ME02203B - Hinolin i hinoksalin derivati kao inhibitori kinaza - Google Patents

Hinolin i hinoksalin derivati kao inhibitori kinaza

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Publication number
ME02203B
ME02203B MEP-2015-120A MEP12015A ME02203B ME 02203 B ME02203 B ME 02203B ME P12015 A MEP12015 A ME P12015A ME 02203 B ME02203 B ME 02203B
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Montenegro
Prior art keywords
pyrido
trifluoroethyl
quinolin
pyrimidin
compound according
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MEP-2015-120A
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Andrew Harry Parton
Mezher Hussein Ali
Daniel Christopher Brookings
Julien Alistair Brown
Daniel James Ford
Richard Jeremy Franklin
Barry John Langham
Judi Charlotte Neuss
Joanna Rachel Quincey
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Ucb Biopharma Sprl
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45810169&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02203(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GBGB1014963.1A external-priority patent/GB201014963D0/en
Priority claimed from GBGB1101128.5A external-priority patent/GB201101128D0/en
Application filed by Ucb Biopharma Sprl filed Critical Ucb Biopharma Sprl
Publication of ME02203B publication Critical patent/ME02203B/me

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    • C07D471/00—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
    • 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 (38)

1. Jedinjenje formule (I) ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat:gdeU predstavlja -CF3, -CHF2 ili -CH2F;Q predstavlja kiseonik, sumpor, N-R4 ili kovalentnu vezu;Z predstavlja opciono supstituisanu bicikličnu heteroaril grupu koja se sastoji od dva kuplovana šesto-člana aromatična prstena, heteroaril grupa Z sadrži najmanje jedan atom azota koji je za ostatak molekula vezan preko atoma ugljenika;M predstavlja aril ili heteroaril grupu, od kojih svaka može biti opciono supstituisana sa jednim ili više supstituenata;W predstavlja C-R5 ili N;R1, R2 i R3 nezavisno predstavljaju vodonik, halogen, cijano, nitro, C1-6 alkil, trifluorometil, C3-7 cikloalkil(C1-6)alkil, C3-7heterocikloalkil(C1-6)alkil, aril(C1-6)-alkil, heteroaril(C1-6)alkil, hidroksi, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio, C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksikarbonilamino, C1-6 alkilsulfonilamino, formil, C2-6 alkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6) alkilaminokarbonil, aminosulfonil, C1- 6 alkilaminosulfonil ili di(C1-6) alkilaminosulfonil;R4 predstavlja vodonik ili C1-6 alkil; iR5 predstavlja vodonik, halogen, C1-6 alkil ili C1-6 alkoksi.
2. N-oksid derivat jedinjenja formule (I) kako je definisano u patentnom zahtevu 1, ili njegova farmaceutski prihvatljiva so ili solvat.
3. Jedinjenje prema patentnom zahtevu 1 ili zahtevu 2, naznačeno time što U predstavlja -CF3.
4. Jedinjenje prema zahtevu 3, naznačeno time što atom ugljenika za koji su -KZ i -CF3 grupe direktno vezane, ima (R) konfiguraciju.
5. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što Q predstavlja N-R4.
6. Jedinjenje prema patentnom zahtevu 5 naznačeno time što R4 predstavlja vodonik ili metil.
7. Jedinjenje prema bilo kom od prethodnih zahteva naznačeno time što Z predstavlja hinolinil, izohinolinil, cinolinil, hinazolinil, hinoksalinil, ftalazinil, naftiridinil, pirido-pirimidinil ili pteridinil grupe koje su sve vezane za ostatak molekula preko atoma ugljenika, i od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata nezavisno izabranih između: halogen, cijano, nitro, C1-6 alkil, trifluorometil, hidroksi, okso, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio , C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6) alkilamino, arilamino, C1-6 alkoksiaril(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksi karbonilamino, C1-6 alkilsulfonilamino, formil, C2-6 alkilkarbonil, C3-6 cikloalkilkarbonil, C3-6 heterocikloalkilkarbonil, (C1-6)alkil-(C3-6) heterocikloalkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6) alkilaminokarbonil, aminosulfonil, C1-6 alkilaminosulfonil i di(C1-6)alkilaminosulfonil.
8. Jedinjenje prema patentnom zahtevu 7, naznačeno time što Z predstavlja pirido[3,2-d]-pirimidin-4-il.
9. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što M predstavlja fenil, pirolil, furil, tienil, imidazolil, oksazolil, izoksazolil, tiazolil, izotiazolil, pirazolil, triazolil, oksadiazolil, tiadiazolil, piridinil, pirimidinil, piridazinil, pirazinil, tetrazolil ili triazinil, od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata izabranih od: halogena, cijano, nitro, C1-6 alkil, trifluorometil, hidroksi, C1-6 alkoksi, difluorometoksi, trifluorometoksi, C1-6 alkiltio, C1-6 alkilsulfinil, C1-6 alkilsulfonil, amino, C1-6 alkilamino, di(C1-6)alkilamino, C2-6 alkilkarbonilamino, C2-6 alkoksikarbonilamino, C1-6 alkilsulfonilamino, formil, C2 -6 alkilkarbonil, karboksi, C2-6 alkoksikarbonil, aminokarbonil, C1-6 alkilaminokarbonil, di(C1-6)alkilaminokarbonil, aminosulfonil, C1-6 alkilaminosulfonil, di(C1-6)alkilamino sulfonil, C3-7cikloalkil, C3-6 heterocikloalkil, (C1-6)alkil(C3-6) heterocikloalkil, monociklični aril i monociklični heteroaril.
10. Jedinjenje prema patentnom zahtevu 9, naznačeno time što M predstavlja fenil, piridinil ili pirazinil, od kojih svaka grupa može biti opciono supstituisana sa jednim ili više supstituenata koji su nezavisno izabrani od: halogena, C1-6 alkil i C1-6 alkoksi.
11. Jedinjenje prema patentnom zahtevu 10 naznačeno time što M predstavlja piridinil.
12. Jedinjenje prema patentnom zahtevu 10 naznačeno time što M predstavlja metilpiridinil.
13. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time što W predstavlja C-R5.
14. Jedinjenje prema patentnom zahtevu 13, naznačeno time što R5 predstavlja vodonik.
15. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što R3 predstavlja vodonik.
16. Jedinjenje prema patentnom zahtevu 1 predstavljeno formulom (IIA); ili njegova farmaceutski prihvatljiva so ili solvat: gde su R1 i R2 kao što je definisano u zahtevu 1; X predstavlja N ili CH; R16 i R17 nezavisno predstavljaju vodonik, halogen, cijano, C1-6 alkil, trifluorometil, amino, C1-6 alkilamino ili di(C1-6)alkilamino; i R18 i R19 nezavisno predstavljaju vodonik, halogen, cijano, C1-6 alkil, trifluorometil ili aminokarbonil.
17. Jedinjenje prema patentnom zahtevu 16 naznačeno time što R19 predstavlja vodonik.
18. Jedinjenje prema patentnom zahtevu 17 predstavljeno formulom (IIb), ili njegova farmaceutski prihvatljiva so ili solvat gde su R1 i R2 kao što je definisano u patentnom zahtevu 1; i X, R16, R17 i R18 su kao što je definisano u patentnom zahtevu 16.
19. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 18 naznačeno time što X predstavlja N.
20. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 19 naznačeno time što R16 predstavlja vodonik.
21. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 20 naznačeno time što R17 predstavlja vodonik.
22. Jedinjenje prema bilo kojem od patentnih zahteva 16 do 21 naznačeno time što R18 predstavlja vodonik ili C1-6 alkil.
23. Jedinjenje prema patentnom zahtevu 22, naznačeno time što R18 predstavlja vodonik.
24. Jedinjenje prema patentnom zahtevu 22, naznačeno time što R18 predstavlja metil.
25. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time što R1 predstavlja vodonik, halogen, C1-6 alkil, trifluorometil ili C1-6 alkilsulfonil.
26. Jedinjenje prema patentnom zahtevu 25, naznačeno time što R1 predstavlja hloro.
27. Jedinjenje prema patentnom zahtevu 25, naznačeno time što R1 predstavlja trifluorometil.
28. Jedinjenje prema bilo kojem od prethodnih patentnih zahteva naznačeno time što R2 predstavlja vodonik, halogen ili C1-6 alkil.
29. Jedinjenje prema patentnom zahtevu 28, naznačeno time što R2 predstavlja vodonik.
30. Jedinjenje prema patentnom zahtevu 1 izabrano od sledećeg: N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-[(R)-1-(8-hloro-2-fenilhinolin-3-il) -2,2,2-trifluoroetil] pirido [3,2-d] pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(4-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(4-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(5-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(5-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(pyrazin-2-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(6-metoksipirazin-2-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(6-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[8-hloro-2-(6-metil-1-oksipiridin-3-il)hinolin-3-y]]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[8-metil-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-amin; N-{(R)-1-[8-metil-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(5-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[7-fluoro-8-metil-2-(5-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[2-(piridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(1-oksipiridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(6-metilpiridin-3-il)-5,6,8-trifluorohinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin; N-{(R)-1-[2-(6-metil-1-oksipiridin-3-il)-5,6,8-trifluorohinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-metil-pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-(1-oksipirido-[3,2-d]pirimidin-4-il) amin; N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-N-(1-oksi-pirido[3,2-d]pirimidin-4-il)amin; N-{(S)-1-[8-hloro-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(S)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]-pirimidin-4-ilamin; N-{(R)-1-[2-(piridin-3-il) hinolin-3-il]-2,2,2-trifluoroetil} pirido [3,2-d] pirimidin-4-amin; N-{(R)-1-[2-(1-oksipiridin-3-il) hinolin-3-il] -2,2,2-trifluoroetil} pirido [3,2-d] -pirimidin-4-amin ; N-{(R)-1-[8-hloro-2-(6-hloropiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin; N-{(R)-1-[2-(2-metil-1-oksipiridin-3-il)-8-(trifluorometil)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; N-{(R)-1-[8-(Metansulfonil)-2-(2-metilpiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin -4-amin; N-{(R)-1-[8-(metansulfonil)-2-(2-metil-1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-amin; i N-{(R)-1-[8-(metansulfonil)-2-(piridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-amin.
31. Jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat, za upotrebu u terapiji.
32. Jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegova farmaceutski prihvatljiva so ili solvat, za upotrebu u lečenju i/ili prevenciji poremećaja za koje je indikovna administracija selektivnog PI3K inhibitora.
33. Farmaceutska kompozicija koja sadrži jedinjenje formule (I) kako je definisano u zahtevu 1 ili njegov N-oksid, ili njegovu farmaceutski prihvatljivu so ili solvat, zajedno sa farmaceutski prihvatljivim nosačem.
34. Upotreba jedinjenja formule (I) kako je definisano u zahtevu 1 ili njegovog N-oksida, ili njegove farmaceutski prihvatljive soli ili solvata, za proizvodnju medikamenta za lečenje i/ili prevenciju poremećaja za koje je indikovana administracija selektivnog PI3K inhibitora.
35. N-{(R)-1-[8-Hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-il amin prema patentnom zahtevu 1.
36. N-{(R)-1-[8-Hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}-pirido[3,2-d]pirimidin-4-ilamin prema zahtevu 1, za upotrebu u lečenju i/ili prevenciji zapaljenskih, autoimunih, kardiovaskularnih, neurodegenerativnih, metaboličkih, onkoloških, noiceptivnih ili oftalmičkih stanja.
37. Farmaceutska kompozicija prema patentnom zahtevu 33, koja sadrži N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d]pirimidin-4-ilamin zajedno sa farmaceutski prihvatljivim nosačem.
38. Upotreba N-{(R)-1-[8-hloro-2-(1-oksipiridin-3-il)hinolin-3-il]-2,2,2-trifluoroetil}pirido[3,2-d] pirimidin-4-ilamina za proizvodnju medikamenta za lečenje i/ili prevenciju inflamatornih, autoimunih, kardiovaskularnih, neurodegenerativnih, metaboličkih, onkoloških, noiceptivnih ili oftalmičkih stanja. 2
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Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2240451T3 (da) 2008-01-04 2017-11-20 Intellikine Llc Isoquinolinonderivater substitueret med en purin, der er anvendelig som pi3k-inhibitorer
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
WO2010036380A1 (en) 2008-09-26 2010-04-01 Intellikine, Inc. Heterocyclic kinase inhibitors
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
EP2571357B1 (en) 2010-05-21 2016-07-06 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
AR082799A1 (es) * 2010-09-08 2013-01-09 Ucb Pharma Sa Derivados de quinolina y quinoxalina como inhibidores de quinasa
WO2012064973A2 (en) 2010-11-10 2012-05-18 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
DK2663309T3 (en) 2011-01-10 2017-06-19 Infinity Pharmaceuticals Inc METHODS FOR PRODUCING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES
US8969363B2 (en) 2011-07-19 2015-03-03 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
KR20140063605A (ko) 2011-07-19 2014-05-27 인피니티 파마슈티칼스, 인코포레이티드 헤테로사이클릭 화합물 및 그의 용도
AR091790A1 (es) 2011-08-29 2015-03-04 Infinity Pharmaceuticals Inc Derivados de isoquinolin-1-ona y sus usos
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
UA125503C2 (uk) 2012-06-13 2022-04-13 Інсайт Холдинґс Корпорейшн Заміщені трициклічні сполуки як інгібітори fgfr
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
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
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
MY181497A (en) 2013-04-19 2020-12-23 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PL3052485T3 (pl) 2013-10-04 2022-02-28 Infinity Pharmaceuticals, Inc. Związki heterocykliczne i ich zastosowania
CN104744435B (zh) * 2013-12-25 2017-03-01 上海医药工业研究院 喹啉类化合物、其盐、其中间体、制备方法及应用
CA2943075C (en) 2014-03-19 2023-02-28 Infinity Pharmaceuticals, Inc. Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
GB201506786D0 (en) * 2015-04-21 2015-06-03 Ucb Biopharma Sprl Therapeutic use
NZ740616A (en) 2015-09-14 2023-05-26 Infinity Pharmaceuticals Inc Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
GB201604970D0 (en) 2016-03-23 2016-05-04 Syngenta Participations Ag Improvements in or relating to organic compounds
GB201608797D0 (en) * 2016-05-19 2016-07-06 Ucb Biopharma Sprl Therapeutic use
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
IL263680B2 (en) 2016-06-24 2025-10-01 Infinity Pharmaceuticals Inc PI3K inhibitors for use in combination with a second therapeutic agent for the treatment, management or prevention of cancer
CN108239076B (zh) * 2016-12-26 2021-07-06 中国医学科学院药物研究所 喹唑啉类化合物及其制备方法、用途和药物组合物
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
GB201708856D0 (en) * 2017-06-02 2017-07-19 Ucb Biopharma Sprl Seletalisib crystalline forms
BR112020022392A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation formas sólidas de um inibidor de fgfr e processos para preparação das mesmas
PE20210919A1 (es) 2018-05-04 2021-05-19 Incyte Corp Sales de un inhibidor de fgfr
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
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
GEP20247679B (en) 2019-10-14 2024-10-10 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之三環雜環
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101715453B (zh) 2007-03-23 2012-06-27 安姆根有限公司 杂环化合物及其应用
MX2009010050A (es) 2007-03-23 2009-10-12 Amgen Inc Derivados de quinolina o quinoxalina 3-sustituidos y su uso como inhibidores de fosfotidilinositol 3-cinasa (p13k).
US7919498B2 (en) * 2007-03-23 2011-04-05 Amgen Inc. Substituted pyrazolo[3,4-d]pyrimidines as PI3K inhibitors
WO2009081105A2 (en) * 2007-12-21 2009-07-02 Ucb Pharma S.A. Quinoxaline and quinoline derivatives as kinase inhibitors
GB0819593D0 (en) 2008-10-24 2008-12-03 Ucb Pharma Sa Therapeutic agents
WO2011058108A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Quinoline and quinoxaline derivatives as kinase inhibitors
AR082799A1 (es) * 2010-09-08 2013-01-09 Ucb Pharma Sa Derivados de quinolina y quinoxalina como inhibidores de quinasa

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