DK2556071T3 - Kinasehæmmere og deres anvendelse til behandling af cancer - Google Patents
Kinasehæmmere og deres anvendelse til behandling af cancer Download PDFInfo
- Publication number
- DK2556071T3 DK2556071T3 DK11764988.9T DK11764988T DK2556071T3 DK 2556071 T3 DK2556071 T3 DK 2556071T3 DK 11764988 T DK11764988 T DK 11764988T DK 2556071 T3 DK2556071 T3 DK 2556071T3
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- DK
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- Prior art keywords
- mmol
- indazol
- title compound
- cancer
- nmr
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
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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
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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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- A—HUMAN NECESSITIES
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
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- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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Claims (13)
1. Forbindelse med følgende strukturformel:
eller et farmaceutisk acceptabelt salt deraf, hvor: Ra er F, methoxy, methyl eller ethyl; R4 er H eller methyl; og R6 er -CH=CH-(eventuelt substitueret phenyl), hvor phenyl i -CH=CH-(phenyl) eventuelt er substitueret med en eller flere substituenter udvalgt uafhængigt fra gruppen, der består af halogen, Ci-6 alkyl, Ci-6 haloalkyl, (Ci-6aminoalkyl), (Ci-6alkylamino)Ci-6 alkyl, (phenyl)Ci-e alkyl, amino, C-i-6alkylamino, Ci-6dialkylamino, -(CH2)0-3-A/-piperidinyl, -(CH2)o-3 -N- morpholinyl, -(CH2)0-3-A/-pyrrolidinyl, -(CH2)0-3-/V-piperazinyl og -(CH2)0-3-A/-oxazepanyl, hvor /V-piperazinyl eventuelt er Ν'-substitueret med C1-6 alkyl eller C-i-6 acyl.
2. Forbindelse ifølge krav 1, hvor forbindelsen har følgende strukturformel:
eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge krav 1, hvor forbindelsen har følgende strukturformel:
eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelsen med følgende strukturformel:
eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse med følgende strukturformel:
eller et farmaceutisk acceptabelt salt deraf.
6. Forbindelse ifølge et hvilket som helst af kravene 1-5 eller et farmaceutisk acceptabelt salt deraf til anvendelse som et medikament.
7. Forbindelse ifølge et hvilket som helst af kravene 1-5 eller et farmaceutisk acceptabelt salt deraf til anvendelse til behandling af cancer.
8. Forbindelse eller salt deraf til anvendelse ifølge krav 7, hvor canceren er udvalgt fra gruppen, der består af lungecancer, brystcancer, coloncancer, hjernecancer, neuroblastom, prostatacancer, melanom, glioblastoma multiforme, ovariecancer, lymfom, leukæmi, melanom, sarkom, paraneoplasi, osteosarkom, germinom, gliom og mesoteliom.
9. Forbindelse eller salt deraf til anvendelse ifølge krav 8, hvor canceren er udvalgt fra gruppen, der består af lungecancer, brystcancer eller coloncancer.
10. Forbindelse eller salt deraf til anvendelse ifølge krav 9, hvor canceren er basal undertype brystcancer eller en luminal B-undertype brystcancer.
11. Forbindelse eller salt deraf til anvendelse ifølge krav 10, hvor canceren er en basal undertype brystcancer, der overudtrykker PLK4.
12. Forbindelse eller salt deraf til anvendelse ifølge krav 9, hvor canceren er basal undertype brystcancer, som er ER-, FIER2- og PR-negativ brystcancer.
13. Forbindelse eller salt deraf til anvendelse ifølge krav 7, hvor canceren er en bløddelscancer, hvor bløddelscanceren er et sarkom, der fortrinsvis er udvalgt fra gruppen, der består af et fibrosarkom, et gastrointestinalt sarkom, et leiomyosarkom, et dedifferentieret liposarkom, et pleomorfisk liposarkom, et malignt fibrøst histiocytom, et rundcellesarkom og et synovialt sarkom.
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| PCT/CA2010/000518 WO2010115279A1 (en) | 2009-04-06 | 2010-04-06 | Kinase inhibitors and method of treating cancer with same |
| PCT/CA2011/000386 WO2011123946A1 (en) | 2010-04-06 | 2011-04-06 | Kinase inhibitors and method of treating cancer with same |
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