ME02453B - Inhibitori protein kinaze - Google Patents

Inhibitori protein kinaze

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Publication number
ME02453B
ME02453B MEP-2016-144A MEP2016144A ME02453B ME 02453 B ME02453 B ME 02453B ME P2016144 A MEP2016144 A ME P2016144A ME 02453 B ME02453 B ME 02453B
Authority
ME
Montenegro
Prior art keywords
alkyl
cycloalkyl
compound according
phenyl
heterocyclic ring
Prior art date
Application number
MEP-2016-144A
Other languages
German (de)
English (en)
French (fr)
Inventor
Tero Linnanen
Gerd Wohlfahrt
Srinivas Nanduri
Ravi Ujjinamatada
Srinivasan Rajagopalan
Subhendu Mukherjee
Original Assignee
Orion Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54261175&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02453(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Orion Corp filed Critical Orion Corp
Publication of ME02453B publication Critical patent/ME02453B/me

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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
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    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Claims (17)

1. Jedinjenje formule (I)pri čemuZ je CH ili N;G je grupa formulepri čemu je A fenilni prsten ili 5 -12 člani heterociklični prsten, iR1 je H, C1-7 alkil, C3-7 cikloalkil, C3-7 cikloalkil C1-7 alkil, C1-7 alkoksi, C1-7 alkil karbonil, amino, hidroksi, hidroksi C1-7 alkil, C1-7 alkilamino C1-7 alkil, fenil C1-7 alkoksi, -NHC(O)-R21, -R12-C(O)-R13, -SO2-R14 ili -E-R6, iR2 je H, halogen, C1-7 alkil ili okso;B je 5-12 člani karbociklični ili heterociklični prsten;R3 je H, halogen, C1-7 alkil, C1-7 alkoksi, cijano ili opciono supstituisani 5-6 člani heterociklični prsten;R4 je H, halogen, C1-7 alkil ili okso;M je hidroksil, C1-7 alkil ili –NHR5;R5 je H, -C(O)R7, -SO2R8, -C(O)-D-R9 ili opciono supstituisani 5-6 člani heterociklični prsten;R6 je opciono supstituisani 5-6 člani heterociklični prsten;R7 je C1-7 alkil, C2-7 alkenil, C3-7 cikloalkil, C1-7alkoksi, C1-7 alkoksi C1-7 alkil, karboksi C1-7 alkil, C1-7 alkoksi karbonil C1-7 alkil, C1-7 alkilamino C1-7 alkil, -NH-R10 ili-NH-X1-R11;R8 je C1-7 alkil, C2-7 alkenil, C3-7 cikloalkil, hidroksi C1-7 alkil, -NR18R19, -NH-X2-R20, fenil ili opciono supstituisani 5-6 člani heterociklični prsten;R9 je fenil ili opciono supstituisani 5-6 člani heterociklični prsten;R10 je C1-7 alkil ili C3-7 cikloalkil;R11 je fenil ili opciono supstituisani 5-6 člani heterociklični prsten;R12 i R21 su C1-7 alkil;R13 je C1-7 alkoksi, amino ili hidroksi;R14 je C1-7 alkil ili C3-7 cikloalkil;R18 i R19 su, nezavisno, H, C1-7 alkil ili C3-7 cikloalkil;R20 je fenil ili opciono supstituisani 5-6 člani heterociklični prsten;E je veza ili C1-7 alkil;D je veza ili C1-7 alkil;X1 i X2 su, nezavisno, veza ili C1-7 alkil;i njegove farmaceutski prihvatljive soli.
2. Jedinjenje prema zahtevu 1, pri čemu je M -NHR5.
3. Jedinjenje prema bilo kom od zahteva 1-2, pri čemu je prsten A bilo koja od sledećih grupa ili njihovih tautomera
4. Jedinjenje prema bilo kom od zahteva 1 -3, pri čemu je prsten B bilo koja od sledećih grupa ili njihovih tautomera
5. Jedinjenje prema bilo kom od zahteva 1 do 4, pri čemu je Z CH.
6. Jedinjenje prema bilo kom od zahteva 1 do 4, pri čemu je Z N.
7. Jedinjenje prema bilo kom od zahteva 1 do 6, pri čemu G je grupa formule pri čemu je A prsten sa formulom (1’), (2’), (3’), (4’), (5’), (7’), (10’), (12’), (14’), (16’) ili (20’) kao što je definisan u zahtevu 3; R1 je H, C1-7 alkil, C1-7 alkoksi, hidroksi C1-7 alkil, C1-7 alkilamino C1-7 alkil ili -E-R6; R2 je H; B je prsten formule (1"), (2"), (3 "), (4") ili (6"), kao što je definisan u zahtevu 4; E je veza ili C1-7 alkil; R6 je bilo koja od sledećih grupa R3 je H, halogen, C1-7 alkil, C1-7 alkoksi ili cijano; R4 je H ili halogen; M je -NHR5; R5 je -C(O)R7, -SO2R8 ili -C(O)-D-R9 ili bilo koja od sledećih grupa R7 je C1-7 alkil, C2-7 alkenil, -NH-R10 ili -NH-X1-R11; R8 je C1-7 alkil, C2-7 alkenil, C3-7 cikloalkil, hidroksi C1-7 alkil, -NR18R19, -NH-X2-R20, fenil ili grupa R9 je fenil ili bilo koja od sledećih grupa R10 je C1-7 alkil ili C3-7 cikloalkil; R11 je fenil, 4-fluorofenil, ili bilo koja od sledećih grupa R18 i R19 su, nezavisno, H, C1-7 alkil ili C3-7 cikloalkil; R20 je grupa X1 i X2 su, nezavisno, veza ili C1-7 alkil, i D je veza ili C1-7 alkil.
8. Jedinjenje prema bilo kom od zahteva 1 do 7, pri čemu je B prsten formule (1") ili (6"), kao što je definisan u zahtevu 4.
9. Jedinjenje prema bilo kom od zahteva 1 do 8, pri čemu je A prsten formule (1’), (2’), (4’), (7’), (10’), (14’), (16’) ili (20’), kao što je definisan u zahtevu 3.
10. Jedinjenje prema bilo kom od zahteva 1 do 9, pri čemu B je fenil, R3 je halogen, a R4 je H ili halogen.
11. Jedinjenje prema bilo kom od zahteva 1 do 10, pri čemu M je -NHC(O)R7, pri čemu R7 je C1-7 alkil, C2-7 alkenil, C3-7 cikloalkil, -NH-R10 ili -NH-X1-R11, pri čemu je R10 C1-7 alkil ili C3-7 cikloalkil, X1 je veza ili C1-7 alkil, i R11 je 5-6 člani heterociklični prsten, koji je opciono supstituisan sa jednom ili dve C1-7 alkil grupe.
12. Jedinjenje prema bilo kom od zahteva 1 do 10, pri čemu M je -NHSO2R8 pri čemu je R8 C1-7 alkil, C2-7 alkenil, C3-7 cikloalkil, fenil ili NR18R19 pri čemu su R18 i R19, nezavisno, H, C1-7 alkil ili C3-7 cikloalkil.
13. Jedinjenje prema bilo kom od zahteva 1 do 10, pri čemu M je -NHC(O)-D-R9 pri čemu je D veza ili C1-7 alkil, a R9 je 5-6 člani heterociklični prsten koji je opciono supstituisan sa jednom ili dve C1-7 alkil grupe.
14. Jedinjenje prema bilo kom od zahteva 1 do 10, pri čemu R5 je 5-6 člani heterociklični prsten, opciono supstituisan sa jednom ili dve C1-7 alkil grupe.
15. Farmaceutska smeša koja sadrži jedinjenje formule (I), kao što je definisano u bilo kom od zahteva 1 do 13 ili njegovu farmaceutski prihvatljivu so zajedno sa farmaceutski prihvatljivim nosačem.
16. Jedinjenje formule (I) kao što je definisano u bilo kom od zahteva 1 do 13 ili njegova farmaceutski prihvatljiva so za korišćenje u lečenju stanja za koje je poželjna inhibicija FGFR kinaze.
17. Jedinjenje formule (I) kao što je definisano u bilo kom od zahteva 1 do 13 ili njegova farmaceutski prihvatljiva so za korišćenje u lečenju raka.
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