DK3205654T3 - Makrocykliske forbindelser som trk-kinaseinhibitorer - Google Patents
Makrocykliske forbindelser som trk-kinaseinhibitorer Download PDFInfo
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- DK3205654T3 DK3205654T3 DK17163978.4T DK17163978T DK3205654T3 DK 3205654 T3 DK3205654 T3 DK 3205654T3 DK 17163978 T DK17163978 T DK 17163978T DK 3205654 T3 DK3205654 T3 DK 3205654T3
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- hexaazapentacyclo
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- C07D471/22—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 systems contains four or more hetero rings
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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Claims (17)
1. Forbindelse valgt fra gruppen, der består af: (6R)- 9-fluor-15-hydroxy-13-oxa-2,11,17,21,22,25-hexaazapentacyclo [17.5.2.02'6.07'12>o22'26]hexacosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R,15R)- 9-fluor-15-hydroxy-13-oxa-2,11, 17,21,22,25-hexaazapentacyclo- [17.5.2.02'6.07'12>o22'26]hexacosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-13-oxa-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.07'12>o21'25]pentacosa-1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-13-oxa-2,11,18,22,23,26-hexaazapentacyclo [18.5.2.O2'6.o7'12.O23'2?] heptacosa-1(26),7,9,11,20(27) , 21,2 4-heptaen-19-on ; (6R)-9-fluor-2,11,13,16,20,21,24- heptaazapentacyclo [16.5.2.02'6.07'12.021'2s]pentacosa-1(24),7,9,11,18(25),19,22-heptaen-17-on; (6R)-9-fluor-2,11,13,17,21,22,25- heptaazapentacyclo [17.5.2.02'6.07'12022'26]hexacosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-17-methyl-13-oxa-2,11,17,21,22,25-hexaazapentacyclo [17.5.2.02'6.07'12>o22'26]hexacosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9,15,15-trifluor-13-oxa-2,11,17,21,22,25-hexaazapentacyclo [17.5.2.02'6.07'12>o22'26]hexacosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'1.01'12>o21'25]pentacosa-1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-15-methyl-2,11,16,20,21,24-hexaazapentacyclo [16.5.2.02'6.07'12>o21'25]pentacosa-1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-15,15-dimethyl-13-oxa-2,11,17,21,22,25-hexaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa-1(25),7,9,11,19(26),20,23-heptaen-18-on; og (6R)-9-fluor-15,15-dimethyl-2,11,16,20,21,24-hexaazapentacyclo [16.5.2.02'6.07'12.021'2s]pentacosa- 1(24),7,9,11,18(25),19,22-heptaen-17-on; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9-fluor-15-hydroxy-13-oxa-2,11,17,21,22,25-hexaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25) , 7, 9, 11, 19(26), 20,23-heptaen-18-on eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge krav 1, hvor forbindelsen er (6R,15R)-9-fluor-15-hydroxy-13-oxa-2,11,17,21,22,25-hexaazapentacyclo-[17.5.2. O2'6. O7'12. O22'26] hexacosa-1 (25),7,9,11,19(26),20,23-heptaen-18-on eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9-fluor-13-oxa-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24) , 7, 9, 11, 18(25), 19, 22-heptaen-17-on eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9- fluor-13-oxa-2,11,18,22,23,26- hexaazapentacyclo [18.5.2.O2'6.O7'12.o23'27] heptacosa- 1(26) , 7, 9, 11,20(27), 21,24-heptaen-19-on eller et farmaceutisk acceptabelt salt deraf.
6. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9-fluor-2,11,13,16,20,21,24- heptaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24) , 7, 9, 11, 18(25), 19, 22-heptaen-17-on eller et farmaceutisk acceptabelt salt deraf.
7. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9- fluor-2,11,13, 17,21,22,25- heptaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25) , 7, 9, 11, 19(26), 20,23-heptaen-18-on eller et farmaceutisk acceptabelt salt deraf.
8. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9-fluor-17-methyl-13-oxa-2,11,17,21,22,25-hexaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on eller et farmaceutisk acceptabelt salt deraf.
9. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9,15,15-trifluor-13-oxa-2,11,17,21,22,25-hexaazapentacyclo [17.5.2.02'6.o1'12>o22'26]hexacosa- 1(25) , 7, 9, 11, 19(26), 20,23-heptaen-18-on eller et farmaceutisk acceptabelt salt deraf.
10. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9-fluor-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24) , 7, 9, 11, 18(25), 19, 22-heptaen-17-on eller et farmaceutisk acceptabelt salt deraf.
11. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9-fluor-15-methyl-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24) , 7, 9, 11, 18(25), 19, 22-heptaen-17-on eller et farmaceutisk acceptabelt salt deraf.
12. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9-fluor-15,15-dimethyl-13-oxa-2,11,17,21,22,25-hexaazapentacyclo [17.5.2.02'6.o7'12>o22'26]hexacosa- 1(25) , 7, 9, 11, 19(26), 20,23-heptaen-18-on eller et farmaceutisk acceptabelt salt deraf.
13. Forbindelse ifølge krav 1, hvor forbindelsen er (6R)-9-fluor-15,15-dimethyl- 2,11, 16,20,21,2 4hexaazapentacyclo [16.5.2.02'6.07'12>o21'25]pentaco sa-1(24) , 7, 9, 11, 18(25), 19, 22-heptaen-17-on eller et farmaceutisk acceptabelt salt deraf.
14. Farmaceutisk sammensætning, der omfatter en forbindelse valgt fra gruppen, der består af: (6R)- 9-fluor-15-hydroxy-13-oxa-2,11,17,21,22,25- hexaazapentacyclo [17.5.2.02'6.07'12.022'26 hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R,15R)- 9-fluor-15-hydroxy-13-oxa-2,11, 17,21,22,25- hexaazapentacyclo- [17.5.2.02'6.o7'12>o22'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-13-oxa-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.o7'12>o21'25]pentacosa- 1(24),7,9,11,18(25),19,22-heptaen-17-on;] (6R)-9-fluor-13-oxa-2,11,18,22,23,26- hexaazapentacyclo [18.5.2.O2'6.o7'12.o23'27] heptacosa- 1(26),7,9,11,20(27) , 21,2 4-heptaen-19-on ; (6R)-9-fluor-2,11,13,16,20,21,24- heptaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-2,11,13,17,21,22,25- heptaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-17-methyl-13-oxa-2,11,17,21,22,25- hexaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9,15,15-trifluor-13-oxa-2,11,17,21,22,25- hexaazapentacyclo [17.5.2.02'6.o7'12>o22'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.o7'1i.o21'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-15-methyl-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.o7'12>o21'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-15,15-dimethyl-13-oxa-2,11,17,21,22,25- hexaazapentacyclo [17.5.2.02'6.o1'12>o22'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; og (6R)-9-fluor-15,15-dimethyl-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt fortyndingsmiddel eller bæremateriale .
15. Sammensætning ifølge krav 14, hvor forbindelsen er i form af et farmaceutisk acceptabelt salt.
16. Forbindelse valgt fra gruppen, der består af: (6R)- 9-fluor-15-hydroxy-13-oxa-2,11, 17,21,22,25- hexaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R,15R)- 9-fluor-15-hydroxy-13-oxa-2,11, 17,21,22,25- hexaazapentacyclo- [17.5.2.02'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-13-oxa-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-13-oxa-2,11,18,22,23,26- hexaazapentacyclo [18.5.2.O2'6.O7'12.o23'27] heptacosa- 1(26),7,9,11,20(27) , 21,2 4-heptaen-19-on ; (6R)-9-fluor-2,11,13,16,20,21,24- heptaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-2,11,13,17,21,22,25- heptaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-17-methyl-13-oxa-2,11,17,21,22,25- hexaazapentacyclo [17.5.2.01'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9,15,15-trifluor-13-oxa-2,11,17,21,22,25- hexaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; (6R)-9-fluor-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'1.o1'12.o21'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-15-methyl-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.07'12.021'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; (6R)-9-fluor-15,15-dimethyl-13-oxa-2,11,17,21,22,25- hexaazapentacyclo [17.5.2.02'6.07'12.022'26]hexacosa- 1(25),7,9,11,19(26),20,23-heptaen-18-on; og (6R)-9-fluor-15,15-dimethyl-2,11,16,20,21,24- hexaazapentacyclo [16.5.2.02'6.o7'2.o21'25]pentacosa- 1(24),7,9,11,18(25),19, 22-heptaen-17-on; eller et farmaceutisk acceptabelt salt deraf til anvendelse til behandling af cancer, hvor canceren er kendetegnet ved en eller flere af overekspression, aktivering, amplifikation og mutation af en Trk-kinase.
17. Forbindelse til anvendelse ifølge krav 16, hvor canceren er valgt fra gruppen, der består af: neuroblastom, ovarie-, pankreas-, kolorektal, prostata-, melanom, hoved- og halscancer, mavekarcinom, lungekarcinom, brystcancer, glioblastom, medulloblastom, sekretorisk brystcancer, spytkirtelcancer og papillært thyreoideakarcinom.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US34676710P | 2010-05-20 | 2010-05-20 | |
US201061426716P | 2010-12-23 | 2010-12-23 | |
EP15150036.0A EP2918588B1 (en) | 2010-05-20 | 2011-05-13 | Macrocyclic compounds as TRK kinase inhibitors |
Publications (1)
Publication Number | Publication Date |
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DK3205654T3 true DK3205654T3 (da) | 2019-04-15 |
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Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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DK15150036.0T DK2918588T3 (da) | 2010-05-20 | 2011-05-13 | Makrocykliske forbindelser som TRK-kinasehæmmere |
DK17163978.4T DK3205654T3 (da) | 2010-05-20 | 2011-05-13 | Makrocykliske forbindelser som trk-kinaseinhibitorer |
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DK15150036.0T DK2918588T3 (da) | 2010-05-20 | 2011-05-13 | Makrocykliske forbindelser som TRK-kinasehæmmere |
Country Status (34)
Country | Link |
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US (8) | US8933084B2 (da) |
EP (4) | EP2918588B1 (da) |
JP (5) | JP5832527B2 (da) |
KR (4) | KR101852169B1 (da) |
CN (3) | CN110003209B (da) |
AR (1) | AR081919A1 (da) |
AU (4) | AU2011256380C1 (da) |
BR (2) | BR122019024201B1 (da) |
CA (1) | CA2800079C (da) |
CL (1) | CL2012003227A1 (da) |
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