačen time da bolest je odabrana od reumatoidnog artritisa, lupus nefritisa, sistemskog lupusa eritematodes.
10. Komplet, naznačen time da sadrži odvojena pakiranja: (a) učinkovite količine spoja s formulom (I) prema zahtjevu 1, te (b) učinkovite količine dodatnog aktivnog sastojka lijeka.
11. Farmaceutski pripravci, naznačeni time da sadrže barem jedan od spojeva s Formulom (I) prema bilo kojem od zahtjeva 1 do 5.
12. Farmaceutski pripravak prema zahtjevu 11, naznačen time da dodatno sadrži barem jedan dodatni lijek koji se koristi u liječenju upalnih bolesti ili imunoloških poremećaja.
13. Farmaceutski pripravak prema zahtjevu 12, naznačen time da dodatno sadrži barem jedno dodatno imunomodulacijsko sredstvo.
14. Postupak za proizvodnju spojeva formule (I) prema zahtjevima 1 do 4, naznačen time da sadrži korak reakcije spoja II [image] pri čemu R1, R2, R4 i n su kako je definirano u zahtjevu 1 i pri čemu PG1 označava H ili dušikove zaštitne skupine, sa spojem s Formulom (III) [image] pri čemu Q, E i R3 su kako je definirano u zahtjevu 1.
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Families Citing this family (59)

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Publication number Priority date Publication date Assignee Title
AR045563A1 (es) 2003-09-10 2005-11-02 Warner Lambert Co Anticuerpos dirigidos a m-csf
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
ME03300B (me) 2012-06-13 2019-07-20 Incyte Holdings Corp Supsтituisana triciklična jedinjenja као inhibiтori fgfr
US9643955B2 (en) 2012-12-20 2017-05-09 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-nitrile-4-substituted orexin receptor antagonists
EP2934516A4 (en) 2012-12-20 2016-07-20 Merck Sharp & Dohme ANTAGONISTS OF 3-ESTER-4-SUBSTITUTED OREXIN RECEPTORS
CA2900442C (en) * 2013-02-07 2021-09-21 Merck Patent Gmbh Macrocyclic pyridazinone derivatives
JP6483624B2 (ja) * 2013-02-07 2019-03-13 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Ｍｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ピリダジノン−アミド誘導体
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
TWI667233B (zh) 2013-12-19 2019-08-01 德商拜耳製藥公司 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途
US10160753B2 (en) 2014-01-10 2018-12-25 Aurigene Discovery Technologies Limited Indazole compounds as IRAK4 inhibitors
PT3466955T (pt) 2014-01-13 2021-01-29 Aurigene Discovery Tech Ltd Método de preparação de derivados de oxazolo[4,5-b] piridina e tiazolo[4,5-b] piridina como inibidores de irak-4 para o tratamento do cancro
US9926330B2 (en) 2014-09-30 2018-03-27 Merck Sharp & Dohme Corp. Inhibitors of IRAK4 activity
US9969749B2 (en) 2014-09-30 2018-05-15 Merck Sharp & Dohme Corp. Inhibitors of IRAK4 activity
EP3200789B1 (en) 2014-09-30 2019-11-06 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
EP3200790B1 (en) 2014-09-30 2020-08-26 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
JO3705B1 (ar) * 2014-11-26 2021-01-31 Bayer Pharma AG إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية
WO2016096709A1 (en) 2014-12-16 2016-06-23 Eudendron S.R.L. Heterocyclic derivatives modulating activity of certain protein kinases
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
BR112017022349B1 (pt) 2015-04-22 2023-11-07 Rigel Pharmaceuticals, Inc Composto, composição o compreendendo, seus usos, e, método
EP3195865A1 (de) 2016-01-25 2017-07-26 Bayer Pharma Aktiengesellschaft Kombinationen von irak4 inhibitoren und btk inhibitoren
TW201701879A (zh) 2015-04-30 2017-01-16 拜耳製藥公司 Ｉｒａｋ４抑制劑組合
EP3423446B1 (de) 2016-03-03 2020-09-16 Bayer Pharma Aktiengesellschaft Neue 2-substituierte indazole, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln
EP3219329A1 (en) 2016-03-17 2017-09-20 Bayer Pharma Aktiengesellschaft Combinations of copanlisib
MA44759B1 (fr) 2016-04-29 2024-01-31 Bayer Pharma AG Forme polymorphe de n-(6-(2-hydroxypropan-2-yl)-2-[2-(méthylsulfonyl)éthyl]-2h-indazol-5-yl)-6-(trifluorométhyl)pyridine-2-carboxamide
SG11201808686VA (en) 2016-04-29 2018-11-29 Bayer Pharma AG Synthesis of indazoles
UA124237C2 (uk) 2016-06-01 2021-08-11 Байєр Енімал Хелс Гмбх Заміщені індазоли, придатні для лікування і попередження алергійних і/або запальних захворювань у тварин
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
HRP20230657T8 (hr) 2017-03-31 2023-11-10 Aurigene Oncology Limited Spojevi i pripravci za liječenje hematoloških poremećaja
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3684366A4 (en) 2017-09-22 2021-09-08 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES OF THE LATEST
AU2018338314A1 (en) 2017-09-22 2020-04-09 Kymera Therapeutics, Inc Protein degraders and uses thereof
WO2019076817A1 (en) 2017-10-19 2019-04-25 Bayer Animal Health Gmbh USE OF FUSED HETEROAROMATIC PYRROLIDONES FOR THE TREATMENT AND PREVENTION OF DISEASES IN ANIMALS
SG11202002386WA (en) 2017-10-31 2020-04-29 Curis Inc Compounds and compositions for treating hematological disorders
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
US10874743B2 (en) 2017-12-26 2020-12-29 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. CRBN LIGANDS AND THEIR USES
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADANTS AND USES THEREOF
GB201801226D0 (en) * 2018-01-25 2018-03-14 Redx Pharma Plc Modulators of Rho-associated protein kinase
EA202092649A1 (ru) 2018-05-04 2021-06-21 Инсайт Корпорейшн Соли ингибитора fgfr
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
TW202136268A (zh) 2018-07-13 2021-10-01 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
BR112021010484A2 (pt) 2018-11-30 2021-08-24 Kymera Therapeutics, Inc. Degradadores de irak e usos dos mesmos
EP3924340A1 (en) * 2019-02-11 2021-12-22 Merck Patent GmbH Indazolyl-isoxazole derivatives for the treatment of diseases such as cancer
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JOP20220050A1 (ar) 2019-08-30 2023-01-30 Rigel Pharmaceuticals Inc مركبات بيرازول، صياغات منها وطريقة لاستخدام المركبات و/ أو صياغات
EP4038062A4 (en) 2019-10-02 2023-10-11 Kainos Medicine, Inc. N-(1H-IMIDAZOL-2-YL)BENZAMIDE COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING IT AS ACTIVE INGREDIENT
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclyl heterocycles as fgr suppressors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN114599652A (zh) * 2019-10-31 2022-06-07 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的氢吡嗪并[1,2-d][1,4]二氮杂䓬化合物
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
BR112022011651A2 (pt) 2019-12-17 2022-08-23 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
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
US11866405B2 (en) 2020-12-10 2024-01-09 Astrazeneca Ab Substituted indazoles as IRAK4 inhibitors
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
KR102607237B1 (ko) * 2023-06-07 2023-11-30 주식회사 젠센 신규한 트리아졸이 치환된 인다졸 유도체 및 이의 용도

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA200503242B (en) * 2002-10-24 2006-10-25 Celgene Corp Treatment of pain with JNK inhibitors
US20040087642A1 (en) 2002-10-24 2004-05-06 Zeldis Jerome B. Methods of using and compositions comprising a JNK inhibitor for the treatment, prevention, management and/or modification of pain
US20050090529A1 (en) * 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
US6984652B2 (en) * 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
US20060258706A1 (en) * 2005-04-29 2006-11-16 Manohar Saindane Solid forms of a JNK inhibitor
BRPI0811065A2 (pt) * 2007-06-08 2014-12-02 Abbott Lab Indazóis 5-heteroaril substituídos como inibidores de quinase

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